C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 401/00 (2006.01) A01N 43/02 (2006.01) A01N 43/08 (2006.01) A01N 43/16 (2006.01) A01N 43/26 (2006.01) A01N 43/30 (2006.01) A01N 45/00 (2006.01) A61K 31/59 (2006.01) A61P 3/10 (2006.01) A61P 5/14 (2006.01) A61P 5/18 (2006.01) A61P 7/00 (2006.01) A61P 9/12 (2006.01) A61P 11/06 (2006.01) A61P 17/00 (2006.01) A61P 17/06 (2006.01) A61P 17/10 (2006.01) A61P 17/14 (2006.01) A61P 19/08 (2006.01) A61P 19/10 (2006.01) A61P 25/00 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 35/02 (2006.01) A61P 37/06 (
Patent
CA 2333103
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 oriented 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.
L'invention concerne un procédé de modification ou d'altération de la structure du composé de vitamine D 1.alpha.-hydrolysé de manière à augmenter son activité biologique par altération de l'équilibre de la forme du cycle A afin de lui faire adopter une forme en chaise présentant le 1.alpha.-hydroxyle en orientation axiale. Pour ce faire, on bloque la forme en chaise du cycle A selon une géométrie présentant un 1.alpha.-hydroxyle orienté axialement ou on ajoute un ou plusieurs substituants au cycle A qui interagissent avec d'autres substituants dans la molécule ou sur le cycle A de manière à exercer une force motrice sur le cycle A pour qu'il adopte la forme en chaise à 1.alpha.-hydroxyle axialement orienté.
Deluca Hector F.
Sicinski Rafal R.
Borden Ladner Gervais Llp
Wisconsin Alumni Research Foundation
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