Title:
FLUORINATED VITAMIN D3 DERIVATIVE
Document Type and Number:
Japanese Patent JP2659345
Kind Code:
B2
Abstract:
PURPOSE: To provide a fluorinated vitamin D3 derivative which inhibits the proliferation of human sebaceous gland cells useful as an agent for the treatment of acne.
CONSTITUTION: A desired fluorinated vitamin D3 is 1α-fluoro-25-hydroxy-16- ene-23-yne-cholecalciferol represented by formula I. The compound of formula I can be obtained by reacting the compound of formula II with the compound of formula III at -90°C--60°C, suitably at -75°C in an aprotic polar organic solvent in the presence of a strong base and removing the protective group from the resulting compound of the formula IV. In the treatment of sebaceous gland diseases the compound of formula I can be locally administered to the human in a dose of 0.01-100 μg per gram of the prescription for local administration daily and also it can be orally administered in a close of 0.01-10 μg daily.
Inventors:
TOOMASU AI DOORAN
SHANNJAN SHUEI
MIRAN RADOOJE USUKOKOITSUKU
SHANNJAN SHUEI
MIRAN RADOOJE USUKOKOITSUKU
Application Number:
JP4542095A
Publication Date:
September 30, 1997
Filing Date:
March 06, 1995
Export Citation:
Assignee:
EFU HOFUMAN RA ROSHU AG
International Classes:
A61K31/593; A61P3/02; A61P17/00; A61K31/59; A61P17/06; A61P17/08; A61P17/10; C07C401/00; (IPC1-7): A61K31/59; A61K31/59
Domestic Patent References:
| JP6500089Y | ||||
| JPH0640975A |
Other References:
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Attorney, Agent or Firm:
津国 肇 （外１名）