# US 12,110,295 B2 · WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds and methods of use > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,110,295 B2 - Document ID: US12110295B2 - Status: Granted - Kind: B2 - Application number: 17/254,345 - Filed: 2019-06-21 - Published: 2022-11-03 - Granted: 2024-10-08 - Earliest claimed: 2018-06-21 - Assignees: Icahn School of Medicine at Mount Sinai; The University of North Carolina at Chapel Hill - Applicants: Icahn School of Medicine at Mount Sinai; The University of North Carolina at Chapel Hill - Inventors: Jian Jin; Gang Wang; Jing Liu; Xufen Yu; Dongxu Li - Web page: https://patentgrep.com/patent/US12110295B2 ## CPC - A61P 35/00: Antineoplastic agents - C07D 487/04: Ortho-condensed systems - C07D 401/14: containing three or more hetero rings - C07D 417/14: containing three or more hetero rings - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) ## Abstract Disclosed herein are WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds including a WDR5 ligand, a degradation/disruption tag, and a linker, and methods of using such compounds in the treatment of WDR5-mediated diseases. ## Claims ### Claim 1 A bivalent compound comprising a WD40 repeat domain protein 5 (WDR5) ligand conjugated to a degradation/disruption tag through a linker, said linker selected from the group consisting of: wherein A, W and B, at each occurrence, are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)N(R1)R″, R′C(S)N(R1)R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCON(R1)R″, R′SR″, R′SOR″, R′SO2R″, R′SO2N(R1)R″, R′N(R1)R″, R′NR″COR″, R′NR1C(O)OR″, R′NR″CON(R2)R″, R′NR″C(S)R″, R′NR1S(O)R″, R′NR1S(O)2R″, and R′NR1S(O)2N(R2)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C5 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C5 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R1 and R2 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R1 and R2, R′ and R1, R1 and R2, R″ and R1, R″ and R2 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; and m is 0 to 15; wherein R1, R2, R3 and R4, at each occurrence, are independently selected from hydrogen, halogen, hydroxyl, amino, cyano, nitro, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxy, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8 alkylamino, and optionally substituted C1-C8 alkylaminoC1-C8 alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 3-8 membered cycloalkoxy, optionally substituted 3-10 membered carbocyclylamino, optionally substituted 4-8 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, or R1 and R2, R3 and R4 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; A, W and B, at each occurrence, are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)N(R5)R″, R′C(S)N(R5)R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCONR5R″, R′SR″, R′SOR″, R′SO2R″, R′SO2N(R5)R″, R′N(R5)R″, R′NR5COR″, R′NR5C(O)OR″, R′NR5CON(R6)R″, R′NR5C(S)R″, R′NR5S(O)R″, R′NR5S(O)2R″, and R′NR5S(O)2N(R6)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C8 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R5 and R6 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R5 and R6, R′ and R5, R′ and R6, R″ and R5, R″ and R6 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; m is 0 to 15; n, at each occurrence, is 0 to 15; and o is 0 to 15; wherein R1 and R2, at each occurrence, are independently selected from hydrogen, halogen, hydroxyl, amino, cyano, nitro, and optionally substituted C1-C8 alkyl, optionally substituted C1-C8 alkoxy, optionally substituted C1-C8 alkoxy C1-C8 alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8 alkylamino, C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 3-8 membered cycloalkoxy, optionally substituted 3-10 membered carbocyclylamino, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, or R1 and R2 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; A and B, at each occurrence, are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)NR3R″, R′C(S)NR3R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCON(R3)R″, R′SR″, R′SOR″, R′SO2R″, R′SO2N(R3)R″, R′N(R3)R″, R′NR3COR″, R′NR3C(O)OR″, R′NR3CON(R4)R′, R′NR3C(S)R″, R′NR3S(O)R″, R′NR3S(O)2R″, and R′NR3S(O)2N(R4)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C8 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R3 and R4, R′ and R3, R′ and R4, R″ and R3, R″ and R4 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; m, at each occurrence, is 0 to 15; and n is 0 to 15; wherein X is selected from O, NH, and NR7; R1, R2, R3, R4, R5, and R6, at each occurrence, are independently selected from hydrogen, halogen, hydroxyl, amino, cyano, nitro, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxy, optionally substituted C1-C8 alkoxy C1-C8 alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8 alkylamino, optionally substituted C1-C8 alkylaminoC1-C8 alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 3-8 membered cycloalkoxy, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; A and B are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)N(R8)R″, R′C(S)N(R8)R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCON(R8)R″, R′SR″, R′SOR″, R′SO2R″, R′SO2N(R8)R″, R′N(R8)R″, R′NRBCOR″, R′NRBC(O)OR″, R′NRBCON(R9)R″, R′NRBC(S)R″, R′NRBS(O)R″, R′NRBS(O)2R″, and R′NRBS(O)2N(R9)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C8 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R7, R8 and R9 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R8 and R9, R′ and R8, R′ and R9, R″ and R8, R″ and R9 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; m, at each occurrence, is 0 to 15; n, at each occurrence, is 0 to 15; o is 0 to 15; and p is 0 to 15; (e) the linker comprises a ring selected from the group consisting of a 3 to 13 membered ring, a 3 to 13 membered fused ring, a 3 to 13 membered bridged ring, and a 3 to 13 membered spiro ring; wherein X is C═O or CH2, Y is C═O or CH2, and n is 0-15; wherein X is C═O or CH2, Y is C═O or CH2, m is 0-15, n is 0-6, and o is 0-15; or wherein X is C═O or CH2, Y is C═O or CH2, R is —CH2—, —CF2—, —CH(C1-3 alkyl)-, —C(C1-3 alkyl)(C1-3 alkyl)-, —CH═CH—, —C(C1-3 alkyl)═C(C1-3 alkyl)-, —C═C—, —O—, —NH—, —N(C1-3 alkyl)-, —C(O)NH—, —C(O)N(C1-3 alkyl)-, a 3-13 membered ring, a 3-13 membered fused ring, a 3-13 membered bridged ring, and/or a 3-13 membered spiro ring, m is 0-15, and n is 0-15; and wherein the WDR5 ligand is selected from wherein R24, R25, R26, R27, and R28 are independently selected from H and CH3; B1 and B2 are independently selected from H and F; and Y1 and Y2 are independently selected from CH and N; and wherein the degradation/disruption tag is selected from wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, C1-C8 alkoxyalkyl, C1-C8 haloalkyl, C1-C8 hydroxyalkyl, C1-C8 aminoalkyl, C1-C8 alkylaminoalkyl, C3-C7 cycloalkyl, C3-C7 heterocyclyl, C2-C8 alkenyl, or C2-C8 alkynyl; R3 is H, C(O)C1-C8 alkyl, C(O)C1-C8 alkoxyalkyl, C(O)C1-C8 haloalkyl, C(O)C1-C8 hydroxyalkyl, C(O)C1-C8 aminoalkyl, C(O)C1-C8 alkylaminoalkyl, C(O)C3-C7 cycloalkyl, C(O)C3-C7 heterocyclyl, C(O)C2-C5 alkenyl, C(O)C2-C5 alkynyl, C(O)OC1-C8 alkoxyalkyl, C(O)OC1-C8 haloalkyl, C(O)OC1-C8 hydroxyalkyl, C(O)OC1-C8 aminoalkyl, C(O)OC1-C8 alkylaminoalkyl, C(O)OC3-C7 cycloalkyl, C(O)OC3-C7 heterocyclyl, C(O)OC2-C8 alkenyl, C(O)OC2-C8 alkynyl, C(O)NC1-C8 alkoxyalkyl, C(O)NC1-C8 haloalkyl, C(O)NC1-C8 hydroxyalkyl, C(O)NC1-C8 aminoalkyl, C(O)NC1-C8 alkylaminoalkyl, C(O)NC3-C7 cycloalkyl, C(O)NC3-C7 heterocyclyl, C(O)NC2-C8 alkenyl, C(O)NC2-C8 alkynyl, P(O)(OH)2, P(O)(OC1-C8 alkyl)2, or P(O)(OC1-C8 aryl)2. ### Claim 2 (depends on 1) The bivalent compound of claim 1, wherein the linker comprises: wherein A, W and B, at each occurrence, are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)N(R1)R″, R′C(S)N(R1)R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCON(R1)R″, R′SR″, R′SOR″, R′SO2R″, R′SO2N(R1)R″, R′N(R1)R″, R′NR″COR″, R′NR1C(O)OR″, R′NR″CON(R2)R″, R′NR″C(S)R″, R′NR1S(O)R″, R′NR1S(O)2R″, and R′NR1S(O)2N(R2)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C8 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R1 and R2 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R1 and R2, R′ and R1, R′ and R2, R″ and R1, R″ and R2 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; and m is 0 to 15. ### Claim 3 (depends on 1) The bivalent compound of claim 1, wherein the linker comprises: wherein R1, R2, R3 and R4, at each occurrence, are independently selected from hydrogen, halogen, hydroxyl, amino, cyano, nitro, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxy, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8 alkylamino, and optionally substituted C1-C8 alkylaminoC1-C8 alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 3-8 membered cycloalkoxy, optionally substituted 3-10 membered carbocyclylamino, optionally substituted 4-8 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, or R1 and R2, R3 and R4 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; A, W and B, at each occurrence, are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)N(R5)R″, R′C(S)N(R5)R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCONR5R″, R′SR″, R′SOR″, R′SO2R′, R′SO2N(R5)R″, R′N(R5)R″, R′NR5COR″, R′NR5C(O)OR″, R′NR5CON(R6)R″, R′NR5C(S)R″, R′NR5S(O)R″, R′NR5S(O)2R″, and R′NR5S(O)2N(R6)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C8 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R5 and R6 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R5 and R6, R′ and R5, R′ and R6, R″ and R5, R″ and R6 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; m is 0 to 15; n, at each occurrence, is 0 to 15; and o is 0 to 15. ### Claim 4 (depends on 1) The bivalent compound of claim 1, wherein the linker comprises: wherein R1 and R2, at each occurrence, are independently selected from hydrogen, halogen, hydroxyl, amino, cyano, nitro, and optionally substituted C1-C8 alkyl, optionally substituted C1-C8 alkoxy, optionally substituted C1-C8 alkoxy C1-C8 alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8 alkylamino, C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 3-8 membered cycloalkoxy, optionally substituted 3-10 membered carbocyclylamino, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, or R1 and R2 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; A and B, at each occurrence, are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)NR3R″, R′C(S)NR3R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCON(R3)R″, R′SR″, R′SOR″, R′SO2R″, R′SO2N(R3)R″, R′N(R3)R″, R′NR3COR″, R′NR3C(O)OR″, R′NR3CON(R4)R′, R′NR3C(S)R″, R′NR3S(O)R″, R′NR3S(O)2R″, and R′NR3S(O)2N(R4)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C8 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R3 and R4, R′ and R3, R′ and R4, R″ and R3, R″ and R4 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; m, at each occurrence, is 0 to 15; and n is 0 to 15. ### Claim 5 (depends on 1) The bivalent compound of claim 1, wherein the linker comprises: wherein R1 and R2, at each occurrence, are independently selected from hydrogen, halogen, hydroxyl, amino, cyano, nitro, and optionally substituted C1-C8 alkyl, optionally substituted C1-C8 alkoxy, optionally substituted C1-C8 alkoxy C1-C8 alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8 alkylamino, C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 3-8 membered cycloalkoxy, optionally substituted 3-10 membered carbocyclylamino, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, or R1 and R2 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; A and B, at each occurrence, are independently selected from null, or bivalent moiety selected from R′-R″, R′COR″, R′CO2R″, R′C(O)NR3R″, R′C(S)NR3R″, R′OR″, R′OC(O)R″, R′OC(O)OR″, R′OCON(R3)R″, R′SR″, R′SOR″, R′SO2R″, R′SO2N(R3)R″, R′N(R3)R″, R′NR3COR″, R′NR3C(O)OR″, R′NR3CON(R4)R′, R′NR3C(S)R″, R′NR3S(O)R″, R′NR3S(O)2R″, and R′NR3S(O)2N(R4)R″, wherein R′ and R″ are independently selected from null, optionally substituted Rr—(C1-C8 alkyl), or a moiety comprising of optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkoxyC1-C8alkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 alkylene, optionally substituted C2-C8 alkenylene, optionally substituted C2-C8 alkynylene, optionally substituted C1-C8 hydroxyalkylene, optionally substituted C1-C8alkoxyC1-C8alkylene, optionally substituted C1-C8alkylaminoC1-C8alkylene, optionally substituted C1-C8 haloalkylene, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; Rr is selected from optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted C3-C13 fused cycloalkyl, optionally substituted C3-C13 fused heterocyclyl, optionally substituted C3-C13 bridged cycloalkyl, optionally substituted C3-C13 bridged heterocyclyl, optionally substituted C3-C13 spiro cycloalkyl, optionally substituted C3-C13 spiro heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C2-C8 alkenyl, optionally substituted C2-C8 alkynyl, optionally substituted C1-C8 alkoxyalkyl, optionally substituted C1-C8 haloalkyl, optionally substituted C1-C8 hydroxyalkyl, optionally substituted C1-C8alkylaminoC1-C8alkyl, optionally substituted 3-10 membered carbocyclyl, optionally substituted 4-10 membered heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl; R′ and R″, R3 and R4, R′ and R3, R′ and R4, R″ and R3, R″ and R4 together with the atom to which they are connected form a 3-20 membered cycloalkyl or 4-20 membered heterocyclyl ring; m, at each occurrence, is 0 to 15; and n is 0 to 15. ### Claim 6 (depends on 1) The bivalent compound of claim 1, wherein the linker comprises: wherein R5 and R6 are at each occurrence, hydrogen; A is R′C(O)NR″R1 or R′NR1C(O)R″, wherein R′ is optionally substituted C1-C8 alkylene and R″ is null; B is R′C(O)R″, wherein both R′ and R″ are null, or B is null; R1 is hydrogen; and o is 6 to 10; and p is 0. ### Claim 7 (depends on 1) The bivalent compound of claim 1, wherein the linker comprises: wherein R5 and R6 are at each occurrence, hydrogen; A is R′C(O)R″, wherein R′ is optionally substituted 4-10 membered heterocyclyl and R″ is optionally substituted C1-C8 alkylene; B is R′C(O)R″, wherein R′ and R″ are each null; o is 4 to 12; and p is 0. ### Claim 8 A method of treating a WD40 repeat domain protein 5 (WDR5)-mediated disease, comprising administering to a subject with a WDR5-mediated disease, a bivalent compound comprising a WDR5 ligand conjugated to a degradation/disruption tag through a linker, wherein said disease is selected from the group consisting of leukemia, lymphoma, ovarian cancer, stomach cancer, cervical cancer, uterine cancer, gastric cancer, head neck squamous cell carcinoma (HNSCC), colorectal cancer (CRC), lung cancer, pancreatic cancer, bladder cancer, breast cancer, and neuroblastoma. ### Claim 9 A method for identifying a bivalent compound which mediates degradation/disruption of WDR5, the method comprising: providing a heterobifunctional test compound comprising a WDR5 ligand conjugated to a degradation/disruption tag through a linker; contacting the heterobifunctional test compound with a cell comprising a ubiquitin ligase and WDR5; determining whether WDR5 levels decrease in the cell; and identifying the heterobifunctional test compound as a bivalent compound which mediates degradation/reduction of WDR5 levels decrease in the cell. ### Claim 10 A bivalent compound selected from the group consisting of: 369 N-(3′-((4-((S)-3-((2S,4R)-4-hydroxy-1- ((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanoyl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 373 N-(3′-((4-(5-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)pentanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 374 N-(3′-((4-(6-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 375 N-(3′-((4-(7-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)heptanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 376 N-(3′-((4-(8-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 377 N-(3′-((4-(9-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)nonanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 378 N-(3′-((4-(10-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)decanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 379 N-(3′-((4-(11-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)undecanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 380 N-(3′-((4-((S)-3-((2S,4R)-1-((S)-2-(1- fluorocyclopropane-1-carboxamido)- 3,3-dimethylbutanoyl)-4- hydroxypyrrolidine-2-carboxamido)- 3-(4-(4-methylthiazol-5- yl)phenyl)propanoyl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 387 N-(3′-((4-(8-((S)-3-((2S,4R)-1-((S)-2-(1- fluorocyclopropane-1-carboxamido)- 3,3-dimethylbutanoyl)-4- hydroxypyrrolidine-2-carboxamido)- 3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 388 N-(3′-((4-(9-((S)-3-((2S,4R)-1-((S)-2-(1- fluorocyclopropane-1-carboxamido)- 3,3-dimethylbutanoyl)-4- hydroxypyrrolidine-2-carboxamido)- 3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)nonanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 389 N-(3′-((4-(10-((S)-3-((2S,4R)-1-((S)-2- (1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)decanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 391 N-(3′-((4-(1′-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanoyl)-[1,4′- bipiperidine]-4-carbonyl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 392 1′-((S)-3-((2S,4R)-4-hydroxy-1-((R)-3- methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanoyl)-N-(2-(4-((4′-(4- methylpiperazin-1-yl)-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)-[1,4′-bipiperidine]-4- carboxamide 396 N-(2′-fluoro-5′-((3-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)propyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 397 N-(2′-fluoro-5′-((4-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)butyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 398 N-(2′-fluoro-5′-((5-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)pentyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 399 N-(2′-fluoro-5′-((6-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 400 N-(2′-fluoro-5′-((7-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)heptyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 401 N-(2′-fluoro-5′-((8-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 402 N-(2′-fluoro-4′-((2-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)ethyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 403 N-(2′-fluoro-4′-((3-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)propyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 404 N-(2′-fluoro-4′-((4-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)butyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 405 N-(2′-fluoro-4′-((5-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)pentyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 406 N-(2′-fluoro-4′-((6-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 407 N-(2′-fluoro-4′-((7-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)heptyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 408 N-(2′-fluoro-4′-((8-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 409 N-(2′-fluoro-5′-((2-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)ethyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 416 N-(2′-fluoro-4′-((2-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)ethyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 417 N-(2′-fluoro-4′-((3-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)propyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 418 N-(2′-fluoro-4′-((4-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)butyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 419 N-(2′-fluoro-4′-((5-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)pentyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 420 N-(2′-fluoro-4′-((6-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 421 N-(2′-fluoro-4′-((7-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)heptyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 422 N-(2′-fluoro-4′-((8-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 423 (3R,5S)-1-((S)-2-(2-(6-fluoro-3′-(6-oxo- 4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- carboxamido)acetamido)-3,3- dimethylbutanoyl)-5-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-3-yl acetate 424 (3R,5S)-1-((S)-2-(2-(6-fluoro-3′-(6-oxo- 4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- carboxamido)acetamido)-3,3- dimethylbutanoyl)-5-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-3-yl isobutyrate. ### Claim 11 A bivalent compound selected from the group consisting of: 369 N-(3′-((4-((S)-3-((2S,4R)-4-hydroxy-1- ((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanoyl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 374 N-(3′-((4-(6-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 375 N-(3′-((4-(7-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)heptanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 376 N-(3′-((4-(8-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 377 N-(3′-((4-(9-((S)-3-((2S,4R)-4-hydroxy- 1-((R)-3-methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)nonanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 378 N-(3′-((4-(10-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)decanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 379 N-(3′-((4-(11-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)undecanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 380 N-(3′-((4-((S)-3-((2S,4R)-1-((S)-2-(1- fluorocyclopropane-1-carboxamido)- 3,3-dimethylbutanoyl)-4- hydroxypyrrolidine-2-carboxamido)- 3-(4-(4-methylthiazol-5- yl)phenyl)propanoyl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 388 N-(3′-((4-(9-((S)-3-((2S,4R)-1-((S)-2-(1- fluorocyclopropane-1-carboxamido)- 3,3-dimethylbutanoyl)-4- hydroxypyrrolidine-2-carboxamido)- 3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)nonanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 389 N-(3′-((4-(10-((S)-3-((2S,4R)-1-((S)-2- (1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)decanoyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 392 1′-((S)-3-((2S,4R)-4-hydroxy-1-((R)-3- methyl-2-(3-methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanoyl)-N-(2-(4-((4′-(4- methylpiperazin-1-yl)-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)-[1,4′-bipiperidine]-4- carboxamide 397 N-(2′-fluoro-5′-((4-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)butyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 398 N-(2′-fluoro-5′-((5-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)pentyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 399 N-(2′-fluoro-5′-((6-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 400 N-(2′-fluoro-5′-((7-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)heptyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 401 N-(2′-fluoro-5′-((8-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 402 N-(2′-fluoro-4′-((2-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)ethyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 403 N-(2′-fluoro-4′-((3-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)propyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 404 N-(2′-fluoro-4′-((4-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)butyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 405 N-(2′-fluoro-4′-((5-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)pentyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 406 N-(2′-fluoro-4′-((6-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 407 N-(2′-fluoro-4′-((7-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)heptyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 408 N-(2′-fluoro-4′-((8-((S)-3-((2S,4R)-4- hydroxy-1-((R)-3-methyl-2-(3- methylisoxazol-5- yl)butanoyl)pyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)octyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 417 N-(2′-fluoro-4′-((3-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)propyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 418 N-(2′-fluoro-4′-((4-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)butyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 419 N-(2′-fluoro-4′-((5-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)pentyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 420 N-(2′-fluoro-4′-((6-((S)-3-((2S,4R)-1- ((S)-2-(1-fluorocyclopropane-1- carboxamido)-3,3-dimethylbutanoyl)- 4-hydroxypyrrolidine-2- carboxamido)-3-(4-(4-methylthiazol-5- yl)phenyl)propanamido)hexyl) carbamoyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide 423 (3R,5S)-1-((S)-2-(2-(6-fluoro-3′-(6-oxo- 4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- carboxamido)acetamido)-3,3- dimethylbutanoyl)-5-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-3-yl acetate 424 (3R,5S)-1-((S)-2-(2-(6-fluoro-3′-(6-oxo- 4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- carboxamido)acetamido)-3,3- dimethylbutanoyl)-5-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-3-yl isobutyrate. ### Claim 12 A bivalent compound selected from the group consisting of: XF048- 133 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N11-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)undecanediamide XF048- 140 N-(3′-((4-(2-(8-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)octanamido)ethyl)piperazin- 1-yl)methyl)-4-(4-methylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 145 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azahenicosan-21-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF050- 169 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N11-(3- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)propyl)undecanediamide XF056- 132 N-(2′-fluoro-5′-((2-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 67 N-(2′-fluoro-5′-((2-(((S)-1-((2S,4R)-4- hydroxy-2-(((S)-1-(4-(4-methylthiazol- 5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2- yl)amino)-2-oxoethyl)carbamoyl)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide ### Claim 13 Bivalent compound: XF067- 67 N-(2′-fluoro-5′-((2-(((S)-1-((2S,4R)-4- hydroxy-2-(((S)-1-(4-(4-methylthiazol- 5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2- yl)amino)-2-oxoethyl)carbamoyl)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide ### Claim 14 A bivalent compound selected from the group consisting of XF048- 117 N-(3′-((4-(2-(2-(2-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2- oxoethoxy)acetamido)ethyl)piperazin- 1-yl)methyl)-4-(4-methylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 118 N-(3′-((4-(2-(3-(3-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy)propanamido)ethyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 130 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N8-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)octanediamide XF048- 131 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N9-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)nonanediamide XF048- 132 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N10-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)decanediamide XF048- 133 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N11-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)undecanediamide XF048- 136 N-(3′-((4-(2-(4-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)butanamido)ethyl)piperazin- 1-yl)methyl)-4-(4-methylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 139 N-(3′-((4-(2-(7-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)heptanamido)ethyl)piperazin- 1-yl)methyl)-4-(4-methylpiperazin- 1-yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 140 N-(3′-((4-(2-(8-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)octanamido)ethyl)piperazin- 1-yl)methyl)-4-(4-methylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 141 N-(3′-((4-(2-(3-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethoxy)propanamido)ethyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 142 N-(3′-((4-(2-(3-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl) amino)ethoxy)ethoxy)propanamido) ethyl)piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 143 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 12-oxo-3,6,9-trioxa-13-azapentadecan- 15-yl)piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 144 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 15-oxo-3,6,9,12-tetraoxa-16- azaoctadecan-18-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 145 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azahenicosan-21-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF050- 166 N1-((S)-1-((2S,4R)-4-hydroxy-2-(((S)- 1-(4-(4-methylthiazol-5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2-yl)- N11-(2-(4-((4′-(4-methylpiperazin-1- yl)-3′-(6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)undecanediamide XF050- 169 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N11-(3- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)propyl)undecanediamide XF050- 161 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N13-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)tridecanediamide XF050- 162 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N14-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)tetradecanediamide XF050- 156 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azadocosan-22-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF050- 158 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azapentacosan-25-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 23 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)oxy)-18- oxo-3,6,9,12,15-pentaoxa-19- azahenicosan-21-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 25 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 27-oxo-3,6,9,12,15,18,21,24-octaoxa- 28-azatriacontan-30-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 26 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 30-oxo-3,6,9,12,15,18,21,24,27- nonaoxa-31-azatritriacontan-33- yl)piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 39 N-(3′-((4-(2-(8-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)oxy)octanamido)ethyl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 132 N-(2′-fluoro-5′-((2-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 134 N-(2′-fluoro-5′-((4-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 4-oxobutyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 137 N-(2′-fluoro-5′-((7-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 7-oxoheptyl)carbamoyl)-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 140 N-(2′-fluoro-5′-((10-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 10-oxodecyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 151 N-(5′-((6-((2-(2,6-dioxopiperidin-3-yl)- 1,3-dioxoisoindolin-4- yl)amino)hexyl)carbamoyl)-2′-fluoro- 4-((3R,5S)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 152 N-(5′-((7-((2-(2,6-dioxopiperidin-3-yl)- 1,3-dioxoisoindolin-4- yl)amino)heptyl)carbamoyl)-2′-fluoro- 4-((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 153 N-(5′-((8-((2-(2,6-dioxopiperidin-3-yl)- 1,3-dioxoisoindolin-4- yl)amino)octyl)carbamoyl)-2′-fluoro- 4-((3R,5S)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 158 N-(2′-fluoro-4′-((2-(3-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy)ethyl)carbamoyl)-4- ((3R,5S)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 159 N-(2′-fluoro-4′-((2-(2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)ethoxy)ethyl)carbamoyl)- 4-((3R,5S)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 162 N-(2′-fluoro-4′-(((S)-14-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-15,15-dimethyl-12-oxo- 3,6,9-trioxa-13- azahexadecyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 166 N-(2′-fluoro-4′-((3-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropyl)carbamoyl)-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 171 N-(2′-fluoro-4′-((8-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 8-oxooctyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 173 N-(2′-fluoro-4′-((10-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 10-oxodecyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 178 N-(4′-((14-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12- tetraoxatetradecyl)carbamoyl)-2′- fluoro-4-((3R,5S)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 186 N-(4′-((8-((2-(2,6-dioxopiperidin-3-yl)- 1,3-dioxoisoindolin-4- yl)amino)octyl)carbamoyl)-2′-fluoro- 4-((3R,5S)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 67 N-(2′-fluoro-5′-((2-(((S)-1-((2S,4R)-4- hydroxy-2-(((S)-1-(4-(4-methylthiazol- 5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2- yl)amino)-2-oxoethyl)carbamoyl)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 131 N-(4-fluoro-5-(6-(4-(4-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 4-oxobutanoyl)piperazin-1-yl)pyridin- 3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 133 N-(4-fluoro-5-(6-(4-(11-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 11-oxoundecanoyl)piperazin-1- yl)pyridin-3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 134 N-(4-fluoro-5-(6-(4-(11-(((S)-1- ((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4- methylthiazol-5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2- yl)amino)-11- oxoundecanoyl)piperazin-1- yl)pyridin-3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 140 N-(4-fluoro-5-(6-(4-(4-((2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)ethyl)amino)-4- oxobutanoyl)piperazin-1-yl)pyridin-3- yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 142 N-(4-fluoro-5-(6-(4-((S)-3-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-2,2-dimethyl-5,14-dioxo- 7,10-dioxa-4,13-diazaheptadecan-17- oyl)piperazin-1-yl)pyridin-3-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF067- 146 N-(4-fluoro-5-(6-(4-((S)-3-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-2,2-dimethyl-5,21-dioxo- 8,11,14,17-tetraoxa-4,20- diazatetracosan-24-oyl)piperazin-1- yl)pyridin-3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 149 N-(4-fluoro-5-(6-(4-(4-((3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropyl)amino)-4- oxobutanoyl)piperazin-1-yl)pyridin-3- yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 152 N-(4-fluoro-5-(6-(4-(4-((6-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 6-oxohexyl)amino)-4- oxobutanoyl)piperazin-1-yl)pyridin-3- yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 1 N-(2′-fluoro-5′-((4-(2-(2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2- oxoethoxy)acetamido)ethyl)piperazin- 1-yl)methyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 2 N-(2′-fluoro-5′-((4-(2-(3-(3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy) propanamido)ethyl)piperazin- 1-yl)methyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 3 N-(2′-fluoro-5′-((4-((S)-13-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-14,14-dimethyl-4,11-dioxo- 6,9-dioxa-3,12- diazapentadecyl)piperazin-1- yl)methyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 4 N-(2′-fluoro-5′-((4-((S)-15-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-16,16-dimethyl-4,13-dioxo- 7,10-dioxa-3,14- diazaheptadecyl)piperazin-1- yl)methyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 5 N-(2′-fluoro-5′-((4-((S)-16-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-17,17-dimethyl-4,14-dioxo- 6,9,12-trioxa-3,15- diazaoctadecyl)piperazin-1- yl)methyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 6 N-(2′-fluoro-5′-((4-((S)-18-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-19,19-dimethyl-4,16-dioxo- 7,10,13-trioxa-3,17- diazaicosyl)piperazin-1-yl)methyl)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 8 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N17- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)- 3,6,9,12,15- pentaoxaheptadecanediamide XF078- 9 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N19- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)- 4,7,10,13,16- pentaoxanonadecanediamide XF078- 12 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N6- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)adipamide XF078- 13 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N7- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)heptanediamide XF078- 14 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N8- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)octanediamide XF078- 15 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N9- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)nonanediamide XF078- 16 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N10- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)decanediamide XF078- 17 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N11- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)undecanediamide XF078- 18 N-(5′-((4-(2-(2-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)acetamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 19 N-(5′-((4-(2-(3-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)propanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 20 N-(5′-((4-(2-(4-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)butanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 21 N-(5′-((4-(2-(5-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)pentanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 22 N-(5′-((4-(2-(6-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)hexanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 23 N-(5′-((4-(2-(7-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)heptanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 24 N-(5′-((4-(2-(8-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)octanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 25 N-(5′-((4-(2-(3-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethoxy)propanamido)ethyl) piperazin-1-yl)methyl)-2′-fluoro-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 26 N-(5′-((4-(2-(3-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)propanamido) ethyl)piperazin-1-yl)methyl)-2′- fluoro-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 27 N-(5′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 12-oxo-3,6,9-trioxa-13-azapentadecan- 15-yl)piperazin-1-yl)methyl)-2′-fluoro- 4-((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 28 N-(5′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 15-oxo-3,6,9,12-tetraoxa-16- azaoctadecan-18-yl)piperazin-1- yl)methyl)-2′-fluoro-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 29 N-(5′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azahenicosan-21-yl)piperazin-1- yl)methyl)-2′-fluoro-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 30 N-(4-fluoro-5-(1-(2-(2-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)acetyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 34 N-(4-fluoro-5-(1-((S)-13-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-14,14-dimethyl-11-oxo- 3,6,9-trioxa-12-azapentadecanoyl)- 1,2,3,6-tetrahydropyridin-4-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 35 N-(4-fluoro-5-(1-((S)-15-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-16,16-dimethyl-13-oxo- 4,7,10-trioxa-14-azaheptadecanoyl)- 1,2,3,6-tetrahydropyridin-4-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 41 N-(4-fluoro-5-(1-(6-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 6-oxohexanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 42 N-(4-fluoro-5-(1-(7-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 7-oxoheptanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 43 N-(4-fluoro-5-(1-(8-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 8-oxooctanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 44 N-(4-fluoro-5-(1-(9-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 9-oxononanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 45 N-(4-fluoro-5-(1-(10-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 10-oxodecanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 46 N-(4-fluoro-5-(1-(11-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 11-oxoundecanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 51 N-(5-(1-(6-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4- yl)amino)hexanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 52 N-(5-(1-(7-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4- yl)amino)heptanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 53 N-(5-(1-(8-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4- yl)amino)octanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 57 N-(5-(1-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12-tetraoxapentadecan-15-oyl)- 1,2,3,6-tetrahydropyridin-4-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 58 N-(5-(1-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12,15-pentaoxaoctadecan-18- oyl)-1,2,3,6-tetrahydropyridin-4-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 61 N-(4-fluoro-5-(2-(4-(4-((2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)ethyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 62 N-(4-fluoro-5-(2-(4-(4-((2-(3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy)ethyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 63 N-(4-fluoro-5-(2-(4-((S)-3-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-2,2-dimethyl-5,14-dioxo- 7,10-dioxa-4,13-diazaheptadecan-17- oyl)piperazin-1-yl)pyrimidin-5-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 69 N-(4-fluoro-5-(2-(4-(4-((2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 70 N-(4-fluoro-5-(2-(4-(4-((3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 71 N-(4-fluoro-5-(2-(4-(4-((4-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 4-oxobutyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 79 N-(5-(2-(4-(4-((2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethoxy)ethyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 80 N-(5-(2-(4-(4-((2-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethoxy)ethoxy)ethyl)amino)- 4-oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 81 N-(5-(2-(4-(1-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl)amino)- 13-oxo-3,6,9-trioxa-12-azahexadecan- 16-oyl)piperazin-1-yl)pyrimidin-5-yl)- 4-fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 84 N-(5-(2-(4-(4-((2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 99 (2S,4R)-1-((S)-2-(2-(2-(4-(5-(2-fluoro- 5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-2-oxoethoxy)acetamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 101 (2S,4R)-1-((S)-2-(2-(2-(2-(4-(5-(2- fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-2-oxoethoxy)ethoxy)acetamido)- 3,3-dimethylbutanoyl)-4-hydroxy-N- (4-(4-methylthiazol-5- yl)benzyl)pyrrolidine-2-carboxamide XF078- 102 (2S,4R)-1-((S)-2-(3-(2-(3-(4-(5-(2- fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-3- oxopropoxy)ethoxy)propanamido)- 3,3-dimethylbutanoyl)-4-hydroxy-N- (4-(4-methylthiazol-5- yl)benzyl)pyrrolidine-2-carboxamide XF078- 103 (2S,4R)-1-((S)-2-(tert-butyl)-14-(4-(5- (2-fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-4,14-dioxo-6,9,12-trioxa-3- azatetradecanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 104 (2S,4R)-1-((S)-2-(tert-butyl)-16-(4-(5- (2-fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-4,16-dioxo-7,10,13-trioxa-3- azahexadecanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 105 (2S,4R)-1-((S)-2-(tert-butyl)-19-(4-(5- (2-fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-4,19-dioxo-7,10,13,16-tetraoxa-3- azanonadecanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 106 (2S,4R)-1-((S)-2-(tert-butyl)-20-(4-(5- (2-fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-4,20-dioxo-6,9,12,15,18-pentaoxa- 3-azaicosanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 110 (2S,4R)-1-((S)-2-(6-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-6-oxohexanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 111 (2S,4R)-1-((S)-2-(7-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-7-oxoheptanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 112 (2S,4R)-1-((S)-2-(8-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-8-oxooctanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 113 (2S,4R)-1-((S)-2-(9-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-9-oxononanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 114 (2S,4R)-1-((S)-2-(10-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-10-oxodecanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 115 (2S,4R)-1-((S)-2-(11-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-11-oxoundecanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 118 N-(5-(2-(4-(4-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)butanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 4-fluoro-2- (trifluoromethyl)benzamide XF078- 119 N-(5-(2-(4-(5-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)pentanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 4-fluoro-2- (trifluoromethyl)benzamide XF078- 120 N-(5-(2-(4-(6-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)hexanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 4-fluoro-2- (trifluoromethyl)benzamide XF078- 121 N-(5-(2-(4-(7-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)heptanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 4-fluoro-2- (trifluoromethyl)benzamide XF078- 122 N-(5-(2-(4-(8-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)octanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 4-fluoro-2- (trifluoromethyl)benzamide XF078- 123 N-(5-(2-(4-(3-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethoxy)propanoyl)piperazin- 1-yl)pyrimidin-5-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-4-fluoro-2- (trifluoromethyl)benzamide XF078- 124 N-(5-(2-(4-(3-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)propanoyl)piperazin- 1-yl)pyrimidin-5-yl)-4-fluoro- 2-((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-4-fluoro-2- (trifluoromethyl)benzamide XF078- 125 N-(5-(2-(4-(3-(2-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)ethoxy)propanoyl) piperazin-1-yl)pyrimidin-5-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-4- fluoro-2-(trifluoromethyl)benzamide XF078- 126 N-(5-(2-(4-(1-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12-tetraoxapentadecan-15- oyl)piperazin-1-yl)pyrimidin-5-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-4- fluoro-2-(trifluoromethyl)benzamide XF078- 127 N-(5-(2-(4-(1-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12,15-pentaoxaoctadecan-18- oyl)piperazin-1-yl)pyrimidin-5-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-4- fluoro-2-(trifluoromethyl)benzamide XF078- 132 N-(4-fluoro-5-(1-(5-((4-(2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)acetyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 133 N-(4-fluoro-5-(1-(5-((4-(3-(3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy)propanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 134 N-(4-fluoro-5-(1-(5-((4-(2-(2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)ethoxy)acetyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 135 N-(4-fluoro-5-(1-(5-((4-(3-(2-(3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy) ethoxy)propanoyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)- 1,2,3,6-tetrahydropyridin-4-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 136 N-(4-fluoro-5-(1-(5-((4-((S)-13- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-14,14-dimethyl-11-oxo- 3,6,9-trioxa-12- azapentadecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 137 N-(4-fluoro-5-(1-(5-((4-((S)-15- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-16,16-dimethyl-13-oxo- 4,7,10-trioxa-14- azaheptadecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 138 N-(4-fluoro-5-(1-(5-((4-((S)-18- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-19,19-dimethyl-16-oxo- 4,7,10,13-tetraoxa-17- azaicosanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 139 N-(4-fluoro-5-(1-(5-((4-((S)-19- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-20,20-dimethyl-17-oxo- 3,6,9,12,15-pentaoxa-18- azahenicosanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 140 N-(4-fluoro-5-(1-(5-((4-((S)-21- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-22,22-dimethyl-19-oxo- 4,7,10,13,16-pentaoxa-20- azatricosanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 141 N-(4-fluoro-5-(1-(5-((4-(4-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 4-oxobutanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 142 N-(4-fluoro-5-(1-(5-((4-(5-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 5-oxopentanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 143 N-(4-fluoro-5-(1-(5-((4-(6-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 6-oxohexanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 144 N-(4-fluoro-5-(1-(5-((4-(7-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 7-oxoheptanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 145 N-(4-fluoro-5-(1-(5-((4-(8-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 8-oxooctanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 146 N-(4-fluoro-5-(1-(5-((4-(9-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 9-oxononanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 147 N-(4-fluoro-5-(1-(5-((4-(10-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 10-oxodecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 148 N-(4-fluoro-5-(1-(5-((4-(11-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 11-oxoundecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 149 N-(5-(1-(5-((4-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)glycyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 150 N-(5-(1-(5-((4-(3-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)propanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 151 N-(5-(1-(5-((4-(4-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)butanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 152 N-(5-(1-(5-((4-(5-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)pentanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 157 N-(5-(1-(5-((4-(3-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)propanoyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)- 1,2,3,6-tetrahydropyridin-4-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 158 N-(5-(1-(5-((4-(3-(2-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)ethoxy)propanoyl) piperazin-1-yl)methyl)pyrimidin- 2-yl)-1,2,3,6-tetrahydropyridin-4-yl)- 4-fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 159 N-(5-(1-(5-((4-(1-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino)-3,6,9,12- tetraoxapentadecan-15-oyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 160 N-(5-(1-(5-((4-(1-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino)- 3,6,9,12,15-pentaoxaoctadecan-18- oyl)piperazin-1-yl)methyl)pyrimidin- 2-yl)-1,2,3,6-tetrahydropyridin-4-yl)- 4-fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF061- 33 (2S,4R)-1-((S)-2-(2-(2-((3-(5-(((R)-6- (6,7-dihydro-5H-pyrrolo[1,2- a]imidazol-2-yl)-2,3-dihydro-1H- inden-1-yl)carbamoyl)-3-methoxy-2- methylphenoxy)propyl)amino)-2- oxoethoxy)acetamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF061- 34 (2S,4R)-1-((S)-2-(3-(3-((3-(5-(((R)-6- (6,7-dihydro-5H-pyrrolo[1,2- a]imidazol-2-yl)-2,3-dihydro-1H- inden-1-yl)carbamoyl)-3-methoxy-2- methylphenoxy)propyl)amino)-3- oxopropoxy)propanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide ### Claim 15 A bivalent compound selected from the group consisting of: TABLE 1 XF048- 130 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N8-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)octanediamide XF048- 131 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N9-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)nonanediamide XF048- 132 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N10-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)decanediamide XF048- 133 N1-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)-N11-(2- (4-((4′-(4-methylpiperazin-1-yl)-3′-(6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)undecanediamide XF048- 139 N-(3′-((4-(2-(7-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)heptanamido)ethyl)piperazin- 1-yl)methyl)-4-(4-methylpiperazin- 1-yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 140 N-(3′-((4-(2-(8-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)octanamido)ethyl)piperazin- 1-yl)methyl)-4-(4-methylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 141 N-(3′-((4-(2-(3-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethoxy)propanamido)ethyl) piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 142 N-(3′-((4-(2-(3-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl) amino)ethoxy)ethoxy)propanamido) ethyl)piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 143 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 12-oxo-3,6,9-trioxa-13-azapentadecan- 15-yl)piperazin-1-yl)methyl)-4-(4- methylpiperazin-1-yl)-[1,1′-biphenyl]- 3-yl)-6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 144 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 15-oxo-3,6,9,12-tetraoxa-16- azaoctadecan-18-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF048- 145 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azahenicosan-21-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF050- 166 N1-((S)-1-((2S,4R)-4-hydroxy-2-(((S)- 1-(4-(4-methylthiazol-5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2-yl)- N11-(2-(4-((4′-(4-methylpiperazin-1- yl)-3′-(6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)- [1,1′-biphenyl]-3-yl)methyl)piperazin- 1-yl)ethyl)undecanediamide XF050- 158 N-(3′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azapentacosan-25-yl)piperazin-1- yl)methyl)-4-(4-methylpiperazin-1-yl)- [1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 132 N-(2′-fluoro-5′-((2-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 162 N-(2′-fluoro-4′-(((S)-14-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-15,15-dimethyl-12-oxo- 3,6,9-trioxa-13- azahexadecyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 171 N-(2′-fluoro-4′-((8-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 8-oxooctyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 173 N-(2′-fluoro-4′-((10-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 10-oxodecyl)carbamoyl)-4-((3R,5S)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 178 N-(4′-((14-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12- tetraoxatetradecyl)carbamoyl)-2′- fluoro-4-((3R,5S)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF056- 186 N-(4′-((8-((2-(2,6-dioxopiperidin-3-yl)- 1,3-dioxoisoindolin-4- yl)amino)octyl)carbamoyl)-2′-fluoro- 4-((3R,5S)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 67 N-(2′-fluoro-5′-((2-(((S)-1-((2S,4R)-4- hydroxy-2-(((S)-1-(4-(4-methylthiazol- 5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2- yl)amino)-2-oxoethyl)carbamoyl)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 131 N-(4-fluoro-5-(6-(4-(4-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 4-oxobutanoyl)piperazin-1-yl)pyridin- 3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 133 N-(4-fluoro-5-(6-(4-(11-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 11-oxoundecanoyl)piperazin-1- yl)pyridin-3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 134 N-(4-fluoro-5-(6-(4-(11-(((S)-1- ((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4- methylthiazol-5- yl)phenyl)ethyl)carbamoyl)pyrrolidin- 1-yl)-3,3-dimethyl-1-oxobutan-2- yl)amino)-11- oxoundecanoyl)piperazin-1- yl)pyridin-3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 140 N-(4-fluoro-5-(6-(4-(4-((2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)ethyl)amino)-4- oxobutanoyl)piperazin-1-yl)pyridin-3- yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 142 N-(4-fluoro-5-(6-(4-((S)-3-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-2,2-dimethyl-5,14-dioxo- 7,10-dioxa-4,13-diazaheptadecan-17- oyl)piperazin-1-yl)pyridin-3-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF067- 146 N-(4-fluoro-5-(6-(4-((S)-3-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-2,2-dimethyl-5,21-dioxo- 8,11,14,17-tetraoxa-4,20- diazatetracosan-24-oyl)piperazin-1- yl)pyridin-3-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF067- 149 N-(4-fluoro-5-(6-(4-(4-((3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropyl)amino)-4- oxobutanoyl)piperazin-1-yl)pyridin-3- yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 1 N-(2′-fluoro-5′-((4-(2-(2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2- oxoethoxy)acetamido)ethyl)piperazin- 1-yl)methyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 2 N-(2′-fluoro-5′-((4-(2-(3-(3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy) propanamido)ethyl)piperazin- 1-yl)methyl)-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 6 N-(2′-fluoro-5′-((4-((S)-18-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-19,19-dimethyl-4,16-dioxo- 7,10,13-trioxa-3,17- diazaicosyl)piperazin-1-yl)methyl)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 8 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N17- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)- 3,6,9,12,15- pentaoxaheptadecanediamide XF078- 14 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N8- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)octanediamide XF078- 15 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N9- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)nonanediamide XF078- 16 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N10- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)decanediamide XF078- 17 N1-(2-(4-((6-fluoro-3′-(6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamido)-4′- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3- yl)methyl)piperazin-1-yl)ethyl)-N11- ((S)-1-((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2- yl)undecanediamide XF078- 18 N-(5′-((4-(2-(2-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)acetamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 19 N-(5′-((4-(2-(3-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)propanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 20 N-(5′-((4-(2-(4-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)butanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 21 N-(5′-((4-(2-(5-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)pentanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 22 N-(5′-((4-(2-(6-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)hexanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 23 N-(5′-((4-(2-(7-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl) amino)heptanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 24 N-(5′-((4-(2-(8-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)octanamido)ethyl)piperazin- 1-yl)methyl)-2′-fluoro-4-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 25 N-(5′-((4-(2-(3-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)ethoxy)propanamido)ethyl) piperazin-1-yl)methyl)-2′-fluoro-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 26 N-(5′-((4-(2-(3-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)propanamido) ethyl)piperazin-1-yl)methyl)-2′- fluoro-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 27 N-(5′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 12-oxo-3,6,9-trioxa-13-azapentadecan- 15-yl)piperazin-1-yl)methyl)-2′-fluoro- 4-((3S,5R)-3,4,5-trimethylpiperazin-1- yl)-[1,1′-biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 28 N-(5′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 15-oxo-3,6,9,12-tetraoxa-16- azaoctadecan-18-yl)piperazin-1- yl)methyl)-2′-fluoro-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 29 N-(5′-((4-(1-((2-(2,6-dioxopiperidin-3- yl)-1,3-dioxoisoindolin-4-yl)amino)- 18-oxo-3,6,9,12,15-pentaoxa-19- azahenicosan-21-yl)piperazin-1- yl)methyl)-2′-fluoro-4-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)-[1,1′- biphenyl]-3-yl)-6-oxo-4- (trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 30 N-(4-fluoro-5-(1-(2-(2-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)acetyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 34 N-(4-fluoro-5-(1-((S)-13-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-14,14-dimethyl-11-oxo- 3,6,9-trioxa-12-azapentadecanoyl)- 1,2,3,6-tetrahydropyridin-4-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 41 N-(4-fluoro-5-(1-(6-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 6-oxohexanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 42 N-(4-fluoro-5-(1-(7-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 7-oxoheptanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 43 N-(4-fluoro-5-(1-(8-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 8-oxooctanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 44 N-(4-fluoro-5-(1-(9-(((S)-1-((2S,4R)-4- hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 9-oxononanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 45 N-(4-fluoro-5-(1-(10-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 10-oxodecanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 46 N-(4-fluoro-5-(1-(11-(((S)-1-((2S,4R)- 4-hydroxy-2-((4-(4-methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 11-oxoundecanoyl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 61 N-(4-fluoro-5-(2-(4-(4-((2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)ethyl)amino)-4- oxobutanoyl)piperazin-1- yl)pyrimidin-5-yl)-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 99 (2S,4R)-1-((S)-2-(2-(2-(4-(5-(2-fluoro- 5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-2-oxoethoxy)acetamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 101 (2S,4R)-1-((S)-2-(2-(2-(2-(4-(5-(2- fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-2-oxoethoxy)ethoxy)acetamido)- 3,3-dimethylbutanoyl)-4-hydroxy-N- (4-(4-methylthiazol-5- yl)benzyl)pyrrolidine-2-carboxamide XF078- 102 (2S,4R)-1-((S)-2-(3-(2-(3-(4-(5-(2- fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-3- oxopropoxy)ethoxy)propanamido)- 3,3-dimethylbutanoyl)-4-hydroxy-N- (4-(4-methylthiazol-5- yl)benzyl)pyrrolidine-2-carboxamide XF078- 103 (2S,4R)-1-((S)-2-(tert-butyl)-14-(4-(5- (2-fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-4,14-dioxo-6,9,12-trioxa-3- azatetradecanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 105 (2S,4R)-1-((S)-2-(tert-butyl)-19-(4-(5- (2-fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-4,19-dioxo-7,10,13,16-tetraoxa-3- azanonadecanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 106 (2S,4R)-1-((S)-2-(tert-butyl)-20-(4-(5- (2-fluoro-5-(4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-4,20-dioxo-6,9,12,15,18-pentaoxa- 3-azaicosanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 110 (2S,4R)-1-((S)-2-(6-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-6-oxohexanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 111 (2S,4R)-1-((S)-2-(7-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-7-oxoheptanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 112 (2S,4R)-1-((S)-2-(8-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-8-oxooctanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 113 (2S,4R)-1-((S)-2-(9-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-9-oxononanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 114 (2S,4R)-1-((S)-2-(10-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-10-oxodecanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 115 (2S,4R)-1-((S)-2-(11-(4-(5-(2-fluoro-5- (4-fluoro-2- (trifluoromethyl)benzamido)-4- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)pyrimidin-2-yl)piperazin-1- yl)-11-oxoundecanamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide XF078- 121 N-(5-(2-(4-(7-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)amino)heptanoyl)piperazin-1- yl)pyrimidin-5-yl)-4-fluoro-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 4-fluoro-2- (trifluoromethyl)benzamide XF078- 125 N-(5-(2-(4-(3-(2-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)ethoxy)propanoyl) piperazin-1-yl)pyrimidin-5-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-4- fluoro-2-(trifluoromethyl)benzamide XF078- 126 N-(5-(2-(4-(1-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12-tetraoxapentadecan-15- oyl)piperazin-1-yl)pyrimidin-5-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-4- fluoro-2-(trifluoromethyl)benzamide XF078- 127 N-(5-(2-(4-(1-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4-yl)amino)- 3,6,9,12,15-pentaoxaoctadecan-18- oyl)piperazin-1-yl)pyrimidin-5-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-4- fluoro-2-(trifluoromethyl)benzamide XF078- 132 N-(4-fluoro-5-(1-(5-((4-(2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)acetyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 133 N-(4-fluoro-5-(1-(5-((4-(3-(3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy)propanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 134 N-(4-fluoro-5-(1-(5-((4-(2-(2-(2-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 2-oxoethoxy)ethoxy)acetyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 135 N-(4-fluoro-5-(1-(5-((4-(3-(2-(3-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 3-oxopropoxy) ethoxy)propanoyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)- 1,2,3,6-tetrahydropyridin-4-yl)-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 136 N-(4-fluoro-5-(1-(5-((4-((S)-13- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-14,14-dimethyl-11-oxo- 3,6,9-trioxa-12- azapentadecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 137 N-(4-fluoro-5-(1-(5-((4-((S)-15- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-16,16-dimethyl-13-oxo- 4,7,10-trioxa-14- azaheptadecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 138 N-(4-fluoro-5-(1-(5-((4-((S)-18- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-19,19-dimethyl-16-oxo- 4,7,10,13-tetraoxa-17- azaicosanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 139 N-(4-fluoro-5-(1-(5-((4-((S)-19- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidine-1- carbonyl)-20,20-dimethyl-17-oxo- 3,6,9,12,15-pentaoxa-18- azahenicosanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 141 N-(4-fluoro-5-(1-(5-((4-(4-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 4-oxobutanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 142 N-(4-fluoro-5-(1-(5-((4-(5-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 5-oxopentanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 143 N-(4-fluoro-5-(1-(5-((4-(6-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 6-oxohexanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 144 N-(4-fluoro-5-(1-(5-((4-(7-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 7-oxoheptanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 145 N-(4-fluoro-5-(1-(5-((4-(8-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 8-oxooctanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 146 N-(4-fluoro-5-(1-(5-((4-(9-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 9-oxononanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 147 N-(4-fluoro-5-(1-(5-((4-(10-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 10-oxodecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 148 N-(4-fluoro-5-(1-(5-((4-(11-(((S)-1- ((2S,4R)-4-hydroxy-2-((4-(4- methylthiazol-5- yl)benzyl)carbamoyl)pyrrolidin-1-yl)- 3,3-dimethyl-1-oxobutan-2-yl)amino)- 11-oxoundecanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-2-((3S,5R)- 3,4,5-trimethylpiperazin-1-yl)phenyl)- 6-oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 149 N-(5-(1-(5-((4-((2-(2,6-dioxopiperidin- 3-yl)-1,3-dioxoisoindolin-4- yl)glycyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 150 N-(5-(1-(5-((4-(3-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)propanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 151 N-(5-(1-(5-((4-(4-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4- yl)amino)butanoyl)piperazin-1- yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 157 N-(5-(1-(5-((4-(3-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)propanoyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)- 1,2,3,6-tetrahydropyridin-4-yl)-4- fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 158 N-(5-(1-(5-((4-(3-(2-(2-(2-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino) ethoxy)ethoxy)ethoxy)propanoyl) piperazin-1-yl)methyl)pyrimidin- 2-yl)-1,2,3,6-tetrahydropyridin-4-yl)- 4-fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF078- 159 N-(5-(1-(5-((4-(1-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino)-3,6,9,12- tetraoxapentadecan-15-oyl)piperazin- 1-yl)methyl)pyrimidin-2-yl)-1,2,3,6- tetrahydropyridin-4-yl)-4-fluoro-2- ((3S,5R)-3,4,5-trimethylpiperazin-1- yl)phenyl)-6-oxo-4-(trifluoromethyl)- 1,6-dihydropyridine-3-carboxamide XF078- 160 N-(5-(1-(5-((4-(1-((2-(2,6- dioxopiperidin-3-yl)-1,3- dioxoisoindolin-4-yl)amino)- 3,6,9,12,15-pentaoxaoctadecan-18- oyl)piperazin-1-yl)methyl)pyrimidin- 2-yl)-1,2,3,6-tetrahydropyridin-4-yl)- 4-fluoro-2-((3S,5R)-3,4,5- trimethylpiperazin-1-yl)phenyl)-6- oxo-4-(trifluoromethyl)-1,6- dihydropyridine-3-carboxamide XF061- 33 (2S,4R)-1-((S)-2-(2-(2-((3-(5-(((R)-6- (6,7-dihydro-5H-pyrrolo[1,2- a]imidazol-2-yl)-2,3-dihydro-1H- inden-1-yl)carbamoyl)-3-methoxy-2- methylphenoxy)propyl)amino)-2- oxoethoxy)acetamido)-3,3- dimethylbutanoyl)-4-hydroxy-N-(4-(4- methylthiazol-5-yl)benzyl)pyrrolidine- 2-carboxamide