Abstract: The invention relates to novel substituted iminoazines of the general formula (I) in which R1, R2, R3, R4, Z1, Z2 and Z3 are each as defined in the disclosure, to a plurality of processes for their preparation, and to their use as herbicides.

Abstract: Agents for coloring keratinic fibers are provided which contain specific m-phenylenediamine derivatives such as N-2-(morpholine-4-yl)ethyl-m-phenylenediamine, N-3-(morpholine-4-yl)propyl-m-phenylenediamine, and N-3-(imidazole-1-yl)-propyl-m-phenylenediamine.

Abstract: This application relates to isotopically labeled affinity markers of the formula (II) for mass spectrometric analysis of proteins. In formula (II), the groups A, PRG, S, Z, L', Z', R, R', k, l, m, and n are as defined in the claims. The application also provides a process for preparing these materials, a method for analyzing proteins using such materials, and a kit containing one or more of these materials.

Abstract: Quinazoline and pyrido[2,3-d]pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, L, Y1, Y2, Y3 and Z are as described herein, are provided which are useful in treating T-cell mediated diseases.

Abstract: The present invention is directed, in part, to fluorescent metal sensors for detecting metal ions, and methods of making and using the same.

Abstract: The present invention is directed to ceramide analog compounds of general formula (I) the process for their preparation and use for the preparation of pharmaceutical formulations for the treatment of tumors.

Abstract: Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.

Abstract: Exploitation of suitably functionalized heterocyclic molecules, in the design and synthesis of Fluorescence Resonance Energy Transfer (FRET) cassettes and their corresponding dideoxynucleotide terminators culminated into efficient reagents for DNA sequencing. Additionally, these FRET cassettes/terminators, of the present invention, derived from different classes of heterocyclic systems have high potential to be used for general labelling of biological molecules to generate highly sensitized signals. Their preparation, energy transfer efficiency, and use as labels, specifically, in DNA sequencing reactions is disclosed.

Abstract: The present invention provides hydroxypyridinone and hydroxypyrimidone chelating agents. Also provides are Gd(III) complexes of these agents, which are useful as contrast enhancing agents for magnetic resonance imaging. The invention also provides methods of preparing the compounds of the invention, as well as methods of using the compounds in magnetic resonance imaging applications.

Abstract: The invention relates to the synthesis of polymers containing self-complementary quadruple hydrogen groups by copolymerizing monomers containing a quadruple hydrogen bonding group with one or more monomers of choice. The resulting polymers show unique new characteristics due to the presence of additional physical interactions between the polymer chains that are based on multiple hydrogen bonding interactions (supramolecular interactions).

Abstract: The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain, cyclic or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In a preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier. In addition, the invention includes methods of preparing synthetic receptors and synthetic receptor libraries. The synthetic library may be linked with identifiers such that the library comprises a plurality of different synthetic receptor members.

Abstract: The preparation of sultams is disclosed. In one embodiment (e.g. scheme (I)), an alkanesulfonyl halide is reacted with a haloalkylamine to obtain the corresponding N-(haloalkyl)alkanesulfonamide which is then cyclized in the presence of a deprotonating agent to give the sultam. The sultams are useful as intermediates in the preparation of naphthyridine carboxamide compounds which are HIV integrase inhibitors.

Abstract: Sequence-specific oligonucleotides are provided having substantially pure chiral Sp phosphorothioate, chiral Rp phosphorothioate, chiral Sp alkylphosphonate, chiral Rp alkylphosphonate, chiral Sp phosphoamidate, chiral Rp phosphoamidate, chiral Sp phosphotriester, and chiral Rp phosphotriester linkages. The novel oligonucleotides are prepared via a stereospecific SN2 nucleophilic attack of a phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate anion on the 3′ position of a xylonucleotide. The reaction proceeds via inversion at the 3′ position of the xylo reactant species, resulting in the incorporation of phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate linked ribofuranosyl sugar moieties into the oligonucleotide.

Abstract: The invention relates to the synthesis of polymers containing self-complementary quadruple hydrogen groups by copolymerizing monomers containing a quadruple hydrogen bonding group with one or more monomers of choice. The resulting polymers show unique new characteristics due to the presence of additional physical interactions between the polymer chains that are based on multiple hydrogen bonding interactions (supramolecular interactions).

Abstract: A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon, which is obtained by nitrosylation of a carbon acid having a pKa less than about 25, is useful as an NO donor. When the compound is obtained from a carbon acid with a pKa less than about 10, it provides vascular relaxing effect when used at micromolar concentrations and this activity is potentiated by glutathione to be obtained at nanomolar concentrations. When the compound is obtained from a carbon acid with a pKa ranging from about 15 to 20, vascular relaxing effect is obtained at nanomolar concentrations without glutathione. In another embodiment, a biocompatible polymer incorporates a C-nitroso moiety.

Abstract: A subject of the invention is the compounds of formula in which Y represents a hydrogen atom or a fluorine atom, n represents an integer comprised between 1 and 8, Z represents a hydrogen atom or the remainder of a carboxylic acid, optionally substituted on the heterocycle by one or more alkyl, alkenyl, alkynyl, O-alkyl, O-alkenyl, O-alkynyl, S-alkyl, S-alkenyl, S-alkynyl radicals containing up to 8 carbon atoms, one or more OH, NH2, C═N, NO2, CF3 radicals or one or more aryl radicals containing up to 14 carbon atoms or heteroaryl radicals containing one or more nitrogen oxygen or sulphur atoms, the aryl or heteroaryl radicals themselves being able to be substituted as well as their addition salts with acids, The products of formula (I) have antibiotic properties.

Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.

Abstract: A silver halide photosensitive material contains a compound of the following general formula (I): 1

Abstract: A sodium salt of Compound A is disclosed, wherein Compound A is of formula: 1

Abstract: The present invention provides for a method for inhibiting growth of a bacterium which consists essentially of contacting the bacterium with a compound having the structure: 1

Abstract: Sterically hindered N-substituted alkoxyamines are prepared by the transition-metal-catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitroxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.

Abstract: Compounds of the formula: where R1, R2, R3, R4, R5, R6, R7, R8, R′5, R′6, R′7, R′8 are hydroxy —NO2, —CN, —CF3, —CONH2, C1-12alkyl, phenyl, naphthyl, phenanthryl, anthryl, R9R10N—, R9—O—or R9—S—, —CONHR10, —CONR9R10 in which R9 and R10 are C1-C6-alkyl, C6-C10-aryl, (C6-C10)-aryl-(C1-C6)-alkyl or (C1-C6)-alkyl-(C6-C10)-aryl, in which the alkyl and/or aryl radicals can optionally be substituted by hydroxyl, C1-C6-alkoxy, C6-C10-aryloxy or halogen; and optionally, two adjacent groups can form an isocyclic or heterocyclic group; are eminently suitable for the mass coloring of polymers, in particular polar polymers, for coloring toners, powders and powder coating materials as well as for coloring ink-jet inks.

Abstract: Methods of using compounds of formula (I): 1

Abstract: The invention relates to serine protease inhibitor compounds of formula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl, amino, hydroxy, or oxo; and R is X—X—Y(R7)—L—Lp(D)n; wherein each X independently is a C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the &agr;-atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylalkenyl, aralkyl, heteroaryl-alkyl

Abstract: The invention is directed to novel cyclic organoselenium compounds useful as antioxidants, pharmaceutical compositions containing them, and methods for their preparation.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemiia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: Fuel additives comprise a compound having a group represented by the formula >C═=N—  (1). Also disclosed are fuel compositions containing such additives. The additives have a superior detergent effect to conventional gasoline detergents and an excellent detergency of the injection nozzles of a diesel engine and is free from being sludge.

Abstract: The invention provides conjugated polymers that have good solubility and semiconductivity, and that display high photoluminescent and electroluminescent efficiency.

Abstract: A compound of formula (I), or a pharmaceutically-acceptable salt thereof, wherein A is an optionally substituted 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 ring heteroatoms; B is optionally substituted phenylene or a 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen heteroatoms; R and R1 are hydrogen or (1-4C)alkyl; n is 1 or 2; R2 and R3 are hydrogen, (1-6C)alkyl, (4-7C)cycloalkyl, or (2-6C)alkenyl, or R2 and R3 may form along with the nitrogen to which they are attached a 5-, 6- or 7-membered heterocyclic ring, wherein each R2 or R3 group or any heterocyclic ring formed from R2 and R3 may be optionally substituted with various substituent groups, and wherein Q may be optionally substituted by various substituent groups, which posseses antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals.

Abstract: The present invention relates to a triazine type monomer, and more particularly, to a 1,3,5-triazine type monomer characterized by having at least one amine group and at least two sulfur atoms, which can be used in manufacturing transparent optical resins having excellent refractive index, surface hardness and absorbance as well as an improved workability and the ability to control a wide range of refractive index according to the change in composition by the monomer itself at room temperature or by polymerizing the monomer with a comonomer in the presence of an organic solvent or an initiator.

Abstract: Compounds of formula (I): their racemates, enantiomers, diastereoisomers and inorganic acid salts and organic acid salts thereof, processes for preparing them and the medicaments containing them are discussed.

Abstract: Novel monocyclic L-Nucleoside compounds have the general formula 1

Abstract: The present application describes novel cyclic sulfonyl derivatives of formula I: 1

Abstract: The invention provides novel conjugated polymers comprised of arylamine-substituted poly(arylene vinylenes). The polymers have the general structure (I) wherein: Ar is arylene, heteroarylene, substituted arylene or substituted heteroarylene containing one to three aromatic rings; R1 is an arylamine substituent having the formula —Ar1—N(R4R5) wherein Ar1 is as defined for Ar and R4 and R5 are independently hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl, or together form a cyclic group; and R2 and R3 are independently selected from the group consisting of hydrido, halo and cyano, or may be as defined for R4 and R5, or may together form a triple bond. Monomeric precursors and methods of synthesizing the precursors are also provided, as are electroluminescence and other devices containing a polymer of the invention.

Abstract: Serine protease inhibitors, prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. The serine protease inhibitors exhibit anticoagulant activity and are useful for treating or preventing thrombin related diseases.

Abstract: Compounds represented by the following formula I: in which: R1 to R5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected from (CR6R7)n in which n=0 or 1, and CO are disclosed. These compounds are useful as anti-tumor drugs, especially with pro-oxidizing activity.

Abstract: The present invention provides a compound of formula I 1

Abstract: Compositions having a texaphyrin-lipophilic molecule conjugate loaded into a biological vesicle and methods for imaging, diagnosis and treatment using the loaded vesicle are provided. For example, liposomes or red blood cells loaded with a paramagnetic texaphyrin-lipophilic molecule conjugate have utility as a blood pool contrast agent, facilitating the enhancement of normal tissues, magnetic resonance angiography, and marking areas of damaged endothelium by their egress through fenestrations or damaged portions of the blood vascular system. Liposomes or cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate can be photolysed, allowing for a photodynamic therapy effect at the site of lysis. Availability of red blood cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate provides a method for delivering a photodynamic therapeutic agent to a desired site with a high concentration of oxygen.

Abstract: The invention provides novel conjugated polymers comprised of arylamine-substituted poly(arylene vinylenes). The polymers have the general structure (I) wherein: Ar is arylene, heteroarylene, substituted arylene or substituted heteroarylene containing one to three aromatic rings; R1 is an arylamine substituent having the formula —Ar1—N(R4R5) wherein Ar1 is as defined for Ar and R4 and R5 are independently hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl, or together form a cyclic group; and R2 and R3 are independently selected from the group consisting of hydrido, halo and cyano, or may be as defined for R4 and R5, or may together form a triple bond. Monomeric precursors and methods of synthesizing the precursors are also provided, as are electroluminescence and other devices containing a polymer of the invention.

Abstract: Described are benzoxazine and benzothiazine compounds of the formula I defined herein, methods for their preparation and methods for their use in pharmaceuticals based on their activity as NO-synthases (NOS) inhibitors.

Abstract: Compositions having a texaphyrin-lipophilic molecule conjugate loaded into a biological vesicle and methods for imaging, diagnosis and treatment using the loaded vesicle are provided. For example, liposomes or red blood cells loaded with a paramagnetic texaphyrin-lipophilic molecule conjugate have utility as a blood pool contrast agent, facilitating the enhancement of normal tissues, magnetic resonance angiography, and marking areas of damaged endothelium by their egress through fenestrations or damaged portions of the blood vascular system. Liposomes or cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate can be photolysed, allowing for a photodynamic therapy effect at the site of lysis. Availability of red blood cells loaded with a photosensitive texaphyrin-lipophilic molecule conjugate provides a method for delivering a photodynamic therapeutic agent to a desired site with a high concentration of oxygen.

Abstract: The present invention provides an intermediate for producing a thienopyridine derivative useful as a GnRH antagonist as well as an efficient and safe method for producing the same in an industrial scale at a high yield.

Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: The current invention concerns the use of a receptor from the RZR/ROR receptor family or of a functional fragment thereof in a test of a compound for anti-autoimmune, anti-arthritic, anti-tumor, melatonin-like and/or melatonin-antagonistic activity and the production of a receptor ligand complex comprising said receptor or a functional fragment thereof and a ligand of said receptor. Described is also a method for testing compounds for said activity (screening for ligands) and the active compounds identified therewith.

Abstract: Naphthalene derivatives of the formula [I]: wherein R1 and R2 are the same or different and are each H, protected or unprotected OH, one of R3 and R4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R5 and R6 are, the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.

Abstract: The use of linear or cyclic silicon compounds containing at least one chromophoric group of quinone or azo type as direct dyes in dye compositions intended for dyeing human keratin fibres and in particular the hair. The invention also relates to novel silicon compounds and dye compositions containing them, as well as to the corresponding direct dyeing process.

Abstract: The use of linear or cyclic silicon compounds containing at least one chromophoric group of quinone or azo type as direct dyes in dye compositions intended for dyeing human keratin fibers and in particular the hair. The invention also relates to novel silicon compounds and dye compositions containing them, as well as to the corresponding direct dyeing process.

Abstract: Non-crystallizing N,N′-disubstituted N-(2-hydroxyalkyl)-ureas are used as hydrolysis protection agents in plastics containing ester groups. These disubstituted hydroxy-alkylureas impart excellent protection from hydrolysis to plastics containing ester groups and can be added directly to the plastics to be stabilized without the addition of special solvents.

Abstract: Benzophenoxazine compounds have formula (I) where X is O or NH, Y is NR.sup.1 R.sup.2 or H, R.sup.1 and R.sup.2 are alkyl or -L-A, L is a linker and A may be a reactive group by means of which the compound is linked to a biomolecule. The compounds can be used as fluorescent dyes for labelling biomolecules.

Abstract: The invention relates to a method of producing a mixture of a quaternary ammonium compound, fatty acid, fatty acid ester and tertiary amine salt in situ which is a highly functional mixture that is manufactured in a single step reaction whereby quaternization is completed without the aid of solvents, especially flammable solvents. The single step reaction process eliminates separate blending of individual components. The compositions obtained can be used as fabric softeners, in modified clays, as hair treating compounds and as disinfectants.