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US 7,678,781 B2Granted
11-phosphorous steroid derivatives useful as progesterone receptor modulators
AssigneeJanssen Pharmaceutica NV
InventorsJames J. Fiordeliso, Weiqin Jiang, Zhihua Sui
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Abstract
The present invention is directed to novel 11-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.
Claims10
A compound of formula (I)
- wherein
- n is an integer from 0 to 3;
- R0 is selected from the group consisting of hydroxy, halogen, C1-3alkyl, C1-3alkoxy, cyano, nitro, amino, (C 1-4alkylamino) and di(C 1-4alkyl)amino;
- X is selected from the group consisting of O and S;
- R1 and R2 are each independently selected from the group consisting of hydroxy, C1-4alkyl, —CH(—O—C1-4alkyl)2, C1-4alkoxy, halogenated C1-4alkyl, halogenated C1-4alkoxy, phenyl, —O-phenyl, —O-aralkyl and NR5R6;
- wherein the phenyl, whether alone or as part of a substituent group, is optionally substituted with one or more substituents independently selected from hydroxy, carboxy, halogen, C1-3alkyl, C1-3alkoxy, cyano, nitro, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
- wherein R5 and R6 are each independently selected from the group consisting of hydrogen and C1-4alkyl;
- alternatively, R5 and R6 are taken together with the nitrogen atom to which they are bound to form a 5- to 7- membered saturated or partially unsaturated nitrogen containing heterocyclyl ring;
- wherein the nitrogen containing heterocyclyl ring is optionally substituted with one or more substituents independently selected from hydroxy, carboxy, C1-4alkyl, C1-4alkoxy, nitro, cyano, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
- alternatively, R1 and R2 are taken together with the phoshorous atom to which they are bound to form a 5- to 7- membered saturated phosphorous containing heterocyclyl ring;
- wherein the phosphorous containing heterocyclyl ring is optionally substituted with one or more substituents independently selected from hydroxy, carboxy, C1-4alkyl, C1-4alkoxy, nitro, cyano, amino, (C1-4alkylamino) and di(C1-4alkyl)amino;
- R3 is selected from the group consisting of—OH and —O—C(O)—C1-4alkyl, —O—C1-4alkyl and —O-benzyl;
- R4 is selected from the group consisting of hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, —C1-4alkyl-CN, halogenated C1-4alkyl, —C1-4alkyl-phenyl, —C2-4alkenyl-phenyl and —C2-4alkynyl-phenyl;
- alternatively, R3 and R4 are taken together with the carbon atom to which they are bound to form C(═O) or a 5- to 7-membered oxygen containing, saturated or partially unsaturated ring structure;
- wherein the oxygen containing ring structure is further optionally substituted with one or more substituents independently selected from the group consisting of hydroxy, carboxy, C1-4alkyl,C1-4alkoxy, ═CH2, nitro, cyano, amino, (C1-4alkylamino) and di(C 1-4alkyl)amino;
- or a pharmaceutically acceptable salt, ester or prodrug thereof.
13 more elements
Dependencies are inferred from the claim text.