PYRAZOLE DERIVATIVE

PURPOSE:To obtain a new derivative useful as an antagonist for angiotensin II in treatment for cardiovascular diseases, especially hypertension, heart failure and vein failure, glaucoma, diabetic retinopathy, central nervous diseases and chronic renal diseases. CONSTITUTION:This compound is represen...

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Hauptverfasser: MASUDA YUKINORI, SATO MASAYUKI, TANIGAWA KEIZO, KAMIKAWAJI KAMIKAWAJI, OODOI KEISUKE, HIGASHIYAMA TSUTOMU
Format: Patent
Sprache:eng
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Zusammenfassung:PURPOSE:To obtain a new derivative useful as an antagonist for angiotensin II in treatment for cardiovascular diseases, especially hypertension, heart failure and vein failure, glaucoma, diabetic retinopathy, central nervous diseases and chronic renal diseases. CONSTITUTION:This compound is represented by formula I[R is H, a 1-10C (substituted)-alkyl, etc.; R to R each is a halogen, nitro, etc.; R is carboxyl, 5-tetrazolyl, etc.; X is N or NO; Y and Z each is N or CR ; A and E each IS methylene, etc.; D IS phenyl, etc.; G is a covalent bond, etc.], its tautomer and salt thereof, e.g. N-[1-(2-phenylethyl)-4-ethoxycarbonyl-5-bromopyrazol-3-yl]- N[(2'-(N-triphenylmethyl-(1H-tetrazol-5-yl) biphenyl-4-yl)methyl]-n-propylamine. The compound of formula 1 (R' is H) is obtained by reacting, e.g., a compound of formula II with a compound of formula III (V is a halogen, etc.) to lead to a compound of formula IV and as necessary, carrying out deprotection of the compound of formula IV.