发明名称 |
Method of locking 1 alpha -OH of vitamin D compounds in axial orientation |
摘要 |
A method of modifying or altering the structure of a 1 alpha -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 1 alpha -hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1 alpha -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 1 alpha -hydroxyl in the axial orientation.
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申请公布号 |
US6114317(A) |
申请公布日期 |
2000.09.05 |
申请号 |
US19980082776 |
申请日期 |
1998.05.21 |
申请人 |
WISCONSIN ALUMNI RESEARCH FOUNDATION |
发明人 |
DELUCA, HECTOR F.;SICINSKI, RAFAL R. |
分类号 |
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;C07C;C07C401/00;C07C403/00;C07D305/00;C07D311/04;C07D321/00;(IPC1-7):A01N45/00 |
主分类号 |
A61K31/59 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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