56 results about "Vitamin D Analogue" patented technology

A composition suitable for topical application comprising a continuous phase and at least one discontinuous phase, said composition comprising at least one polyaphron dispersion, at least one vitamin D or vitamin D analogue and at least one corticosteroid.

The invention provides therapeutic methods for inhibiting, ameliorating or alleviating the hyperproliferative cellular activity of diseases of the prostate, e.g., prostatic cancer and prostatic hyperplasia, which includes administering to a patient in need thereof an active vitamin D analogue and another anticancer agent. Cell differentiation is promoted, induced or enhanced without causing to the patient dose-limiting hypercalcemia and hypercalciuria.

The present invention relates generally to compositions and methods using mammalian, dsDNA (Double Stranded Deoxyribonucleic Acid) vaccination for the induction and maintenance of regulator suppressor T cells resulting in suppression of non infectious, and post infectious, inflammatory, allergic, auto-immune, vasculitic, certain degenerative vascular, and graft versus host diseases, with or without the use of IL-10, and with or without the use or TGFβ, with or without the use of anti-IL 6 receptor antibody, anti TNF antibody and or Plasmapheresis, IVIG, Corticosteroids, Methotrexate, Bromocriptine, and or vitamin D analogues.

Compounds according to formula I

in which formula R1 and R2, which may be the same or different, represent halogen, (C₁-C₆)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 (C₃-C₆)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 (C₁-C₃)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond;

Y and Z independently represent hydrogen or methyl; the bond between C#16 and C#17 is depicted with a dotted line to illustrate that said bond may be either a single bond, in which case the projection of the ring substituent is beta, or a double bond; A represents hydroxyl, fluorine or hydrogen; B represents CH₂ or H₂; the configuration in the 3-position corresponds to the same configuration as in natural vitamin D₃ (normal), or the configuration in the 3-position is opposite to that of natural vitamin D₃ (epi); with the proviso that when X represents (E)-ethylene or (Z)-ethylene, one of R1 and R2 taken together with R3 may not form a direct bond, such that a triple bond is constituted; with the further proviso that when X represents a bond R1 and R2 are not hydrogen; with the further proviso that the compound of formula I is not 3(S)-hydroxy-9,10-secocholesta-5(Z),7(E),10(19),22(E),24-penta-ene;

and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

The present invention discloses methods for preparing vitamin D2 derivatives and intermediates of vitamin D2 derivatives. The present invention discloses an improved photolysis process for the preparation of cis intermediates (I) from trans starting materials (II). Also disclosed is an improved method for the formation of a trans double bond at C22-C23 of a vitamin D2 derivative, which has a negative effect on the desired cis double bond of compound (IIIA) relative to the undesired cis double bond of compound (IIIA). The trans double bond provides high selectivity.

The present invention relates to analogues of vitamin D namely 14-epi-2-alkyl-19-nor vitamin D derivatives. Also a general method for the synthesis and the biological activities are described. The general formula is: (I) where R (α or β oriented) represents an alkyl substituent and X part of a typical side chain of vitamin D or of one of its established analogues.

The present invention relates to an isomerisation method of vitamin D analogues, such as compounds useful for the synthesis of calcipotriol, and to and to the use of a flow-through photoreactor or continuous flow photoreactor reactor for making said vitamin D analogues. The present invention relates further to the use of intermediates produced with said method for making calcipotriol or calcipotriol monohydrate, or pharmaceutical formulations thereof.

The present invention relates to a topical spray composition comprising a biologically active vitamin D derivative and a corticosteroid, and its use in the treatment of dermal diseases and conditions. The spray comprises especially a propellant selected from the group consisting of dimethyl ether, diethyl ether and methylethyl ether or a mixture thereof and further a pharmaceutically acceptable lipid carrier solubilised or suspended in said propellant.

The present invention relates to processes for epimerising alcohols of compounds having a hydroxyl substituent on an asymmetric allylic carbon, such as compounds useful for the synthesis of vitamin D analogues where the epimeric hydroxyl substituent is at the 24 position. The Invention further relates to methods of producing intermediates useful for the synthesis of calcipotriol by said epimerisation processes.

The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.

The present invention relates to a pharmaceutical composition for dermal use, said composition comprising a first pharmacologically active component A consisting of at least one vitamin D or vitamin D analogue and a second pharmacologically active component B consisting of at least one corticosteroid.