公开(公告)号：US08946197B2

公开(公告)日：2015-02-03

申请号：US13509783

申请日：2010-11-12

Applicant: Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

Inventor： Celia Dominguez ,  John Wityak ,  Michael Prime ,  Stephen Martin Courtney ,  Christopher Yarnold ,  Frederick Brookfield ,  Richard Marston ,  Douglas Macdonald

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08158662B2

公开(公告)日：2012-04-17

申请号：US10589087

申请日：2005-02-11

Applicant: Valentina Molteni ,  Xiaolin Li ,  Juliet Nabakka ,  David Archer Ellis ,  Beth Anaclerio ,  Enrique Saez ,  John Wityak

Inventor： Valentina Molteni ,  Xiaolin Li ,  Juliet Nabakka ,  David Archer Ellis ,  Beth Anaclerio ,  Enrique Saez ,  John Wityak

IPC: A61K31/433 ,  C07D285/12

CPC classification number: C07D285/12 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: 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).

Abstract translation: 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。

公开(公告)号：US20090298872A1

公开(公告)日：2009-12-03

申请号：US11720907

申请日：2005-12-13

Applicant: Pierre-Yves Michellys ,  Wei Pei ,  John Wityak

Inventor： Pierre-Yves Michellys ,  Wei Pei ,  John Wityak

IPC: A61K31/4418 ,  C07D211/90 ,  C07D401/02 ,  C07D409/04 ,  C07D215/48 ,  C07D405/04 ,  A61K31/444 ,  A61K31/4436 ,  A61K31/47 ,  A61K31/443

CPC classification number: C07D211/90 ,  C07D215/48 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20060030598A1

公开(公告)日：2006-02-09

申请号：US11236375

申请日：2005-09-27

Applicant: Joel Barrish ,  Jagabandhu Das ,  Steven Kanner ,  Chunjian Liu ,  Steven Spergel ,  John Wityak ,  Arthur Doweyko ,  Joseph Furch

Inventor： Joel Barrish ,  Jagabandhu Das ,  Steven Kanner ,  Chunjian Liu ,  Steven Spergel ,  John Wityak ,  Arthur Doweyko ,  Joseph Furch

IPC: C07D277/18 ,  A61K31/4439 ,  A61K31/427

CPC classification number: C07D417/12 ,  C07D277/46 ,  C07D277/54 ,  C07D417/14 ,  C07D491/10

Abstract: 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.

公开(公告)号：US06979694B2

公开(公告)日：2005-12-27

申请号：US10378372

申请日：2003-03-03

Applicant: Jagabandhu Das ,  Ramesh Padmanabha ,  Ping Chen ,  Derek J. Norris ,  Arthur M. P. Doweyko ,  Joel C. Barrish ,  John Wityak

Inventor： Jagabandhu Das ,  Ramesh Padmanabha ,  Ping Chen ,  Derek J. Norris ,  Arthur M. P. Doweyko ,  Joel C. Barrish ,  John Wityak

IPC: 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 classification number: 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

Abstract: 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.

公开(公告)号：US06455560B1

公开(公告)日：2002-09-24

申请号：US09905417

申请日：2001-07-13

Applicant: John Wityak ,  Prabhakar K. Jadhav

Inventor： John Wityak ,  Prabhakar K. Jadhav

IPC: A61K3142

CPC classification number: C07D413/06

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US5773411A

公开(公告)日：1998-06-30

申请号：US338977

申请日：1994-11-14

Applicant: Gregory James Wells ,  John Wityak ,  Anju Parthasarathy ,  William Frank DeGrado ,  Sharon Anne Jackson ,  Shaker Ahmed Mousa

Inventor： Gregory James Wells ,  John Wityak ,  Anju Parthasarathy ,  William Frank DeGrado ,  Sharon Anne Jackson ,  Shaker Ahmed Mousa

IPC: A61K38/00 ,  A61P7/02 ,  C07K5/02 ,  C07K5/10 ,  C07K5/103 ,  C07K7/56 ,  C07K14/75 ,  A61K38/12 ,  C07K7/54

CPC classification number: C07K5/101 ,  C07K14/75 ,  C07K5/0207 ,  C07K5/1027 ,  A61K38/00 ,  Y10S514/802 ,  Y10S930/27

Abstract: 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).

Abstract translation: 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）。

公开(公告)号：US20170283436A1

公开(公告)日：2017-10-05

申请号：US15507208

申请日：2015-08-28

Applicant: Celia DOMINGUEZ ,  John WITYAK ,  Jonathan BARD ,  Alex KISELYOV ,  Christopher John BROWN ,  Sebastien Rene Gabriel GALAN ,  Michael Edward PRIME ,  Paul Richard GILES ,  Elise Luciennen Paulette GADOULEAU ,  Thomas Martin KRÜLLE ,  Daniel CLARKFREW ,  Peter David JOHNSON ,  Sabinc SCHAERTI ,  Steffen Kaspar GRIMM ,  Jan Dirk KAHMANN ,  Christoph SCHEICH ,  Samuel COE ,  Sarah HAYES ,  CHDI Foundation, Inc.

Inventor： Celia Dominguez ,  John Wityak ,  Jonathan Bard ,  Alex Kiselyov ,  Christopher John Brown ,  Sébastien René Gabriel Galan ,  Michael Edward Prime ,  Paul Richard Giles ,  Elise Luciennen Paulette Gadouleau ,  Thomas Martin Krülle ,  Daniel Clark-Frew ,  Peter David Johnson ,  Samuel Coe ,  Sarah Hayes

IPC: C07D513/04 ,  C07D413/04 ,  C07D413/14 ,  A61K51/04 ,  C07D498/04 ,  C07D405/14 ,  C07D471/04 ,  C07D263/57 ,  C07D413/12

CPC classification number: C07D513/04 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463 ,  C07D263/57 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D498/04

Abstract: Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use.

公开(公告)号：US08569345B2

公开(公告)日：2013-10-29

申请号：US13414385

申请日：2012-03-07

Applicant: Valentina Molteni ,  Xiaolin Li ,  Juliet Nabakka ,  David Archer Ellis ,  Beth Anaclerio ,  Enrique Saez ,  John Wityak

Inventor： Valentina Molteni ,  Xiaolin Li ,  Juliet Nabakka ,  David Archer Ellis ,  Beth Anaclerio ,  Enrique Saez ,  John Wityak

IPC: A61K31/4439 ,  A61K31/433 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D285/12 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K45/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: 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).

Abstract translation: 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。

公开(公告)号：US07846949B2

公开(公告)日：2010-12-07

申请号：US10589410

申请日：2005-02-11

Applicant: Valentina Molteni ,  Xiaolin Li ,  Fang Liang ,  Juliet Nabakka ,  Enrique Saez ,  John Wityak

Inventor： Valentina Molteni ,  Xiaolin Li ,  Fang Liang ,  Juliet Nabakka ,  Enrique Saez ,  John Wityak

IPC: A61K31/44 ,  A61K31/42 ,  A61K31/41 ,  C07D213/55 ,  C07D498/00 ,  C07D231/12 ,  C07C229/00

CPC classification number: 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

Abstract: 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).

Abstract translation: 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。