公开(公告)号：US07521589B2

公开(公告)日：2009-04-21

申请号：US11400572

申请日：2006-04-06

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

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

IPC: A01K67/00 ,  A01K67/033

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.

公开(公告)号：US07514564B2

公开(公告)日：2009-04-07

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

IPC: C07D211/94 ,  C07D211/98 ,  A61K31/44

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.

Abstract translation: 选择的胺对于预防和治疗疾病如血管生成介导的疾病是有效的。 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：US20080227779A1

公开(公告)日：2008-09-18

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: A61K31/5377 ,  A61K31/506 ,  C07D413/14 ,  A61P35/00 ,  C07D413/12

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R 1-5，X，Y和Z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：US07320992B2

公开(公告)日：2008-01-22

申请号：US10926238

申请日：2004-08-24

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

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

IPC: A61K31/4439 ,  C07D401/12

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：US07307088B2

公开(公告)日：2007-12-11

申请号：US10615809

申请日：2003-07-08

Applicant: Qi Huang ,  Guoqing Chen ,  Aiwen Li ,  Babak Riahi ,  Andrew Tasker ,  Kevin Yang ,  Chester Chenguang Yuan

Inventor： Qi Huang ,  Guoqing Chen ,  Aiwen Li ,  Babak Riahi ,  Andrew Tasker ,  Kevin Yang ,  Chester Chenguang Yuan

IPC: A61K31/4709 ,  A61K31/4725 ,  A61K31/404 ,  A61K31/357 ,  C07D217/04 ,  C07D215/38 ,  C07D209/08 ,  C07D319/18

CPC classification number: C07D401/12 ,  C07D209/20 ,  C07D213/36 ,  C07D215/12 ,  C07D217/02 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D471/12 ,  C07D487/04

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 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：US20070185324A1

公开(公告)日：2007-08-09

申请号：US11643261

申请日：2006-12-20

Applicant: Frenel De Morin ,  Jian Chen ,  Elizabeth Doherty ,  Stephen Hitchcock ,  Qi Huang ,  Joseph Kim ,  Gang Liu ,  Thomas Nixey ,  Nick Paras ,  Jeffrey Petkus ,  Daniel Retz ,  Adrian Smith ,  Andrew Tasker ,  Jiawang Zhu

Inventor： Frenel De Morin ,  Jian Chen ,  Elizabeth Doherty ,  Stephen Hitchcock ,  Qi Huang ,  Joseph Kim ,  Gang Liu ,  Thomas Nixey ,  Nick Paras ,  Jeffrey Petkus ,  Daniel Retz ,  Adrian Smith ,  Andrew Tasker ,  Jiawang Zhu

IPC: A61K31/541 ,  A61K31/5377 ,  C07D417/02 ,  C07D403/02

CPC classification number: C07D401/14 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z′, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase 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Raf激酶的新一类化合物，因此可用于治疗Raf激酶介导的疾病，包括黑素瘤，肿瘤和其它癌症相关病症。 这些化合物具有通式I，其中R 1是和A 1，A 2，A 3，A 3， X，Z，Z'，R 1，R 2，R 3，R 3， 本文定义了R 5，R 5和R 6。 本发明还包括药物组合物，用于治疗Raf激酶介导的疾病的方法，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：US20070054916A1

公开(公告)日：2007-03-08

申请号：US11240590

申请日：2005-09-30

Applicant: Vinod Patel ,  Joseph Kim ,  Stephanie Geuns-Meyer ,  Stuart Chaffee ,  Victor Cee ,  Brian Hodous ,  Steven Bellon ,  Jean-Christophe Harmange ,  Philip Olivieri ,  Maya Thaman ,  Erin DiMauro ,  John Buchanan ,  David McGowan ,  Brian Albrecht ,  Holly Deak ,  Jean Bemis ,  Ryan White ,  Matthew Martin ,  Gregory Habgood ,  Paul Tempest ,  Craig Masse ,  William Buckner ,  Bradley Herberich ,  Russell Graceffa ,  Dawei Zhang ,  Shimin Xu ,  Kelvin Sham ,  Robert Rzasa ,  James Falsey ,  Partha Chakrabarti ,  Guo-Qiang Cao ,  Susan Tomlinson ,  Liping Pettus ,  Adrian Smith ,  Nick Paras ,  Gang Liu ,  Frenel DeMorin ,  Andrew Tasker ,  Anthony Reed

Inventor： Vinod Patel ,  Joseph Kim ,  Stephanie Geuns-Meyer ,  Stuart Chaffee ,  Victor Cee ,  Brian Hodous ,  Steven Bellon ,  Jean-Christophe Harmange ,  Philip Olivieri ,  Maya Thaman ,  Erin DiMauro ,  John Buchanan ,  David McGowan ,  Brian Albrecht ,  Holly Deak ,  Jean Bemis ,  Ryan White ,  Matthew Martin ,  Gregory Habgood ,  Paul Tempest ,  Craig Masse ,  William Buckner ,  Bradley Herberich ,  Russell Graceffa ,  Dawei Zhang ,  Shimin Xu ,  Kelvin Sham ,  Robert Rzasa ,  James Falsey ,  Partha Chakrabarti ,  Guo-Qiang Cao ,  Susan Tomlinson ,  Liping Pettus ,  Adrian Smith ,  Nick Paras ,  Gang Liu ,  Frenel DeMorin ,  Andrew Tasker ,  Anthony Reed

IPC: A61K31/525 ,  A61K31/519 ,  A61K31/517

CPC classification number: C07D215/38 ,  C07C205/37 ,  C07D215/12 ,  C07D217/12 ,  C07D217/22 ,  C07D217/26 ,  C07D239/26 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  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, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.

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，癌症和相关病症的化合物。 化合物具有通式I，其中A 1，A 2，A 3，B，R 1， R 2，R 3和R 4在本文中定义。 因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，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：US20070054903A1

公开(公告)日：2007-03-08

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 Fellows ,  Julie Germain ,  Timothy Harvey ,  Joseph Kim ,  Matthew Lee ,  Longbin Liu ,  Vinod Patel ,  Andrew Tasker

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

IPC: A61K31/538 ,  A61K31/5377 ,  A61K31/4709 ,  C07D403/02 ,  C07D413/02

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：US07101868B2

公开(公告)日：2006-09-05

申请号：US10823809

申请日：2004-04-12

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

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

IPC: A61K31/33 ,  A61K31/44 ,  C07D211/62 ,  C07D213/72

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.

公开(公告)号：US08642624B2

公开(公告)日：2014-02-04

申请号：US13297213

申请日：2011-11-15

Applicant: Guoqing Chen ,  Jeffrey A. Adams ,  Jean E. Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian V. DiPietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael K. Handley ,  Qi Huang ,  Joseph L. Kim ,  Tae-Seong Kim ,  Alexander S. Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian M. Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael D. Croghan

Inventor： Guoqing Chen ,  Jeffrey A. Adams ,  Jean E. Bemis ,  Shon Booker ,  Guolin Cai ,  Lucian V. DiPietro ,  Celia Dominguez ,  Daniel Elbaum ,  Julie Germain ,  Stephanie Geuns-Meyer ,  Michael K. Handley ,  Qi Huang ,  Joseph L. Kim ,  Tae-Seong Kim ,  Alexander S. Kiselyov ,  Xiaohu Ouyang ,  Vinod F. Patel ,  Leon M. Smith ,  Markian M. Stec ,  Andrew Tasker ,  Ning Xi ,  Shimin Xu ,  Chester Chenguang Yuan ,  Michael D. Croghan

IPC: A01N43/40 ,  A61K31/44 ,  A01N43/38 ,  A61K31/40 ,  A61K31/405

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.

Abstract translation: 所选择的杂环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。