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1. 发明授权

US6031111A Indolin-2-one derivatives 失效
公开(公告)号：US6031111A
公开(公告)日：2000-02-29
申请号：US182638
申请日：1998-10-30
申请人： Toru Esaki , Takashi Emura , Eiichi Hoshino
发明人： Toru Esaki , Takashi Emura , Eiichi Hoshino
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/18 , A61P43/00 , C07D209/34 , C07D209/38 , C07D209/40 , C07D209/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12
CPC分类号： C07D405/12 , C07D209/34 , C07D209/40 , C07D401/06 , C07D401/12 , C07D405/06
摘要： A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.

2. 发明授权

US06207836B1 Indolin-2-one derivatives 失效
标题翻译：二氢吲哚-2-酮衍生物
公开(公告)号：US06207836B1
公开(公告)日：2001-03-27
申请号：US09182490
申请日：1998-10-30
申请人： Toru Esaki , Takashi Emura , Eiichi Hoshino
发明人： Toru Esaki , Takashi Emura , Eiichi Hoshino
IPC分类号： C07D40112
CPC分类号： C07D405/12 , C07D209/34 , C07D209/40 , C07D401/06 , C07D401/12 , C07D405/06
摘要： A compound represented by formula (I): wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, —OR5, —SR5 or —NR6R7 (wherein R5, R6, and R7 each represent a lower alkyl group, etc.); X and Y each represent —CH2—, —NH— or —O—; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.
摘要翻译：由式（I）表示的化合物：其中R1表示卤素原子，低级烷基，低级烷氧基，羟基，硝基，三氟甲基，低级烷硫基，酰基，羧基，巯基或氨基; R2表示氢原子，低级烷基，低级烯基，低级炔基，烷氧基，酰基，芳基或杂环基; R3表示低级烷基，环烷基，芳基或杂环基; R4表示氢原子，低级烷基，芳基，杂环基，-OR5，-SR5或-NR6R7（其中R5，R6和R7各自表示低级烷基等）; X和Y各自表示-CH 2 - ， - NH-或-O-; 并且n表示0至4的整数，并且公开了其合成中间体。本发明化合物对胃泌素受体表现出选择性拮抗作用，而不引起归因于CCK-A受体拮抗作用的副作用，并且可用于治疗和预防消化性溃疡，胃炎，反流性食管炎和佐林格 - 埃里森综合征，并用于治疗的起源于胃肠系统的肿瘤。

3. 发明授权

US5952511A Indolin-2-one derivatives 失效
公开(公告)号：US5952511A
公开(公告)日：1999-09-14
申请号：US963547
申请日：1997-11-03
申请人： Toru Esaki , Takashi Emura , Eiichi Hoshino
发明人： Toru Esaki , Takashi Emura , Eiichi Hoshino
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/18 , A61P43/00 , C07D209/34 , C07D209/38 , C07D209/40 , C07D209/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12
CPC分类号： C07D405/12 , C07D209/34 , C07D209/40 , C07D401/06 , C07D401/12 , C07D405/06
摘要： A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.

4. 发明授权

US6127544A Indolin-2-one derivatives 失效
公开(公告)号：US6127544A
公开(公告)日：2000-10-03
申请号：US182491
申请日：1998-10-30
申请人： Toru Esaki , Takashi Emura , Eiichi Hoshino
发明人： Toru Esaki , Takashi Emura , Eiichi Hoshino
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/18 , A61P43/00 , C07D209/34 , C07D209/38 , C07D209/40 , C07D209/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12
CPC分类号： C07D405/12 , C07D209/34 , C07D209/40 , C07D401/06 , C07D401/12 , C07D405/06
摘要： A compound represented by formula (I): wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.

5. 发明授权

US06114536A Indolin-2-one derivatives 失效
标题翻译：二氢吲哚-2-酮衍生物
公开(公告)号：US06114536A
公开(公告)日：2000-09-05
申请号：US182463
申请日：1998-10-30
申请人： Toru Esaki , Takashi Emura , Eiichi Hoshino
发明人： Toru Esaki , Takashi Emura , Eiichi Hoshino
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/18 , A61P43/00 , C07D209/34 , C07D209/38 , C07D209/40 , C07D209/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/06 , C07D405/12
CPC分类号： C07D405/12 , C07D209/34 , C07D209/40 , C07D401/06 , C07D401/12 , C07D405/06
摘要： A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed. The compound of the present invention exhibits selective antagonism against gastrin receptors without causing side effects attributed to CCK-A receptor antagonism and is useful for the treatment and prevention of peptic ulcers, gastritis, reflux esophagitis, and Zollinger-Ellison syndrome, and for the treatment of neoplasm originating in the gastrointestinal system.
摘要翻译：由式（I）表示的化合物：其中R1表示卤素原子，低级烷基，低级烷氧基，羟基，硝基，三氟甲基，低级烷硫基，酰基，羧基，巯基或氨基; R2表示氢原子，低级烷基，低级烯基，低级炔基，烷氧基，酰基，芳基或杂环基; R3表示低级烷基，环烷基，芳基或杂环基; R4表示氢原子，低级烷基，芳基，杂环基，-OR5，-SR5或-NR6R7（其中R5，R6和R7各自表示低级烷基等）; X和Y各自表示-CH 2 - ， - NH-或-O-; 并且n表示0至4的整数，并且公开了其合成中间体。本发明化合物对胃泌素受体表现出选择性拮抗作用，而不引起归因于CCK-A受体拮抗作用的副作用，并且可用于治疗和预防消化性溃疡，胃炎，反流性食管炎和佐林格 - 埃里森综合征，并用于治疗的起源于胃肠系统的肿瘤。

6. 发明授权

US09169254B2 Spiroimidazolone derivative 有权
标题翻译：螺咪唑啉酮衍生物
公开(公告)号：US09169254B2
公开(公告)日：2015-10-27
申请号：US13266517
申请日：2010-04-27
申请人： Toru Esaki , Yoshikazu Nishimura , Yoshiaki Isshiki , Naoki Okamoto , Yoshiyuki Furuta , Akemi Mizutani , Masateru Ohta , Wayne Wen Lai , Tomoya Kotake
发明人： Toru Esaki , Yoshikazu Nishimura , Yoshiaki Isshiki , Naoki Okamoto , Yoshiyuki Furuta , Akemi Mizutani , Masateru Ohta , Wayne Wen Lai , Tomoya Kotake
IPC分类号： C07D487/10 , C07D491/107 , A61K31/5377 , A61K31/4545 , C07D515/20 , C07D471/10 , C07D513/20 , C07D513/22
CPC分类号： C07D471/10 , C07D471/20 , C07D491/107 , C07D513/20 , C07D513/22 , C07D515/20
摘要： The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.
摘要翻译：本发明涉及由下式（1）表示的化合物：其中W，X，Y，R 1，R 2，R 33，R 34，m和n如权利要求中所定义，或其药理学上可接受的盐。

7. 发明申请

US20120270838A1 SPIROIMIDAZOLONE DERIVATIVE 有权
标题翻译： SPIROIMIDAZOLONE衍生物
公开(公告)号：US20120270838A1
公开(公告)日：2012-10-25
申请号：US13266517
申请日：2010-04-27
申请人： Toru Esaki , Yoshikazu Nishimura , Yoshiaki Isshiki , Naoki Okamoto , Yoshiyuki Furuta , Akemi Mizutani , Masateru Ohta , Wayne Wen Lai , Tomoya Kotake
发明人： Toru Esaki , Yoshikazu Nishimura , Yoshiaki Isshiki , Naoki Okamoto , Yoshiyuki Furuta , Akemi Mizutani , Masateru Ohta , Wayne Wen Lai , Tomoya Kotake
IPC分类号： A61K31/438 , C07D487/10 , A61K31/55 , A61K31/4188 , A61K31/497 , A61K31/444 , A61K31/5377 , A61K31/496 , A61K31/506 , A61K31/541 , C07D491/107 , C07F7/10 , A61K31/695 , C07D515/20 , A61K31/4545 , A61P19/10 , A61P19/02 , A61P5/00 , A61P7/00 , A61P19/08 , A61P35/00 , C07D471/10
CPC分类号： C07D471/10 , C07D471/20 , C07D491/107 , C07D513/20 , C07D513/22 , C07D515/20
摘要： The present invention relates to a compound represented by the following formula (1): wherein W, X, Y, R1, R2, R33, R34, m and n are as defined in the claims, or a pharmacologically acceptable salt thereof.
摘要翻译：本发明涉及由下式（1）表示的化合物：其中W，X，Y，R 1，R 2，R 33，R 34，m和n如权利要求中所定义，或其药理学上可接受的盐。

8. 发明授权

US06887890B2 Compounds exhibiting thrombopoietin-like activities 失效
标题翻译：表现出血小板生成素样活性的化合物
公开(公告)号：US06887890B2
公开(公告)日：2005-05-03
申请号：US10296638
申请日：2001-05-30
申请人： Shinya Fujiwara , Tomokazu Ozaki , Toshiro Kozono , Kunihiro Hattori , Toru Esaki
发明人： Shinya Fujiwara , Tomokazu Ozaki , Toshiro Kozono , Kunihiro Hattori , Toru Esaki
IPC分类号： A61K38/00 , A61P7/04 , C07C237/22 , C07D209/18 , C07D213/78 , C07D333/24 , C07D333/34 , C07D401/14
CPC分类号： C07D213/78 , A61K38/00 , C07C237/22 , C07D209/18 , C07D333/24 , C07D333/34
摘要： The compounds of the invention are compounds represented by the following general formula (1): wherein E represents one selected from the group consisting of a methylidyne group and a nitrilo group, R1 represents one selected from the group consisting of optionally substituted aryl groups and optionally substituted heteroaryl groups, R2 represents one selected from the group consisting of a hydrogen atom and alkyl groups, W1 represents an amino acid residue, A represents one selected from the group consisting of a carbonyl group and a sulfonyl group, X1 represents one selected from the group consisting of optionally substituted alkylene groups and optionally substituted alkenylene groups, and p represents 0 or 1; and their pharmacologically acceptable salts, which exhibit thrombopoietin-like activity.
摘要翻译：本发明的化合物是由以下通式（1）表示的化合物：其中E表示选自亚甲基和亚硝基的一个，R 1表示选自下列通式由任选取代的芳基和任选取代的杂芳基组成，R 2表示选自氢原子和烷基的一个，W 1表示氨基酸残基 A表示选自羰基和磺酰基的一个，X 1表示选自任选取代的亚烷基和任选取代的亚烯基的一个，p表示0或 1; 及其药理学上可接受的盐，其表现出血小板生成素样活性。

9. 发明授权

US06500854B1 Chondrongenesis promotors and indolin-2-one derivatives 失效
标题翻译：二茂铁衍生物和二氢吲哚-2-酮衍生物
公开(公告)号：US06500854B1
公开(公告)日：2002-12-31
申请号：US09890071
申请日：2001-09-21
申请人： Hidetomo Kitamura , Atsuhiko Kato , Toru Esaki
发明人： Hidetomo Kitamura , Atsuhiko Kato , Toru Esaki
IPC分类号： A61K31404
CPC分类号： C07D401/06 , A61K31/404 , A61K31/405 , A61K31/443 , A61K31/4433 , A61K31/4439 , C07D209/38 , C07D209/40 , C07D403/12 , C07D405/06
摘要： A chondrogenesis promoter comprising as an active ingredient a compound represented by general formula (I) or a salt thereof: wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, etc.; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, an acyl group, an aryl group, a heterocyclic group, etc.; R1 represents a lower alkyl group, a cycloalkyl group, an aryl group, a heterocyclic group, etc.; R4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, etc.; X and Y represent —CH2—, —NH—or —O—; and n represents an integer of 0-4.
摘要翻译：一种软骨形成促进剂，其包含作为活性成分的由通式（I）表示的化合物或其盐：其中R1表示卤素原子，低级烷基，低级烷氧基等; R2表示氢原子，低级烷基，低级烯基，低级炔基，低级烷氧基，酰基，芳基，杂环基等。 R1表示低级烷基，环烷基，芳基，杂环基等; R4表示氢原子，低级烷基，芳基，杂环基等; X和Y表示-CH 2 - ， - NH-或-O-; n表示0〜4的整数。

10. 发明授权

US06716628B2 Chondrogenesis promoters and indolin-2-one derivatives 失效
标题翻译：软骨形成启动子和二氢吲哚-2-酮衍生物
公开(公告)号：US06716628B2
公开(公告)日：2004-04-06
申请号：US10224311
申请日：2002-08-21
申请人： Hidetomo Kitamura , Atsuhiko Kato , Toru Esaki
发明人： Hidetomo Kitamura , Atsuhiko Kato , Toru Esaki
IPC分类号： C12N502
CPC分类号： C07D401/06 , A61K31/404 , A61K31/405 , A61K31/443 , A61K31/4433 , A61K31/4439 , C07D209/38 , C07D209/40 , C07D403/12 , C07D405/06
摘要： A chondrogenesis promoter comprising as an active ingredient a compound represented by general formula (I) or a salt thereof: wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, etc.; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, an acyl group, an aryl group, a heterocyclic group, etc.; R3 represents a lower alkyl group, a cycloalkyl group, an aryl group, a heterocyclic group, etc.; R4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, etc.; X and Y represent —CH2—, —NH— or —O—; and n represents an integer of 0-4.
摘要翻译：一种软骨形成促进剂，其包含作为活性成分的由通式（I）表示的化合物或其盐：其中R 1表示卤素原子，低级烷基，低级烷氧基等; R 2表示氢原子，低级烷基，低级烯基，低级炔基，低级烷氧基，酰基，芳基，杂环基等。 R 3表示低级烷基，环烷基，芳基，杂环基等; R 4表示氢原子，低级烷基，芳基，杂环基等; X和Y表示-CH 2 - ， - NH-或-O-; n表示0〜4的整数。

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