公开(公告)号：US20130018033A1

公开(公告)日：2013-01-17

申请号：US13393116

申请日：2010-08-27

Applicant: Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Wendy Lee ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Guiling Zhao ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

Inventor： Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Wendy Lee ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Guiling Zhao ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

IPC: A61K31/517 ,  C07D471/04 ,  A61K31/519 ,  C07D405/12 ,  A61P35/02 ,  C07D401/12 ,  C07D413/12 ,  A61K31/5377 ,  C07D239/72 ,  A61P35/00 ,  C07D239/94 ,  C07D403/12

CPC classification number: C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20110092479A1

公开(公告)日：2011-04-21

申请号：US12920050

申请日：2009-02-27

Applicant: Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A61K31/437 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/496 ,  A61P35/00 ,  A61P35/02 ,  A61P13/12

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20220162193A1

公开(公告)日：2022-05-26

申请号：US17598389

申请日：2020-04-06

Applicant: Michelle Ann ESTRADA ,  Jonas GRINA ,  Paul WEHN ,  Rui XU ,  Peloton Therapeutics, Inc.

Inventor： Michelle Ann Estrada ,  Jonas Grina ,  Paul Wehn ,  Rui Xu

IPC: C07D403/12 ,  C07D405/14 ,  A61P35/00

Abstract: Compounds of formula I, that induce RBM39 protein degradation, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with RBM39 protein activity are described herein.

公开(公告)号：US20110110889A1

公开(公告)日：2011-05-12

申请号：US12920045

申请日：2009-02-27

Applicant: Kateri A. Ahrendt et al. ,  Alexander J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt et al. ,  Alexander J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A61K38/21 ,  C07D471/04 ,  C07D401/10 ,  C07D401/02 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/497 ,  A61K39/395 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式（I）的化合物可用于抑制Raf激酶。 公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US07566716B2

公开(公告)日：2009-07-28

申请号：US11436353

申请日：2006-05-18

Applicant: Ellen Laird ,  George Topalov ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse

Inventor： Ellen Laird ,  George Topalov ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse

IPC: A61K31/497

CPC classification number: C07D487/04

Abstract: Compounds of Formula I are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using compounds of Formula I, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I的化合物可用于抑制Raf激酶和用于治疗由此介导的病症。 公开了使用式I化合物及其立体异构体，互变异构体，溶剂合物及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US08394795B2

公开(公告)日：2013-03-12

申请号：US12920050

申请日：2009-02-27

Applicant: Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven Mark Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jason De Meese ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  Paul Lunghofer ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Jeongbeob Seo ,  Hongqi Tian ,  Steven Mark Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A61K31/535 ,  A61K31/44 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I化合物可用于抑制Raf激酶。 公开了使用式I化合物和立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US08338452B2

公开(公告)日：2012-12-25

申请号：US12920045

申请日：2009-02-27

Applicant: Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

Inventor： Kateri A. Ahrendt ,  Alexandre J. Buckmelter ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen R. Laird ,  David Moreno ,  Brad Newhouse ,  Li Ren ,  Steven M. Wenglowsky ,  Bainian Feng ,  Janet Gunzner ,  Kim Malesky ,  Simon Mathieu ,  Joachim Rudolph ,  Zhaoyang Wen ,  Wendy B. Young

IPC: A01N43/42 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02

CPC classification number: C07D471/04 ,  C07C311/08

Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式（I）的化合物可用于抑制Raf激酶。 公开了使用式（I）化合物及其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20120157439A1

公开(公告)日：2012-06-21

申请号：US13393163

申请日：2010-08-27

Applicant: Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Simon Mathieu ,  Rebecca Pulk ,  Joachim Rudolph ,  Zhaoyang Wen ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

Inventor： Ignacio Aliagas ,  Stefan Gradl ,  Janet Gunzner ,  Simon Mathieu ,  Rebecca Pulk ,  Joachim Rudolph ,  Zhaoyang Wen ,  Jonas Grina ,  Joshua D. Hansen ,  Ellen Laird ,  David Moreno ,  Li Ren ,  Steven Mark Wenglowsky

IPC: A61K31/519 ,  C07D495/04 ,  A61P35/00 ,  A61K31/5377 ,  A61K31/53 ,  C07D487/04 ,  C07D513/04

CPC classification number: C07D487/04 ,  C07D495/04 ,  C07D513/04

Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式I化合物可用于抑制Raf激酶。 公开了使用式I化合物和其立体异构体，互变异构体，前药和其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20090176809A1

公开(公告)日：2009-07-09

申请号：US12347412

申请日：2008-12-31

Applicant: Ellen Laird ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse ,  Alan Olivero ,  George Topalov

Inventor： Ellen Laird ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse ,  Alan Olivero ,  George Topalov

IPC: A61K31/4439 ,  C07D401/04 ,  C07D401/14 ,  C07D487/04 ,  A61K31/4545 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D405/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/02 ,  C07D487/04

Abstract: Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式Ia和Ib的吡唑基化合物可用于抑制Raf激酶和用于治疗由此介导的病症。 公开了使用吡唑基化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞中的这种疾病或相关病理状况的方法。

公开(公告)号：US07491829B2

公开(公告)日：2009-02-17

申请号：US11345828

申请日：2006-02-02

Applicant: Ellen Laird ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse ,  Alan Olivero ,  George Topalov

Inventor： Ellen Laird ,  Joseph P. Lyssikatos ,  Mike Welch ,  Jonas Grina ,  Josh Hansen ,  Brad Newhouse ,  Alan Olivero ,  George Topalov

IPC: C07D231/14 ,  A61K31/4155 ,  A61K31/416

CPC classification number: C07D405/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/02 ,  C07D487/04

Abstract: Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Abstract translation: 式Ia和Ib的吡唑基化合物可用于抑制Raf激酶和用于治疗由此介导的病症。 公开了使用吡唑基化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞中的这种疾病或相关病理状况的方法。