Burroughs Wellcome Co.

Gertrude B Elion

George H Hitchings

Charles A Nichol

William S Simmons

Dwight R Stickney

Janet L Rideout

Thomas A Krenitsky

Robert A Strelitz

Howard J Schaeffer

Lowrie M Beacham, Iii

Richard L Miller

Janet E Litster

Janet E Rideout

Paulo M DeMiranda

Pharmaceutical preparations containing compounds of the formula ##STR1## where R is alkyl of 1 to 11 carbons. The preparations are useful in inhibiting adenosine deaminase in mammals thereby providing a method for prolonging the effectiveness of pharamaceutical agents which are biologically degraded by adenosine deaminase and thus converted into other compounds.

Adenosine deaminase inhibitors

4-Substituted alkyl-1-.alpha.-D-ribofuransylpyrazole-(3,4-d) pyrimidines are active against coccidia in vivo and unlike the 4-methylthio analogue, are non-toxic. Methods for preparing and using the compounds, intermediates in the preparation and compositions of the compounds are also described.

Pyrazolo pyrimidine riboside compounds, pharmaceutical compositions and

4-Alkenylthio-1-.beta.-D-ribofuranosylpyrazolo[3,4-d]-pyrimidines are active against coccidia in vivo, and unlike the 4-methylthio analogue, are non-toxic. Methods for the preparation and use of the compounds, intermediates in the preparation and formulations of the compounds are also described.

Substituted pyrazolo pyrimidine riboside compounds, pharmaceutical

The nucleotide derivatives of certain 2,6 substituted purines have been discovered to have anti-viral activity. Novel compounds and their pharmaceutically acceptable salts, pharmaceutical formulations containing the compounds of this invention, and the treatment of viral infections with these formulations are all disclosed. 2,6 Diamino-9-(.beta.-D arabinofuranosyl)-purine-5'-phosphate is an example of a more active compound of this invention.

Purine nucleotide antiveral composition and methods of use

A method and composition of treating a mammal suffering from an autoimmune disease which comprises internally administering to the mammal an effective autoimmune suppressant amount of the compound of formula or its pharmaceutically acceptable salts ##STR1## where R.sup.1 is amino or lower alkylamino and R.sup.2 is amino or hydrogen, provided that when R.sup.1 is amino, R.sup.2 is amino.

Amino purine nucleosides as autoimmune suppressant agents

Compounds of the formula ##STR1## where R.sup.1 is amino or lower alkylamino, R.sup.2 is amine or hydrogen and pharmaceutically acceptable salts thereof, provided that when R.sup.1 is amino, R.sup.2 is amino. The compounds are useful as immune suppressants and as antivirals.

Amino purine derivatives

Method and pharmaceutical preparations for treating meningeal leukemia, CNS lymphoma and neoplasms in the brain which comprises treating an infected mammal such as a human with a dose of an effective treatment amount of a compound of Formula I ##STR1## where R is a straight or branched chain lower alkyl of 1 to 4 carbon atoms, and X is a halogen atom (fluorine, chlorine, bromine or iodine) and pharmaceutically acceptable salts thereof. Preferred compounds for treatment of the aforementioned diseases are 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methyl-pyrimidine and 2,4-diamino-5-(3',4'-dichlorophenyl)-6-ethyl-pyrimidine.

Treating CNS lymphoma

Method and pharmaceutical preparations for treating meningeal leukemia, CNS Iymphoma and neoplasma in the brain which comprises treating an infected mammal such as a human with a dose of an effective treatment amount of a compound of Formula I ##STR1## where R is a straight or branched chain lower alkyl of 1 to 4 carbon atoms, and X is a halogen atom (fluorine, chlorine, bromine or iodine) and pharmaceutically acceptable salts thereof. Preferred compounds for treatment of the aforementioned diseases are 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methylpyrimidine and 2,4-diamino-5-(3',4'-dichlorophenyl)-6-ethylpyrimidine.

Treatment of meningeal leukemia with diamino dichlorophenyl pyrimidine

Method and pharmaceutical preparations for treating meningeal leukemia, CNS Iymphoma and neoplasms in the brain which comprises treating an infected mammal such as a human with a dose of an effective treatment amount of a compound of Formula I ##STR1## where R is a straight or branched chain lower alkyl of 1 to 4 carbon atoms, and X is a halogen atom (fluorine, chlorine, bromine or iodine) and pharmaceutically acceptable salts thereof. Preferred compounds for treatment of the aforementioned diseases are 2,4-diamino-5-(3',4'-dichlorophenyl)-6-methylpyrimidine and 2,4-diamino-5-(3',4'-dichlorophenyl)-6-ethylpyrimidine.

Treatment of neoplasms in the brain with diamino dichloroalkyl pyrimidine

This invention relates to purine sugar derivatives which are useful as suppressors of the immune response and as antiviral agents, and to methods of preparation thereof.

Growing community of inventors

Chapel Hill, NC, United States of America

Gertrude B Elion