C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/94 (2006.01) A61K 31/517 (2006.01) A61P 35/02 (2006.01)
Patent
CA 2612459
Crystalline forms of the sulfate salt of 4-[6-methoxy-7-(3-piperidin-1-yl- propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid (4-isopropoxyphenyl)- amide, which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of the sulfate salt are characterized by a variety of properties and physical measurements. As well, methods of producing the sulfate salts, and using such salts to inhibit excessive tyrosine kinase activity in subjects to treat a number of diseases including cardiovascular disease (e.g., arteriosclerosis and vascular reobstruction), cancer (e.g., leukemia such as acute lymphocytic leukemia), glomerulosclerosis fibrotic diseases and inflammation, and general treatment of cell-proliferative diseases, are also discussed.
L'invention porte sur des formes cristallines du sel sulfate de l'acide (4-isopropoxyphényl)-amide 4-[6-méthoxy-7-(3-pipéridin-1-yl- propoxy)quinazolin-4-yl]pipérazine-1-carboxylique, qui peut être utilisé dans des applications pharmaceutiques. Des formes monocristallines particulières du sel sulfate sont caractérisées par une variété de propriétés et de mesures physiques. L'invention concerne également des procédés de production des sels sulfates et l'utilisation de ces sels pour inhiber une activité tyrosine kinase excessive chez des sujets afin de traiter un nombre de maladies, y compris les maladies cardiovasculaires (p.ex., l'artériosclérose et la réobustruction vasculaire), le cancer (p.ex., la leucémie, telle e la leucémie aiguë lymphoblastique), la glomérulose, les maladies fibrotiques et l'inflammation, et leur utilisation dans le traitement général de maladies à prolifération cellulaire.
Angelino Mark D.
Grant Craig
Luong Hoa Q.
Millennium Pharmaceuticals Inc.
Robic
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