Inhibitors of cyp 17
AssigneeNovartis AG
InventorsMark Gary BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
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Abstract
The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17α-hydroxylase/C17,20-lyase inhibitors.
Claims17
A method for treating prostate cancer in a subject in need of such treatment comprising the step of administering a compound of Formula (Ib)
- wherein:
- n is 1;
- R53 is
- (i) a phenyl optionally substituted with 1 to 2 substituents each independently selected from fluoro, chloro, methyl, methoxy, trifluoromethyl, difluoromethyl, or cyano;
- (ii) a biphenyl;
- (iii) a fused phenyl selected from naphthalen-2-yl, quinolin-6-yl, 3,4-dihydro-2-oxo-quinolin-6-yl, benzo[b]thiophen-5-yl, benzo[d]isoxazol-5-yl, 1H-indazol-6-yl, 1H-indazol-5-yl, benzothiazol-6-yl, 1,2-dihydro-3-oxo-indazol-6-yl, indan-5-yl, 1H-benzotriazol-5-yl, benzofuran-5-yl, 2,3-dihydro-benzo[1,4]dioxin-6-yl, 2,3-dihydro-benzofuran-5-yl, or benzo[1,3]dioxol-5-yl where said fused phenyl is optionally substituted with 1 to 2 substituents each independently selected from chloro, fluoro, methyl, ethyl, difluoromethyl, trifluoromethyl, cyclopropyl, cyano, or amino;
- (iv) a 5- to 6-membered heteroaryl selected from isothiazol-4-yl, thiophen-2-yl, thiophen-3-yl, or pyridin-4-yl, where said isothiazol-4-yl, said thiophen-2-yl, said thiophen-3-yl, and said pyridin-4-yl are optionally substituted with fluoro, chloro, methyl, trifluoromethyl, difluoromethyl, or methoxy;
- or
- (v) a fused heteroaryl selected from thieno[3,2-c]pyridin-2-yl, thieno[3,2-c]pyridin-3-yl, thieno[3,2-c]pyridin-2-yl, imidazo[1,2-a]pyridin-7-yl, or benzo[b]thiophen-2-yl, where said fused heteroaryl is optionally substituted with 1 to 2 substituents each independently selected from fluoro, chloro, methyl, difluoromethyl, trifluoromethyl, cyclopropyl, or amino;
- R54 is (C1-C4)alkyl, halo-substituted (C1-C4)alkyl, or —CH2OH, or two R54 taken together with the carbon atom(s) to which they are attached form a 3- to 6-membered fully or partially saturated carbocyclic ring;
- p is 0,1,2, or 3;
- R50, R51 and R52 are each independently H, halo, —OH, —CN, (C1-C4)alkyl, halo-substituted (C1-C4)alkyl, hydroxy-substituted (C1-C4)alkyl, —(CH2)r—O(C1-C4)alkyl, —(CH2)r—CH(O(C1-C4)alkyl)2, —NH2, —NH(C1-C4)alkyl, —N((C1-C4)alkyl)2, —NHC(O)—(C1-C4)alkyl, —C(O)NH2, —C(O)—NH(C1-C4)alkyl, —C(O)—N((C1-C4)alkyl)2, or —C(O)—O(C1-C4)alkyl;
- r is 0, 1 or 2;
- with the proviso that when R50, R51, and R52 are H and R53 is phenyl, R53 is not unsubstituted or substituted with halogen or CF3;
- or a pharmaceutically acceptable salt thereof.
A method for treating prostate cancer in a subject in need of such treatment comprising the step of administering 1-(2-Chloro-pyridin-4-yl)-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one having the structure:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.