Abstract: The present invention relates to novel compounds which are protein kinase C inhibitors, methods for their preparation, intermediates therefor and pharmaceutical compositions comprising them. More particularly, the present invention relates to compounds of formula (I): wherein: one of Ar1 and Ar2 is optionally substituted bicyclic heteroaryl or optionally substituted tricyclic heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X is O or S; and R is H, OH, NH2 or C1-6 alkyl (itself optionally substituted by amino or hydroxy); or a salt or solvate thereof, or a solvate of a salt thereof; and the use of such compounds in medical therapies.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g.

Abstract: A composition for treating or preventing glomerulopathy which contains a compound of the formula (I): wherein, for example, R1 and R2 are each independently hydrogen atom, optionally substituted lower alkyl, optionally substituted aralkyl, etc.; R3 is 1,4-phenylene and 2,5-thiophendiyl; R4 is the substituents represented by the formula, etc.: wherein R6 is hydrogen atom, optionally substituted amino, etc.; and Y is NHOH or OH, its optically active substance, their pharmaceutically acceptable salt, or hydrate thereof.

Abstract: There is disclosed a process for producing an acid salt of a (Z)-2-aminothiazole compound of the formula (I): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, Y represents a halogen atom, —OSO3H or —OPO(OH)2, m indicates the valence number of an inorganic acid of the formula: HY wherein Y represents the same as defined above, and n indicates an integer of 1 or 2, which process is characterized by: reacting an acid salt of a 2-aminothiazole compound of the formula (II): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, X represents a bromine atom or an iodine atom, and the wavy line means that this compound is a mixture of the E- and Z-isomers, with the inorganic acid of the formula HY.

Abstract: The present invention relates to an ocular hypotensive treatment of glaucoma which comprising employing 20-substituted-PGs or 20-substituted15-keto-PGs effective as an ocular hypotensive agent; these compounds exhibit no or little side effect such as transient ocular hypertensive response, hyperemia of conjunctiva or of iris, dacryops, lema, closed eye and the like.

Abstract: Derivatives of N-phenylbenzamide with general formula (1) in which R.sub.1 is a cyano, nitro, halogen, hydrozy, C.sub.1 -C.sub.4 alkyl methyl, methoxy or tetrazol-5-yl group, R.sub.2 is hydrogen, hydroxy, or methoxy, R.sub.3 is a tetrazol-5-yl group or hydrogen, R.sub.4 and R.sub.5 are hydrogen if R.sub.3 is tetrazolyl but are independently selected from the group consisting of carboxy, methoxycarbonyl, ethoxycarbonyl and carbamoyl if R.sub.3 is hydrogen, and R.sub.6 is hydrogen or methyl. The derivatives have an anti-ulcer and anti-allergy activity.

Abstract: Novel benzo-1,2,3-thiadiazole derivatives of the formula ##STR1## in which; A is --OR.sub.4, --SR.sub.4, --N(R.sub.5)R.sub.6, --N(R.sub.7)--N(R.sub.5)R.sub.6, --O--N.dbd.C(R.sub.8)R.sub.9, --N(R.sub.7)--OR.sub.10, or ##STR2## R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.3 -C.sub.35 alkyl which is interrupted by an oxygen or sulfur atom, C.sub.1 -C.sub.8 alkyl which is substituted by halogen or --COOR.sub.7, C.sub.3 -C.sub.6 alkenyl which is unsubstituted or substituted by halogen, C.sub.3 -C.sub.6 alkinyl which is unsubstituted or substituted by halogen, C.sub.4 -C.sub.7 cycloalkyl which is unsubstituted or substituted by halogen or methyl, an aryl or heterocyclic radical U having not more than 3 heteroatoms O, N and/or S, or a radical U which is linked via an alkylene bridge containing not more than 6 carbon atoms and up to 2 oxygen atoms.

Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.

Abstract: A process is disclosed for the deprotection of allylic esters and ethers. The process comprises reacting an allyl ester of a carboxylic acid or an allyl ether of a phenol with pyrrolidine or piperidine and a catalytic amount of an organic-soluble palladium complex having a coordinating phosphine ligand to cleave the allyl moiety. The resultant carboxylic acid or phenol is then recovered.

Abstract: Prostaglandin derivatives, and specifically derivatives of isocarbacyclin, have an optionally substituted methylene group as a substituent on the .alpha.-carbon atom of the .alpha.-side chain. They have a variety of physiological effects, notably a strong ability to inhibit blood platelet aggregation and a strong anti-ulcer activity.

Abstract: A diaryl sulphide derivative of the formula ##STR1## in which R.sup.1 represents a thiazolamino radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, alkyl, aralkyl or acyl,R.sup.6 and R.sup.6 ' are identical or different and represent hydrogen, alkyl, aralkyl or aryl,R.sup.7 represents alkyl, cycloalkyl, aralkyl, acyl or aryl andn represents the number 1 or 2,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represent a group of the formula ##STR3## wherein R.sup.8 and R.sup.9 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, acyl, trifluoroacetyl, alkylsulphonyl, arylsulphonyl, trifluoromethylphenylsulphonyl or tolylsulphonyl andR.sup.4 has one of the abovementioned meanings or R.sup.

Abstract: Novel 5-alkylidene-4-substituted-2-cyclopentenones and 5-(1-hydroxy-aliphatic hydrocarbon)-4-substituted-2-cyclopentenones.These novel cyclopentenones and 5-alkylidene-3-hydroxy-4-substituted cyclopentanones have a pharmaceutical activity for treatment of tumors.

Abstract: The present invention relates to new compounds of the general formula: ##STR1## in which Ar represents thienyl, furyl, pyridyl or an optionally substituted phenyl group,R represents a linear or branched alkyl group with 1 to 7 carbon atoms, andeither X.sub.1 or X.sub.2 represents nitrogen, the other being carbon,and pharmaceutically acceptable acid addition salts thereof, having valuable cardiovascular properties.

Abstract: The compounds of formula ##STR1## wherein the group ##STR2## represents the residue of a natural amino acid selected from the group consisting of glycine, alanine, beta-alanine, phenylalanine, isoleucine, methionine, proline, aspartic acid and arginine; R represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl; and their acid-addition salts with pharmaceutically acceptable organic or inorganic acids; are useful in the preventive and curative treatment of pathologic syndromes due to the lowering of glutathione (GSH) levels.

Abstract: N-alkyl-N'-(2-aminomethyl-4-thiazolylmethylthio)alkyl guanidines, thioureas, ethenediamines and related compounds, H.sub.2 -receptor antagonists, useful in inhibiting gastric acid secretion in mammals.

Abstract: Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an --SO.sub.3 H group and having in the 3-position an acylamino group of the formula ##STR1## wherein X is --(CH.sub.2).sub.

Abstract: Derivatives of 3-aminopropane-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR.sub.1 and R.sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.

Abstract: This invention relates to a method of lowering blood pressure in humans and mammals using 2,6-disubstituted phenyl amidinoureas in which the phenyl ring is additionally substituted by a hydroxy, alkoxy, aralkoxy, alkenyloxy, alkynyloxy, haloacyloxy, or acyloxy group and to novel 2,6-disubstituted phenyl amidinoureas which possess pharmaceutical properties, including blood pressure lowering activity.

Abstract: A method for controlling nematodes in agricultural crops utilizing selected 3-substituted-4-phenyl-1,2,5-thiadiazoles, nematicidal compositions thereof, and novel compounds useful therefor are disclosed and exemplified.

Abstract: This disclosure describes 11-deoxy-11-substituted members of the E.sub.2, F.sub.2, E.sub.1, F.sub.1, dihydro E.sub.1 and dihydro F.sub.1 prostaglandin series which are useful as hypotensive agents and as anti-ulcer agents.