公开(公告)号：US20060040956A1

公开(公告)日：2006-02-23

申请号：US11234713

申请日：2005-09-23

Applicant: Guoqing Chen ,  Jeffrey Adams ,  Jean Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael Handley ,  Qi Huang ,  Joseph Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod Patel ,  Leon Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Yuan ,  Michael Croghan

Inventor： Guoqing Chen ,  Jeffrey Adams ,  Jean Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael Handley ,  Qi Huang ,  Joseph Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod Patel ,  Leon Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Yuan ,  Michael Croghan

IPC: A61K31/506 ,  C07D403/02

CPC classification number: C07D213/82 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Selected heterocyclic 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.

公开(公告)号：US20050245547A1

公开(公告)日：2005-11-03

申请号：US11042398

申请日：2005-01-24

Applicant: Tae-Seong Kim ,  Jean-Christophe Harmange ,  David Bauer ,  Shon Booker ,  Yuan Cheng ,  Shimin Xu ,  Ning Xi ,  Joseph Kim ,  Andrew Tasker

Inventor： Tae-Seong Kim ,  Jean-Christophe Harmange ,  David Bauer ,  Shon Booker ,  Yuan Cheng ,  Shimin Xu ,  Ning Xi ,  Joseph Kim ,  Andrew Tasker

IPC: A61K31/47 ,  A61K31/4709 ,  A61K31/4745 ,  A61K31/517 ,  A61K31/519 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/02 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/02 ,  C07D495/04

CPC classification number: C07D495/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

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：US08772481B2

公开(公告)日：2014-07-08

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: A61K31/4375 ,  A61K31/50 ,  C07D413/14 ,  C07D487/04

CPC classification number: C07D471/04

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatments of protein kinase mediated diseases, including inflammation and related conditions.

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。

公开(公告)号：US20140187553A1

公开(公告)日：2014-07-03

申请号：US14006285

申请日：2012-03-21

Applicant: Hui-Ling Wang ,  Victor J. Cee ,  Bradley J. Herberich ,  Claire L.M. Jackson ,  Brian Alan Lanman ,  Thomas Nixey ,  Liping H. Pettus ,  Anthony B. Reed ,  Bin Wu ,  Ryan Wurz ,  Andrew Tasker

Inventor： Hui-Ling Wang ,  Victor J. Cee ,  Bradley J. Herberich ,  Claire L.M. Jackson ,  Brian Alan Lanman ,  Thomas Nixey ,  Liping H. Pettus ,  Anthony B. Reed ,  Bin Wu ,  Ryan Wurz ,  Andrew Tasker

IPC: C07D413/14 ,  C07D487/04 ,  C07D417/04 ,  C07D471/04 ,  C07D417/14

CPC classification number: C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

Abstract: The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Abstract translation: 本发明涉及式I和Ia的双环化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。

公开(公告)号：US08420649B2

公开(公告)日：2013-04-16

申请号：US13060675

申请日：2009-08-26

Applicant: Liping H. Pettus ,  Andrew Tasker ,  Bin Wu

Inventor： Liping H. Pettus ,  Andrew Tasker ,  Bin Wu

IPC: A01N43/58 ,  A61K31/50

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 R1, R2, R3, R4, R5, W and X 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。 化合物具有通式I，其中R 1，R 2，R 3，R 4，R 5，W和X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p38地图激酶介导的疾病包括类风湿性关节炎，银屑病，慢性阻塞性肺病，疼痛和其它炎性疾病以及中间体 和可用于制备式I化合物的方法。

公开(公告)号：US08349831B2

公开(公告)日：2013-01-08

申请号：US11977777

申请日：2007-10-25

Applicant: Thomas S. Coulter ,  Adam James Davenport ,  Christopher H. Fotsch ,  Chiara Ghiron ,  Paul E. Harrington ,  Michael Gerard Kelly ,  Steve Fong Poon ,  Andrew Tasker ,  Ning Xi ,  Qing Ping Zeng

Inventor： Thomas S. Coulter ,  Adam James Davenport ,  Christopher H. Fotsch ,  Chiara Ghiron ,  Paul E. Harrington ,  Michael Gerard Kelly ,  Steve Fong Poon ,  Andrew Tasker ,  Ning Xi ,  Qing Ping Zeng

IPC: A61K31/5377 ,  A61K31/137 ,  C07C211/29 ,  A61P13/12 ,  A61P9/00 ,  C07D401/04

CPC classification number: C07D261/18 ,  C07C211/29 ,  C07C217/58 ,  C07C233/43 ,  C07C233/44 ,  C07C233/80 ,  C07C271/28 ,  C07C311/37 ,  C07C317/32 ,  C07C323/32 ,  C07C2601/08 ,  C07C2601/16 ,  C07D207/06 ,  C07D207/09 ,  C07D207/48 ,  C07D211/22 ,  C07D211/62 ,  C07D213/30 ,  C07D213/38 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D233/60 ,  C07D235/06 ,  C07D237/14 ,  C07D239/42 ,  C07D249/08 ,  C07D261/08 ,  C07D263/24 ,  C07D263/34 ,  C07D271/06 ,  C07D285/06 ,  C07D295/088 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  C07D307/68 ,  C07D317/58 ,  C07D333/38 ,  C07D333/40 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04

Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Abstract translation: 本发明一般涉及式I所示的化合物，包含它们的药物组合物以及治疗与钙敏感受体的功能有关的疾病或病症的方法。 本发明还涉及制备这些化合物和在这些方法中有用的中间体的方法。

公开(公告)号：US08338455B2

公开(公告)日：2012-12-25

申请号：US12004156

申请日：2007-12-19

Applicant: Yuan Cheng ,  Deborah Choquette ,  Jean-Christophe Harmange ,  Andrew Tasker

Inventor： Yuan Cheng ,  Deborah Choquette ,  Jean-Christophe Harmange ,  Andrew Tasker

IPC: C07D401/02 ,  A61K31/47

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D417/14

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as VEGF 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: 选择的化合物对于预防和治疗诸如VEGF介导的疾病的疾病是有效的。 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：US08247409B2

公开(公告)日：2012-08-21

申请号：US12616646

申请日：2009-11-11

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

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

IPC: A61K31/5052 ,  A61K31/5377 ,  C07D413/14 ,  C07D487/04 ,  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

公开(公告)号：US20120083449A1

公开(公告)日：2012-04-05

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: A61K38/03 ,  A61P25/22 ,  A61K38/08 ,  A61K38/10 ,  A61K38/17 ,  A61K38/07

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：US20120040983A1

公开(公告)日：2012-02-16

申请号：US13123889

申请日：2009-10-07

Applicant: Andrew Tasker ,  James R. Falsey ,  Robert M. Rzasa ,  Bradley J. Herberich ,  Dawei Zhang

Inventor： Andrew Tasker ,  James R. Falsey ,  Robert M. Rzasa ,  Bradley J. Herberich ,  Dawei Zhang

IPC: C07D401/04 ,  A61K31/50 ,  C07D413/02 ,  A61P25/28 ,  A61P3/10 ,  A61P11/06 ,  A61P31/12 ,  A61P1/04 ,  A61P19/02 ,  A61P11/00 ,  A61P9/10 ,  A61P31/18 ,  A61P25/00 ,  A61P37/08 ,  A61P17/00 ,  A61P19/00 ,  A61P31/22 ,  A61P17/06 ,  A61K31/501

CPC classification number: C07D401/12 ,  C07D237/30 ,  C07D237/32 ,  C07D237/34 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04

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 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。 该化合物具有通式I，其中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。