Enzyme inhibitors, their synthesis and methods for use

Details Enzyme inhibitors, their synthesis and methods for use Enzyme inhibitors, their synthesis and methods for use

1993-11-02

1995-12-19

Tsang, Cecilia

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514270, 514274, 544300, 544301, 544302, 544303, 544310, 544311, 544314, A61K 31505, C07D23902

Patent

active

054768551

ABSTRACT:
Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2.
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.

REFERENCES:
patent: 4613604 (1986-09-01), Chu et al.
patent: 5077280 (1991-12-01), Sommadossi et al.
patent: 5141943 (1992-08-01), Naguib et al.
Wasternack, Pharmac. Ther., 8:629-651 (1981).
Naguib, et al, Cancer Res., 45:5405-5412 (1985).
Harris, et al, Biochem, Pharmac., 37:4759-4762 (1988).
Harris, et al, Cancer Res., 49:6610-6614 (1989).
Naguib, et al, Biochem Pharmac., 45:667-673, (1993).
Petit, et al, Cancer Res., 48:1676-1679 (1988).
von Roemeling et al, Advances in Chronobiology, Part B, 357-373 (1987).
Cooper et al, Cancer Res., 32:390-397 (1972).
Gentry et al, Cancer Res. 31:909-912 (1971).
Bakkeren et al, Clinica Chimica Acta, 140:246-247 (1984).
Tuchman et al, N. Engl. J. Med., 313:235-249 (1985).
Diasio et al, J. Clin, Invest., 81:47-51 (1988).
Wadman et al, Adv. Exp. Med. Biol., 165A:109-114 (1984).
Chauduri et al, Cancer Res., 18:318-328 (1958).
Heidelberger et al, Cancer Res., 30:1549-1569 (1970).
Mukherjee et al, J. Biol. Chem., 235:433-437 (1960).
Monks et al, Biochem. Pharmac., 32, 2003-2009 (1983).
Darnowski et al, Cancer Res., 45:5364-5368 (1985).
Cretton et al, Molec., Pharmac., 39:258-266 (1991).
Sommadossi et al, Antimicrob. Agents Chemother., 32, 997-1000 (1988).
Niedzwicki et al, Biochem Pharmac., 31:1857 (1982).
Naguib et al, Biochem Pharmac., 36:2195 (1987).
Naguib et al, Biochem Pharmac., 46:1273-1283 (1993).

Affiliated with

Also associated with

Rating

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 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 Enzyme inhibitors, their synthesis and methods for use will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-992245