专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US5981557A Aminothiazole derivative, medicament containing the same, and intermediate for preparation of said compound 失效
标题翻译：氨基噻唑衍生物，含有该氨基噻唑衍生物的药物和用于制备所述化合物的中间体
公开(公告)号：US5981557A
公开(公告)日：1999-11-09
申请号：US952106
申请日：1997-11-18
申请人： Masaaki Nagasawa , Masakazu Murata , Hiroyasu Nishioka , Tadashi Kurimoto , Shigeru Ueki , Osamu Kitagawa
发明人： Masaaki Nagasawa , Masakazu Murata , Hiroyasu Nishioka , Tadashi Kurimoto , Shigeru Ueki , Osamu Kitagawa
IPC分类号： C07D277/56 , C07D417/12 , C07D521/00 , A61K31/425
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/56 , C07D417/12
摘要： The present invention relates to an aminothiazole derivative represented by the following formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represents a hydrogen atom, a hydroxy group, a lower alkyl group, a lower alkoxy group or the like; R.sup.4 represents a hydrogen atom or a lower alkyl group; R.sup.5 represents a hydrogen atom, a halogen atom or a lower alkyl group; m stands for an integer of 0 to 4, A represents a substituted amino group, a substituted imino group, a heterocyclic group or the like; and B stands for an imino group or an oxygen atom, a medicament containing it and an intermediate for the preparation of said compound. The compound has strong restoration effects on dysmotility in the gastrointestinal tract and at the same time has high safety so that it is useful as an excellent gastroprokinetic.
摘要翻译： PCT No.PCT / JP96 / 01297 Sec。 371日期：1997年11月18日 102（e）1997年11月18日日期PCT提交1996年5月16日PCT公布。第WO96 / 36619号公报日期：1996年11月21日本发明涉及由下式（I）表示的氨基噻唑衍生物：其中R1，R2和R3各自独立地表示氢原子，羟基，低级烷基，低级烷氧基或喜欢; R4代表氢原子或低级烷基; R5表示氢原子，卤素原子或低级烷基; m表示0〜4的整数，A表示取代氨基，取代亚氨基，杂环基等， B代表亚氨基或氧原子，含有它的药物和制备所述化合物的中间体。该化合物对胃肠道运动障碍具有很强的恢复作用，同时具有较高的安全性，因此作为优良的胃动力学有用。

2. 发明授权

US06562373B2 Colonic motor dysfunction remedies comprising aminothiazole derivatives as active ingredients 有权
标题翻译：包含氨基噻唑衍生物作为活性成分的结肠运动功能障碍疗法
公开(公告)号：US06562373B2
公开(公告)日：2003-05-13
申请号：US09853746
申请日：2001-05-14
申请人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
发明人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
IPC分类号： A61K3136
CPC分类号： A61K31/426 , A61K31/381
摘要： Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.
摘要翻译：治疗有助于改善结肠运动功能障碍，如肠易激综合征，便秘或肠痛，而不会对中枢神经系统造成副作用。这些结肠运动障碍疗法包括作为活性成分的由下式（I）表示的氨基噻唑衍生物或其盐或水合物：其中R1，R2和R3可以相同或不同，并且各自独立地表示氢原子或羟基，低级烷基，低级烷氧基，氨基，硝基或氰基，R 4和R 5可以相同或不同，各自独立地表示氢原子或低级烷基，n表示2〜4的整数。

3. 发明授权

US06673368B2 Colonic motor dysfunction remedies comprising aminothiazole derivatives as active ingredients 有权
标题翻译：包含氨基噻唑衍生物作为活性成分的结肠运动功能障碍疗法
公开(公告)号：US06673368B2
公开(公告)日：2004-01-06
申请号：US09853746
申请日：2001-05-14
申请人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
发明人： Shigeru Ueki , Yuko Hori , Yugo Matsunaga , Masaaki Nagasawa , Hiroyasu Nishioka , Masakazu Murata
IPC分类号： A61K3136
CPC分类号： A61K31/426 , A61K31/381
摘要： Remedies effective for the improvement of colonic motor dysfunction such as irritable bowel syndrome, constipation or intestinal atony without causing side effects on the central nerve system. These colonic motor dysfunction remedies comprise, as active ingredients, aminothiazole derivatives represented by the following formula (I) or a salt or hydrate thereof: wherein R1, R2 and R3 may be the same or different and each independently represent a hydrogen atom or a hydroxyl, lower alkyl, lower alkoxy, amino, nitro or cyano group, R4 and R5 may be the same or different and each independently represent a hydrogen atom or a lower alkyl group, and n stands for an integer of from 2 to 4.
摘要翻译：治疗有助于改善结肠运动功能障碍，如肠易激综合征，便秘或肠痛，而不会对中枢神经系统造成副作用。作为活性成分，这些结肠运动障碍疗法包含由下式（I）表示的氨基噻唑衍生物或其盐或水合物：其中R 1，R 2和R 3可以相同或不同，各自独立地表示氢原子或羟基，低级烷基，低级烷氧基，氨基，硝基或氰基，R 4和R 5可以相同或不同，各自独立地表示氢原子或低级烷基，n表示2〜4的整数。

4. 发明授权

US6121301A Substituted benzoylaminothiazole derivatives and drugs containing the same 有权
标题翻译：取代苯甲酰氨基噻唑衍生物和含有它们的药物
公开(公告)号：US6121301A
公开(公告)日：2000-09-19
申请号：US284477
申请日：1999-04-21
申请人： Masaaki Nagasawa , Kenji Sato , Tadashi Kurimoto , Shigeru Ueki
发明人： Masaaki Nagasawa , Kenji Sato , Tadashi Kurimoto , Shigeru Ueki
IPC分类号： C07D277/46 , C07D277/56 , C07D417/12 , A61K31/425
CPC分类号： C07D417/12 , C07D277/46 , C07D277/56
摘要： The present invention relates to a substituted benzoylaminothiazole derivative represented by the following formula (I): ##STR1## wherein X represents an imino group which may be substituted by a lower alkyl group, or an oxygen atom, R.sup.1 represents a cyano group, a lower alkoxycarbonyl group, a lower alkoxycarbonylamino group, a lower alkylsulfonylamino group, a lower alkanoyl or lower alkylsulfonyl group which may be substituted by a halogen atom, a 1-ureido group, a halo-substituted lower alkyl group or a 2-pyrrolylimino group, R.sup.2 and R.sup.3 are the same or different and each independently represents a hydrogen atom or a lower alkyl group and m stands for an integer of 2 to 4, or a salt thereof; and a medicament comprising the compound as an effective ingredient. The compound of the invention is useful as a preventive and therapeutic agent for epigastric dyscomfort, nausea, vomiting, heartburn, anorexia, bellyache, abdominal flatulence, chronic gastritis or the like.
摘要翻译： PCT No.PCT / JP97 / 03774 Sec。 371 1999年4月21日第 102（e）1999年4月21日PCT PCT 1997年10月20日PCT公布。公开号WO98 / 17654 日期：1998年04月30日本发明涉及由下式（I）表示的取代苯甲酰氨基噻唑衍生物：其中X表示可被低级烷基或氧原子取代的亚氨基，R 1表示氰基，低级烷氧基羰基，低级烷氧基羰基氨基，低级烷基磺酰基氨基，可被卤素原子取代的低级烷酰基或低级烷基磺酰基，1-脲基，卤代低级烷基或2-吡咯基咪唑基，R2和R3相同或不同，各自独立地表示氢原子或低级烷基，m表示2〜4的整数，或其盐; 以及包含该化合物作为有效成分的药物。本发明的化合物可用作上腹部不适，恶心，呕吐，胃灼热，厌食，腹痛，腹胀气，慢性胃炎等的预防和治疗剂。

5. 发明授权

US06884810B2 Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US06884810B2
公开(公告)日：2005-04-26
申请号：US10380158
申请日：2002-09-18
申请人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Yutaka Shinozaki , Hitoshi Morita
发明人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Yutaka Shinozaki , Hitoshi Morita
IPC分类号： A61K31/4439 , A61P1/04 , C07D401/12
CPC分类号： C07D401/12 , A61K31/4439
摘要： A benzimidazole derivative of formula (1): (wherein R represents a hydrogen atom or a methoxy group, and n is 0 or 1) or a salt thereof; and a medicament containing the same. The compounds of the present invention, due to minimized difference in therapeutic effect between subjects, which difference would otherwise be derived from different CYP2C19 activity from subject to subject, ensure that all patients can enjoy proper therapeutic effects at the same dose of the drug. Also, the compounds of the invention have low risk of drug interaction caused by induction of CYP1A family member enzymes, as well as low risk of development of cancer, and thus is useful as a remedy for peptic ulcer, reliably providing therapeutic effects with safety.
摘要翻译：式（1）的苯并咪唑衍生物：其中R表示氢原子或甲氧基，n为0或1;或其盐; 和含有该药物的药物。本发明的化合物由于受试者之间治疗效果的差异最小化，否则从受试者到受试者的不同CYP2C19活性的差异将确保所有患者在相同剂量的药物中可以获得适当的治疗效果。此外，本发明的化合物由CYP1A家族成员酶的诱导引起的药物相互作用的风险低，并且癌症发展的风险低，因此可用作消化性溃疡的补救剂，可靠地提供安全的治疗效果。

6. 发明授权

US06197970B1 Process for producing 2-hydroxybenzamide derivatives 有权
标题翻译： 2-羟基苯甲酰胺衍生物的制备方法
公开(公告)号：US06197970B1
公开(公告)日：2001-03-06
申请号：US09446108
申请日：1999-12-23
申请人： Masaaki Nagasawa , Hiroyasu Nishioka , Takanori Suzuki , Eiichi Nagano , Katsuyuki Ishii , Ryu Nakao
发明人： Masaaki Nagasawa , Hiroyasu Nishioka , Takanori Suzuki , Eiichi Nagano , Katsuyuki Ishii , Ryu Nakao
IPC分类号： C07D27756
CPC分类号： C07D277/56
摘要： The present invention is directed to a process for producing 2-hydroxybenzamide derivatives (2) or (5) according to either one of the following reaction schemes.
摘要翻译：本发明涉及根据以下反应方案之一制备2-羟基苯甲酰胺衍生物（2）或（5）的方法。

7. 发明申请

US20050148634A1 1-N-Aminobenzimidazole derivatives 审中-公开
标题翻译： 1-N-氨基苯并咪唑衍生物
公开(公告)号：US20050148634A1
公开(公告)日：2005-07-07
申请号：US10507361
申请日：2003-03-28
申请人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Hideki Nakamura , Hitoshi Morita
发明人： Masaaki Nagasawa , Hiroyasu Nishioka , Kazuyasu Asami , Naoyoshi Miura , Hideki Nakamura , Hitoshi Morita
IPC分类号： A61P1/04 , A61P43/00 , C07D401/12 , A61K31/4439 , C07D43/02
CPC分类号： C07D401/12 , C07D471/04 , C07D495/04
摘要： Provided are 1-N-aminobenzimidazole derivatives represented by the following formula (I): wherein R1 and R2 each represents a substituted or unsubstituted alkyl group or the like, R3, R5 and R6 each represents an alkyl group, alkoxy group, hydrogen atom or the like, R4 represents a substituted or unsubstituted alkyl group or the like, A represents a benzene ring or the like, B represents a hydrogen atom or the like, an n stands for an integer of from 0 to 2, or salts thereof; and medicines containing them. The compounds (I) according to the present invention do not bring about much individual differences in therapeutic effects despite the existence of individual differences in the CYP2C19 activity. At the same dose, they can hence bring about appropriate therapeutic effects for all patients. In addition, they are low in the risk of induction of an interaction or a cancer caused by induction of the CYP1A family. Accordingly, they are useful as peptic ulcer therapeutic agents which are safe and surely bring about therapeutic effects.
摘要翻译：提供由下式（I）表示的1-N-氨基苯并咪唑衍生物：其中R 1和R 2各自表示取代或未取代的烷基等，R R 5，R 5和R 6各自表示烷基，烷氧基，氢原子等，R 4， SUP>表示取代或未取代的烷基等，A表示苯环等，B表示氢原子等，n表示0〜2的整数，或其盐; 和含有它们的药物。尽管CYP2C19活性存在个体差异，但是本发明的化合物（I）不会在治疗效果上产生太多的个体差异。在相同剂量下，它们可以为所有患者带来适当的治疗效果。此外，它们诱导由CYP1A家族诱导引起的相互作用或癌症的风险较低。因此，它们可用作消化性溃疡治疗剂，其是安全的并且确实具有治疗效果。

8. 发明授权

US07276511B2 Benzylamine derivative 有权
标题翻译：苄胺衍生物
公开(公告)号：US07276511B2
公开(公告)日：2007-10-02
申请号：US10566252
申请日：2004-08-02
申请人： Masaaki Nagasawa , Nobuo Kawase , Nobuyuki Tanaka , Hideki Nakamura , Naoki Tsuzuike , Masakazu Murata
发明人： Masaaki Nagasawa , Nobuo Kawase , Nobuyuki Tanaka , Hideki Nakamura , Naoki Tsuzuike , Masakazu Murata
IPC分类号： A61K31/438 , C07D495/10
CPC分类号： C07D471/10 , A61K31/438 , A61K31/451 , C07D211/58
摘要： The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof
摘要翻译：本发明提供了对NK-1受体或NK-2受体表现出令人满意的口服吸收性和优异的拮抗活性的化合物。该化合物是由式（1）表示的苄胺衍生物或其盐

9. 发明申请

US20060194841A1 Benzylamine derivative 有权
标题翻译：苄胺衍生物
公开(公告)号：US20060194841A1
公开(公告)日：2006-08-31
申请号：US10566252
申请日：2004-08-02
申请人： Masaaki Nagasawa , Nobuo Kawase , Nobuyuki Tanaka , Hideki Nakamura , Naoki Tsuzuike , Masakazu Murata
发明人： Masaaki Nagasawa , Nobuo Kawase , Nobuyuki Tanaka , Hideki Nakamura , Naoki Tsuzuike , Masakazu Murata
IPC分类号： A61K31/445 , C07D211/68 , C07D401/02 , A61K31/4545 , A61K31/453
CPC分类号： C07D471/10 , A61K31/438 , A61K31/451 , C07D211/58
摘要： The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof.
摘要翻译：本发明提供了对NK-1受体或NK-2受体表现出令人满意的口服吸收性和优异的拮抗活性的化合物。该化合物是由式（1）表示的苄胺衍生物或其盐。

10. 发明授权

US08299255B2 3,8-diaminotetrahydroquinoline derivative 有权
标题翻译： 3,8-二氨基四氢喹啉衍生物
公开(公告)号：US08299255B2
公开(公告)日：2012-10-30
申请号：US12866843
申请日：2009-02-06
申请人： Takeshi Watanabe , Masaru Terauchi , Masaaki Nagasawa , Kouichirou Tanaka , Masataka Washiduka
发明人： Takeshi Watanabe , Masaru Terauchi , Masaaki Nagasawa , Kouichirou Tanaka , Masataka Washiduka
IPC分类号： C07D409/14
CPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D405/06 , C07D409/14 , C07K5/06 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06156
摘要： To provide a compound which has a potent agonistic activity on GHS-R and which is useful as a therapeutic agent for systemic wasting diseases such as cachexia.A 3,8-diaminotetrahydroquinoline derivative represented by formula (1a) (wherein X represents CH2, C═O, CH—OR, CH—SR, or CH—NRR′; m is a number of 1 or 2; Ar represents a phenyl group, a naphthyl group, a 5-membered or 6-membered aromatic heterocyclic group having one or two elements selected from S, N, and O, or a similar group; R1 and R2, which may be identical to or different from each other, each represent a hydrogen atom or a methyl group; R3 represents a C1 to C6 alkyl group or a similar group; n is a number of 0 or 1; R4 and R5, which may be identical to or different from each other, each represent a hydrogen atom, or a C1 to C6 alkyl group, etc.; and R6, R7, R, and R′, which may be identical to or different from one another, each represent a hydrogen atom or a C1 to C6 alkyl group), or a salt thereof.
摘要翻译：提供对GHS-R具有强烈的激动活性的化合物，其可用作系统性消耗性疾病如恶病质的治疗剂。由式（1a）表示的3,8-二氨基四氢喹啉衍生物（其中X表示CH 2，C = O，CH-OR，CH-SR或CH-NRR'; m为1或2的数; Ar表示基团，萘基，具有选自S，N和O的一个或两个元素的5元或6元芳族杂环基或相似的基团; R 1和R 2可以彼此相同或不同各自表示氢原子或甲基; R3表示C1〜C6烷基或类似基团; n为0或1的数; R4和R5可以相同或不同，表示氢原子或C1-C6烷基等;并且可以相同或不同的R6，R7，R和R'各自表示氢原子或C1-C6烷基），或其盐。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式