Abstract: The compound 2-amino-5,6-dichloro-3,4-dihydroquinazoline has been found to have enhanced platelet count reducing properties. Also provided are methods for synthetically making the compound and a method of reducing the platelet count in a patient by administering to the patient a platelet reducing effective amount of the compound preferably together with a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which contains the above compound as the active ingredient together with pharmaceutically acceptable excipients.

Abstract: A process for making alpha-HMX comprises the steps of: (a) combining phosphorus pentoxide and nitric acid at a temperature of about 0-25° C., forming a reaction mixture; and (b) adding a compound having the formula: wherein R is straight chain or branched alkyl having 1-5 carbon atoms, to the reaction mixture, whereby a product comprising alpha-HMX is produced.

Abstract: Pyrimidinone derivatives of the general formula: wherein R1 is hydrogen or alkyl; R2 is haloalkyl; R3 is nitrogen or CH; G is optionally substituted ethylene, trimethylene, or vinylene; and Q is selected from several optionally substituted or heterocyclic-condensed phenyl groups, are useful as the active ingredients of herbicides because of their excellent herbicidal activity.

Abstract: The invention is directed to a process for the separation of oxygen from an oxygen containing gas using an oxygen selective material comprising a transition element complex comprising a first transition element ion and one or more chelating ligands, wherein: i) said first transition element ion is capable of accepting intermolecular donation; ii) said chelating ligand or ligands provides up to four intramolecular donor sites to said transition element ion; iii) said chelating ligand or ligands provides an intermolecular donor site to a second transition element ion which is contained in second discrete transition element complex; and iv) said chelating ligand or ligands contains at least one substituent that inhibits &mgr;-peroxo dimer formation on said sorbent; wherein when said material is in deoxy form, the total number of donor sites to said first transition element ion is five.

Abstract: Disclosed are novel prodrugs represented by the following structural formula: Z is oxygen or sulfur; Y is, together with a hydroxy group, acyclovir or an analog of acyclovir; A is a substituted benzyl group with one or more protected hydroxy or protected amine groups in the ortho or para positions, relative to the phosphate ester, which can be converted in vivo to a hydroxy or amino group. Also disclosed is a method of treating a viral infection in an individual or animal. The method comprises administering to the individual or animal a therapeutically effective amount of a prodrug represented by structural formula shown above.

Abstract: A method for removing heavy metals, selected from palladium, tin and nickel, from heavy metal complexes with thiazole compounds in aqueous or alcoholic solution, by precipitation as sulfides, characterised in that such solutions are treated with a water-soluble ammonium, alkaline or alkaline-earth sulfide.

Abstract: The present invention relates to a process for preparing acid amides by reacting an acid with an aliphatic amine in molten urea. This invention also concerns a process for metalating compounds which can be bonded to a metal ion by reacting the compound with a metal ion in molten urea. Furthermore, the invention deals with the thus obtained products and their use for the therapy and/or diagnosis of tumors or inflammatory diseases.

Abstract: Compounds of formulae (I) and (II) wherein the R, R1, R2, R3 and R4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.

Abstract: The present invention relates to novel tetrahydropyrimidine derivatives of the formula (I) in which A represents one of the groupings (Ia) —(CH2)m—COXR1 or (Ib) Het represents a five- or six-membered heterocyclic grouping which contains 1, 2, 3 or 4 nitrogen atoms and/or one or two oxygen or sulphur atoms as hetero atom ring members—the number of the ring hetero atoms being 1, 2, 3 or 4—and which is optionally substituted by halogen, cyano, nitro, alkyl, halogenoalkyl, alkenyl, halogenoalkenyl, alkinyl, alkoxy, halogenoalkoxy, alkenyloxy, halogenoalkenyloxy, alkinyloxy, alkylthio, halogenoalkylthio, alkenylthio, halogenoalkenylthio, alkinylthio, alkylsulphinyl, halogenoalkylsulphinyl, alkylsulphonyl, halogenoalkylsulphonyl, amino, alkylamino, dialkylamino, aryl, aryloxy, arylthio, arylamino, aralkyl, formylamino, alkylcarbonylamino, formyl, carbamoyl, alkylcarbonyl and/or alkoxycarbonyl. For other substituents see specification.

Abstract: Phosphonic acid compounds I wherein Eth is optionally substituted 1,2-ethynediyl, ethanediyl or ethene-1,2-diyl; Y1 is oxygen or sulfur; Y2 is oxygen, sulfur or —N(R6)—; Y3 is oxygen, sulfur or —N(R7)—; R1, R2, R6 and R7 are hydrogen or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or heterocyclyl, or R1 and R2, R1 and R6, R2 and R7 together are optionally substituted 1,2-ethanediyl, 1,3-propylene, tetramethylene, pentamethylene or ethyleneoxyethylene, or R1 and R2 together are optionally substituted 1,2-phenylene; R3 is cyano, halogen, alkyl, haloalkyl, alkoxy or haloalkoxy; R4 is hydrogen or halogen, and R5 is a heterocycle &PHgr;1 to &PHgr;22 as defined in the specification, their manufacture and intermediates therefore. The phosphonic acid compounds are effective against unwanted plants and act as desiccants and defoliants.

Abstract: A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.

Abstract: Phospholipid derivatives of Formula X: wherein A is the ring system in which R is a linear or branched alkyl radical having 10 to 24 carbon atoms which may contain one or more double or triple bonds; R1 and R2 are independently hydrogen or linear alkyl radicals having 1 to 3 carbon atoms; y is 0, 1, 2 or 3; m and n are independently 0 or in an integer, with the proviso that m+n is between 2 and 8; or A is a tropanio or quinuclidinio ring system, which is linked via a carbon-carbon bond and is optionally substituted by one or more methyl groups; processes for the preparation of the derivatives, and methods for treating tumors therewith.

Abstract: 1,3 Diazines and pharmaceutically acceptable salts thereof inhibit phosphorylation of platelet-derived growth factor receptor and thereby hinder abnormal cell growth and cell wandering. The compounds may be used to treat or prevent cell-proliferative disorders such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (R,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and their use for the treatment of fungal infection are also disclosed.

Abstract: Organosilane compounds having the structural formula ##STR1## wherein R is a linear or branched C.sub.1-4 alkyl, 4-methylpiperidyl, C.sub.6-12 aryl or C.sub.5-7 cycloalkyl; R.sup.1 is hydrogen, methyl or ethyl, R.sup.2 is methyl or ethyl and; n is 4 to 7.These organosilane compounds are useful as electron donors in Ziegler-Natta type catalyst systems.

Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: A process for the preparation of 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid and the salts thereof of formula (I) ##STR1## which comprises the following steps: a) carboxymethylation reaction of a suitable precursor in water, with a haloacetic acid,b) hydrolysis reaction in basic conditions by addition of the base added at the previous step.

Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles .

Abstract: The subject matter of the present invention relates to a reagent and a process useful for cleaving a functional group protected by an alkoxycarbonyl group during an organic synthesis. This reagent comprises: a) an aqueous phase; b) a catalyst comprising at least one group VIII element in the periodic table of elements and at least one water-soluble ligand, wherein the group VIII element in the periodic table is maintained in the aqueous phase by the formation of a complex with at least one water-soluble ligand; and c) a nucleophilic compound soluble in the aqueous phase; and optionally d) an organic phase.