C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 239/95 (2006.01)
Patent
CA 2333274
The present invention provides for thermally stable forms of 2,4-diamino-5- methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline, or trimetrexate. A crystalline 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline monohydrate, or trimetrexate monohydrate, belonging to the space group P<o>1</o>(#2) and having a triclinic cell with dimensions of about a = 7.699 .ANG., b = 9.606 .ANG. and c = 13.012 .ANG. is disclosed. A novel Schiff base compound, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyphenylimino)-methinyl] quinazoline, is also disclosed. The present invention further provides novel methods of producing stable trimetrexate free base compounds, including crystalline trimetrexate monohydrate. The crystalline monohydrate form provides increased stability over the anhydrous form.
L'invention concerne des formes stables à la chaleur de 2,4-diamino-5-méthyl-6-[(3,4,5-triméthoxyanilino)méthyl]quinazoline ou trimétrexate. Elle concerne un monohydrate cristallin de 2,4-diamino-5-méthyl-6-[(3,4,5-triméthoxyanilino)méthyl]quinazoline ou monohydrate de trimétrexate appartenant au groupe spatial P<o>1</o>(#2) et possédant une cellule triclinique présentant des dimensions de a = 7,699 .ANG., b = 9,606 .ANG. et c = 13,012 .ANG.. Elle concerne également un nouveau composé de base de Schiff, 2,4-diamino-5-méthyl-6-[(3,4,5-triméthoxyphénylimino)-méthinyl]quinazoline. Elle concerne, de plus, de nouveaux procédés servant à préparer des composés stables de base libre de trimétrexate, y compris monohydrate de trimétrexate cristallin. Cette forme cristalline de monohydrate présente une stabilité améliorée par rapport à la forme anhydre.
Grafe Ingomar
Morsdorf Johann
Stogniew Martin
Osler Hoskin & Harcourt Llp
U.s. Bioscience Inc.
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