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1. 发明申请

WO2004089297A3 COMPOUNDS AND METHODS FOR TREATMENT OF THROMBOSIS 审中-公开
标题翻译：用于治疗血栓形成的化合物和方法
公开(公告)号：WO2004089297A3
公开(公告)日：2006-03-30
申请号：PCT/US2004010300
申请日：2004-04-02
申请人： SUNTORY PHARMACEUTICAL RES LAB , ABDEL-MEGUID SHERIN S , BABINE ROBERT E , DENG HONGFENG , JIN LEI , LIN JIAN , MAGEE SCOTT R , MEYERS HAROLD V , PANDEY PRAMOD , RYNKIEWICZ MICHAEL J , WEAVER DAVID T
发明人： ABDEL-MEGUID SHERIN S , BABINE ROBERT E , DENG HONGFENG , JIN LEI , LIN JIAN , MAGEE SCOTT R , MEYERS HAROLD V , PANDEY PRAMOD , RYNKIEWICZ MICHAEL J , WEAVER DAVID T
IPC分类号： A61K20060101 , A61K38/00 , A61K38/04 , C07K2/00 , C07K5/04 , C07K5/06 , C07K5/065 , C07K5/078 , C07C233/00 , A61K38/02 , C07C233/01 , C07C237/00 , C07C237/04
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06034 , C07K5/06139 , C07K5/06191
摘要： The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.
摘要翻译：本发明提供了通过向哺乳动物施用本发明的化合物来抑制因子XIa的化合物和预防或治疗不期望的血栓形成的方法。本发明还提供了因子XIa的三维结构以及使用这些结构设计或选择另外的因子XIa抑制剂的方法。

2. 发明申请

WO9933431A3 PREPARATION AND SELECTION OF PHARMACEUTICALLY USEFUL COMPOUNDS FROM A DIVERSE UNIVERSAL LIBRARY 审中-公开
标题翻译：从多样化通用图书馆制备和选择药用有效化合物
公开(公告)号：WO9933431A3
公开(公告)日：1999-09-16
申请号：PCT/US9827695
申请日：1998-12-29
申请人： PAVIA MICHAEL R , MEYERS HAROLD V , MILOT GUY , HEDIGER MARK E
发明人： PAVIA MICHAEL R , MEYERS HAROLD V , MILOT GUY , HEDIGER MARK E
IPC分类号： A61K20060101 , A61K31/00 , C07B61/00 , C07C59/40 , C07C59/48 , C07C59/54 , C07C215/00 , G01N33/53 , G01N33/543
CPC分类号： C07C43/23 , C07B2200/11 , C07C219/22 , C40B40/04 , C40B50/14
摘要： This invention relates to novel combinatorial libraries of bridged biaromatic and triaromatic ring compounds, methods for preparing such libraries, and an apparatus for storing such libraries and for use as a component of assay systems for identifying compounds for drug development.
摘要翻译：本发明涉及桥接双芳族和三芳族环化合物的新型组合文库，制备这种文库的方法，以及用于存储这种文库和用作鉴定用于药物开发的化合物的测定系统的组分的装置。

3. 发明申请

WO1994013629A1 MANNITOL DERIVATIVES AND THEIR USE AS INHIBITORS OF ASPARTYL PROTEASE 审中-公开
标题翻译：曼尼托酮衍生物及其作为ASPARTYL PROTEASE的抑制剂的用途
公开(公告)号：WO1994013629A1
公开(公告)日：1994-06-23
申请号：PCT/US1993012059
申请日：1993-12-09
申请人： VERTEX PHARMACEUTICALS INCORPORATED , BOGER, Joshua, S. , MEYERS, Harold, V. , MULLICAN, Michael, D.
发明人： VERTEX PHARMACEUTICALS INCORPORATED
IPC分类号： C07C271/22
CPC分类号： C07D213/80 , C07C271/22 , C07C327/28 , C07C333/04 , C07D285/06 , C07D295/21
摘要： The present invention relates to a class of compounds which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of mannitol-derived HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features represented by formula (I), each A and A' is independently selected from the group consisting of a naturally occurring alpha-amino acid and an unnatural alpha-amino acid (e.g., whereineach n is independently selected from the group consisting of 0, 1 and 2; wherein each B and B' is independently selected from the group consisting of oxygen and sulfur; wherein each D and D' is independently selected from the group consisting of H2, oxygen and sulfur; wherein each E and E' is independently selected from the group consisting of Ar and N (R11R12). The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting the activity of HIV aspartyl protease. Accordingly, they may be advantageously used as anti-viral agents against HIV viruses, including the HIV-1 and HIV-2 viruses.
摘要翻译：本发明涉及一类天冬氨酰蛋白酶抑制剂的化合物。在一个实施方案中，本发明涉及由式（I）表示的具有特定结构和物理化学特征的新型甘露醇衍生的HIV天冬氨酰蛋白酶抑制剂，每个A和A'独立地选自天然存在的α - 氨基酸和非天然α-氨基酸（例如，其中n独立地选自0,1和2;其中每个B和B'独立地选自氧和硫;其中每个D 和D'独立地选自H 2，氧和硫;其中每个E和E'独立地选自Ar和N（R 11 R 12）。本发明的化合物和药物组合物特别适合用于抑制HIV天冬氨酰蛋白酶的活性，因此，它们可有利地用作抗HIV病毒（包括HIV-1和HIV-2病毒）的抗病毒剂。

4. 发明申请

WO2006012504A3 COMPOUNDS AND METHODS FOR TREATMENT OF THROMBOSIS 审中-公开
标题翻译：用于治疗血栓形成的化合物和方法
公开(公告)号：WO2006012504A3
公开(公告)日：2006-05-18
申请号：PCT/US2005026022
申请日：2005-07-22
申请人： DAIAMED INC , DENG HONGFENG , LIN JIAN , GUO ZIHONG , MEYERS HAROLD V , ABDEL-MEGUID SHERIN S , BABINE ROBERT E
发明人： DENG HONGFENG , LIN JIAN , GUO ZIHONG , MEYERS HAROLD V , ABDEL-MEGUID SHERIN S , BABINE ROBERT E
IPC分类号： C07D209/42 , A61K31/40 , A61P7/02 , C07D401/14 , C07D405/12 , C07D471/04
CPC分类号： C07D471/04 , C07D209/42 , C07D401/14 , C07D405/12
摘要： The invention provides compounds, pharmaceutical compositions, and methods for the treatment of thromboembolic disorders, such as, for example, arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, or thromboembolic disorders in the chambers of the heart.
摘要翻译：本发明提供了用于治疗血栓栓塞障碍的化合物，药物组合物和方法，例如动脉血管栓塞性疾病，静脉心血管血栓栓塞障碍或心脏腔室中的血栓栓塞性疾病。

5. 发明申请

WO2004103270A3 COMPOUNDS AND METHODS FOR TREATMENT OF THROMBOSIS 审中-公开
标题翻译：用于治疗血栓形成的化合物和方法
公开(公告)号：WO2004103270A3
公开(公告)日：2005-05-12
申请号：PCT/US2004010349
申请日：2004-04-02
申请人： SUNTORY PHARMACEUTICAL RES LAB , ABDEL-MEGUID SHERIN S , BABINE ROBERT E , DENG HONGFENG , JIN LEI , LIN JIAN , MAGEE SCOTT R , MEYERS HAROLD V , PANDEY PRAMOD , RYNKIEWICZ MICHAEL J , WEAVER DAVID T
发明人： ABDEL-MEGUID SHERIN S , BABINE ROBERT E , DENG HONGFENG , JIN LEI , LIN JIAN , MAGEE SCOTT R , MEYERS HAROLD V , PANDEY PRAMOD , RYNKIEWICZ MICHAEL J , WEAVER DAVID T
IPC分类号： A61K20060101 , A61K38/00 , A61K38/04 , C07K2/00 , C07K5/04 , C07K5/06 , C07K5/065 , C07K5/078
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06034 , C07K5/06139 , C07K5/06191
摘要： The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.
摘要翻译：本发明提供了通过向哺乳动物施用本发明的化合物来抑制因子XIa的化合物和预防或治疗不期望的血栓形成的方法。本发明还提供了因子XIa的三维结构以及使用这些结构设计或选择另外的因子XIa抑制剂的方法。

6. 发明申请

WO2004103270A2 COMPOUNDS AND METHODS FOR TREATMENT OF THROMBOSIS 审中-公开
标题翻译：用于治疗血栓形成的化合物和方法
公开(公告)号：WO2004103270A2
公开(公告)日：2004-12-02
申请号：PCT/US2004/010349
申请日：2004-04-02
申请人： SUNTORY PHARMACEUTICAL RESEARCH LABORATORIES LLC , ABDEL-MEGUID, Sherin, S. , BABINE, Robert, E. , DENG, Hongfeng , JIN, Lei , LIN, Jian , MAGEE, Scott, R. , MEYERS, Harold, V. , PANDEY, Pramod , RYNKIEWICZ, Michael, J. , WEAVER, David, T.
发明人： ABDEL-MEGUID, Sherin, S. , BABINE, Robert, E. , DENG, Hongfeng , JIN, Lei , LIN, Jian , MAGEE, Scott, R. , MEYERS, Harold, V. , PANDEY, Pramod , RYNKIEWICZ, Michael, J. , WEAVER, David, T.
IPC分类号： A61K
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06034 , C07K5/06139 , C07K5/06191
摘要： The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.
摘要翻译：本发明提供了通过向哺乳动物施用本发明的化合物来抑制因子XIa的化合物和预防或治疗不期望的血栓形成的方法。本发明还提供了因子XIa的三维结构以及使用这些结构设计或选择另外的因子XIa抑制剂的方法。

7. 发明申请

WO2004089297A2 COMPOUNDS AND METHODS FOR TREATMENT OF THROMBOSIS 审中-公开
标题翻译：化合物和治疗血栓症的方法
公开(公告)号：WO2004089297A2
公开(公告)日：2004-10-21
申请号：PCT/US2004/010300
申请日：2004-04-02
申请人： SUNTORY PHARMACEUTICAL RESEARCH LABORATORIES, LLC , ABDEL-MEGUID, Sherin, S. , BABINE, Robert, E. , DENG, Hongfeng , JIN, Lei , LIN, Jian , MAGEE, Scott, R. , MEYERS, Harold, V. , PANDEY, Pramod , RYNKIEWICZ, Michael, J. , WEAVER, David, T.
发明人： ABDEL-MEGUID, Sherin, S. , BABINE, Robert, E. , DENG, Hongfeng , JIN, Lei , LIN, Jian , MAGEE, Scott, R. , MEYERS, Harold, V. , PANDEY, Pramod , RYNKIEWICZ, Michael, J. , WEAVER, David, T.
IPC分类号： A61K
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06034 , C07K5/06139 , C07K5/06191
摘要： The present invention provides compounds that inhibit Factor XIa and methods of preventing or treating undesired thrombosis by administering a compound of the invention to a mammal. The invention also provides three-dimensional structures of Factor XIa and methods for designing or selecting additional Factor XIa inhibitors using these structures.
摘要翻译：本发明提供了抑制因子XIa的化合物和通过将本发明的化合物给予哺乳动物来预防或治疗不希望的血栓形成的方法。本发明还提供因子XIa的三维结构和使用这些结构设计或选择另外的因子XIa抑制剂的方法。

8. 发明申请

WO2006012504A2 COMPOUNDS AND METHODS FOR TREATMENT OF THROMBOSIS 审中-公开
标题翻译：化合物和治疗血栓症的方法
公开(公告)号：WO2006012504A2
公开(公告)日：2006-02-02
申请号：PCT/US2005/026022
申请日：2005-07-22
申请人： DAIAMED, INC. , DENG, Hongfeng , LIN, Jian , GUO, Zihong , MEYERS, Harold, V. , ABDEL-MEGUID, Sherin, S. , BABINE, Robert, E.
发明人： DENG, Hongfeng , LIN, Jian , GUO, Zihong , MEYERS, Harold, V. , ABDEL-MEGUID, Sherin, S. , BABINE, Robert, E.
IPC分类号： C07D209/42
CPC分类号： C07D471/04 , C07D209/42 , C07D401/14 , C07D405/12
摘要： The invention provides compounds, pharmaceutical compositions, and methods for the treatment of thromboembolic disorders, such as, for example, arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, or thromboembolic disorders in the chambers of the heart.
摘要翻译：本发明提供了用于治疗心室中的血栓栓塞病症例如动脉心血管血栓栓塞病症，静脉心血管血栓栓塞病症或血栓栓塞病症的化合物，药物组合物和方法

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