Warner-lambert Company

Phillip D Cook

Dennis Joseph McNamara

Roland K Robins

David A Berry

3'-Acyl-2-chloro-2'-deoxy-5'-adenylic acids (I) as well as a method for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compound in dosage forms. The compounds of the invention have pharmacological properties and are useful antimicrobial agents and antitumor agents.

Deoxyadenosine compounds and methods of making and using the same

Nucleotide compounds are provided, namely 2-chloro-2'-deoxyadenosine 5'-phosphate compounds (I) especially as the monosodium and disodium salt, as well as a method for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. The compounds of the invention have pharmacological properties and are useful antimicrobial agents, antiviral agents, and antileukemic agents. ##STR1##

Methods of using 2-chloro-2'-deoxyadenosine-5'-phosphate and its salts

The aminoglycoside and aminoglycotide N.sup.4 -(2,3,5-tri-O-acetyl-.beta.-D-ribofuranosyl)pyrimido[4,5-d]pyrimidine-4,8- diamine and N.sup.4 -(5-O-phosphono-.beta.-D-ribofuranosyl-pyrimido[4,5-d]pyrimidine-4,8-diami ne exhibit antiviral activity as well as cytotoxic activity against the L1210 and mammary 16/C tumor cell lines. An improved method for their production involves the production of a sylilated intermediate and reaction of the intermediate with tetra-O-acetyl-.beta.-D-ribofuranose in the presence of the specific catalyst trimethylsilyltrifluoromethanesulfonate.

Process for preparing diaminopyrimido(4,5-d)pyrimidine glycoside and

Nucleotide and nucleoside compounds are provided, namely 2-halo-2'-deoxyadenosine 5'-phosphate compounds (I) especially as the monosodium and disodium salt, and 2-iodo-2'-deoxyadenosine (II); as well as a method for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. The compounds of the invention have pharmacological properties and are useful antimicrobial agents, antiviral agents, and antileukemic agents. ##STR1##

Compound 2-iodo-2'-deoxyadenosine

4-Amino-3-halo-1-.beta.-D-ribofuranosyl-2-(1H)-pyridinone, 4-amino-3-halo-1-(2-deoxy-.beta.-D-pentofuranosyl)-2(1H)-pyridinone, and nucleosides and 4-amino-3-halo-1-(2-deoxy-2,2-difluoro.beta.-D-pentofuranosyl)-2(1H)-pyrid inone nucleosides and nucleotides are useful as antiviral agents and possess in vivo activity against the L1210 murine leukemia cell line.

4-amino-3-halo-2-pyridinone nucleoside and nucleotide compounds

A process is provided for producing 4-carbamoyl-1H-imidazolium-5-olate (I) ##STR1## by reacting aminomalonamide H.sub.2 N--CH(CONH.sub.2).sub.2 and formamidine CH(.dbd.NH)NH.sub.2 compound in a liquid medium comprising alcohol under conditions such that the product I can be obtained in a solid form that is directly recoverable from the medium, free of aminomalonamide and recrystallizable.

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Ann Arbor, MI, United States of America

Phillip D Cook