发明名称 PHENYL DERIVATIVES USEFUL AS ENDOTHELIN RECEPTOR ANTAGONISTS
摘要 <p>Compounds of Formula (I), wherein R is a group Ar as defined hereinafter; R1 is hydrogen, hydroxy, C¿1-6?alkyl, C1-6alkoxy, X(CH2)pAr; or a methylenedioxy group attached to two adjacent ring carbon atoms; R?2¿ is -(CH¿2?)xC(O)N(R?4)S(O)¿yR5, -(CH¿2?)xS(O)yN(R?4)C(O)R5¿, -(CH¿2?)xC(O)N(R?4)C(O)R5¿, -(CH¿2?)xS(O)yN(R?4)S(O)¿yR5, -(CH¿2?)xCO2R?4¿, or tetrazol-5-yl optionally substituted by C¿1-6?alkyl; R?3¿ is X(CH¿2?)pAr or -X(CH2)pR?4¿ or a group of formula (a): Ar is a group of formula (b) or (c); or Ar is naphthyl, indolyl, pyridyl, thienyl, furyl, oxazolidinyl, oxazolyl, thiazolyl, isothiazolyl, pyrazolyl, triazolyl, tetrazolyl, imidazolyl, imidazolidinyl, thiazolidinyl, isoxazolyl, oxadiazolyl, thiadiazolyl, morpholinyl, piperidinyl, piperazinyl, pyrrolyle, or pyrimidyl; all of which may be unsubstituted or substituted by one or more R7 or R8 groups; A is C=O, or (C(R4)2)m; each B is independently -CH2- or -O-; and their pharmaceutically acceptable salts are endothelin antagonists and are useful e.g. for the treatment of renal failure, cerebrovascular disease and hypertension.</p>
申请公布号 WO1996030358(A1) 申请公布日期 1996.10.03
申请号 EP1996001237 申请日期 1996.03.21
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