Vitamin D amide derivatives
First Claim
1. A compound of the formula (I) ##STR10## where R1 and R2, which may be the same or different, each represent a hydrogen atom or an aliphatic, cycloaliphatic, araliphatic or aryl group or together with the nitrogen atom to which they are attached form a heterocyclic group;
- R3 represents a methyl group having α
- or β
-configuration;
X represents a valence bond or a C1-2 alkylene group;
Y represents --O--, --S--, --CH2 -- or --NR-- where R is a hydrogen atom or an organic group;
Z represents a valence bond or a C1-3 alkylene group; and
A═
represents a cyclohexylidene moiety characteristic of the A-ring of a 1α
-hydroxylated vitamin D or analogue thereof, with the proviso that when --X--Y--Z-- together represent an alkylene group containing up to 4 carbon atoms A═
does not carry an exocyclic methylene group at the 10-position.
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Accused Products
Abstract
The invention relates to novel 1α-hydroxy vitamin D derivatives and their 20-epi analogues, comprising compounds of general formula (I) ##STR1## where R1 and R2, which may be the same or different, each represents a hydrogen atom or an aliphatic, cycloaliphatic, araliphatic or aryl group or together with the nitrogen atom to which they are attached form a heterocyclic group; R3 represents a methyl group having α- or β-configuration; X represents a valence bond or a C1-2 alkylene group; Y represents --O--, --S--, --CH2 -- or --NR-- where R is a hydrogen atom or an organic group; Z represents a valence bond or a C1-3 alkylene group; and A═ represents a cyclohexylidene moiety characteristic of the A-ring of a 1α-hydroxylated vitamin D or analogue thereof, with the proviso that when --X--Y--Z-- together represent an alkylene group containing up to 4 carbon atoms A═ does not carry an exocyclic methylene group at the 10-position. Active compounds of the invention exhibit cell modulating activity while exhibiting a substantial lack of calcemic effect.
16 Citations
14 Claims
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1. A compound of the formula (I) ##STR10## where R1 and R2, which may be the same or different, each represent a hydrogen atom or an aliphatic, cycloaliphatic, araliphatic or aryl group or together with the nitrogen atom to which they are attached form a heterocyclic group;
- R3 represents a methyl group having α
- or β
-configuration;
X represents a valence bond or a C1-2 alkylene group;
Y represents --O--, --S--, --CH2 -- or --NR-- where R is a hydrogen atom or an organic group;
Z represents a valence bond or a C1-3 alkylene group; and
A═
represents a cyclohexylidene moiety characteristic of the A-ring of a 1α
-hydroxylated vitamin D or analogue thereof, with the proviso that when --X--Y--Z-- together represent an alkylene group containing up to 4 carbon atoms A═
does not carry an exocyclic methylene group at the 10-position. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14)
- R3 represents a methyl group having α
Specification