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Title:
2-アルキリデン-19-ノル-ビタミンD化合物及びその治療的使用
Document Type and Number:
Japanese Patent JP4022071
Kind Code:
B2
Abstract:
This invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula: where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 and R8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group -(CH2)X- where X is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by relatively high intestinal calcium transport activity and relatively high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.

Inventors:
Deluca, Hector Ef
Rafal Earl
Application Number:
JP2001572461A
Publication Date:
December 12, 2007
Filing Date:
March 29, 2001
Export Citation:
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Assignee:
WISCONSIN ALUMNI RESEARCH FOUNDATION
International Classes:
C07C401/00; A61K31/593; A61P1/00; A61P3/02; A61P3/10; A61P3/14; A61P5/18; A61P7/00; A61P9/10; A61P9/12; A61P13/08; A61P15/00; A61P17/00; A61P17/06; A61P17/14; A61P19/00; A61P19/02; A61P19/10; A61P25/00; A61P29/00; A61P35/00; A61P35/02; A61P37/06; C07F7/18
Domestic Patent References:
JP6321894A
JP61267549A
Foreign References:
WO1998041500A1
WO1998041501A1
Attorney, Agent or Firm:
Kazuo Shamoto
Tadashi Masui
Yasushi Kobayashi
Akio Chiba
Hiroyuki Tomita
Reiko Izumiya