9-Substituted-8-halo or -8-hydroxy-9-deazaguanines as inhibitors

Details 9-Substituted-8-halo or -8-hydroxy-9-deazaguanines as inhibitors 9-Substituted-8-halo or -8-hydroxy-9-deazaguanines as inhibitors

1993-03-04

1994-01-25

Berch, Mark L.

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C07D48704, A61K 31505

Patent

active

052817083

ABSTRACT:
The present invention is novel 9-substituted-8-hydroxy or -8-halo-9-deazaguanines of the Formula (I) ##STR1## and pharmaceutical compositions and methods of use therefor. The derivatives are inhibitors of purine nucleoside phosphorylase selectively cytotoxic to T-cells but not to B-cells in the presence of 2'-deoxyguanosine and, therefore, are for use in the treatment of autoimmune diseases, gout, psoriasis or rejection of transplantation.
The present invention also includes certain novel intermediates of the Formula (II) ##STR2## wherein Z is N.sub.2.sup.+ PF.sub.6.sup.-, or N.sub.2.sup.+ Cl.

REFERENCES:
patent: 4923872 (1990-05-01), Kostlan
patent: 4985433 (1991-01-01), Secrist
patent: 4985434 (1991-01-01), Secrist
patent: 5008265 (1991-04-01), Secrist
patent: 5008270 (1991-04-01), Secrist

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