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。

公开(公告)号：US20100222347A1

公开(公告)日：2010-09-02

申请号：US12680307

申请日：2008-09-29

申请人： Masanori Ashikawa ,  Junya Tagashira ,  Akiyasu Koketsu ,  Toshiharu Morimoto ,  Tatsuaki Nishiyama ,  Satoshi Goda ,  Masaki Yamabi ,  Takeshi Doi ,  Hiroyuki Ishiwata

发明人： Masanori Ashikawa ,  Junya Tagashira ,  Akiyasu Koketsu ,  Toshiharu Morimoto ,  Tatsuaki Nishiyama ,  Satoshi Goda ,  Masaki Yamabi ,  Takeshi Doi ,  Hiroyuki Ishiwata

IPC分类号： A61K31/5377 ,  C07D215/08 ,  A61K31/4706 ,  C07D413/12 ,  C07D215/233 ,  A61K31/47 ,  A61P7/00

CPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  C07D215/22 ,  C07D215/44 ,  C07D413/04 ,  C07D413/12

摘要： Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the general formula (1); [wherein R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N—R11 or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.

摘要翻译： 公开了具有EPO生产促进活性和/或血红蛋白表达增强活性的低分子量化合物。 具体公开的是EPO生产促进剂和/或血红蛋白表达增强剂，其包含1-酰基-4-（苯氧基，苄氧基或苯基氨基）-1,2,3,4-四氢喹啉衍生物，更具体地是由通式 公式1）; [其中R1，R2，R2'，R3和R3'独立地表示氢原子，C1-6烷基等; R 4，R 5，R 6，R 7，R 8，R 9和R 10独立地表示氢原子，卤素原子，C 1-6烷基等; A表示N-R11或氧原子; R 11表示氢原子，C 1-6烷基等; n表示0或1的整数]，四氢喹啉化合物的盐或四氢喹啉化合物或其盐的溶剂合物。

公开(公告)号：US08791090B2

公开(公告)日：2014-07-29

申请号：US13256549

申请日：2010-03-31

申请人： Masanori Ashikawa ,  Junya Tagashira ,  Akiyasu Koketsu ,  Toshiharu Morimoto ,  Takahiro Kitamura ,  Syunji Takemura ,  Gen Watanabe ,  Tatsuaki Nishiyama ,  Satoshi Goda ,  Masaki Yamabi ,  Takeshi Doi ,  Hiroyuki Ishiwata

发明人： Masanori Ashikawa ,  Junya Tagashira ,  Akiyasu Koketsu ,  Toshiharu Morimoto ,  Takahiro Kitamura ,  Syunji Takemura ,  Gen Watanabe ,  Tatsuaki Nishiyama ,  Satoshi Goda ,  Masaki Yamabi ,  Takeshi Doi ,  Hiroyuki Ishiwata

IPC分类号： A01N57/00 ,  A61K31/385

CPC分类号： C07D215/42 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/69 ,  C07D215/233 ,  C07D215/44 ,  C07D215/46 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

摘要： Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N—R11, a sulfur atom, or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; B represents a C6-14 aryl group, or a 5- to 10-membered heterocyclic group; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.

摘要翻译： 公开了具有低分子量且具有增强EPO产生活性和/或提高血红蛋白生成活性的化合物。 具体公开的是EPO生产增强剂和/或包含1-酰基-4-（取代的氧基，取代的氨基或取代的硫代）-1,2,3,4-四氢喹啉衍生物，更具体地是四氢喹啉化合物的血红蛋白生成增强剂 由通式（1）表示[其中R1，R2，R2'，R3和R3'独立地表示氢原子，C1-6烷基等; R 4，R 5，R 6，R 7，R 8，R 9和R 10独立地表示氢原子，卤素原子，C 1-6烷基等; A表示N-R11，硫原子或氧原子; R 11表示氢原子，C 1-6烷基等; B表示C 6-14芳基或5至10元杂环基; n表示0或1的整数]，四氢喹啉化合物的盐或四氢喹啉化合物或其盐的溶剂合物。

公开(公告)号：US20120004197A1

公开(公告)日：2012-01-05

申请号：US13256549

申请日：2010-03-31

申请人： Masanori Ashikawa ,  Junya Tagashira ,  Akiyasu Koketsu ,  Toshiharu Morimoto ,  Takahiro Kitamura ,  Syunji Takemura ,  Gen Watanabe ,  Tatsuaki Nishiyama ,  Satoshi Goda ,  Masaki Yamabi ,  Takeshi Doi ,  Hiroyuki Ishiwata

发明人： Masanori Ashikawa ,  Junya Tagashira ,  Akiyasu Koketsu ,  Toshiharu Morimoto ,  Takahiro Kitamura ,  Syunji Takemura ,  Gen Watanabe ,  Tatsuaki Nishiyama ,  Satoshi Goda ,  Masaki Yamabi ,  Takeshi Doi ,  Hiroyuki Ishiwata

IPC分类号： A61K31/4706 ,  C07D413/12 ,  C07D215/14 ,  C07D215/233 ,  C07D401/12 ,  A61P7/06 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/47 ,  A61K31/496 ,  A61K31/69 ,  C07D215/44 ,  C07F5/02

CPC分类号： C07D215/42 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/69 ,  C07D215/233 ,  C07D215/44 ,  C07D215/46 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

摘要： Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N—R11, a sulfur atom, or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; B represents a C6-14 aryl group, or a 5- to 10-membered heterocyclic group; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.

摘要翻译： 公开了具有低分子量且具有增强EPO产生活性和/或提高血红蛋白生成活性的化合物。 具体公开的是EPO生产增强剂和/或包含1-酰基-4-（取代的氧基，取代的氨基或取代的硫代）-1,2,3,4-四氢喹啉衍生物，更具体地是四氢喹啉化合物的血红蛋白生成增强剂 由通式（1）表示[其中R1，R2，R2'，R3和R3'独立地表示氢原子，C1-6烷基等; R 4，R 5，R 6，R 7，R 8，R 9和R 10独立地表示氢原子，卤素原子，C 1-6烷基等; A表示N-R11，硫原子或氧原子; R 11表示氢原子，C 1-6烷基等; B表示C 6-14芳基或5至10元杂环基; n表示0或1的整数]，四氢喹啉化合物的盐或四氢喹啉化合物或其盐的溶剂合物。

公开(公告)号：US20120108581A1

公开(公告)日：2012-05-03

申请号：US13260711

申请日：2010-03-25

申请人： Masanori Ashikawa ,  Toshiharu Morimoto ,  Hajime Yamada ,  Shunji Takemura ,  Tatsuaki Nishiyama ,  Takeshi Doi ,  Hiroyuki Ishiwata

发明人： Masanori Ashikawa ,  Toshiharu Morimoto ,  Hajime Yamada ,  Shunji Takemura ,  Tatsuaki Nishiyama ,  Takeshi Doi ,  Hiroyuki Ishiwata

IPC分类号： A61K31/473 ,  A61K31/4375 ,  C12N5/02 ,  C07D495/04 ,  A61K31/4365 ,  A61P7/06 ,  A61K31/4745 ,  C07D491/052 ,  A61K31/4741 ,  C07D491/056 ,  C07D498/04 ,  A61K31/5383 ,  C07D471/04 ,  C07D221/10

CPC分类号： C07D221/06 ,  C07D471/04 ,  C07D491/052 ,  C07D491/056 ,  C07D498/04

摘要： The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.

摘要翻译： 本发明提供具有EPO生产促进作用和/或血红蛋白生产促进作用的低分子量化合物。 本发明涉及由以下通式（1）表示的稠合哌啶化合物：其中环A表示C10-14芳基或5-至10-元杂环基，X表示N-R7，硫原子 或氧原子，R 1，R 2，R 2'，R 3和R 3'独立地表示氢原子，C 1-6烷基或C 3-6环烷基，R 4，R 5和R 6独立地表示氢原子或卤素原子） 或其盐，或其溶剂合物。

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。

公开(公告)号：US08604030B2

公开(公告)日：2013-12-10

申请号：US13260711

申请日：2010-03-25

申请人： Masanori Ashikawa ,  Toshiharu Morimoto ,  Hajime Yamada ,  Shunji Takemura ,  Tatsuaki Nishiyama ,  Takeshi Doi ,  Hiroyuki Ishiwata

发明人： Masanori Ashikawa ,  Toshiharu Morimoto ,  Hajime Yamada ,  Shunji Takemura ,  Tatsuaki Nishiyama ,  Takeshi Doi ,  Hiroyuki Ishiwata

IPC分类号： A61K31/5377 ,  A61K31/4706 ,  A61K31/47 ,  C07D215/08 ,  C07D413/12 ,  C07D215/233

CPC分类号： C07D221/06 ,  C07D471/04 ,  C07D491/052 ,  C07D491/056 ,  C07D498/04

摘要： The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.

摘要翻译： 本发明提供具有EPO生产促进作用和/或血红蛋白生产促进作用的低分子量化合物。 本发明涉及由以下通式（1）表示的稠合哌啶化合物：其中环A表示C10-14芳基或5-至10-元杂环基，X表示N-R7，硫原子 或氧原子，R 1，R 2，R 2'，R 3和R 3'独立地表示氢原子，C 1-6烷基或C 3-6环烷基，R 4，R 5和R 6独立地表示氢原子或卤素原子） 或其盐，或其溶剂合物。