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1. 发明申请

WO2005019200A2 ARYL PIPERIDINE DERIVATIVES AS VLA-1 INTEGRIN ANTAGONISTS AND USES THEREOF 审中-公开
标题翻译： ARYL PIPERIDINE衍生物作为VLA-1整合拮抗剂及其用途
公开(公告)号：WO2005019200A2
公开(公告)日：2005-03-03
申请号：PCT/US2004/026206
申请日：2004-08-12
申请人： ICOS CORPORATION , BOYD, Steven, A. , DEMEESE, Jason , GUNAWARDANA, Indrani , JACOBSON, Irina, C. , LEHUEROU, Yvan , LUPHER, Mark, L., Jr. , MCLAUGHLIN, Martin , MILLER, Scott , THOMAS, Allen , THORSETT, Eugene , XU, Rui , YANIK, Matthew , ZHANG, Gan
发明人： BOYD, Steven, A. , DEMEESE, Jason , GUNAWARDANA, Indrani , JACOBSON, Irina, C. , LEHUEROU, Yvan , LUPHER, Mark, L., Jr. , MCLAUGHLIN, Martin , MILLER, Scott , THOMAS, Allen , THORSETT, Eugene , XU, Rui , YANIK, Matthew , ZHANG, Gan
IPC分类号： C07D401/00
CPC分类号： C04B35/632 , C07D211/62 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/14
摘要： Compounds that are VLA-1 integrin antagonists are disclosed. Also disclosed are compositions containing such compounds and methods of using such compounds in treating diseases mediated, at least in part, by the VLA-1 integrin.
摘要翻译：公开了作为VLA-1整联蛋白拮抗剂的化合物。还公开了含有这些化合物的组合物和使用这些化合物治疗由至少部分由VLA-1整联蛋白介导的疾病的方法。

2. 发明申请

WO2005016883A3 ACRYLAMIDE DERIVATIVES AS VLA-1 INTEGRIN ANTAGONISTS AND USES THEREOF 审中-公开
公开(公告)号：WO2005016883A3
公开(公告)日：2005-02-24
申请号：PCT/US2004/026653
申请日：2004-08-12
申请人： ICOS CORPORATION , BOYD, Steven, A. , MILLER, Scott , THOMAS, Allen , XU, Rui , LEHUEROU, Yvan , GUNAWARDANA, Indrani , ZHANG, Gan , DEMEESE, Jason , MCLAUGHLIN, Martin , YANIK, Matthew , LUPHER, Mark, L., Jr. , JACOBSON, Irina, C. , THORSETT, Eugene, D. , FAROUZ, Francine, S. , KASAR, Ramesh, A.
发明人： BOYD, Steven, A. , MILLER, Scott , THOMAS, Allen , XU, Rui , LEHUEROU, Yvan , GUNAWARDANA, Indrani , ZHANG, Gan , DEMEESE, Jason , MCLAUGHLIN, Martin , YANIK, Matthew , LUPHER, Mark, L., Jr. , JACOBSON, Irina, C. , THORSETT, Eugene, D. , FAROUZ, Francine, S. , KASAR, Ramesh, A.
IPC分类号： C07D211/62
摘要： Compounds that are VLA-1 integrin antagonists are disclosed. Also disclosed are compositions containing such compounds, and methods of using such compounds in treating diseases mediated, at least in part, by the VLA-1 integrin.

3. 发明申请

WO2005019177A1 AMINOPIPERIDINE AMIDE DERIVATIVES AS VLA-1 INTEGRIN ANTAGONISTS AND USES THEREOF 审中-公开
标题翻译：氨基肽酰胺衍生物作为VLA-1整合拮抗剂及其用途
公开(公告)号：WO2005019177A1
公开(公告)日：2005-03-03
申请号：PCT/US2004/026207
申请日：2004-08-12
申请人： ICOS CORPORATION , BOYD, Steven, A. , MILLER, Scott , THOMAS, Allen , XU, Rui , LEHUEROU, Yvan , GUNAWARDANA, Indrani , ZHANG, Gan , DEMEESE, Jason , MCLAUGHLIN, Martin , YANIK, Matthew , LUPHER, Mark, L., Jr. , JACOBSON, Irina, C. , THORSETT, Eugene
发明人： BOYD, Steven, A. , MILLER, Scott , THOMAS, Allen , XU, Rui , LEHUEROU, Yvan , GUNAWARDANA, Indrani , ZHANG, Gan , DEMEESE, Jason , MCLAUGHLIN, Martin , YANIK, Matthew , LUPHER, Mark, L., Jr. , JACOBSON, Irina, C. , THORSETT, Eugene
IPC分类号： C07D211/58
CPC分类号： C07D211/62 , C04B35/632 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12
摘要： Compounds of formula (I) that are VLA-1 integrin antagonists are disclosed. Also disclosed are compositions containing such compounds and methods of using such compounds in treating diseases mediated, at least in part, by the VLA-1 integrin.
摘要翻译：公开了作为VLA-1整联蛋白拮抗剂的式（I）化合物。还公开了含有这些化合物的组合物和使用这些化合物治疗由至少部分由VLA-1整联蛋白介导的疾病的方法。

4. 发明申请

WO2005000821A1 TACHYKININ RECEPTOR ANTAGONISTS 审中-公开
标题翻译： TACHYKININ受体拮抗剂
公开(公告)号：WO2005000821A1
公开(公告)日：2005-01-06
申请号：PCT/US2004/015579
申请日：2004-06-03
申请人： ELI LILLY AND COMPANY , AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HIPSKIND, Philip, Arthur , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , SAVIN, Kenneth, Allen , THRASHER, Kenneth, Jeff , BOYD, Steven, A.
发明人： AMEGADZIE, Albert, Kudzovi , GARDINIER, Kevin, Matthew , HEMBRE, Erik, James , HIPSKIND, Philip, Arthur , JUNGHEIM, Louis, Nickolaus , MUEHL, Brian, Stephen , SAVIN, Kenneth, Allen , THRASHER, Kenneth, Jeff , BOYD, Steven, A.
IPC分类号： C07D233/90
CPC分类号： C07D401/04 , C07D249/04 , C07D249/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/06 , C07D417/12 , C07D487/04
摘要： The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
摘要翻译：本发明涉及式（I）的选择性NK-1受体拮抗剂或其药学上可接受的盐，用于治疗与过速速激肽相关的疾病。

5. 发明申请

WO2005095391A1 THIAZOLIUMS AS TRANSKETOLASE INHIBITORS 审中-公开
标题翻译：作为转铁蛋白酶抑制剂的THIAZOLIUMS
公开(公告)号：WO2005095391A1
公开(公告)日：2005-10-13
申请号：PCT/US2005/009970
申请日：2005-03-23
申请人： ARRAY BIOPHARMA INC. , BOYD, Steven, A.
发明人： BOYD, Steven, A.
IPC分类号： C07D417/06
CPC分类号： C07D417/06 , C07D417/14
摘要： The present invention provides N-3'-pyridylmethyl or N-2'-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R 1 , R 2 , R 3 , Y, R 5 -R 9 , R a -R d , n and X - are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.
摘要翻译：本发明提供可用作转酮酶抑制剂的式（I）的N-3'-吡啶基甲基或N-2'-吡嗪基甲基噻唑鎓衍生物，其中R 1，R 2，R 3，Y， R 9 -R 9，R a -R d，n和X - 如本文所定义。本发明还提供包含式（I）化合物的药物组合物。本发明提供了抑制转酮醇酶活性，减少细胞核糖-5-磷酸水平，抑制核酸合成，抑制体外和体内细胞增殖和肿瘤细胞生长，刺激肿瘤细胞凋亡和通过给予式（I）化合物或其药物组合物。

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