首页> 外国专利> NEW 6-AMINO- OR 6-HYDRAZINO-SULPHONYL-3-QUINOLINYL-PHOSPHONIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

NEW 6-AMINO- OR 6-HYDRAZINO-SULPHONYL-3-QUINOLINYL-PHOSPHONIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:新的6-氨基或6-肼基-磺酰基-3-喹啉基-膦酸衍生物,其制备方法和包含它们的药物组合物

摘要

The present invention relates to compounds of formula I, their enantiomers and diastereomers, and addition salts thereof with pharmaceutically acceptable acids or bases, wherein R 1 is halogen or trifluoromethyl, R 2 is hydrogen or alkyl or cycloalkyl, R 3 is alkyl, cycloalkyl, aryl, arylalkyl, alkoxy, aryloxy, arylalkoxy, hydroxy, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkylcarbonyl, arylcarbonyl or arylalkylcarbonyl or NHR6 (wherein R6 is hydrogen or alkyl, cycloalkyl, aryl, alkylcarbonyl); arylcarbonyl, arylalkyl or arylalkylcarbonyl) or R 2 and R 3 taken together with the nitrogen atom to which they are attached form a 5 or 6 membered ring in which one carbon atom is replaced by an oxygen, nitrogen or sulfur atom or an SO or SO 2 group or an NRa Is hydrogen or alkyl, cycloalkyl, aryl or arylalkyl), R4 and R5 may be or different and are selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, and arylalkyl, or a group of the general formula (wherein R 7 and R 8 may be the same or different and are hydrogen or alkyl, cycloalkyl or aryl). The invention also relates to a process for the preparation of the above compounds of formula (I) and to pharmaceutical compositions containing such compounds as active ingredients. The above compounds are contraindicated in neurological and psychological disorders. HE
机译:本发明涉及式I的化合物,其对映异构体和非对映异构体及其与药学上可接受的酸或碱的加成盐,其中R 1为卤素或三氟甲基,R 2为氢或烷基或环烷基,R 3为烷基,环烷基,芳基,芳基烷基,烷氧基,芳氧基,芳基烷氧基,羟基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,烷基羰基,芳基羰基或芳基烷基羰基或NHR6(其中R6为氢或烷基,环烷基,芳基,烷基羰基);芳基羰基,芳基烷基或芳基烷基羰基)或R 2和R 3与它们所连接的氮原子一起形成5或6元环,其中一个碳原子被氧,氮或硫原子或SO或SO取代(R 2为氢或烷基,环烷基,芳基或芳基烷基),R 4和R 5可以相同或不同,并且选自氢,烷基,环烷基,芳基和芳基烷基或通式的基团(其中R 7和R 8可以相同或不同,并且是氢或烷基,环烷基或芳基)。本发明还涉及制备上述式(I)化合物的方法,并涉及含有这类化合物作为活性成分的药物组合物。上述化合物禁忌神经和心理疾病。他

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