Vitamin D3 analog useful for the treatment of osteoporosis
申请人:Bouillon Roger
公开号:US20060135491A1
公开(公告)日:2006-06-22
The present invention relates to the vitamin D
3
analog (1R,3R)-5-(E)-(2R, 5R)-2-[2-(4-hydroxy-4-methylpentyl)-spiro[4.5]dec-7-ylidene]-ethylidene}-cyclohexane-1,3-diol which is useful in the treatment of osteoporosis.
The present invention relates to 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]-decanes, compositions which comprise said 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]-decanes, and methods for treating diseases, illnesses, and the like with said 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]decanes.
The present invention relates to 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]-decanes, compositions which comprise said 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]-decanes, and methods for treating diseases, illnesses, and the like with said 7-(2-cyclohexylidene-ethylidene)-spiro[4.5]decanes.
Synthesis and biological activity of 22-oxa CD-ring modified analogues of 1α,25-dihydroxyvitamin D3: spiro[5.5]undecane CF-ring analogues
作者:Wim Schepens、Dirk Van Haver、Maurits Vandewalle、Pierre J De Clercq、Roger Bouillon、Annemieke Verstuyf
DOI:10.1016/j.bmcl.2004.05.058
日期:2004.8
The synthesis and biological activity of novel CD-ring modified analogues of 22-oxa-1alpha,25-dihydroxyvitamin D(3), lacking the D-ring and featuring a connection between C-18 and C-21 (spiro[5.5]undecane CF-ring analogues), is described. The central ring system is conveniently synthesised from an achiral intermediate. The analogues have marginal binding affinity for the nVDR and possess low to moderate