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1. 发明授权

US6071943A Imidazole derivative and medicine comprising the same as active ingredient 失效
标题翻译：咪唑衍生物和包含与活性成分相同的药物
公开(公告)号：US6071943A
公开(公告)日：2000-06-06
申请号：US200750
申请日：1998-11-30
申请人： Noriaki Shioiri , Tadashi Mikami , Shinichi Morimoto , Kazuo Yamazaki , Hiroyuki Naito , Junji Okawa , Noriyuki Kawamoto , Hiroshi Hasegawa , Koichi Tachibana , Susumu Sato , Toshio Yokoyama
发明人： Noriaki Shioiri , Tadashi Mikami , Shinichi Morimoto , Kazuo Yamazaki , Hiroyuki Naito , Junji Okawa , Noriyuki Kawamoto , Hiroshi Hasegawa , Koichi Tachibana , Susumu Sato , Toshio Yokoyama
IPC分类号： C07D233/54 , C07D233/64 , C07D233/70 , C07D405/12 , A01N43/50
CPC分类号： C07D233/64 , C07D405/12
摘要： Disclosed herein are an imidazole derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom, or an alkyl, alkoxy or alkoxycarbonyl group, and R.sup.2, R.sup.3 and R.sup.4 are the same or different from one another and are independently a hydrogen or halogen atom, an alkyl, halogenoalkyl, hydroxyl or alkoxy group, or the like, or a salt thereof, and a medicine comprising such a compound. The compound specifically suppresses the production of particular cytokine and is hence useful as an active ingredient for immune function modulators and the like.
摘要翻译：本文公开了由以下通式（1）表示的咪唑衍生物：其中R1是氢原子或烷基，烷氧基或烷氧基羰基，R2，R3和R4彼此相同或不同，独立地为氢或卤素原子，烷基，卤代烷基，羟基或烷氧基等，或其盐，以及包含这种化合物的药物。该化合物特别抑制特定细胞因子的产生，因此可用作免疫功能调节剂等的活性成分。

2. 发明授权

US6046218A Pyridine derivative and medicament containing the same as an effective ingredient 失效
标题翻译：吡啶衍生物和含有与有效成分相同的药物
公开(公告)号：US6046218A
公开(公告)日：2000-04-04
申请号：US952072
申请日：1997-11-17
申请人： Hiroshi Hasegawa , Tadashi Mikami , Koichi Tachibana , Kazuo Yamazaki , Noriyuki Kawamoto , Noriaki Shioiri , Koji Kusano , Susumu Sato , Hideaki Matsuda , Toshio Yokoyama
发明人： Hiroshi Hasegawa , Tadashi Mikami , Koichi Tachibana , Kazuo Yamazaki , Noriyuki Kawamoto , Noriaki Shioiri , Koji Kusano , Susumu Sato , Hideaki Matsuda , Toshio Yokoyama
IPC分类号： C07D213/69 , C07D405/06 , C07D409/06 , A61K31/435 , A61K31/44 , C07D211/72
CPC分类号： C07D213/69 , C07D405/06 , C07D409/06 , Y10S514/885
摘要： Described is a pyridine derivative represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 individually represent H, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkoxyalkyl group which may have a substituent, a carboxyalkyl group, an alkoxycarbonylalkyl group, an aralkyl group which may have a substituent, a phenacyl group or an acyl group, R.sup.3 represents an alkyl group, a phenyl group which may have a substituent, a heteroaryl group or a cyclic amino group, X represents O or combination of OH and H, or a salt thereof; and a medicament, such as cytokine production suppressant, comprising the derivative or salt thereof as an effective ingredient. The invention compound has potential, highly specific and highly safe immunoregulating capacity so that it can suppress the excessive production of a specific cytokine in various diseases related to the immune system.
摘要翻译： PCT No.PCT / JP97 / 00712 Sec。 371日期：1997年11月17日 102（e）日期1997年11月17日PCT 1997年3月7日PCT公布。出版物WO97 / 33870 PCT 日期：1997年9月18日是由下式（1）表示的吡啶衍生物：其中R1和R2分别表示H，烷基，环烷基，羟烷基，可具有取代基的烷氧基烷基，羧基烷基烷氧基羰基烷基，可具有取代基的芳烷基，苯甲酰甲酰基或酰基，R3表示烷基，可具有取代基的苯基，杂芳基或环状氨基，X表示O 或OH和H的组合或其盐; 以及包含其衍生物或其盐作为有效成分的药物，例如细胞因子产生抑制剂。本发明化合物具有潜在的，高度特异性和高度安全的免疫调节能力，从而可以抑制与免疫系统相关的各种疾病中特定细胞因子的过量产生。

3. 发明授权

US5935977A Substituted vinyl pyridine derivative and drugs containing the same 失效
标题翻译：取代的乙烯基吡啶衍生物和含有它的药物
公开(公告)号：US5935977A
公开(公告)日：1999-08-10
申请号：US68986
申请日：1998-05-26
申请人： Kazuo Yamazaki , Yoichiro Ogawa , Hidehiko Kohya , Tadashi Mikami , Noriyuki Kawamoto , Noriaki Shioiri , Hiroshi Hasegawa , Susumu Sato
发明人： Kazuo Yamazaki , Yoichiro Ogawa , Hidehiko Kohya , Tadashi Mikami , Noriyuki Kawamoto , Noriaki Shioiri , Hiroshi Hasegawa , Susumu Sato
IPC分类号： C07D213/69 , C07D401/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D417/14 , A61K31/44
CPC分类号： C07D213/69 , C07D401/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D417/14
摘要： The present invention relates to a substituted vinylpyridine derivative represented by the following formula (1): ##STR1## (wherein R.sup.1 represents a hydrogen atom, an alkyl group, etc., R.sup.2 represents an alkyl group; one of R.sup.3 and R.sup.4, which are different from each other, represents a hydrogen atom and the other represents a nitrile group, R.sup.5 represents an aryl group or a heteroaryl group, X represents an oxygen atom, etc., and one of Q.sup.1, Q.sup.2, and Q.sup.3 represents a nitrogen atom and the other two represent CH); a salt of the derivative; and a drug containing the derivative or salt as the active ingredient. Due to strong PDE inhibitory action and TNF-.alpha. production inhibitory action, the derivative, salt, and drug are useful for the prevention and treatment of a wide variety of inflammatory diseases and autoimmune diseases.
摘要翻译： PCT No.PCT / JP97 / 03354 Sec。 371日期：1998年5月26日 102（e）日期1998年5月26日PCT 1997年9月22日PCT公布。公开号WO98 / 13348 日期：1998年4月2日本发明涉及由下式（1）表示的取代乙烯基吡啶衍生物：其中，R1表示氢原子，烷基等，R2表示烷基，R3和R4之一，彼此不同，表示氢原子，另一个表示腈基，R 5表示芳基或杂芳基，X表示氧原子等，Q 1，Q 2和Q 3中的一个表示氮原子，另外两个表示CH）; 衍生物的盐; 和含有衍生物或盐的活性成分的药物。由于强烈的PDE抑制作用和TNF-α产生抑制作用，衍生物，盐和药物可用于预防和治疗各种炎性疾病和自身免疫性疾病。

4. 发明授权

US5190951A Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US5190951A
公开(公告)日：1993-03-02
申请号：US773432
申请日：1991-10-09
申请人： Hiroshi Hasegawa , Kazuo Isomae , Takeshi Kotsugai , Noriaki Shioiri , Kumiko Sekine , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
发明人： Hiroshi Hasegawa , Kazuo Isomae , Takeshi Kotsugai , Noriaki Shioiri , Kumiko Sekine , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
IPC分类号： C07D219/06 , C07D221/16 , C07D401/06 , C07D471/04
CPC分类号： C07D401/06 , C07D219/06 , C07D221/16 , C07D471/04
摘要： Quinoline derivatives of the formula, ##STR1## wherein > A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior antiacetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

5. 发明授权

US5300517A Piperidine compounds having anti-acetylcholinesterase activity 失效
标题翻译：具有抗乙酰胆碱酯酶活性的哌啶化合物
公开(公告)号：US5300517A
公开(公告)日：1994-04-05
申请号：US53202
申请日：1993-04-28
申请人： Hiroshi Hasegawa , Kazuo Isomae , Takeshi Kotsugai , Noriaki Shioiri , Kumiko Sekine , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
发明人： Hiroshi Hasegawa , Kazuo Isomae , Takeshi Kotsugai , Noriaki Shioiri , Kumiko Sekine , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
IPC分类号： C07D219/06 , C07D221/16 , C07D401/06 , C07D471/04 , A61K31/445 , C07D401/04
CPC分类号： C07D401/06 , C07D219/06 , C07D221/16 , C07D471/04
摘要： Piperidine compounds of formula II: ##STR1## that exhibit anticholinesterase activity and are effective in treating dementia.
摘要翻译：具有抗胆碱酯酶活性并有效治疗痴呆的式II的哌啶化合物：IMAGE（II）。

6. 发明授权

US5240934A Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US5240934A
公开(公告)日：1993-08-31
申请号：US946620
申请日：1992-09-18
申请人： Hiroshi Hasegawa , Kazuo Isomae , Takeshi Kotsugai , Noriaki Shioiri , Kumiko Sekine , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
发明人： Hiroshi Hasegawa , Kazuo Isomae , Takeshi Kotsugai , Noriaki Shioiri , Kumiko Sekine , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
IPC分类号： C07D219/06 , C07D221/16 , C07D401/06 , C07D471/04
CPC分类号： C07D401/06 , C07D219/06 , C07D221/16 , C07D471/04
摘要： Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.
摘要翻译：其中> A表示基团> N-（CH 2）n - ，> C = C = CH（CH 2）n - 或> CH（CH 2）n - ，其中n为 0-7的整数; Y表示C = O或> CHOH基团，R1表示氢原子，卤素原子，烷基，烷氧基或烷硫基，R2表示氢原子，卤原子，烷基，羟基，烷氧基，可以具有取代基的苯基，苯氧基，烷酰氧基或可以具有取代基的氨基，R3是氢原子，卤素原子，烷基或烷氧基，m为1-3的整数。化合物及其盐具有优异的抗乙酰胆碱酯酶活性，无副作用，对预防或治愈老年痴呆或记忆障碍有效。

7. 发明授权

US4977275A Pyrrole derivatives 失效
标题翻译：吡咯衍生物
公开(公告)号：US4977275A
公开(公告)日：1990-12-11
申请号：US333239
申请日：1989-04-05
申请人： Hiroshi Hasegawa , Kinichi Mogi , Noriaki Shioiri , Susumu Sato , Tatsuhiko Katori
发明人： Hiroshi Hasegawa , Kinichi Mogi , Noriaki Shioiri , Susumu Sato , Tatsuhiko Katori
IPC分类号： A61K31/40 , A01N43/36 , A61K31/4025 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61P17/00 , C07D207/34 , C07D401/12 , C07D409/12
CPC分类号： C07D207/34
摘要： A pyrrole derivative having excellent anti-microbial activities is disclosed. This compound is represented by the following formula (I): ##STR1## wherein X.sub.1 and X.sub.2 are the same or different and mean individually a halogen atom, R.sub.1 denotes an alkyl, cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl group or a group --COR.sub.3 in which R.sub.3 is an alkyl group having at least five carbon atoms or a cycloalkyl, haloalkyl, alkenyl, substituted or unsubstituted phenyl, substituted or unsubstituted aralkyl, or heterocyclic group, and R.sub.2 stands for a hydrogen or halogen atom or an alkyl group, with a proviso that R.sub.1 is other than a hydrogen atom or methyl group when X.sub.1, X.sub.2 and R.sub.2 are each a bromine atom.

8. 发明授权

US4876359A Novel gamma-butyrolactone derivatives 失效
标题翻译：新型γ-丁内酯衍生物
公开(公告)号：US4876359A
公开(公告)日：1989-10-24
申请号：US103415
申请日：1987-10-01
申请人： Hiroshi Hasegawa , Noriaki Shioiri , Tadashi Narita , Tatsuhiko Katori
发明人： Hiroshi Hasegawa , Noriaki Shioiri , Tadashi Narita , Tatsuhiko Katori
IPC分类号： C07K5/02
CPC分类号： C07K5/0222
摘要： Novel .gamma.-butyrolactone derivatives having strong ACE inhibitory activity are provided. They are represented by the following general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and mean individually a hydrogen atom or a straight-chain or branched alkyl or cycloalkyl group, or R.sup.1 and R.sup.2 are bonded together to mean an alkylene group having 2-6 carbon atoms, R.sup.3 denotes a hydrogen atom or a lower alkyl, aralkyl, amino lower alkyl or lower alkoxycarbonylamino lower alkyl group, R.sup.4 means a lower alkyl, cycloalkyl or aralkyl group, R.sup.5 means a hydrogen atom or a lower alkyl group, or R.sub.4 and R.sub.5 are bonded together to denote an alkylene group having 2-4 carbon atoms, and R.sup.6 stands for a hydrogen atom or a lower alkyl or aralkyl group; or a pharmacologically acceptable salt thereof.
摘要翻译：提供了具有强ACE抑制活性的新型γ-丁内酯衍生物。它们由以下通式（I）表示：其中R 1和R 2可以相同或不同，并且分别表示氢原子或直链或支链烷基或环烷基，或者R1和R2 键合在一起表示具有2-6个碳原子的亚烷基，R3表示氢原子或低级烷基，芳烷基，氨基低级烷基或低级烷氧基羰基氨基低级烷基，R4表示低级烷基，环烷基或芳烷基，R5表示氢原子或低级烷基，或者R4和R5键合在一起，表示具有2-4个碳原子的亚烷基，R6代表氢原子或低级烷基或芳烷基; 或其药理学上可接受的盐。

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