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公开(公告)号:US20100168159A1
公开(公告)日:2010-07-01
申请号:US12696327
申请日:2010-01-29
申请人: Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Masataka Morita , Sunao Imada , Yoshito Abe , Hiromichi Itani , Tatsuaki Morokata , Hideo Tsutsumi
发明人: Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Masataka Morita , Sunao Imada , Yoshito Abe , Hiromichi Itani , Tatsuaki Morokata , Hideo Tsutsumi
IPC分类号: A61K31/4439 , A61K31/4709 , C07D471/04 , C07D413/14 , A61P35/02 , A61P37/06 , A61P29/00 , A61P9/10 , A61P35/00
CPC分类号: C07D413/04 , C07D417/04 , C07D471/04
摘要: [Problems]To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.[Means for solving]Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.
摘要翻译: [问题]提供一种有用的化合物作为活性成分,用于预防和/或治疗移植器官,骨髓或组织,自身免疫疾病等中的排斥反应,其具有优异的S1P1激动剂 活动。 [解决方法]由于本发明的化合物具有S1P1激动剂活性,因此可用作由不利的淋巴细胞浸润引起的疾病的治疗或预防剂的活性成分,例如自身免疫性疾病如移植排斥反应 器官移植,骨髓或组织,移植物抗宿主病,风湿性关节炎,多发性硬化,系统性红斑狼疮,肾病综合征,脑炎,重症肌无力,胰腺炎,肝炎,肾炎,糖尿病,肺功能障碍 哮喘,特应性皮炎,炎症性肠病,动脉粥样硬化,局部缺血再灌注损伤,炎症性疾病等疾病,以及癌症,白血病等细胞异常生长或积累引起的疾病。
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公开(公告)号:US20070043084A1
公开(公告)日:2007-02-22
申请号:US10555656
申请日:2004-04-26
IPC分类号: A61K31/444 , A61K31/4439 , C07D403/04
CPC分类号: C07D401/12 , C07D233/90 , C07D417/12
摘要: A compound of the formula (1): wherein R1 is cyano, and the like; R2 is hydroxy, and the like; R3 is (lower)alkoxy, and the like; X and Y are each CH or N; or pharmaceutically acceptable salts thereof, which are useful as a medicament.
摘要翻译: 式(1)的化合物:其中R 1是氰基等; R 2是羟基等; R 3是(低级)烷氧基等; X和Y各自为CH或N; 或其药学上可接受的盐,其可用作药物。
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公开(公告)号:US08163767B2
公开(公告)日:2012-04-24
申请号:US11995445
申请日:2006-07-13
申请人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
发明人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Yutaka Nakajima , Keiko Hatanaka , Shohei Shirakami , Hiroshi Sasaki , Akira Tanaka , Fumie Takahashi , Koichiro Mukoyoshi , Yasuyuki Higashi , Akira Okimoto , Takeshi Hondo , Hitoshi Sawada
IPC分类号: A61K31/44 , C07D471/14
CPC分类号: C07D471/14 , C07D519/00
摘要: The invention relates to compound of the formula (I) or its salt, wherein —R1, —R2, —R3, —R4, —R5, -M-, —X— and —Y═ are as defined in the description, their use of as, medicament, the process for their preparation and use for the treatment of JAK3 mediated diseases.
摘要翻译: 本发明涉及式(I)化合物或其盐,其中-R1,-R2,-R3,-R4,-R5,-M-,-X-和-Y =如说明书中所定义,它们 使用as,药物,其制备方法和用于治疗JAK3介导的疾病。
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公开(公告)号:US20090076070A1
公开(公告)日:2009-03-19
申请号:US12244102
申请日:2008-10-02
申请人: Hironori HARADA , Kazuyuki Hattori , Kazuya Fujita , Masataka Morita , Sunao Imada , Yoshito Abe , Hiromichi Itani , Tatsuaki Morokata , Hideo Tsutsumi
发明人: Hironori HARADA , Kazuyuki Hattori , Kazuya Fujita , Masataka Morita , Sunao Imada , Yoshito Abe , Hiromichi Itani , Tatsuaki Morokata , Hideo Tsutsumi
IPC分类号: A61K31/4245 , C07D413/14 , A61K31/437 , A61P35/02 , A61P19/02 , A61P1/00 , A61P9/10 , A61P37/06 , A61P35/00 , A61K31/4709
CPC分类号: C07D413/04 , C07D417/04 , C07D471/04
摘要: [Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 agonist activity.[Means for Solving] Since the compound of the invention has an S1P1 agonist activity, it is useful as an active ingredient for a treating or preventing agent for a disease caused by unfavorable lymphocytic infiltration, for example, an autoimmune disease such as graft rejection in the transplantation of an organ, bone marrow, or a tissue, a graft-versus-host disease, rheumatic arthritis, multiple sclerosis, systemic lupus erythematosus, a nephrotic syndrome, encephalomeningitis, myasthenia gravis, pancreatitis, hepatitis, nephritis, diabetes, pulmonary disorder, asthma, atopic dermatitis, inflammatory bowel disease, atherosclerosis, ischemia-reperfusion injury, or an inflammatory disease, and further, a disease caused by the abnormal growth or accumulation of cells such as cancer and leukemia.
摘要翻译: [问题]提供一种有用的化合物作为活性成分,用于预防和/或治疗移植器官,骨髓或组织,自身免疫疾病等中的排斥反应,其具有优异的S1P1激动剂 活动。 [解决手段]由于本发明的化合物具有S1P1激动剂活性,因此可用作由不利的淋巴细胞浸润引起的疾病的治疗或预防剂的活性成分,例如自身免疫性疾病例如移植排斥反应 器官移植,骨髓或组织,移植物抗宿主病,风湿性关节炎,多发性硬化,系统性红斑狼疮,肾病综合征,脑炎,重症肌无力,胰腺炎,肝炎,肾炎,糖尿病,肺功能障碍 哮喘,特应性皮炎,炎症性肠病,动脉粥样硬化,局部缺血再灌注损伤,炎症性疾病等疾病,以及癌症,白血病等细胞异常生长或积累引起的疾病。
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公开(公告)号:US07442715B2
公开(公告)日:2008-10-28
申请号:US11505321
申请日:2006-08-17
申请人: Akira Nagashima , Takayuki Inoue , Mitsuru Ohkubo , Kousei Yoshihara , Takashi Tojo , Masataka Morita
发明人: Akira Nagashima , Takayuki Inoue , Mitsuru Ohkubo , Kousei Yoshihara , Takashi Tojo , Masataka Morita
IPC分类号: A61K31/427
CPC分类号: C07D417/06 , C07D277/46 , C07D277/48 , C07D277/56 , C07D417/12
摘要: A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.
摘要翻译: 式(I)化合物:其中各符号如说明书中所定义,或其药学上可接受的盐可用作血管粘附蛋白-1(1R) VAP-1)抑制剂,药物组合物,预防或治疗VAP-1相关疾病,尤其是黄斑水肿的方法,该方法包括将有效量的化合物或其药学上可接受的盐给予哺乳动物等 。
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公开(公告)号:US20070254931A1
公开(公告)日:2007-11-01
申请号:US11572772
申请日:2005-07-27
申请人: Takayuki Inoue , Takashi Tojo , Masataka Morita
发明人: Takayuki Inoue , Takashi Tojo , Masataka Morita
IPC分类号: A61K31/426 , A61P19/02 , A61P19/08 , A61P3/10 , A61P9/10 , C07D277/46
CPC分类号: C07D277/46
摘要: A compound of the formula (I), (II), (III) or (IV): wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a subject, and the like.
摘要翻译: 式(I),(II),(III)或(IV)的化合物:其中每个符号如说明书中所定义,或其药学上可接受的盐可用作血管粘附蛋白-1(VAP-1) 抑制剂,药物组合物,预防或治疗VAP-1相关疾病,特别是黄斑水肿的方法,该方法包括向受试者施用有效量的化合物或其药学上可接受的盐等。
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公开(公告)号:US07214177B2
公开(公告)日:2007-05-08
申请号:US10422852
申请日:2003-04-25
申请人: Masaharu Aizawa , Masataka Morita
发明人: Masaharu Aizawa , Masataka Morita
IPC分类号: B04B5/02
CPC分类号: B01L3/5021 , B01L3/50825 , B04B5/0414 , C12M23/08 , C12M23/38 , C12M33/10
摘要: A culture/centrifugal tube includes a tube and a cap. The cap has a disk portion and an annular portion that define an annular groove therebetween. The annular groove opens at a position level with the surface of the disk portion. The open end of the tube extends into the annular groove, with the open end of the vessel in abutment against the surface of the disk portion when the cap is fully engaged on the tube. An angle rotor that is used in a centrifuge is formed with an accommodation hole that receives the culture/centrifugal tube. The accommodation hole including a smaller-diameter tube accommodating portion that accommodates the tube and a larger-diameter cap accommodating portion that accommodates the cap. The cap accommodating portion includes a region that entirely encompasses a corresponding portion of the outer periphery of the annular portion of the cap.
摘要翻译: 培养/离心管包括管和帽。 盖具有在其间限定环形槽的圆盘部分和环形部分。 环形槽在与盘部分的表面的位置水平位置处打开。 管的开口端延伸到环形槽中,当盖完全接合在管上时,容器的开口端抵靠盘部分的表面。 在离心机中使用的角度转子形成有容纳培养/离心管的容纳孔。 容纳孔包括容纳管的较小直径的管容纳部分和容纳盖的较大直径的盖容纳部分。 盖容纳部分包括完全包围盖的环形部分的外周的相应部分的区域。
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公开(公告)号:US07125901B2
公开(公告)日:2006-10-24
申请号:US10764529
申请日:2004-01-27
申请人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
发明人: Takayuki Inoue , Takashi Tojo , Masataka Morita , Mitsuru Ohkubo , Kousei Yoshihara , Akira Nagashima
IPC分类号: A61K31/427 , C07D277/44
CPC分类号: C07D417/06 , C07D277/46 , C07D277/48 , C07D277/56 , C07D417/12
摘要: A compound of the formula (I): R1—NH—X—Y-Z (I) wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, a method for preventing or treating a VAP-1 associated disease, especially macular edema, which method includes administering an effective amount of the compound or a pharmaceutically acceptable salt thereof to a mammal, and the like.
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公开(公告)号:US20060014948A1
公开(公告)日:2006-01-19
申请号:US10968473
申请日:2004-10-20
申请人: Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
发明人: Kazuhiko Take , Nobukiyo Konishi , Shinji Shigenaga , Natsuko Kayakiri , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Junya Ishida , Masataka Morita
IPC分类号: A61K31/5377 , C07D413/02 , C07D43/02
CPC分类号: C07D401/06 , C07D241/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D471/04 , C07D491/08 , C07D495/04 , C07D498/04 , C07D498/08 , C07F7/1804
摘要: This invention relates to piperazine derivatives of the formula: wherein each symbol is as defined in the description, and its pharmaceutically acceptable salt, to processes for preparation thereof, to pharmaceutical composition comprising the same, and to a use of the same for treating or preventing Tachykinin-mediated diseases in human being or animals.
摘要翻译: 本发明涉及下式的哌嗪衍生物:其中每个符号如说明书中所定义,及其药学上可接受的盐,其制备方法,包含其的药物组合物及其用于治疗或预防的用途 速激肽介导的人类或动物疾病。
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公开(公告)号:US06787543B2
公开(公告)日:2004-09-07
申请号:US10297937
申请日:2002-12-20
申请人: Kazuhiko Take , Chiyoshi Kasahara , Shinji Shigenaga , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Masataka Morita
发明人: Kazuhiko Take , Chiyoshi Kasahara , Shinji Shigenaga , Hidenori Azami , Yoshiteru Eikyu , Kazuo Nakai , Masataka Morita
IPC分类号: A61K31495
CPC分类号: C07D265/30 , C07C45/71 , C07D241/04 , C07D241/08 , C07D403/10 , C07D487/04 , C07C47/575
摘要: A compound of the formula (I): in which Z, R1, R2, R8, R10, R11, R12, R13 and R14 are each as defined in the description, or a salt thereof. The object compound of the present invention has pharmacological activities such as Tachykinin antagonism, and is useful for manufacture of a medicament for treating or preventing Tachykinin-mediated diseases.
摘要翻译: 式(I)的化合物:其中Z,R 1,R 2,R 8,R 10,R 11,R 12,R 13和R 13, 14>各自如说明书中所定义,或其盐。 本发明的目的化合物具有速激肽拮抗作用等药理活性,可用于制备治疗或预防速激肽介导的疾病的药物。
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