N-PIPERIDIN-4-YL DERIVATIVES

摘要

The invention relates to a N-piperidin-4-yl derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same and to the use of said N-piperidin-4-yl derivatives for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, or for the treatment of uterine fibroids or other menstrual-related disorders.;

主权项

1. A N-piperidin-4-yl derivative having the general Formula I wherein W is C(O)NH or NH(CO); Y is CHR3 or a bond; X is N, CH, CF or CR8; A is a (hetero)aromatic group selected from R1 is H, halogen, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy or halo(C1-4)alkyloxy; R2 is H, halogen, di(C1-4 alkylamino, (C1-4)alkyl, (C2-4)alkenyl, (C2-4)alkynyl, halo(C1-4)alkyl or (C1-6)alkyloxy, optionally substituted with one or more halogens, hydroxy or (C1-4)alkyloxy; or R2 is OCH2R7; R3 is H, (C1-3)alkyl or COOR8; R4 is H, halogen or (C1-3)alkyl; or R4 forms together with R3 and the carbon atoms to which they are bonded a (C3-5)cycloalkyl group; R5 is, halogen, (C1-4)alkyl, halo(C1-4)alkyl, hydroxy(C1-4)alkyl, CN, COOH, CONR9,R10, pyridyl or a 5-membered heteroaryl group comprising 1, 2 or 3 nitrogen atoms and optionally an oxygen or a sulfur atom; R6 is H, hydroxy or halogen; or R6 forms together with R5 and the carbon atoms to which they are bonded a ‘fused 5-membered heteroaryl group comprising 1 or 2 nitrogen atoms and optionally an oxygen or a sulfur atom; R7 is vinyl, ethynyl, cyano, (C3-6)cycloalkyl, CONR11,R12 CH2NR13R14, phenyl or a 5 or 6-membered heteroaryl group comprising 1-3 heteroatoms selected from O, N and S; each R8 is independently (C1-3)alkyl; R9 is H or (C1-6)alkyl, optionally substituted with 1-3 halogens, hydroxyl or COOR8; R10 is H, (C1-3)alkyl or a 5-membered heteroaryl group comprising 1-3 heteroatoms selected from N, S and O; or R9 and R10 form together with the nitrogen atom to which they are bonded a saturated 5-7 membered ring; R11, R12, R13 and R14 are independently selected from H or (C1-3)alkyl; or a pharmaceutically acceptable salt thereof.