公开(公告)号：US20130261119A1

公开(公告)日：2013-10-03

申请号：US13878557

申请日：2011-10-27

Applicant: Antony Wilks Burgess ,  Francesca Walker ,  Keith Geoffrey Watson ,  Helen Witchard ,  Guillaume Lessene

Inventor： Antony Wilks Burgess ,  Francesca Walker ,  Keith Geoffrey Watson ,  Helen Witchard ,  Guillaume Lessene

IPC: C07D403/12

CPC classification number: C07D403/12 ,  A61K31/53

Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or pro-drug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.

Abstract translation: 本发明提供式（I）的化合物或其药学上可接受的衍生物，盐或其前体药物。 还提供了一种治疗患者癌症的方法，包括向所述受试者施用有效量的式（I）化合物或其药学上可接受的衍生物，盐或前药。 还提供式（I）化合物或其药学上可接受的衍生物，盐或前药在制备用于治疗癌症的药物中的用途。 此外，本发明还提供包含式（I）化合物或其药学上可接受的衍生物，其盐或前药的药物组合物。

公开(公告)号：US20110021563A1

公开(公告)日：2011-01-27

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 ,  A61K31/4725 ,  A61K31/4433 ,  C12Q1/37

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：US20100190782A1

公开(公告)日：2010-07-29

申请号：US12641063

申请日：2009-12-17

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

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

IPC: A61K31/536 ,  C07D417/14 ,  A61K31/4709 ,  C07D487/04 ,  A61K31/519 ,  A61K31/502 ,  A61K31/428 ,  A61K31/5377 ,  A61P35/02 ,  A61P35/00 ,  A61P7/02 ,  A61P9/00

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。

公开(公告)号：US08232273B2

公开(公告)日：2012-07-31

申请号：US12641141

申请日：2009-12-17

Applicant: Jonathan Bayldon Baell ,  Chinh Thien Bui ,  Peter Colman ,  Peter Czabotar ,  Danette A. Dudley ,  Wayne J. Fairbrother ,  John A. Flygare ,  Guillaume Laurent Lessene ,  Chudi Ndubaku ,  George Nikolakopoulos ,  Brad Edmund Sleebs ,  Brian John Smith ,  Keith Geoffrey Watson ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Andrew M. Petros ,  Andrew J. Souers ,  Zhi-Fu Tao ,  Le Wang ,  Xilu Wang ,  Kurt Deshayes

Inventor： Jonathan Bayldon Baell ,  Chinh Thien Bui ,  Peter Colman ,  Peter Czabotar ,  Danette A. Dudley ,  Wayne J. Fairbrother ,  John A. Flygare ,  Guillaume Laurent Lessene ,  Chudi Ndubaku ,  George Nikolakopoulos ,  Brad Edmund Sleebs ,  Brian John Smith ,  Keith Geoffrey Watson ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Andrew M. Petros ,  Andrew J. Souers ,  Zhi-Fu Tao ,  Le Wang ,  Xilu Wang ,  Kurt Deshayes

IPC: A61K31/5377 ,  C07D413/14

CPC classification number: C07D417/14 ,  C07D471/06 ,  C07D473/00 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D513/06

Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described 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，本发明提供了其中变量X1a，X1b，X1c，X1d，Q，A，R1，B，L，E和下标m和n具有如本文所述的含义的式I化合物 。 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。

公开(公告)号：US08114893B2

公开(公告)日：2012-02-14

申请号：US12641063

申请日：2009-12-17

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: C07D417/14 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4709

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。

公开(公告)号：US6147260A

公开(公告)日：2000-11-14

申请号：US230678

申请日：1999-06-21

Applicant: Graham John Bird ,  Keith Geoffrey Watson

Inventor： Graham John Bird ,  Keith Geoffrey Watson

IPC: C07B61/00 ,  C07C45/46 ,  C07C49/83 ,  C07C49/835 ,  C07C249/04 ,  C07C249/08 ,  C07C251/42

CPC classification number: C07C249/08 ,  C07C45/46 ,  C07C49/83 ,  C07C49/835 ,  C07C2101/16

Abstract: A process of preparing the compound of formula (I) which comprises: (a) reacting butyryl chloride with the compound of formula (IV) in the presence of a Friedel-Crafts catalyst in an inert diluent to produce a compound of formula (II) and (b) reacting the compound of formula (II) with ethoxyamine. Compound (II) is also claimed.

Abstract translation: PCT No.PCT / AU97 / 00471 Sec。 371 1999年6月21日第 102（e）1999年6月21日PCT PCT 1997年7月25日PCT公布。 第WO98 / 04510号公报 日本公开日1998年2月5日制备式（I）化合物的方法，其包括：（a）在Friedel-Crafts催化剂存在下，在惰性稀释剂中使丁酰氯与式（Ⅳ）化合物反应，生成化合物 式（II）和（b）使式（II）化合物与乙氧基胺反应。 化合物（II）也被要求保护。

公开(公告)号：US08835629B2

公开(公告)日：2014-09-16

申请号：US13878557

申请日：2011-10-27

Applicant: Antony Wilks Burgess ,  Francesca Walker ,  Keith Geoffrey Watson ,  Helen Witchard

Inventor： Antony Wilks Burgess ,  Francesca Walker ,  Keith Geoffrey Watson ,  Helen Witchard

IPC: C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D401/14 ,  A61K31/53 ,  A61P35/00

CPC classification number: C07D403/12 ,  A61K31/53

Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的衍生物，其盐或前药。 还提供了一种治疗患者癌症的方法，包括向所述受试者施用有效量的式（I）化合物或其药学上可接受的衍生物，盐或前药。 还提供式（I）化合物或其药学上可接受的衍生物，盐或前药在制备用于治疗癌症的药物中的用途。 此外，本发明还提供包含式（I）化合物或其药学上可接受的衍生物，其盐或前药的药物组合物。

公开(公告)号：US08518970B2

公开(公告)日：2013-08-27

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: C07D417/14 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4709

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.

公开(公告)号：US20100210622A1

公开(公告)日：2010-08-19

申请号：US12641141

申请日：2009-12-17

Applicant: Jonathan Bayldon Baell ,  Chinh Thien Bui ,  Peter Colman ,  Peter Czabotar ,  Danette A. Dudley ,  Wayne J. Fairbrother ,  John A, Flygare ,  Guillaume Laurent Lessene ,  Chudi Ndubaku ,  George Nikolakopoulos ,  Brad Edmund Sleebs ,  Brian John Smith ,  Keith Geoffrey Watson ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Andrew M. Petros ,  Andrew J. Souers ,  Zhi-Fu Tao ,  Le Wang ,  Xilu Wang ,  Kurt Deshayes

Inventor： Jonathan Bayldon Baell ,  Chinh Thien Bui ,  Peter Colman ,  Peter Czabotar ,  Danette A. Dudley ,  Wayne J. Fairbrother ,  John A, Flygare ,  Guillaume Laurent Lessene ,  Chudi Ndubaku ,  George Nikolakopoulos ,  Brad Edmund Sleebs ,  Brian John Smith ,  Keith Geoffrey Watson ,  Steven W. Elmore ,  Lisa A. Hasvold ,  Andrew M. Petros ,  Andrew J. Souers ,  Zhi-Fu Tao ,  Le Wang ,  Xilu Wang ,  Kurt Deshayes

IPC: A61K31/4725 ,  C07D417/14 ,  A61P35/02 ,  A61P35/00 ,  A61P9/00 ,  A61P7/02 ,  C07D471/04 ,  A61K31/5377 ,  C07D487/04 ,  A61K31/519 ,  A61K31/496 ,  C07D471/06 ,  A61K31/4745

CPC classification number: C07D417/14 ,  C07D471/06 ,  C07D473/00 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04 ,  C07D513/06

Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described 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，本发明提供了其中变量X1a，X1b，X1c，X1d，Q，A，R1，B，L，E和下标m和n具有如本文所述的含义的式I化合物 。 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。

公开(公告)号：US06680054B1

公开(公告)日：2004-01-20

申请号：US09308076

申请日：1999-07-16

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

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

IPC: A61K3944

CPC classification number: G01N33/56983 ,  C08B37/0021 ,  C08F8/30 ,  G01N2333/11 ,  G01N2333/924

Abstract: The invention provides novel macromolecules, methods for their preparation, pharmaceutical formulations thereof and their use as anti-influenza agents. The invention also provides a novel diagnostic method which can be used for detection of all types of influenza A and B virus. The macromolecular compound of the invention has attached to it one or more molecules (neuraminidase binders) which bind to the active site of influenza virus neuraminidase but which are not cleaved by the neuraminidase.

Abstract translation: 本发明提供新型大分子，其制备方法，药物制剂及其作为抗流感药物的用途。 本发明还提供了一种可用于检测所有类型的甲型和乙型流感病毒的新型诊断方法。 本发明的高分子化合物与其结合了一种或多种结合流感病毒神经氨酸酶的活性位点但不被神经氨酸酶切割的分子（神经氨酸酶结合剂）。