Title:
【発明の名称】ビタミンD化合物の1α-OHをアキシアル配向にロックする方法
Document Type and Number:
Japanese Patent JP2002515481
Kind Code:
A
Abstract:
A method of modifying or altering the structure of a 1alpha-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1alpha-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1alpha-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1alpha-hydroxyl in the axial orientation.
Inventors:
Deluca, Hector Ef
Rafal Earl
Rafal Earl
Application Number:
JP2000549585A
Publication Date:
May 28, 2002
Filing Date:
March 10, 1999
Export Citation:
Assignee:
WISCONSIN ALUMNI RESEARCH FOUNDATION
International Classes:
A61K31/59; A01N43/02; A01N43/08; A01N43/16; A01N43/26; A01N43/30; A01N45/00; A61K31/335; A61P3/10; A61P5/14; A61P5/18; A61P7/00; A61P9/12; A61P11/06; A61P17/00; A61P17/06; A61P17/10; A61P17/14; A61P19/08; A61P19/10; A61P25/00; A61P29/00; A61P35/00; A61P35/02; A61P37/06; C07C401/00; C07C403/00; C07D305/00; C07D311/04; C07D321/00; C07C; (IPC1-7): C07C401/00; A61K31/59; A61P3/10; A61P5/14; A61P5/18; A61P7/00; A61P9/12; A61P11/06; A61P17/00; A61P17/06; A61P17/10; A61P17/14; A61P19/08; A61P19/10; A61P25/00; A61P29/00; A61P35/00; A61P35/02; A61P37/06
Attorney, Agent or Firm:
Kazuo Shamoto (5 outside)