Farnesoid x receptor agonists and uses thereof
AssigneeMetacrine, Inc.
InventorsNicholas D. SMITH, Steven P. GOVEK, Johnny Y. NAGASAWA
Life of this patent
Estimating the term…
Abstract
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Claims144
A compound that has the structure of Formula (II), or a pharmaceutically acceptable salt or solvate thereof:
- wherein
- R1 and R2 are each independently selected from H, D, F, C1-C4alkyl, or C1-C4fluoroalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a substituted or unsubstituted C3-C10cycloalkyl, or substituted or unsubstituted C2-C10heterocycloalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a carbonyl (C═O);
- R3 is selected from substituted or unsubstituted C4-C10alkyl, substituted or unsubstituted C1-C10alkoxy, substituted or unsubstituted C2-C10alkenyl, or unsubstituted substituted C2-C10alkynyl, substituted or unsubstituted cyclopropyl, substituted or unsubstituted cyclobutyl, substituted or unsubstituted cyclopentyl, substituted cyclohexyl, substituted or unsubstituted cycloheptyl, substituted or unsubstituted cyclooctyl, substituted or unsubstituted C2-C10heterocycloalkyl containing 1 O or S atom, substituted aryl, or substituted or unsubstituted heteroaryl, wherein if R3 is substituted then R3 is substituted with one or more R12 groups;
- each R12 is independently selected from D, halogen, —CN, —NO2, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —S(═O)2N(R10)2, —NR10S(═O)2R11, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —N(R10)2, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10fluoroalkyl, unsubstituted or substituted C2-C10alkenyl, unsubstituted or substituted C2-C10alkynyl, unsubstituted or substituted C1-C10heteroalkyl, unsubstituted or substituted C3-C10cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, and -L4-L5-R13;
- L4 is absent, —O—, —S—, —S(═O)—, —S(═O)2—, —NR10—, —C(═O)—, —C(═O)NH—, —NHC(═O)—, —C(═O)O—, —OC(═O)—, —OC(═O)NH—, —NHC(═O)NH—, —NHC(═O)O—, —(CH2)r—, or —(OCH2CH2)r—, r is 1, 2, 3, or 4;
- L5 is absent, unsubstituted or substituted C1-C10alkylene, unsubstituted or substituted C1-C10heteroalkylene, unsubstituted or substituted C2-C10alkenylene, unsubstituted or substituted C2-C10alkynylene, unsubstituted or substituted C3-C10cycloalkylene, unsubstituted or substituted C2-C10heterocycloalkylene, unsubstituted or substituted arylene, or unsubstituted or substituted heteroarylene;
- R13 is H, halogen, —N(R10)2, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10alkenyl, unsubstituted or substituted C1-C10alkynyl, unsubstituted or substituted C1-C10cycloalkyl, unsubstituted or substituted C1-C10heterocycloalkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl;
- or R3 is —N(R14)2, wherein each R14 is independently selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C3-C6cycloalkyl, and substituted or unsubstituted benzyl, or two R13 on the same N atom are taken together with the N atom to which they are attached to form a N-containing heterocycle, provided that R3 is not —NHCH(CH3)2;
- R4 is -L3-Y;
- L3 is —C(R5)(R6)—, —C(R5)(R6)—C(R7)(R8)—, —C≡C—, —O—C(R7)(R8)—, or —C(R5)(R6)—O—;
- R5 and R7 are each independently selected from H, D, C1-C4alkyl and C3-C6cycloalkyl;
- or R5 and R7 are taken together with the intervening atoms to form a double bond;
- or R5 and R7 are taken together with the intervening atoms to form an epoxide or an substituted or unsubstituted C3-C6cycloalkyl;
- R6 and R8 are each independently selected from H, D, C1-C4alkyl or C3-C6cycloalkyl;
- Y is —CH2OR9, —C(═O)OR9,
- R9 is selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, or substituted or substituted or unsubstituted heterocycle;
- L1 is —X1-L2-, -L2-X1—;
- X1 is absent, —O—, —S—, —S(═O)—, —S(═O)2—, —S(═O)2NR10—, —CH2—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —OC(═O)O—, —C(═O)NR10—, —NR10C(═O)—, —OC(═O)NR10—, —NR10C(═O)O—, —NR10C(═O)NR10—, —NR10S(═O)2—, or —NR10—;
- L2 is absent or substituted or unsubstituted C1-C4alkylene;
- A is CRA, or N;
- each RA is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- B is CRB, or N;
- each RB is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —N(R10)2, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- ring C is monocyclic carbocycle, bicyclic carbocycle, monocyclic heterocycle, or bicyclic heterocycle;
- each RC is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —NO2, —N(R10)2, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted phenyl and substituted or unsubstituted monocyclic heteroaryl;
- each R10 is independently selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- or two R10 on the same N atom are taken together with the N atom to which they are attached to form a N-containing heterocycle;
- each R11 is independently selected from substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- m is 0, 1, or 2;
- n is 0, 1, or 2;
- p is 0, 1, 2, 3, or 4.
A compound that has the structure of Formula (I), or a pharmaceutically acceptable salt or solvate thereof:
- wherein,
- R1 and R2 are each independently selected from H, D, F, C1-C4alkyl, or C1-C4fluoroalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a substituted or unsubstituted C3-C10cycloalkyl, or substituted or unsubstituted C2-C10heterocycloalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a carbonyl (C═O);
- R3 is selected from substituted or unsubstituted C1-C10alkyl, substituted or unsubstituted C2-C10alkenyl, substituted or unsubstituted C2-C10alkynyl, substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C2-C10heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if R3 is substituted then R3 is substituted with one or more R12 groups;
- each R12 is independently selected from D, halogen, —CN, —NO2, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —S(═O)2N(R10)2, —NR10S(═O)2R11, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —N(R10)2, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10fluoroalkyl, unsubstituted or substituted C2-C10alkenyl, unsubstituted or substituted C2-C10alkynyl, unsubstituted or substituted C1-C10heteroalkyl, unsubstituted or substituted C3-C10cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, and -L4-L5-R13;
- L4 is absent, —O—, —S—, —S(═O)—, —S(═O)2—, —NR10—, —C(═O)—, —C(═O)NH—, —NHC(═O)—, —C(═O)O—, —OC(═O)—, —OC(═O)NH—, —NHC(═O)NH—, —NHC(═O)O—, —(CH2)r—, or —(OCH2CH2)r—, r is 1, 2, 3, or 4;
- L5 is absent, unsubstituted or substituted C1-C10alkylene, unsubstituted or substituted C1-C10heteroalkylene, unsubstituted or substituted C2-C10alkenylene, unsubstituted or substituted C2-C10alkynylene, unsubstituted or substituted C3-C10cycloalkylene, unsubstituted or substituted C2-C10heterocycloalkylene, unsubstituted or substituted arylene, or unsubstituted or substituted heteroarylene;
- R13 is H, halogen, —N(R10)2, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10alkenyl, unsubstituted or substituted C1-C10alkynyl, unsubstituted or substituted C1-C10cycloalkyl, unsubstituted or substituted C1-C10heterocycloalkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl;
- R4 is -L3-Y;
- L3 is —C(R5)(R6)—, —C(R5)(R6)—C(R7)(R8)—, —C≡C—, —O—C(R7)(R8)—, or —C(R5)(R6)—O—;
- R5 and R7 are each independently selected from H, D, C1-C4alkyl and C3-C6cycloalkyl;
- or R5 and R7 are taken together with the intervening atoms to form a double bond;
- or R5 and R7 are taken together with the intervening atoms to form an epoxide or an substituted or unsubstituted C3-C6cycloalkyl;
- R6 and R8 are each independently selected from H, D, C1-C4alkyl or C3-C6cycloalkyl;
- Y is —CH2OR9, —C(═O)OR9,
- R9 is selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, or substituted or substituted or unsubstituted heterocycle;
- L1 is —X1-L2-, -L2-X1—;
- X1 is —O—, —S—, —S(═O)—, —S(═O)2—, —S(═O)2NR10—, —CH2—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —OC(═O)O—, —C(═O)NR10—, —NR10C(═O)—, —OC(═O)NR10—, —NR10C(═O)O—, —NR10C(═O)NR10—, —NR10S(═O)2—, or —NR10—;
- L2 is absent or substituted or unsubstituted C1-C4alkylene;
- A is CRA, or N;
- each RA is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- B is CRB, or N;
- each RB is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —N(R10)2, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- ring C is monocyclic carbocycle, bicyclic carbocycle, monocyclic N-containing heterocycle, or bicyclic heterocycle;
- each RC is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —NO2, —N(R10)2, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted phenyl and substituted or unsubstituted monocyclic heteroaryl;
- each R10 is independently selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- or two R10 on the same N atom are taken together with the N atom to which they are attached to form a N-containing heterocycle;
- each R11 is independently selected from substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- m is 0, 1, or 2;
- n is 0, 1, or 2;
- p is 0, 1, 2, 3, or 4.
A compound that has the structure of Formula (IV), or a pharmaceutically acceptable salt or solvate thereof:
- wherein
- R1 and R2 are each independently selected from H, D, F, C1-C4alkyl, or C1-C4fluoroalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a substituted or unsubstituted C3-C10cycloalkyl, or substituted or unsubstituted C2-C10heterocycloalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a carbonyl (C═O);
- R3 is selected from substituted or unsubstituted C1-C10alkyl, substituted or unsubstituted C2-C10alkenyl, substituted or unsubstituted C2-C10alkynyl, substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C2-C10heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if R3 is substituted then R3 is substituted with one or more R12 groups;
- each R12 is independently selected from D, halogen, —CN, —NO2, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —S(═O)2N(R10)2, —NR10S(═O)2R11, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —N(R10)2, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10fluoroalkyl, unsubstituted or substituted C2-C10alkenyl, unsubstituted or substituted C2-C10alkynyl, unsubstituted or substituted C1-C10heteroalkyl, unsubstituted or substituted C3-C10cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, and -L4-L5-R13;
- L4 is absent, —O—, —S—, —S(═O)—, —S(═O)2—, —NR10—, —C(═O)—, —C(═O)NH—, —NHC(═O)—, —C(═O)O—, —OC(═O)—, —OC(═O)NH—, —NHC(═O)NH—, —NHC(═O)O—, —(CH2)r—, or —(OCH2CH2)r—, r is 1, 2, 3, or 4;
- L5 is absent, unsubstituted or substituted C1-C10alkylene, unsubstituted or substituted C1-C10heteroalkylene, unsubstituted or substituted C2-C10alkenylene, unsubstituted or substituted C2-C10alkynylene, unsubstituted or substituted C3-C10cycloalkylene, unsubstituted or substituted C2-C10heterocycloalkylene, unsubstituted or substituted arylene, or unsubstituted or substituted heteroarylene;
- R13 is H, halogen, —N(R10)2, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10alkenyl, unsubstituted or substituted C1-C10alkynyl, unsubstituted or substituted C1-C10cycloalkyl, unsubstituted or substituted C1-C10heterocycloalkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl;
- R4 is -L3-Y;
- L3 is —C(R5)(R6)—, —C(R5)(R6)—C(R7)(R8)—, —C≡C—, —O—C(R7)(R8)—, or —C(R5)(R6)—O—;
- R5 and R7 are each independently selected from H, D, C1-C4alkyl and C3-C6cycloalkyl;
- or R5 and R7 are taken together with the intervening atoms to form a double bond;
- or R5 and R7 are taken together with the intervening atoms to form an epoxide or an substituted or unsubstituted C3-C6cycloalkyl;
- R6 and R8 are each independently selected from H, D, C1-C4alkyl or C3-C6cycloalkyl;
- Y is —CH2OR9, —C(═O)OR9,
- R9 is selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, or substituted or substituted or unsubstituted heterocycle;
- each RA is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- B is CRB, or N;
- each RB is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —N(R10)2, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- ring C is a 5-membered N-containing heteroaryl, or a N-containing C2-C8heterocycloalkyl;
- each RC is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —NO2, —N(R10)2, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted phenyl and substituted or unsubstituted monocyclic heteroaryl;
- each R10 is independently selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- or two R10 on the same N atom are taken together with the N atom to which they are attached to form a N-containing heterocycle;
- each R11 is independently selected from substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- m is 0, 1, or 2;
- n is 0, 1, or 2;
- p is 0, 1, 2, 3, or 4.
A compound that has the structure of Formula (VI), or a pharmaceutically acceptable salt or solvate thereof:
- wherein
- R1 and R2 are each independently selected from H, D, F, C1-C4alkyl, or C1-C4fluoroalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a substituted or unsubstituted C3-C10cycloalkyl, or substituted or unsubstituted C2-C10heterocycloalkyl;
- or R1 and R2 are taken together with the carbon atom to which they are attached to form a carbonyl (C═O);
- R3 is selected from substituted or unsubstituted C1-C10alkyl, substituted or unsubstituted C2-C10alkenyl, substituted or unsubstituted C2-C10alkynyl, substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C2-C10heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl, wherein if R3 is substituted then R3 is substituted with one or more R12 groups;
- each R12 is independently selected from D, halogen, —CN, —NO2, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —S(═O)2N(R10)2, —NR10S(═O)2R11, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —N(R10)2, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10fluoroalkyl, unsubstituted or substituted C2-C10alkenyl, unsubstituted or substituted C2-C10alkynyl, unsubstituted or substituted C1-C10heteroalkyl, unsubstituted or substituted C3-C10cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, and -L5-L6-R13;
- L5 is absent, —O—, —S—, —S(═O)—, —S(═O)2—, —NR10—, —C(═O)—, —C(═O)NH—, —NHC(═O)—, —C(═O)O—, —OC(═O)—, —OC(═O)NH—, —NHC(═O)NH—, —NHC(═O)O—, —(CH2)r—, or —(OCH2CH2)r—, r is 1, 2, 3, or 4;
- L6 is absent, unsubstituted or substituted C1-C10alkylene, unsubstituted or substituted C1-C10heteroalkylene, unsubstituted or substituted C2-C10alkenylene, unsubstituted or substituted C2-C10alkynylene, unsubstituted or substituted C3-C10cycloalkylene, unsubstituted or substituted C2-C10heterocycloalkylene, unsubstituted or substituted arylene, or unsubstituted or substituted heteroarylene;
- R13 is H, halogen, —N(R10)2, unsubstituted or substituted C1-C10alkyl, unsubstituted or substituted C1-C10alkenyl, unsubstituted or substituted C1-C10alkynyl, unsubstituted or substituted C1-C10cycloalkyl, unsubstituted or substituted C1-C10heterocycloalkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heteroaryl;
- ring A is a monocyclic carbocycle, monocyclic heterocycle, or bicyclic heterocycle;
- each RA is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- L1 is —X1-L2-, or -L2-X1—;
- X1 is absent, —O—, —S—, —S(═O)—, —S(═O)2—, —S(═O)2NR10—, —CH2—, —CH═CH—, —C≡C—, —C(═O)—, —C(═O)O—, —OC(═O)—, —OC(═O)O—, —C(═O)NR10—, —NR10C(═O)—, —OC(═O)NR10—, —NR10C(═O)O—, —NR10C(═O)NR10—, —NR10S(═O)2—, or —NR10—;
- L2 is absent or substituted or unsubstituted C1-C4alkylene;
- ring C is monocyclic carbocycle, bicyclic carbocycle, monocyclic heterocycle, or bicyclic heterocycle;
- each RC is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —NO2, —N(R10)2, —S(═O)2R11, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted phenyl and substituted or unsubstituted monocyclic heteroaryl;
- ring B is a monocyclic carbocycle, bicyclic carbocycle, monocyclic heterocycle or bicyclic heterocycle;
- each RB is independently selected from H, D, halogen, —CN, —OH, —OR10, —SR10, —S(═O)R11, —S(═O)2R11, —N(R10)2, —NHS(═O)2R11, —S(═O)2N(R10)2, —C(═O)R11, —OC(═O)R11, —CO2R10, —OCO2R11, —C(═O)N(R10)2, —OC(═O)N(R10)2, —NR10C(═O)N(R10)2, —NR10C(═O)R11, —NR10C(═O)OR11, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C2-C6alkynyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl;
- R5 and R7 are each independently selected from H, D, C1-C4alkyl and C3-C6cycloalkyl;
- or R5 and R7 are taken together with the intervening atoms to form a double bond;
- or R5 and R7 are taken together with the intervening atoms to form an epoxide or an substituted or unsubstituted C3-C6cycloalkyl;
- R6 and R8 are each independently selected from H, D, C1-C4alkyl or C3-C6cycloalkyl;
- Y is —CH2OR9, —C(═O)OR9, —CH2C(═O)OR9,
- each R9 is independently selected from H, substituted or unsubstituted C2-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C6alkenyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, and substituted or substituted or unsubstituted heterocycle;
- each R10 is independently selected from H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- or two R10 on the same N atom are taken together with the N atom to which they are attached to form a N-containing heterocycle;
- each R11 is independently selected from substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C3-C6cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted monocyclic heteroaryl, and substituted or unsubstituted benzyl;
- m is 0, 1, or 2;
- n is 0, 1, or 2;
- p is 0, 1, 2, 3, or 4.
A compound selected from the group consisting of:
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)pivalamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)butyramido)phenyl)acrylate;
- (E)-Methyl 3-(3-(((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)(ethoxycarbonyl)amino)phenyl)acrylate;
- (E)-Methyl 3-(3-(4-cyano-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)benzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)tetrahydro-2H-pyran-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)oxetane-3-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-3,3-dimethylbutanamido)phenyl)acrylate;
- (E)-Methyl 3-(3-((1r,4r)-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-methoxycyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-((1s,4s)-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-methoxycyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-methoxybenzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cycloheptanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)adamantane-1-carboxamido)phenyl)acrylate;
- (E)-methyl 3-(3-(N-(4-cyclohexylbenzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-3,4-difluorobenzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-fluorobenzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-1-methylcyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-5-fluorophenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)bicyclo[2.2.1]heptane-2-carboxamido)-5-fluorophenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-methyltetrahydro-2H-pyran-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-2-methoxybenzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-1,1-dioxidotetrahydro-2H-thiopyran-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)tetrahydro-2H-thiopyran-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-3-methoxybenzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-1-(methylsulfonyl)azetidine-3-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-(2-morpholinoethoxy)benzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-(methylthio)cyclohexanecarboxamido)phenyl)acrylate;
- cis-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-(methylsulfonyl)cyclohexanecarboxamido)phenyl)acrylate;
- trans-(E)-methyl 3 -(3 -(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-(methylsulfonyl)cyclohexanecarboxamido)phenyl)acrylate;
- trans-4-(((4′-(Dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)(3-((E)-3-methoxy-3-oxoprop-1-en-1-yl)phenyl)carbamoyl)cyclohexanecarboxylic acid;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-6-oxopiperidine-3-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-2-oxopiperidine-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-1-oxidotetrahydro-2H-thiopyran-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-(methylsulfinyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-hydroxybenzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-(2-hydroxyethoxy)benzamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-3-hydroxy-2,2-dimethylpropanamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(3-chloro-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-2,2-dimethylpropanamido)phenyl)acrylate;
- trans-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-2-hydroxycyclohexanecarboxamido)phenyl)acrylate;
- cis-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-2-hydroxycyclohexanecarboxamido)phenyl)acrylate;
- cis-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-3-hydroxycyclohexanecarboxamido)phenyl)acrylate;
- trans-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-3-hydroxycyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclopentanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclobutanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)amino)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-oxocyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)tetrahydro-2H-pyran-2-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-1,4-dioxane-2-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)tetrahydro-2H-pyran-3-carboxamido)phenyl)acrylate;
- cis-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-hydroxycyclohexanecarboxamido)phenyl)acrylate;
- trans-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-hydroxycyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-3′-methyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2′-methyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(pyridin-4-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-cyano-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-cyano-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-fluoro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-fluoro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2′-fluoro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(1-methyl-1H-pyrazol-4-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(pyridin-3-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-(trifluoromethoxy)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(3,5-dimethylisoxazol-4-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-isopropoxy-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2′-fluoro-4′-methoxy-[1,1′-biphenyl]-4-y1)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-chloro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(6-(dimethylamino)pyridin-3-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-5-methylphenyl)acrylate;
- (E)-Methyl 3-(5-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-2-methylphenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-2-methylphenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-4-methylphenyl)acrylate;
- Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)propanoate;
- (E)-N-((4′-(Dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-N-(3-(3-methoxyprop-1-en-1-yl)phenyl)cyclohexanecarboxamide;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)but-2-enoate;
- (E)-Methyl 3-(3-(N-(1-(4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)ethyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-isopropyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(pyrrolidin-1-yl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(1H-indazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-methyl 3-(3-(N-((4′-(dimethylamino)-2-fluoro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-methyl 3-(3-(N-((4′-(dimethylamino)-3-fluoro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-methoxy-3′-methyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-2-methyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-3-methyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-hydroxy-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2′-hydroxy-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-hydroxy-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-methoxy-4′-methyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2′,6′-difluoro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-((tert-butoxycarbonyl)(methyl)amino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(methylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(1-methyl-1H-indol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-methoxy-3′-methyl-[1,1′-biphenyl]-4-yl)methyl)isonicotinamido)phenyl)acrylate;
- (E)-Methyl 4′-((N-(3-(3-methoxy-3-oxoprop-1-en-1-yl)phenyl)cyclohexanecarboxamido)methyl)-[1,1′-biphenyl]-3-carboxylate;
- (E)-Methyl 4′-((N-(3-(3-methoxy-3-oxoprop-1-en-1-yl)phenyl)cyclohexanecarboxamido)methyl)-[1,1′-biphenyl]-4-carboxylate;
- (E)-Methyl 3-(3-(N-((4′-(methylsulfonyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-tert-Butyl 4-(((4′-methoxy-3′-methyl-[1,1′-biphenyl]-4-yl)methyl)(3-(3-methoxy-3-oxoprop-1-en-1-yl)phenyl)carbamoyl)piperidine-1-carboxylate;
- (E)-Methyl 3-(3-(N-((3′-(hydroxymethyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(hydroxymethyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-(methylsulfonyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d][1,3]dioxol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-chloro-4′-methoxy-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2-cyano-4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3-cyano-4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-2-ethyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-3-ethyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-methoxy-3′-methyl-[1,1′-biphenyl]-4-yl)methyl)piperidine-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(1-acetyl-N-((4′-methoxy-3′-methyl-[1,1′-biphenyl]-4-yl)methyl)piperidine-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-methoxy-3′-methyl-[1,1′-biphenyl]-4-yl)methyl)-1-(methylsulfonyl)piperidine-4-carboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)-2-methylacrylate;
- (E)-Methyl 3-(3-(N-((3′-cyano-4′-methoxy-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(pyridin-2-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2′-cyano-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(thiazol-2-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(thiazol-4-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(thiazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-isopropyl-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(prop-1-en-2-yl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-cyano-4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-3′-fluoro-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-methyl 3-(3-(N-((4′-(dimethylamino)-3′-methoxy-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(1-methyl-1H-benzo[d][1,2,3]triazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(azetidin-1-yl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(2-(dimethylamino)pyrimidin-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(5-(dimethylamino)pyrazin-2-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(6-(dimethylamino)pyridazin-3-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(N-methylmethylsulfonamido)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-fluoro-4′-(methylsulfonyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((2′-fluoro-4′-(methylsulfonyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]thiazol-6-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((3′-chloro-4′-(methylsulfonyl)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]oxazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]oxazol-6-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]isoxazol-6-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]thiazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]isoxazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]isothiazol-6-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzo[d]isothiazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(3-fluoro-1-methyl-1H-indazol-5-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(3-methylbenzo[d]isothiazol-6-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(4-methylpiperazin-1-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-morpholinobenzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(piperidin-1-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(piperazin-1-yl)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(naphthalen-1-ylmethyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-([1,1′-biphenyl]-2-ylmethyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-([1,1′-biphenyl]-3-ylmethyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-iso-Propyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Ethyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-5-ethylphenyl)acrylate;
- (E)-2-Hydroxyethyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Cyclohexyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Isobutyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-2-Methoxyethyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-2-(Dimethylamino)ethyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-(Tetrahydrofuran-2-yl)methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-2,2,2-Trifluoroethyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Benzyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-5-methoxyphenyl)acrylate;
- (E)-Methyl 3-(3-cyano-5-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-chloro-5-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-5-(trifluoromethyl)phenyl)acrylate;
- Methyl 3-(3-(N-((4′-(Dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)propiolate;
- (E)-3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylic acid;
- (E)-3-(3-((1s,4s)-N-((4′-(Dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-hydroxycyclohexanecarboxamido)phenyl)acrylic acid;
- Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-5-methylphenyl)propanoate;
- Methyl 3-(5-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-2-methylphenyl)propanoate;
- Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-2-methylphenyl)propanoate;
- Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)-4-methylphenyl)propanoate;
- Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)butanoate;
- Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)-2-methylpropanoate;
- (E)-Methyl 3-(3-(trans-4-((tert-butoxycarbonyl)amino)-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(trans-4-amino-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3 -(trans-N 4(4′ -(di methylamino)-[1,1′-biphenyl]-4-yl)methyl)-4- ((methoxycarbonyl)amino)cyclohexanecarboxamido)phenyl)acrylate;
- trans-(E)-Methyl 3-(3-(4-acetamido-N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate;
- trans-(E)-Methyl 3-(3-(N-((4′-(dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-4-(methylsulfonamido)cyclohexanecarboxamido)phenyl)acrylate;
- N-((4′-(Dimethylamino)-[1,1′-biphenyl]-4-yl)methyl)-N-(3-(3-methylbut-2-en-1-yl)phenyl)cyclohexanecarboxamide;
- (E)-Methyl 3-(3-(N-(4-benzamidobenzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(N-methylbenzamido)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzylamino)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- (E)-Methyl 3-(3-(N-(4-(benzyl(methyl)amino)benzyl)cyclohexanecarboxamido)phenyl)acrylate;
- or a pharmaceutically acceptable salt, or solvate thereof.
Dependencies are inferred from the claim text.