公开(公告)号：US06242582B1

公开(公告)日：2001-06-05

申请号：US09142088

申请日：1999-01-11

Applicant: Phillip A. Reece ,  Wen-Yang Wu ,  Betty Jin ,  Guy Y. Krippner ,  Keith Geoffrey Watson

Inventor： Phillip A. Reece ,  Wen-Yang Wu ,  Betty Jin ,  Guy Y. Krippner ,  Keith Geoffrey Watson

IPC: C07G300

CPC classification number: C07D407/06 ,  C07D309/28 ,  C07D495/04 ,  G01N33/56983 ,  G01N33/573

Abstract: The invention provides a method of detection of influenza virus which utilizes compounds able to bind specifically to the active site of influenza virus neuraminidase, and novel compounds for use in the method.

Abstract translation: 本发明提供一种使用能够特异性结合流感病毒神经氨酸酶活性位点的化合物的流感病毒检测方法和用于该方法的新型化合物。

公开(公告)号：US08377963B2

公开(公告)日：2013-02-19

申请号：US13570938

申请日：2012-08-09

Applicant: Siew Yeen Chai ,  Michael William Parker ,  Anthony Lloyd Albiston ,  Frederick A. O. Mendelsohn ,  Keith Geoffrey Watson

Inventor： Siew Yeen Chai ,  Michael William Parker ,  Anthony Lloyd Albiston ,  Frederick A. O. Mendelsohn ,  Keith Geoffrey Watson

IPC: C07D407/04 ,  A61K31/4433 ,  A61K31/4725

CPC classification number: C07D405/04

Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.

Abstract translation: 本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。 特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能。

公开(公告)号：US08263775B2

公开(公告)日：2012-09-11

申请号：US12743225

申请日：2008-11-18

Applicant: Siew Yeen Chai ,  Michael William Parker ,  Anthony Lloyd Albiston ,  Frederick A. O. Mendelsohn ,  Keith Geoffrey Watson

Inventor： Siew Yeen Chai ,  Michael William Parker ,  Anthony Lloyd Albiston ,  Frederick A. O. Mendelsohn ,  Keith Geoffrey Watson

IPC: C07D407/04

CPC classification number: C07D405/04

Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.

Abstract translation: 本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。 特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能。

公开(公告)号：US20100197711A1

公开(公告)日：2010-08-05

申请号：US12678836

申请日：2007-09-27

Applicant: Keith Geoffrey Watson ,  Guillaume Laurent Lessene ,  Jonathan Bayldon Baell ,  David Ching Siang Huang ,  Ian Philip Street ,  Jerry McKee Adams ,  Peter Malcolm Colman ,  Brad Edmund Sleebs ,  Brian John Smith ,  Peter Edward Czabotar

Inventor： Keith Geoffrey Watson ,  Guillaume Laurent Lessene ,  Jonathan Bayldon Baell ,  David Ching Siang Huang ,  Ian Philip Street ,  Jerry McKee Adams ,  Peter Malcolm Colman ,  Brad Edmund Sleebs ,  Brian John Smith ,  Peter Edward Czabotar

IPC: A61K31/428 ,  C07D277/82 ,  C07D417/12 ,  C12N5/09 ,  A61K31/506 ,  A61K31/4439 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P35/02 ,  A61P19/02

CPC classification number: C07D417/12 ,  C07D277/82 ,  C07D417/14

Abstract: The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.

Abstract translation: 本发明涉及苯并噻唑化合物，其类似于仅BH3蛋白的活性并且能够结合和中和生存的Bcl 2蛋白。 本发明还涉及这些化合物在调节细胞死亡或细胞存活以及治疗和/或预防与细胞死亡或细胞存活失调相关的疾病或病症中的用途。

公开(公告)号：US20120309787A1

公开(公告)日：2012-12-06

申请号：US13570938

申请日：2012-08-09

Applicant: SIEW YEEN CHAI ,  Michael William Parker ,  Anthony Lloyd Albiston ,  Frederick A.O. Mendelsohn ,  Keith Geoffrey Watson

Inventor： SIEW YEEN CHAI ,  Michael William Parker ,  Anthony Lloyd Albiston ,  Frederick A.O. Mendelsohn ,  Keith Geoffrey Watson

IPC: A61K31/4709 ,  A61P25/00

CPC classification number: C07D405/04

Abstract: The present invention relates to inhibitors of insulin-regulated aminopeptidase (IRAP) and methods for inhibiting same, as well as compositions comprising said inhibitors. In particular, the inhibitors of the present invention may be useful in therapeutic applications including enhancing memory and learning functions.

Abstract translation: 本发明涉及胰岛素调节氨基肽酶抑制剂（IRAP）及其抑制方法，以及包含所述抑制剂的组合物。 特别地，本发明的抑制剂可用于治疗应用，包括增强记忆和学习功能。

公开(公告)号：US20120184541A1

公开(公告)日：2012-07-19

申请号：US13347364

申请日：2012-01-10

Applicant: Jonathan Bayldon Baell ,  Chinh Thien Bui ,  Peter Colman ,  Danette A. Dudley ,  Wayne J. Fairbrother ,  John A. Flygare ,  Guillaume Laurent Lessene ,  Chudi Ndubaku ,  George Nikolakopoulos ,  Carl Steven Rye ,  Brad Edmund Sleebs ,  Brian John Smith ,  Keith Geoffrey Watson ,  Steven W. Elmore ,  Andrew M. Petros ,  Andrew J. Souers ,  Peter Czabotar

Inventor： Jonathan Bayldon Baell ,  Chinh Thien Bui ,  Peter Colman ,  Danette A. Dudley ,  Wayne J. Fairbrother ,  John A. Flygare ,  Guillaume Laurent Lessene ,  Chudi Ndubaku ,  George Nikolakopoulos ,  Carl Steven Rye ,  Brad Edmund Sleebs ,  Brian John Smith ,  Keith Geoffrey Watson ,  Steven W. Elmore ,  Andrew M. Petros ,  Andrew J. Souers ,  Peter Czabotar

IPC: A61K31/4709 ,  A61K31/519 ,  A61P9/00 ,  A61P35/00 ,  A61P35/02 ,  A61P7/02 ,  A61K31/538 ,  A61K31/498

CPC classification number: C07D417/14 ,  C07D417/12 ,  C07D487/04

Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.

Abstract translation: 一方面，本发明提供式I化合物，其中在式I中，变量X1，X2a，X2b，X2c，R1，B，L，E，A和下标n如本文所定义。 另一方面，本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症（例如，癌症，血小板增多症等）的方法 的Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。