Abstract: The present invention is directed to certain 2'-fluoro, 2-substituted purine nucleosides which are toxic to cancerous cell lines.

Abstract: 2'-Deoxy-4'-thio-ribonucleosides, intermediates in their production, and their use as antiviral and anticancer agents are disclosed.

Abstract: The specification discloses the compounds of formula I ##STR1## wherein (a) --CH.sub.2 Ar represents ##STR2## in which R.sub.1 represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, benzyloxy, hydroxy or trifluoromethyl; and R.sub.2 represents hydrogen, halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkoxy, benzyloxy, hydroxy or trifluoromethyl; provided that R.sub.2 represents hydrogen or C.sub.1 -C.sub.3 -alkyl if R.sub.1 represents trifluoromethyl, or that R.sub.1 represents hydrogen or C.sub.1 -C.sub.3 -alkyl if R.sub.2 represents trifluoromethyl; or(b) --CH.sub.2 Ar represents ##STR3## in which X represents sulfur or oxygen and in which attachment to the thiophene or furan ring is at the 2- or 3-position; and tautomers thereof; as purine nucleoside phosphorylase inhibitors.

Abstract: The present invention provides for the preparation and use of ribo- and deoxyribo-nucleosides and polynucleotide analogs. The polynucleotide analogs are made of polynucleosides which contain sulfonate and sulfonamide linkages.

Abstract: Laser marking systems (60, 80, 160, 250) having increased part throughput are obtained by disposing diffractive optics (70, 70A, 94, 170, 252) across a primary laser beam. Preferred diffractive optics for high power marking lasers are defined in optical materials with discrete surface levels.

Abstract: 2',3'-dideoxy-4'-thioribonucleosides useful as antiviral agents in the treatment and prevention of AIDS are disclosed. In accordance with one aspect of the invention there are provided compounds of the formula ##STR1## where X.dbd.H, N.sub.3 or F, and B is a member selected from the group consisting of pyrimidine, 5-azapyrimidine, 6-azapyrimidine, 3-deazapyrimidine, purine, 3-deazapurine, 7-deazapurine, 8-azapurine, and 2-azapurine bases. The intermediate 1-O-acetyl-5-O-t-butyldiphenylsilyl-4-thio-2,3-dideoxyribofuranose is useful in the production of certain of the 2',3'-dideoxy-4'-thioribonucleosides. Other intermediates include the 4-thio-2,3-dideoxyribofuranose having different hydroxyl protecting groups and leaving groups.

Abstract: The present invention is directed to certain 2'-fluoro, 2-substituted purine nucleosides which are toxic to cancerous cell lines.

Abstract: Disclosed is a compound of the formula ##STR1## wherein R.sup.1 is H, NH.sub.2, or OCH.sub.3, R.sup.2 is an optionally substituted cyclic group optionally containing one or more heteroatoms, R.sup.3 and R.sup.4 are independently H or C.sub.1-4 alkyl, m is 0-4, n is 0-6, p is 0.1, X is CN, CSNH.sub.2, PO(OH).sub.2, COOH, SO.sub.2 NH.sub.2, NH.sub.2, OH, CNHNH.sub.2, tetrazole, triazole, or COR.sup.5 where R.sup.5 is C.sub.1-4 alkyl, CF.sub.3, NH.sub.2, or OC.sub.1-4 alkyl, and Y is O or NH that is useful as a pharmaceutical.

Abstract: 2'3'-dideoxy-4'-thioribonucleosides useful as antiviral agents in the treatment and prevention of AIDS are disclosed. In accordance with one aspect of the invention there are provided compounds of the formula ##STR1## where X=H, N.sub.3 or F, and B is a member selected from the group consisting of pyrimidine, 5-azapyrimidine, 6-azapyrimidine, 3-deazapyrimidine, purine, 3-deazapurine, 7-deazapurine, 8-azapurine, and 2-azapurine bases.The intermediate 1-O-acetyl-5-O-t-butyldiphenylsilyl-4-thio-2,3-dideoxyribofuranose useful in the production of certain of the 2',3'-dideoxy-4'-thioribonucleosides is also disclosed.

Abstract: Substituted 1-(benzyloxy)adenosines and the use of substituted 1-(benzyloxy)adenosines and adenosine-N.sup.1 -oxides in the prevention and treatment of vaccinia virus infections are disclosed.

Abstract: 5,10-Dialkyl substituted 5,10-dideazaaminopterins and a cyclized derivative thereof are disclosed as potent antineoplastic agents. Also disclosed is an improved process for the preparation of 10-ethyl-10-deazaaminopterin using the intermediate methyl 4-[[2-(2,4-diamino-6-pteridinyl)-1-ethyl]ethenyl]benzoate.

Abstract: There are disclosed nucleosides having Formula I: ##STR1## wherein R is H or acyl. These compounds have anticancer activity.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted heteroalicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted alicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is optionally substituted pyridinyl, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: Disclosed is a compound containing 2-amino-7-(R)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein R is optionally substituted cyclohexenyl or cyclohexyl, a pharmaceutical composition containing the compound, and a method for the selective suppresion of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: It is disclosed that 5-methyl-5-deazamethotrexate and 5-methyl-5-deaza-10-ethylaminopterin are more than 10 times as potent as 5-deazamethotrexate in the L1210 cell growth inhibition test.

Abstract: 1,2-Dihydropyrido[3,4-b]pyrazines are provided which possess anticancer activity. The compounds have the structure: ##STR1## wherein Y is CH.sub.2 or N(CH.sub.3); R.sub.1 is a lower alkyl group; e.g., an alkyl group containing up to six carbon atoms such as methyl, ethyl, propyl, butyl, etc.; R.sub.2 is a member selected from the group consisting of hydrogen, CH.sub.3 O or Cl; and R.sub.3 and R.sub.4 are either both hydrogen or one is hydrogen and the other is a lower alkyl group.

Abstract: There are disclosed novel intermediates useful in the preparation of pyrido[2,3-d]pyrimidines having the following structures: ##STR1## wherein R is CH.sub.3, CH.sub.3 CH.sub.2, CH.sub.3 CH.sub.2 CH.sub.2, CH.sub.2 .dbd.CHCH.sub.2 or CH.tbd.CCH.sub.2 ; and ##STR2## wherein R is CH.sub.3, CH.sub.3 CH.sub.2, CH.sub.3 CH.sub.2 CH.sub.2, CH.sub.2 .dbd.CHCH.sub.2 or CH.tbd.CCH.sub.2. These intermediates have the formulas: ##STR3## wherein Y is CHO, CH.sub.2 OH or CH.sub.2 Br; and Z is CH.sub.2 OH or CH.sub.2 Br.

Abstract: The present invention is a method for making radar chaff consisting of metal rings having varying diameters, using photolithographic processes. One aspect of the invention has the steps of: providing a metal foil having a thickness suitable for use in radar chaff; overcoating the metal foil with a photoresist, to form a layered structure; undercoating the metal foil with a removable backing; exposing the photoresist to a quantity of actinic radiation for chemically modifying the photoresist into a photoproduct suitable for subsequent development, where the actinic radiation is patterned into a series of concentric rings; developing the photoresist, to expose the underlying metal in a series of concentric rings; removing the exposed metal to form a series of concentric metal rings on the removable backing; and removing the removable backing. Another aspect of the invention is a metal chaff precursor, comprising: a removable backing, coated with a plurality of concentric metal foil rings.