Title:
1-ACYLOXYVITAMIN D DERIVATIVE
Document Type and Number:
Japanese Patent JP3182215
Kind Code:
B2
Abstract:
PURPOSE: To provide a new compound useful for preventing or curing osteoporosis, curing dermatic ulcer, and as an antineoplastic agent.
CONSTITUTION: The compound of formula I [X is H or acyl derived from vitamin A acid; Y is acyl derived from vitamin A acid; R is a group of formula II (R1 and R2 are each H or combined into C=C double bond; R3 is H, 1-4C alkyl or OX; R4 is H or OH)], e.g. 1α-hydroxycholecalcipherol vitamin A acid (whole trans-type)ester. The compound of the formula I can be obtained by the following process: the OH group of a 1-acetoxyvitamin D compound of formula III [R' is of formula IV (R3' is H, 1-4C alkyl or O-Ac; Ac is acetyl; R4' is H or O-Ac)] is protected followed by deacetylation and then esterification with vitamin A acid followed by elimination of the protecting group for the OH group. The present compound can be made into a pharmaceutical preparation in the form of powder, tablets, capsules, granules, injection, suppository, or ointment, its dose being 0.1-100μg/adult/day.
Inventors:
Yoji Tachibana
Application Number:
JP16904992A
Publication Date:
July 03, 2001
Filing Date:
June 26, 1992
Export Citation:
Assignee:
NISSHIN FLOUR MILLING CO.,LTD.
International Classes:
A61K31/59; A61P17/00; A61P19/10; A61P35/00; A61P43/00; C07C401/00; (IPC1-7): C07C401/00
Other References:
【文献】特許3108474(JP,B2)
Attorney, Agent or Firm:
Chika Takagi (2 outside)