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12. 发明授权

US08569345B2 Compounds and compositions as LXR modulators 失效
标题翻译：化合物和组合物作为LXR调节剂
公开(公告)号：US08569345B2
公开(公告)日：2013-10-29
申请号：US13414385
申请日：2012-03-07
申请人： Valentina Molteni , Xiaolin Li , Juliet Nabakka , David Archer Ellis , Beth Anaclerio , Enrique Saez , John Wityak
发明人： Valentina Molteni , Xiaolin Li , Juliet Nabakka , David Archer Ellis , Beth Anaclerio , Enrique Saez , John Wityak
IPC分类号： A61K31/4439 , A61K31/433 , C07D417/04 , C07D417/14
CPC分类号： C07D285/12 , A61K31/433 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
摘要翻译：本发明提供化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与肝脏X受体（LXR）活性相关的疾病或病症的方法。

13. 发明授权

US07846949B2 Compounds and compositions as LXR modulators 有权
标题翻译：化合物和组合物作为LXR调节剂
公开(公告)号：US07846949B2
公开(公告)日：2010-12-07
申请号：US10589410
申请日：2005-02-11
申请人： Valentina Molteni , Xiaolin Li , Fang Liang , Juliet Nabakka , Enrique Saez , John Wityak
发明人： Valentina Molteni , Xiaolin Li , Fang Liang , Juliet Nabakka , Enrique Saez , John Wityak
IPC分类号： A61K31/44 , A61K31/42 , A61K31/41 , C07D213/55 , C07D498/00 , C07D231/12 , C07C229/00
CPC分类号： C07C233/83 , C07C237/38 , C07C237/42 , C07C239/20 , C07C255/29 , C07C255/54 , C07C255/60 , C07C271/28 , C07C311/08 , C07C317/22 , C07C323/42 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D239/26
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
摘要翻译：本发明提供化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与肝脏X受体（LXR）活性相关的疾病或病症的方法。

14. 发明申请

US20090325981A1 Compounds and compositions as lxr modulators 失效
标题翻译：化合物和组合物作为lxr调节剂
公开(公告)号：US20090325981A1
公开(公告)日：2009-12-31
申请号：US10589087
申请日：2005-02-11
申请人： Valentina Molteni , Xiaolin Li , Juliet Nabakka , David Archer Ellis , Beth Anaclerio , Enrique Saez , John Wityak
发明人： Valentina Molteni , Xiaolin Li , Juliet Nabakka , David Archer Ellis , Beth Anaclerio , Enrique Saez , John Wityak
IPC分类号： A61K31/506 , C07D285/12 , A61K31/433 , A61K31/4439 , C07D417/04 , C07D417/12 , A61P3/00
CPC分类号： C07D285/12 , A61K31/433 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).
摘要翻译：本发明提供化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与肝脏X受体（LXR）活性相关的疾病或病症的方法。

15. 发明申请

US20060069101A1 Prodrugs of protein tyrosine kinase inhibitors 审中-公开
标题翻译：蛋白酪氨酸激酶抑制剂的前药
公开(公告)号：US20060069101A1
公开(公告)日：2006-03-30
申请号：US11235507
申请日：2005-09-26
申请人： Kyoung Kim , Francis Lee , Louis Lombardo , Feng Luo , John Wityak
发明人： Kyoung Kim , Francis Lee , Louis Lombardo , Feng Luo , John Wityak
IPC分类号： A61K31/506 , C07D417/14
CPC分类号： C07D417/12 , C07D417/14
摘要： Novel compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as oncologic and immunologic disorders.
摘要翻译：新颖的化合物及其盐，含有这些化合物的药物组合物，以及使用这些化合物治疗蛋白质酪氨酸激酶相关疾病例如肿瘤和免疫疾病的方法。

16. 发明授权

US06953795B2 Thiazolyl inhibitors of Tec family tyrosine kinases 有权
标题翻译： Tec家族酪氨酸激酶的噻唑基抑制剂
公开(公告)号：US06953795B2
公开(公告)日：2005-10-11
申请号：US10642040
申请日：2003-08-15
申请人： Joel C. Barrish , Jagabandhu Das , Steven B. Kanner , Chunjian Liu , Steven H. Spergel , John Wityak , Arthur M. P. Doweyko , Joseph A. Furch III
发明人： Joel C. Barrish , Jagabandhu Das , Steven B. Kanner , Chunjian Liu , Steven H. Spergel , John Wityak , Arthur M. P. Doweyko , Joseph A. Furch III
IPC分类号： C07D277/20 , A61K31/438 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/00 , A61P1/04 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D277/32 , C07D277/46 , C07D277/54 , C07D417/12 , C07D417/14 , C07D491/10 , C07D491/107 , C07D419/10 , C07D419/12
CPC分类号： C07D417/12 , C07D277/46 , C07D277/54 , C07D417/14 , C07D491/10
摘要： Novel thiazolyl compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of Tec family tyrosine kinase-associated disorders such as cancer, immunologic disorders and allergic disorders.
摘要翻译：新的噻唑基化合物及其盐，含有这些化合物的药物组合物，以及使用这些化合物治疗Tec家族酪氨酸激酶相关疾病如癌症，免疫学障碍和过敏性疾病的方法。

17. 发明授权

US06358976B1 Integrin receptor antagonists 失效
标题翻译：整合素受体拮抗剂
公开(公告)号：US06358976B1
公开(公告)日：2002-03-19
申请号：US09510379
申请日：2000-02-22
申请人： John Wityak , Aleksandra Ewa Tobin
发明人： John Wityak , Aleksandra Ewa Tobin
IPC分类号： A61K3147
CPC分类号： C07D401/12 , C07D215/56 , C07D413/14
摘要： This invention relates to novel fused heterocycles which are useful as antagonists of the &agr;v&bgr;3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
摘要翻译：本发明涉及可用作阿尔法博3和相关整联蛋白受体的拮抗剂的新型稠合杂环，含有这些化合物的药物组合物，制备这些化合物的方法，以及使用这些化合物单独或与其它治疗剂组合的方法，用于抑制细胞粘附，血管生成障碍，炎症，骨退化，癌转移，糖尿病性视网膜病变，血栓形成，再狭窄，黄斑变性以及由细胞粘附和/或细胞迁移和/或血管发生介导的其它病症的治疗。

18. 发明授权

US5849693A Cyclic compounds linked by a heterocyclic ring useful as inhibitors of platelet glycoprotein IIb/IIIa 失效
标题翻译：通过杂环连接的环化合物可用作血小板糖蛋白IIb / IIIa的抑制剂
公开(公告)号：US5849693A
公开(公告)日：1998-12-15
申请号：US820424
申请日：1997-03-12
申请人： Gregory James Wells , John Wityak , Anju Parthasarathy , William Frank DeGrado , Sharon Anne Jackson , Shaker Ahmed Mousa
发明人： Gregory James Wells , John Wityak , Anju Parthasarathy , William Frank DeGrado , Sharon Anne Jackson , Shaker Ahmed Mousa
IPC分类号： A61K38/00 , A61P7/02 , C07K5/02 , C07K5/10 , C07K5/103 , C07K7/56 , C07K14/75 , A61K38/12 , C07K7/54
CPC分类号： C07K5/101 , C07K14/75 , C07K5/0207 , C07K5/1027 , A61K38/00 , Y10S514/802 , Y10S930/27
摘要： This invention relates to novel cyclic compounds linked by a heterocyclic ring system, which are useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, and to methods of using these compounds for the inhibition of platelet aggregation.
摘要翻译：本发明涉及通过杂环系统连接的新型环状化合物，其可用作血小板糖蛋白IIb / IIIa复合物的拮抗剂，含有这种环状化合物的药物组合物，以及使用这些化合物抑制血小板聚集的方法。

19. 发明申请

US20150232420A1 TRANSGLUTAMINASE TG2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF 审中-公开
标题翻译：转谷氨酰胺酶TG2抑制剂，药物组合物及其使用方法
公开(公告)号：US20150232420A1
公开(公告)日：2015-08-20
申请号：US14429288
申请日：2013-09-19
申请人： Celia DOMINGUEZ , Michael PRIME , Richard MARSTON , Frederick A. BROOKFIELD , Stephen M. COURTNEY , Douglas MACDONALD , John WITYAK , Christopher John YARNOLD , Darshan VAIDYA
发明人： Celia Dominguez , Michael Prime , Richard Marston , Frederick A. Brookfield , Stephen M. Courtney , Douglas Macdonald , John Wityak , Christopher John Yarnold , Darshan Vaidya
IPC分类号： C07C271/22 , C07D207/06 , C07D213/74 , C07D205/04 , C07D211/08 , C07D295/185 , C07D223/04
CPC分类号： C07C271/22 , C07D205/04 , C07D207/06 , C07D207/16 , C07D211/08 , C07D211/16 , C07D213/72 , C07D213/74 , C07D223/04 , C07D277/42 , C07D295/18 , C07D295/185 , C07D309/08 , C07D401/12
摘要： Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
摘要翻译：本文提供了某些化合物和药学上可接受的盐。还提供了包含至少一种化合物或其药学上可接受的盐的药物组合物和一种或多种药学上可接受的载体。描述了治疗患有某种疾病状态的患者对抑制转谷氨酰胺酶TG2活性有反应的方法。这些疾病状态包括神经变性疾病如亨廷顿病。还描述了治疗方法，包括给予至少一种化合物或其药学上可接受的盐作为单一活性剂，或者与一种或多种其它治疗剂组合施用至少一种化合物或其药学上可接受的盐。

20. 发明授权

US08691824B2 Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof 失效
标题翻译：某些犬尿氨酸-3-单加氧酶抑制剂，药物组合物及其使用方法
公开(公告)号：US08691824B2
公开(公告)日：2014-04-08
申请号：US13056919
申请日：2009-08-03
申请人： John Wityak , Leticia M. Toledo-Sherman , Celia Dominguez , Stephen Martin Courtney , Christopher John Yarnold , Paula C. De Aguiar Pena , Andreas Scheel , Dirk Winkler
发明人： John Wityak , Leticia M. Toledo-Sherman , Celia Dominguez , Stephen Martin Courtney , Christopher John Yarnold , Paula C. De Aguiar Pena , Andreas Scheel , Dirk Winkler
IPC分类号： A61K31/497
CPC分类号： A61K31/42 , Y02A50/401 , Y02A50/411 , Y02A50/465
摘要： Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
摘要翻译：本文提供了某些化学实体。还提供了包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。描述了治疗患有对KMO活性的抑制作用的某些疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症的体征或症状的化学实体。这些疾病包括神经变性疾病如亨廷顿氏病。还描述了治疗方法，包括给予至少一种作为单一活性剂的化学实体或与一种或多种其它治疗剂组合施用至少一种化学实体。还提供了用于筛选能够抑制KMO活性的化合物的方法。

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