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。

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：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：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：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。

公开(公告)号：US06552188B2

公开(公告)日：2003-04-22

申请号：US09893699

申请日：2001-06-29

申请人： Tatsuhiko Kodama ,  Masahiro Tamura ,  Toshiaki Oda ,  Yukiyoshi Yamazaki ,  Masahiro Nishikawa ,  Shunji Takemura ,  Takeshi Doi ,  Yoshinori Kyotani

发明人： Tatsuhiko Kodama ,  Masahiro Tamura ,  Toshiaki Oda ,  Yukiyoshi Yamazaki ,  Masahiro Nishikawa ,  Shunji Takemura ,  Takeshi Doi ,  Yoshinori Kyotani

IPC分类号： A61K31496

CPC分类号： C07D213/81 ,  C07D213/36 ,  C07D213/82 ,  C07D401/12

摘要： Cyclic diamine compounds of formula (1) are disclosed: wherein A is (CH2)n, (CH2)n—CH═CH, CO—(CH2)n or CO—(CH2)n—CH═CH, in which n is a number of 0 to 3; Z represents a formula (2) or (3): in which R1, R2, R4, R5 and R6 are individually a hydrogen atom, alkyl group, alkoxy group, halogen atom or nitro group; R3is a hydrogen atom, alkyl group, alkoxy group, halogen atom, nitro group, naphthyl group, or phenyl group which may be substituted by 1 to 3 substituents selected from the group consisting of alkyl groups, alkoxy groups, halogen atoms, a nitro group and a phenyl group; and X and Y are individually CH or a nitrogen atom; and m is 1 or 2; an acid-addition salt thereof, or a hydrate thereof, and a medicine containing such a compound.

摘要翻译： 公开了式（1）的环二胺化合物：其中A是（CH 2）n，（CH 2）n -CH = CH，CO-（CH 2）n或CO-（CH 2）n -CH = CH，其中n是 数字0到3; Z表示式（2）或（3）：其中R1，R2，R4，R5和R6分别为氢原子，烷基，烷氧基，卤素原子或硝基; R3是氢原子，烷基，烷氧基，卤素原子，硝基，萘基或可以被1〜3个选自烷基，烷氧基，卤原子，硝基的取代基取代的苯基 和苯基; X和Y分别是CH或氮原子; m为1或2;其酸加成盐或其水合物，以及含有这种化合物的药物。

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。

公开(公告)号：US20050176764A1

公开(公告)日：2005-08-11

申请号：US10510759

申请日：2003-04-11

申请人： Chikage Mataki ,  Tatsuhiko Kodama ,  Takeshi Doi ,  Masahiro Tamura ,  Toshiaki Oda ,  Yukiyoshi Yamazaki ,  Masahiro Nishikawa ,  Shunji Takemura ,  Masao Ohkuch

发明人： Chikage Mataki ,  Tatsuhiko Kodama ,  Takeshi Doi ,  Masahiro Tamura ,  Toshiaki Oda ,  Yukiyoshi Yamazaki ,  Masahiro Nishikawa ,  Shunji Takemura ,  Masao Ohkuch

IPC分类号： C07D295/12 ,  A61K31/445 ,  A61K31/4545 ,  A61K48/00 ,  A61P35/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D491/10

CPC分类号： C07D401/06 ,  A61K31/445 ,  A61K31/4545 ,  C04B35/632 ,  C07D295/12 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D491/10

摘要： Abstract The present invention is directed to a method for treating cancer, a method for inhibiting histone deacetylase, and a method for facilitating gene therapy, comprising administering an effective amount of a cyclic amine compound represented by the following formula (1):(wherein R1, R2, and R3 each independently represent a hydrogen atom, a halogen atom, a hydroxy group, an alkyl group, a halogen-substituted alkyl group, an alkoxy group, an alkylthio group, a carboxyl group, an alkoxycarbonyl group, or an alkanoyl group; W1 and W2, which are identical to or different from each other, represent N or CH; X represents O, NR4, CONR4, or NR4CO; R4 represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted heteroaralkyl group; and l, m, and n each represent a number of 0 or 1), a salt thereof, or a hydrate thereof.208

摘要翻译： 摘要本发明涉及一种治疗癌症的方法，一种抑制组蛋白脱乙酰酶的方法和一种促进基因治疗的方法，包括给予有效量的由下式（1）表示的环胺化合物:(其中R1 R 2和R 3各自独立地表示氢原子，卤素原子，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 基团W 1和W 2彼此相同或不同，表示N或CH; X表示O，NR 4，CONR 4或NR 4 CO; R 4表示氢原子，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），其盐， o 其水合物

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。

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。