公开(公告)号：US20100173823A1

公开(公告)日：2010-07-08

申请号：US12722879

申请日：2010-03-12

Applicant: Kevin D. McCormick ,  Christopher W. Boyce ,  Neng-Yang Shih ,  Robert G. Aslanian ,  Pietro Mangiaracina ,  Manuel de Lera Ruiz ,  Younong Yu ,  Purakkattle Biju ,  Chia-Yu Huang ,  Bo Liang ,  Ruiyan Liu ,  Rong-Qiang Liu ,  Lisa Guise-Zawacki

Inventor： Kevin D. McCormick ,  Christopher W. Boyce ,  Neng-Yang Shih ,  Robert G. Aslanian ,  Pietro Mangiaracina ,  Manuel de Lera Ruiz ,  Younong Yu ,  Purakkattle Biju ,  Chia-Yu Huang ,  Bo Liang ,  Ruiyan Liu ,  Rong-Qiang Liu ,  Lisa Guise-Zawacki

IPC: A61K31/553 ,  C07D265/36 ,  A61K31/538 ,  C12N5/00 ,  C07D279/16 ,  A61K31/5415 ,  C07D241/36 ,  A61K31/498 ,  C07D267/14 ,  C07D471/04 ,  A61K31/56 ,  A61K38/02 ,  A61P11/00 ,  A61P37/08 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P13/00

CPC classification number: C07D413/06 ,  C07D403/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.

Abstract translation: 在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新一类苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。

公开(公告)号：US20090221555A1

公开(公告)日：2009-09-03

申请号：US12162851

申请日：2007-10-23

Applicant: Gulzar Ahmed ,  Adolph Bohnstedt ,  Henry Joseph Breslin ,  Jason Burke ,  Matthew A. Curry ,  James L. Diebold ,  Bruce Dorsey ,  Benjamin J. Dugan ,  Daming Feng ,  Diane E. Gingrich ,  Tao Guo ,  Koc-Kan Ho ,  Keith S. Learn ,  Joseph G. Lisko ,  Rong-qiang Liu ,  Eugen Mesaros ,  Karen Milkiewicz ,  Gregory R. Ott ,  Jonathan Parrish ,  Jay P. Theroff ,  Tho V. Thieu ,  Rabindranath Tripathy ,  Theodore L. Underiner ,  Jason C. Wagner ,  Linda Weinberg ,  Gregory J. Wells ,  Ming You ,  Craig A. Zificsak

Inventor： Gulzar Ahmed ,  Adolph Bohnstedt ,  Henry Joseph Breslin ,  Jason Burke ,  Matthew A. Curry ,  James L. Diebold ,  Bruce Dorsey ,  Benjamin J. Dugan ,  Daming Feng ,  Diane E. Gingrich ,  Tao Guo ,  Koc-Kan Ho ,  Keith S. Learn ,  Joseph G. Lisko ,  Rong-qiang Liu ,  Eugen Mesaros ,  Karen Milkiewicz ,  Gregory R. Ott ,  Jonathan Parrish ,  Jay P. Theroff ,  Tho V. Thieu ,  Rabindranath Tripathy ,  Theodore L. Underiner ,  Jason C. Wagner ,  Linda Weinberg ,  Gregory J. Wells ,  Ming You ,  Craig A. Zificsak

IPC: A61K31/55 ,  C07D239/02 ,  A61K31/505 ,  C07D403/00 ,  C07D413/14 ,  A61K31/5377 ,  C07D413/00 ,  C07D403/14

CPC classification number: C07D239/48 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.

Abstract translation: 本发明提供式I或II化合物或其药学上可接受的盐形式，其中R1，R2，R3，R4，R5，A1，A2，A3，A4和A5如本文所定义。 式I或II的化合物具有ALK和/或c-Met抑制活性，并且可用于治疗增殖性疾病。