Leo Pharmaceutical Products Ltd. A/s

Other

Leo-pharma A/s

Claus Aage Svensgaard Bretting

Martin John Calverley

Welf Von Daehne

Ernst T Binderup

Kai Holst Hansen

Gunnar Grue-S&oslash;rensen

Ernst Torndal Binderup

Compounds according to formula I in which formula R1 and R2, which may be the same or different, represent halogen, (C-C)hydrocarbyl, optionally substituted with one or two hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C-C)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C-C)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

Vitamin d analogues, compositions comprising said analogues and their use

Vitamin D analogues

The present invention relates to compounds of formula (I), in which formula X is hydrogen or hydroxy; R,and R,, which may be the same or different, stand for hydrogen or a C,-C,alkyl radical; or R,and R,, taken together with the carbon atom bearing the group X, can form a C,-C,carbocyclic ring, R,stands for a C,-C,alkyl radical, an aryl or an aralkyl radical, or for YR,, in which Y stands for the radicals &mdash;CO&mdash;S&mdash;, &mdash;CS&mdash;O&mdash; or &mdash;CS&mdash;S&mdash;, and R,stands for a C,-C,alkyl radical or an aryl or an aralkyl radical; Q is (CH,),, n being 1-4. R,, R,and Q independently may optionally be substituted with one or more fluorine atoms. The compounds show strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells as well as immunomodulating and antiinflammatory effects.

Growing community of inventors

Frederiksberg, Denmark

Claus Aage Svensgaard Bretting