Abstract: The present invention relates to 4,10-dihydro-4,10-dioxo-1H-1-benzopyrano[3,2-b]pyridine-3-carboxylic acids, salts and esters having the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy; R.sub.2 is hydrogen, aralkyl or lower alkyl; R.sub.3 is hydrogen or lower alkyl and their pharmaceutically acceptable salts.These compounds are indicated in the management of allergic conditions such as bronchial asthma, hay fever and the like.

Abstract: The present invention relates to 8-(1H-tetrazol-5-yl)-11H-pyrido[2,1-b]quinazolin-11-ones having the following structure: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, alkyl, alkyloxy, halogen, hydroxy and methylenedioxy; R.sub.3 is carboxamido, cyano or 5-tetrazolyl groupings and the pharmaceutically acceptable salts of acids and bases thereof.These compounds exhibit anti-allergic properties and are useful as anti-asthmatic agents.

Abstract: The present invention relates to compounds of the formula: ##STR1## wherein A represents a grouping of the formula: ##STR2## B represents an oxygen or sulphur atom, R.sup.1 and R.sup.2, which may be the same or different, each represent a hydrogen or halogen atom, a trifluoromethyl group, or a straight- or branched-chain alkyl or alkoxy group containing from 1 to 4 carbon atoms, R represents a group of the formula --COOR.sup.3, in which R.sup.3 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, or a group of the formula --CH.sub.2 OR.sup.4, in which R.sup.4 represents a hydrogen atom or an alkylcarbonyl group containing from 2 to 5 carbon atoms and the double bonds depicted in positions C.sub.2 -C.sub.3, C.sub.5 -C.sub.6 and C.sub.13 -C.sub.14 are trans, cis and trans respectively, the cyclodextrin clathrates thereof and, when R.sup.3 in the group --COOR.sup.3 represents a hydrogen atom, non-toxic salts thereof.

Abstract: This invention relates to novel indolothiopyrones having the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or aryl; R.sub.2 is hydrogen or halogen; and R.sub.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, nitro-substituted-aryl, or .omega.-substituted lower alkyl wherein the substituent is: ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen, lower alkyl, or together with the nitrogen atom, form a heterocyclic ring; and R.sub.6 is lower alkoxy or amino, and novel intermediates used in their preparation. The indolothiopyrones are prepared by reacting a 3-mercaptoindole with sodium propiolate or a substituted sodium propiolate followed by acidification to obtain an intermediate acid; the intermediate acid cyclizes in the presence of an acid catalyst to obtain the indolothiopyrone structure which may be additionally subjected to halogenation, alkylation or hydrolysis to obtain derivatives having the various substituent groups disclosed.

Abstract: New pentapeptides having the formula X-R-Tyr(methyl)-Ser(benzyl)-R.sup.1 -Y wherein X is t-butoxycarbonyl or benzyloxycarbonyl, R is a single amino acid fragment, a dipeptide fragment or tripeptide fragment utilizing amino acids selected from the group consisting of Pro, Aze, His(benzyl) and Trp; R.sup.1 is a single bond or a single amino acid fragment or a dipeptide fragment utilizing amino acids selected from the group consisting of Ala, Trp and His and Y is lower alkoxy, amino, lower alkylamino or di(lower alkyl)amino with the proviso that the total number of amino acid units when R and R.sup.1 are combined is three.

Abstract: Prostaglandin compounds of the formula: ##STR1## wherein A represents a grouping of formula II, III or IV indicated below and (i)R.sub.1 represents an unsubstituted n-butyl, n-pentyl, n-hexyl or n-heptyl radical, or such a radical carrying one, two or three alkyl substituents of 1 to 4 carbon atoms, or R.sub.1 represents a methyl, ethyl, propyl or butyl radical carrying a phenyl, cyclohexyl or cyclopentyl substituent, R.sub.2 represents a hydrogen atom or an alkyl radical of 1 to 4 carbon atoms, and R.sub.3 represents a hydrogen atom, or (ii) R.sub.1 represents n-butyl, or n-butyl or n-pentyl carrying one, two or three alkyl substituents of 1 to 4 carbon atoms, or R.sub.1 represents a methyl, ethyl, propyl or butyl radical carrying a phenyl, cyclohexyl or cyclopentyl substituent, R.sub.2 represents a hydrogen atom or an alkyl radical of 1 to 4 carbon atoms, and R.sub.3 represents an alkyl radical of 1 to 4 carbon atoms are disclosed. These compounds exhibit characteristic prostaglandin-like activity.

Abstract: The invention relates to 1-phenyl-4-amino-cyclohex-2-ene-1-carboxylic-acid-esters of the general formula I ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and may be H, alkyl, hydroxyalkyl, alkenyl, preferably with 1 to 4 C-atoms, aralkyl which may be bonded to each other, in which connection the heterocyclic system formed may be substituted further by the OH- group and where attachment takes place by an oxygen or a nitrogen atom, if desired, which in its turn carries an H, alkyl with 1 to 4 C-atoms, aryl which may be substituted by chlorine, preferably in 3 or 4-position, and by methoxy, preferably in 2 or 4-position, acyl, preferably alkanoyl with 1 to 4 C-atoms, and aroyl, or aralkyl, and R.sub.3 represents an alkyl radical with 1 to 4 C-atoms, the salts thereof and quarternary ammonium compounds, and a process for their preparation. These compounds have analgesic and neuroleptic properties.

Abstract: Methods for treating certain cardiovascular disorders by administering 3-phenoxypyridine or a pharmaceutically acceptable acid-addition salt thereof.

Abstract: Naphthalenone phthalazinylhydrazones of the formula: ##STR1## are disclosed. In the above formula R.sub.1 is hydrogen or alkyl, R.sub.2 is alkyl, preferably branched alkyl, or N, R.sub.1 and R.sub.2 taken together forming a heterocyclic ring. These compounds are useful as antihypertensive agents.

Abstract: 1-Substituted-2-(2-pyridinyl)ethanone N-oxides having the formula I or II: ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are each hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, or benzyloxy; R.sub.4 is halogen, hydroxy, lower alkyl, lower alkoxy, benzyloxy, ortho-amino, ortho-lower alkylamino, ortho-alkanoylamino or ortho-benzoylamino; and R.sub.5 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or benzyloxy; the pharmaceutically acceptable acid addition salts thereof, and a process for the preparation thereof, are described. The compounds of this invention are useful for the treatment of allergic conditions and for the treatment of hyperacidity.

Abstract: The present invention relates to novel benzo(b)thiophene derivatives of the general formula: ##STR1## wherein Y represents a hydrogen or halogen atom; A represents a hydrogen atom or a phenyl group which may be substituted with a halogen atom or a lower alkoxy group; B represents a radical of the formula OR' or NR.sup.2 R.sup.3, wherein R' is an alkyl radical of 1 to 5 carbons which may be substituted with hydroxy, lower alkoxy, phenyl or phenoxy groups or a cycloalkyl or phenyl group which may be substituted by lower alkoxy or halogen atoms; R.sup.2 and R.sup.3, which may be identical or different, represent, if identical, hydrogen, alkyl radicals of 1 to 5 carbon atoms which may be substituted by hydroxy, lower alkoxy, phenoxy, di-lower alkylamino, or phenyl groups; or, if R.sup.2 is hydrogen, R.sup.

Abstract: Alpha-aryl-2-pyridineethanol 1-oxides and alpha-pyridinyl-2-pyridineethanol 1-oxides having the formula I or II: ##STR1## wherein R.sub.1 is hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, ortho-amino or ortho-lower alkylamino; R.sub.2 and R.sub.3 are each hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, benzyloxy or lower alkanoyloxy; the pharmaceutically acceptable acid addition salts thereof and a process for the preparation thereof are described. The compounds of this invention are useful in the prevention of allergic and asthmatic reactions.

Abstract: A stable, colored reference standard suitable for use in diagnostic determinations involving enzymatic reactions in which colorless 2-(p-iodophenyl)-3-(p-nitrophenyl)-5-phenyltetrazolium chloride is reduced to the red-colored 1-(p-iodophenyl)-5-(p-nitrophenyl)-3-phenylformazan, is described. The reference standard of this invention is an aqueous solution containing, in specified amounts, 1-(p-iodophenyl)-5-(p-nitrophenyl)-3-phenylformazan; serum albumin; an N,N'-dimethylformamide or a dimethylsulfoxide solvent; and isopropyl alcohol. An inert bulking agent may be added to the aqueous colored standard and the solution obtained may then be lyophilized. The lyophilized form of the colored reference standard is stable for at least 3 months at 4.degree. C. and 24.degree. C. and can be easily reconstituted with water or with dilute aqueous hydrochloric acid solutions. The novel colored reference standard solution has an absorbence maximum of 500 nanometers.

Abstract: 9-(3-O-Acyl-.beta.-D-arabinofuranosyl)adenine compounds, 9-(2,3-di-O-acyl-.beta.-D-arabinofuranosyl)adenine compounds, and their production by reacting in each case the corresponding 5-silyl ether derivative with a tetraalkylammonium fluoride. The compounds are useful as antiviral agents. The compounds are water-soluble and lipophilic, thereby being adaptable to a wide variety of pharmaceutical formulations.

Abstract: 9-(2-O-Acyl-.beta.-D-arabinofuranosyl)adenine compounds and their production by enzymatic removal of the 3-O-acyl and 5-O-acyl groups of a 9-(2,3-di-O-acyl-.beta.-D-arabinofuranosyl)adenine compound or a 9-(2,3,5-tri-O-acyl-.beta.-D-arabinofuranosyl)adenine compound. The monoester compounds are useful as antiviral agents. The compounds are watersoluble and lipophilic, thereby being adaptable to a wide variety of pharmaceutical formulations.

Abstract: A contact lens composition, having improved dimensional stability, suitable for use in the preparation of a corrective hydrated lens or an eye bandage, comprises polymerized random graft copolymers containing (in the dry state) from 67.2% to 79.3% HEMA; from 14.25% to 35% PVP; from 0.1% to 4.04% EDMA; from 0.1% to 2.5% MA; from 0.1% to 5.0% water; from 0 to 4 ppm HQ inhibitor; and from 50 to 250 ppm MEHQ inhibitor. The contact lens composition contains from 45% to 65% water after hydration. An improved method for shaping, polymerizing, and cutting and hydrating the contact lens composition is provided. The polymerization is conducted using only a low temperature initiator, by de-gassing prior to polymerization to remove substantially all oxygen, and by conducting the initial polymerization reaction at from 23.degree. C to 30.degree. C for 16 to 30 hours, during which the heat of the reaction is continuously absorbed to control the reaction exotherm.

Abstract: New trans-.DELTA..sup.2 -prostaglandins of the formula ##STR1## (wherein R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, R.sup.2 represents a 1,1-dimethyl-pentyl group or a 2-ethylheptyl group, the wavy line indicates attachment of the depicted group in .alpha.-configuration or racemic form consisting of equimolecular mixtures of .alpha.-configuration and .beta.-configuration and the C.sub.2 -C.sub.3 and C.sub.13 -C.sub.14 double bonds are trans), which are useful for the treatment of hypertension, contraception menstrual regulation.

Abstract: 9-(3,5-Di-O-acyl-.beta.-D-arabinofuranosyl)adenine compounds and their production by reacting in each case a 9-(5-O-tri-substituted-silyl-2,3-di-O-acyl-.beta.-D-arabinofuranosyl)adeni ne compound with a tetraalkylammonium fluoride. The compounds are useful as antiviral agents. The compounds are stable and being lipophilic are adaptable to long-acting and depot injectable pharmaceutical formulation.

Abstract: Processes for the production of the compounds of the formula: ##STR1## are disclosed. In the above formula, R.sub.1 is aryl which may be substituted or unsubstituted; R.sub.2 is hydrogen, alkyl, aryl, aralkyl, alkoxy, halogen, cyano, nitro, trifluoromethyl and the like.These compounds are prepared by the following reaction schemes: ##STR2## These compounds are useful as anti-inflammatory agents.

Abstract: There is disclosed 4,10-dihydro-4,10-dioxo-1H-1-benzopyrano[3,2-b]pyridine-2-carboxylic acids, salts and esters of the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, hydroxy or lower alkoxy; R.sub.2 is hydrogen, aralkyl or lower alkyl; R.sub.3 is hydrogen or lower alkyl and their pharmaceutically acceptable salts.These compounds are useful in the management of allergic conditions such as bronchial asthma, hay fever and so on.