Compositions and methods of reducing side effects and...

Details Compositions and methods of reducing side effects and... Compositions and methods of reducing side effects and...

2007-01-18

2009-10-13

Marschel, Ardin (Department: 1614)

Organic compounds -- part of the class 532-570 series

Organic compounds

Plural nitrogens bonded directly to the pteridine ring system

C514S262100

Reexamination Certificate

active

07601834

ABSTRACT:
This invention is in the field of chemical restructuring of antimetabolite agents known to have poor oral bioavailability and to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concerns orotate derivatives of the methotrexate and trimetrexate, that are found to improve the oral bioavailability and clearance compared with their respective forms—methotrexate and trimetrexate, currently in use. The present invention provides methotrexate orotate having the formula:

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patent: 6184227 (2001-02-01), Karmali
patent: 6559149 (2003-05-01), Matsuoka
Gould, P.L. International Journal of Pharmaceutics, 1986, vol. 33, pp. 201-217.

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