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1. 发明授权

US5434164A Carbostyril derivatives and salts thereof and pharmaceutical compositions for inhibiting adhesion of thrombocytes 失效
标题翻译：卡波他特尔衍生物及其盐和用于抑制凝血细胞粘附的药物组合物
公开(公告)号：US5434164A
公开(公告)日：1995-07-18
申请号：US958489
申请日：1992-10-08
申请人： Takao Nishi , Tetsuyuki Uno , Yasuo Koga , Gil-Namg Chu
发明人： Takao Nishi , Tetsuyuki Uno , Yasuo Koga , Gil-Namg Chu
IPC分类号： A61K31/47 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D403/02
CPC分类号： C07D401/12 , A61K31/47 , C07D401/14 , C07D405/12 , C07D417/12
摘要： Carbostyril derivatives and salts thereof represented by the general formula (1a), including some known compounds, possess activities for inhibiting adhesion of thrombocytes. ##STR1## Z, A, X, R, R.sup.1 and R.sup.2 are defined in the specification. Some carbostyril derivatives having chemical structural formulas similar to those of carbostyril derivatives and salts thereof represented by the general formula (1a) have been known in prior art references, however the above-mentioned pharmacological activities have not been known to the present date.
摘要翻译：包括一些已知化合物的由通式（1a）表示的卡博司坦衍生物及其盐具有抑制凝血细胞粘附的活性。（1a）Z，A，X，R，R1和R2在说明书中定义。具有与由通式（1a）表示的喹诺酮衍生物及其盐类似的化学结构式的喹诺酮衍生物在现有技术参考文献中是已知的，然而上述药理学活性在当前日期尚未知晓。

2. 发明授权

US5008274A Carbostyril derivatives and salts thereof and pharmaceutical composition for inhibiting adhesion of thrombocytes 失效
标题翻译：碳青霉烯衍生物及其盐和用于抑制凝血细胞粘附的药物组合物
公开(公告)号：US5008274A
公开(公告)日：1991-04-16
申请号：US232524
申请日：1988-08-16
申请人： Takao Nishi , Tetsuyuki Uno , Yasuo Koga , Gil-Namg Chu
发明人： Takao Nishi , Tetsuyuki Uno , Yasuo Koga , Gil-Namg Chu
IPC分类号： A61K31/47 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12
CPC分类号： C07D401/12 , A61K31/47 , C07D401/14 , C07D405/12 , C07D417/12
摘要： A carbostyril derivative or pharmaceutically acceptable salt thereof represented by the following general formula: ##STR1## wherein Z, A, XN, R, R.sup.1, and R.sup.2 are as defined in the specification. These carbostyril derivatives are useful in pharmaceutical compositions for inhibiting adhesion of thrombocytes.
摘要翻译：由下列通式表示的喹诺酮衍生物或其药学上可接受的盐：其中Z，A，XN，R，R1和R2如说明书中所定义。这些喹诺酮衍生物可用于抑制凝血细胞粘附的药物组合物。

3. 发明授权

US5541198A Carbostyril derivatives 失效
标题翻译：卡波他汀衍生物
公开(公告)号：US5541198A
公开(公告)日：1996-07-30
申请号：US367196
申请日：1995-01-18
申请人： Takao Nishi , Tetsuyuki Uno , Yoshio Shu , Katsumi Tamura , Minoru Okada
发明人： Takao Nishi , Tetsuyuki Uno , Yoshio Shu , Katsumi Tamura , Minoru Okada
IPC分类号： A61K31/47 , A61K31/33 , A61P7/02 , A61P9/10 , C07D401/00 , C07D401/12
CPC分类号： C07D401/12
摘要： Carbostyril derivatives useful for inhibiting the adhesion of platelets represented by general formula ##STR1## [wherein, R.sup.1 is a hydrogen atom, a fluorine atom or a methyl group; R is a group of the formula ##STR2## (R.sup.2 is a methyl group, a trifluoromethyl group or a nitro group), or a group of the formula ##STR3## (R.sup.3 is a fluorine atom and p is an integer of 2 or 3); and n is an integer of 2 or 3], or salts thereof.Said carbostyril derivatives or salts are useful as an agent for inhibiting the adhesion of platelets.
摘要翻译： PCT No.PCT / JP94 / 00760 Sec。 371 1995年1月18日第 102（e）日期1995年1月18日PCT提交1994年5月11日PCT公布。第WO94 / 26732号公报日期：1994年11月24日用于抑制由通式表示的血小板的粘附的卡波斯特尔衍生物[其中，R1是氢原子，氟原子或甲基; R是下式的基团（R 2是甲基，三氟甲基或硝基）或下式的基团（R 3是氟原子，p是2或3的整数））; n为2或3的整数]或其盐。所述喹诺酮衍生物或盐可用作抑制血小板粘附的药剂。

4. 发明授权

US5401740A Carbostyril derivative 失效
标题翻译：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。

5. 发明授权

US5227381A Carbostyril derivative 失效
标题翻译：碳青霉烯衍生物
公开(公告)号：US5227381A
公开(公告)日：1993-07-13
申请号：US929097
申请日：1992-08-13
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
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： Carbostyril compounds or salts thereof of the formula ##STR1## wherein A is a C.sub.1 -C.sub.6 alkylene group; R.sup.1 is a C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl group which may have, as a substituent, a group selected from the group consisting of C.sub.1 -C.sub.6 alkoxycarbonyl groups, a carboxy group, C.sub.2 -C.sub.6 alkanoyloxy-C.sub.1 -C.sub.6 alkyl groups, amino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkylamino-C.sub.1 -C.sub.6 alkyl groups and hydroxy-C.sub.1 -C.sub.6 alkyl groups, a C.sub.3 -C.sub.8 cycloalkyl group, a tetrahydropyranyl-C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.3 alkylenedioxy group-substituted C.sub.1 -C.sub.6 alkyl group, a phenyl-C.sub.1 -C.sub.6 alkyl group having, as a substituent on the phenyl ring, 1 to 3 groups selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and a hydroxyl group, or a piperidinyl-C.sub.1 -C.sub.6 alkyl group having a C.sub.1 -C.sub.6 alkyl group as a substituent; R.sup.2 is a 5-membered or 6-membered saturated or unsaturated heterocyclic-C.sub.1 -C.sub.6 alkyl group, said heterocyclic being selected from the group consisting of pyrrolidinyl, morpholino, piperidinyl, thiomorpholino, imidazolyl, 1,2,4-triazolyl, furyl, piperazinyl, pyridyl, tetrahydropyranyl and 1,3-oxathiolranyl groups which may have, as a substituent thereon 1 to 3 groups selected from the group consisting of hydroxy-C.sub. 1 -C.sub.6 alkyl groups, C.sub.2 -C.sub.6 alkanoyloxy-C.sub.1 -C.sub.6 alkyl groups, a hydroxyl group, C.sub.1 -C.sub.6 alkyl groups, amino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkylamino-C.sub.1 -C.sub.6 alkyl groups, C.sub.1 -C.sub.6 alkoxy groups, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkoxy groups, C.sub.1 -C.sub.6 alkoxy-C.sub.1 -C.sub.6 alkyl groups, a thio group and C.sub.1 -C.sub.6 alkylamido groups; the carbon-carbon bond between the 3- and 4-positions in the carbostyril skeleton being a single bond or a double bond and pharmaceutical compositions containing the compound as the active ingredient.
摘要翻译：其中A为C1-C6亚烷基的卡波斯特尔化合物或其盐， R1是可以具有选自C1-C6烷氧基羰基，羧基，C2-C6烷酰氧基-C1-C6烷基的基团作为取代基的C3-C8环烷基-C1-C6烷基，氨基-C 1 -C 6烷基，C 1 -C 6烷基氨基-C 1 -C 6烷基和羟基-C 1 -C 6烷基，C 3 -C 8环烷基，四氢吡喃基-C 1 -C 6烷基，C 1 -C 3亚烷基二氧基 - 取代的C 1 -C 6烷基，作为苯环上的取代基的苯基-C 1 -C 6烷基，选自C 1 -C 6烷基和羟基的1至3个基团或哌啶基-C 1 具有C 1 -C 6烷基的-C 6烷基作为取代基; R2是5元或6元饱和或不饱和杂环-C 1 -C 6烷基，所述杂环选自吡咯烷基，吗啉代，哌啶基，硫代吗啉代，咪唑基，1,2,4-三唑基，呋喃基，哌嗪基，吡啶基，四氢吡喃基和1,3-氧硫杂环戊酰基，其可以具有1至3个选自羟基-C 1 -C 6烷基，C 2 -C 6烷酰氧基-C 1 -C 6烷基，羟基，C 1 -C 6烷基，氨基-C 1 -C 6烷基，C 1 -C 6烷基氨基-C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷氧基-C 1 -C 6烷氧基，C 1 -C 6烷氧基 -C 1 -C 6烷基，硫基和C 1 -C 6烷基酰胺基; 喹诺酮骨架中3-和4-位之间的碳 - 碳键是单键或双键，以及含有该化合物作为活性成分的药物组合物。

6. 发明授权

US6143763A Carbostyril derivatives 失效
标题翻译：卡波他汀衍生物
公开(公告)号：US6143763A
公开(公告)日：2000-11-07
申请号：US849664
申请日：1997-05-29
申请人： Yasuo Koga , Yoshito Kihara , Minoru Okada , Takao Nishi , Yoshihiro Inoue , Yukio Kimura , Hiroyoshi Hidaka , Norio Fukuda
发明人： Yasuo Koga , Yoshito Kihara , Minoru Okada , Takao Nishi , Yoshihiro Inoue , Yukio Kimura , Hiroyoshi Hidaka , Norio Fukuda
IPC分类号： C07D215/22 , C07D215/227 , A61K31/4704
CPC分类号： C07D215/227
摘要： A carbostyril derivative of the formula (1): ##STR1## wherein A is lower alkylene, R is H, halogen or lower alkoxy, R.sup.1 and R.sup.2 are each lower alkyl being optionally substituted by OH, lower alkoxy, phenyl-lower alkoxy or lower alkanoyloxy; cycloalkyl being optionally substituted by OH, hydroxy-lower alkoxy or lower alkanoyloxy; or amino being optionally substituted by lower alkyl or cycloalkyl, R.sup.3 is H, lower alkyl, lower alkenyl or hydroxy-lower alkyl, and the bond between 3- and 4-positions of the carbostyril nucleus is single or double, provided that when R and R.sup.3 are H, R.sup.1 and R.sup.2 should not be either unsubstituted lower alkyl or unsubstituted cycloalkyl, or a salt thereof, which shows antithrombotic activities, intima thickening inhibitory activity, the platelet mass dissociating activity and increasing activity of the blood flow in the brain and the peripheral vessel, and hence, is useful as medicines in the prophylaxis or treatment of various ischemic diseases.
摘要翻译： PCT No.PCT / JP96 / 02892 Sec。 371日期：1998年5月29日 102（e）日期1998年5月29日PCT提交1996年10月4日PCT公布。公开号WO97 / 12869 日期：1997年04月10日式（1）的喹诺酮衍生物：其中A为低级亚烷基，R为H，卤素或低级烷氧基，R1和R2各自为低级烷基，任选被OH，低级烷氧基，苯基 - 低级烷氧基或低级烷酰氧基; 任选被OH，羟基 - 低级烷氧基或低级烷酰氧基取代的环烷基; 或氨基任选被低级烷基或环烷基取代，R 3是H，低级烷基，低级烯基或羟基 - 低级烷基，并且喹诺酮环的3-和4-位之间的键是单或双，条件是当R和 R3是H，R1和R2不应该是未取代的低级烷基或未取代的环烷基或其盐，其显示抗血栓形成活性，内膜增厚抑制活性，血小板质量分解活性和增加脑中血流的活性，外周血管，因此可用作预防或治疗各种缺血性疾病的药物。

7. 发明授权

US06133264A Carbostyril derivatives for inhibiting skin erythema and/or skin pigmentation 失效
标题翻译：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）。

8. 发明授权

US4663323A Tetrazole derivatives, anti-ulcer composition containing the same and method for treating ulcers 失效
标题翻译：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。

9. 发明授权

US07399864B2 Process for producing carbostyril derivatives 有权
标题翻译：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。

10. 发明授权

US5786367A Cyclic amide derivatives 失效
标题翻译：环状酰胺衍生物
公开(公告)号：US5786367A
公开(公告)日：1998-07-28
申请号：US600987
申请日：1996-03-05
申请人： Yasuo Oshiro , Tatsuyoshi Tanaka , Takao Nishi , Keiichi Kuwahara , Shigeki Fujisawa , Keiko Takasu , Yutaka Wada
发明人： Yasuo Oshiro , Tatsuyoshi Tanaka , Takao Nishi , Keiichi Kuwahara , Shigeki Fujisawa , Keiko Takasu , Yutaka Wada
IPC分类号： A61K8/49 , A61Q17/04 , C07D215/22 , C07D215/227 , C07D263/58 , C07D265/36 , C07D277/68 , C07D401/06 , C07D405/12 , C07D521/00 , C07F9/60 , A61K31/47
CPC分类号： C07D215/227 , A61K8/49 , A61K8/4926 , A61Q17/04 , C07D231/12 , C07D233/56 , C07D249/08 , C07D263/58 , C07D265/36 , C07D277/68 , C07D401/06 , C07D405/12 , C07F9/60
摘要： The present invention provides novel cyclic amide derivatives having activity for protecting against the ultraviolet rays, activity for scavenging active oxygen species and activity for inhibiting the formation of lipid peroxides, which is represented by the following general formula (1): ##STR1## wherein R.sup.2 is a hydroxyl group, a lower alkenyloxy group, a phenyl-lower alkenyloxy group, a cycloalkenyloxy group, a tetrahydropyranyloxy group, a pyridyloxy group, or a lower alkanoyloxy group which may have carboxyl group(s).
摘要翻译： PCT No.PCT / JP95 / 01392 Sec。 371日期：1996年3月5日 102（e）日期1996年3月5日PCT提交1995年7月12日PCT公布。公开号WO96 / 02508 日本1996年2月1日本发明提供了具有防紫外线活性，清除活性氧的活性和抑制脂质过氧化物形成活性的新型环状酰胺衍生物，由以下通式（1）表示：其中R2是可以具有羧基的羟基，低级链烯氧基，苯基 - 低级链烯氧基，环烯氧基，四氢吡喃氧基，吡啶氧基或低级烷酰氧基。

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