Thermally stable trimetrexates and processes for producing the same
US6258952A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Nov 9, 1999 |
| Grant date | Jul 10, 2001 |
| Priority date | — |
| Expiry date | Nov 9, 2019 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P35/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.