US 12,110,295 B2Granted

WD40 repeat domain protein 5 (WDR5) degradation/disruption compounds and methods of use

AssigneesIcahn School of Medicine at Mount Sinai, The University of North Carolina at Chapel Hill

InventorsJian Jin, Gang Wang, Jing Liu, Xufen Yu, Dongxu Li

Life of this patent

Estimating the term…

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.

Claims15

Dependent claims

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.

66 more elements

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.

71 more elements

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.

55 more elements

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

293 more elements

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

190 more elements

Dependencies are inferred from the claim text.

Facts

Application: 17/254,345Filed 21 Jun 2019 · us provisional application
Priority: 21 Jun 2018
Published: US 2022/0348580 A13 Nov 2022
Granted: 8 Oct 2024
Term ends: Not estimatedThe source records don’t support an estimate.

Classification6 codes

A61P 35/00
Antineoplastic agents
C07D 487/04
In which the condensed system contains two hetero rings: ortho-condensed systems
C07D 401/14
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a…:…
C07D 417/14
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms,…

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Application62/688,343Us provisional application · filed 21 Jun 2018
US 2022/0348580 A1Pre-grant publication · published 3 Nov 2022
US 11,905,291 B2Related patent
US 12,110,295 B2This patent

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Abstract

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.

66 more elements

Facts

Application

17/254,345Filed 21 Jun 2019 · us provisional application

Priority

21 Jun 2018

Published

US 2022/0348580 A13 Nov 2022

Granted

8 Oct 2024

Term ends

Not estimatedThe source records don’t support an estimate.

Classification6 codes

A61P 35/00
Antineoplastic agents
C07D 487/04
In which the condensed system contains two hetero rings: ortho-condensed systems
C07D 401/14
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a…:…
C07D 417/14
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms,…