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2. 发明授权

US4302460A 4-Quinolinones having antihypertensive activity 失效
标题翻译：具有抗高血压活性的4-喹啉酮
公开(公告)号：US4302460A
公开(公告)日：1981-11-24
申请号：US133310
申请日：1980-03-24
申请人： Roy V. Davies , James Fraser , Kenneth J. Nichol , Raymond Parkinson , Malcolm F. Sim , David B. Yates
发明人： Roy V. Davies , James Fraser , Kenneth J. Nichol , Raymond Parkinson , Malcolm F. Sim , David B. Yates
IPC分类号： A61K31/47 , C07D215/36 , C07D265/26
CPC分类号： C07D265/26 , A61K31/47 , C07D215/36
摘要： Compositions which contain a quinolone compound of the general formula ##STR1## wherein n is 0, 1 or 2; R.sub.1 is lower alkyl optionally substituted by hydroxy or C.sub.1-4 alkoxycarbonyl; allyl; propynyl or phenyl- lower alkyl in which the phenyl ring is optionally substituted by 1 or 2 C.sub.1-4 alkoxy groups; R.sub.2 is C.sub.1-4 alkyl with the proviso that when n is 0, R.sub.2 is methyl; and R.sub.3, R.sub.4 and R.sub.5, which may be the same or different, are hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, halo, trifluoromethyl or lower alkylthio show antihypertensive activity.Compounds of general formula ##STR2## in which n, R.sub.1 R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as described above are novel subject to the following provisos (a) when R.sub.3, R.sub.4 and R.sub.4 and R.sub.5 are hydrogen R.sub.2 is methyl and R.sub.1 is lower alkyl, R.sub.1 contains more than one carbon atom, and(b) when R.sub.3 and R.sub.4 are hydrogen, R.sub.5 is hydrogen or 7-methyl, and R.sub.1 is ethyl, R.sub.2 contains more than one carbon atom.The specification describes and claims methods of making the compounds and novel intermediates used in such methods.
摘要翻译：含有通式为“IMAGE”的喹诺酮化合物的组合物，其中n为0,1或2; R1是任选被羟基或C 1-4烷氧基羰基取代的低级烷基; 烯丙基丙炔基或苯基 - 低级烷基，其中苯环任选被1或2个C 1-4烷氧基取代; R2为C1-4烷基，条件是当n为0时，R2为甲基; R 3，R 4和R 5可以相同或不同，为氢，低级烷基，低级烷氧基，低级烷酰基，卤素，三氟甲基或低级烷硫基，表示抗高血压活性。其中n，R1R2，R3，R4和R5如上所述的通式为“IMAGE”的化合物是新的，具有以下条件（a）当R3，R4和R4和R5为氢时R2为甲基，R1为低级烷基，R 1含有多于一个碳原子，和（b）当R 3和R 4为氢时，R 5为氢或7-甲基，R 1为乙基，R 2为多于一个碳原子。该说明书描述并要求制备在这些方法中使用的化合物和新型中间体的方法。

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