Tremextrexate derivatives and pharmaceutical compositions comprising the same

Number of patents in Portfolio can not be more than 2000

United States of America Patent

APP PUB NO 20020107393A1
SERIAL NO

09882260

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Abstract

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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-trimethoxyanil-ino)methyl] quinazoline monohydrate, or trimetrexate monohydrate, belonging to the space group P{overscore (1)} (#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.

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Patent Owner(s)

Patent OwnerAddress
MEDIMMUNE ONCOLOGY INCGAITHERSBURG MD

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Grafe, Ingomar Nurnberg, DE 13 137
Morsdorf, Johann Langenzenn, DE 4 19
Stogniew, Martin Blue Bell, PA 95 465

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