公开(公告)号：US08017601B2

公开(公告)日：2011-09-13

申请号：US11479187

申请日：2006-06-30

Applicant: Tae-Seong Kim ,  Jean-Christophe Harmange ,  Steven Bellon ,  Shon Booker ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid M. Fellows ,  Julie Germain ,  Timothy S. Harvey ,  Joseph L. Kim ,  Matthew Lee ,  Longbin Liu ,  Vinod F. Patel ,  Andrew Tasker

Inventor： Tae-Seong Kim ,  Jean-Christophe Harmange ,  Steven Bellon ,  Shon Booker ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid M. Fellows ,  Julie Germain ,  Timothy S. Harvey ,  Joseph L. Kim ,  Matthew Lee ,  Longbin Liu ,  Vinod F. Patel ,  Andrew Tasker

IPC: C07D403/02 ,  A61K31/538

CPC classification number: C07D333/38 ,  C07D217/02 ,  C07D217/24 ,  C07D401/10 ,  C07D401/12 ,  C07D409/12 ,  C07D417/10 ,  C07D417/12

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：US07872128B2

公开(公告)日：2011-01-18

申请号：US11879831

申请日：2007-07-18

Applicant: Ning Chen ,  Essa Hu ,  Roxanne Kunz ,  Shannon Rumfelt ,  Andrew Tasker

Inventor： Ning Chen ,  Essa Hu ,  Roxanne Kunz ,  Shannon Rumfelt ,  Andrew Tasker

IPC: C07D239/42 ,  C07D498/04 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D413/12 ,  C07D261/20 ,  C07D413/14

Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit protein kinase and, accordingly, useful for treatment of c-kit mediated diseases including, without limitation, autoimmune disease, allergies, mastcytosis, mast cell related tumors and various fibrotic diseases. The compounds have a general Formula I wherein R1-5, X, Y and Z are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括能够调节c-kit蛋白激酶的新一类化合物，因此可用于治疗c-kit介导的疾病，包括但不限于自身免疫疾病，过敏症，肥大细胞增多症，肥大细胞相关肿瘤和各种​​纤维化 疾病 化合物具有通式I，其中R1-5，X，Y和Z如本文所定义。 本发明还包括药物组合物，用于治疗c-kit介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：US20100292234A1

公开(公告)日：2010-11-18

申请号：US12681823

申请日：2008-09-19

Applicant: Liping H. Pettus ,  Kelvin K.C. Sham ,  Andrew Tasker ,  Shimin Xu

Inventor： Liping H. Pettus ,  Kelvin K.C. Sham ,  Andrew Tasker ,  Shimin Xu

IPC: A61K31/5377 ,  C07D249/18 ,  A61K31/4192 ,  A61P19/10 ,  A61P35/04 ,  A61P19/02 ,  A61P11/06 ,  A61P25/28 ,  A61P37/06 ,  A61P9/10 ,  A61P3/10 ,  A61P33/06 ,  A61P31/18 ,  A61P31/16 ,  A61P31/22 ,  C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  C07D413/04 ,  C07D403/04 ,  C07D401/04 ,  A61K31/454

CPC classification number: C07D249/18 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention comprises a new class of compounds useful for modulating the activity of p38 MAP kinase. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R1 and R5 are defined herein. The invention further provides pharmaceutical compositions including one or more compounds of Formula I, use of such compounds and compositions for treatment of p38 MAP kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括一类可用于调节p38 MAP激酶活性的化合物。 该化合物具有通式I，其中A1，A2，A3，A4，A5，A6，R1和R5如本文所定义。 本发明进一步提供包含一种或多种式I化合物的药物组合物，使用这些化合物和组合物用于治疗p38MAP激酶介导的疾病，包括类风湿性关节炎，牛皮癣和其它炎症性疾病，以及可用于制备 式Ⅰ的化合物。

公开(公告)号：US07745449B2

公开(公告)日：2010-06-29

申请号：US11789189

申请日：2007-04-23

Applicant: Fang-Tsao Hong ,  James R. Falsey ,  Robert M. Rzasa ,  Seifu Tadesse ,  Andrew Tasker

Inventor： Fang-Tsao Hong ,  James R. Falsey ,  Robert M. Rzasa ,  Seifu Tadesse ,  Andrew Tasker

IPC: C07D495/04 ,  C07D413/12 ,  A61K31/519 ,  A61K31/5355 ,  A61P29/00 ,  A61P23/00 ,  C07D413/04 ,  C07D513/04 ,  A61K31/5025

CPC classification number: C07D495/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 该化合物具有通式I，其中A1，A2，B，R2和R3在本文中定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗激酶介导的疾病包括类风湿性关节炎，牛皮癣和其它炎症疾病的用途，以及可用于制备 一级方程式

公开(公告)号：US20100160312A1

公开(公告)日：2010-06-24

申请号：US12711167

申请日：2010-02-23

Applicant: Essa HU ,  Jason Brooks Human ,  Roxanne Kunz ,  Andrew Tasker ,  Ryan White

Inventor： Essa HU ,  Jason Brooks Human ,  Roxanne Kunz ,  Andrew Tasker ,  Ryan White

IPC: A61K31/5377 ,  C07D471/02 ,  A61K31/4375 ,  A61K31/519 ,  C07D401/02 ,  A61K31/517 ,  C07D413/14

CPC classification number: C07D471/04 ,  C07D401/04

Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

Abstract translation: 本发明包括能够调节c-kit受体的新一类化合物，因此可用于治疗c-kit介导的疾病，包括各种炎性，纤维化和/或肥大细胞介导的疾病如肥大细胞增多症。 化合物具有通式I，其中A0-3和R1-6在本文中定义。 本发明还包括药物组合物，用于治疗c-kit介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。

公开(公告)号：US20080161303A1

公开(公告)日：2008-07-03

申请号：US11973076

申请日：2007-10-05

Applicant: Dawei Zhang ,  Andrew Tasker ,  Kelvin K.C. Sham ,  Partha Pratim Chakrabarti ,  James Richard Falsey ,  Bradley J. Herberich ,  Liping H. Pettus ,  Robert M. Rzasa

Inventor： Dawei Zhang ,  Andrew Tasker ,  Kelvin K.C. Sham ,  Partha Pratim Chakrabarti ,  James Richard Falsey ,  Bradley J. Herberich ,  Liping H. Pettus ,  Robert M. Rzasa

IPC: A61K31/5377 ,  C07D221/02 ,  A61K31/496 ,  A61P29/00 ,  C07D295/00 ,  A61K31/437

CPC classification number: C07D471/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 化合物具有通式I，其中A，B，R 1，R 2，R 3和R 4， >在本文中定义。 本发明还包括包含一种或多种式I化合物的药物组合物，这些化合物和组合物用于治疗P38地图激酶介导的疾病（包括类风湿性关节炎，牛皮癣和其它炎症疾病）的用途，以及可用于制备 式Ⅰ的化合物。

公开(公告)号：US20060241115A1

公开(公告)日：2006-10-26

申请号：US11042634

申请日：2005-01-24

Applicant: Michele Potashman ,  Tae-Seong Kim ,  Steven Bellon ,  Shon Booker ,  Yuan Cheng ,  Joseph Kim ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Jean-Christophe Harmange ,  George Borg ,  Matthew Weiss ,  Brian Hodous ,  Russell Graceffa ,  William Buckner ,  Craig Masse ,  Deborah Choquette ,  Matthew Martin ,  Julie Germain ,  Lucian DiPietro ,  Stuart Chaffee ,  Joseph Nunes ,  John Buchanan ,  Gregory Habgood ,  David McGowan ,  Douglas Whittington

Inventor： Michele Potashman ,  Tae-Seong Kim ,  Steven Bellon ,  Shon Booker ,  Yuan Cheng ,  Joseph Kim ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Jean-Christophe Harmange ,  George Borg ,  Matthew Weiss ,  Brian Hodous ,  Russell Graceffa ,  William Buckner ,  Craig Masse ,  Deborah Choquette ,  Matthew Martin ,  Julie Germain ,  Lucian DiPietro ,  Stuart Chaffee ,  Joseph Nunes ,  John Buchanan ,  Gregory Habgood ,  David McGowan ,  Douglas Whittington

IPC: A61K31/517 ,  A61K31/502 ,  A61K31/498 ,  A61K31/4709 ,  C07D43/02

CPC classification number: C07D213/64 ,  C07D213/81 ,  C07D215/233 ,  C07D215/38 ,  C07D215/48 ,  C07D215/54 ,  C07D237/34 ,  C07D239/34 ,  C07D239/47 ,  C07D239/84 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

公开(公告)号：US20060229280A1

公开(公告)日：2006-10-12

申请号：US11063476

申请日：2005-02-23

Applicant: Martin Winn ,  Steven Boyd ,  Charles Hutchins ,  Hwan-Soo Jae ,  Andrew Tasker ,  Thomas von Geldern ,  Jeffrey Kester ,  Bryan Sorensen ,  Bruce Szczepankiewicz ,  Kenneth Henry ,  Gang Liu ,  Steven Wittenberger ,  Steven King

Inventor： Martin Winn ,  Steven Boyd ,  Charles Hutchins ,  Hwan-Soo Jae ,  Andrew Tasker ,  Thomas von Geldern ,  Jeffrey Kester ,  Bryan Sorensen ,  Bruce Szczepankiewicz ,  Kenneth Henry ,  Gang Liu ,  Steven Wittenberger ,  Steven King

IPC: A61K31/675 ,  A61K31/454 ,  C07D413/02 ,  C07D43/02

CPC classification number: C07D207/16 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14

Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

公开(公告)号：US20060199817A1

公开(公告)日：2006-09-07

申请号：US11367123

申请日：2006-03-02

Applicant: Andrew Tasker ,  Dawei Zhang ,  Guo-Qiang Cao ,  Partha Chakrabarti ,  James Falsey ,  Bradley Herberich ,  Randall Hungate ,  Liping Pettus ,  Anthony Reed ,  Robert Rzasa ,  Kelvin Sham ,  Maya Thaman ,  Shimin Xu

Inventor： Andrew Tasker ,  Dawei Zhang ,  Guo-Qiang Cao ,  Partha Chakrabarti ,  James Falsey ,  Bradley Herberich ,  Randall Hungate ,  Liping Pettus ,  Anthony Reed ,  Robert Rzasa ,  Kelvin Sham ,  Maya Thaman ,  Shimin Xu

IPC: A61K31/5377 ,  A61K31/503 ,  A61K31/53 ,  C07D487/02

CPC classification number: C07D409/04 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/10

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.

Abstract translation: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症和相关病症的化合物。 化合物具有通式I，其中A 1，A 2，B，R 1，R 2， R 3和R 4在本文中定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，这些化合物和组合物用于治疗激酶介导的疾病包括类风湿性关节炎，牛皮癣和其它炎症疾病的用途，以及可用于制备 一级方程式

公开(公告)号：US20060154961A1

公开(公告)日：2006-07-13

申请号：US11251846

申请日：2005-10-18

Applicant: Qingping Zeng ,  Guomin Yao ,  George Wohlhieter ,  Vellarkad Viswanadhan ,  Andrew Tasker ,  James Rider ,  Holger Monenschein ,  Celia Dominguez ,  Matthew Bourbeau

Inventor： Qingping Zeng ,  Guomin Yao ,  George Wohlhieter ,  Vellarkad Viswanadhan ,  Andrew Tasker ,  James Rider ,  Holger Monenschein ,  Celia Dominguez ,  Matthew Bourbeau

IPC: C07D417/02 ,  A61K31/433 ,  A61K31/4709 ,  A61K31/4745

CPC classification number: C07D417/14 ,  C07D417/04 ,  C07D471/04

Abstract: The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract translation: 本发明涉及可用于治疗由蛋白激酶B（PKB）介导的疾病的噻二唑化合物。 本发明还涉及这种噻二唑化合物及其组合物在治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病状态中的治疗用途。