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4-(2-hydroxyphenyl)-pyrazoles and isoxazoles

机译:4-(2-羟苯基)-吡唑和异恶唑

摘要

The invention comprises compounds of the formula FORM:1025697/C2/1 where X represents O, NH or N-CH3, R represents a methyl, ethyl, n-butyl, phenyl or benzyl radical and R1 represents a hydrogen atom or a methyl, ethyl, n-butyl, phenyl, 4-hydroxyphenyl, 4 - methoxyphenyl, 4 - (b - N - diethylaminoethoxy) - phenyl, 3,4,5 - trimethoxyphenyl, 2 - methoxyphenyl, 2 - thienyl or 4-pyridyl radical, and their alkali metal salts, and acid addition salts of the compounds where X represents NH or N-CH3, or where X represents oxygen and R1 represents a 4-pyridyl or 4 - (b - N - diethylaminoethoxy) - phenyl radical, and the preparation thereof by reaction of a benzofuran of the formula FORM:1025697/C2/2 with an amine of the formula NH2.XH, and, if desired, where X represents an -NH- or -NCH3- group or when X represents an oxygen atom and R1 represents a 4-pyridyl or 4 - (b - N - diethylaminoethoxy) phenyl group, converting the product into the appropriate acid addition salt. Therapeutic compositions, with anti-inflammatory activity, in the form of capsules, tablets, pills, powders, solutions and ampoules for oral or parenteral administration, comprise compounds of the Formula I or pharmaceutically acceptable acid addition salts thereof together with a pharmaceutical carrier.
机译:本发明包括式的化合物,其中X代表O,NH或N-CH 3,R代表甲基,乙基,正丁基,苯基或苄基,R1代表氢原子或甲基,乙基,正丁基,苯基,4-羟基苯基,4-甲氧基苯基,4-(b-N-二乙基氨基乙氧基)-苯基,3,4,5-三甲氧基苯基,2-甲氧基苯基,2-噻吩基或4-吡啶基,以及其中X代表NH或N-CH3,或X代表氧且R1代表4-吡啶基或4-(b-N-二乙基氨基乙氧基)-苯基的化合物的碱金属盐和酸加成盐,以及通过使式的苯并呋喃与式NH2.XH的胺反应,以及如果需要,其中X代表-NH-或-NCH3-基团或当X为R 1表示氧原子,R 1表示4-吡啶基或4-(b-N-二乙基氨基乙氧基)苯基,将产物转化为适当的酸加成盐。具有抗炎活性的用于口服或肠胃外给药的胶囊,片剂,丸剂,散剂,溶液剂和安瓿剂形式的治疗组合物包含式I化合物或其药学上可接受的酸加成盐以及药物载体。

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