Abstract: A method to make squaraine dyes involves the reaction of 1,8-diaminonaphthalene with 1,3-dihydroxyacetone dimer in a first reaction mixture comprising the appropriate solvents to prepare a first intermediate. This first intermediate is then reacted with an organic acylating agent in the presence of a suitable solvent to form a second intermediate. Lastly, after isolation, the second intermediate is reacted with squaric acid in a particular hydroxylic solvent/nonpolar solvent mixture that dissolves squaric acid and forms a ternary azeotrope with water and the water is at least partially removed. The resulting dyes have the following general structure wherein R is an organic radical derived from the organic acylating agent.

Abstract: The invention relates to novel substituted 2,4-diamino-1,3,5-triazines of the formula (I) in which R1 represents, for exampe, H or C1-C6-alkyl, R2 represents, for example, H, C1-C6-alkyl or —CO—R6, R3 represents, for example, H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl or C3-C6-cycloalkyl, R4 represents, for example, H, C1-C6-alkyl or C3-C6-cycloalkyl, R5 represents one of the groupings below, where R6 represents, for example, C1-C6-alkyl, C1-C6-alkoxy or C2-C6-alkenyl, R7 to R12 represents, for example, H or certain organic radicals and Q represents O or S, to processes and novel intermediates for their preparation and to their use as herbicides.

Abstract: The invention relates to novel substituted 2-amino-4-alkylamino-1,3,5-triazines of the formula (I) in which R1 represents in each case optionally substituted alkyl having 2 to 6 carbon atoms or cycloalkyl having 3 to 6 carbon atoms, R2 represents hydrogen or represents alkyl having 1 to 4 carbon atoms, A represents oxygen or methylene, Ar represents in each case optionally substituted phenyl, naphthyl or heterocyclyl, and Z represents hydrogen, represents halogen or represents in each case optionally substituted alkyl, alkoxy, alkylcarboxyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenyl or alkinyl, to processes and to novel intermediates for their preparation and to their use as herbicides.

Abstract: The present invention provides compounds comprising propynyl uracils having the formula wherein R1 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R2 is iodine or bromine; and R3 is propynyl, 3-iodopropynyl, 3-bromopropynyl, substituted or unsubstituted 2-furanyl, substituted or unsubstituted 3-furanyl, substituted or unsubstituted 2-pyrrolidinyl, substituted or unsubstituted 3-pyrrolidinyl, D-ribose, or deoxyribose. Another embodiment of the invention encompasses propynyl uracils having the formula wherein R4 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R5 is hydrogen or propynyl; and R6 is iodine or bromine. Also, methods of preparing these propynyl uracils are provided.

Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.

Abstract: This invention provides an industrially useful process for producing a quinazoline derivative (I) of the general formula: [wherein R1 is hydrogen or halogen; R2 is carboxy or protected carboxy; A is lower alkylene] or its salt on a commercial scale which comprises reacting a compound of the general formula: [wherein R1 is hydrogen or halogen] or its salt with a silylating agent and then with a compound of the general formula: Cl—A—R2  (III) [wherein R2 is carboxy or protected carboxy; A is lower alkylene] or its salt, optionally followed by desilylation.

Abstract: Compounds of formula (I) in which R is in which R is hydrogen, a straight or branched or cyclic C1-C6 alkyl group, unsubstituted or substituted by 1 to 10 oxygen atoms, or a C1-C20 alkyl group, optionally interrupted by a phenylene, in turn substituted by a straight or branched C1-C6 alkyl group, unsubstituted or substituted by 1 to 3 C1-C7 alkyl groups; the phenylene group being unsubstituted or substituted by alkoxy, carboxy, sulfamoyl, hydroxyalkyl, amino groups; as well as its complexes with a bi- or trivalent metal ion having an atomic number from 20 to 31, 39, 42, 43, 44, 49, or from 57 to 83, as well as its salts with anions of physiologically acceptable organic acids chelated complexes of these compounds are used as contrast agents for nuclear magnetic resonance imaging.

Abstract: Provided herein is a novel and useful process for preparing 2-methoxy-4-methyl-6-methylamino-1,3,5-triazine that broadly comprises the steps of (a) reacting zinc bis(imino-bis-carbimic acid methyl ester) with acetic anhydride to give 2,4-dimethoxy-6-methyl-1,3,5-triazine and (b) reacting the 2,4-dimethoxy-6-methyl-1,3,5-triazine, formed in step (a), with methylamine to give 2-methoxy-4-methyl-6-methylamino-1,3,5-triazine.

Abstract: Antiatherosclerotic agents are provided having the following structure: wherein: R1 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenylalkyl of 7-10 carbon atoms; and R2, R3, R4, R5, and R6 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy of 6-12 carbon atoms, aralkyloxy of 7-12 carbon atoms, fluoroalkoxy of 1-6 carbon atoms, trifluoromethyl, alkylthio of 1-3 carbon atoms, alkylsulfonyl of 1-3 carbon atoms, —SCF3, nitro, alkylamino in which the alkylamino moiety has 1-6 carbon atoms, or dialkylamino in which each alkyl group has 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.

Abstract: A compound of the formula: wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula: wherein R5 is hydrogen or R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH-antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.

Abstract: Described are neuroprotective agents of Formula I wherein R is an amino acid or nitrogen heterocyclic ring which is saturated or unsaturated of from 5 to 8 members which may have additional oxygen or sulfur atoms therein. The other provisions or substituents are described in the specification.

Abstract: The present invention is to provide a novel 6-(1-fluoroalkyl)-4-pyrimidone represented by the following formula (1): wherein R1 represents an alkyl group; R2 represents a hydrogen atom or an alkyl group; and R3 represents a hydrogen atom, an alkyl group or a chlorine atom, which is important for a synthetic intermediate for aminopyrimidine derivatives which are useful as acaricides, fungicides or nematocides, and processes for producing the same.

Abstract: The uracil compounds represented by the formula [V]: wherein R1 represents C1-C5 perfluoroalkyl group and Q represents an aromatic group, can be produced by making the amide compounds represented by the formula [II]: wherein R1 and Q have the same meanings defined above, or its hydrate react with a cyanate salt in the presence of a protonic acid.

Abstract: A pyrimidine nucleus-containing compound represented by the formula (I): wherein ring A represents the ring of the formula (a): in which R1 is a nitro group, an amino group, a substituted amino group or a halogen atom, or the ring of the formula (b): in which R1′ is the group such as an alkyl group or an alkenyl group; R2 to R5 independently represent the group such as an alkyl group or an alkenyl group; with the proviso that at least one of R2 to R5 is an alkenyl group, or acid addition salts thereof.

Abstract: N-Cyanoaryl nitrogen heterocycles having sulfur-containing groups of the formula (1), in which Q1 represents oxygen or sulfur, R1 represents hydrogen or halogen, R2 represents halogen, cyano, nitro, amino or the grouping —N(A1)SO2A, in which A represents, in each case, optionally substituted alkyl, alkenyl, alkinyl, dialkylamino, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, and A1 represents hydrogen, formyl or, in each case optionally substituted, alkyl, alkenyl, alkinyl, alkylcarbonyl, alkoxycarbonyl or alkylsulphonyl, or together with A represents alkanediyl, R3 represents hydrogen, halogen, cyano or optionally substituted alkyl, R4 represents optionally substituted alkyl or together with R3 represents alkanediyl, and Z represents one of the groups in which Q2 represents oxygen or sulfur and R5 represents hydrogen or, in each case optionally substituted, alkyl, alkenyl, alkinyl or alkylcarbonyl, and salts of compounds of the formula (1) with the pro

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: This invention provides novel compounds and methods and compositions using them in the treatment of central nervous system disorders, including depression and anxiety, the compounds having the formula: wherein Ar is an aryl group of 4 to 10 carbon atoms or a heteraryl group of 4 to 10 carbon atoms; R1 and R2 are independently selected from hydrogen, straight chain alkyl of 1 to 12 carbon atoms, branched alkyls of 3 to 10 carbon atoms or cycloalkyl of 3 to 10 carbon atoms; R3 is H, straight chain, branched or cyclic alkyl, halogen, alkoxy, haloalkyl, OH, nitro, nitrile, amino, CN, carboxy, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl and alkylaminocarbonyl; or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to new macrocyclic phthalocyanine-like systems. In particular, object of the invention are new macrocyclic porphyrazine-type compounds and metal derivatives thereof, in which heterocycle rings are provided at the periphery of the inner porphyrazine fragment. A further object of the invention is a process for obtaining, as an example, tetra(thiadiazolo)porphyrazine, or tetra(selenediazolo)porphyrazine, by means of cyclotetramerization of the monomers 3,4-dicyano-1,25-thiadizole, or 3,4-dicyano-1,2,5-selenodiazole with metallorganico or inorganic salts, in organic solvents, extraction, if any, of the metal from the complexes thus formed by treatment with strong acids to obtain tetra(thiadiazolo)porphyrazine, or tetra(selenediazolo)porphyrazine, and by treatment, if any, of these compounds with a metallorganic or inorganic salt to obtain the metal derivatives thereof different from those previously extracted.

Abstract: Phthalocyanine compounds substituted by from 1 to 8 substituents of formula (—O—R—O—) wherein R is a 1,2-arylene group are provided. Preferably, the phthalocyanine compounds are substituted by catechol. Additional substituents which may be present include hydrocarlyloxy, hydrocarbylthio, halogen and sulphonic acid or a salt thereof.

Abstract: A novel process for the preparation of benzonitrile compounds useful for herbicides or their intermediates is provided. A process for the preparation of compounds of the formula (1), characterized in comprising reacting a compound of the formula (1a) with one or more cyanides selected from potassium cyanide, sodium cyanide and zinc cyanide in the presence of a metallic catalyst. In the scheme, X is hydrogen, fluorine or chlorine atom; Z is nitro, amino or C1-C4 alkylsulfonylamino group or the like; Y is fluorine, chlorine or bromine atom or the like; and Q is hydrogen atom, or nitro or amino group or the like.