公开(公告)号：US07354944B2

公开(公告)日：2008-04-08

申请号：US11251846

申请日：2005-10-18

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

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

IPC: A61K31/433 ,  A61K31/4725 ,  A61K31/416 ,  A61K31/4162 ,  C07D285/135 ,  C07D217/02 ,  C07D405/04 ,  C07D417/04 ,  C07D217/00

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。

公开(公告)号：US20080032973A1

公开(公告)日：2008-02-07

申请号：US11879243

申请日：2007-07-16

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

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

IPC: C07D239/80 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P19/00 ,  C07D413/14 ,  C07D471/04 ,  C07D413/02 ,  A61P3/00 ,  A61P31/12 ,  A61P7/00

CPC classification number: C07D471/04 ,  C07D239/82

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, 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 kinase 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，s，T，R 1，R 2， / SUP>，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激酶介导的疾病，以及可用于制备 式Ⅰ的化合物。

公开(公告)号：US20070173506A1

公开(公告)日：2007-07-26

申请号：US11652728

申请日：2007-01-11

Applicant: Qingping Zeng ,  John Allen ,  Matthew Bourbeau ,  Celia Dominguez ,  Christopher Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew Lee ,  Aiwen Li ,  Qingyian Liu ,  James Rider ,  Seifu Tadesse ,  Andrew Tasker ,  Vellarkad Viswanadhan ,  Xianghong Wang ,  Kurt Weiler ,  George Wohlhieter ,  Guomin Yao ,  Chester Yuan

Inventor： Qingping Zeng ,  John Allen ,  Matthew Bourbeau ,  Celia Dominguez ,  Christopher Fotsch ,  Nianhe Han ,  Fang-Tsao Hong ,  Xin Huang ,  Matthew Lee ,  Aiwen Li ,  Qingyian Liu ,  James Rider ,  Seifu Tadesse ,  Andrew Tasker ,  Vellarkad Viswanadhan ,  Xianghong Wang ,  Kurt Weiler ,  George Wohlhieter ,  Guomin Yao ,  Chester Yuan

IPC: A61K31/502 ,  A61K31/4745 ,  A61K31/4709 ,  A61K31/427 ,  C07D417/02

CPC classification number: C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04

Abstract: The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Abstract translation: 本发明涉及式I和式II的噻唑化合物及其用于治疗由蛋白激酶B（PKB）介导的疾病的组合物，其中变量具有本文提供的定义。 本发明还涉及这种噻唑化合物及其组合物治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病的治疗用途。

公开(公告)号：US20060252777A1

公开(公告)日：2006-11-09

申请号：US11289659

申请日：2005-11-29

Applicant: Tae-Seong Kim ,  Steven Bellon ,  Shon Booker ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid Fellows ,  Matthew Lee ,  Longbin Liu ,  Elizabeth Rainbeau ,  Aaron Siegmund ,  Andrew Tasker ,  Ning Xi ,  Yuan Cheng

Inventor： Tae-Seong Kim ,  Steven Bellon ,  Shon Booker ,  Noel D'Angelo ,  Celia Dominguez ,  Ingrid Fellows ,  Matthew Lee ,  Longbin Liu ,  Elizabeth Rainbeau ,  Aaron Siegmund ,  Andrew Tasker ,  Ning Xi ,  Yuan Cheng

IPC: A61K31/519 ,  A61K31/517 ,  A61K31/513 ,  A61K31/4709 ,  A61K31/4745 ,  C07D403/04 ,  C07D487/02 ,  C07D471/02

CPC classification number: C07D401/14 ,  C07D215/233 ,  C07D401/12 ,  C07D409/14 ,  C07D413/12

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：US20060194848A1

公开(公告)日：2006-08-31

申请号：US11417329

申请日：2006-05-02

Applicant: Guoqing Chen ,  Jeffrey Adams ,  Jean Bemis ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Qi Huang ,  Joseph Kim ,  Xiaohu Ouyang ,  Vinod Patel ,  Leon Smith ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Yuan ,  Michael Croghan ,  Tae-Seong Kim

Inventor： Guoqing Chen ,  Jeffrey Adams ,  Jean Bemis ,  Lucian Di Pietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Qi Huang ,  Joseph Kim ,  Xiaohu Ouyang ,  Vinod Patel ,  Leon Smith ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Yuan ,  Michael Croghan ,  Tae-Seong Kim

IPC: A61K31/44 ,  A61K31/40

CPC classification number: C07D401/14 ,  A61K31/00 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  Y02A50/401

Abstract: Selected amines 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.

公开(公告)号：US06995162B2

公开(公告)日：2006-02-07

申请号：US10046681

申请日：2002-01-10

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 L. Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang 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 L. Kim ,  Tae-Seong Kim ,  Alexander Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael Croghan

IPC: A61K31/435 ,  C07D213/82

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：US20050124695A1

公开(公告)日：2005-06-09

申请号：US10728357

申请日：2003-12-04

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

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

IPC: A01K67/027 ,  A01N37/12 ,  A61K31/198 ,  A61K31/40 ,  A61K49/00 ,  C12Q1/00

CPC classification number: A61K49/0008 ,  A61K31/198

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。