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1. 发明授权

US5635477A Cyclic compounds useful as inhibitors of platelet glycoprotein IIB/IIIA 失效
标题翻译：可用作血小板糖蛋白IIB / IIIA抑制剂的循环化合物
公开(公告)号：US5635477A
公开(公告)日：1997-06-03
申请号：US461611
申请日：1995-06-05
申请人： William F. Degrado , Sharon A. Jackson , Shaker A. Mousa , Anju Parthasarathy , Michael Sworin , Maria Rafalski
发明人： William F. Degrado , Sharon A. Jackson , Shaker A. Mousa , Anju Parthasarathy , Michael Sworin , Maria Rafalski
IPC分类号： A61K38/00 , C07K7/56 , C07K14/75 , A61K38/12
CPC分类号： C07K14/75 , C07K7/56 , A61K38/00
摘要： This invention relates to novel cyclic compounds containing carbocyclic ring systems useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, with or without other therapeutic agents, and to methods of using these compounds, with or without other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of other thromboembolic disorders. This invention also relates to methods of using the cyclic compounds of the invention in combination with anti-coagulants such as warfarin or heparin, or additional anti-platelet agents such as aspirin, piroxicam or ticlopidine, or thrombin inhibitors such as boropeptides, hirudin or argatroban, or thrombolytic agents such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, for the treatment of thromboembolic disorders. A representative compound of the invention is cyclo(D-Val-(.sup..alpha. N-methyl Arg)-Gly-Asp-(3-aminomethylbenzoic acid).
摘要翻译：本发明涉及含有可用作血小板糖蛋白IIb / IIIa复合物的拮抗剂的碳环系的新型环状化合物，含有或不含其它治疗剂的含有环状化合物的药物组合物，以及使用或不使用其它治疗剂的方法治疗剂，用于抑制血小板聚集，作为血栓溶解剂，和/或用于治疗其他血栓栓塞障碍。本发明还涉及使用本发明的环状化合物与抗凝血剂如华法林或肝素或另外的抗血小板药如阿司匹林，吡罗昔康或噻氯匹定或凝血酶抑制剂如硼多肽，水蛭素或阿加曲班联合使用的方法，或血栓溶解剂如组织纤溶酶原激活剂，anistreplase，尿激酶或链激酶或其组合，用于治疗血栓栓塞性疾病。本发明的代表性化合物是环（D-Val-（αN-甲基Arg）-Gly-Asp-（3-氨基甲基苯甲酸）。

2. 发明申请

US20110223210A1 HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS 有权
公开(公告)号：US20110223210A1
公开(公告)日：2011-09-15
申请号：US13076220
申请日：2011-03-30
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravikumar Jalluri , Jordan S. Fridman , Krishna Vaddi
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravikumar Jalluri , Jordan S. Fridman , Krishna Vaddi
IPC分类号： A61K31/519 , A61K9/00 , A61P35/00 , A61P35/02 , A61P7/00 , A61P43/00
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.

3. 发明申请

US20100022522A1 HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS 有权
标题翻译：异丙基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]吡嗪类作为甘薯激酶抑制剂
公开(公告)号：US20100022522A1
公开(公告)日：2010-01-28
申请号：US12549170
申请日：2009-08-27
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravikumar Jalluri , Jordan S. Fridman , Krishna Vaddi
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravikumar Jalluri , Jordan S. Fridman , Krishna Vaddi
IPC分类号： A61K31/437 , C07D471/04 , C07D401/14 , C07D487/04 , C07D413/14 , C07D417/14 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , A61P37/06 , A61P17/00 , A61P31/12 , A61P35/00 , A61P29/00
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译：本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病，例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

4. 发明申请

US20110224157A1 HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS 有权
标题翻译：异丙基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]吡嗪类作为甘薯激酶抑制剂
公开(公告)号：US20110224157A1
公开(公告)日：2011-09-15
申请号：US13076176
申请日：2011-03-30
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
IPC分类号： A61K31/519 , A61K31/704 , A61K31/675 , A61K31/7048 , A61K31/573 , A61K31/69 , A61P35/00 , A61P43/00 , A61P35/02 , A61P9/00
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译：本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病，例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

5. 发明申请

US20090181959A1 HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS 有权
标题翻译：异丙基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]吡嗪类作为甘薯激酶抑制剂
公开(公告)号：US20090181959A1
公开(公告)日：2009-07-16
申请号：US12138082
申请日：2008-06-12
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
IPC分类号： A61K31/519 , A61P37/06 , A61P17/00 , A61P31/12 , A61P29/00 , A61P11/00 , A61K31/437 , C07D471/04 , C07D487/04 , A61K31/541 , A61K31/5377 , A61K31/496
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译：本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，并且可用于治疗与Janus激酶活性有关的疾病，例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

6. 发明申请

US20060106020A1 Tetracyclic inhibitors of Janus kinases 审中-公开
标题翻译： Janus激酶的四环抑制剂
公开(公告)号：US20060106020A1
公开(公告)日：2006-05-18
申请号：US11115702
申请日：2005-04-27
申请人： James Rodgers , Darius Robinson , Argrios Arvanitis , Thomas Maduskuie , Stacey Shepard , Louis Storace , Haisheng Wang , Maria Rafalski , Ravi Jalluri , Andrew Combs , Matthew Crawley
发明人： James Rodgers , Darius Robinson , Argrios Arvanitis , Thomas Maduskuie , Stacey Shepard , Louis Storace , Haisheng Wang , Maria Rafalski , Ravi Jalluri , Andrew Combs , Matthew Crawley
IPC分类号： A61K31/503 , A61K31/519 , C07D487/14
CPC分类号： C07D471/22 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D498/04 , C07D498/14 , C07D513/04 , C07D513/14
摘要： The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
摘要翻译：本发明提供调节Janus激酶活性的化合物，并且可用于治疗与Janus激酶（例如免疫相关疾病和癌症）的活性相关的疾病。

7. 发明授权

US08415362B2 Pyrazolyl substituted pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors 有权
标题翻译：吡唑基取代的吡咯并[2,3-b]嘧啶作为Janus激酶抑制剂
公开(公告)号：US08415362B2
公开(公告)日：2013-04-09
申请号：US12138082
申请日：2008-06-12
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri
IPC分类号： C07D487/04 , A61K31/519 , A61K31/437 , C07D471/04 , A61P35/00 , A61P29/00
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines of Formula I: that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译：本发明提供式I的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶：其调节Janus激酶的活性，并且可用于治疗与 Janus激酶包括例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

8. 发明申请

US20090215766A1 TETRACYCLIC INHIBITORS OF JANUS KINASES 审中-公开
标题翻译： JANK KINASES的四氯化碳抑制剂
公开(公告)号：US20090215766A1
公开(公告)日：2009-08-27
申请号：US12187061
申请日：2008-08-06
申请人： James D. Rodgers , Darius J. Robinson , Argyrios G. Arvanitis , Thomas P. Maduskuie, JR. , Stacey Shepard , Louis Storace , Haisheng Wang , Maria Rafalski , Ravi Kumar Jalluri , Andrew P. Combs , Matthew L. Crawley
发明人： James D. Rodgers , Darius J. Robinson , Argyrios G. Arvanitis , Thomas P. Maduskuie, JR. , Stacey Shepard , Louis Storace , Haisheng Wang , Maria Rafalski , Ravi Kumar Jalluri , Andrew P. Combs , Matthew L. Crawley
IPC分类号： A61K31/5377 , C07D513/04 , A61K31/437 , C07D487/04 , A61P37/02 , C12N9/12 , A61P35/00 , A61P3/10 , C12N9/99 , A61K31/5025 , C07D417/14 , A61K31/496
CPC分类号： C07D471/22 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D498/04 , C07D498/14 , C07D513/04 , C07D513/14
摘要： The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.
摘要翻译：本发明提供调节Janus激酶活性的化合物，并且可用于治疗与Janus激酶（例如免疫相关疾病和癌症）的活性相关的疾病。

9. 发明申请

US20070135461A1 Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors 有权
标题翻译：杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]
公开(公告)号：US20070135461A1
公开(公告)日：2007-06-14
申请号：US11637545
申请日：2006-12-12
申请人： James Rodgers , Stacey Shepard , Thomas Maduskuie , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios Arvanitis , Louis Storace , Ravi Jalluri , Jordan Fridman , Krishna Vaddi
发明人： James Rodgers , Stacey Shepard , Thomas Maduskuie , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios Arvanitis , Louis Storace , Ravi Jalluri , Jordan Fridman , Krishna Vaddi
IPC分类号： A61K31/519 , A61K31/4745 , C07D487/02 , C07D471/02
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译：本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病，例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。

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