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1. 发明授权

US07951825B2 Hetero compound 有权
标题翻译：杂环化合物
公开(公告)号：US07951825B2
公开(公告)日：2011-05-31
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： C07D413/02 , C07D413/14 , C07D401/02 , C07D401/14 , A61K31/443
CPC分类号： C07D413/04 , C07D417/04 , C07D471/04
摘要： 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.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：为了提供具有优异的S1P1激动剂活性的器官，骨髓或组织，自身免疫疾病等的移植中的预防和/或治疗剂的有效成分的有用化合物。由于本发明的化合物具有S1P1激动剂活性，因此可用作治疗或预防由不利淋巴细胞浸润引起的疾病的活性成分，例如自体免疫疾病例如器官移植中的移植排斥反应骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化症，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，肺病，哮喘，特应性皮炎炎症性肠病，动脉粥样硬化，缺血再灌注损伤或炎性疾病，以及由细胞如癌症和白血病的异常生长或积累引起的疾病。

2. 发明授权

US07678820B2 Hetero compound 有权
标题翻译：杂环化合物
公开(公告)号：US07678820B2
公开(公告)日：2010-03-16
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 , C07D271/06
CPC分类号： C07D413/04 , C07D417/04 , C07D471/04
摘要： 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. 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：为了提供具有优异的S1P1激动剂活性的器官，骨髓或组织，自身免疫疾病等的移植中的预防和/或治疗剂的有效成分的有用化合物。由于本发明的化合物具有S1P1激动剂活性，因此可用作治疗或预防由不利淋巴细胞浸润引起的疾病的活性成分，例如自体免疫疾病例如器官移植中的移植排斥反应骨髓或组织，移植物抗宿主病，风湿性关节炎，多发性硬化症，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，肺病，哮喘，特应性皮炎炎症性肠病，动脉粥样硬化，缺血再灌注损伤或炎性疾病，以及由细胞如癌症和白血病的异常生长或积累引起的疾病。

3. 发明申请

US20100168159A1 HETERO COMPOUND 有权
标题翻译： HETERO化合物
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。

4. 发明申请

US20090076070A1 HETERO COMPOUND 有权
标题翻译： HETERO化合物
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。

5. 发明申请

US20120178735A1 2H-CHROMENE COMPOUND AND DERIVATIVE THEREOF 审中-公开
标题翻译： 2H-氯化合物及其衍生物
公开(公告)号：US20120178735A1
公开(公告)日：2012-07-12
申请号：US13396861
申请日：2012-02-15
申请人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Sunao Imada , Tatsuaki Morokata
发明人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Sunao Imada , Tatsuaki Morokata
IPC分类号： A61K31/4025 , A61K31/397 , A61K31/427 , A61P29/00 , A61K31/444 , A61K31/5377 , A61K31/497 , A61P37/06 , A61K31/453 , A61K31/4155
CPC分类号： C07D403/12 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Provided is a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action. The 2H-chromene compound or derivative is particularly useful for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.
摘要翻译：提供具有优异的S1P1激动剂作用的2H-色烯化合物或其衍生物。 2H-色烯化合物或衍生物特别可用于预防和/或治疗由不希望的淋巴细胞浸润引起的疾病或由细胞的异常增殖或积聚引起的疾病。

6. 发明授权

US08193378B2 2H-chromene compound and derivative thereof 有权
标题翻译： 2H-色烯化合物及其衍生物
公开(公告)号：US08193378B2
公开(公告)日：2012-06-05
申请号：US13131343
申请日：2009-12-04
申请人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Sunao Imada , Tatsuaki Morokata
发明人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Sunao Imada , Tatsuaki Morokata
IPC分类号： C07D311/00
CPC分类号： C07D403/12 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells. According to the present invention, a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient of an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells can be provided. The 2H-chromene compound and a derivative thereof which are the compounds of the present invention have an S1P1 agonist action, and can be used particularly for prevention and/or treatment of a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.
摘要翻译：本发明提供了具有优异的S1P1激动剂作用的化合物，特别是用于预防和/或治疗由不希望的淋巴细胞浸润引起的疾病或由细胞的异常增殖或积聚引起的疾病的活性成分。根据本发明，具有优异的S1P1激动剂作用的2H-色烯化合物或其衍生物，并且特别用作预防和/或治疗由不想要的淋巴细胞浸润或疾病引起的疾病的药剂的活性成分可以提供异常增殖或细胞积聚诱导的细胞。作为本发明化合物的2H-色烯化合物及其衍生物具有S1P1激动剂作用，可以特别用于预防和/或治疗由不想要的淋巴细胞浸润引起的疾病或由异常增殖诱导的疾病或细胞积聚。

7. 发明申请

US20110230463A1 2H-CHROMENE COMPOUND AND DERIVATIVE THEREOF 有权
标题翻译： 2H-氯化合物及其衍生物
公开(公告)号：US20110230463A1
公开(公告)日：2011-09-22
申请号：US13131343
申请日：2009-12-04
申请人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Sunao Imada , Tatsuaki Morokata
发明人： Hironori Harada , Kazuyuki Hattori , Kazuya Fujita , Sunao Imada , Tatsuaki Morokata
IPC分类号： A61K31/397 , C07D405/06 , A61K31/4025 , C07D417/14 , A61K31/428 , A61K31/453 , C07D405/14 , A61K31/404 , C07D409/14 , A61K31/427 , A61K31/4155 , A61K31/4433 , C07D311/58 , A61K31/352 , A61P29/00 , A61P37/06 , A61P25/28
CPC分类号： C07D403/12 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14
摘要： [Object] Provided is a compound which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient for an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.[Means for Solution] According to the present invention, a 2H-chromene compound or a derivative thereof which has an excellent S1P1 agonist action, and is useful particularly as an active ingredient of an agent for preventing and/or treating a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells can be provided. The 2H-chromene compound and a derivative thereof which are the compounds of the present invention have an S1P1 agonist action, and can be used particularly for prevention and/or treatment of a disease induced by undesirable lymphocyte infiltration or a disease induced by abnormal proliferation or accumulation of cells.
摘要翻译：本发明提供具有优异的S1P1激动剂作用的化合物，特别是用于预防和/或治疗由不希望的淋巴细胞浸润引起的疾病或由细胞的异常增殖或积聚引起的疾病的活性成分。 [解决方案]根据本发明，具有优异的S1P1激动剂作用的2H-色烯化合物或其衍生物，特别是作为用于预防和/或治疗由不希望的可以提供淋巴细胞浸润或由细胞的异常增殖或积聚诱导的疾病。作为本发明化合物的2H-色烯化合物及其衍生物具有S1P1激动剂作用，可以特别用于预防和/或治疗由不想要的淋巴细胞浸润引起的疾病或由异常增殖诱导的疾病或细胞积聚。

8. 发明授权

US07816558B2 Triarylcarboxylic acid derivative 失效
标题翻译：三芳基羧酸衍生物
公开(公告)号：US07816558B2
公开(公告)日：2010-10-19
申请号：US11910072
申请日：2006-10-06
申请人： Junji Sato , Kazuyuki Hattori , Hirokazu Kubota , Ryosuke Munakata , Toru Asano , Junko Maeda , Masakatsu Kawakami , Akio Kamikawa
发明人： Junji Sato , Kazuyuki Hattori , Hirokazu Kubota , Ryosuke Munakata , Toru Asano , Junko Maeda , Masakatsu Kawakami , Akio Kamikawa
IPC分类号： C07C63/33 , C07C321/00 , C07D277/04 , C07D333/62 , C07D231/10 , C07D211/78 , A01N43/40 , A01N43/82 , A01N43/06
CPC分类号： C07D213/79 , C07D231/14 , C07D261/18 , C07D275/03 , C07D277/56 , C07D333/38 , C07D333/60 , C07D333/76 , C07D401/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.
摘要翻译：提供由以下通式（I）表示的三芳基羧酸衍生物或其异构体，前药，水合物，溶剂合物，多晶型物或其药学上可接受的盐：其中A是任选取代的芳基或杂芳基，和B是任选取代的单环杂芳基; 以及包含其的药物组合物和药学上可接受的载体。三芳基羧酸衍生物（I）表现出有效的黄嘌呤氧化酶抑制作用，因此可用作预防或治疗高尿酸血症，痛风，炎性肠病，糖尿病性肾病和糖尿病性视网膜病变的治疗剂。

9. 发明授权

US07612108B2 2-phenylthiophene derivative 失效
标题翻译： 2-苯基噻吩衍生物
公开(公告)号：US07612108B2
公开(公告)日：2009-11-03
申请号：US11661294
申请日：2005-08-26
申请人： Junji Miyata , Masaki Yokota , Ryo Naito , Akio Kamikawa , Masakatsu Kawakami , Kazuyuki Hattori
发明人： Junji Miyata , Masaki Yokota , Ryo Naito , Akio Kamikawa , Masakatsu Kawakami , Kazuyuki Hattori
IPC分类号： A61K31/381 , C07D333/16
CPC分类号： C07D333/40 , C07D409/04 , C07D409/10 , C07D417/10 , C07D417/12
摘要： The present invention relates to a 2-phenylthiophene derivative or a salt thereof, wherein the thiophene ring is substituted with a carboxyl group or the like and the benzene ring has an electron-withdrawing group such as a cyano group and an electron-donating group such as a substituted alkoxy group at the same time. Since the compound of the invention has good xanthine oxidase-inhibitory action and uric acid-lowering action and does not have a structure derived from nucleic acid, the compound has advantages of high safety and excellent effects as compared with conventional compounds and is useful as a therapeutic or preventive agent for hyperuricemia, gout, inflammatory bowel diseases, diabetic kidney diseases, diabetic retinopathy, or the like.
摘要翻译：本发明涉及2-苯基噻吩衍生物或其盐，其中噻吩环被羧基等取代，苯环具有吸电子基如氰基和给电子基团，例如作为取代的烷氧基。由于本发明的化合物具有良好的黄嘌呤氧化酶抑制作用和尿酸降低作用，并且不具有衍生自核酸的结构，与常规化合物相比，该化合物具有安全性高，效果优异的优点，可用作高尿酸血症，痛风，炎性肠病，糖尿病性肾病，糖尿病性视网膜病变等的治疗或预防剂。

10. 发明申请

US20070265289A1 2-Aminopyrimidine Derivative 审中-公开
标题翻译： 2-氨基嘧啶衍生物
公开(公告)号：US20070265289A1
公开(公告)日：2007-11-15
申请号：US11578608
申请日：2005-04-13
申请人： Yoshinori Okamoto , Hirokazu Kubota , Ippei Sato , Kazuyuki Hattori , Takatoshi Kanayama , Kazuhiro Yokoyama , Yoshiya Terai , Masahiro Takeuchi
发明人： Yoshinori Okamoto , Hirokazu Kubota , Ippei Sato , Kazuyuki Hattori , Takatoshi Kanayama , Kazuhiro Yokoyama , Yoshiya Terai , Masahiro Takeuchi
IPC分类号： A61K31/506 , C07D403/02
CPC分类号： C07D401/04 , A61K31/506 , A61K31/55 , C07D401/12 , C07D403/04 , C07D413/04
摘要： The invention relates to a compound useful as remedies or preventives for IKK2-related inflammatory diseases or autoimmune diseases, or that is, a 2-aminopyrimidine derivative having a 2-hydroxyphenyl group at the 6-position thereof and having a saturated cyclic group that contains one nitrogen atom, such as piperidine, at the 4-position thereof. The pharmaceutical composition of the invention and the compound of the invention have an excellent antiinflammatory effect based on the IKK2-inhibitory effect thereof, and are therefore useful for remedies and preventives for inflammatory diseases and autoimmune diseases, especially for rheumatoid arthritis.
摘要翻译：本发明涉及可用作IKK2相关炎性疾病或自身免疫性疾病的补救措施或预防药物的化合物，或其6-位上具有2-羟基苯基并具有饱和环状基团的2-氨基嘧啶衍生物，其含有一个氮原子，例如哌啶，在其4-位。本发明的药物组合物和本发明化合物基于IKK2抑制作用具有优异的抗炎作用，因此可用于炎性疾病和自身免疫疾病，特别是类风湿性关节炎的治疗和预防药物。

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