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1. 发明授权

US06174900B1 Substituted piperidine derivative for treating urinary disturbance 失效
标题翻译：用于治疗尿失禁的替代哌啶衍生物
公开(公告)号：US06174900B1
公开(公告)日：2001-01-16
申请号：US09332444
申请日：1999-06-14
申请人： Tomomi Okada , Fujiko Konno , Terumitsu Kaihoh , Masago Ishikawa , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
发明人： Tomomi Okada , Fujiko Konno , Terumitsu Kaihoh , Masago Ishikawa , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
IPC分类号： A61K31445
CPC分类号： C07D401/12 , C07D211/58 , C07D409/12
摘要： Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): wherein R1 means an aryl or heteroaryl group which may have at least one substituent, R2 denotes an alkyl, alkenyl or aralkyl group, R3 stands for a hydrogen atom or an alkyl group, and R4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.
摘要翻译：本文公开了由以下通式（1）表示的取代的哌啶衍生物：其中R 1表示可具有至少一个取代基的芳基或杂芳基，R 2表示烷基，烯基或芳烷基，R 3表示氢原子或烷基，可以具有至少一个取代基的芳基，杂芳基，芳烷基，芳烯基或杂芳烷基，或其盐。还公开了包含该化合物的药物。该化合物具有优异的抗胆碱能作用和钙拮抗作用并抑制反射膀胱收缩，因此可用于预防和治疗尿频紊乱如尿频。

2. 发明授权

US5968956A Substituted piperidine derivative and medicine comprising the same 失效
标题翻译：取代的哌啶衍生物及含有它们的药物
公开(公告)号：US5968956A
公开(公告)日：1999-10-19
申请号：US672058
申请日：1996-06-26
申请人： Tomomi Okada , Fujiko Konno , Terumitsu Kaihoh , Masago Ishikawa , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
发明人： Tomomi Okada , Fujiko Konno , Terumitsu Kaihoh , Masago Ishikawa , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
IPC分类号： C07D211/58 , C07D401/12 , C07D409/12 , A61K31/445 , C07D211/56
CPC分类号： C07D401/12 , C07D211/58 , C07D409/12
摘要： Disclosed herein is a substituted piperidine derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 means an aryl or heteroaryl group which may have at least one substituent, R.sup.2 denotes an alkyl, alkenyl or aralkyl group, R.sup.3 stands for a hydrogen atom or an alkyl group, and R.sup.4 is a hydrogen atom, an alkyl group, or an aryl, heteroaryl, aralkyl, aralkenyl or heteroaralkyl group which may have at least one substituent, or a salt thereof. A medicine including this compound is also disclosed. The compound has excellent anticholinergic effect and calcium antagonism and inhibits reflex bladder contraction and is hence useful for prophylaxis of and treatment for a urinary disturbance such as pollakiuria.
摘要翻译：本文公开了由以下通式（1）表示的取代的哌啶衍生物：其中R 1表示可具有至少一个取代基的芳基或杂芳基，R 2表示烷基，烯基或芳烷基，R 3表示氢原子或烷基，可以具有至少一个取代基的芳基，杂芳基，芳烷基，芳烯基或杂芳烷基，或其盐。还公开了包含该化合物的药物。该化合物具有优异的抗胆碱能作用和钙拮抗作用并抑制反射膀胱收缩，因此可用于预防和治疗尿频紊乱如尿频。

3. 发明授权

US6124347A Chromene derivatives and salts thereof, and pharmaceuticals containing the same 失效
标题翻译：色烯衍生物及其盐，以及含有它们的药物
公开(公告)号：US6124347A
公开(公告)日：2000-09-26
申请号：US162451
申请日：1998-09-29
申请人： Fumio Ishii , Haruyoshi Honda , Fujiko Konno , Tomomi Okada , Terumitsu Kaihoh , Yoshihiro Nagao , Susumu Sato , Hideaki Matsuda
发明人： Fumio Ishii , Haruyoshi Honda , Fujiko Konno , Tomomi Okada , Terumitsu Kaihoh , Yoshihiro Nagao , Susumu Sato , Hideaki Matsuda
IPC分类号： A61K31/35 , A61K31/352 , A61P3/08 , A61P3/10 , A61P43/00 , C07D311/58 , C07D311/64 , A61K31/353 , C07D311/60
CPC分类号： C07D311/58
摘要： Disclosed are chromene derivatives represented by the following formula: ##STR1## wherein R.sup.1 s represent alkyl, alkoxy or like groups, R.sup.2 represents a hydrogen atom or an alkyl group, R.sup.3 represents a substituted or unsubstituted phenyl, naphthyl or heterocyclic group, and m stands for an integer of from 0 to 4, and their salts; and pharmaceuticals containing them as effective ingredients. The chromene derivatives and their salts show excellent AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.
摘要翻译：公开了由下式表示的色烯衍生物：其中R 1表示烷基，烷氧基或类似基团，R 2表示氢原子或烷基，R 3表示取代或未取代的苯基，萘基或杂环基，m表示 0至4，及其盐; 和含有它们作为有效成分的药物。色烯衍生物及其盐显示优异的AGE形成抑制作用，并且可用作糖尿病并发症的预防剂和治疗剂。

4. 发明授权

US6060485A Arylacetic amide derivative or salt thereof, and pharmaceutical comprising it 失效
标题翻译：芳酰乙酰胺衍生物或其盐，以及包含它的药物
公开(公告)号：US6060485A
公开(公告)日：2000-05-09
申请号：US181091
申请日：1998-10-28
申请人： Terumitsu Kaihoh , Tomomi Okada , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato
发明人： Terumitsu Kaihoh , Tomomi Okada , Yoshinori Takahashi , Hiroyuki Mizuno , Haruyoshi Honda , Susumu Sato
IPC分类号： C07D211/58 , C07D211/94 , C07D401/12 , A61K31/445
CPC分类号： C07D401/12 , C07D211/58 , C07D211/94
摘要： Described is an arylacetic amide derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents an aryl group or the like, R.sup.2 and R.sup.3 each independently represents an alkyl group, a cycloalkyl group or the like, and R.sup.4 represents an aralkyl group, an alkyl group or the like; or salt thereof. The compound according to the present invention has both excellent anticholinergic action and calcium antagonism and at the same time has high selectivity to bladder, so that it is useful as a preventive or remedy for urinary disorders.
摘要翻译：描述了由下式（1）表示的芳基乙酰胺衍生物：其中R 1表示芳基等，R 2和R 3各自独立地表示烷基，环烷基等，R 4表示芳烷基，烷基等; 或其盐。根据本发明的化合物具有优异的抗胆碱能作用和钙拮抗作用，同时对膀胱具有高选择性，因此可用作尿障碍的预防或治疗方法。

5. 发明授权

US06958353B2 Imidazole derivatives or salts thereof and drugs containing the derivatives or the salts 失效
标题翻译：咪唑衍生物或其盐和含有衍生物或盐的药物
公开(公告)号：US06958353B2
公开(公告)日：2005-10-25
申请号：US10258610
申请日：2001-06-08
申请人： Fujiko Konno , Yoshihiro Nagao , Kazuo Isomae , Mari Ohtsuka , Yoshiyuki Takahashi , Fumio Ishii , Hiroyuki Hirota , Sunao Takeda , Noriyuki Kawamoto , Haruyoshi Honda , Susumu Sato
发明人： Fujiko Konno , Yoshihiro Nagao , Kazuo Isomae , Mari Ohtsuka , Yoshiyuki Takahashi , Fumio Ishii , Hiroyuki Hirota , Sunao Takeda , Noriyuki Kawamoto , Haruyoshi Honda , Susumu Sato
IPC分类号： A61P19/02 , A61P19/10 , A61P29/00 , A61P43/00 , C07D233/22 , C07D233/60 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D521/00 , A61K31/4178 , A61K31/444
CPC分类号： C07D401/14 , C07D231/12 , C07D233/22 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/14 , C07D409/14
摘要： The invention is directed to an imidazole derivative represented by formula (1): wherein each of R1 and R2 represents an aryl group, a heteroaryl group, etc.; each of A, X1, and X2 represents N or CH; each of Y and Z represents O, S, etc.; each of R3, R4, and R5 represents a hydrogen atom, an alkyl group, etc.; m is a number of 1 to 4; and n is a number of 0 to 4, or a salt thereof. The invention is also directed to a drug containing the derivative or the salt as an active ingredient. These compounds exert excellent effects of inhibiting production of NO and IL-6 and are useful for preventing or treating diseases induced by overproduction of NO and IL-6.
摘要翻译：本发明涉及由式（1）表示的咪唑衍生物：其中R 1和R 2各自表示芳基，杂芳基等; A，X 1和X 2各自表示N或CH; Y和Z各自表示O，S等; R 3，R 4和R 5各自表示氢原子，烷基等; m是1到4的数字; n为0〜4的数，或其盐。本发明还涉及含有衍生物或盐作为活性成分的药物。这些化合物具有抑制NO和IL-6产生的优异效果，可用于预防或治疗由过量产生NO和IL-6引起的疾病。

6. 发明授权

US5231101A Benzo[5,6]cyclohepta[1,2-B]pyridine derivatives and antiallergic agents comprising same 失效
标题翻译：苯并（5,6）环辛基（1,2-B）吡啶衍生物和包含其的抗菌剂
公开(公告)号：US5231101A
公开(公告)日：1993-07-27
申请号：US821803
申请日：1992-01-17
申请人： Haruyoshi Honda , Hiroyuki Mizuno , Kinichi Mogi , Yoshikuni Ito , Yasushi Kaneko , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
发明人： Haruyoshi Honda , Hiroyuki Mizuno , Kinichi Mogi , Yoshikuni Ito , Yasushi Kaneko , Naokata Taido , Susumu Sato , Tadayuki Kuraishi
IPC分类号： A61K31/445 , A61K31/4427 , A61P37/08 , A61P43/00 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04
摘要： Benzo[5,6]cyclohepta[1,2-b]pyridine derivatives of the following formula: ##STR1## wherein R.sup.1 represents a cyano, carbamoyl, alkylsulfoxy, alkylsulfonyl, tetrazolyl or sulfonic acid group, and R.sup.2 represents a hydrogen atom, a cyano, phenyl, aralkyl, alkoxycarbonylalkyl, aminoalkylcarbamoylalkyl or lower alkyl group, or a group ##STR2## or --X--R.sub.4, X being an oxygen or sulfur atom, R.sup.3 standing for a hydrogen atom or a substituted or unsubstituted lower alkyl, phenyl or aralkyl group, and R.sup.4 being a substituted or unsubstituted lower alkyl, phenyl or aralkyl group or an aminoalkyl group, and salts thereof. Antiallergic and antihistamic agents containing one of the above derivatives or salts as an active ingredient are also described.

7. 发明授权

US5710152A Benzoazine derivative or salt thereof and pharmaceutical compostion comprising the same 失效
标题翻译：苯并嗪衍生物或其盐和包含其的药物组合物
公开(公告)号：US5710152A
公开(公告)日：1998-01-20
申请号：US791269
申请日：1997-01-30
申请人： Yoshihiro Nagao , Yoshikuni Ito , Jiro Kotake , Tadayuki Kouda , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
发明人： Yoshihiro Nagao , Yoshikuni Ito , Jiro Kotake , Tadayuki Kouda , Haruyoshi Honda , Susumu Sato , Hideaki Matsuda
IPC分类号： C07D417/12 , A61K31/505 , A61K31/535 , A61K31/54
CPC分类号： C07D417/12
摘要： A benzoazine derivative represented by the following formula (1), ##STR1## wherein R.sup.1 represents an alkyl group, alkoxy group, halogen atom, halogenoalkyl group, amino group, hydroxy group, benzyloxy group which may have a substituent, cyano group, carbamoyl group, acyl group, nitro group, carboxy group, or sulfonamide group; R.sup.2 and R.sup.3 may be the same or different and each individually represents a hydrogen atom or an alkyl group, or R.sup.2 and R.sup.3 indicate in combination an alkylene group having 2-7 carbon atoms; R.sup.4 and R.sup.5 may be the same or different and each individually represents a hydrogen atom or an alkyl group; X denotes O, S, or N--R.sup.6 (wherein R.sup.6 represents a hydrogen atom, an alkyl group, or an aryl group or pyridyl group which may have a substituent); m is an integer from 0 to 4; and n is an integer from 1 to 3, or a salt of the benzoazine derivative. The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, and is useful as a medicament for preventing or treating diabetes, hyperlipidemia, and obesity.
摘要翻译：由下式（1）表示的苯并嗪衍生物，其中R1表示烷基，烷氧基，卤素原子，卤代烷基，氨基，羟基，可具有取代基的苄氧基，氰基，氨基甲酰基，酰基，硝基，羧基或磺酰胺基; R2和R3可以相同或不同，各自独立地表示氢原子或烷基，或R2和R3组合表示具有2-7个碳原子的亚烷基; R 4和R 5可以相同或不同，各自独立地表示氢原子或烷基; X表示O，S或N-R6（其中R6表示氢原子，烷基或可具有取代基的芳基或吡啶基）; m为0〜4的整数; n为1〜3的整数，或苯并嗪衍生物的盐。该化合物对于降低血糖值，血浆胰岛素值和血浆甘油三酯值具有优异的效果，并且可用作预防或治疗糖尿病，高脂血症和肥胖症的药物。

8. 发明授权

US4866176A 8-Piperazinyl-1,7-naphthyridine derivative having pharmaceutical activity 失效
标题翻译：具有药物活性的8-哌嗪基-1,7-萘啶衍生物
公开(公告)号：US4866176A
公开(公告)日：1989-09-12
申请号：US84836
申请日：1987-08-13
申请人： Haruyoshi Honda , Yuko Yoshida , Tadayuki Kouda , Hideaki Matsuda , Tatsuhiko Katori
发明人： Haruyoshi Honda , Yuko Yoshida , Tadayuki Kouda , Hideaki Matsuda , Tatsuhiko Katori
IPC分类号： A61K31/495 , A61P9/04 , A61P9/06 , A61P25/04 , A61P29/00 , C07D471/04
CPC分类号： C07D471/04
摘要： A 8-piperazinyl-1,7-naphthyridine derivative represented by the following formula (I): ##STR1## in which R represents a hydrogen atom, formyl group, acyl group, aroyl group, heteroaroyl group, substituted phenyl group, pyridyl group, aralkyl group or substituted or unsubstituted benzenesulfonyl group; and an acid adduct salt thereof. The compound has excellent antiinflammatory, antiarrhythmic and cardiotonic effects, and thus is useful as an antiinflammatory drug and a medicine for circulatory organs.

9. 发明授权

US6028081A Substituted quinolone derivatives and pharmaceuticals containing the same 失效
标题翻译：取代的喹诺酮衍生物和含有它们的药物
公开(公告)号：US6028081A
公开(公告)日：2000-02-22
申请号：US141374
申请日：1998-08-27
申请人： Yoshihisa Sada , Shigeru Adegawa , Kinichi Mogi , Haruyoshi Honda , Hiromichi Eto , Shinichi Morimoto , Junji Okawa , Norimitsu Umehara , Susumu Sato
发明人： Yoshihisa Sada , Shigeru Adegawa , Kinichi Mogi , Haruyoshi Honda , Hiromichi Eto , Shinichi Morimoto , Junji Okawa , Norimitsu Umehara , Susumu Sato
IPC分类号： A61K31/47 , A61K31/495 , A61K31/535 , A61P1/04 , A61P31/04 , C07D215/42 , C07D215/44 , C07D215/46 , C07D401/04 , C07D501/12 , A61K31/55 , C07D215/16
CPC分类号： C07D401/04 , C07D215/42 , C07D215/44 , C07D215/46
摘要： Substituted quinolone derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted (hetero)aryl group, R.sup.2 represents H or an alkoxycarbonyl, substituted aminocarbonyl, cyano or like group, and R.sup.3 and R.sup.4 each independently represent H or a substituted alkyl, aryl, amino or like group, and salts thereof; pharmaceuticals containing the same. These derivatives and salts have excellent anti-ulcer activities.
摘要翻译：由下式表示的取代喹诺酮衍生物：其中R1表示取代或未取代的（杂）芳基，R2表示H或烷氧基羰基，取代氨基羰基，氰基或类似基团，R3和R4各自独立地表示H或取代的烷基，芳基，氨基或类似基团，及其盐; 含有相同药物。这些衍生物和盐具有优异的抗溃疡活性。

10. 发明授权

US4659710A 1,7-Naphthyridine derivatives and pharmaceutical compositions 失效
标题翻译： 1,7-萘啶衍生物和药物组合物
公开(公告)号：US4659710A
公开(公告)日：1987-04-21
申请号：US850820
申请日：1986-04-11
申请人： Susumu Sato , Haruyoshi Honda , Teruo Koumoto , Kazuo Isomae , Tadayuki Kuraishi , Tatsuhiko Katori
发明人： Susumu Sato , Haruyoshi Honda , Teruo Koumoto , Kazuo Isomae , Tadayuki Kuraishi , Tatsuhiko Katori
IPC分类号： A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61P7/10 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/12 , A61P11/00 , A61P11/08 , A61P25/02 , A61P25/04 , A61P29/00 , C07D471/04 , A61K31/535 , C07D221/00 , C07D413/14
CPC分类号： C07D471/04
摘要： Certain 1,7-naphthyridine derivatives and their acid addition salts have strong antiarrhythmic effects, cardiotonic effects, diuretic effects, bronchodilation effects, anti-acetylcholine effects, anti-inflammatory effects, analgesic effects and the like and are hence useful for various diseases such as heart diseases, hypertension, asthma, arthritis, lumbago, toothache, etc.
摘要翻译：某些1,7-萘啶衍生物及其酸加成盐具有强烈的抗心律失常作用，强心作用，利尿作用，支气管扩张作用，抗乙酰胆碱作用，抗炎作用，镇痛作用等，因此可用于各种疾病如心脏病，高血压，哮喘，关节炎，腰痛，牙痛等。

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