发明名称 ARALKOXY AND ARALKYLTHIO SUBSTITUTED AZACYCLIC COMPOUNDS AS TACHYKININ ANTAGONISTS
摘要 The present invention relates to compounds of formula (I) wherein n is 1, 2 or 3 and where any carbon atom of (CH2)n may be substituted by R4 and/or R5; X represents O or S; R1 represents (CH2)qphenyl, wherein q is 0, 1, 2 or 3, which may be optionally substituted in the phenyl ring; R2 represents aryl selected from phenyl and naphthyl; heteroaryl selected from indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl and quinolyl; benzhydryl; or benzyl; wherein each aryl or heteroaryl moiety may be substituted; R4 and R5 each independently represent H, halo, C1-6alkyl, oxo, CO2Ra or CONRaRb; R6 represents H or C1-6alkyl; R7 represents trifluoromethyl, C2-6alkenyl, C37cycloalkyl, C3-7cycloalkylC1-4alkyl, (CH2)pNR9R10, CO2R16, CONR9R10, (CH2)pCO2R16, (CH2)pCONR9R10, (CH2)pNR9COR16, (CH2)pNHSO2R11, (CH2)pOR16, (CH2)pOC(O)R9 or (CH2)pOC1-4alkylCOR17 or C1-6alkyl substituted by a hydroxy group; R8 represents H, CORa, CO2Ra, COCONRaRb, COCO2Ra, C3-7cycloalkyl, C37cycloalkylC1-4alkyl, C1-6alkyl optionally substituted by a group selected from (CO2Ra, CONRaRb, hydroxy, cyano, CORa, NRaRb, C(NOH)NRaRb, CONHphenyl(C14alkyl), COCO2Ra, CONHNRaRb, C(S)NRaRb, CONRaC1-6alkylR12, CONR13C2-6alkynyl, CONR13C2-6alkenyl, COCONRaRb, CONRaC(NRb)NRaRb, CONRaheteroaryl, and optionally substituted phenyl or C1-6alkyl, optionally substituted by oxo, substituted by an optionally substituted aromatic heterocycle; Ra and Rb each independently represent H, C1-6alkyl, trifluoromethyl or phenyl optionally substituted by C1-6alkyl, halo or trifluoromethyl. The compounds are of particular use in the treatment of pain, inflammation, migraine and emesis.
申请公布号 CA2182734(A1) 申请公布日期 1995.08.17
申请号 CA19952182734 申请日期 1995.02.06
申请人 MERCK SHARP & DOHME LIMITED 发明人 BAKER, RAYMOND;MACLEOD, ANGUS MURRAY;SEWARD, EILEEN MARY;SWAIN, CHRISTOPHER JOHN
分类号 A61K31/4427;A61K31/445;A61K31/451;A61P1/00;A61P1/08;A61P9/00;A61P11/00;A61P25/04;A61P25/08;A61P25/18;A61P25/20;A61P25/24;A61P25/26;A61P25/28;A61P25/30;A61P29/00;A61P35/02;A61P37/00;A61P37/08;A61P43/00;C07D211/42;C07D211/54;C07D401/06;(IPC1-7):C07D211/42;C07D401/00;C07D403/00;C07D405/00;C07D409/00;C07D413/00;C07D417/00;C07D453/02;C07D205/04;C07D417/08;C07F7/10;C07D207/12;A61K31/395;A61K31/695 主分类号 A61K31/4427
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