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1. 发明授权

US5710159A Integrin receptor antagonists 失效
标题翻译：整合素受体拮抗剂
公开(公告)号：US5710159A
公开(公告)日：1998-01-20
申请号：US647132
申请日：1996-05-09
申请人： Matthew Ernst Voss , Prabhakar Kondaji Jadhav , Joanne Marie Smallheer , Douglas Guy Batt , William John Pitts , John Wityak
发明人： Matthew Ernst Voss , Prabhakar Kondaji Jadhav , Joanne Marie Smallheer , Douglas Guy Batt , William John Pitts , John Wityak
IPC分类号： C07D413/06 , C07D413/12 , C07D417/06 , A61K31/505
CPC分类号： C07D413/06 , C07D413/12 , C07D417/06
摘要： This invention relates to novel heterocycle compounds including but not limited to 3-�3-�3-(imidazolin-2-yl amino)propyloxy!isoxazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)-propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.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 and the treatment of angiogenic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions.
摘要翻译：本发明涉及包括但不限于3- [3- [3-（咪唑啉-2-基氨基）丙氧基]异恶唑-5-基羰基氨基] -2-（苄氧基羰基氨基） - 丙酸的新型杂环化合物，其可用作 αvβ3和相关整联蛋白受体的拮抗剂，含有这些化合物的药物组合物，制备此类化合物的方法，以及使用这些化合物单独或与其它治疗剂组合用于抑制细胞粘附和血管生成障碍，炎症，骨退化，肿瘤，转移，血栓形成和其他细胞聚集相关病症的治疗。

2. 发明授权

US5849736A Isoxazoline and isoxazole fibrinogen receptor antagonists 失效
标题翻译：异恶唑啉和异恶唑纤维蛋白原受体拮抗剂
公开(公告)号：US5849736A
公开(公告)日：1998-12-15
申请号：US455436
申请日：1995-05-31
申请人： John Wityak , Chu-Biao Xue , Thais Motria Sielecki-Dzurdz , Richard Eric Olson , William Frank Degrado , Gary Avonn Cain , Douglas Guy Batt , Donald Pinto , Munir Alwan Hussain , Shaker Ahmed Mousa
发明人： John Wityak , Chu-Biao Xue , Thais Motria Sielecki-Dzurdz , Richard Eric Olson , William Frank Degrado , Gary Avonn Cain , Douglas Guy Batt , Donald Pinto , Munir Alwan Hussain , Shaker Ahmed Mousa
IPC分类号： A61K31/42 , A61K31/423 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/535 , A61K31/5377 , A61K31/55 , A61K31/66 , A61K31/665 , A61K45/00 , A61P1/00 , A61P3/08 , A61P3/10 , A61P7/02 , A61P7/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P19/10 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D261/04 , C07D261/06 , C07D261/10 , C07D261/12 , C07D261/18 , C07D261/20 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/10 , C07F7/10 , C07F9/653 , C07F9/6571 , C07D261/02 , A61K31/54 , C07D217/00
CPC分类号： C07D413/04 , C07D261/04 , C07D261/10 , C07D413/06 , C07D413/12
摘要： This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, 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 platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
摘要翻译：本发明涉及可用作血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物或玻连蛋白受体的拮抗剂的新的异恶唑和异恶唑，含有这些化合物的药物组合物，制备这些化合物的方法，以及单独使用这些化合物的方法或与其它治疗剂组合，用于抑制血小板聚集，作为血栓溶解剂，和/或用于治疗血栓栓塞性疾病。

3. 发明授权

US6114328A Isoxazoline and isoxazole fibrogen receptor antagonists 失效
标题翻译：异恶唑啉和异恶唑纤维素受体拮抗剂
公开(公告)号：US6114328A
公开(公告)日：2000-09-05
申请号：US978295
申请日：1997-11-25
申请人： John Wityak , Chu-Biao Xue , Thais Motria Sielecki-Dzurdz , Richard Eric Olson , William Frank Degrado , Gary Avonn Cain , Douglas Guy Batt , Donald Pinto , Munir Alwan Hussain , Shaker Ahmed Mousa
发明人： John Wityak , Chu-Biao Xue , Thais Motria Sielecki-Dzurdz , Richard Eric Olson , William Frank Degrado , Gary Avonn Cain , Douglas Guy Batt , Donald Pinto , Munir Alwan Hussain , Shaker Ahmed Mousa
IPC分类号： A61K31/42 , A61K31/423 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/535 , A61K31/5377 , A61K31/55 , A61K31/66 , A61K31/665 , A61K45/00 , A61P1/00 , A61P3/08 , A61P3/10 , A61P7/02 , A61P7/04 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P19/10 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D261/04 , C07D261/06 , C07D261/10 , C07D261/12 , C07D261/18 , C07D261/20 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/10 , C07F7/10 , C07F9/653 , C07F9/6571 , A61K31/54 , C07D217/00 , C07D261/02
CPC分类号： C07D413/04 , C07D261/04 , C07D261/10 , C07D413/06 , C07D413/12
摘要： This invention relates to novel isoxazolines and isoxazoles which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex or the vitronectin receptor, 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 platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
摘要翻译：本发明涉及可用作血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物或玻连蛋白受体的拮抗剂的新的异恶唑和异恶唑，含有这些化合物的药物组合物，制备这些化合物的方法，以及单独使用这些化合物的方法或与其它治疗剂组合，用于抑制血小板聚集，作为血栓溶解剂，和/或用于治疗血栓栓塞性疾病。

4. 发明授权

US08946197B2 Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof 有权
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：US08946197B2
公开(公告)日：2015-02-03
申请号：US13509783
申请日：2010-11-12
申请人： Celia Dominguez , John Wityak , Michael Prime , Stephen Martin Courtney , Christopher Yarnold , Frederick Brookfield , Richard Marston , Douglas Macdonald
发明人： Celia Dominguez , John Wityak , Michael Prime , Stephen Martin Courtney , Christopher Yarnold , Frederick Brookfield , Richard Marston , Douglas Macdonald
IPC分类号： A61K31/635 , C07C311/46 , C07D211/34 , C07D211/54 , C07D211/58 , C07D211/96 , C07D213/38 , C07D213/40 , C07D213/56 , C07D215/38 , C07D217/14 , C07D217/22 , C07D239/42 , C07D263/58 , C07D277/42 , C07D295/205 , C07D295/26 , C07D307/52 , C07D401/04 , C07D487/04 , C07D495/04
CPC分类号： C07C311/46 , C07C2601/14 , C07D211/34 , C07D211/54 , C07D211/58 , C07D211/96 , C07D213/38 , C07D213/40 , C07D213/56 , C07D215/38 , C07D217/14 , C07D217/22 , C07D239/42 , C07D263/58 , C07D277/42 , C07D295/205 , C07D295/26 , C07D307/52 , C07D401/04 , C07D487/04 , C07D495/04
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。

5. 发明授权

US08158662B2 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：US08158662B2
公开(公告)日：2012-04-17
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： A61K31/433 , C07D285/12
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。

6. 发明申请

US20090298872A1 COMPOUNDS AND COMPOSITIONS AS MODULATORS OF STEROIDAL RECEPTORS AND CALCIUM CHANNEL ACTIVITIES 审中-公开
标题翻译：化合物和组合物作为STEROIDAL受体和钙通道活性的调节剂
公开(公告)号：US20090298872A1
公开(公告)日：2009-12-03
申请号：US11720907
申请日：2005-12-13
申请人： Pierre-Yves Michellys , Wei Pei , John Wityak
发明人： Pierre-Yves Michellys , Wei Pei , John Wityak
IPC分类号： A61K31/4418 , C07D211/90 , C07D401/02 , C07D409/04 , C07D215/48 , C07D405/04 , A61K31/444 , A61K31/4436 , A61K31/47 , A61K31/443
CPC分类号： C07D211/90 , C07D215/48 , C07D401/04 , C07D405/04 , C07D409/04
摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorder associated with the activation of steroid hormone nuclear receptors.
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类固醇激素核受体激活相关的疾病或病症的方法。

7. 发明申请

US20060030598A1 Thiazolyl inhibitors of Tec family tyrosine kinases 有权
公开(公告)号：US20060030598A1
公开(公告)日：2006-02-09
申请号：US11236375
申请日：2005-09-27
申请人： Joel Barrish , Jagabandhu Das , Steven Kanner , Chunjian Liu , Steven Spergel , John Wityak , Arthur Doweyko , Joseph Furch
发明人： Joel Barrish , Jagabandhu Das , Steven Kanner , Chunjian Liu , Steven Spergel , John Wityak , Arthur Doweyko , Joseph Furch
IPC分类号： C07D277/18 , A61K31/4439 , A61K31/427
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.

8. 发明授权

US06979694B2 Cyclic protein tyrosine kinase inhibitors 有权
公开(公告)号：US06979694B2
公开(公告)日：2005-12-27
申请号：US10378372
申请日：2003-03-03
申请人： Jagabandhu Das , Ramesh Padmanabha , Ping Chen , Derek J. Norris , Arthur M. P. Doweyko , Joel C. Barrish , John Wityak
发明人： Jagabandhu Das , Ramesh Padmanabha , Ping Chen , Derek J. Norris , Arthur M. P. Doweyko , Joel C. Barrish , John Wityak
IPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/438 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P1/00 , A61P5/14 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C237/40 , C07D213/81 , C07D213/82 , C07D231/38 , C07D233/90 , C07D239/42 , C07D263/48 , C07D277/30 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/56 , C07D277/62 , C07D409/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/20 , A61K31/44
CPC分类号： C07D277/56 , C07C233/65 , C07C237/40 , C07D213/81 , C07D213/82 , C07D231/38 , C07D233/90 , C07D239/42 , C07D263/48 , C07D409/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/113
摘要： Novel cyclic 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 immunologic and oncologic disorders.

9. 发明授权

US06455560B1 Isoxazoline fibrinogen receptor antagonists 有权
标题翻译：异恶唑啉纤维蛋白原受体拮抗剂
公开(公告)号：US06455560B1
公开(公告)日：2002-09-24
申请号：US09905417
申请日：2001-07-13
申请人： John Wityak , Prabhakar K. Jadhav
发明人： John Wityak , Prabhakar K. Jadhav
IPC分类号： A61K3142
CPC分类号： C07D413/06
摘要： This invention relates to novel isoxazolines of formula (I): or a pharmaceutically acceptable salt form thereof. This invention also relates to novel isoxazolines of formula (I) which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, 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 platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
摘要翻译：本发明涉及式（I）的新型异恶唑啉或其药学上可接受的盐形式。本发明还涉及可用作血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物的拮抗剂的式（I）的新型异恶唑，含有这些化合物的药物组合物，制备这些化合物的方法，以及单独使用这些化合物的方法或与其它治疗剂组合，用于抑制血小板聚集，作为血栓溶解剂，和/或用于治疗血栓栓塞性疾病。

10. 发明授权

US5773411A 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：US5773411A
公开(公告)日：1998-06-30
申请号：US338977
申请日：1994-11-14
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. A representative compound of the invention is cyclo-(D-Val-N(Me)Arg-Gly-Asp-�5-aminomethyl!-2-furoate).
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。本发明的代表性化合物是环 - （D-Val-N（Me）Arg-Gly-Asp- [5-氨基甲基] -2-糠酸酯）。

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