发明申请
US20050209217A1 3-Mercaptopyrrolidines as farnesyl protein transferase inhibitors
审中-公开
3-巯基吡咯烷酮作为法呢基蛋白转移酶抑制剂
- 专利标题: 3-Mercaptopyrrolidines as farnesyl protein transferase inhibitors
- 专利标题(中): 3-巯基吡咯烷酮作为法呢基蛋白转移酶抑制剂
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申请号: US11124278申请日: 2005-05-09
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公开(公告)号: US20050209217A1公开(公告)日: 2005-09-22
- 发明人: Francis Boyle , James Wardleworth
- 申请人: Francis Boyle , James Wardleworth
- 优先权: GB9617302.6 19960817; GB9701417.9 19970124
- 主分类号: A61K31/40
- IPC分类号: A61K31/40 ; A61K31/427 ; A61K31/4439 ; A61K31/496 ; A61P25/00 ; A61P35/00 ; A61P43/00 ; C07D207/12 ; C07D401/12 ; C07D403/06 ; C07D403/12 ; C07D417/12 ; A61K31/551 ; C07D43/02
摘要:
The present invention relats to inhibitors of ras farnesylation of Formula (I) wherein: R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CH2—NH— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S— dimer thereof when R2=H; or a N-oxide or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.
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