发明名称 New cyclic peroxisome proliferator activated receptor activators, used to prevent or treat dyslipidemia, atherosclerosis and diabetes
摘要 New cyclic compounds and their salts are new. Cyclic compounds are of formula (I): X, Y = CH2, O, S o NRa; R = H, 1-7C alkyl, phthalamido-(1-7C) alkyl, 3-12C cycloalkyl, (CH2)pCOORb or 6-10C aryl or 3-10-membered heterocycle comprising 1-4 endocyclic heteroatoms of O, S and N (both optionally substituted by one or more of Z or 1-7C alkylene), 6-10C aryl-(1-7C) alkyl; R1 = H, 1-7C alkyl, 1-7C hydroxyalkyl, 6-10C aryl (optionally substituted by one or more of W), P(O)(OR8)(OR9), (CH2)tCOORc or CONR10R11; R2, R3 = H, 1-7C alkyl, 3-12C cycloalkyl, 6-10C aryl, 6-10C aryl-(1-7C) alkyl, 3-10-membered heterocycle comprising 1-4 endocyclic heteroatoms of O, S and N or fluorenyl (aryl, heterocycle and fluorenyl optionally substituted by one or more of Z or 1-7C alkylene) or, together, R2 and R3 form (CH2)r1 or group of formula (a); and R4-R7 = H, 1-7C alkyl or 6-10C aryl or 3-10-membered heterocycle comprising 1-4 endocyclic heteroatoms of O, S and N (optionally substituted by one or more of Z), provided that: (i) when R2, R3, R5 and R7 = H, X, Y = O, R4 = CH3 and R6 = H or CH3, then R1 and R, together with the C to which they are attached, do not form C(CH3)(COOCH3), C(CH3)(CH2OH), C(C6H5)(COOCH3) or C(C6H5)(CH2OH); and (ii) when R4-R7 = H, X, Y = O and R = pyridyl or optionally substituted piperidyl, then R1 is not optionally substituted phenyl. An Independent claim is also included for intermediate diols chosen from 2,2-bis-(4-fluorophenyl)propane-1,3-diol, 2,2-bis(3-trifluoromethylphenyl)propane-1,3-diol, 5-hydroxymethyl-5H-dibenzo(a,d)cyclohepten-5-ylmethanol and (9-hydroxymethyl-9H-xanthen-9-yl)methanol.
申请公布号 FR2781222(A1) 申请公布日期 2000.01.21
申请号 FR19980009164 申请日期 1998.07.17
申请人 LIPHA LYONNAISE INDUSTRIELLE PHARMACEUTIQUE 发明人 BERTHELON JEAN JACQUES;GUERRIER DANIEL;RASPE ERIC;ZEILLER JEAN JACQUES
分类号 A61K31/357;A61K31/381;A61K31/4035;A61K31/443;A61K31/4433;A61K31/453;A61P3/06;A61P3/10;A61P9/10;C07C33/36;C07C33/46;C07D311/82;C07D319/06;C07D319/08;C07D405/06;C07D407/04;C07D409/04;C07D493/10 主分类号 A61K31/357
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