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    Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation
    3.
    发明授权
    Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation 失效
    用于抑制皮肤红斑和/或皮肤色素沉着的碳青霉烯衍生物

    公开(公告)号：US06133264A

    公开(公告)日：2000-10-17

    申请号：US485454

    申请日：2000-02-10

    申请人： Yasuo Oshiro ,  Takao Nishi ,  Keiichi Kuwahara ,  Kozo Watanabe

    发明人： Yasuo Oshiro ,  Takao Nishi ,  Keiichi Kuwahara ,  Kozo Watanabe

    IPC分类号： C07D215/22 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61P17/00 ,  C07D215/227 ,  C07D215/26 ,  C07D405/12 ,  A61K31/5377 ,  A61D17/00 ,  C07D401/02

    CPC分类号： C07D215/227 ,  C07D215/26 ,  C07D405/12

    摘要： The present invention provides an agent for inhibiting skin erythema and/or skin pigmentation, containing at least one selected from the group consisting of the carbostyril derivative and salt thereof represented by the general formula, ##STR1## (wherein R.sup.1 is a hydrogen atom, a lower alkyl group or the like; R.sup.2 is a hydrogen atom, a lower alkyl group, a lower alkoxy group or the like; R.sup.3 and R.sup.4 are lower alkyl groups which may have hydroxyl groups as substituents or the like; the carbon--carbon bond between 3- and 4-positions in the carbostyril skeleton is a single bond or double bond).

    摘要翻译： PCT No.PCT / JP98 / 03657 Sec。 371日期2000年2月10日 102（e）日期2000年2月10日PCT提交1998年8月18日PCT公布。 第WO99 /​​ 09011号公报 日期1999年2月25日本发明提供一种抑制皮肤红斑和/或皮肤色素沉着的药剂，其含有选自由通式表示的喹诺酮衍生物及其盐的至少一种（其中，R 1为氢原子 ，低级烷基等; R 2为氢原子，低级烷基，低级烷氧基等; R 3和R 4为可具有羟基作为取代基的低级烷基等;碳 - 碳 喹诺酮骨架中3-和4-位之间的键是单键或双键）。

    Carbostyril derivative
    5.
    发明授权
    Carbostyril derivative 失效
    碳青霉烯衍生物

    公开(公告)号：US5401740A

    公开(公告)日：1995-03-28

    申请号：US273624

    申请日：1994-07-12

    申请人： Takao Nishi ,  Makoto Komatsu ,  Yasuo Koga ,  Yoshio Shu ,  Katsumi Tamura

    发明人： Takao Nishi ,  Makoto Komatsu ,  Yasuo Koga ,  Yoshio Shu ,  Katsumi Tamura

    IPC分类号： C07D215/22 ,  C07D215/227 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D411/12 ,  C07D417/12 ,  C07D521/00 ,  A61K31/47 ,  A61K31/505 ,  C07D403/12

    CPC分类号： C07D215/227 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D411/12 ,  C07D417/12

    摘要： The novel carbostyril derivative represented by the general formula (1) ##STR1## [in the formula, A, R.sup.1, R.sup.2 and the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton have the same definitions as above] has an excellent platelet aggregation inhibitory activity, a phosphodiesterase inhibitory activity, a venticular contraction activity (a positive contraction activity), an anti-ulcer activity, an anti-inflammatory activity, a cerebral blood flow increasing activity, a thrombus dissociation activity, a thromboxane A.sub.2 antagonism activity, etc. The carbostyril derivative of the present invention is characterized in that it exhibits the above activities for a long time, is low in toxicity (particularly low in toxicity to hearts of cardiovascular hyperplasia, myocardipathy, etc.), and is low in circulation activities such as heart rate increasing activity, blood pressure decreasing activity and the like. Also, the carbostyril derivative of the present invention has advantages in that it is easily absorbed by the intestinal tract and easily migrates into blood. Therefore, the carbostyril derivative of the present invention can be used most suitably as a preventive and remedy for thrombi such as apoplexia, cerebral infarction, myocardial infarction and the like, a cerebral circulation improving agent, an anti-inflammatory agent, an anti-asthmatic agent, a cardiotonic agent and a phosphodiesterase inhibitory agent.

    摘要翻译： 由通式（1）表示的新型喹诺酮衍生物（1）[在式中，A，R1，R2和喹诺酮骨架中3-和4-位之间的碳 - 碳键具有相同的定义 上述]具有优异的血小板聚集抑制活性，磷酸二酯酶抑制活性，通气收缩活性（正收缩活性），抗溃疡活性，抗炎活性，脑血流增加活性，血栓解离活性， 血栓素A2拮抗活性等。本发明的喹诺酮衍生物的特征在于其长时间显示上述活性，毒性低（对心脏心脏增生，心肌病等的心脏毒性特别低）， 并且循环活动低，如心率增加活动，降血压活动等。 此外，本发明的喹诺酮衍生物具有容易被肠道吸收并易于迁移到血液中的优点。 因此，本发明的喹诺酮衍生物可以最适合地用作血栓形成的预防和治疗方法，例如复杂不良，脑梗死，心肌梗塞等，脑循环改善剂，抗炎剂，抗哮喘 药剂，强心剂和磷酸二酯酶抑制剂。

    Tetrazole derivatives, anti-ulcer composition containing the same and method for treating ulcers
    6.
    发明授权
    Tetrazole derivatives, anti-ulcer composition containing the same and method for treating ulcers 失效
    四唑衍生物，含有其的抗溃疡组合物和治疗溃疡的方法

    公开(公告)号：US4663323A

    公开(公告)日：1987-05-05

    申请号：US609333

    申请日：1984-05-11

    申请人： Minoru Uchida ,  Takao Nishi ,  Kazuyuki Nakagawa

    发明人： Minoru Uchida ,  Takao Nishi ,  Kazuyuki Nakagawa

    IPC分类号： C07D257/04 ,  A61K31/535 ,  C07D413/06 ,  C07D413/12

    CPC分类号： C07D257/04

    摘要： Tetrazole derivatives of the formula: ##STR1## wherein R.sup.1 is an optional defined substituent; A is sulfur or a lower alkylene-thio, l is 0 or 1; B is a lower alkylene; R.sup.2 is hydroxy, a lower alkoxy, or a group: ##STR2## wherein R.sup.3 and R.sup.4 are optional defined substituents, or the R.sup.3 and R.sup.4 may combine together with the nitrogen atom to which they are joined to form a defined heterocyclic group, and a pharmaceutically acceptable salt thereof, which have prophylactic or therapeutic activities against peptic and/or duodenal ulcers and also anti-inflammatory activity and are useful as an anti-ulcer or anti-inflammatory drug; processes for the preparation of the tetrazole derivatives; and pharmaceutical composition containing said tetrazole derivatives.

    摘要翻译： 下式的四唑衍生物：其中R 1是任选的限定取代基; A是硫或低级亚烷基 - 硫基，l是0或1; B是低级亚烷基; R 2是羟基，低级烷氧基或基团：其中R 3和R 4是任选的定义的取代基，或者R 3和R 4可以与它们连接的氮原子一起形成定义的杂环基，和 其药学上可接受的盐具有针对消化性溃疡和/或十二指肠溃疡以及抗炎活性的预防或治疗活性，并且可用作抗溃疡或抗炎药物; 制备四唑衍生物的方法; 和含有所述四唑衍生物的药物组合物。

    Process for producing carbostyril derivatives
    7.
    发明授权
    Process for producing carbostyril derivatives 有权
    喹诺酮衍生物的制备方法

    公开(公告)号：US07399864B2

    公开(公告)日：2008-07-15

    申请号：US10208738

    申请日：2002-08-01

    申请人： Shinji Aki ,  Muneaki Kurimura ,  Takao Nishi ,  Junichi Minamikawa ,  Michiaki Tominaga

    发明人： Shinji Aki ,  Muneaki Kurimura ,  Takao Nishi ,  Junichi Minamikawa ,  Michiaki Tominaga

    IPC分类号： C07D215/38

    CPC分类号： C07D401/12 ,  A61K31/4709

    摘要： The present invention provides a process for producing carbostyril derivatives (I) which are known to be useful as medical drug such as antithrombotic agent, cerebral circulation improver, anti-inflammatory agent, antiulcer agent, etc. in a high yield and a high purity. The carbostyril derivatives (I) can be produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase transfer catalyst.

    摘要翻译： 本发明提供了以高产率和高纯度制备喹诺酮衍生物（I）的方法，已知其可用作药物如抗血栓形成剂，脑循环改进剂，抗炎剂，抗溃疡剂等。 喹诺酮衍生物（I）可以通过在相转移催化剂存在下使喹诺酮衍生物（II）与四唑衍生物（III）反应来制备。