FSH receptor antagonists
AssigneeMerck Sharp & Dohme Corp.
InventorsWesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
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Abstract
The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
Claims12
A compound according to Formula I
- or a pharmaceutically acceptable salt thereof, wherein
- X is C(R10) or N;
- Y is N;
- R3 is phenyl, (2-8C)heteroaryl, benzoyl, (2-8C)heteroarylcarbonyl, the phenyl or heteroaryl moieties of which may optionally be substituted with one or more substituents selected from R11, or
- R3 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-6C)cycloalkyl, (1-6C)alkylcarbonyl, (2-6C)alkenylcarbonyl, (2-6C)alkynylcarbonyl or (3-6C)cycloalkylcarbonyl;
- R7 and R8 are independently H or (1-4C)alkoxy;
- R9 is hydroxy or H, or
- R9 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-4C)alkoxy, (2-4C)alkenoxy, (3-6C)cycloalkyl, (3-6)cycloalkoxy, (3-6C)cycloalkyl(1-4C)alkoxy, (2-6C)heterocycloalkylcarbonyl, (di)[1-4C]alkylaminocarbonyl, (2-6C)heterocycloalkyl, the alkyl or (hetero)cycloalkyl moieties of which may optionally be substituted with one or more substituents selected from R12 or,
- R9 is (2-8C)heteroaryl, phenyl, phenyl(1-4C)alkoxy, (2-8C)heteroaryl(1-4C)alkoxy, the phenyl or heteroaryl moieties of which may optionally be substituted with one or more substituents selected from R16;
- R10 is H or (1-4C)alkoxy;
- R11 is hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (1-4C)alkyl, (1-4C)alkoxy or (di)[1-4C)alkyl]amino;
- R12 is hydroxy, amino, halogen, cyano, (1-4C)alkoxy or (di)[1-4C)alkyl]amino;
- R13 and R14 are independently H or (1-3C)alkyl;
- R15 is H, (1-3C)alkyl, or
- R14 and R15 may be joined in a (3-6C)cycloalkyl ring;
- and
- R16 is hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (1-4C)alkyl, (1-4C)alkoxy or (di)[1-4C)alkyl]amino.
Dependencies are inferred from the claim text.