公开(公告)号：US20110105498A1

公开(公告)日：2011-05-05

申请号：US12150158

申请日：2008-04-24

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

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

IPC: A61K31/5377 ,  C07D471/04 ,  A61K31/437 ,  A61P19/02 ,  A61P19/10 ,  A61P35/02 ,  A61P17/00 ,  A61P3/10 ,  A61P9/10 ,  A61P37/06 ,  A61P11/06 ,  A61P31/18 ,  A61P31/16 ,  A61P31/22 ,  A61P17/06 ,  A61P29/00 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/496

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.

公开(公告)号：US07935709B2

公开(公告)日：2011-05-03

申请号：US11879243

申请日：2007-07-16

Applicant: Fang-Tsao Hong ,  Kelvin K. C. Sham ,  Seifu Tadesse ,  Andrew Tasker

Inventor： Fang-Tsao Hong ,  Kelvin K. C. Sham ,  Seifu Tadesse ,  Andrew Tasker

IPC: A61K31/517

CPC classification number: C07D471/04 ,  C07D239/82

Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of pro-inflammatory cytokine mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein s, T, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use such as treatment of p38 mediated diseases by administering the compounds of Formula I or compositions including the compounds of Formula I, and 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，包括炎症和相关病症的化合物。 化合物具有通式I，其中s，T，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，使用方法例如通过施用式I化合物或包含式I化合物的组合物治疗p38介导的疾病，以及可用于制备 式Ⅰ的化合物。

公开(公告)号：US07759337B2

公开(公告)日：2010-07-20

申请号：US11367123

申请日：2006-03-02

Applicant: Andrew Tasker ,  Dawei Zhang ,  Guo-Qiang Cao ,  Partha Pratim Chakrabarti ,  James Richard Falsey ,  Bradley J. Herberich ,  Randall W. Hungate ,  Liping H. Pettus ,  Anthony Reed ,  Robert M. Rzasa ,  Kelvin K. C. Sham ,  Maya C. Thaman ,  Shimin Xu

Inventor： Andrew Tasker ,  Dawei Zhang ,  Guo-Qiang Cao ,  Partha Pratim Chakrabarti ,  James Richard Falsey ,  Bradley J. Herberich ,  Randall W. Hungate ,  Liping H. Pettus ,  Anthony Reed ,  Robert M. Rzasa ,  Kelvin K. C. Sham ,  Maya C. Thaman ,  Shimin Xu

IPC: C07D237/34 ,  C07D413/12 ,  C07D498/08 ,  C07D279/12 ,  C07D243/08 ,  A61K31/498 ,  A61K31/5355 ,  A61K31/537 ,  A61K31/541 ,  A61K31/551 ,  A61P29/00 ,  A61P23/00 ,  C07D487/04 ,  A61K31/4985

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 B, R1, R2, R3, R4 and R5 are d.efined 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B，R 1，R 2，R 3，R 4和R 5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：US07700607B2

公开(公告)日：2010-04-20

申请号：US11879830

申请日：2007-07-18

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 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：US07622101B2

公开(公告)日：2009-11-24

申请号：US11400571

申请日：2006-04-06

Applicant: Tracey Doucette ,  Henriette Husum Bak-Jensen ,  Melissa Perry ,  Catherine Ryan ,  R. Andrew Tasker

Inventor： Tracey Doucette ,  Henriette Husum Bak-Jensen ,  Melissa Perry ,  Catherine Ryan ,  R. Andrew Tasker

IPC: A61K49/00

CPC classification number: A61K31/401 ,  A61K49/0008

Abstract: Disclosed is a developmental animal model of temporal lobe epilepsy and other seizure-related disorders. In particular, the invention provides a method of inducing a permanent change in the neurological development of a rodent, such as a rat, comprising daily administration of low doses of a kainate receptor agonist to the animal in the second postnatal week, wherein after treatment with the kainate receptor agonist the animal exhibits reproducible seizure-like symptoms when exposed to mild to moderate stressors. Rats treated using the above method are particularly useful as a non-human system for studying temporal lobe epilepsy, as well as for studying the efficacy of potential anti-epileptic compounds and pharmaceutical preparations.

Abstract translation: 公开了颞叶癫痫和其他癫痫相关疾病的发育动物模型。 特别地，本发明提供了诱导啮齿动物（例如大鼠）的神经发育的永久性变化的方法，其包括在第二个出生后周期内向动物中每日施用低剂量的红藻氨酸受体激动剂，其中在用 当暴露于轻度至中度的应激物时，该动物的红藻氨酸受体激动剂显示可重现的发作样症状。 使用上述方法治疗的大鼠特别可用作研究颞叶癫痫的非人系统，以及用于研究潜在的抗癫痫化合物和药物制剂的功效。

公开(公告)号：US20090036376A1

公开(公告)日：2009-02-05

申请号：US12165983

申请日：2008-07-01

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: A61K38/10 ,  A61K38/08 ,  A61K38/16 ,  A61P25/22

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：US20090012299A1

公开(公告)日：2009-01-08

申请号：US12151478

申请日：2008-05-06

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

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

IPC: C07D487/04

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, B, R1, R2, R3, R4 and R5 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A1，A2，A3，A4，B，R1，R2，R3，R4和R5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：US07435823B2

公开(公告)日：2008-10-14

申请号：US11042634

申请日：2005-01-24

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 ,  Gregory J. Habgood ,  David C. McGowan ,  Douglas A. Whittington ,  Daniel La ,  Vinod F. Patel

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 ,  Gregory J. Habgood ,  David C. McGowan ,  Douglas A. Whittington ,  Daniel La ,  Vinod F. Patel

IPC: C07D215/38 ,  C07D265/34

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：US20080221101A1

公开(公告)日：2008-09-11

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 ,  C07C211/29 ,  A61K31/137 ,  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：US20080119468A1

公开(公告)日：2008-05-22

申请号：US11899363

申请日：2007-09-04

Applicant: Andrew Tasker ,  Dawei Zhang ,  Liping H. Pettus ,  Rob M. Rzasa ,  Kelvin K.C. Sham ,  Shimin Xu ,  Partha Chakrabarti

Inventor： Andrew Tasker ,  Dawei Zhang ,  Liping H. Pettus ,  Rob M. Rzasa ,  Kelvin K.C. Sham ,  Shimin Xu ,  Partha Chakrabarti

IPC: A61K31/502 ,  C07D403/12 ,  C07D237/34 ,  C07D413/02 ,  C07D471/04 ,  A61P19/10 ,  A61P11/00 ,  A61P9/00 ,  A61P25/00 ,  A61P21/00 ,  A61P35/02 ,  A61K31/496 ,  C07D413/14 ,  A61K31/5377 ,  C07D237/30

CPC classification number: C07D403/12 ,  C07D237/30 ,  C07D237/34 ,  C07D403/10 ,  C07D413/12 ,  C07D417/10 ,  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, 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