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1. 发明授权

US08063077B2 Factor Xa inhibitors 有权
标题翻译：因子Xa抑制剂
公开(公告)号：US08063077B2
公开(公告)日：2011-11-22
申请号：US12777956
申请日：2010-05-11
申请人： Yonghong Song , Zhaozhong J. Jia , Robert M. Scarborough , Carroll Scarborough, legal representative , Anjali Pandey
发明人： Yonghong Song , Zhaozhong J. Jia , Robert M. Scarborough , Anjali Pandey
IPC分类号： A61K31/4412 , C07D401/14
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

2. 发明授权

US08349873B2 Factor XA inhibitors 有权
标题翻译：因子XA抑制剂
公开(公告)号：US08349873B2
公开(公告)日：2013-01-08
申请号：US13270170
申请日：2011-10-10
申请人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough, legal representative
发明人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough
IPC分类号： A61K31/4412
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

3. 发明申请

US20110160196A1 FACTOR XA INHIBITORS 审中-公开
标题翻译：因子XA抑制剂
公开(公告)号：US20110160196A1
公开(公告)日：2011-06-30
申请号：US12976602
申请日：2010-12-22
申请人： Zhaozhong J. Jia , Yonghong Song , Robert M. Scarborough , Carroll Scarborough , Anjali Pandey
发明人： Zhaozhong J. Jia , Yonghong Song , Robert M. Scarborough , Carroll Scarborough , Anjali Pandey
IPC分类号： A61K31/4439 , C07D409/14 , C12N9/99 , C07D413/14 , A61K31/444 , A61K31/4545 , A61K31/5377 , A61K31/496 , C07D417/14 , A61K31/541 , A61P7/02 , A61P9/10
CPC分类号： C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及由式（I）表示的化合物或其药学上可接受的盐，酯或前药，其是因子Xa的抑制剂。本发明还涉及用于制备这些化合物的中间体，含有这些化合物的药物组合物，预防或治疗特征在于不想要的血栓形成的某些病症的方法以及抑制血液样品凝固的方法。

4. 发明申请

US20070259924A1 FACTOR XA INHIBITORS 有权
标题翻译：因子XA抑制剂
公开(公告)号：US20070259924A1
公开(公告)日：2007-11-08
申请号：US11744735
申请日：2007-05-04
申请人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough
发明人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough
IPC分类号： A61K31/4439 , A61K31/4178 , A61K31/4172 , C07D403/02 , C07D409/02 , C07D405/02
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法以及抑制血液样品凝固的方法。

5. 发明申请

US20120088795A1 FACTOR XA INHIBITORS 有权
标题翻译：因子XA抑制剂
公开(公告)号：US20120088795A1
公开(公告)日：2012-04-12
申请号：US13270170
申请日：2011-10-10
申请人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough
发明人： Yonghong Song , Zhaozhong J. Jia , Anjali Pandey , Robert M. Scarborough , Carroll Scarborough
IPC分类号： A61K31/4439 , A61P7/02 , C12N9/99
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

6. 发明申请

US20090030045A1 FACTOR XA INHIBITORS 有权
标题翻译：因子XA抑制剂
公开(公告)号：US20090030045A1
公开(公告)日：2009-01-29
申请号：US12166944
申请日：2008-07-02
申请人： Yonghong Song , Zhaozhong J. Jia , Robert M. Scarborough , Anjali Pandey , Carroll Scarborough
发明人： Yonghong Song , Zhaozhong J. Jia , Robert M. Scarborough , Anjali Pandey , Carroll Scarborough
IPC分类号： A61K31/4439 , C07D409/14 , A61P7/00 , A61P7/02
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及作为因子Xa抑制剂的式（I）化合物及其药学上可接受的盐，酯和前药。本发明还涉及用于制备这种化合物的中间体，含有这种化合物的药物组合物，预防或治疗许多不希望的血栓形成特征的病症的方法和抑制血液样品凝固的方法。

7. 发明申请

US20080293704A1 FACTOR Xa INHIBITORS 审中-公开
标题翻译：因子Xa抑制剂
公开(公告)号：US20080293704A1
公开(公告)日：2008-11-27
申请号：US11969758
申请日：2008-01-04
申请人： Zhaozhong J. Jia , Yonghong Song , Robert M. Scarborough , Carroll Scarborough , Anjali Pandey
发明人： Zhaozhong J. Jia , Yonghong Song , Robert M. Scarborough , Carroll Scarborough , Anjali Pandey
IPC分类号： A61K31/4439 , C07D409/14 , A61K31/4545 , A61K31/541 , A61P7/00 , A01N1/00 , A61K31/496 , C07D279/12
CPC分类号： C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及由式（I）表示的化合物或其药学上可接受的盐，酯或前药，其是因子Xa的抑制剂。本发明还涉及用于制备这些化合物的中间体，含有这些化合物的药物组合物，预防或治疗特征在于不想要的血栓形成的某些病症的方法以及抑制血液样品凝固的方法。

8. 再颁专利

USRE43098E1 Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof 失效
标题翻译：含氮杂环化合物及其制备含氮杂环化合物的方法及其中间体
公开(公告)号：USRE43098E1
公开(公告)日：2012-01-10
申请号：US11866275
申请日：2007-10-02
申请人： James Kanter , Anjali Pandey , James Robinson , Robert M. Scarborough , Carroll Scarborough, legal representative
发明人： James Kanter , Anjali Pandey , James Robinson , Robert M. Scarborough
IPC分类号： A61K31/495 , C07D487/00 , C07D487/04 , C07D239/94
摘要： The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.
摘要翻译：本发明提供了含氮杂环化合物及其药学上可接受的盐及其制备方法。这些化合物对抑制这种激酶活性的激酶的磷酸化具有抑制活性。本发明还提供了可用于该方法的中间体化合物，以及通过该方法生产的最终产物及其盐或前药。本发明进一步提供了通过抑制激酶的磷酸化来抑制哺乳动物激酶和治疗疾病状态的方法，包括向有需要的患者施用有效量的本发明化合物。

9. 发明授权

US07109332B2 2,4-dioxo-3-quinazolinylaryl sulfonylureas 失效
标题翻译： 2,4-二氧代-3-喹唑啉基芳基磺酰脲
公开(公告)号：US07109332B2
公开(公告)日：2006-09-19
申请号：US10956004
申请日：2004-09-29
申请人： Robert M. Scarborough , Wolin Huang , Anjali Pandey , Shawn M. Bauer , Xiaoming Zhang , Zhaozhong J. Jia
发明人： Robert M. Scarborough , Wolin Huang , Anjali Pandey , Shawn M. Bauer , Xiaoming Zhang , Zhaozhong J. Jia
IPC分类号： C07D409/12 , C07D409/14 , A61K31/517 , A61P7/02
CPC分类号： C07D409/12 , C07D409/14
摘要： 2,4-Dioxo-3-quinazolinylaryl sulfonylurea compounds having the formula: wherein R is a member selected from the group consisting of H and C1-6 alkyl; R1 is a member selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C3-5 cycloalkyl and C3-5 cycloalkyl-alkyl; R2 is a member selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, cyano and —C(O)R2a, wherein R2a is a member selected from the group consisting of C1-6 alkoxy and (C1-6 alkyl)0-2 amino; L is a 1 to 3 carbon linking group selected from the group consisting of —CH2—, —CH(CH3)—, —CH2CH2—, —CH2CH(CH3)— and —CH2CH2CH2—; L1 is a linking group selected from the group consisting of a bond and —CH2—; L2 is a linking group selected from the group consisting of a bond, —NH— and —CH2—; and Ar1 is an aromatic ring selected from the group consisting of benzene, pyridine and pyrimidine; are provided. The compounds are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
摘要翻译： 2,4-二氧代-3-喹唑啉基芳基磺酰脲类化合物，其具有下式：其中R是选自H和C 1-6烷基的成员; R 1是选自H，C 1-6烷基，C 1-6卤代烷基，C 1 -C 6烷基，C 1 -C 6烷基， 3-5个环烷基和C 3-5环烷基 - 烷基; R 2是选自H，卤素，C 1-6 - 烷基，C 2-6 - 烯基，C 1 -C 6烷基， C 1-6烷基，C 1-6烷氧基，氰基和-C（O）R 2a，其中R 2a是选自C 1-6烷氧基和（C 1-6烷基）烷基的成员， 0-2氨基; L是选自-CH 2 - ， - CH（CH 3 CH 3） - ， - CH 2 - ， - CH 2 CH 2（CH 3 CH 3） - 和-CH 2 CH _{2 CH 2 - ; L 1是选自键和-CH 2 - 的连接基团。 L 2是从由-NH-和-CH 2 - 的键组成的组中的连接基团。和Ar 1是选自苯，吡啶和嘧啶的芳环; 被提供。该化合物可用于抑制ADP-血小板聚集，特别是在治疗血栓形成和血栓相关病症或病症中。}

10. 发明申请

US20100234352A1 FACTOR XA INHIBITORS 审中-公开
标题翻译：因子XA抑制剂
公开(公告)号：US20100234352A1
公开(公告)日：2010-09-16
申请号：US12697135
申请日：2010-01-29
申请人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough
发明人： Bing-Yan Zhu , Shawn M. Bauer , Zhaozhong J. Jia , Yonghong Song , Gary D. Probst , Yanchen Zhang , Robert M. Scarborough
IPC分类号： A61K31/55 , A61K31/497 , A61K31/513 , A61K31/501 , A61K31/551 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/4178 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61K31/538 , A61K31/4709 , A61P7/02 , A61P9/00
CPC分类号： C07D409/14 , C07D333/38 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
摘要翻译：本发明涉及由式（I）表示的化合物或其药学上可接受的盐，酯或前药，其是因子Xa的抑制剂。本发明还涉及用于制备这种化合物的中间体，含有这些化合物的药物组合物，预防或治疗多种不想要的血栓形成特征的病症的方法以及抑制血液样品凝固的方法。

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