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    • 5. 发明授权
      US4847256A 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines 失效
    • 4,5-dihydro and 4,5,6,7-tetrahydropyrazolo(1,5-A)-pyrimidines
    • 4,5-二氢和4,5,6,7-四氢吡唑并（1,5-A） - 嘧啶
    • US4847256A
    • 1989-07-11
    • US919730
    • 1986-10-16
    • Shin S. Tseng , John P. Dusza , Joseph W. Epstein
    • Shin S. Tseng , John P. Dusza , Joseph W. Epstein
    • A61K31/505 , A61P25/20 , C07D487/04
    • C07D487/04
    • Novel compounds having the following structural formula: ##STR1## wherein - - - may represent the presence of a double bond between the C.sub.6 and C.sub.7 position, Ia, or the absence of a double bond between the C.sub.6 and C.sub.7 position, Ib; R.sub.1 is selected from the group consisting essentially of hydrogen, bromo, chloro, carbamoyl, carboxyl, carboxyalkoxyl where alkoxyl is (C.sub.1 -C.sub.3), cyano, --CO--CF.sub.3, COONa, ##STR2## --CO--C(CH.sub.3).sub.3, and ##STR3## where X is hydrogen, cyano, halogen and nitro; R.sub.2, R.sub.4 and R.sub.5 may be hydrogen and lower alkyl (C.sub.1 -C.sub.3); R.sub.3 is hydrogen, alkyl (C.sub.1 -C.sub.3), ##STR4## where R.sub.7 and R.sub.8 may be the same or different and are selected from the group consisting essentially of hydrogen, halogen, alkyl (C.sub.1 -C.sub.3), nitro, alkoxy (C.sub.1 -C.sub.3), trifluoro-methyl, acetylamino or N-alkylacetylamino where alkyl is (C.sub.1 -C.sub.3), and R.sub.3 may also be selected from a monovalent radical selected from the class consisting essentially of 3-thienyl, 2-pyridinyl, 3-pyridinyl and 4-pyridinyl, either of said pyridinyl radicals being optionally substituted with an alkyl radical R.sub.9, where alkyl is (C.sub.1 -C.sub.4), and the structures of the monovalent 2-pyridinyl, 3-pyridinyl and 4-pyridinyl moieties are depicted respectively as: ##STR5## R.sub.6 is hydrogen or alkyl-(C.sub.1 -C.sub.3); pharmaceutical compositions of matter containing the above-defined compounds; methods for using the compounds as anxiolytic agents, antihypertensive agents or antidepressant agents in mammals; processes for the preparation of the compounds.
    • 具有以下结构式的新化合物：其中 - - 可以表示在C6和C7位置之间存在双键，Ia或在C6和C7位置之间不存在双键，Ib ; R 1选自基本上由氢，溴，氯，氨基甲酰基，羧基，羧基烷氧基，其中烷氧基是（C1-C3），氰基，-CO-CF3，COONa，-CO-C（CH3）3， 和，其中X是氢，氰基，卤素和硝基; R2，R4和R5可以是氢和低级烷基（C1-C3）; R3是氢，烷基（C1-C3），其中R7和R8可以相同或不同，并且选自基本上由氢，卤素，烷基（C1-C3），硝基，烷氧基（C1- C3），三氟甲基，乙酰氨基或N-烷基乙酰氨基，其中烷基是（C1-C3），R3也可以选自基本上由3-噻吩基，2-吡啶基，3-吡啶基和 所述吡啶基任选被烷基基团R 9取代，其中烷基是（C 1 -C 4），并且一价2-吡啶基，3-吡啶基和4-吡啶基部分的结构分别描述为： R6是氢或烷基 - （C1-C3）; 含有上述化合物的物质的药物组合物; 在哺乳动物中使用化合物作为抗焦虑剂，抗高血压药或抗抑郁药的方法; 制备化合物的方法。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 7. 发明授权
      US5219857A Method of treating cognitive and related neural behavioral problems 失效
    • Method of treating cognitive and related neural behavioral problems
    • US5219857A
    • 1993-06-15
    • US869573
    • 1992-04-15
    • Shin S. Tseng , Herbert J. Brabander , Joseph W. Epstein
    • Shin S. Tseng , Herbert J. Brabander , Joseph W. Epstein
    • C07D487/04
    • C07D487/04
    • Novel compounds of the formula ##STR1## wherein n is an integer from 1 to 4 inclusive; R.sub.1 represents a mono-or disubstituent of hydrogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy(C.sub.1 -C.sub.3), halogen, nitro or trifluoromethyl; R.sub.2 is cyano, carboxamido, ethyl carboxylate or halogen; R.sub.3 is hydrogen, straight or branched chain lower alkyl(C.sub.1 -C.sub.3), alkenyl(C.sub.2 -C.sub.3), alkynyl(C.sub.2 -C.sub.3), cycloalkyl(C.sub.3 -C.sub.6), hydroxyalkyl(C.sub.1 -C.sub.3), dimethylaminoalkyl(C.sub.1 -C.sub.3), ethylcarboxylate, alkyl(C.sub.1 -C.sub.13)carbonyl, 1-(methylethyl)acetamide, cyclohexylethyl, phenyl, mono-or disubstituted phenyl (wherein the phenyl substituent is halogen, trifluoromethyl, lower alkyl(C.sub.1 -C.sub.3) or lower alkoxy(C.sub.1 -C.sub.3)), benzyl, mono-or disubstituted benzyl (wherein the benzyl substituent is halogen, lower alkyl(C.sub.1 -C.sub.3), lower alkoxy(C.sub.1 -C.sub.3) or trifluoromethyl), benzoyl, 4-methoxybenzoyl, straight or branched chain alkyl(C.sub.2 -C.sub.3)phenyl, 4-chlorophenylphenylmethyl, 1,3-benzodioxol-5-ylmethyl, 1,3-benzodioxol-5-yl, 2-furanylcarbonyl, 2-pyrimidinyl, 2-pyridinyl, 4-morpholinyl-2-oxoethyl, 1-pyrrolidinyl-2-oxoethyl, bis(4-fluorophenyl)methyl, phenylcarboxamido, mono- and disubstituted phenylcarboximido (wherein the phenyl substituents is halogen, trifluoromethyl or lower alkyl(C.sub.1 -C.sub.3)), adamantanoyl, 3-phenoxypropyl,5-chloro-2-methoxyphenylacetamide, (2-oxo-1-pyrrolidinyl)-2-butynyl, phenylmethylcarboxylate, or (2-phenyl-2H-1,2,3-triazol-4-yl)methyl; R.sub.4 and R.sub.5 are independently hydrogen or lower alkyl(C.sub.1 -C.sub.3); the dotted line between positions 6 and 7 of the pyrimidine ring represents the presence or absence of a double bond; and the pharmacologically acceptable salts thereof: methods of producing them; therapeutic compositions containing them: and methods of using them to treat anxiety, hypertension, depression, senile dementia, cognitive defects and other neural behavior problems in warm-blooded animals.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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