Estrogen receptor ligands
AssigneeKaro Bio AB
InventorsLars Hagberg, Sandra Gordon, Aiping Cheng, Theresa Apelqvist, Patrik Rhönnstad, Mattias Wennerstål
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Abstract
The invention provides a compound of formula(I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula(I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined in the specification.
Claims11
A compound of formula(I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt,
- wherein R1 is selected from the group consisting of halogen, cyano, nitro, ORA, N(RB)2, —C(O)C1-4alkyl, —SO2C1-4alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, dihaloC1-6alkyl, trihaloC1-6alkyl, haloC2-6alkenyl, dihaloC2-6alkenyl, trihaloC2-6alkenyl, cyanoC1-6alkyl, C1-4alkoxyC1-6 alkyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, phenyl, benzyl, and 5-10 membered heterocyclyl, wherein said phenyl, benzyl or heterocyclyl group can be either unsubstituted or substituted with from 1 to 3 substituents, each substituent being independently selected from the group consisting of ORA, halogen, cyano, nitro, —C(O)C1-4alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, dihaloC1-6alkyl and trihaloC1-6alkyl;
- R2 is selected from the group consisting of cyano, nitro, N(OH)2, —CHO, —CH═N—OH, —C(O)C1-4alkyl optionally substituted with from 1 to 3 halogens, —SO2C1-4alkyl, —C(O)NH—OH, —C(NH2)═N—OH, —C(CO2H)═N—OH, —C(NH2)═NH, —C(NH2)═N—NH2, —NH—C(NH2)═NH, —NH—C(O) NH2, —N═C(—NH—CH2CH2—NH—), —S—CN, —S—C(NH2)═NH, —S—C(NH2)═N—OH, —CO2H, —CH(OH) CO2H, —C(O)N(RC) 2, —SO2C1-6alkyl, SO2N(RC)2, —C(O)—C(O)—NH2, —CH2NH—CONH2, —SO2ORC , —C(O)CO2H, —CH2SO3H and 5-10 membered heterocyclyl wherein said heterocyclyl group can be either unsubstituted or substituted with from 1 to 3 substituents each substituent being independently selected from the group consisting of ORA, halogen, cyano, nitro, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, dihaloC1-6alkyl and trihaloC1-6alkyl;
- each of R3, R4, R5, R6, R7, R8, R9 and R10 is independently selected from the group consisting of hydrogen, ORA, halogen, cyano, nitro, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, dihaloC1-6alkyl and trihaloC1-6alkyl;
- each RA is independently selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, phenyl, benzyl and 5-10 membered heterocyclyl, each optionally substituted by from 1 to 3 halogen atoms;
- and
- each RB is independently selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, phenyl, benzyl and 5-10 membered heterocyclyl, each optionally substituted by from 1 to 3 halogen atoms;
- and
- each RC is independently selected from the group consisting of hydrogen and C1-6alkyl.
Dependencies are inferred from the claim text.