Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.

Abstract: A pharmaceutical preparation treats Friedreich's ataxia and treats or prevents pathologies related thereto. In particular, the pharaceutical preparation concerns the use of diazoxide or 7-chloro-3-methyl-4H-1,2,4 benzothiadiazine 1,1-dioxide, in combination with glucose and/or leucine, for the treatment of Friedreich's ataxia (FRDA) and for the treatment or prevention of pathologies related thereto.

Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.

Abstract: A ligand design allows compact nanoparticle materials, such as quantum dots (QDs), with excellent colloidal stability over a wide range of pH and under high salt concentrations. Self-assembled biomolecular conjugates with QDs can be obtained which are stable in biological environments. Energy transfer with these ligands is maximized by minimizing distances between QDs/nanoparticles and donors/acceptors directly attached to the ligands or assembled on their surfaces.

Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

Abstract: The compounds of a certain formula (1), in which R1, R2, R3 and R9 have the meanings as given in the description, are novel effective PDE4 inhibitors.

Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Abstract: A pigment dispersing agent of the formula (1) capable of providing a printing ink or a coating composition excellent in fluidity and dispersion stability and a dry coating excellent in gloss, a pigment composition containing the same and a pigment dispersion containing the same, wherein X1 is —NH—, —O—, —CONH—, —SO2NH—, —CH2NH—, —CH2NHCOCH2NH— or —X3—Y—X4—, X2 and X4 are —NH— or —O—, X3 is —CONH—, —SO2NH—, —CH2NH—, —NHCO— or —NHSO2—, Y is an alkylene group, an alkenylene group or an arylene group, Z is —SO3M or —COOM, R1 is a heterocyclic ring residue or an aromatic ring residue, Q is —O—R2, —NH—R2, a halogen group, —X1—R1 or —X2—Y-Z, R2 is a hydrogen atom, an alkyl group or an alkenyl group, and M is one equivalent of a monovalent to trivalent cation.

Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.

Abstract: The invention relates to novel pyrazolopyridine derivatives of formula (I) wherein R1 represents H, Cl or NH2, and R2 and R3 form; together with the heteroatoms to which they are bonded, a five to six-membered heterocycle which can be saturated or partially unsaturated, can optionally contain at least one other heteroatom from the group N, O, S and can be optionally substituted. The invention also relates to salts, isomers and hydrates of said derivatives, in the form of stimulators of soluble guanylate cyclase and as agents for treating cardiovascular diseases, hypertonia, thrombo-embolic diseases and ischaemia, sexual dysfunction, inflammations, and diseases of the central nervous system.

Abstract: The invention relates to novel guanidine derivatives of the formula (I) in which A, R1, R2, R3 and Z are as defined in the description, to a process for their preparation and to their use for controlling animal pests.

Abstract: The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

Abstract: The invention is directed to organosilicon compounds of the general formula prepared by reacting triazine compounds with functional groups (e.g., chlorine) and corresponding compounds (e.g., mercapto). The organosilicon compounds can be used in rubber mixtures.

Abstract: Compounds of formula (I), in which R1, R2 and R3 are as defined in claim 1, are particularly suitable as herbicides.

Abstract: Compounds of formula (I) in which Qi is an unsaturated five-membered optionally substituted or condensed heterocyclic ring and X is O, S, SO or SO2, and agronomically tolerated salts/N-oxides/isomers/enantiomers of these compounds are suitable as herbicides

Abstract: There are provided novel (2-imidazolin-2-yl) fused heteropyridine compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: Compounds of the Formula (5) and processes for their preparation and use, particularly in the manufacture of unsymmetrical triphenodioxazine dyes: ##STR1## wherein: Y is H, alkyl, substituted alkyl, alkoxy, Cl or Br;R is a group of Formula (3) ##STR2## R.sup.1 and R.sup.2 are each independently alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form an optionally substituted 4, 5 or 6 membered alicyclic or heterocyclic ring;R.sup.3 is H;Z is Cl, Br or A--NH; andA is H or the residue of a primary amine.

Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.

Abstract: An improved superabrasive composition for grinding applications comprising a superabrasive material, a bismaleimide-triazine addition copolymer resin which as a cured polymer exhibits (i) a glass transition temperature (Tg) of at least about 280.degree. C. and (ii) a long term thermal resistance of at least about 180.degree. C., a free radical generating initiator, and preferably a catalyst, is disclosed. The superabrasive abrasive composition is particularly useful as a cutting edge in a high performance cutting wheel.

Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.

Abstract: Methods and apparatus for electrochemical extraction of a ligand such as molecular oxygen from a first fluid environment and for release of a ligand such as molecular oxygen, as well as ligand carrier compounds therefor comprising macrocyclic amines having the general formulas: ##STR1## where: A, B, C, D, E, and F are each nitrogen, oxygen, sulfur, or phosphorous;m, n, o, p, q, and r are each typically 2, 3, 4, 5, or 6;the R substituents are each generally H or short chain (linear or branched) alkyl, although R.sub.2 may represent ketyl (.dbd.o); andM is a suitable transition metal ion.

Abstract: A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including gastrointestinal anti-ulcerogenic and cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

Abstract: This invention relates to novel pyrazolesulfonamides, agricultural compositions thereof and the methods of their use as general and/or selective herbicides and/or plant growth regulants.

Abstract: A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including anti-ulcerogenic and gastrointestinal cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.

Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.

Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.

Abstract: Herbicidally active novel N,N'-bis-sulphonyl guanidines of the formula ##STR1## in which M is hydrogen, a metal or an ammonium radical, andR.sup.4, R.sup.5, R.sup.40 and R.sup.41 are various organic radicals.

Abstract: Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophen esulfonamide are useful as herbicides and plant growth regulants.

Abstract: The compounds of the general formula (I) ##STR1## in which X denotes O or --SO.sub.2 --, Y denotes CH or N, R.sub.1 denotes alkyl, alkenyl or (C.sub.2 -C.sub.6)-alkinyl which are optionally substituted, R.sub.2 denotes alkyl, alkenyl, alkinyl or cyclohexyl, R.sub.3 and R.sub.4 denote H or alkyl, and R.sub.5 and R.sub.6 denote H, (substituted) alkyl, (substituted) alkoxy, halogen, alkylthio, monoalkylamino or dialkylamino, and also salts thereof, possess advantageous herbicidal properties against monocotyledonous and dicotyledonous weeds and are suitable for selective use in large-scale crops. In addition, they possess a good plant growth-regulating action.

Abstract: A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including gastrointestinal anti-ulcerogenic and cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.

Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.

Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.

Abstract: Novel pyridinesulfonamide compounds containing ortho-heterocyclic substituents such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-(1H-1,2,4-triazol-1-yl)-3 -pyridinesulfonamide display utility as herbicides and plant growth regulants.

Abstract: BIS-Imido carbonate sulphones of the formula: ##STR1## in which R represents phenyl which is unsubstituted or substituted by one or two substituents, which is the same or different, selected from methyl, trifluoromethyl, nitro and cyano groups, and chlorine, flourine and bromine atoms, and p represents the integer 1, are produced by reacting a compound of formula VI ##STR2## in which R is as defined above, with thionyl chloride in the presence of an organic base. The compounds of formula II are useful in the production of 1, 2, 4, 6-thiatriazines.

Abstract: A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including gastrointestinal anti-ulcerogenic and cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.

Abstract: 1,2,4,6-Thiatriazine 1,1-dioxide ethers of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, Y, Z and n have the meanings given in the description, are used for controlling undesirable plant growth.

Abstract: This invention relates to new derivatives of oxazinobenzothiazine-6,6-dioxide, to a process for the production thereof and to the use thereof as medicaments.The new derivatives according to the present invention correspond to the general formula I: ##STR1## wherein: R represents a linear or branched lower C.sub.1 -C.sub.4 alkyl radical, in particular the methyl and ethyl radicals,X represents an oxygen atom or a sulphur atom, andHet represents a mono- or bicyclic unsaturated heterocycle containing a nitrogen heteroatom in the ortho position relative to the link between the said heterocycle and the nitrogen atom of the oxazine ring, the said heterocycle optionally containing one or two other additional heteroatoms selected from nitrogen, oxygen and sulphur, and also being able to be substituted by one or two methyl radicals.

Abstract: Novel N-alkoxycarbonyl- and N-alkoxythiocarbonyl-amidines and a process for the preparation of alkoxycarbonyl- and alkoxythiocarbonyl- amidines by reacting an amidine with an ester of chlorocarbonic acid or chlorothiocarbonic acid in the presence of an inorganic acid acceptor and a 2-phase aqueous/organic solvent mixture at from 0.degree. to 60.degree.0 C.The novel end products which can be prepared by this process are useful starting materials for crop protection agents, and can be used in particular for the preparation of novel, selective herbicides.

Abstract: There are disclosed novel 1,2,4,6-thiatriazine-1,1-dioxides and related compounds which are connected to a substituted phenyl or heterocyclic group through a linear or cyclic connecting group. Processes are provided for the preparation of such compounds. The compounds are useful for the suppression of gastric acid secretions in mammals and compositions for such uses are also disclosed.

Abstract: 1,2,4,6-Thiatriazine-1,1-dioxides of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, Y and n have the meanings given in the description, are used for controlling undesirable plant growth.

Abstract: 2H-1,2,4,6-Thiatriazine-1,1-dioxides of the formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3 and Y have the meanings given in the description, are used for controlling undesirable plant growth.

Abstract: 2H-1,2,4,6-thiatriazine-1,1-dioxides of the formula I ##STR1## where R.sup.1, R.sup.2 and Hal have the meanings given in the description, are used for controlling undesirable plant growth.

Abstract: 2H-1,2,4,6-Thiatriazin-3-one,1,1-dioxides of the formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3 have the meanings given in the description, are used for controlling undesirable plant growth.

Abstract: This invention relates to novel benzothiazine derivatives having therapeutic effect on autoimmune diseases, to processes for preparation of such derivatives, and to pharmaceutical compositions containing such derivatives, the derivatives having the formula: ##STR1## wherein R.sup.1 is lower alkyl which may have one or more substituents selected from carboxy, aryl and carboxy(lower)cycloalkyl; aryl which may have one or more substituents selected from halogen, lower alkyl, halo(lower)alkyl and lower alkoxy; haloarylamino; or heterocyclic group;R.sup.2 is hydrogen, lower alkyl, lower alkylamino(lower)alkyl, aryl or ar(lower)alkyl;R.sup.3 is hydrogen, halogen, lower alkyl or lower alkoxy; andn is an integer 0 to 2.

Abstract: A process for the preparation of a 1-amino-1,3,5-triazine-2,4(1H, 3H)-dione compounds comprising the steps of reacting an N-substituted imido-dicarboxylic acid diaryl ester with an isothiosemicarbazone at a temperature of between 50.degree. and 150.degree. C. to form a 1-alkylidene-amino-1,3,5-triazine-2,4(1H, 3H)-dione reaction product; and thereafter, hydrolyzing the reaction product in an acid medium. The reaction product need not be separated from the reaction mixture before the hydrolysis step. Certain novel 1-amino-1,3,5-triazine-2,4(1H, 3H)-dione compounds are provided. The compounds are useful as herbicides.

Abstract: 3,4,5,6-Tetrahydro-thiatriazine-3,5-dione-1,1-dioxides of the formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3 have the meanings given in the main text, which possess herbicidal properties.

Abstract: 6H-1,2,4,6-Thiatriazine-1,1-dioxides of the formula ##STR1## where R.sup.1 and R.sup.2 are an aliphatic radical, a cycloaliphatic radical or a substituted aliphatic radical, R.sup.1 may also be unsubstituted or substituted phenyl, unsubstituted or substituted benzyl, or tetrahydrofurylmethyl and R.sup.2 may also be lower alkoxycarbo-lower alkoxy, lower alkylmercapto-carbo-lower alkoxy, lower alkoxy-carbo-lower alkylmercapto, lower alkylmercapto-carbo-lower alkylmercapto, unsubstituted or substituted aryl or unsubstituted or substituted benzyl,R.sup.3 is hydrogen, an aliphatic radical, a cycloaliphatic radical or substituted aliphatic radical,R.sup.4 and R.sup.5 are lower alkyl and R.sup.5 may also be hydrogen,X and Y are oxygen, sulfur, sulfinyl or sulfonyl andX.sup.1 is oxygen or sulfur, and herbicides containing these compounds.