发明申请
US20050272801A1 Isoprenoid pathway inhibitors for stimulating cartilage growth
审中-公开
用于刺激软骨生长的异戊二醛途径抑制剂
- 专利标题: Isoprenoid pathway inhibitors for stimulating cartilage growth
- 专利标题(中): 用于刺激软骨生长的异戊二醛途径抑制剂
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申请号: US11167054申请日: 2005-06-24
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公开(公告)号: US20050272801A1公开(公告)日: 2005-12-08
- 发明人: Shirley Gasper , Robert West , Theresa Martinez , Kirk Robbins , Patricia McKernan , Nand Baindur , Virender Labroo , Gregory Mundy
- 申请人: Shirley Gasper , Robert West , Theresa Martinez , Kirk Robbins , Patricia McKernan , Nand Baindur , Virender Labroo , Gregory Mundy
- 主分类号: A23L1/30
- IPC分类号: A23L1/30 ; A61K31/00 ; A61K31/192 ; A61K31/22 ; A61K31/225 ; A61K31/366 ; A61K31/40 ; A61K31/404 ; A61K31/405 ; A61K31/4409 ; A61K31/47 ; A61K31/505 ; A61K45/06 ; A61P1/02 ; A61P3/14 ; A61P5/20 ; A61P19/08 ; A61P19/10 ; C07D207/416 ; C07D213/54 ; C07D215/14
摘要:
Compounds of the formula wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6C; Y is of the formula or a stereoisomer thereof, wherein R1 is substituted or unsubstituted alkyl; each R2 is independently H, hydroxy, alkoxy (1-6C) or lower alkyl (1-4C); R3 is H, hydroxy, or alkoxy (1-6C); or Y is of the formula wherein each n is 1, Z is N, K comprises a substituted or unsubstituted aromatic carbocyclic or heterocyclic ring system which may optionally be spaced from the linkage position shown in formula (7) by a linker of 1-2C, or in formula (7), Z may be spaced from the carbon bonded to X by ═CR6— wherein R6 is H or linear, branded or cyclic alkyl (1-6C), R5 is H or linear, branched or cyclic alkyl, and R′ represents a cation, H or a substituted or unsubstituted alkyl group of 1-6C, promote bone formation and are thus useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation. Also disclosed is a method to identify additional compounds which are inhibitors of enzymes in the isoprenoid scheme especially of HMG-CoA reductase which results in prenylation of proteins and in the synthesis of steroids or of inhibitors of their production which are useful in treating bone disorders.
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