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1. 发明授权

US07314877B2 Benzofuran derivative 失效
标题翻译：苯并呋喃衍生物
公开(公告)号：US07314877B2
公开(公告)日：2008-01-01
申请号：US10547779
申请日：2004-03-03
申请人： Seiichi Sato , Tomoyuki Koshi , Toshimi Mizoguchi , Kyoko Yasuoka , Natsuyo Kumai , Junko Totsuka , Masahiro Tamura , Masao Ohkuchi
发明人： Seiichi Sato , Tomoyuki Koshi , Toshimi Mizoguchi , Kyoko Yasuoka , Natsuyo Kumai , Junko Totsuka , Masahiro Tamura , Masao Ohkuchi
IPC分类号： C07D405/04 , A61K31/501
CPC分类号： C07D405/04
摘要： The present invention is directed to a compound represented by formula (1): (wherein R1 represents an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and each of R2 and R3 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a dihydroxyalkyl group, or an alkynyl group, or R2 and R3 form, together with the nitrogen atom adjacent thereto, a nitrogen-containing saturated heterocyclic group which may have a substituent) and a drug composition containing the compound. The compound exhibits tumor necrosis factor (TNF-α) production inhibitory effect and improved absorption upon oral administration.
摘要翻译：本发明涉及由式（1）表示的化合物：其中R 1表示可以具有取代基的烷基或可具有取代基的烯基; R 1， SO 2和R 3表示氢原子，烷基，羟基烷基，二羟基烷基或炔基，或R 2和 R 3形式与与其相邻的氮原子，可以具有取代基的含氮饱和杂环基）和含有该化合物的药物组合物。该化合物表现出肿瘤坏死因子（TNF-α）产生抑制作用和口服给药改善吸收。

2. 发明申请

US20060189621A1 Benzofuran derivative 失效
标题翻译：苯并呋喃衍生物
公开(公告)号：US20060189621A1
公开(公告)日：2006-08-24
申请号：US10547779
申请日：2004-03-03
申请人： Seiichi Sato , Tomoyuki Koshi , Toshimi Mizoguchi , Kyoko Yasuoka , Junko Totsuka , Masahiro Tamura , Masao Ohkuchi
发明人： Seiichi Sato , Tomoyuki Koshi , Toshimi Mizoguchi , Kyoko Yasuoka , Junko Totsuka , Masahiro Tamura , Masao Ohkuchi
IPC分类号： A61K31/501 , C07D405/02
CPC分类号： C07D405/04
摘要： The present invention is directed to a compound represented by formula (1): (wherein R1 represents an alkyl group which may have a substituent or an alkenyl group which may have a substituent; and each of R2 and R3 represents a hydrogen atom, an alkyl group, a hydroxyalkyl group, a dihydroxyalkyl group, or an alkynyl group, or R2 and R3 form, together with the nitrogen atom adjacent thereto, a nitrogen-containing saturated heterocyclic group which may have a substituent) and a drug composition containing the compound. The compound exhibits tumor necrosis factor (TNF-α) production inhibitory effect and improved absorption upon oral administration.
摘要翻译：本发明涉及由式（1）表示的化合物：其中R 1表示可以具有取代基的烷基或可具有取代基的烯基; R 1， SO 2和R 3表示氢原子，烷基，羟基烷基，二羟基烷基或炔基，或R 2和 R 3形式与与其相邻的氮原子，可以具有取代基的含氮饱和杂环基）和含有该化合物的药物组合物。该化合物表现出肿瘤坏死因子（TNF-α）产生抑制作用和口服给药改善吸收。

3. 发明申请

US20060040986A1 Erythropoietin production accelerator 审中-公开
标题翻译：促红细胞生成素促进剂
公开(公告)号：US20060040986A1
公开(公告)日：2006-02-23
申请号：US10537407
申请日：2003-12-05
申请人： Shigehiko Imagawa , Takeshi Dol , Masahiro Tamura , Masao Ohkuchi
发明人： Shigehiko Imagawa , Takeshi Dol , Masahiro Tamura , Masao Ohkuchi
IPC分类号： A61K31/4545 , A61K31/444 , A61K31/4439 , A61K31/40 , C07D403/02 , C07D401/14
CPC分类号： A61K31/444 , A61K31/4468 , A61K31/4545 , C07D211/58 , C07D213/38 , C07D401/06 , C07D401/12 , C07D401/14
摘要： The present invention relates to a preventive or therapeutic agent for pathological conditions caused by reduced production of erythropoietin, or for anemia, or for chronic anemia, renal anemia, aplastic anemia, or pure red cell aplasia, the agent comprising, as an active ingredient, a cyclic amine compound represented by the following formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom, a halogen atom, or hydroxy, alkyl, halogen-substituted alkyl, alkoxy, alkylthio, carboxyl, alkoxycarbonyl or alkanoyl group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each represents a hydrogen atom, or an alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkyl, or substituted or unsubstituted heteroaralkyl group; and l, m and n each represents a number of 0 or 1, or a salt thereof or a solvate thereof.
摘要翻译：本发明涉及由促红细胞生成素或贫血，贫血，慢性贫血，肾性贫血，再生障碍性贫血或纯红细胞发育不全引起的病理状况的预防或治疗剂，所述药物包含作为活性成分的，由下式（1）表示的环胺化合物：其中R 1，R 2和R 3各自独立地表示氢原子卤素原子或羟基，烷基，卤素取代的烷基，烷氧基，烷硫基，羧基，烷氧基羰基或烷酰基; W 1和W 2各自独立地表示N或CH; X表示O，NR 4，CONR 4或NR 4 CO; R 4各自表示氢原子或烷基，烯基，炔基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的芳烷基或取代或未取代的杂芳烷基; l，m和n各自表示0或1的数，或其盐或其溶剂合物。

4. 发明授权

US06498169B1 Cyclic amine compounds and pharmaceutical composition containing the same 有权
标题翻译：环胺化合物和含有其的药物组合物
公开(公告)号：US06498169B1
公开(公告)日：2002-12-24
申请号：US09983928
申请日：2001-10-26
申请人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号： A61K314545
CPC分类号： C07D401/06 , A61K31/4545 , C07D211/58 , C07D401/12 , C07D401/14 , C07D403/14
摘要： A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 an W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each independently represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroalkyl group; and l, m and n each represents a number of 0 to 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译：由以下通式（1）表示的环胺化合物：其中，R 1，R 2和R 3各自独立地表示氢原子或烷氧基; W 1，W 2各自独立地表示N或CH; X表示O，NR 4，CONR 4或 NR4CO; R4各自独立地表示氢原子，或烷基，芳基，杂芳基，芳烷基或杂烷基; 和l，m和n各自表示0至1的数，其盐和其水合物。这些化合物对细胞粘附和细胞浸润均具有抑制作用，可用作抗哮喘剂，抗过敏剂，抗风湿剂，抗动脉硬化剂，抗炎剂，抗干燥素综合征剂等。

5. 发明申请

US20090143430A1 ERYTHROPOIETIN PRODUCTION ACCELERATOR 审中-公开
标题翻译：生产加速器
公开(公告)号：US20090143430A1
公开(公告)日：2009-06-04
申请号：US12326204
申请日：2008-12-02
申请人： Shigehiko IMAGAWA , Takeshi Doi , Masahiro Tamura , Masao Ohkuchi
发明人： Shigehiko IMAGAWA , Takeshi Doi , Masahiro Tamura , Masao Ohkuchi
IPC分类号： A61K31/4545
CPC分类号： A61K31/444 , A61K31/4468 , A61K31/4545 , C07D211/58 , C07D213/38 , C07D401/06 , C07D401/12 , C07D401/14
摘要： The present invention relates to a preventive or therapeutic agent for pathological conditions caused by reduced production of erythropoietin, or for anemia, or for chronic anemia, renal anemia, aplastic anemia, or pure red cell aplasia, the agent comprising, as an active ingredient, a cyclic amine compound represented by the following formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom, a halogen atom, or hydroxy, alkyl, halogen-substituted alkyl, alkoxy, alkylthio, carboxyl, alkoxycarbonyl or alkanoyl group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each represents a hydrogen atom, or an alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkyl, or substituted or unsubstituted heteroaralkyl group; and l, m and n each represents a number of 0 or 1, or a salt thereof or a solvate thereof.
摘要翻译：本发明涉及由促红细胞生成素或贫血，贫血，慢性贫血，肾性贫血，再生障碍性贫血或纯红细胞发育不全引起的病理状况的预防或治疗剂，所述药物包含作为活性成分的，由下式（1）表示的环胺化合物：其中，R 1，R 2和R 3各自独立地表示氢原子，卤素原子或羟基，烷基，卤素取代的烷基，烷氧基，烷硫基，羧基，烷氧基羰基或烷酰基组; W1和W2各自独立地表示N或CH; X表示O，NR4，CONR4或NR4CO; R 4各自表示氢原子，或烷基，烯基，炔基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的芳烷基或取代或未取代的杂芳烷基; l，m和n各自表示0或1的数，或其盐或其溶剂合物。

6. 发明授权

US06867221B2 Cyclic amine compounds and pharmaceutical composition containing the same 失效
标题翻译：环胺化合物和含有其的药物组合物
公开(公告)号：US06867221B2
公开(公告)日：2005-03-15
申请号：US10191534
申请日：2002-07-10
申请人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号： A61K31/4545 , A61P9/10 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D211/58 , C07D211/62 , C07D213/38 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
CPC分类号： C07D401/06 , A61K31/4545 , C07D211/58 , C07D211/62 , C07D213/38 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/14
摘要： A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译：由以下通式（1）表示的环胺化合物：其中，R 1，R 2和R 3各自独立地表示氢原子或烷氧基; W 1和W 2均为氢原子，各自独立地表示N或CH; X表示O，NR 4，CONR 4或NR 4 CO; R 4表示氢原子或烷基，芳基，杂芳基，芳烷基或杂芳烷基; 和l，m和n各自表示0或1的数，其盐和其水合物。这些化合物对细胞粘附和细胞浸润都具有抑制作用，并且可用作抗哮喘剂，抗过敏剂，抗风湿剂，抗动脉硬化剂，抗炎剂，抗干燥素综合征剂等。

7. 发明授权

US06605620B1 Cyclic amine compounds and pharmaceutical composition containing the same 有权
标题翻译：环胺化合物和含有其的药物组合物
公开(公告)号：US06605620B1
公开(公告)日：2003-08-12
申请号：US10107180
申请日：2002-03-28
申请人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号： A61K314545
CPC分类号： C07D401/06 , C07D211/58 , C07D213/38 , C07D401/12 , C07D401/14
摘要： A cyclic amine compound by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译：通式（1）表示的环状胺化合物：其中，R 1，R 2和R 3各自独立地表示氢原子或烷氧基，W 1和W 2各自独立地表示N或CH; X表示O，NR 4，CONR 4或NR 4 CO; R 4 表示氢原子，或烷基，芳基，杂芳基，芳烷基或杂芳烷基; 和l，m和n各自表示0或1的数，其盐和其水合物。这些化合物对细胞粘附和细胞浸润具有抑制作用，并且可用作抗哮喘药，抗过敏剂，抗风湿剂，抗动脉硬化剂，抗炎剂，抗干燥素综合征剂等。

8. 发明授权

US06395753B1 Cyclic amine compounds and pharmaceutical composition containing the same 有权
标题翻译：环胺化合物和含有其的药物组合物
公开(公告)号：US06395753B1
公开(公告)日：2002-05-28
申请号：US09941684
申请日：2001-08-30
申请人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
发明人： Tatsuhiko Kodama , Masahiro Tamura , Toshiaki Oda , Yukiyoshi Yamazaki , Masahiro Nishikawa , Shunji Takemura , Takeshi Doi , Yoshinori Kyotani , Masao Ohkuchi
IPC分类号： A61K314545
CPC分类号： C07D401/06 , A61K31/4545 , C07D211/58 , C07D401/12 , C07D401/14 , C07D403/14
摘要： A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each independently represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.
摘要翻译：由以下通式（1）表示的环胺化合物：其中，R1，R2和R3各自独立地表示氢原子或烷氧基; W1和W2各自独立地表示N或CH; X表示O，NR4，CONR4或 NR4CO; R4各自独立地表示氢原子，或烷基，芳基，杂芳基，芳烷基或杂芳烷基; 和l，m和n各自表示0或1的数，其盐和其水合物。这些化合物对细胞粘附和细胞浸润都具有抑制作用，并且可用作抗哮喘剂，抗过敏剂，抗风湿剂，抗动脉硬化剂，抗炎剂，抗干燥素综合征剂等。

9. 发明授权

US08575153B2 Pyridine-3-carboxyamide derivative 有权
标题翻译：吡啶-3-甲酰胺衍生物
公开(公告)号：US08575153B2
公开(公告)日：2013-11-05
申请号：US13131561
申请日：2009-11-27
申请人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
发明人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
IPC分类号： A61K31/506 , C07D239/48
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12
摘要： To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.
摘要翻译：提供可用作器官移植，类风湿关节炎，多发性硬化症，系统性红斑狼疮，Sjögren综合征，Behcet氏病，I型糖尿病的排斥反应和宿主疾病（GvHD）的预防和/或治疗剂的新型JAK3抑制剂过敏性甲状腺炎，特发性血小板减少性紫癜，溃疡性结肠炎，克罗恩病，哮喘，过敏性鼻炎，特应性皮炎，接触性皮炎，荨麻疹，湿疹，牛皮癣，过敏性结膜炎，葡萄膜炎，癌症，白血病等。由通式（1）表示的吡啶-3-甲酰胺衍生物或其盐或其溶剂化物。

10. 发明申请

US20110237590A1 PYRIDINE-3-CARBOXYAMIDE DERIVATIVE 有权
标题翻译：吡啶-3-羧酰胺衍生物
公开(公告)号：US20110237590A1
公开(公告)日：2011-09-29
申请号：US13131561
申请日：2009-11-27
申请人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
发明人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
IPC分类号： A61K31/5377 , C07D213/74 , C07D401/12 , C07D413/12 , C07D211/46 , A61K31/44 , A61K31/497 , A61K31/4545 , A61P37/02 , A61P37/06
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12
摘要： To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.
摘要翻译：提供可用作器官移植，类风湿关节炎，多发性硬化症，系统性红斑狼疮，Sjögren综合征，Behcet氏病，I型糖尿病的排斥反应和宿主疾病（GvHD）的预防和/或治疗剂的新型JAK3抑制剂过敏性甲状腺炎，特发性血小板减少性紫癜，溃疡性结肠炎，克罗恩病，哮喘，过敏性鼻炎，特应性皮炎，接触性皮炎，荨麻疹，湿疹，牛皮癣，过敏性结膜炎，葡萄膜炎，癌症，白血病等。由通式（1）表示的吡啶-3-甲酰胺衍生物或其盐或其溶剂合物。

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