公开(公告)号：US08378104B2

公开(公告)日：2013-02-19

申请号：US13025281

申请日：2011-02-11

Applicant: Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

Inventor： Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

IPC: C07D471/02

CPC classification number: C07D491/048

Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.

Abstract translation: 式1的化合物，如下文所定义：其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分由TAK1驱动的肿瘤，或适合于 TAK1抑制剂有效。 本发明并不限于本发明。

公开(公告)号：US07081454B2

公开(公告)日：2006-07-25

申请号：US10263448

申请日：2002-10-02

Applicant: Mark D. Wittman ,  Neelakantan Balasubramanian ,  Upender Velaparthi ,  Kurt Zimmermann ,  Mark G. Saulnier ,  Peiying Liu ,  Xiaopeng Sang ,  David B. Frennesson ,  Karen M. Stoffan ,  James G. Tarrant ,  Anne Marinier ,  Stephan Roy

Inventor： Mark D. Wittman ,  Neelakantan Balasubramanian ,  Upender Velaparthi ,  Kurt Zimmermann ,  Mark G. Saulnier ,  Peiying Liu ,  Xiaopeng Sang ,  David B. Frennesson ,  Karen M. Stoffan ,  James G. Tarrant ,  Anne Marinier ,  Stephan Roy

IPC: C07D267/10 ,  C07D413/14 ,  A61K31/553 ,  A66K31/5377

CPC classification number: C07D417/14 ,  A61K45/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐。 式I化合物抑制酪氨酸激酶，从而使其成为抗癌剂。 式I化合物还可用于治疗可通过抑制酪氨酸激酶的治疗的其它疾病。

公开(公告)号：US08865752B2

公开(公告)日：2014-10-21

申请号：US13935517

申请日：2013-07-04

Applicant: Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J. W. M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

Inventor： Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J. W. M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

IPC: C07D417/12 ,  A61K31/428 ,  C07D417/06 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D417/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

Abstract translation: 本发明提供具有一般结构式（I）的化合物及其药学上可接受的衍生物，如本文中一般和本类和亚类所述，并且另外提供其药物组合物，以及用于治疗任何一种 涉及纤维化和增殖的病症或疾病，其中抗纤维化或抗增殖活性是有益的。

公开(公告)号：US07223757B2

公开(公告)日：2007-05-29

申请号：US11289834

申请日：2005-11-30

Applicant: Mark D. Wittman ,  Neelakantan Balasubramanian ,  Upender Velaparthi ,  Kurt Zimmermann ,  Mark G. Saulnier ,  Peiying Liu ,  Xiaopeng Sang ,  David B. Frennesson ,  Karen M. Stoffan ,  James G. Tarrant ,  Anne Marinier ,  Stephan Roy

Inventor： Mark D. Wittman ,  Neelakantan Balasubramanian ,  Upender Velaparthi ,  Kurt Zimmermann ,  Mark G. Saulnier ,  Peiying Liu ,  Xiaopeng Sang ,  David B. Frennesson ,  Karen M. Stoffan ,  James G. Tarrant ,  Anne Marinier ,  Stephan Roy

IPC: C07D401/14 ,  C07D413/14 ,  A61K31/496 ,  A61K31/5377

CPC classification number: C07D417/14 ,  A61K45/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases which can be treated by inhibiting tyrosine kinase enzymes.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐。 式I化合物抑制酪氨酸激酶，从而使其成为抗癌剂。 式I化合物还可用于治疗可通过抑制酪氨酸激酶的治疗的其它疾病。

公开(公告)号：US20120046267A1

公开(公告)日：2012-02-23

申请号：US13025281

申请日：2011-02-11

Applicant: Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

Inventor： Keith R. Hornberger ,  Dan M. Berger ,  Xin Chen ,  Andrew P. Crew ,  Hanqing Dong ,  Andrew Kleinberg ,  An-Hu Li ,  Lifu Ma ,  Mark J. Mulvihill ,  Bijoy Panicker ,  Kam W. Siu ,  Arno G. Steinig ,  James G. Tarrant ,  Jing Wang ,  Qinghua Weng ,  Rajaram Sangem ,  Ramesh C. Gupta

IPC: A61K31/4355 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/5377 ,  C07D495/04 ,  A61K31/4365 ,  A61K31/519 ,  A61K31/5025 ,  C07D513/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/502 ,  C12N9/99 ,  A61P35/00 ,  A61P29/00 ,  C07D491/048

CPC classification number: C07D491/048

Abstract: Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.

Abstract translation: 式1的化合物，如下文所定义：其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分由TAK1驱动的肿瘤，或适合于 TAK1抑制剂有效。 本发明并不限于本发明。

公开(公告)号：US07253168B2

公开(公告)日：2007-08-07

申请号：US11100355

申请日：2005-04-06

Applicant: Alan J. Hutchison ,  Bertrand L. Chenard ,  James G. Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George P. Luke ,  John M. Peterson ,  Wallace C. Pringle ,  Mary-Margaret E. O'Donnell ,  Kyungae Lee ,  Linda M. Gustavson ,  Dario Doller

Inventor： Alan J. Hutchison ,  Bertrand L. Chenard ,  James G. Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George P. Luke ,  John M. Peterson ,  Wallace C. Pringle ,  Mary-Margaret E. O'Donnell ,  Kyungae Lee ,  Linda M. Gustavson ,  Dario Doller

IPC: A07D241/36 ,  A61K31/498 ,  A61P3/04 ,  A61P3/10 ,  C07D239/70 ,  C07D487/08 ,  C07D471/14 ,  A61K31/517 ,  A61K31/407

CPC classification number: C07D213/74 ,  C07D213/82 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract translation: 提供了式I化合物，其中变量如本文所述：这样的化合物可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗各种代谢，进食和性障碍 在人类，驯养的伴侣动物和家畜中。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

公开(公告)号：US06750246B1

公开(公告)日：2004-06-15

申请号：US09712352

申请日：2000-11-14

Applicant: John F. Kadow ,  Harold Mastalerz ,  Qiufen May Xue ,  Steven Hansel ,  Mary Edson Zoeckler ,  William C. Rose ,  James G. Tarrant

Inventor： John F. Kadow ,  Harold Mastalerz ,  Qiufen May Xue ,  Steven Hansel ,  Mary Edson Zoeckler ,  William C. Rose ,  James G. Tarrant

IPC: A61K31337

CPC classification number: C07D305/14 ,  A61K31/337

Abstract: The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations. The invention claims compounds of formula I and the use of compounds of formula I or pharmaceutical salts thereof as oral drugs for the treatment of human or veterinary disease. in which: R is phenyl, isopropyl, or tert butyl; R1 is —C(O)Rz in which Rz is (CH3)3CO—, (CH3)3CCH2—, CH3(CH2)3O—, cyclobutyl-, cyclohexyloxy, or (2-furyl); R2 is CH3C(O)O—.

Abstract translation: 本发明涉及新型紫杉烷衍生物，其作为抗肿瘤剂的用途和药物制剂。本发明要求式I化合物和式I化合物或其药用盐作为口服药物用于治疗人类或兽医疾病的用途。 其中R是苯基，异丙基或叔丁基; R 1是-C（O）R z，其中R z是（CH 3）3 CO-，（CH 3）3 CCH 2 - ，CH 3（CH 2）3 O - ，环丁基 - ，环己氧基或（2-呋喃基）; R 2是CH 3 C（O）O-。

公开(公告)号：US20140018401A1

公开(公告)日：2014-01-16

申请号：US13935517

申请日：2013-07-04

Applicant: Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

Inventor： Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

IPC: C07D417/12

CPC classification number: C07D417/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

Abstract translation: 本发明提供具有一般结构式（I）的化合物及其药学上可接受的衍生物，如本文中一般和本类和亚类所述，并且另外提供其药物组合物，以及用于治疗任何一种 涉及纤维化和增殖的病症或疾病，其中抗纤维化或抗增殖活性是有益的。

公开(公告)号：US08513291B2

公开(公告)日：2013-08-20

申请号：US13700730

申请日：2011-06-01

Applicant: Bijoy Panicker ,  Lambertus J. W. M. Oehlen ,  James G. Tarrant ,  Dong Sung Lim ,  Xiaokang Zhu ,  Dawoon Jung ,  Rama K. Mishra

Inventor： Bijoy Panicker ,  Lambertus J. W. M. Oehlen ,  James G. Tarrant ,  Dong Sung Lim ,  Xiaokang Zhu ,  Dawoon Jung ,  Rama K. Mishra

IPC: C07D277/66 ,  C07D277/74 ,  C07D277/82 ,  A61K31/428

CPC classification number: C07D417/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

Abstract translation: 本发明提供具有一般结构式（I）的化合物及其药学上可接受的衍生物，如本文中一般和本类和亚类所述，并且另外提供其药物组合物，以及用于治疗任何一种 涉及纤维化和增殖的病症或疾病，其中抗纤维化或抗增殖活性是有益的。

公开(公告)号：US20150158853A1

公开(公告)日：2015-06-11

申请号：US14493976

申请日：2014-09-23

Applicant: Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

Inventor： Bijoy Panicker ,  Dong Sung Lim ,  Rama K. Mishra ,  Lambertus J.W.M. Oehlen ,  James G. Tarrant ,  Xiaokang Zhu ,  Dawoon Jung

IPC: C07D417/06 ,  C07D417/14

CPC classification number: C07D417/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.

Abstract translation: 本发明提供具有一般结构式（I）的化合物及其药学上可接受的衍生物，如本文中一般和本类和亚类所述，并且另外提供其药物组合物，以及用于治疗任何一种 涉及纤维化和增殖的病症或疾病，其中抗纤维化或抗增殖活性是有益的。