Research Institute for Medicine & Chemistry, Inc.

Malathi Ramgopal

Robert H Hesse

Sundara Katugam Setty

Sundara Katugam Srinivasasetty Setty

Gaddam Subba Reddy

Sanga Kugabalnsooriar

Novel sterol derivatives of formula (I), in which: Rrepresents a hydroxyl group or protected hydroxyl group, Rrepresents a hydrogen atom and a double bond is present at c, or Rand Rtogether represent an oxo group and a double bond is present at b or double bonds are present at a and b; Rrepresents a methyl group having &#x3b1;- or &#x3b2;-configuration; Rand R, 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&#x2013;5 carbon atoms, an oxa group-containing analogue thereof in which a methylene group other than that attached to the &#x2014;CO.NRRmoiety is replaced by an oxygen atom, or an unsaturated analogue thereof containing up to two double bonds. Active compounds of the invention exhibit potent effects on the modulation of cell growth and differentiation and possess an advantageous therapeutic ratio by virtue of their low levels of calcaemic activity.

Cholenic acid amides and pharmaceutical compositions thereof

Compounds of Formula (I) in which: Rand R, which may be the same or different, each represents a lower alkyl, alkenyl or alkynyl group; Rrepresents a methyl group having &#x3b1;- or &#x3b2;-configuration; Rrepresents a hydrogen atom or an etherifying or esterifying group; Rrepresents a hydrogen atom, a hydroxyl group or a lower alkoxy group; X represents a group OR, wherein Ris as defined above, or a group NRRwherein Rrepresents 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 Ris 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 cell growth and differentiation, while having low calcaemic activity.

Steroid compounds with a c17-alkyl side chain and an aromatic a-ring for use in therapy

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.

Vitamin D analogues

Vitamin D amine and amide derivatives

Vitamin D amide derivatives

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Andover, MA, United States of America

Malathi Ramgopal