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11. 发明授权

US07528140B2 Substituted pyrrolo[3,2-d]pyrimidines as glycogen synthase kinase (GSK) inhibitors 失效
标题翻译：取代的吡咯并[3,2-d]嘧啶作为糖原合酶激酶（GSK）抑制剂
公开(公告)号：US07528140B2
公开(公告)日：2009-05-05
申请号：US10504583
申请日：2003-02-24
申请人： Kenichiro Kataoka , Tomomi Kosugi , Toshihiro Ishii , Takahiro Takeuchi , Takaharu Tsutsumi , Akira Nakano , Gen Unoki , Masanori Yamamoto , Yuri Sakai
发明人： Kenichiro Kataoka , Tomomi Kosugi , Toshihiro Ishii , Takahiro Takeuchi , Takaharu Tsutsumi , Akira Nakano , Gen Unoki , Masanori Yamamoto , Yuri Sakai
IPC分类号： C07D487/04 , C07D417/12 , C07D417/06 , C07D413/12 , C07D413/06 , C07D519/00 , A61K31/519 , A61K31/541 , A61K31/5355 , A61K31/497
CPC分类号： C07D487/04
摘要： The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and are therefore expected to be useful as therapeutic or prophylactic agents for conditions in which GSK-3 is implicated, such as diabetes, diabetes complications, Alzheimer's disease, neurodegenerative diseases, manic depression, traumatic encephalopathy, alopecia, inflammatory diseases, cancer and immune deficiency.
摘要翻译：本发明提供由式（I）表示的吡咯并[3,2-d]嘧啶衍生物及其医学上可接受的盐。本发明的化合物显示出GSK-3抑制活性，因此预期其可用作GSK-3涉及的病症的治疗或预防剂，例如糖尿病，糖尿病并发症，阿尔茨海默病，神经变性疾病，躁狂抑郁症，创伤性脑病，脱发，炎性疾病，癌症和免疫缺陷。

12. 发明申请

US20050171094A1 Pyrrolopyrimidine derivatives 审中-公开
标题翻译：吡咯并嘧啶衍生物
公开(公告)号：US20050171094A1
公开(公告)日：2005-08-04
申请号：US10505228
申请日：2003-02-24
申请人： Kenichiro Kataoka , Tomomi Kosugi , Toshihiro Ishii , Takahiro Takeuchi , Takaharu Tsutsumi , Akira Nakano , Yoji Yamamoto , Noboru Yoshioka
发明人： Kenichiro Kataoka , Tomomi Kosugi , Toshihiro Ishii , Takahiro Takeuchi , Takaharu Tsutsumi , Akira Nakano , Yoji Yamamoto , Noboru Yoshioka
IPC分类号： A61P3/00 , A61P3/04 , A61P3/10 , A61P9/10 , A61P9/12 , A61P15/00 , A61P17/14 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D487/14 , A61K31/551 , A61K31/519
CPC分类号： C07D487/14
摘要： A pyrrolo[3,2-d]pyrimidine derivative represented by the formula (I) or a pharamaceutically acceptable salt of the derivative. The derivative or salt is useful as a GSK-3 inhibitor.
摘要翻译：由式（I）表示的吡咯并[3,2-d]嘧啶衍生物或衍生物的药学上可接受的盐。衍生物或盐可用作GSK-3抑制剂。

13. 发明授权

US5731452A 7-thiaprostaglandins and method of production thereof 失效
标题翻译： 7-硫代前列腺素及其生产方法
公开(公告)号：US5731452A
公开(公告)日：1998-03-24
申请号：US532743
申请日：1995-09-18
申请人： Toru Minoshima , Kenichiro Kataoka , Hiroko Tanaka , Koji Ishii , Noriaki Endo
发明人： Toru Minoshima , Kenichiro Kataoka , Hiroko Tanaka , Koji Ishii , Noriaki Endo
IPC分类号： C07C405/00 , C07F7/08
CPC分类号： C07C405/0033
摘要： 7-thiaprostaglandins having the formula (I) which inhibit cell migration induced by monocyte chemoattractant protein MCP-1/MCAF and other chemokines and can serve as drugs for the treatment of atherosclerosis, diabetic angiopathy, and other disorders, their enantiomers, mixtures of the same, and methods of production thereof. ##STR1##
摘要翻译： PCT No.PCT / JP95 / 00042 Sec。 371 1995年9月18日第 102（e）1995年9月18日PCT PCT 1995年1月18日PCT公布。 WO95 / 19340BC出版物日期：1997年7月20日 - 具有抑制由单核细胞趋化蛋白MCP-1 / MCAF和其他趋化因子诱导的细胞迁移的式（I）的thiaprostaglandins，可用作治疗动脉粥样硬化，糖尿病性血管病和其他疾病的药物对映异构体，其混合物及其生产方法。（一）

14. 发明授权

US5496853A Benzoxa condensed ring compounds, process for producing the same and pharmaceutical composition comprising the same 失效
标题翻译：苯并恶稠环化合物，其制备方法和包含其的药物组合物
公开(公告)号：US5496853A
公开(公告)日：1996-03-05
申请号：US429023
申请日：1995-04-26
申请人： Tatsuki Shiota , Takumi Takeyasu , Kenichiro Kataoka , Tsutomu Mochizuki , Hirofumi Tanabe , Mikio Ota , Masatoshi Kano , Hisao Yamaguchi
发明人： Tatsuki Shiota , Takumi Takeyasu , Kenichiro Kataoka , Tsutomu Mochizuki , Hirofumi Tanabe , Mikio Ota , Masatoshi Kano , Hisao Yamaguchi
IPC分类号： C07D263/56 , C07D263/57 , C07D307/79 , C07D407/12 , C07D413/04 , A61K31/34 , A61K31/42
CPC分类号： C07D263/56 , C07D263/57 , C07D307/79 , C07D407/12 , C07D413/04
摘要： Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R.sub.1, R.sub.2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.
摘要翻译：含有苯并恶唑化合物和下式（I）表示的2,3-二氢苯并呋喃化合物及其药学上可接受的盐的药物组合物：其中，P，Q，R和S中的任一个为由下式表示的基团：和R 1，R 2和取代基P至S中的取代三个取代基各自独立地代表各种取代基。这些组合物用作ATCAT抑制剂或用于治疗高脂血症和动脉粥样硬化。

15. 发明授权

US5378700A Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient 失效
标题翻译：熔融嘧啶衍生物，其制备方法和包含与活性成分相同的药物制剂
公开(公告)号：US5378700A
公开(公告)日：1995-01-03
申请号：US839769
申请日：1992-06-09
申请人： Yasuji Sakuma , Masaichi Hasegawa , Kenichiro Kataoka , Kenji Hoshina , Noboru Yamazaki , Takashi Kadota , Hisao Yamaguchi
发明人： Yasuji Sakuma , Masaichi Hasegawa , Kenichiro Kataoka , Kenji Hoshina , Noboru Yamazaki , Takashi Kadota , Hisao Yamaguchi
IPC分类号： A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed is a fused pyrimidine of the formula [I] ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined in the specification, Y represents a linking group of the formula ##STR2## wherein n is an integer of from 4 to 6, ##STR3## wherein A is a hydrogen atom or alkyl group; and Z represents a hydrogen atom, or other substituents; or Y and Z together represent an unsubstituted or substituted alkyl, alkenyl or arylalkyl group; or a 5- to 7-member heterocyclic ring which has a nitrogen atom, and further, an oxygen or sulfur atom as a hetero atom other than the nitrogen atom, being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I), a 5- to 7-member unsaturated heterocyclic ring which has 1 to 3 nitrogen atoms being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I), or a fused biheterocyclic ring constructed with 5- or 6-membered aromatic or non-aromatic rings, which has 1 to 3 nitrogen atoms in any position, being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I); andm is an integer of from 1 to 3;and a pharmaceutically acceptable acid addition salt thereof, as well as a process for producing same and a pharmaceutical preparation useful for a treatment of hypoxemia associated with respiratory diseases.
摘要翻译： PCT No.PCT / JP90 / 01313 Sec。 371日期：1992年6月9日 102（e）日期1992年6月9日PCT提交1990年10月11日PCT公布。出版物WO91 / 05784 日期：1991年5月2日。公开是式[I]的融合嘧啶其中R 1，R 2和R 3如说明书中所定义，Y表示式的连接基团，其中n 是4至6的整数，其中A是氢原子或烷基; O（S） Z表示氢原子或其它取代基; 或Y和Z一起表示未取代或取代的烷基，烯基或芳基烷基; 或具有氮原子的5-至7-元杂环，以及作为氮原子以外的杂原子的氧或硫原子通过氮原子键合到嘧啶环的4-位上式（I）的通式（I）中的氮原子数为1〜3的5〜7元不饱和杂环与式（I）的嘧啶环的4-位连接，在其中具有1至3个氮原子的5-或6-元芳族或非芳族环经由其中的氮原子键合到式（I）的嘧啶环的4-位上构成的双杂环， ; m为1〜3的整数，和其药学上可接受的酸加成盐，以及其制备方法和用于治疗与呼吸系统疾病相关的低氧血症的药物制剂。

16. 发明授权

US5574061A Benzopyran derivative, process for producing the same and pharmaceutical composition containing the same 失效
标题翻译：苯并吡喃衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5574061A
公开(公告)日：1996-11-12
申请号：US216779
申请日：1994-03-23
申请人： Tatsuki Shiota , Takumi Takeyasu , Kenichiro Kataoka , Tsutomu Mochizuki , Hirofumi Tanabe , Mikio Ota , Hisao Yamaguchi
发明人： Tatsuki Shiota , Takumi Takeyasu , Kenichiro Kataoka , Tsutomu Mochizuki , Hirofumi Tanabe , Mikio Ota , Hisao Yamaguchi
IPC分类号： C07D311/22 , C07D311/28 , C07D311/58 , C07D311/64 , A61K31/35 , C07D311/04
CPC分类号： C07D311/28 , C07D311/22 , C07D311/58 , C07D311/64
摘要： A benzopyran derivative represented by the formula (I) or its pharmaceutically acceptable salt: ##STR1## wherein either one of X and Y stands for the following formula ##STR2## and the other one of X and Y and R.sup.1 -R.sup.10 stand for various substituents,and ACAT inhibitor, anti-hyperlipidemia agent and anti-atherosclerosis agent compositions containing the same as an active ingredient.
摘要翻译：由式（I）表示的苯并吡喃衍生物或其药学上可接受的盐：其中X和Y中的任一个代表下式（IMAGE），X和Y中的另一个代表R 1 -R 10 各种取代基，ACAT抑制剂，抗高脂血症药和含有其作为活性成分的抗动脉粥样硬化剂组合物。

17. 发明申请

US20080287544A1 Method for Screening Substance by Measuring PPAR DELTA Activating Effect and Agent 审中-公开
标题翻译：通过测量PPAR DELTA激活效应和试剂筛选物质的方法
公开(公告)号：US20080287544A1
公开(公告)日：2008-11-20
申请号：US12142652
申请日：2008-06-19
申请人： Kazuyoshi YAMAOKA , Kenichiro Takagi , Kenichiro Kataoka , Masanori Yamamoto , Toshihiro Chikanishi
发明人： Kazuyoshi YAMAOKA , Kenichiro Takagi , Kenichiro Kataoka , Masanori Yamamoto , Toshihiro Chikanishi
IPC分类号： A61K31/19 , A61P3/10 , A61P9/10
CPC分类号： G01N33/5079 , G01N33/6872
摘要： The present invention provides a method for screening a substance having a thermogenesis enhancing effect containing a compound having an effect activating PPARδ, an agent containing the compound, and an agent having antidiabetic, antiobestic or visceral accumulated fat-lowering function.The present invention provides an agent containing a compound having an effect activating PPARδ, which is a peroxisome proliferator activated receptor, and having effects which enhances nonshivering thermogenesis (nST), specifically enhances uncoupling respiration in mitochondria of cells in an adipose tissue or the like, or proton leak in inner membranes of mitochondria, and increases the amount of expression of UCP1, and provides an antidiabetic agent, an antiobestic gent and a visceral accumulated fat-lowering agent containing the compound. Further, the present invention provides a method for screening the compound by measuring a PPARδ activating effect.
摘要翻译：本发明提供一种筛选具有生发促进效果的物质的方法，其含有具有活化PPARδ的作用的化合物，含有该化合物的药剂和具有抗糖尿病，抗胆固醇或内脏积累的降脂功能的药剂。本发明提供含有具有激活PPARdta的作用的化合物的药剂，其是过氧化物酶体增殖物激活受体，并且具有增强非发热生成（nST）的作用，特别地增强脂肪组织等中的细胞的线粒体中的解偶联呼吸，或线粒体内膜中的质子泄漏，并增加UCP1的表达量，并提供含有该化合物的抗糖尿病剂，抗胆碱剂和内脏积累的降脂剂。此外，本发明提供了通过测量PPARδ激活效应来筛选化合物的方法。

18. 发明授权

US06686353B1 Diarylalkyl cyclic diamine derivatives as chemokine receptor antagonists 失效
标题翻译：二芳基烷基环二胺衍生物作为趋化因子受体拮抗剂
公开(公告)号：US06686353B1
公开(公告)日：2004-02-03
申请号：US09180994
申请日：1999-07-15
申请人： Tatsuki Shiota , Shinsuke Yamagami , Kenichiro Kataoka , Noriaki Endo , Hiroko Tanaka , Doug Barnum , Jonathan Greene , Wilna Moree , Michele Ramirez Weinhouse , Christine M. Tarby
发明人： Tatsuki Shiota , Shinsuke Yamagami , Kenichiro Kataoka , Noriaki Endo , Hiroko Tanaka , Doug Barnum , Jonathan Greene , Wilna Moree , Michele Ramirez Weinhouse , Christine M. Tarby
IPC分类号： A61K3155
CPC分类号： C07D417/06 , A61K31/495 , A61K31/496 , A61K31/551 , C07D213/38 , C07D243/08 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/06
摘要： Cyclic diamines of formula (I) or their pharmacologically acceptable acid addition salts, and their medical applications are described. These compounds inhibit the action of chemokines such as MIP-1a and/or MCP-1 on target cells, and are useful as a therapeutic drug and/or preventative drug in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissue.
摘要翻译：描述式（I）的环状二胺或其药理学上可接受的酸加成盐及其医疗应用。这些化合物抑制趋化因子例如MIP-1a和/或MCP-1对靶细胞的作用，并且可用作血液单核细胞等疾病如动脉粥样硬化，类风湿性关节炎等中的治疗药物和/或预防药物淋巴细胞浸润到组织中。

19. 发明授权

US5661148A Pyrrolo[2,3-d]pyrimidine derivatives, process for producing the same and pharmaceutical preparation comprising the same as active ingredient 失效
标题翻译：吡咯并[2,3-d]嘧啶衍生物，其制备方法以及含有活性成分的药物制剂
公开(公告)号：US5661148A
公开(公告)日：1997-08-26
申请号：US478686
申请日：1995-06-07
申请人： Yasuji Sakuma , Masaichi Hasegawa , Kenichiro Kataoka , Kenji Hoshina , Noboru Yamazaki , Takashi Kadota , Hisao Yamaguchi
发明人： Yasuji Sakuma , Masaichi Hasegawa , Kenichiro Kataoka , Kenji Hoshina , Noboru Yamazaki , Takashi Kadota , Hisao Yamaguchi
IPC分类号： C07D487/04 , C07D519/00 , A61K31/305 , C07D239/48
CPC分类号： C07D487/04
摘要： A pyrrolo[2,3-d]pyrimidine derivative having the general formula [I] ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z have the same definitions as those given in the description, a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutical preparation comprising the same, are provided.
摘要翻译：具有通式[I]的吡咯并[2,3-d]嘧啶衍生物其中R1，R2，R3，R4，R5，Y和Z具有与说明书中给出的相同的定义，提供其药学上可接受的酸加成盐和包含其的药物制剂。

20. 发明授权

US07396642B2 Methods of screening for a compound that enhances thermogenesis 失效
标题翻译：筛选增强产热的化合物的方法
公开(公告)号：US07396642B2
公开(公告)日：2008-07-08
申请号：US10483627
申请日：2002-07-17
申请人： Kazuyoshi Yamaoka , Kenichiro Takagi , Kenichiro Kataoka , Masanori Yamamoto , Toshihiro Chikanishi
发明人： Kazuyoshi Yamaoka , Kenichiro Takagi , Kenichiro Kataoka , Masanori Yamamoto , Toshihiro Chikanishi
IPC分类号： C12Q1/00 , C12Q1/68 , G01N33/53
CPC分类号： G01N33/5079 , G01N33/6872
摘要： The present invention provides a method for screening a substance having a thermogenesis enhancing effect containing a compound having an effect activating PPAR δ, an agent containing the compound, and an agent having antidiabetic, antiobestic or visceral accumulated fat-lowering function.The present invention provides an agent containing a compound having an effect activating PPAR δ, which is a peroxisome proliferator activated receptor, and having effects which enhances nonshivering thermogenesis (nST), specifically enhances uncoupling respiration in mitochondria of cells in an adipose tissue or the like, or proton leak in inner membranes of mitochondria, and increases the amount of expression of UCP1, and provides an antidiabetic agent, an antiobestic gent and a visceral accumulated fat-lowering agent containing the compound. Further, the present invention provides a method for screening the compound by measuring a PPAR δ activating effect.
摘要翻译：本发明提供一种筛选具有生发增强效果的物质的方法，其含有具有活化PPARδ的作用的化合物，含有该化合物的药剂和具有抗糖尿病，抗胆固醇或内脏积累的降脂功能的药剂。本发明提供了含有具有活化PPARδ作用的化合物的化合物，其是过氧化物酶体增殖物激活受体，并且具有增强非发热生成（nST）的作用，特别地增强脂肪组织等中的细胞的线粒体中的解偶联呼吸或线粒体内膜中的质子泄漏，并增加UCP1的表达量，并提供含有该化合物的抗糖尿病药，抗胆碱剂和内脏累积降脂剂。此外，本发明提供了通过测量PPARδ激活效应来筛选化合物的方法。

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