9-substituted-8-unsubstituted-9-deazaguanines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514263, 514269, A61K 31495, C07D47300, C07D47318

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active

057212406

ABSTRACT:
The specification discloses the compounds of formula I ##STR1## wherein (a) --CH.sub.2 Ar represents ##STR2## in which R.sub.1 represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, benzyloxy, hydroxy or trifluoromethyl; and R.sub.2 represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, benzyloxy, hydroxy or trifluoromethyl; provided that R.sub.2 represents hydrogen or C.sub.1 -C.sub.3 -alkyl if R.sub.1 represents trifluoromethyl, or that R.sub.1 represents hydrogen or C.sub.1 -C.sub.3 -alkyl if R.sub.2 represents trifluoromethyl; or

REFERENCES:
patent: 4772606 (1988-09-01), Sircar et al.
patent: 4923872 (1990-05-01), Kostlan et al.
Comparative in vitro and in vivo activities of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase, CI-972 and PD 141955, Biochemical Pharmacology, vol. 44, No. 5, 1992, pp. 996-999 Month Not Available.
Gilbertsen et al., Activities of Two-9-Deazaguanine Analogue Inhibitors of Purine Nucleoside Phosphorylase, CI-972 and PD 141955, in Vitro and in Vivo, Annals New York Academy of Sciences, vol. 685, 1993, pp. 248-251 Month Not Available.
Wilburn et al., PD 141955 and CI-972: 9-deazaguanine analog purine nucleoside phosphorylase inhibitors. I. Suppression of the human mixed lymphocyte reaction (MLR), Agents Actions, vol. 39, Special Conference Issue, 1993, pp. C96-C98 Month Not Available.
Dong et al., PD 141955 and CI-972: 9-deazaguanine analog purine nucleoside phosphorylase inhibitors. II. Effects on nucleoside catabolism in human and rat blood in vitro, Agents Actions, vol. 39, Special Conference Issue, 1993, pp. C99-C100 Month Not Available. C!CI-1000), Journal of Labelled Compounds and Radiopharmaceuticals, vol. XXXVI, No. 11, pp. 1029-1035, 1995 Month Not Available.
Sircar et al., Purine Nucleoside Phosphorylase (PNP) Inhibitors: Potentially Selective Immunosuppressive Agents, Drugs of the Future, vol. 13, No. 7, 1988, pp. 653-668 Month Not Available.
Sircar et al., 8-amino-9-substituted guanines: Potent purine nucleoside phosphorylase (PNP) inhibitors, Agents and Actions, vol. 21, No. 3/4, 1987, pp. 253-256 Month Not Available. 3-Amino-2-carboalkoxypyrroles, J. Org. Chem., vol. 44, No. 22, 1979, pp. 3826-3829 Month Not Available.

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