Novel structural analogues of vitamin d

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 401/00 (2006.01) A61K 31/045 (2006.01) A61K 31/335 (2006.01) A61K 31/59 (2006.01) C07C 35/22 (2006.01) C07C 35/27 (2006.01) C07C 43/188 (2006.01) C07C 47/192 (2006.01) C07C 47/198 (2006.01) C07C 47/28 (2006.01) C07C 47/36 (2006.01) C07C 47/37 (2006.01) C07C 49/242 (2006.01) C07C 49/29 (2006.01) C07C 49/517 (2006.01) C07C 49/687 (2006.01) C07C 49/743 (2006.01) C07C 49/755 (2006.01) C07C 57/26 (2006.01) C07C 59/01 (2006.01) C07C 62/00 (2006.01) C07C 69/03 (2006.01) C07C 309/63 (2006.01) C07D 303/14 (2006

Patent

CA 2166898

The present invention relates to analogues of vitamin D, which lack the combined presence of the trans-fused six-membered C-ring and of five-membered D-ring, but still possess a central part consisting of a subsituted chain of five atoms, atoms which correspond to positions 8, 14, 13 17 and 20 of vitamin D, and at the ends of which are connected, at position 20 a structural moiety representing part of the side chain of vitamin D or of an analogue of vitamin D, and at position 8 the .DELTA.(5,7)-diene moiety connected to the A-ring of the active 1-alpha-hydroxy metabolite or of an established vitamin D analogue, to their preparation process, to preparation intermediates, to pharmaceutical preparations comprising these compounds and to their use in medicine.

La présente invention se rapporte à des analogues de la vitamine D auxquels manque la présence combinée du noyau C hexagonal trans-condensé et du noyau D penthagonal, mais qui possède toujours une partie centrale se composant d'une chaîne substituée de 5 atomes, atomes qui correspondent aux positions 8, 14, 13, 17 et 20 de la vitamine D, et aux extrémités desquelles sont raccordées, à la position 20, une fraction structurale représentant une partie de la chaîne latérale de la vitamine D ou d'un analogue de celle-ci, et à la position 8, la fraction DELTA (5,7)-diène raccordée au noyau A du métabolite actif 1-alpha-hydroxy ou d'un analogue établi de la vitamine D. L'invention se rapporte également à leur procédé de préparation, aux intermédiaires de préparation, aux préparations pharmaceutiques comprenant ces composés et à leur utilisation en médecine.

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