Research Institute for Medicine & Chemistry, Inc.

Sundara Katugam Srinivasasetty Setty

Robert H Hesse

Malathi Ramgopal

Maurice Murdoch Pechet

Sanga Kugabalnsooriar

Michael Gile

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: Rrepresents a hydrogen atom or an O-protecting group; Rrepresents a hydroxyl, lower alkoxy, carboxaldehyde, lower alk-1-enyl or hydroxy- or lower alkoxy-substituted lower alkyl group; Rrepresents a methyl group having &#x3b1;- or &#x3b2;-configuration; X represents a Calkylene group or a valence bond; Y represents a carboxaldehyde group or a group of formula &#x2014;C(R)(R)ORwhere Ris as defined above and Rand R, 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 Rand Rdoes not exceed three atoms, with the proviso that X is a valence bond when both Rand Rare 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.

2-substituted pregna-1-3,5(10) triene and chola-1,3,5(10) triene derivatives and their biological activity

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

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

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Cambridge, MA, United States of America

Sundara Katugam Srinivasasetty Setty