发明名称 Heterocyclic carboxylic acid derivatives their preparation and use as endothelin receptor antagonists
摘要 Heterocyclic compounds of formula (I) and their salts are new. R1 = tetrazolyl, or COR; R = OR6, O(CH2)pS(O)kR7, NHS(O)2R8 or a 5-membered azaheteroaryl; R2 = 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl (all optionally substituted), H, halo, 1-4C alkoxy, 1-4C haloalkoxy, 3-6C alkenyloxy, 3-6C alkynyloxy, 1-4C alkylthio, 1-4C alkylcarbonyl, 1-4C alkoxycarbonyl, NH(1-4C alkyl), N(1-4C alkyl)2, OH, carboxy or amino; R3, R4 = phenyl, naphthyl or 3-8C cycloalkyl (all optionally substituted); or R3+R4 = two of phenyl, naphthyl linked at the o-position by a bond, methylene, ethylene, ethenyl, S, SO2, NH or N-alkyl; R5 = H, 1-8C alkyl, 3-8C alkenyl, 3-8C alkynyl, Ph, naphthyl, 5-6 membered heteroaromatic (containing 1-3 N, S and/or O), or 3-8C cycloalkyl (all optionally substituted); R6 = H, alkali metal or earth-alkali metal, organic ammonium, 3-8C cycloalkyl, 1-8C alkyl, or (all optionally substituted) benzyl, 3-8C alkenyl, 3-8C alkynyl or phenyl; R7 = 1-4C alkyl, 3-8C cycloalkyl, 3-8C alkenyl, 3-8C alkynyl or optionally substituted phenyl; R8 = 1-4C alkyl, 3-8C alkenyl, 3-8C alkynyl, 3-8C cycloalkyl (all optionally substituted by 1-4C alkoxy, 1-4C alkylthio and/or phenyl), 1-4C haloalkyl or optionally substituted phenyl; X = N, Y = N or CR9 and Z = N; or X = CH, Y = N or CR9 and Z = N or CR10 provided that Y or Z = N; R9, R10 = 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (all optionally substituted), H, OH, NH2, NH(1-4C alkyl), N(1-4C alkyl)2, halo, 1-4C alkoxy, 1-4C haloalkoxy or 1-4C alkylthio; or CR2+CR9 or CR2+CR10 completes a 5-6 membered alkylene or alkenyl ring (optionally substituted) with one or more CH2 optionally replaced by O, S, NH or N(1-4C alkyl); Q = N and W = bond; or Q = O and W = S, O or a bond; k = 0-2; and p = l-4.
申请公布号 ZA9711305(B) 申请公布日期 1999.06.17
申请号 ZA19970011305 申请日期 1997.12.17
申请人 BASF AKTIENGESELLSCHAFT 发明人 WILHELM AMBERG;ROLF JANSEN;ANDREAS KLING;DAGMAR KLINGE;HARTMUT RIECHERS;STEFAN HERGENROEDER;MANFRED RASCHACK;LILIANE UNGER
分类号 C07D237/14;C07D237/16;C07D241/18;C07D253/07;C07D253/075;C07D253/10;C07D491/04 主分类号 C07D237/14
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