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11. 发明授权

US4963544A 3-pyrrolidinylthio-1-azabicyclo[3.2.0]-hept-2-ene-2-carboxylic acid compounds 失效
公开(公告)号：US4963544A
公开(公告)日：1990-10-16
申请号：US347579
申请日：1989-05-05
申请人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
发明人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/435 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/505 , A61P31/04 , C07D477/20 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/20 , Y02P20/55
摘要： 3-Pyrrolidinylthio-1-azabicyclo[3.2.0]-hept-2-ene carboxylic acids substituted on the pyrrolidine by unsaturated heterocyclyl have been prepared.

12. 发明授权

US4963543A 3-pyrolidinylthio-1-azabicyclo-[3.2.0]hept-2-ene-2-carboxylic acid derivatives and processes for the preparation thereof 失效
标题翻译： 3-吡咯烷硫基-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸衍生物及其制备方法
公开(公告)号：US4963543A
公开(公告)日：1990-10-16
申请号：US121881
申请日：1987-11-17
申请人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
发明人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/44 , A61P31/04 , C07D207/12 , C07D401/12 , C07D403/12 , C07D417/12 , C07D477/20
CPC分类号： C07D477/20 , C07D207/12 , C07D401/12 , C07D403/12 , C07D417/12 , Y02P20/55
摘要： 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hepten-2-ene-2-carboxylic acid derivatives are prepared.

13. 发明授权

US5608056A Substituted 3-pyrrolidinylthio-carbapenems as antimicrobial agents 失效
标题翻译：取代的3-吡咯烷硫基 - 碳青霉烯作为抗微生物剂
公开(公告)号：US5608056A
公开(公告)日：1997-03-04
申请号：US302780
申请日：1994-09-21
申请人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
发明人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/00 , A61P31/04 , C07D477/20 , C07D519/00 , C07D521/00 , C07D487/04
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D477/20 , Y02P20/55
摘要： A compound of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,R.sup.2 is 1-hydroxyethyl,R.sup.3 is methyl,R.sup.4 is optionally substituted pyridyl(lower)alkyl, optionally N-substituted 2-oxopiperazin-1-yl-(lower)alkyl, optionally substituted imidazol-1-yl(C.sub.2 -C.sub.3)alkyl, optionally substituted imidazol-5-yl-(lower)alkyl, optionally substituted imidazol-2-yl-(lower)alkyl, optionally substituted pyrazol-4-(or 5-)yl(lower)alkyl, optionally substituted pyrazol-1-ylethyl, optionally substituted triazolyl(lower)alkyl, optionally substituted pyrimidinyl(lower)alkyl, optionally substituted dihydropyrimidinyl(lower)alkyl, or optionally substituted (2,3-dihydroimidazo-[1,2-b]pyrazol-1-yl)ethyl, andR.sup.5 is hydrogen or imino-protective group,and pharmaceutically acceptable salts thereof, which have antimicrobial activity.
摘要翻译： PCT No.PCT / JP93 / 00469 Sec。 371日期1994年9月21日 102（e）1994年9月21日PCT PCT 1993年4月9日PCT公布。公开号WO93 / 21186 日期：1993年10月28日，下式化合物：其中R 1为羧基或被保护的羧基，R 2为1-羟乙基，R 3为甲基，R 4为任选取代的吡啶基（低级）烷基，任意取代的2-氧代哌嗪（低级）烷基，任选取代的咪唑-1-基（C 2 -C 3）烷基，任选取代的咪唑-5-基 - （低级）烷基，任选取代的咪唑-2-基 - （低级）烷基，任选取代的吡唑-1-基乙基，任选取代的三唑基（低级）烷基，任选取代的嘧啶基（低级）烷基，任选取代的二氢嘧啶基（低级）烷基，或任选取代的（2,3-二氢咪唑并[1,2-b]吡唑-1-基）乙基，R 5为具有抗微生物活性的氢或亚氨基保护基及其药学上可接受的盐。

14. 发明授权

US5286721A 1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds 失效
标题翻译： 1-氮杂双环[3.2.0]庚-2-烯-2-羧酸化合物
公开(公告)号：US5286721A
公开(公告)日：1994-02-15
申请号：US853746
申请日：1992-06-12
申请人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
发明人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
IPC分类号： C07D477/14 , C07D477/00
CPC分类号： C07D477/14
摘要： 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds of the formula: ##STR1## in which R.sup.1 is carboxy, COO.sup.-- or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.8 is hydrogen or lower alkyl,Z is a group of the formula: ##STR2## wherein R.sup.3 is hydrogen; lower alkyl or lower alkenyl, each of which is optionally substituted by the group consisting of lower alkoxy, carbamoyl, hydroxy, halogen, mono(or di)(lower)alkylcarbamoyl, mono(or di)(lower)alkenylcarbamoyl, mono(or bis)[hydroxy(lower)alkyl]carbamoyl, optionally substituted cyclic-aminocarbonyl, acylamino, ureido, optionally substituted heterocyclic-carbonylamino, carbamoyloxy, mono(or di)(lower)alkylcarbamoyloxy, lower alkylthio, halo(lower)alkylthio, optionally substituted heterocyclicthio, optionally substituted heterocyclic group, optionally substituted aryl, and acyl;R.sup.9 is hydrogen or lower alkyl, andR.sup.10 is lower alkyl,or pharmaceutically acceptable salts thereof, which is useful as an antimicrobial agent.
摘要翻译： PCT No.PCT / JP91 / 01394 Sec。 371日期：1992年6月12日 102（e）日期1992年6月12日PCT 1991年10月14日PCT PCT。出版物WO92 / 06978 日期：4月30日，1992.1-氮杂双环（3.2.0）庚-2-烯-2-羧酸化合物，其结构式如下：（*化学结构*）其中R 1为羧基，COO-或被保护的羧基，R 2为羟基（低级）烷基或被保护的羟基（低级）烷基，R 8是氢或低级烷基，Z是下列基团：（*化学结构*）其中R 3是氢; 羟基，卤素，单（或二）（低级）烷基氨基甲酰基，单（或二）（低级）烯基氨基甲酰基，单（或双（低级））链烯基氨基甲酰基，）（羟基（低级）烷基）氨基甲酰基，任选取代的环氨基羰基，酰氨基，脲基，任选取代的杂环羰基氨基，氨基甲酰氧基，单（或二）（低级）烷基氨基甲酰氧基，低级烷硫基，卤（低级）烷硫基，，任选取代的杂环基，任选取代的芳基和酰基; R9为氢或低级烷基，R10为低级烷基，或其药学上可接受的盐，可用作抗微生物剂。

15. 发明授权

US5102877A 1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds 失效
标题翻译： 1-氨基胆碱（3.2.0）HEPT-2-环己-2-羧酸化合物
公开(公告)号：US5102877A
公开(公告)日：1992-04-07
申请号：US508167
申请日：1990-04-12
申请人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
发明人： Masayoshi Murata , Toshiyuki Chiba , Hideo Tsutsumi , Kohji Hattori , Satoru Kuroda , Hiroaki Ohtake , Fumiyuki Shirai
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61P31/04 , C07D477/14 , C07D519/00 , C07F7/18
CPC分类号： C07D477/14 , C07F7/186 , Y02P20/55
摘要： 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxyic acids having antimicrobial activity have been prepared.

16. 发明授权

US4921852A 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds 失效
标题翻译： 3-吡咯烷基硫代-1-氮杂双环[3.2.0]庚-2-烯-2-羧酸化合物
公开(公告)号：US4921852A
公开(公告)日：1990-05-01
申请号：US124603
申请日：1987-11-24
申请人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
发明人： Masayoshi Murata , Hideo Tsutsumi , Keiji Matsuda , Kohji Hattori , Takashi Nakajima
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/415 , A61K31/425 , A61P31/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D477/20
CPC分类号： C07D477/20 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , Y02P20/55
摘要： 3-Pyrrolidinylthio-1-azabicyclo [320] hept-2-ene-2-carboxylic acid anti-microbiotic compounds are prepared.

17. 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。

18. 发明授权

US4554269A Kasugamycin derivatives, pharmaceutical compositions and method of use 失效
标题翻译：春日霉素衍生物，药物组合物和使用方法
公开(公告)号：US4554269A
公开(公告)日：1985-11-19
申请号：US573377
申请日：1984-01-24
申请人： Takao Takaya , Nobuyoshi Yasuda , Hideo Tsutsumi , Keiji Matsuda
发明人： Takao Takaya , Nobuyoshi Yasuda , Hideo Tsutsumi , Keiji Matsuda
IPC分类号： C07H15/207 , A61K31/71 , C07H15/20
CPC分类号： C07H15/207
摘要： This invention relates to new aminoglycoside derivatives and pharmaceutically acceptable salts thereof. More particularly it relates to new aminoglycoside derivatives and pharmaceutically acceptable salts thereof which have anti-viral activity, and immuno-stimulating activity and pharmaceutical compositions comprising the same. In addition, this invention also relates to methods of preparing the aminoglycoside derivatives and salts thereof.
摘要翻译：本发明涉及新的氨基糖苷衍生物及其药学上可接受的盐。更具体地说，本发明涉及具有抗病毒活性的新的氨基糖苷衍生物及其药学上可接受的盐以及免疫刺激活性以及包含其的药物组合物。此外，本发明还涉及制备氨基糖苷衍生物及其盐的方法。

19. 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。

20. 发明申请

US20050043315A1 Aminopyrimidine compounds, processes for their preparation and pharmaceutical compositions containing them 审中-公开
标题翻译：氨基嘧啶化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US20050043315A1
公开(公告)日：2005-02-24
申请号：US10498016
申请日：2002-12-27
申请人： Hideo Tsutsumi , Satoshi Yonishi , Atsushi Akahane
发明人： Hideo Tsutsumi , Satoshi Yonishi , Atsushi Akahane
IPC分类号： C07D401/14 , C07D403/04 , C07D409/14 , C07D43/02 , A61K31/501
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14
摘要： An aminopyrimidine compound of the following formula (I) wherein Q is (a) or (b) in which R and R′ are each optionally substituted aryl or heterocyclic group,R5 is hydrogen, halogen, lower alkyl,optionally substituted hydroxy, optionally substituted amino which may form N-containing heterocyclic group, optionally substituted mercapto, lower alkylsulfinyl or lower alkylsulfonyl, and X is oxygen or sulfur; R1 is hydrogen, optionally substituted lower alkyl or cyclo(lower) alkyl which may be interrupted by an oxygen atom; R2 and R3 are each independently hydrogen, lower alkyl, acyl, aryl or heterocyclic(lower)alkyl, R2 and R3 may be combined together with N atom to which they are attached to form N-containing heterocyclic group; or a salt thereof. The aminopyrimidine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：其中Q为（a）或（b）的下式（I）的氨基嘧啶化合物，其中R和R'各自为任选取代的芳基或杂环基，R 5为氢，卤素，低级烷基，任选取代的羟基，可以形成含氮杂环基的任选取代的氨基，任选取代的巯基，低级烷基亚磺酰基或低级烷基磺酰基，X是氧或硫; R 1是氢，任选取代的可被氧原子间隔的低级烷基或环（低级）烷基; R 2和R 3各自独立地为氢，低级烷基，酰基，芳基或杂环（低级）烷基，R 2和R 3可以与它们所连接的N原子一起形成含氮杂环基; 或其盐。本发明的氨基嘧啶化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

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