Synthesis of diamides from 1,4-benzodioxane-2- and isochroman-1-carboxylic acids
摘要:
1,4-Benzodioxane-2-carboxylic acid and isochroman-1-carboxylic acid were treated with thionyl chloride, and the resulting acid chlorides reacted with p-aminobenzoic acid in dioxane in the presence of pyridine to produce the corresponding amido acids. The latter were converted into acid chlorides which were brought into reaction with various amines to obtain a number of new diamides.
[EN] TUBULYSIN ANALOGS AND METHODS FOR THEIR PREPARATION<br/>[FR] ANALOGUES DE LA TUBULYSINE ET LEURS PROCÉDÉS DE PRÉPARATION
申请人:PFIZER
公开号:WO2017134547A1
公开(公告)日:2017-08-10
The present invention is directed to novel cytotoxic tubulysin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
Substituted Dihydroimidazoles and their Use in the Treatment of Tumors
申请人:Chamoin Sylvie
公开号:US20100075966A1
公开(公告)日:2010-03-25
The invention relates to dihydroimidazoles of formula rac-(I),
wherein the radicals and symbols are as defined herein; their use as inhibitors of the interaction of the MDM2 protein with a p53-like peptide, new pharmaceutical formulations comprising said compounds, said compounds for use in the therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of proliferative diseases or for the manufacture of pharmaceutical formulations useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide, a pharmaceutical formulation e.g. useful in the treatment of proliferative diseases that respond to modulation of the interaction of the MDM2 protein with a p53-like peptide comprising said compound, methods of treatment comprising administration of said compounds to a warm-blooded animal, and/or processes for the manufacture of said compounds.
Disclosed are compounds of formula (I):
and pharmaceutical compositions containing such compounds. Methods of treating neurological or psychiatric disease and disorders in a subject in need are also disclosed.
Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
[EN] ADRENERGIC RECEPTOR MODULATING COMPOUNDS AND METHODS OF USING THE SAME<br/>[FR] COMPOSÉS DE MODULATION DES RÉCEPTEURS ADRÉNERGIQUES ET LEURS PROCÉDÉS D'UTILISATION
申请人:UNIV LELAND STANFORD JUNIOR
公开号:WO2017197324A1
公开(公告)日:2017-11-16
Adrenergic receptor modulating compounds and methods of using the same are provided. Also provided are methods of treating a subject for a disease or condition associated with an adrenergic receptor including administering a therapeutically effective amount of the subject compound. Aspects of the disclosure include a method of modulating an inflammatory pathway in a cell, such as the production of TNF-alpha in the cell. The method can include contacting a cell with a β1-selective adrenergic receptor modulating compound to selectively activate a cAMP pathway over a beta-arrestin pathway in the cell. Pharmaceutical compositions and kits which include the subject compounds are provided.