Title:
VITAMIN D3 ANALOG
Document Type and Number:
Japanese Patent JP2602633
Kind Code:
B2
Abstract:
PURPOSE: To provide the subject compound, a vitamin D3 analog, which has activities to stimulate differentiation and to inhibit proliferation of human keratinocytes and is useful for the treatment and so on of hyperproliferative skin diseases such as psoriasis, neoplastic diseases such as leukemia, breast cancer and sebaceous gland diseases such as acne.
CONSTITUTION: There is provided a novel compound of formula I (wherein R is H, hydroxy or F; X is H2 or =CH2; and the 23, 24 double bond is E or Z) which is effective for stimulating differentiation and inhibiting proliferation of human keratinocytes and is useful as an agent for the treatment of hyperproliferative skin diseases such as psoriasis, basal cell carcinomas, keratinization disorder, keratosis and the like, as an agent for the prevention and treatment of neoplastic diseases such as leukemia and the like, as an antineoplastic for the treatment and prevention of tumors such as breast cancer and the like and as an agent for the treatment of sebaceous gland diseases such as acne, seborrheic dermatitis or the like. This compound is obtained by treating a compound of formula II with a reducing agent in the presence of a base followed by reaction with a compound of formula III (wherein tBu is t-butyl) in the presence of n-butyl lithium and subsequent deprotection.
Inventors:
Thomas I Doran
Bernard Michael Hennessy
John Arthur MacLaine
Giacomo Pizzoreto
Farhad Sedalet
Milan Radoje Uskokovik
Bernard Michael Hennessy
John Arthur MacLaine
Giacomo Pizzoreto
Farhad Sedalet
Milan Radoje Uskokovik
Application Number:
JP28775394A
Publication Date:
April 23, 1997
Filing Date:
November 22, 1994
Export Citation:
Assignee:
F. Hoffman-La Rochille Age
International Classes:
A61K31/593; A61P17/00; A61K31/59; A61P35/00; A61P35/02; C07C401/00; (IPC1-7): C07C401/00; A61K31/59
Attorney, Agent or Firm:
Hajime Tsukuni (1 person outside)