发明授权
US07381737B2 Crystalline forms and process for preparing spiro-hydantoin compounds
有权
结晶形式和制备螺 - 乙内酰脲化合物的方法
- 专利标题: Crystalline forms and process for preparing spiro-hydantoin compounds
- 专利标题(中): 结晶形式和制备螺 - 乙内酰脲化合物的方法
-
申请号: US11238427申请日: 2005-09-29
-
公开(公告)号: US07381737B2公开(公告)日: 2008-06-03
- 发明人: Albert J. DelMonte , T. G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
- 申请人: Albert J. DelMonte , T. G. Murali Dhar , Yu Fan , Jack Z. Gougoutas , Mary F. Malley , Douglas D. McLeod , Robert E. Waltermire , Chenkou Wei
- 申请人地址: US NJ Princeton
- 专利权人: Bristol-Myers Squibb Company
- 当前专利权人: Bristol-Myers Squibb Company
- 当前专利权人地址: US NJ Princeton
- 代理机构: Lucas & Mercanti, LLP
- 主分类号: A61K31/4188
- IPC分类号: A61K31/4188 ; C07D235/00
摘要:
A process is provided for preparing spiro-hydantoin compounds of the formula II wherein Z is N or CR4b; K and L are independently O or S; Ar is an optionally substituted aryl or heteroaryl; A2 is a linker, G′ is a linker; Q is a linker; and R2, R4a, R4c, and Rh are defined in the specification. The process optionally includes the enantiomeric separation of intermediates to allow preparation of enantiomers of the spiro-hydantoin compounds of formula II. Substituted spiro-hydantoin compounds may be prepared from the spiro-hydantoin compounds of formula II. The spiro-hydantoin compound of formula II and the substituted spiro-hydantoin compounds are useful in the treatment of immune or inflammatory diseases. Also, provided are products made by the instant inventive process and crystalline forms (prepared by any process) of the substituted spiro-hydantoin compound, 5-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-ylmethyl]-thiophene-3-carboxylic acid, including solvates and salts thereof, as well as methods of use thereof. Crystalline forms of certain intermediates are provided.