公开(公告)号：US20050153960A1

公开(公告)日：2005-07-14

申请号：US10996035

申请日：2004-11-22

Applicant: Daniel Elbaum ,  Benny Askew ,  Shon Booker ,  Julie Germain ,  Gregory Habgood ,  Michael Handley ,  Tae-Seong Kim ,  Aiwen Li ,  Nobuko Nishimura ,  Vinod Patel ,  Chester Yuan ,  Joseph Kim ,  Guolin Cai ,  Guoqing Chen ,  Michael Croghan ,  Lucian Di Pietro ,  Celia Dominguez ,  Qi Huang ,  Leon Smith ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu

Inventor： Daniel Elbaum ,  Benny Askew ,  Shon Booker ,  Julie Germain ,  Gregory Habgood ,  Michael Handley ,  Tae-Seong Kim ,  Aiwen Li ,  Nobuko Nishimura ,  Vinod Patel ,  Chester Yuan ,  Joseph Kim ,  Guolin Cai ,  Guoqing Chen ,  Michael Croghan ,  Lucian Di Pietro ,  Celia Dominguez ,  Qi Huang ,  Leon Smith ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu

IPC: A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  A61P1/04 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P15/00 ,  A61P15/08 ,  A61P17/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P21/00 ,  A61P25/28 ,  A61P27/02 ,  A61P27/06 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P31/22 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61P37/02 ,  A61P37/04 ,  A61P37/08 ,  A61P43/00 ,  C07D213/81 ,  C07D213/82 ,  C07D237/04 ,  C07D237/24 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  A61K31/4545 ,  C07D413/02 ,  C07D41/02

CPC classification number: C07D213/81 ,  C04B35/632 ,  C07D213/82 ,  C07D237/04 ,  C07D237/24 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives 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血管生成介导的疾病等疾病是有效的。 本发明包括新型化合物，类似物，前药及其药学上可接受的衍生物，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：US20050054670A1

公开(公告)日：2005-03-10

申请号：US10926238

申请日：2004-08-24

Applicant: Christopher Tegley ,  Jeffrey Adams ,  Benny Askew ,  Michael Croghan ,  Daniel Elbaum ,  Julie Germain ,  Gregory Habgood ,  Scott Harried ,  Aiwen Li ,  Nobuko Nishimura ,  Rana Nomak ,  Andrew Tasker ,  Kevin Yang

Inventor： Christopher Tegley ,  Jeffrey Adams ,  Benny Askew ,  Michael Croghan ,  Daniel Elbaum ,  Julie Germain ,  Gregory Habgood ,  Scott Harried ,  Aiwen Li ,  Nobuko Nishimura ,  Rana Nomak ,  Andrew Tasker ,  Kevin Yang

IPC: A61P29/00 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D471/02 ,  A61K31/4035 ,  A61K31/4745

CPC classification number: C04B35/632 ,  C07D401/12 ,  C07D401/14

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis 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血管生成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：US08536129B2

公开(公告)日：2013-09-17

申请号：US13186418

申请日：2011-07-19

Applicant: Andrew Tasker ,  Tracy Doucette ,  Michael Tymianski ,  Kenneth Mendoza ,  Michael P. Belmares ,  David Garman ,  Peter S. Lu

Inventor： Andrew Tasker ,  Tracy Doucette ,  Michael Tymianski ,  Kenneth Mendoza ,  Michael P. Belmares ,  David Garman ,  Peter S. Lu

IPC: A61K38/04

CPC classification number: A61K38/1787 ,  A61K38/07

Abstract: The invention provides methods of treating or effecting prophylaxis of a patient having or at risk of developing symptoms of anxiety in which an effective regime of an agent that inhibits specific binding of PSD95 to an NMDA receptor is administered to a patient.

Abstract translation: 本发明提供了治疗或预防患有或有发生焦虑症状的患者的方法，其中向患者施用抑制PSD95与NMDA受体的特异性结合的药剂的有效方案。

公开(公告)号：US08178557B2

公开(公告)日：2012-05-15

申请号：US12157303

申请日：2008-06-09

Applicant: Michele Potashman ,  Tae-Seong Kim ,  Steven Bellon ,  Shon Booker ,  Yuan Cheng ,  Joseph L. Kim ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Jean-Christophe Harmange ,  George Borg ,  Matthew Weiss ,  Brian L. Hodous ,  Russell Graceffa ,  William H. Buckner ,  Craig E. Masse ,  Deborah Choquette ,  Matthew W. Martin ,  Julie Germain ,  Lucian V. DiPietro ,  Stuart C. Chaffee ,  Joseph J. Nunes ,  John L. Buchanan ,  David C. McGowan ,  Douglas A. Whittington ,  Gregory J. Habgood ,  Vinod F. Patel ,  Daniel La

Inventor： Michele Potashman ,  Tae-Seong Kim ,  Steven Bellon ,  Shon Booker ,  Yuan Cheng ,  Joseph L. Kim ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Jean-Christophe Harmange ,  George Borg ,  Matthew Weiss ,  Brian L. Hodous ,  Russell Graceffa ,  William H. Buckner ,  Craig E. Masse ,  Deborah Choquette ,  Matthew W. Martin ,  Julie Germain ,  Lucian V. DiPietro ,  Stuart C. Chaffee ,  Joseph J. Nunes ,  John L. Buchanan ,  David C. McGowan ,  Douglas A. Whittington ,  Gregory J. Habgood ,  Vinod F. Patel ,  Daniel La

IPC: A61K31/04

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.

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：US20120108587A1

公开(公告)日：2012-05-03

申请号：US13123885

申请日：2009-10-07

Applicant: Andrew Tasker ,  Liping H. Pettus ,  Ryan Wurz

Inventor： Andrew Tasker ,  Liping H. Pettus ,  Ryan Wurz

IPC: A61K31/5377 ,  A61K31/5025 ,  A61P29/00 ,  A61P1/00 ,  A61P11/06 ,  A61P11/00 ,  A61P17/06 ,  A61P19/02 ,  A61P7/00 ,  A61P19/10 ,  A61P27/02 ,  A61P35/02 ,  A61P1/18 ,  A61P19/06 ,  A61P11/02 ,  A61P21/00 ,  A61P3/10 ,  A61P19/08 ,  A61P37/06 ,  A61P25/28 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P33/06 ,  C07D471/04

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 A1, A2, A3, A4, L, R1, R2, R3, R5 and m are as 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, chronic obstructive pulmonary disease, ankylosing spondylitis, pain 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A1，A2，A3，A4，L，R1，R2，R3，R5和m如本文所定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，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，慢性阻塞性肺病，强直性脊柱炎，疼痛和其它炎症性疾病的化合物和组合物的用途，如 以及可用于制备式（I）化合物的中间体和方法。

公开(公告)号：US08080546B2

公开(公告)日：2011-12-20

申请号：US12288950

申请日：2008-10-24

Applicant: Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu ,  Ryan Wurz

Inventor： Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu ,  Ryan Wurz

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, and in particular, p38 activity mediated inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, A5, R1, 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 inflammatory diseases including rheumatoid arthritis, psoriasis and other 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促炎细胞因子介导的疾病，特别是p38活性介导的炎症和相关病症的化合物。 所述化合物具有通式I，其中A1，A2，A3，A4，A5，R1，R2和R3如本文所定义。 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炎性疾病（包括类风湿性关节炎，牛皮癣和其它病症）的用途，以及可用于制备式I化合物的中间体和方法 。

公开(公告)号：US20110294805A1

公开(公告)日：2011-12-01

申请号：US13197322

申请日：2011-08-03

Applicant: Liping H. PETTUS ,  Andrew Tasker ,  Shimin Xu ,  Ryan Wurz

Inventor： Liping H. PETTUS ,  Andrew Tasker ,  Shimin Xu ,  Ryan Wurz

IPC: A61K31/437 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/5377 ,  A61P19/02 ,  A61P29/00 ,  A61P19/08 ,  A61P19/10 ,  A61P35/00 ,  A61P35/02 ,  A61P11/00 ,  A61P1/00 ,  A61P17/00 ,  A61P11/06 ,  A61P3/10 ,  A61P25/28 ,  A61P31/16 ,  A61P31/22 ,  A61P17/06 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D487/04

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, R1, R2, R4, R5, R6 and Z 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, chronic obstructive pulmonary disease, pain 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，R1，R2，R4，R5，R6和Z如本文所定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，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，慢性阻塞性肺病，疼痛和其它炎症性疾病）的这些化合物和组合物的用途以及中间体 和可用于制备式I化合物的方法。

公开(公告)号：US08063055B2

公开(公告)日：2011-11-22

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: A61K31/517

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：US08022085B2

公开(公告)日：2011-09-20

申请号：US12150158

申请日：2008-04-24

Applicant: Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu

Inventor： Liping H. Pettus ,  Andrew Tasker ,  Shimin Xu

IPC: C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D491/02 ,  C07D498/02 ,  A01N43/42 ,  A61K31/44

CPC classification number: C07D471/04 ,  C07D487/04

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, R1, R2, R4, R5, R6 and Z 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, chronic obstructive pulmonary disease, pain 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，R1，R2，R4，R5，R6和Z如本文所定义。 本发明还包括药物组合物，其包含一种或多种式I化合物，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，慢性阻塞性肺病，疼痛和其它炎症性疾病）的这些化合物和组合物的用途以及中间体 和可用于制备式I化合物的方法。

公开(公告)号：US20100125074A1

公开(公告)日：2010-05-20

申请号：US12616646

申请日：2009-11-11

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: A61K31/5025 ,  C07D413/14 ,  C07D487/04 ,  A61K31/5377 ,  A61P17/00 ,  A61P19/00 ,  A61P25/00 ,  A61P31/12 ,  A61P11/00

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