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US 10,766,877 B2Granted
Melanocortin subtype-2 receptor (MC2R) antagonists and uses thereof
AssigneeCrinetics Pharmaceuticals, Inc.
InventorsSangdon Han, Yunfei Zhu, Sun Hee Kim, Jian Zhao
Life of this patent
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Abstract
Described herein are compounds that are melanocortin subtype-2 receptor (MC2R) modulators, 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 that would benefit from modulation of MC2R activity.
Claims20
A compound of Formula (IX), or a pharmaceutically acceptable salt, or solvate thereof:
- wherein:
- V is N;
- Ra is selected from the group consisting of hydrogen, halogen, —OR8, —CN, —N(R7)2, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C1-C6 fluoroalkyl, unsubstituted or substituted C1-C6 heteroalkyl, and unsubstituted or substituted C3-C6 cycloalkyl, wherein any substituted group of Ra is substituted with one or more R9 groups;
- Rb and Rc are each independently selected from the group consisting of hydrogen, halogen, —OR8, —CN, —N(R7)2, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C1-C6 fluoroalkyl, and unsubstituted or substituted C1-C6 heteroalkyl, wherein any substituted group of Rb and Rc is substituted with one or more R9 groups;
- RB is unsubstituted or substituted carbocycle, unsubstituted or substituted heterocycle, unsubstituted or substituted C1-C7 alkyl, unsubstituted or substituted C1-C7 fluoroalkyl, or unsubstituted or substituted C1-C6 heteroalkyl, wherein if RB is substituted then R8 is substituted with Rd, Re and Rf;
- Rd is selected from the group consisting of hydrogen, halogen, —OR8, —CN, —N(R7)2, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C1-C6 fluoroalkyl, unsubstituted or substituted C1-C6 heteroalkyl, unsubstituted or substituted C3-C6 cycloalkyl, unsubstituted or substituted C2-C7 heterocycloalkyl, unsubstituted or substituted phenyl, and or unsubstituted or substituted monocyclic heteroaryl, wherein any substituted group of Rd is substituted with one or more R9 groups;
- Re and Rf are each independently selected from the group consisting of hydrogen, halogen, —OR8, —CN, —N(R7)2, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C1-C6 fluoroalkyl, and unsubstituted or substituted C1-C6 heteroalkyl, wherein any substituted group of Rd is substituted with one or more R9 groups;
- X1 is CR6;
- R2 and R3 are hydrogen;
- or R2 and R3 are taken together with the carbon atom to which they are attached to form —C(═O)—;
- R4 is selected from the group consisting of hydrogen, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted monocyclic carbocycle, unsubstituted or substituted monocyclic heterocycle, unsubstituted or substituted —(C1-C6 alkyl)-carbocycle, and unsubstituted or substituted —(C1-C6 alkyl)-heterocycle, wherein any substituted group of R4 is substituted with one or more halogen, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted monocyclic heterocycle, —N(R7)2, —CN, —CO2R8, —C(═O)N(R7)2, —SR8, —S(═O)R10, —S(═O)2R10, —NR7C(═O)R8, —NR7SO2R10, —SO2R10, or —SO2N(R7)2;
- R6 is H or F;
- each R7 is independently selected from the group consisting of hydrogen, substituted C1-C6 alkyl, unsubstituted or substituted C3-C6 cycloalkyl, unsubstituted or substituted C1-C6fluoroalkyl, unsubstituted or substituted aryl, and unsubstituted or substituted heteroaryl;
- or two R7 are taken together with the nitrogen atom to which they are attached to form an unsubstituted or substituted 3- to 6-membered monocyclic heterocycle;
- each R8 is independently selected from the group consisting of hydrogen, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C3-C6 cycloalkyl, unsubstituted or substituted C1-C6fluoroalkyl, unsubstituted or substituted aryl, and unsubstituted or substituted heteroaryl;
- each R9 is independently hydrogen, halogen, unsubstituted or substituted C1-C4alkyl, unsubstituted or substituted C1-C4alkoxy, unsubstituted or substituted C1-C4fluoroalkyl, unsubstituted or substituted C1-C4fluoroalkoxy, unsubstituted or substituted monocyclic carbocycle, unsubstituted or substituted monocyclic heterocycle, —CN, —OH, —CO2R8, —CH2CO2R8, —C(═O)N(R7)2, —C(═O)N(R7)01e, —CH2C(═O)N(R7)2, —N(R7)2, —CH2N(R7)2, —C(R8)2N(R7)2, —NR7C(═O)R8, —CH2NR7C(═O)R8, —NR7C(═O)N(R7)2, —NR7C(═O)N(R7)2, C(R8)═N(R7)—OR8, —SR8, —S(═O)R10, —SO21110, or —SO2N(R7)2;
- and
- each R10 is independently selected from the group consisting unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C3-C6 cycloalkyl, unsubstituted or substituted C1-C6fluoroalkyl, unsubstituted or substituted phenyl, and unsubstituted or substituted heteroaryl.
15 more elements
Dependencies are inferred from the claim text.