Abstract: Novel sterol derivatives of formula (I), in which: R1 represents a hydroxyl group or protected hydroxyl group, R2 represents a hydrogen atom and a double bond is present at c, or R1 and R2 together represent an oxo group and a double bond is present at b or double bonds are present at a and b; R3 represents a methyl group having ?- or ?-configuration; R4 and R5, which may be the same or different, are selected from hydrogen atoms and aliphatic, cycloaliphatic, araliphatic and aryl groups, or together with the nitrogen atom to which they are attached form a heterocyclic group; and X represents a polymethylene group containing 2–5 carbon atoms, an oxa group-containing analogue thereof in which a methylene group other than that attached to the —CO.NR4R5 moiety is replaced by an oxygen atom, or an unsaturated analogue thereof containing up to two double bonds.

Abstract: Compounds of formula (I) in which: R1 represents a hydrogen atom or an O-protecting group; R2 represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R3 represents a methyl group having ?- or ?-configuration; X represents a C1-3 alkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula —C(R4)(R5)OR1 where R1 is as defined above and R4 and R5, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R4 and R5 does not exceed three atoms, with the proviso that X is a valence bond when both R4 and R5 are other than hydrogen; and the dotted line signifies that a double bond may optionally be present at the 16(17)-position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.

Abstract: Compounds of Formula (I) in which: R1 and R2, which may be the same or different, each represents a lower alkyl, alkenyl or alkynyl group; R3 represents a methyl group having ?- or ?-configuration; R4 represents a hydrogen atom or an etherifying or esterifying group; R5 represents a hydrogen atom, a hydroxyl group or a lower alkoxy group; X represents a group OR4, wherein R4 is as defined above, or a group NR6R7 wherein R6 represents a hydrogen atom, an aliphatic or araliphatic organic group, or an acyl group comprising an aliphatic, araliphatic or aryl organic group linked to the nitrogen atom by way of a carbonyl group; and R7 is a hydrogen atom or a lower alkyl group; Y represents a lower alkylene, alkenylene or alkynylene group optionally substituted by a hydroxyl, etherified hydroxyl or esterified hydroxyl group; and the dotted lines signify that double bonds may be present at the 16(17)-position and/or either at the 6(7)- and 8(9)-positions or at the 7(8)-position exhibit potent effects on modulation of

Abstract: Compounds of formula (I) in which: R1 represents a hydrogen atom or an O-protecting group; R2 represents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; R3 represents a methyl group having &agr;- or &bgr;-configuration; X represents a C1-3 alkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula —C(R4)(R5)OR1 where R1 is as defined above and R4 and R5, which may be the same or different, are each selected from hydrogen atoms, alkyl, alkenyl and alkynyl groups such that the total carbon content of R4 and R5 does not exceed three atoms, with the proviso that X is a valence bond when both R4 and R5 are other than hydrogen; and the dotted line signifies that a double bond may optionally be present at the 16(17)-position exhibit potent cell modulating activity, including antiproliferative and antiangiogenic effects.

Abstract: 1-Hydroxy pregnacalciferol derivatives of formula (I) and their corresponding 5,6-trans isomers wherein R1 is hydroxyl or lower alkoxy and R2 is optionally hydroxylated or lower alkoxylated lower alkynyl and R1 is C(RA) (RB)CH3 where RA is optionally hydroxylated or lower alkoxylated lower alkynyl and RB is hydroxyl or lower alkoxy or RA and RB together represent oxo and R2 is hydrogen, hydroxyl or lower alkoxy, and R3 and R4 represent hydrogen atoms, exhibit anti-progesterone activity and may be useful as antineoplastic, antifertility, antiproliferative, immunosuppressive and/or antiinflammatory agents.

Abstract: 1-Hydroxy pregnacalciferol derivatives of formula (I) and their corresponding 5,6-trans isomers wherein R1 is hydroxyl or lower alkoxy and R2 is optionally hydroxylated or lower alkoxylated lower alkynyl or R1 is C(RA) (RB)CH3 where RA is optionally hydroxylated or lower alkoxylated lower alkynyl and RB is hydroxyl or lower alkoxy or RA and RB together represent oxo and R2 is hydrogen, hydroxyl or lower alkoxy, and R3 and R4 represent hydrogen atoms, exhibit anti-progesterone activity and may be useful as antineoplastic, antifertility, antiproliferative, immunosuppressive and/or antiinflammatory agents.

Abstract: The present invention relates to novel 1.alpha.-hydroxy vitamin D derivatives in which the 17-position side chain carries an azide or optionally substituted 1,2,3-triazole group, including compounds of general formula (I) where R.sup.1 represents a methyl group having .alpha.- or .beta.-configuration; W represents a valence bond or a C.sub.1-5 alkylene group; X represents azide or an optionally substituted triazole group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof. Active compounds of the invention exhibit cell modulating activity while exhibiting a substantial lack of calcaemic effect.

Abstract: The present invention relates to novel 1.alpha.-hydroxy vitamin D derivatives in which the 17-position side chain carries an azide or optionally substituted 1,2,3-triazole group, including compounds of general formula (I) where R.sup.1 represents a methyl group having .alpha.- or .beta.-configuration; W represents a valence bond or a C.sub.1-5 alkylene group; X represents azide or an optionally substituted triazole group; and A=represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof. Active compounds of the invention exhibit cell modulating activity while exhibiting a substantial lack of calcaemic effect.

Abstract: The present invention relates to compounds of general formula (I) ##STR1## where R.sup.1 and R.sup.2, 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; R.sup.3 represents a methyl group having .alpha.- or .beta.-configuration; one of R.sup.a and R.sup.b represents a hydroxy group or protected hydroxy group and the other represents a hydrogen atom; Y represents a valence bond or an alkylene group containing up to 3 carbon atoms; and A= represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-hydroxylated vitamin D or analogue thereof. Active compounds of the invention exhibit separation of cell modulating and calcaemic activities coupled with enhanced duration of activity.

Abstract: The invention relates to novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues, comprising compounds of general formula (I) ##STR1## where R.sup.1 and R.sup.2, 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; R.sup.3 represents a methyl group having .alpha.- or .beta.-configuration; X represents a valence bond or a C.sub.1-2 alkylene group; Y represents --O--, --S--, --CH.sub.2 -- or --NR-- where R is a hydrogen atom or an organic group; Z represents a valence bond or a C.sub.1-3 alkylene group; and A.dbd. represents a cyclohexylidene moiety characteristic of the A-ring of a 1.alpha.-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.dbd. does not carry an exocyclic methylene group at the 10-position.

Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.