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1. 发明申请

US20070142409A1 3-Substituted-4-pyrimidone derivatives 失效
标题翻译： 3-取代的-4-嘧啶酮衍生物
公开(公告)号：US20070142409A1
公开(公告)日：2007-06-21
申请号：US10538766
申请日：2003-12-12
申请人： Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
发明人： Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
IPC分类号： A61K31/513 , C07D403/14
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor:wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
摘要翻译：用作tau蛋白激酶1抑制剂的由式（I）表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中X表示CH或氮原子; R 1表示可被取代的C 1〜1 191〜C 12〜191烷基; R 2表示可以被取代的C 1〜191-C 18〜191烷基，可被取代的苯环，可被取代的萘环，可以被取代的萘环可被取代的四氢萘环，或具有1-4个选自氧原子，硫原子和氮原子的杂原子的任意取代的杂环，并且总共具有5至10个环构成原子。

2. 发明授权

US07683069B2 3-substituted-4-pyrimidone derivatives 失效
标题翻译： 3-取代-4-嘧啶酮衍生物
公开(公告)号：US07683069B2
公开(公告)日：2010-03-23
申请号：US10538766
申请日：2003-12-12
申请人： Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
发明人： Yoshihiro Usui , Masahiro Okuyama , Tokushi Hanano
IPC分类号： C07D401/14 , A61K31/505
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor: wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
摘要翻译：用作tau蛋白激酶1抑制剂的由式（I）表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中X表示CH或氮原子; R1表示可被取代的C 1〜191-C 12〜191烷基; R2表示可被取代的C 1〜191-C 18〜191烷基，可被取代的苯环，可被取代的萘环，可被取代的茚满环，可以被取代的四氢萘环，或具有1〜4个选自氧原子，硫原子和氮原子的杂原子的任意取代的杂环，并且总共具有5〜10个构成环的原子。

3. 发明授权

US06977262B2 Dihydropyrazolopyridine compounds and pharmaceutical use thereof 失效
标题翻译：二氢吡唑并吡啶化合物及其药物用途
公开(公告)号：US06977262B2
公开(公告)日：2005-12-20
申请号：US10631847
申请日：2003-08-01
申请人： Toshiyuki Kohara , Kenji Fukunaga , Masatake Fujimura , Tokushi Hanano , Hirotaka Okabe
发明人： Toshiyuki Kohara , Kenji Fukunaga , Masatake Fujimura , Tokushi Hanano , Hirotaka Okabe
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The present invention provides dihydropyrazolopyridine compounds represented by the formula (I): wherein each symbol is as defined in the specification, optically active forms thereof, and pharmaceutically acceptable salts thereof and hydrates thereof. The compounds of the present invention show a selective and strong inhibitory activity on glycogen synthase kinase-3 beta (GSK-3β), and are useful as medicaments for prevention and/or treatment of diabetes, diabetic complications and neurodegenerative diseases or as immunopotentiators.
摘要翻译：本发明提供由式（I）表示的二氢吡唑并吡啶化合物：其中每个符号如本说明书中所定义，其光学活性形式及其药学上可接受的盐及其水合物。本发明化合物对糖原合酶激酶-3β（GSK-3β）具有选择性和强抑制活性，可用作预防和/或治疗糖尿病，糖尿病并发症和神经变性疾病或作为免疫增强剂的药物。

4. 发明授权

US06214873B1 2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same 有权
标题翻译： 2-氨基丙烷-1,3-二醇化合物，其药学用途和合成它们的中间体
公开(公告)号：US06214873B1
公开(公告)日：2001-04-10
申请号：US09402375
申请日：2000-01-05
申请人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Koji Teshima , Yukio Hoshino , Tetsuro Fujita
发明人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Koji Teshima , Yukio Hoshino , Tetsuro Fujita
IPC分类号： A61H3122
CPC分类号： C07C225/16 , C07C215/34 , C07C223/02 , C07F7/1804
摘要： The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.
摘要翻译：本发明涉及一般化学式R 1，R 2，R 3和R 4的化合物各自为氢或酰基，其药学上可接受的酸加成盐或其水合物; 包含该化合物的药物; 包含该化合物和药学上可接受的载体的药物组合物; 和2-氨基-2-（2-（4-（1-羟基-5-苯基戊基）苯基）乙基）丙烷-1,3-二醇或2-氨基-2-（2-（4-甲酰基苯基）乙基）丙烷-1,3-二醇，其氨基和/或羟基被保护的两种化合物的衍生物或其盐。本发明的化合物显示出较好的免疫抑制作用，毒性小，安全性更高，可用作预防或抑制器官排斥或骨髓移植的药物，或作为预防或治疗各种自身免疫性疾病或过敏性疾病的药物疾病

5. 发明授权

US08877779B2 Benzimidazole compound and pharmaceutical use thereof 有权
标题翻译：苯并咪唑化合物及其药物用途
公开(公告)号：US08877779B2
公开(公告)日：2014-11-04
申请号：US12449874
申请日：2008-02-28
申请人： Masakazu Nakano , Masanori Minoguchi , Tokushi Hanano , Shin-ichiro Ono , Hideki Horiuchi , Koji Teshima
发明人： Masakazu Nakano , Masanori Minoguchi , Tokushi Hanano , Shin-ichiro Ono , Hideki Horiuchi , Koji Teshima
IPC分类号： A61K31/445 , C07D401/04 , C07D417/14 , C07D405/14 , C07D471/04
CPC分类号： C07D401/04 , C07D405/14 , C07D417/14 , C07D471/04
摘要： Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) wherein each symbol is as defined in the claims.
摘要翻译：本发明提供的ORL-1受体激动剂与常规化合物相比，具有基于优异的代谢稳定性和强和高选择性的改善的生物利用度。由式（I）表示的化合物，其中每个符号如权利要求中所定义。

6. 发明申请

US20100120841A1 BENZIMIDAZOLE COMPOUND AND PHARMACEUTICAL USE THEREOF 有权
标题翻译：苯并咪唑化合物及其药物用途
公开(公告)号：US20100120841A1
公开(公告)日：2010-05-13
申请号：US12449874
申请日：2008-02-28
申请人： Masakazu Nakano , Masanori Minoguchi , Tokushi Hanano , Shin-ichiro Ono , Hideki Horiuchi , Koji Teshima
发明人： Masakazu Nakano , Masanori Minoguchi , Tokushi Hanano , Shin-ichiro Ono , Hideki Horiuchi , Koji Teshima
IPC分类号： A61K31/437 , C07D401/04 , A61K31/445 , C07D471/02 , A61P25/00
CPC分类号： C07D401/04 , C07D405/14 , C07D417/14 , C07D471/04
摘要： Provided is an ORL-1 receptor agonist having improved bioavailability based on superior metabolic stability and strong and high selectivity, as compared to conventional compounds. A compound represented by the formula (I) wherein each symbol is as defined in the claims.
摘要翻译：本发明提供的ORL-1受体激动剂与常规化合物相比，具有基于优异的代谢稳定性和强和高选择性的改善的生物利用度。由式（I）表示的化合物，其中每个符号如权利要求中所定义。

7. 发明授权

US06455528B1 Piperazine compounds and medicinal use thereof 失效
标题翻译：哌嗪类化合物及其医药用途
公开(公告)号：US06455528B1
公开(公告)日：2002-09-24
申请号：US09529491
申请日：2000-04-14
申请人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
发明人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
IPC分类号： A61K31506
CPC分类号： C07D239/42 , C07C2601/02 , C07D213/74 , C07D233/88 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/52 , C07D239/545 , C07D277/42 , C07D295/135
摘要： The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-&agr; production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-&agr; production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-&agr; production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-&agr; mediated diseases.
摘要翻译：本发明涉及式R 1和R 2的哌嗪化合物各自为氢，卤素，低级烷基，低级烷氧基，氨基，取代的氨基，硝基，羟基或氰基，R 3，R 4和R 5各自为氢，卤素，低级烷基，低级烷氧基，硝基，氨基，取代的氨基或羟基，R6和R7各自为氢，低级烷基，被卤素取代的低级烷基，芳烷基，酰基或被卤素取代的低级酰基，R8和R9分别为氢或低级烷基，Y 是低级亚烷基等，环A是苯基，嘧啶基，噻唑基，吡啶基，吡唑基或咪唑基，其药学上可接受的盐和含有这些化合物的药物。本发明的化合物具有优异的TNF-α产生抑制作用和/或IL-10产生促进作用，并且由于其没有或显示出仅显着降低对中枢神经系统的作用的表达，所以该化合物是有用的作为高度安全和优越的TNF-α产生抑制剂和/或IL-10产生促进剂，并且可用作预防或治疗由异常TNF-α产生引起的各种疾病的药剂，可用IL-10固化的疾病，例如慢性炎性疾病，急性炎性疾病，感染引起的炎性疾病，自身免疫疾病，过敏性疾病和TNF-α介导的疾病。

8. 发明申请

US20060167014A1 Piperazine compounds and medicinal use thereof 审中-公开
标题翻译：哌嗪类化合物及其医药用途
公开(公告)号：US20060167014A1
公开(公告)日：2006-07-27
申请号：US11298980
申请日：2005-12-12
申请人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
发明人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Hiroshi Morimoto , Masao Hisadome
IPC分类号： A61K31/495 , C07D241/04
CPC分类号： C07D239/42 , C07C2601/02 , C07D213/74 , C07D233/88 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/52 , C07D239/545 , C07D277/42 , C07D295/135
摘要： The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-α production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-α production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-α production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-α mediated diseases.
摘要翻译：本发明涉及下式的哌嗪化合物其中R 1和R 2各自为氢，卤素，低级烷基，低级烷氧基，氨基，取代的氨基，硝基，羟基或氰基，R 3，R 4和R 5各自为氢，卤素，低级烷基，低级烷氧基，硝基，氨基，取代的氨基或羟基，R 6和R 7各自为氢，低级烷基，被卤素取代的低级烷基，芳烷基，酰基或被卤素取代的低级酰基， 8和R 9各自为氢或低级烷基，Y为低级亚烷基等，环A为苯基，嘧啶基，噻唑基，吡啶基，吡唑基或咪唑基，其药学上可接受的盐和含有这些化合物的药剂。本发明的化合物具有优异的TNF-α产生抑制作用和/或IL-10产生促进作用，并且由于其没有或显示出仅显着降低对中枢神经系统的作用的表达，所以该化合物是有用的作为高度安全和优越的TNF-α产生抑制剂和/或IL-10产生促进剂，并且可用作预防或治疗由异常TNF-α产生引起的各种疾病的药剂，可用IL-10固化的疾病，例如慢性炎性疾病，急性炎性疾病，感染引起的炎性疾病，自身免疫疾病，过敏性疾病和TNF-α介导的疾病。

9. 再颁专利

USRE39072E1 2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same 有权
标题翻译： 2-氨基丙烷-1,3-二醇化合物，其药学用途和合成它们的中间体
公开(公告)号：USRE39072E1
公开(公告)日：2006-04-18
申请号：US10410387
申请日：1998-04-03
申请人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Koji Teshima , Yukio Hoshino , Tetsuro Fujita
发明人： Kunitomo Adachi , Yoshiyuki Aoki , Tokushi Hanano , Koji Teshima , Yukio Hoshino , Tetsuro Fujita
IPC分类号： A61K31/22
CPC分类号： C07C225/16 , C07C215/34 , C07C223/02 , C07F7/1804
摘要： The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.
摘要翻译：本发明涉及以下通式的化合物：其中R 1，R 2，R 3和R 4，各自为氢或酰基，其药学上可接受的酸加成盐或其水合物; 包含该化合物的药物; 包含该化合物和药学上可接受的载体的药物组合物; 和2-氨基-2-（2-（4-（1-羟基-5-苯基戊基）苯基）乙基）丙烷-1,3-二醇或2-氨基-2-（2-（4-甲酰基苯基）乙基）丙烷-1,3-二醇，其氨基和/或羟基被保护的两种化合物的衍生物或其盐。本发明的化合物显示出较好的免疫抑制作用，毒性小，安全性更高，可用作预防或抑制器官排斥或骨髓移植的药物，或作为预防或治疗各种自身免疫性疾病或过敏性疾病的药物疾病

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