Southern Research Institute

University of Minnesota

The United States of America As Represented by the Department of Health

The UAB Research Foundation (the University of Alabama at Birmingham)

William M Shannon

Thomas R Tice

Richard M Gilley

John A Montgomery

Robert Vince

William E Meyers

Jay K Staas

Y Fulmer Shealy

John H Eldridge

C Allen O'Dell

Peter K Chiang

Melinda G Hollingshead

John P Bader

H Jeanette Thomas

Guilio L Cantoni

Antiviral and antitumor compositions are disclosed comprising a mixture of AZT, ribavirin, d4T or CS-87 with a compound of general formula: ##STR1## wherein Z is H, OH or NH.sub.2, Y is CH, and X is selected from the group consisting of H, N(R).sub.2, SR, OR or halogen, wherein R is H, lower(C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically-acceptable derivatives thereof.

Antiviral combination comprising nucleoside analogs

A method of delivering a bioactive agent to an animal entailing the steps of encapsulating effective amounts of the agent in a biocompatible excipient to form microcapsules having a size ranging from between approximately one micrometer to approximately ten micrometers and admnistering effective amounts of the microcapsules to the animal. A pulsatile response is obtained, as well as mucosal and systemic immuity. Related compositions are also provided.

Method of potentiating an immune response

There is disclosed, in one aspect, a long-acting biocidal composition. This composition comprises a chlorine dioxide-liberating compound, such as sodium chlorite, and sufficient organic acid-generating compound, such as poly(lactic acid), to lower the pH of the composition to less than about 7. The organic acid-generating compound is present in a form whereby it is released gradually in the presence of water. Preferably the organic acid-generating compound is encapsulated within or by a film-forming polymer. In another aspect, there is disclosed a method of disinfecting a surface over a prolonged period of time. This method comprises applying to the surface a small but effective amount of the long-acting biocidal composition described above.

Long-acting biocidal compositions and method therefor

There is provided a method for the treatment of viral infections by treating a host animal with a pharmaceutically effective amount of a carbocyclic analog of a nucleoside represented by Formula I: ##STR1## wherein X is chlorine, bromine, iodine, a lower alkyl group or an amino group of the formula --NHR.sup.2 wherein R.sup.2 is a lower alkyl group; and R and R' can be the same or different members selected from the group consisting of hydrogen, an alkanoyl group or an aroyl group.

Carbocyclic analogs of uracil nucleosides as antiviral agents

5'-Deoxy-5'-(isobutylthio)-3-deazaadenosine and a method for preparation of same. In the preparation, 3-deazaadenosine is utilized as a starting material and is chlorinated at the 5' position. Subsequently, the chloro group is converted to isobutylthio by reaction with isobutyl mercaptan in ethanol containing sodium methoxide giving the desired compound. A most preferred starting material, i.e., 3-deazaadenosine, was prepared according to the method of Montgomery et al, J. Heterocyclic Chem., 14:195 (1977). The key fusion of this process is 4,6-dichloroimidazo[4,5-c]pyridine with 1,2,3,5-tetra-O-acetyl-.beta.-D-ribofuranose, which, after removal of protective groups and reductive dechlorination of the chlorine at 6, gives 3-deazaadenosine. This new compound has good activity as an adenosylhomocysteine (AdoHcy) hydrolase inhibitor and has shown activity against Rous sarcoma virus (RSV) in chick embryo cells and Gross murine leukemia virus (Gross MLV) in mouse embryo cells, where the activity is as a non-competitive inhibitor of AdoHcy hydrolase showing A K.sub.i of 0.4 mM.

5'-Deoxy-5'-(isobutylthio)-3-deazaadenosine, method of making same and

Growing community of inventors

Birmingham, AL, United States of America

William M Shannon