Abstract: .alpha. and .beta.-ribonucleosides of substituted pyrimido[5,4-d]pyrimidines are used in treating malignant tumors in vivo. A novel synthesis for preparing these compounds and other related compounds is further disclosed.
Type:
Grant
Filed:
June 3, 1988
Date of Patent:
August 20, 1991
Assignee:
Nucleic Acid Research Institute
Inventors:
Roland K. Robins, Ganapathi R. Revankar, Yogesh S. Sanghvi
Abstract: 6-Sulfenamide, 6-sulfinamide and 6-sulfonamide purines, purine nucleosides, purine nucleotides and 3 and 7 deaza and 8 aza derivatives thereof of structure: ##STR1## wherein Z is H or --NH.sub.2 ;X is --S--NH.sub.2, ##STR2## T is C--H, G is N and Q is N; or T is C--H, G is N and Q is C--H; orT is N, G is N and Q is C--H; orT is C--H, G is C--H and Q is N;Y is H or an .alpha.-pentofuranose or .beta.-pentofuranose of the formula: ##STR3## wherein R.sub.1 and R.sub.2 independently are H, OH, --O-acyl or ##STR4## or together R.sub.1 and R.sub.2 are ##STR5## and R.sub.3 and R.sub.4 are H or one of R.sub.3 or R.sub.4 is OH and the other is H; provided that when Y is H, Z is --NH.sub.2 ; and acceptable salt thereof are prepared and are useful as antitumor agents or they are intermediates for compounds which are antitumor agents. The compounds are used to treat an affected warm blooded host by serving as the active ingredients of suitable pharmaceutical compositions.
Type:
Grant
Filed:
November 22, 1988
Date of Patent:
June 25, 1991
Assignee:
Nucleic Acid Research Institute
Inventors:
Roland K. Robins, Ganapathi R. Revankar, Naeem B. Hanna
Abstract: The triazole nucleosides 1-(5'-O-sulfamoyl-.beta.-D-ribofuranosyl)[1,2,4]triazole-3-carboxamide, 1-(5'-O-sulfamoyl-.beta.-D-ribofuranosyl)[1,2,4]triazole-3-thiocarboxamide and 1-(5'-O-sulfamoyl-.beta.-D-ribofuranosyl)[1,2,4]triazole-3-carbonitrile ar e prepared and used as antiparasitic agents.
Abstract: A novel class of alkyl-1-(.beta.-D-ribofuranosyl)[1,2,4]triazole-3-carboximidates of the formula: ##STR1## wherein R.sub.1 is methyl or ethyl and R.sub.2 is .beta.-D-ribofuranosyl, are useful as anti-leukemic agents.
Abstract: The compound 8-Chloroadenosine 3',5'-cyclic phosphate is used to treat malignant tumors in warm blooded animals. Two novel single step syntheses of 8-chloroadenosine 3',5'-cyclic phosphate and other related adenine and adenosine compounds from corresponding adenosine 3', 5'-cyclic phosphate and other respective related adenosine compounds are disclosed.
Type:
Grant
Filed:
December 21, 1987
Date of Patent:
August 29, 1989
Assignee:
Nucleic Acid Research Institute
Inventors:
Roland K. Robins, Ganapathi R. Revankar, Yu-an Chang