New amide compounds used for therapy and/or prophylaxis of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy
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New amide compounds act as progesterone receptor modulators with gynecological analgesic and cytostatic activity for the therapy or prophylaxis of endometriosis, female fertility control, and hormone replacement therapy.
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Abstract
Amide compounds (I), are new. Amide compounds of formula (I), are new. q : 0 or 1 R 1>mono 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) p heterocycIo alkyl, -(CH 2) pCN, -(CH 2) pHaI, -(CH 2) pNO 2, (CH 2) pC 6-C 12 aryl with Z substituent, -(CH 2) p-heteroaryl with Z substituent, -(CH 2) pPO3(R 4>) 2, -(CH 2) pNR 5>R 6>, -(CH 2) pNR 7>COR 4>, -(CH 2) pNR 7>CSR 4>, -(CH 2) pNR 7>S(O)R 4>, -(CH 2) pNR 7>S(O) 2R 4>, -(CH 2) pNR 7>CONR 5>R 6>, -(CH 2) pNR 7>COOR 4> -(CH 2) pNR 7>C(NH)NR 5>R 6>, -(CH 2) pNR 7>CSNR 5>R 6> -(CH 2) pNR 7>S(O)NR 5>R 6>, -(CH 2) pNR 7>S(O)2NR 5>R 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 5>R 6>, -(CH 2) pSO 2OR 4>, -(CH 2) pCO 2R 4>, -(CH 2) pCONR 5>R 6>, -(CH 2) pCSNR 5>R 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 5>R 6>, -C(O)-NR 5>R 6>, -OC(O)-NR 5>R 6>, -C=NOR 4>, -NR 5>R 6> or partially or completely fluorinated 1-6C alkyl or alkoxy R 4>H, 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 5> and R 6>H, 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 8>R 9> R 8>H or 1-3C alkyl R 9>H or 1-3C alkyl R 5>hydroxy group R 6>H, 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl or 6-12C aryl R 7>H, 1-6C alkyl, 2-8C alkenyl, 2-8C alkynyl, 3-10C cycloalkyl or 6-12C aryl R 2>mono 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 3>a group of formula (i)-(xx) R 5a>, R 5b>H or alkyl optionally at least partially substituted by F, or R 5a> + R 6a> + attached atoms : 3-6 membered ring, and R 4a>H 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.
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- last seen: 2026-08-11T06:11:44.160905+00:00