Nucleic Acid Research Institute

Icn Pharmaceuticals, Inc.

Other

Brigham Young University

Ganapathi R Revankar

Roland K Robins

Richard L Tolman

Yu-An Chang

Brahma S Sharma

Naeem B Hanna

Yogesh S Sanghvi

Robert W Sidwell

.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.

Substituted pyrimido[5,4-d]pyrimidine nucleosides

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 ;

6-sulfenamide, 6-sulfinamide and 6-sulfonamide purines, purine

##STR1## 6-Amino-1-(2-deoxy-.alpha.D-erythro-pentofuranosyl)imidazo [4,5-C]pyridin-4-one (also know as .alpha.-2'-deoxy-3-deazaguanosine) is non mitogenic to human peripheral blood lymphocytes; however, it displays a potent immunoenhancing activity on human T cells. This compound causes a marked increase in both phytohemagglutinin and Concanavalin A induced proliferation of T cells. When added during allogeneic mixed lymphocyte response, it also potentiates the proliferation of alloreative T cells. The compound shows no potentiating effect on B lymphocytes activated either with Staphylococcus aureus cowan or Pokeweed mitogen, suggesting that it is mainly a T cell function immunopotentiator. The compound overcomes induced immunosuppression and is able to restore depressed proliferative responses of T cells. Further it potentiates the generation of antigen-specific primary cytotoxic T lymphocytes.

T cell immunopotentiator

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.

8-Chloroadenosine 3', 5'-cyclic monophosphate preparations

A method that is direct and stereospecific is provided for the production of 2'-deoxyadenosine derivatives and related analogs. The method comprises glycosylation of the sodium salt of 2,6-dichloropurine or 6-chloropurine and ammonolysis of the glycosylate to obtain the corresponding 2-chloro-2'-deoxyadenosine or 2'-deoxyadenosine.

Method for the production of 2'-deoxyadenosine compounds

A class of novel azole dinucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties and are well tolerated, being useful, for example, in treating leukemias in warm blooded animals.

Azole dinucleotide compositions and methods of use

Azole dinucleotide compounds and methods for their production

Imidazo[1,2-a]-s-triazines including the base, the nucleoside, derivatives of the nucleoside, and the 5' nucleotide are prepared and are useful as antiviral Agents against RNA viruses.

Imidazo[1,2-a]-s-triazine

Compounds of the structure ##STR1## wherein Y is O, NH or NAc; X is H, .beta.-D-ribofuranosyl or 2,3,5-tri-O-Ac-.beta.-D-ribofuranosyl and Ac is acetyl; are useful as antimicrobal agent.

1,2,4-Thiadiazolidine-3,5-dione

9-.beta.-D-Arabinofuranosyl nucleotides of the following structure are disclosed: ##STR1## wherein AP is a 3' or 5' phosphorylated arabinofuranoside or the corresponding 3', 5' cyclic phosphate joined by a glycoside linkage to N.sup.9 of the aglycon component of said nucleotide, and Z is H, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.10 aralkoxy, or hydroxy. Compounds prepared according to the invention exhibit antiviral activity in vitro, while others are precursors useful in the synthesis of bioactive compounds.

Growing community of inventors

Orem, UT, United States of America

Ganapathi R Revankar