Novel enzyme inhibitors, their synthesis, and methods for use

Details Novel enzyme inhibitors, their synthesis, and methods for use Novel enzyme inhibitors, their synthesis, and methods for use

C - Chemistry, Metallurgy

07

D

C07D 239/46 (2006.01) A61K 31/515 (2006.01) C07D 239/24 (2006.01) C07D 239/60 (2006.01)

Patent

CA 2176720

Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have general formula (I) or (II), where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R1 is an acyclo tail having general formula (III), where R2 is H, CH2OH or CH2NH2; R3 is OH, NH2, or OCOCH2CH2CO2H; and R4 is O, S, or CH2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.

L'invention concerne des nouveaux composés efficaces pour inhiber l'activité de la DHUDase et l'UrdPase. Lesdits composés sont représentés par la formule (I) ou (II) dans lesquelles X correspond à S ou Se; Y à I, F, Cl, Br, méthoxy, benzyle, sélénylphényle, ou thiophényle, et R¿1? à une terminaison acyclo représentée par la formule (III) dans laquelle R¿2? correspond à H, CH¿2?OH ou CH¿2?NH¿2?; R¿3? à OH, NH¿2?, ou à OCOCH¿2?CH¿2?CO¿2?H; et R¿4? à O, S, ou CH¿2?. Les composés selon l'invention peuvent être utilisés dans des compositions pharmaceutiques ainsi qu'avec divers agents chimiothérapeutiques de manière à augmenter l'efficacité du traitement. Ils peuvent également être utilisés dans des méthodes de traitement de patients par coadministration ou administration séquentielle des composés inhibant les enzymes avec un agent chimiothérapeutique efficace pour traiter des cancers, ou des infections virales, fongiques, bactériennes ou parasitaires. Lesdits composés sont également utiles pour améliorer l'imagerie. Ils peuvent aussi être administrés seuls pour prévenir et/ou traiter les troubles du catabolisme de la pyrimidine et d'autres troubles physiologiques.

Affiliated with

Also associated with

Rating

Novel enzyme inhibitors, their synthesis, and methods for use does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Novel enzyme inhibitors, their synthesis, and methods for use, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Novel enzyme inhibitors, their synthesis, and methods for use will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-2044291