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5-Amino-5-(N-formyl-carbamoyl)-pyrazole derivs - prepd. by cyclizing N-formyl-alpha-(acylhydrazinomethylene)-cyanoacetamides

机译:5-氨基-5-(N-甲酰基-氨基甲酰基)-吡唑衍生物-制备。通过环化N-甲酰基-α-(酰基肼基亚甲基)-氰基乙酰胺

摘要

5-Amino-5-(N-formylcarbamoyl)-pyrazole derivs. of formula (I) (where alk is opt. branched -15C alkylene; n is 0 or 1; and R3 is a heterocyclic residue having aromatic character, or a partially or pre-hydrogenated deriv. of such a residue), e.g. 5-amino-3-formylcarbamoyl-1-nicotinoylpyrazole, 5-amino-3-formylcarbamoyl-1-(2,4-dioxo-1, 2,3,4-tetrahydro-6-pyrimidinylcarbonyl)-pyrazole and 5-amino-3-formylcarbamoyl-1- 2-1(1,3,5-triphenyl-1H-pyrazol-4-yl)- -acetyl -pyrazole, and their salts are new cpds. (I) are xanthine oxidase inhibitors with considerably lower acute toxicity than allopurinol, and are useful in the treatment of gout.
机译:5-氨基-5-(N-甲酰基氨基甲酰基)-吡唑衍生物。式(I)的通式(I1)(其中alk是任选的支链-15C亚烷基; n是0或1; R 3是具有芳族特性的杂环残基,或该残基的部分或预氢化的衍生物),例如5-氨基-3-甲酰基氨基甲酰基-1-烟酰基吡唑,5-氨基-3-甲酰基氨基甲酰基-1-(2,4-二氧代-1、2,3,4-四氢-6-嘧啶基羰基)-吡唑和5-氨基- 3-甲酰基氨基甲酰基-1-2-1(1,3,5-三苯基-1H-吡唑-4-基)-乙酰基-吡唑及其盐是新的cpds。 (I)是黄嘌呤氧化酶抑制剂,其急性毒性比别嘌呤醇低得多,可用于治疗痛风。

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