New amide compounds used for therapy and/or prophylaxis of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy

摘要

Amide compounds (I), are new. Amide compounds of formula (I), are new. q : 0 or 1; R 1mono or bicyclic 6-12C aryl, 5-12 membered hetero aryl, 3-10C cycloalkyl, or 3-10 membered hetero cycloalkyl residue, which is unsubstituted or substituted up to 3 residue, where the substituents are 1-8C alkyl, 2-8C alkenyl, 2-8C alkynyl, partialy or completely fluorinated 1-6C alkyl or alkoxy, 1-6 alkoxy-1-6C alkyl, 1-6C aIkoxy-1-6C alkoxy, -(CH 2) pC 3-C 10 cycloaIkyl, -(CH2) pheterocycIo alkyl, -(CH 2) pCN, -(CH 2) pHaI, -(CH 2) pNO 2, (CH 2) pC 6-C 12aryl with Z substituent, -(CH 2) p-heteroaryl with Z substituent, -(CH 2) pPO3(R 4) 2, -(CH 2) pNR 5R 6, -(CH 2) pNR 7COR 4, -(CH 2) pNR 7CSR 4, -(CH 2) pNR 7S(O)R 4, -(CH 2) pNR 7S(O) 2R 4, -(CH 2) pNR 7CONR 5R 6, -(CH 2) pNR 7COOR 4-(CH 2) pNR 7C(NH)NR 5R 6, -(CH 2) pNR 7CSNR 5R 6-(CH 2) pNR 7S(O)NR 5R 6, -(CH 2) pNR 7S(O)2NR 5R 6, -(CH 2) pCOR 4, -(CH 2) pCSR 4, -(CH 2) pS(O)R 4, -(CH 2) pS(O)(NH)R 4, -(CH 2) pS(O) 2R 4, -(CH 2) pS(O) 2NR 5R 6, -(CH 2) pSO 2OR 4, -(CH 2) pCO 2R 4, -(CH 2) pCONR 5R 6, -(CH 2) pCSNR 5R 6, -(CH 2) pOR 4, -(CH 2) pSR 4, -(CH 2) pCR 4(OH)-R 4, -(CH 2) pC=NOR 4, -O-(CH 2) n-O-, -O-(CH 2) n-CH2-, -O-CH=CH- or -(CH 2) n+2 -, where n=1 or 2; p : 1,2,3,4,5 or 6; Z : cyano, halogen, nitro, -(CH 2) pOR 4, -(CH 2)S(O) 2R 4, -C(O)R 4, -CO 2R 4, -O-R 4, -S-R 4, -SO 2NR 5R 6, -C(O)-NR 5R 6, -OC(O)-NR 5R 6, -C=NOR 4, -NR 5R 6or partially or completely fluorinated 1-6C alkyl or alkoxy; R 4H, 1-6C alkyl, 1-3C hydroxy alkyl, 1-3C alkoxy-1-3C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C, cycloalkyl, 6-12C aryl or partialy or completely fluorinated 1-3C alkyl; R 5and R 6H, with W' substituent 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl, 6-12C aryl or a hydroxy group, where W'=NR 8R 9; R 8H or 1-3C alkyl; R 9H or 1-3C alkyl; R 5hydroxy group; R 6H, 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl or 6-12C aryl; R 7H, 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl or 6-12C aryl; R 2mono or bicyclic 6-12C aryl, 5-12 membered hetero aryl reidue, which is unsubstituted or substituted up to 3 residue as specified under R 1, preferably phenyl or naphthyl substituted derivatives; R 3a group of formula (i)-(xx); R 5a, R 5bH or alkyl optionally at least partially substituted by F, or R 5a+ R 6a+ attached atoms : 3-6 membered ring, and R 4aH or 1-4C alkyl optionally at least partially substituted by F. An independent claim is also included for a pharmaceutical composition which comprises compound (I), an additional active subsatance i.e. selective estrogen receptor modulator and a pharmaceutically acceptable carrier. [Image] [Image] [Image] [Image] ACTIVITY : Gynecological; Analgesic; Cytostatic. MECHANISM OF ACTION : Progesterone receptor modulators.