Abstract: An aromatic compound represented by the general formula Ar1X is reacted with a palladium compound and a phosphine derivative, in the presence of a first basic substance, thereby producing a palladium-complex compound represented by the general formula Ar1—PdL2X. This palladium-complex compound is reacted with a benzoic acid represented by the general formula Ar2—COOH, in the presence of a second basic substance, thereby producing another palladium-complex compound represented by the following general formula. The above palladium-complex compounds are useful as catalysts and can be produced easily by the above reactions. In the above general formulas, Ar1 is an aryl group; and X is a halogen that is fluorine, chlorine, bromine or iodine, trifluoromethanesulfonate group, an alkylsulfonate group having a carbon atom number of 1-4, or a substituted or unsubstituted arylsulfonate group; each L is independently a phosphine ligand; and Ar2 is an aryl group.

Abstract: The invention relates to a novel process for preparing substituted cyanophenyluracils of the general formula (I) in which R1, R2, R3 and R4 are each as defined in the description, said compounds being known as herbicidally active compounds, to novel substituted N-(cyanophenyl)aminoalkenamides as intermediates therefor and to an inventive process for their preparation.

Abstract: A process is useful for making compounds of the formula: wherein R is hydro, methyl, or fluoro.Valuable intermediates in this process include: ##STR1## wherein R is hydro, methyl, or fluoro, and L is a leaving group.

Abstract: Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.

Abstract: The object of the present invention is to provide a method for producing substituted-1,3,5-triazine derivatives at high yield, in which at least one of carbon atoms in the ring thereof is substituted by a secondary amine group having at leat one of alkyl groups. The method of the present invention is a method for alkylation of 1,3,5-triazine derivatives, characterized by reacting 1,3,5-triazine derivatives (melamines, melamine derivatives, various kinds of guanaminde derivatives, etc.) which has at least one or more amino groups or mono-substituted amino groups on carbon atom of the ring thereof, with aldehydes or ketones alcohols in the presence of a catalyst of a metal of group VII and/or group VIII in the periodic table and a hydrogen-containing gas to alkylate said at least one of amino groups or mono-substituted amino groups.

Abstract: The invention relates to thienopyrimidine of the formula (I) as well as to their physiologically acceptable salts, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and n have the meaning cited in claim 1. Said compounds exhibit a phosphodiesterase V inhibition and can be used in the treatment of cardiovascular dieases and for the treatment and/or therapy potency disorder.

Abstract: This invention is directed to aryl and heterocyclyl substituted pyrimidine derivatives selected from the following formulae: ##STR1## wherein Z.sup.1, Z.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined herein. These compounds are useful as anti-coagulants.

Abstract: A method for modifying 1,3,5-triazine derivatives characterized by heating and reacting a 1,3,5-triazine derivatives having at least one amino or mono-substituted amino group on a carbon atom or atoms on its ring with an alcohol in the presence of a metal catalyst and a hydrogen atom to introduce an alkyl group or an alkenyl group into each amino or mono-substituted amino group; another method for modifying 1,3,5-triazine derivatives characterized by heating and reacting a 1,3,5-triazine derivatives having at least one amino or mono-substituted amino group on a carbon atom or atoms on its ring with a dihydric alcohol in the presence of a metal catalyst and a hydrogen atom to introduce an alkyl group having a hydroxyl group into each amino or mono-substituted amino group; and 1,3,5-triazine derivatives obtained by the methods. The various modified sustituted 1,3,5-triazine derivatives thus produced are generally obtained as a mixture.

Abstract: A compound of formula I ##STR1## wherein R.sub.1 is nitro, halogeno or cyano group and R.sub.2 is a group selected from ##STR2## wherein Y and Z are independently oxygen, sulfur or NR, wherein R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group and X.sub.1 and X.sub.2 are NR, where R is hydrogen, straight or branched C.sub.1-8 alkyl, C.sub.5-7 cycloalkyl, phenylC.sub.1-8 alkyl or phenyl group, or a pharmaceutically acceptable salt or ester thereof. Pharmaceutical compositions are also disclosed.

Abstract: A 1,3,5-triazine derivative salt of a polyacid comprising phosphorus, sulfur and oxygen, which has a solubility of from 0.01 to 0.10 g/100 ml in water (25.degree. C.) and a pH of from 2.0 to 7.0 as a 10 wt % aqueous slurry (25.degree. C.), and which is obtained from the following steps (a) and (b):(a) a step of obtaining a reaction product by mixing melamine, phosphoric acid and sulfuric acid at a temperature of from 0 to 330.degree. C. in such ratios that the melamine is from 1.0 to 4.0 mols per mol of the total molar amount of the phosphoric acid (as calculated as orthophosphoric acid content) and the sulfuric acid (as sulfuric acid content), and the sulfuric acid (as sulfuric acid content) is from 0.05 to 20 mols per mol of the phosphoric acid (as calculated as orthophosphoric acid content), and(b) a step of baking the reaction product obtained in step (a) at a temperature of from 340 to 400.degree. C. for from 0.1 to 30 hours; and a process for its production.

Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.

Abstract: Carboxylic acid derivatives of the formula I ##STR1## where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.

Abstract: There are provided novel compounds of formula (I) ##STR1## wherein A represents a benzo ring; a six membered heterocyclic aromatic ring containing 1 to 3 nitrogen atoms; or a five membered heterocyclic aromatic ring containing 1 to 3 heteroatoms which may be the same or different and are selected from O, N and S; and R.sup.1, R.sup.2, R.sup.3 and X are as defined in the Specification and pharmaceutically acceptable salts thereof and enantiomers and tautomers thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment and prophylaxis of inflammatory disease and pain.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of heteroaryl derivatives of imidazolone compounds of Formula 1. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: This invention provides a convenient process for the preparation of monoacylhydrazines from carboxylic acids or their salts and hydrazine or substituted hydrazine in the presence of a 1,3,5-triazine substituted with at least one chloro or fluoro. The resulting monoacylhydrazine can further be converted to a diacylhydrazine by effectively either repeating the reaction or through reaction with a carboxylic acid chloride.

Abstract: There is provided a process for the preparation of unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds. The unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds are useful as pesticidal agents.

Abstract: Novel quinazolinone compounds, methods of using such compounds in the treatment of cGMP-associated conditions such as erectile dysfunction, and pharmaceutical compositions containing such compounds.

Abstract: Pesticidal substituted oxadiazines having the formula: ##STR1## wherein R is a substituted or unsubstituted heterocyclic group, pesticidal compositions containing these oxadiazines, and methods for their use.

Abstract: The present invention is directed to spiro-ketal derivatives of the formula (I): ##STR1## (wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9a, R.sup.9b, m and n are defined herein) which are tachykinin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.

Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: ##STR2## R.sup.2 and R.sup.3 are each independently (a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ;(c) halo;(d) hydroxyl;(e) cyano;(f) nitro;(g) --C(O)H or --C(O)R.sup.6 ;(h) --CO.sub.2 H or --CO.sub.2 R.sup.6 ;(i) --SH, --S(O).sub.n R.sup.6, --S(O).sub.m --OH, --S(O).sub.m --OR.sup.6, --O--S(O).sub.m --R.sup.6, --O--S(O).sub.m OH or --O--S(O).sub.m --OR.sup.6 ;(j) --Z.sup.4 --NR.sup.7 R.sup.8 ; or(k) --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;and the remaining symbols are as defined in the specification.