公开(公告)号：US20140179711A1

公开(公告)日：2014-06-26

申请号：US14191620

申请日：2014-02-27

Applicant: Bristol-Myers Squibb Company

Inventor： Jean Lajeunesse ,  John D. DiMarco ,  Michael Galella ,  Ramakrishnan Chidambaram

IPC: C07D403/12

CPC classification number: C07D403/12 ,  C07D277/56 ,  C07D417/12

Abstract: The invention relates to processes for preparing compounds having the formula, and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.

Abstract translation: 本发明涉及制备具有下式的化合物及其结晶形式的方法，其中Ar为芳基或杂芳基，L为任选的亚烷基连接基，R2，R3，R4和R5如本说明书中所定义， 化合物可用作激酶抑制剂，特别是蛋白酪氨酸激酶和p38激酶的抑制剂。

公开(公告)号：US20140121155A1

公开(公告)日：2014-05-01

申请号：US14142081

申请日：2013-12-27

Applicant: Bristol-Myers Squibb Company

Inventor： Jack Z. Gougoutas ,  Mary F. Malley ,  John D. DiMarco ,  Xiaotian S. Yin ,  Chenkou Wei ,  Jurong Yu ,  Truc Chi Vu ,  Gregory Scott Jones ,  Scott A. Savage

IPC: C07D209/52 ,  A61K45/06 ,  A61K31/403

CPC classification number: C07D209/52 ,  A61K31/403 ,  A61K45/06 ,  A61K2300/00

Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.

Abstract translation: 提供式I化合物的物理晶体结构：包括其游离碱一水合物（形式H-1）及其盐酸盐，包括含有0.75当量H 2 O（H0.75-3）的盐酸盐和 含有2当量H 2 O（形式H2-1）的盐酸盐和盐酸盐图案P-5，优选基本上纯的形式，以及本文所述的其它形式，含有化合物I或IA的结构的药物组合物，制备方法 相同的，用于制备其的中间体，以及使用这种结构治疗疾病如糖尿病的方法。

公开(公告)号：US20130303467A1

公开(公告)日：2013-11-14

申请号：US13938763

申请日：2013-07-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jack Z. Gougoutas ,  Hildegard Lobinger ,  Srividya Ramakrishnan ,  Prashant P. Deshpande ,  Jeffrey T. Bien ,  Chiajen Lai ,  Chenchi Wang ,  Peter Riebel ,  John Anthony Grosso ,  Alexandra A. Nirschl ,  Janak Singh ,  John D. DiMarco

IPC: C07H15/207 ,  A61K45/06 ,  A61K31/7034

CPC classification number: C07H15/207 ,  A61K31/7034 ,  A61K45/06 ,  A61P3/10 ,  C07H7/04

Abstract: The present invention relates to physical crystal structures of a compound of the formula I: wherein R1, R2, R2a, R3 and R4 are as defined herein, especially pharmaceutical compositions containing structures of compound I or II, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.

Abstract translation: 本发明涉及式I化合物的物理结晶结构：其中R1，R2，R2a，R3和R4如本文所定义，特别是含有化合物I或II结构的药物组合物，其制备方法， 制备方法以及使用这种结构治疗糖尿病等疾病的方法。