Thermally stable trimetrexates and processes for producing the s

Details Thermally stable trimetrexates and processes for producing the s Thermally stable trimetrexates and processes for producing the s

1998-05-18

2000-01-25

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544291, A61K 31505, C07D23995

Patent

active

060179228

ABSTRACT:
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 P1(#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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