New amide compounds used for treatment of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy, has general formula
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Abstract
Amide compounds (I), are new. Amide compounds of formula (I), are new. A : H, Z substituted 1-8C-alkyl, 2-8C-alkenyl, 2-8C alkinyl, M substituted 3-10C-cycloalkyl, 3-12-membered heterocycloalkyl residue, where Z is cyano, halogen, hydroxy, nitro, -C(O)R 8>, CO 2R 8>, -O-R 8>, -S-R 8>, SO 2NR 5>R 6>, -C(O)-NR 5>R 6>, -OC(O)-NR 5>R 6>, -C=NOR 8>, -NR 5>R 6>, -PO 3(R 8>) 2, -NR 7>COR 8>, -NR 7>CSR 8>, -NR 7>S(O)R 8>, -NR 7>S(O) 2R 8>, -NR 7>CONR 5>R 6>, -NR 7>COOR 8>,-NR 7>C(NH)NR 5>R 6>, -NR 7>CSNR 5>R 6>, -NR 7>S(O)NR 5>R 6>, -NR 7>S(O) 2NR 5>R 6>, -S(O)R 8>,-S(O)NR 5>R 6>, -S(O) 2R 8>, -SO 2OR 8>, -CSNR 5>R 6>, -CR 8>(OH)-R 8> and M is 1-6C-alkyl or - COR 8> , CO 2R 8> , -0-R 8> , or -NR 5>R 6> group, where R 8> is hydrogen or 1-6C-aKyl, 2-8C-alkenyl, 2-8C-alkinyl, 3-10C-cycloalkyl, 6-12C-aryl or a partially or completely fluorinated 1-3C-alkyl residue and R 5> and R 6> are independently of each other, a hydrogen, 1-6C-alkyl, 2-6C-alkenyl, 2-8C-alkinyl, 3-10C-cycloalkyl, 6-12C-aryl residue, or a hydroxy group, and R 7> is a hydrogen, 1-6C-aIkYl, 2-8C-alkenyl and , alkinyl, 3-10C-cycloalkyl or a 6-12C aryl R 1>,R 2>independently an unbranched or branched 1-5C-alkyl group or form a 3-7 members ring with the C-atom, R 3>H, K substituted 1-8C-alkyl, 2-8C-alkenyl, 2-8C-alkinyl, 3-10C-cycloalkyl, 3-12-member heterocycloalkyl residue with L substituted, mono or bicyclic 6-12C-aryl or 3-12-member heterocycloalkyl residue, where K is cyano, halogen, hydroxy, nitro, - C(O)R 4> , CO 2R 4>, -O-R 4>,-S-R 4>, SO 2NR 5>R 6>,- C(O)-NR 5>R 6>, -OC(O)-NR 5>R 6>, -C=NOR 4>,-NR 5>R 6>, where L is 1-8C alkyl, 2-8C akenyl, partially or completely fluorinated 1-6C alkyl, 1-6C alkoxy, 1-6 alkoxy-1-6C alkyl, 1-6C alkoxy-1-6C alkoxy, mono or bicyclic (CH 2) pC 3-C 10 cycloalkyl, mono or bicyclic 3-12 membered (CH 2) p heterocyclo alkyl residue, (CH 2) pCN, (CH 2) pC 6-C 12 aryl residue, (CH 2) p-heteroaryl residue,-O-CH=CH- or (CH 2) n+2, where n is 1 or 2, p=0,1,2,3,4,5 or 6 X : an oxygen or two hydrogen atoms Y : (CH 2) m, -CH=CH, where m is 0 or 1 R 4unsubtituted or substituted up to 1-3 residue, mono or bicyclic 3-12 membered aromatic or hetero aromatic residue or bicyclic compound having general formulae (II) or (III). An independent claim is also included for a pharmaceutical composition which comprises compound (I), an additional active substance i.e. selective estrogen receptor modulator and a pharmaceutically acceptable carrier. [Image] [Image] - ACTIVITY : Gynecological Analgesic Cytostatic. - MECHANISM OF ACTION : None given.
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