The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmaceutical formulations and processes for the preparation of compounds according to the invention.
[EN] THIADIAZOLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF DISORDERS MEDIATED BY SLPL RECEPTORS<br/>[FR] DÉRIVÉS DE THIADIAZOLE ET LEUR UTILISATION POUR LE TRAITEMENT DE TROUBLES MÉDIÉS PAR LES RÉCEPTEURS SLPL
申请人:GLAXO GROUP LTD
公开号:WO2010146104A1
公开(公告)日:2010-12-23
The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
Steroids of the formula ##STR1## wherein R.sup.1 to R.sup.4, X and n have the significance given in the description, which lower the intestinal resorption of cholesterol and plasma cholesterol and a process of making same from corresponding steroids having an alcohol residue of the formula --O--X--OH in the 3-position.
Benzodiazepine derivatives and their pharmaceutical use
申请人:Hoffmann-La Roche Inc.
公开号:US04474777A1
公开(公告)日:1984-10-02
There are presented novel pharmaceutically active substances which inhibit the intestinal resorption of cholesterol and which accordingly can be used in the control or prevention of atherosclerosis. These active substances are benzodiazepines of the formula ##STR1## wherein R.sup.1 is (C.sub.1 -C.sub.4)-alkyl, R.sup.2 is hydrogen or methyl, R.sup.3 and R.sup.4 each are halogen and R.sup.5 is (C.sub.3 -C.sub.9)-alkylamino substituted by at least two hydroxy groups, (C.sub.3 -C.sub.6)-cycloalkylamino substituted by at least one hydroxy group, glucosamino, galactosamino, mannosamino, monohydroxy-1-azetidinyl, mono- or dihydroxy-1-pyrrolidinyl or mono-, di- or trihydroxy-1-piperidinyl, and the readily hydrolyzable esters and ethers thereof, as well as pharmaceutically acceptable salts of these compounds.
[EN] PYRIDINE DERIVATIVES AS KIF18A INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDINE EN TANT QU'INHIBITEURS DE KIF18A
申请人:AMGEN INC
公开号:WO2021026100A1
公开(公告)日:2021-02-11
Amide compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.