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    • 1. 发明授权
      US4435404A Carbostyril derivatives 失效
    • Carbostyril derivatives
    • US4435404A
    • 1984-03-06
    • US261177
    • 1981-04-30
    • Takao Nishi , Tatsuyoshi Tanaka , Kazuyuki Nakagawa
    • Takao Nishi , Tatsuyoshi Tanaka , Kazuyuki Nakagawa
    • A61K31/47 , A61K31/4704 , A61P1/04 , A61P7/02 , A61P9/00 , A61P9/12 , A61P29/00 , A61P43/00 , C07D213/38 , C07D215/06 , C07D215/22 , C07D215/227 , C07D309/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
    • C07D215/227 , C07D213/38 , C07D215/22 , C07D309/04 , Y10S514/826 , Y10S514/926 , Y10S514/927
    • Novel carbostyril derivative and its salt represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a phenyl-lower alkyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a group of the formula ##STR2## wherein A is a lower alkylene group; R.sup.3 is a lower alkyl group, a hydroxy lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or a benzoyloxy-lower alkyl group; and R.sup.4 is a C.sub.3-10 -cycloalkyl group which may have at least one hydroxyl group as the substituent(s) in the cycloalkyl ring, a C.sub.3-10 -cycloalkyl-lower alkyl group, a phenyl group, a phenyl-lower alkyl group which may have at least one lower alkoxy group as the substituent(s) in the phenyl ring, a lower alkyl group which may have at least one hydroxyl group as the substituent(s), a heterocyclic ring residue or a lower alkyl group having one heterocyclic ring residue as the substituent; further, R.sup.3, R.sup.4 and the adjacent nitrogen atom, as well as with or without another nitrogen atom, may form a group of the formula ##STR3## (wherein R.sup.5 is a phenyl group, a C.sub.3-10 -cycloalkyl group or a phenyl-lower alkyl group; and B is a methine group or a nitrogen atom); the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton is a single or double bond; the substituted position of the group of the formula ##STR4## is any one of 5-, 6-, 7- or 8-position in the carbostyril skeleton; when the group of the formula ##STR5## is substituted at 5-, 6-, 7- or 8-position in the carbostyril skeleton, then R.sup.2 is a hydrogen atom or a lower alkyl group; alternatively, when R.sup.2 is a group of the formula ##STR6## then 5-, 6-, 7- and 8-positions in the carbostyril skeleton are hydrogen atoms and are not substituted with groups of the formula ##STR7## and when R.sup.3 is a lower alkyl group, then R.sup.4 should be neither of a C.sub.3-10 -cycloalkyl group, a C.sub.3-10 -cycloalkyl-lower alkyl group nor a lower alkyl group, having effects for preventing and treating thrombosis and embolism.
    • 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
    • 3. 发明授权
      US4564619A Carbostyril derivative 失效
    • Carbostyril derivative
    • 碳青霉烯衍生物
    • US4564619A
    • 1986-01-14
    • US528887
    • 1983-09-02
    • Tatsuyoshi Tanaka , Kazuyoshi Nagami , Shigeharu Tamada , Kazuyuki Nakagawa
    • Tatsuyoshi Tanaka , Kazuyoshi Nagami , Shigeharu Tamada , Kazuyuki Nakagawa
    • C07D215/22 , C07D215/227 , C07D401/12 , A61K31/47
    • C07D215/227 , C07D401/12
    • Carbostyril derivative or a pharmaceutically acceptable acid addition salt thereof, having excellent platelate aggregation inhibitory effect, calcium antagonism, hypotensive effect and phosphodiesterase inhibitory effect are useful as prophylactic or treating agents for thrombosis, circulation improving agents for coronary blood flow such as coronary vasodilators, hypotensive agents and phosphodiesterase inhibitors. Furthermore, the carbostyril derivatives are weak in heart rate increasing activity and also in cardiac muscle contraction increasing activity, and the carbostyril derivatives are useful agents for curing and treating heart diseases such as cardiac angina and myocardial infarction caused by hypercoagulability of the platelets. Processes are disclosed for preparation of the carbostyril derivatives.
    • 具有极好的铂性聚集抑制作用，钙拮抗作用，降血压作用和磷酸二酯酶抑制作用的卡波他特里尔衍生物或其药学上可接受的酸加成盐可用作血栓形成的预防或治疗剂，用于冠状动脉血管扩张剂的血液循环改善剂，降血压 药剂和磷酸二酯酶抑制剂。 此外，喹诺酮衍生物的心率增加活性弱，心肌收缩增加活性也较弱，而喹诺酮衍生物可用于治疗和治疗由心血管病和心肌梗塞引起的血小板高凝状态引起的心脏病。 公开了制备喹诺酮衍生物的方法。
    • 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
    • 8. 发明授权
      US07582781B2 Optically active halohydrin derivative and process for producing optically active epoxy alcohol derivative from the same 失效
    • Optically active halohydrin derivative and process for producing optically active epoxy alcohol derivative from the same
    • 光学活性卤代醇衍生物及其制备光学活性环氧醇衍生物的方法
    • US07582781B2
    • 2009-09-01
    • US10563635
    • 2004-07-05
    • Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
    • Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
    • C07D301/24 , C07D301/26 , C07D405/06 , C07C33/26 , C07C69/353 , C07F7/04
    • C07C67/29 , C07B2200/07 , C07C29/10 , C07D301/24 , C07C33/46
    • The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxy alcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.
    • 本发明提供了一种工业上安全，易于操作的方法，用于制备用作药物的廉价可得材料的中间体的光学活性环氧醇衍生物，并且还提供了作为环氧醇衍生物的重要中间体的新型卤代醇衍生物。 此外，本发明提供了通过使卤代醇与三唑磺酰胺反应来制备三唑抗真菌剂的中间体的方法，该方法包括少量的步骤。 制备光学活性环氧醇衍生物的方法包括使光学活性的α-取代的丙酸酯衍生物与卤代乙酸衍生物在碱的存在下反应以制备光学活性的卤代酮衍生物，使所得到的卤代酮衍生物与 芳基金属化合物立体选择性地制备卤代醇衍生物，除去卤代醇衍生物的羟基的取代基，并用碱进行环氧化。 此外，制备三唑抗真菌剂中间体的方法包括使卤代醇衍生物与三唑磺酰胺反应，该方法包括少量步骤。
    • 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 Espacenet 法律信息 同族专利 专利引用
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