Abstract: Substituted 2,3-dihydro-6-substituted-pyrimido[2,1-f]purine-4,8(1H,9H)-diones, their tautomers and salts, are disclosed for use as antihyperproliferative skin disease agents.Methods for their preparation and use are described.

Abstract: Stereoisomerically pure forms of normorphine analogs which have superior analgesic and nonaddicting qualities are described. In addition, a method of separating diastereomeric forms of N-sec-alkyl-substituted analogs utilizes the hydrocarbyl(1-8C) diesters of the normorphine derivatives. A new method for preparing the N-methylalkylmethyl derivatives of normorphine and norcodeine and their conventional analogs is also disclosed. This method employs the corresponding methyl alkyl ketones and a reducing agent.

Abstract: Novel 2H-v-triazolo[4,5-d]pyrimidines of the general formula ##STR1## where R.sup.1 and R.sup.2 independently of one another are each alkyl, unsubstituted or substituted phenyl or phenalkyl, or ##STR2## is a saturated 5-membered or 6-membered heterocyclic ring, X is alkyl, halogen or phenyl n is 0, 1 or 2, and A is ##STR3## hydrogen, halogen, cyano, thiocyano, alkoxy, alkoxyalkoxy, unsubstituted or substituted phenoxy, phenylalkoxy, alkylthio, phenylthio, --S--(CH.sub.2).sub.m --COO-alkyl, where m is from 1 to 4, alkylcarbonyl, benzoyl, carboxyl, carboalkoxy, alkylsulfonyl, phenylsulfonyl, an N-imidazole, benzimidazole, 1,2,3-triazole, benzotriazole, 2-mercaptobenzothiazole, 2-mercaptobenzimidazole, 2-mercaptothiazole or 2-mercapto-1,3,4-thiadiazole radical, or a radical of the formula ##STR4## where R.sup.4 is H or C.sub.1 -C.sub.4 -alkyl, p is from 2 to 5 and R.sup.5 and R.sup.6 are each C.sub.1 -C.sub.

Abstract: The compound 4,7-dimethyl-2-(4-pyridinyl)-1,2,4-triazolo[1,5-a]pyrimidin-5(4H)-one and the pharmaceutically acceptable salts thereof are analgesic and anti-inflammatory agents. Methods for preparing and using the compound and salts are described.

Abstract: Imidazoquinazolin-2-one compounds having platelet aggregation inhibitory activity is disclosed. These compounds have high water-solubility and reduced influences on the circulatory system and are useful for treatment and prophylaxis of intravascular thromboembolism and temporary ischemia as well as prevention of thrombus upon use of prosthetic apparatus.

Abstract: Amino derivatives of benzylidene-Pyrrolo[2,1-b] Quinazolines are provided, together with pharmaceutical compositions containing them. The compounds and the compositions have pharmaceutical utility and are particularly useful as anti allergy agents.

Abstract: Angiotensin converted enzyme inhibitor activity if exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is hydrogen, aryl, or heteroaryl; R.sub.2 is hydrogen, amino, alkanoylamino, arylcarbonylamino, or heteroarylcarbonylamino;R.sub.3 is hydrogen, alkyl, or aminoalkyl;R.sub.4 and R.sub.5 are the same or different and each is hydrogen, alkyl, halogen, aryl, arylalkyl, hydroxy, alkoxy, alkylthio, aryloxy, arylthio, or cycloalkyl, or R.sub.4 and R.sub.5 taken together are oxo, ethylenedithio or propylenedithio;one of R.sub.6 and R.sub.7 is ##STR2## and the other is hydrogen, alkyl or arylalkyl; R.sub.8 is hydrogen, alkl or aryl;R.sub.9 is hydrogen or alkyl;n is 0 or an integer of 1 to 8;m is 0 or 1; andA is --(CH.sub.2).sub.p --wherein p is 0 or 1, --NH--, or --O--.

Abstract: 2-Mercaptoalkylsulphides and 2-mercaptoalkylethers are obtained by the hydrazinolysis of 3-thiaalkylisothiuronium salts and 3-oxaalkylisothiuronium salts.

Abstract: Disclosed is a process for the preparation of otho-(hydrocarbylthio)-phenols, having at least one hydrogen on a carbon atom ortho to a hydroxy group, with hydrocarbyl disulfides in the presence of catalytic amounts of aluminum phenoxide.

Abstract: Tricyclic isoindole derivatives characterized by having a 1,2,3,4,6,10b-hexahydropyrazino[2,1-a]isoindole or 1,3,4,10b-tetrahydropyrimido[6,1-a]isoindol-6(2H)-one nucleus are disclosed. The foregoing compounds are useful antihypertensive agents.

Abstract: A photolithographic plate, method for preparation thereof, and salt compound useful in the preparation, the method involving the treatment of a metallic silver image on a substrate with a homogeneously stable acidic aqueous salt solution comprising a ferricyanide anion for oxidizing the metallic silver and an organic cation capable of forming a water-insoluble, inherently oleophilic complex with oxidized silver, the cation being derived from a protonatable nitrogen-substituted hydrocarbon compound containing a formal imine group therein which is in resonant association with adjacent groups within the hydrocarbon compound.

Abstract: 3-Acetoxymethyl cephalosporin antibiotics in which the 7.beta.-acylamido group has the structure ##STR1## where R is thienyl, furyl or phenyl; R.sup.a is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, carboxy, C.sub.2 -C.sub.5 carbalkoxy or any of the groups designated for R.sup.a, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases. The compounds, which are syn isomers or exist as mixtures of syn and anti isomers containing at least 90% of the syn isomer, have particularly high in vitro activity against strains of Escherichia coli. Haemophilus influenzae and Proteus organisms; and also shown unusually high activity against Pseudomonas organisms.

Abstract: Cephalosporin antibiotics having the formula: ##STR1## (where R is thienyl, furyl or phenyl; R.sup.a is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl or phenyl, and R.sup.b is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, carboxy or C.sub.2-5 alkoxycarbonyl, or R.sup.a and R.sup.b together with the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.13 is C.sub.1 -C.sub.6 alkyl, C.sub.3-7 cycloalkyl, phenylalkyl, phenyl or naphthyl, thiadiazolyl, diazolyl, triazolyl, tetrazolyl, thiazolyl, thiatriazolyl, oxazolyl, oxadiazolyl, pyridyl, pyrimidyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, triazolopyridyl or purinyl, and n is 0, 1 or 2 and their physiologically acceptable derivatives exhibit broad spectrum antibiotic activity characterized by particularly high activity against gram negative microorganisms, including those which produce .beta.-lactamases.

Abstract: Imidazo[2,1-b]thiazole derivatives are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl or carboxy, and R.sup.2 is hydrogen, lower alkyl or phenyl.In addition, a method is provided for treating or inhibiting helminthiasis by parenterally, perorally or topically administering a pharmaceutical composition containing such imidazo[2,1-b]thiazole derivatives. Pharmaceutical compositions for use in the above method are also provided.

Abstract: Thiazolo[3,4-b]isoquinoline derivatives of the general formula: ##STR1## wherein A represents 3-pyridyl, 4-pyridyl or 5-isoquinolyl and, when A represents 3-pyridyl, X.sub.1 represents hydrogen, halogen, dimethylamino or cyano, X.sub.2 represents hydrogen or fluorine and X.sub.3 represents hydrogen or nitro, at least two of X.sub.1, X.sub.2 and X.sub.3 representing hydrogen, or X.sub.1 X.sub.2 together represent methylenedioxy and X.sub.3 represents hydrogen, and when A represents 4-pyridyl or 5-isoquinolyl, X.sub.1, X.sub.2 and X.sub.3 each represent hydrogen, and non-toxic pharmaceutically acceptable acid addition salts thereof, possess useful pharmacodynamic properties, in particular analgesic and antipyretic activity. This invention relates to new therapeutically useful thiazolo[3,4-b]isoquinoline derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

Abstract: This invention relates to novel compounds of the isoindoline series. More particularly, the present invention relates to certain novel 1-imino-3-(2-oxo-4-thioxo-5-thiazolidinylidene)isoindolines, 1-imino-3-(2,4-dithioxo-5-thiazolidinylidene)isoindolines, water-insoluble pigments prepared therefrom, and to methods for their preparation.

Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and an ureidoalkyl substituted tetrazolylthiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.

Abstract: Allantoin compound with a metal salt of 2-pyrrolidone-5-carboxylic acid has a solubility which is from 2.5 to 4 times greater than that of pure allantoin. The compound has almost the same pharmacological effect as allantoin itself and is harmless, and therefore it can be used in medicines, cosmetics, creams, ointments, etc.

Abstract: A process for the dehydrohalogenation of a 7-halo- or a 1,7-dihalodihydrocodeinone dialkyl ketal of the general formula (I): ##STR1## in which R represents an alkyl group containing from 1 to 6 carbon atoms, X represents hydrogen or chlorine or bromine and Y represents chlorine or bromine which comprises subjecting the ketal to the action of a base in the presence of a polar aprotic solvent. The process has utility in facilitating the production of codeine.

Abstract: Compounds of the formula ##STR1## wherein R may be hydrogen or a straight or branched chain alkyl radical of from 1 to 10 carbon atoms, aryl of from 6 to 10 carbon atoms, or aralkyl of from 7 to 10 carbon atoms;Y may be hydrogen, alkyl of from 1 to 4 carbons, CF.sub.3, F, Cl, or Br; andZ may be hydrogen or as defined hereinafter.These compounds are useful as central nervous system stimulants or more specifically in enhancing performance or as mood elevators.