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1. 发明申请

US20050090498A1 3-Quinolin-2(1h)-ylideneindolin-2-one derivative 审中-公开
标题翻译： 3-喹啉-2（1h） - 亚基二氢吲哚-2-酮衍生物
公开(公告)号：US20050090498A1
公开(公告)日：2005-04-28
申请号：US10478504
申请日：2002-05-23
申请人： Kiyohiro Samizu , Hiroyuki Hisamichi , Akira Matsuhisa , Isao Kinoyama , Masahiko Hayakawa , Nobuaki Taniguchi , Yukitaka Ideyama , Sadao Kuromitsu , Kiyoshi Yahiro , Minoru Okada
发明人： Kiyohiro Samizu , Hiroyuki Hisamichi , Akira Matsuhisa , Isao Kinoyama , Masahiko Hayakawa , Nobuaki Taniguchi , Yukitaka Ideyama , Sadao Kuromitsu , Kiyoshi Yahiro , Minoru Okada
IPC分类号： A61P27/02 , A61P35/00 , A61P43/00 , C07D209/34 , C07D211/22 , C07D215/12 , C07D215/60 , C07D263/10 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/10 , C07D491/113 , C07D493/04 , C07D471/02 , A61K31/4709 , A61K31/4745 , A61K31/498 , A61K31/519
CPC分类号： C07D263/10 , C07D209/34 , C07D211/22 , C07D215/12 , C07D215/60 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/10 , C07D493/04
摘要： There is provided medicaments, particularly a vascular endothelial growth factor (VEGF) inhibitor which is useful as a therapeutic drug for solid tumors, diabetic retinopathy and the like diseases in which angiogenesis is taking a role. That is, since a novel 3-quinolin-2(1H)-ylideneindolin-2-one derivative or a salt thereof has good VEGF inhibitory action, angiogenesis inhibitory action and anti-tumor action, it is useful as ideal VEGF inhibitor, angiogenesis inhibitor and anti-tumor agent.
摘要翻译：提供了药物，特别是血管内皮生长因子（VEGF）抑制剂，其可用作实体瘤的治疗药物，糖尿病性视网膜病变等血管生成正在起作用的疾病。也就是说，由于新型3-喹啉-2（1H） - 亚基二氢吲哚-2-酮衍生物或其盐具有良好的VEGF抑制作用，血管生成抑制作用和抗肿瘤作用，因此可用作理想的VEGF抑制剂，血管生成抑制剂和抗肿瘤剂。

2. 发明授权

US07960562B2 Propane-1,3-dione derivative or salt thereof 有权
标题翻译：丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US07960562B2
公开(公告)日：2011-06-14
申请号：US11887384
申请日：2006-03-30
申请人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
发明人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahashi , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
IPC分类号： A61K31/4184 , C07D235/12
CPC分类号： C07D235/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14
摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
摘要翻译：旨在提供可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙烷-1,3-二酮衍生物。结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

3. 发明申请

US20090181964A1 Propane-1,3-Dione Derivative or Salt Thereof 有权
标题翻译：丙烷-1,3-二酮衍生物或其盐
公开(公告)号：US20090181964A1
公开(公告)日：2009-07-16
申请号：US11887384
申请日：2006-03-30
申请人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahisa , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
发明人： Masaaki Hirano , Isao Kinoyama , Shunichiro Matsumoto , Eiji Kawaminami , Kei Ohnuki , Hirofumi Yamamoto , Kazuhiko Osoda , Tatsuhisa Takahisa , Takashi Shin , Takanori Koike , Itsuro Shimada , Hiroyuki Hisamichi , Toshiyuki Kusayama
IPC分类号： A61K31/5377 , C07D235/04 , A61K31/4184 , C07D401/02 , A61K31/4439 , C07D403/02 , A61K31/496 , C07D413/14 , A61K31/506 , A61K31/501 , A61P35/00
CPC分类号： C07D235/12 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14
摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.
摘要翻译：旨在提供可用作GnRH受体拮抗剂的化合物。本发明人进一步研究了丙烷-1,3-二酮衍生物。结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

4. 发明申请

US20100227866A1 TETRAHYDROISOQUINOLIN-1-ONE DERIVATIVE OR SALT THEREOF 有权
标题翻译：四氢喹啉-1-酮衍生物或其盐
公开(公告)号：US20100227866A1
公开(公告)日：2010-09-09
申请号：US12600894
申请日：2008-05-26
申请人： Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
发明人： Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
IPC分类号： A61K31/4725 , C07D401/12 , C07D401/14 , A61K31/53 , A61K31/506 , A61P1/00 , A61P35/00
CPC分类号： A61K31/4725 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/472 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/695 , C07D217/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04
摘要： [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS).[Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
摘要翻译： [问题]提供药物，特别是可用作肠易激综合征（IBS）治疗剂的化合物。 [解决问题的手段]发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2（BB2）受体拮抗作用。还发现四氢异喹啉-1-酮衍生物对肠运动障碍是高度有效的。从上述可以看出，本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体，特别是IBS相关疾病的治疗剂。

5. 发明授权

US6136810A Pyrido[2,3-D]pyrimidine derivatives and pharmaceutical compositions thereof 失效
标题翻译：吡啶并[2,3-D]嘧啶衍生物及其药物组合物
公开(公告)号：US6136810A
公开(公告)日：2000-10-24
申请号：US66370
申请日：1998-04-30
申请人： Kazuhisa Takayama , Hiroyuki Hisamichi , Masahiro Iwata , Hideki Kubota , Motonori Aoki
发明人： Kazuhisa Takayama , Hiroyuki Hisamichi , Masahiro Iwata , Hideki Kubota , Motonori Aoki
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： This invention relates to compounds (I) or pharmaceutically acceptable salts thereof, having a function to inhibit type IV phosphodiesterase (PDE) ##STR1## [X: an oxygen atom or a sulfur atom, R.sup.1 : a lower alkyl group, a cycloalkyl-lower alkyl group or a cycloalkyl group,R.sup.2 : a hydrogen atom, a halogen atom, a lower alkyl group, a halogeno-lower alkyl group, a hydroxy-lower alkyl group, a mercapto-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkylthio-lower alkyl group, a lower alkanoyloxy-lower alkyl group, a lower alkanoylthio-lower alkyl group, a lower alkanoyl-lower alkyl group, a hydroxyimino-lower alkyl group, a lower alkoxyimino-lower alkyl group, a cycloalkyl group, an aryl group or a lower alkanoyl group,R.sup.3 : a hydrogen atom, a halogen atom or a lower alkyl group,R.sup.4 : a hydrogen atom or a lower alkyl group,R.sup.5 : a cycloalkyl group; a naphthyl group substituted; a five- or six-membered monocyclic hetero ring group having 1 to 4 hetero atoms selected from nitrogen atom, oxygen atom and sulfur atom; or a group represented by the formula ##STR2## amd F.sup.6 : a halogen atom, a lower alkyl group, a halogeno-lower alkyl group, a hydroxyl group, a lower alkoxy group, a cyano group or a nitro group].
摘要翻译： PCT No.PCT / JP96 / 03389。 371日期：1998年4月30日 102（e）1998年4月30日PCT PCT 1996年11月20日PCT公布。公开号WO97 / 19078 日期：1997年5月29日本发明涉及具有抑制IV型磷酸二酯酶（PDE）的功能的化合物（I）或其药学上可接受的盐[X：氧原子或硫原子，R 1：低级烷基，环烷基 - 低级烷基或环烷基，R2：氢原子，卤素原子，低级烷基，卤代低级烷基，羟基低级烷基，巯基低级烷基，低级烷氧基 - 低级烷基低级烷酰氧基 - 低级烷基，低级烷酰硫基 - 低级烷基，低级烷酰基 - 低级烷基，低级烷酰基 - 低级烷基，羟基亚氨基 - 低级烷基，低级烷氧基亚氨基 - 低级烷基，低级烷酰氧基 - 低级烷基环烷基，芳基或低级烷酰基，R3：氢原子，卤素原子或低级烷基，R4表示氢原子或低级烷基，R5表示环烷基。萘基取代; 具有1-4个选自氮原子，氧原子和硫原子的杂原子的五元或六元单环杂环基; 或由式amd F6表示的基团：卤素原子，低级烷基，卤代低级烷基，羟基，低级烷氧基，氰基或硝基]。

6. 发明授权

US08486970B2 Tetrahydroisoquinolin-1-one derivative or salt thereof 有权
标题翻译：四氢异喹啉-1-酮衍生物或其盐
公开(公告)号：US08486970B2
公开(公告)日：2013-07-16
申请号：US12600894
申请日：2008-05-26
申请人： Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
发明人： Hiroyuki Hisamichi , Itsuro Shimada , Tsukasa Ishihara , Tomofumi Takuwa , Takafumi Shimizu , Noriko Ishikawa , Kyoichi Maeno , Norio Seki
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： A61K31/4725 , A61K31/435 , A61K31/439 , A61K31/445 , A61K31/472 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/695 , C07D217/26 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/04
摘要： [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS).[Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
摘要翻译： [问题]提供药物，特别是可用作肠易激综合征（IBS）治疗剂的化合物。 [解决问题的手段]发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2（BB2）受体拮抗作用。还发现四氢异喹啉-1-酮衍生物对肠运动障碍是高度有效的。从上述可以看出，本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体，特别是IBS相关疾病的治疗剂。

7. 发明授权

US06797706B1 Heterocyclecarboxamide derivative 有权
标题翻译：杂环酰胺衍生物
公开(公告)号：US06797706B1
公开(公告)日：2004-09-28
申请号：US10009276
申请日：2001-12-10
申请人： Hiroyuki Hisamichi , Souichirou Kawazoe , Kazuhito Tanabe , Atsushi Ichikawa , Akiko Orita , Takayuki Suzuki , Kenichi Onda , Makoto Takeuchi
发明人： Hiroyuki Hisamichi , Souichirou Kawazoe , Kazuhito Tanabe , Atsushi Ichikawa , Akiko Orita , Takayuki Suzuki , Kenichi Onda , Makoto Takeuchi
IPC分类号： A61K3133
CPC分类号： C07D213/82 , C07D239/48 , C07D241/26 , C07D253/07
摘要： A nitrogen-containing six-membered heterocyclic compound having substituents —X—A—R3, —N(R1)-(Ph substituted by R2), and —CONH2, a salt thereof, a prodrug thereof, and a Syk inhibitor containing the same as an active ingredient. (In the formula, A: a (substituted) lower alkylene, a (substituted) arylene, or the like; X: NR4, CONR4, NR4CO, O, or S; R1, R4: H, a lower alkyl, —CO-lower alkyl, or —SO2-lower alkyl; R2: H, a (substituted) lower alkyl, —O-lower alkyl, —S-lower alkyl, —O-aryl, nitro, cyano, or the like; R3: —CO2H, —CO2-lower alkyl, -lower alkylene-CO2H, —NH2, -alkylene-NH2 or the like.
摘要翻译：具有取代基-XAR 3，-N（R 1） - （Ph被R 2取代的）的含氮六元杂环化合物和-CONH 2，其盐，其前药和含有与活性成分相同的Syk抑制剂。（式中，A：（取代的）低级亚烷基，（取代的）亚芳基等; X：NR 4，CONR 4，NR 4 CO，O或S; R 1 R 4：H，低级烷基，-CO-低级烷基或-SO 2 - 低级烷基; R 2：H，（取代的）低级烷基，-O-低级烷基，-S-低级烷基，-O-芳基，硝基，氰基等; R 3：-CO 2 H，-CO 2 - 低级烷基， - 低级亚烷基-CO 2 H，-NH 2， - 亚烷基-NH 2等。

8. 发明授权

US06432963B1 Pyrimidine-5-carboxamide derivatives 有权
标题翻译：嘧啶-5-甲酰胺衍生物
公开(公告)号：US06432963B1
公开(公告)日：2002-08-13
申请号：US09581595
申请日：2000-06-15
申请人： Hiroyuki Hisamichi , Ryo Naito , Souichirou Kawazoe , Akira Toyoshima , Kazuhito Tanabe , Eiichi Nakai , Atsushi Ichikawa , Akiko Orita , Makoto Takeuchi
发明人： Hiroyuki Hisamichi , Ryo Naito , Souichirou Kawazoe , Akira Toyoshima , Kazuhito Tanabe , Eiichi Nakai , Atsushi Ichikawa , Akiko Orita , Makoto Takeuchi
IPC分类号： C07D23948
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/38 , C07D239/47 , C07D239/48 , C07D239/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].
摘要翻译：由通式（I）表示的嘧啶-5-甲酰胺衍生物或其盐[其中每个符号具有以下含义; X：O，S，NR1，CO，NR1CO，CONR1，C = N-OR1或键，Y 可以被OR 1或-NHR 1取代的低级亚烷基或键，Z：O，NR 2或键，A：H或可以具有取代基的低级烷基，可以是-CO-低级烷基具有取代基，可以具有取代基的芳基，可以具有取代基的杂芳基，可以具有取代基的环烷基或可以具有取代基的含氮饱和杂环基，B：可以具有取代基的芳基，或可以具有取代基的杂芳基，R 1，R 2：H，低级烷基或-CO-低级烷基]。

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