公开(公告)号：US07612200B2

公开(公告)日：2009-11-03

申请号：US11295433

申请日：2005-12-07

Applicant: Enrique Luis Michelotti ,  William R. Moore, Jr. ,  Eric Bruce Springman

Inventor： Enrique Luis Michelotti ,  William R. Moore, Jr. ,  Eric Bruce Springman

IPC: C07D285/36

CPC classification number: C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention is directed to a compound having the formula wherein R1, R2, R3, R4, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The present invention is also directed to compounds that stabilize the open conformation of a protein kinase, a crystallized protein kinase in the open conformation, and uses thereof. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease.

Abstract translation: 本发明涉及具有下式的化合物：其中R1，R2，R3，R4，G和Q如本文所定义。 本发明的化合物可用作蛋白激酶的抑制剂。 本发明还涉及包含根据上式的化合物的组合物。 本发明还涉及稳定蛋白激酶，开放构象中的结晶蛋白激酶的开放构象的化合物及其用途。 本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。

公开(公告)号：US07741479B2

公开(公告)日：2010-06-22

申请号：US11295638

申请日：2005-12-07

Applicant: Enrique Luis Michelotti ,  Eric Bruce Springman ,  Duyan Nguyen ,  Rupa S. Shetty ,  Younghee Lee ,  Kristofer Kent Moffett ,  Jennifer Lee Ludington ,  Ted Tsutomis Fujimoto ,  Zenon D. Konteatis ,  Bin Liu ,  Frank Hollinger ,  Bruce D. Dorsey

Inventor： Enrique Luis Michelotti ,  Eric Bruce Springman ,  Duyan Nguyen ,  Rupa S. Shetty ,  Younghee Lee ,  Kristofer Kent Moffett ,  Jennifer Lee Ludington ,  Ted Tsutomis Fujimoto ,  Zenon D. Konteatis ,  Bin Liu ,  Frank Hollinger ,  Bruce D. Dorsey

IPC: C07D273/06

CPC classification number: C07D333/38 ,  C07D231/40 ,  C07D243/08 ,  C07D277/48 ,  C07D277/56 ,  C07D295/192 ,  C07D333/36 ,  C07D403/06 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D495/04

Abstract: The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.

Abstract translation: 本发明涉及具有下式的化合物：其中R1，R2，G和Q如本文所定义。 本发明的化合物可用作蛋白激酶如MAP激酶，特别是p38激酶的抑制剂。 本发明还涉及包含根据上式的化合物的组合物。 本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。 本发明还涉及治疗或预防蛋白激酶介导的病症的方法。

公开(公告)号：US20090192307A1

公开(公告)日：2009-07-30

申请号：US11295433

申请日：2005-12-07

Applicant: Enrique Luis Michelotti ,  William R. Moore, JR. ,  Eric Bruce Springman

Inventor： Enrique Luis Michelotti ,  William R. Moore, JR. ,  Eric Bruce Springman

IPC: C07D417/14 ,  C07D409/14

CPC classification number: C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention is directed to a compound having the formula wherein R1, R2, R3, R4, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The present invention is also directed to compounds that stabilize the open conformation of a protein kinase, a crystallized protein kinase in the open conformation, and uses thereof. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease.

Abstract translation: 本发明涉及具有下式的化合物：其中R1，R2，R3，R4，G和Q如本文所定义。 本发明的化合物可用作蛋白激酶的抑制剂。 本发明还涉及包含根据上式的化合物的组合物。 本发明还涉及稳定蛋白激酶，开放构象中的结晶蛋白激酶的开放构象的化合物及其用途。 本文所述的化合物和组合物可用于治疗和预防炎性疾病或疾病。