Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10.degree. C. ##STR1## wherein R.sub.1 and L are as defined herein.

Abstract: Glutamic acid derivatives in which the amino group is substituted with a 2-amino-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-ylalkyl-Z-carbonyl group, in which Z is a divalent, five-membered, nitrogen-containing heterocyclic ring system optionally containing a sulfur or nitrogen atom as a second hetero ring member, are antineoplastic agents. A typical embodiment is N-{3-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)e thyl]-pyrazol-5-ylcarbonyl}-L-glutamic acid.

Abstract: Neuroprotective agents have forumula I ##STR1## wherein a is a ring of 6 to 8 members; n and n' are 1 or 2,R.sub.2 is hydrogen or oxygen of carbonyl,R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 independently include hydrogen, alkyl, aralkyl, and carboxyalkyl.

Abstract: The invention provides a compound of formula (I) wherein A, B, X, Y and R are as defined in the description, and a process for preparing them. The compounds of formula (I) arc useful as pharmaceuticals for the treatment of glaucoma and myopia.

Abstract: Described are antibacterial agents of formula (I): X is O, S or N--R.sub.8 ; R.sub.1, R.sub.2, R.sub.3 and R.sub.8 are independently H, straight or branched alkyl of 1-6 carbons, cycloalkyl of 3-6 carbons, alkenyl or alkynyl of from 2 to 6 atoms, R heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur, or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, CO.sub.2 R, COR, CON(R).sub.2, CON(R").sub.2, SR, SON, SCO.sub.2 R or SCON(R).sub.2 ; R.sub.4 is H, straight or branched alkyl of from 1-6 carbon atoms, alkenyl or alkynyl of from 2 to 6 atoms, heterocyclic ring of from 5-8 atoms with 1-3 heteroatoms as nitrogen, oxygen or sulfur or phenyl, all of which rings may be optionally substituted up to 3 times by halogen, OR, NR.sub.2, NR'COR', CN, CO.sub.2 R' or CONR.sub.2 ', halogen, CN, NO.sub.2, N(R).sub.2, NRCOR, NRCOR", COR, CO.sub.2 R, CON(R).sub.2, CON(R").sub.2, NRCON(R).sub.

Abstract: A process is described for the preparation of an aryl-1,3-5-triazine compound of formula (1). This process comprises reacting an aldehyde compound of formula (2) with biuret, compound of formula (3), in hydrochloric medium or with methyl sulfate (1.sup.st reaction step), then oxidizing the resulting compound of formula (4) to the compound of formula (5) or (6) (2.sup.nd reaction step) and subsequently chlorinating the compound so obtained to the compound of formula (1) (3.sup.rd reaction step) according to the following scheme: ##STR1## In the above scheme: R.sub.1 and R.sub.2 are each independently of the other hydrogen; hydroxy or C.sub.1 -C.sub.5 alkoxy. The compounds of formula (1) are used as UV absorbers or as starting products for the preparation of UV absorbers.

Abstract: This invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C.sub.1-6 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, aryl or aryl C.sub.1-6 alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, trifluoromethyl, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)amino, carboxyl, C.sub.1-6 alkyloxycarbonyl or C.sub.1-6 alkylcarbonyl; R.sup.5 is hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, or a radical of formula --NR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are each independently selected from hydrogen, C.sub.1-6 alkyl, phenyl or phenylC.sub.1-6 alkyl; R.sup.7 is hydrogen or C.sub.1-6 alkyl; or R.sup.6 and R.sup.7 taken together may form a bivalent radical of formula --R.sup.6 --R.sup.

Abstract: The invention relates to pyrazolo[3,4d]pyrimidin-4(5H)-ones and pyrazolo[3,4-d]pyrimidine-4(5H)-thiones and their tautomers and pharmaceutically acceptable salts, which contain a benzyl radical in the 2-position, processes for their preparation and their use as medicaments, in particular for the treatment of epilepsies of various forms and of allergic/asthmatic diseases.

Abstract: A method of preparing tris(2-hydroxyethyl)isocyanurate (THEIC) is disclosed. The method comprises the step of heating a mixture of ethylene carbonate and isocyanuric acid in the presence of a catalyst at a temperature between about 160.degree. C. and 170.degree. C. The molar ratio of ethylene carbonate to isocyanuric acid is at least about 3 to 1, and the catalyst has at least one amine functional group. THEIC produced by the disclosed method can be used without purification as a cross-linking agent in polyester-based magnet wire enamels.

Abstract: A compound of Formula (I): ##STR1## or pharmaceutical acceptable salts thereof wherein X is S(O).sub.g or O; R.sub.2 is H, methyl, or OH; R.sub.3 and R.sub.4 are independently H or halo; R.sub.5 is H, C.sub.1-12 alkyl, optionally substituted with one or more halo, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy; and g is 0, 1, or 2. The compounds are useful antimicrobial agents.

Abstract: The invention relates to pharmaceutically useful pyrazolo[3,4-d]pyrimidinedione compounds, processes for their production, pharmaceutical compositions containing them and their use for the treatment of various diseases.

Abstract: Cyclic amine monomers and polymers and N-halamine biocidal polymer compounds are provided. Representative monomers have the structure: ##STR1## wherein R.sup.1 is selected from the group consisting of hydrogen and from C.sub.1 to C.sub.4 alkyl; R.sup.10 is a bond or parasubstituted phenyl; and R.sup.11 is cyclic amine unit of a 5- to 6-membered heterocyclic ring selected from the group consisting of: (a) 1,3,5-triazine-2,4-dione; (b) 3,4,5,6-tetrahydro(1H)pyrimidin-2-one; and (c) 2-oxazolidinone; R.sup.10 is attached to a linkage carbon of R.sup.11, wherein said linkage carbon of R.sup.11 is a carbon located on the ring of R.sup.11 and is substituted with a substituent selected from the group consisting of C.sub.1 -C.sub.4 alkyl, benzyl, and alkyl-substituted benzyl; from 0 to 2 non-linkage carbon members are a carbonyl group; and from 0 to 1 non-linkage carbon member is substituted with a moiety selected from the group consisting of C.sub.1 -C.sub.

Abstract: The novel compounds of formula I: whereinR.sup.1 represents an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl, or aryl group, or an optionally substituted cycloalkyl or cycloalkenyl group, in which one CH.sub.2 group may also be replaced by O, S or NR.sup.2, in which R.sup.2 represents a hydrogen atom or an alkyl group;X represents a hydrogen or halogen atom, or an alkoxy, aryloxy, aralkyloxy, haloalkoxy, alkylthio, cyano, amino, alkylamino or dialkylamino group;L.sup.1, L.sup.2, L.sup.3, L.sup.4 and L.sup.5 each independently represent an hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group or a nitro or cyano group show selective fungicidal activity. The new compounds are processed with carriers and, optionally, adjuvants, to afford fungicidal compositions, useful in agricultural applications.

Abstract: The present invention concerns new s-triazines of the formula ##STR1## wherein W.sup.1, W.sup.2 and W.sup.3 each independently signifies C.sub.1 -C.sub.20 alkyl or a group SpSil;X.sup.1, X.sup.2 and X.sup.3 each independently signifies O or NH;Sp signifies a spacer group;Sil signifies a silane, an oligosiloxane or a polysiloxane moiety; with the proviso that at least one of W.sup.1, W.sup.2 and W.sup.3 signifies SpSil.

Abstract: New quinazolines are described of general formula (I), in which Ar is an unsubstituted phenyl group or a phenyl group mono-substituted with a methoxy, ethoxy or methyl group; an unsubstituted pyridyl group (2-, 3- or 4-yl) or a pyridyl group mono-substituted with a methoxy or methyl group; an unsubstituted furyl group (2- or 3-yl) or a furyl group substituted with a methoxy or methyl group; a benzofuryl group (2- or 3-yl); an indolyl group (2- or 3-yl); a thiophenyl group (2- or 3-yl); a naphthyl group (1- or 2-yl) and their salts obtained from pharmaceutically acceptable inorganic or organic acids. These new quinazolines are useful in the treatment of hypertension, congestive heart failure, prostate hypertrophy, various urinary tract disorders and pathological symptoms caused by hyperactivity or disfunctioning of the noradrenergic neural system.

Abstract: N-(substituted aryl)?1,2,4!triazoloazinesulfonamide compounds, such as N-(2,6-difluorophenyl)-8-fluoro-5-methoxy?1,2,4!triazolo?1,5-c!pyrimidine- 2-sulfonamide, were prepared at a good reaction rate and in good yield by the reaction of a chlorosulfonyl?1,2,4!triazoloazine compound, such as 2-chlorosulfonyl-8-fluoro-5-methoxy?1,2,4!triazolo?1,5-c!pyrimidine, and an arylamine compound, such as 2,6-difluoroaniline, in an organic medium containing a relatively acidic alcohol, such as propylene glycol or 2,2,2-trifluoroethanol.