Crystalline trimetrexate salts and the process for making the sa

Details Crystalline trimetrexate salts and the process for making the sa Crystalline trimetrexate salts and the process for making the sa

1998-02-04

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

06017921&

ABSTRACT:
The present invention provides for a crystalline form of trimetrexate either as a glucuronate, acetate, hydrochloride, methanosulfonate or lactate salt, which can be processed galenically as a stable, well-defined solid substance and processes for producing the crystalline forms. Such crystalline forms allow for prolonged stability in storage and for oral and intravenous administration of the drug.

REFERENCES:
patent: 4376858 (1983-03-01), Colbry
patent: 4853221 (1989-08-01), Elslager et al.
patent: 5716960 (1998-02-01), Kennedy
Robinson, C., 1994, "Trimetrexate glucuronate", Drugs of Today 30(5):347-355.
Hempel, A. et al., 1988, "Trimetrexate: Molecular structures and conformational similarities in two crystal forms", Cancer Biochem. Biophys. 10(1):25-30 .
Sutton, P.A. & Cody, V., 1987, "Conformational Analysis of Antineoplastic Antifolates: The Crystal Structure of Trimetrexate and the Aminopterine Derivative 4-[N-[2,4-Diamino-6-pteridinyl)methyl]amino]benzoic Acid", J. Med. Chem. 30:1843-1848.
Cell cycle effects of trimextrexate (CI-898), Cancer Chemotherapy and Pharmacology, Hook et al., vol. 16, No. 2, 1986, pp. 116-120 (1985).

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