24-homo vitamin D derivatives, process for their production and pharmaceutical preparations obtained therefrom
First Claim
1. A 24-homo vitamin D derivative of formula I ##STR10## in which R1 is hydrogen, hydroxy, alkanoyloxy of 1 to 8 carbon atoms or benzoyloxy,R2 and R3, independently of one another, each is alkyl of 1 to 4 carbon atoms, or trifluoromethyl or together form a saturated carbocyclic ring of 3 to 9 carbon atoms formed with carbon atom 25,R4 and R5, independently of one another, each is hydrogen, alkanoyl of 1 to 8 carbon atoms or benzoyl,A and B each are hydrogen or together form a second bond, andn is 1, 2, 3,4 or 5.
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Abstract
New 24-homo vitamin D derivatives of formula I ##STR1## are described, in which R1 means a hydrogen atom, a hydroxy, an alkanoyloxy group with 1 to 8 carbon atoms or an aralkanoyloxy group with up to 8 carbon atoms,
R2 and R3, independently of one another, mean a linear or branched alkyl group with 1 to 4 carbon atoms, a trifluoromethyl group or together mean a saturated carbocyclic ring with 3 to 9 carbon atoms formed with carbon atom 25,
R4 and R5, independently of one another, mean a hydrogen atom, an alkanoyl group with 1 to 8 carbon atoms or an aralkanoyl group with up to 8 carbon atoms, and
A and B each mean a hydrogen or together a second bond, and
n stands for 1, 2, 3,4 or 5.
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Citations
16 Claims
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1. A 24-homo vitamin D derivative of formula I ##STR10## in which R1 is hydrogen, hydroxy, alkanoyloxy of 1 to 8 carbon atoms or benzoyloxy,
R2 and R3, independently of one another, each is alkyl of 1 to 4 carbon atoms, or trifluoromethyl or together form a saturated carbocyclic ring of 3 to 9 carbon atoms formed with carbon atom 25, R4 and R5, independently of one another, each is hydrogen, alkanoyl of 1 to 8 carbon atoms or benzoyl, A and B each are hydrogen or together form a second bond, and n is 1, 2, 3,4 or 5.
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7. A 24-homo-vitamin D derivative of formula I ##STR11## in which R1 is hydroxy,
R2 and R3 each are methyl, ethyl, or together form a cyclopropyl, cyclopentyl, or cyclohexyl ring with carbon atom 25, R4 and R5 each are a hydrogen atom, A and B together each are hydrogen or together stand for a second bond and n is 1, 2 or 3.
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11. A compound selected from the group consisting of:
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(5Z,7E,22E)-(1S,3R,24S)-24-cyclopropylmethyl-9,10-secochola-5,7,10(19),22-tetraene-1,3,24-triol; (5Z,7E,22E)-(1S,3R24S)-24-isoamyl-9,10-secochola-5,7,10(19),22-tetraene-1,3,24-triol; (5Z,7E,22E)-(1S,3R,24S)-24-cyclopentylmethyl-9,10,-secochola-5,7,10(19),22-tetraene-1,3,24-triol; (5Z,7E,22E)-(1S,3R,24S)-24-(2-ethylbutyl)-9,10-secochola-5,7,10(19),22-tetraene-1,3,24-triol; and (5Z,7E,22E)-(1S,3R,24R)-24-(2-ethylbutyl)-9,10-secochola-5,7,10(19),22-tetraene-1,3,24-triol. - View Dependent Claims (12)
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Specification