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 water-soluble and lipophilic, thereby being adaptable to a wide variety of pharmaceutical formulations.

Abstract: The present invention relates to 1,5-dihydro-1,5-dioxo-N-1H-tetrazol-5-yl-4H-[1]benzopyrano[3,4-b]pyridine- 2-carboxamides having the following structural formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, or nitro and R.sub.2 is hydrogen or lower alkyl and the pharmaceutically acceptable salts thereof.These compounds and their pharmaceutically acceptable salts are useful in the management of allergic manifestations such as bronchial asthma, hay fever and the like.

Abstract: The invention relates to prostaglandin analogues of the general formula: ##STR1## (wherein A represents a grouping of the formula: ##STR2## B represents an alkylene group containing from 1 to 7 carbon atoms or a group ##STR3## (wherein the group --(CH.sub.2).sub.n --may be attached to the ortho, meta or para position of the phenyl ring and m and n, which may be the same or different, each represent an integer from 1 to 5 inclusive, the sum of the integers represented by m and n being from 2 to 6 inclusive), X represents ethylene or cis-vinylene, Y represents ethylene or trans-vinylene, W represents ethylene or trans-vinylene, Z represents a halogen atom, and R.sup.1 represents a hydrogen atom or an alkyl group containing from 1 to 12 carbon atoms) and cyclodextrin clathrates of such acids and esters and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, which possess characteristic prostaglandin-like properties.

Abstract: A new and chemically unique one-pot process for the preparation of thiazolidin-4-one-acetic acid derivatives of the general formula: ##STR1## wherein R.sub.1 is a lower alkyl radical.

Abstract: Amino-substituted imidazo[1,2-a:3,4-a']diquinolin-15-ium salts having the formula I: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, C.sub.4 -C.sub.6 cycloalkyl, di(lower alkyl)amino, 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, methyl-1-pyrrolidinyl, methyl-1-piperidinyl, 4-morpholinyl or 2,2-dimethylhydrazino;R.sub.2 is hydrogen, lower alkyl, lower alkylamino, di(lower alkyl)amino, C.sub.4 -C.sub.6 cycloalkylamino, lower alkoxy(lower alkyl)amino, 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, methyl-1-pyrrolidinyl, methyl-1-piperidinyl, hexahydro-1H-azepin-1-yl, 4-morpholinyl, benzylamino, N-methylbenzylamino or 2-phenylethylamino;R.sub.3 is hydrogen or methyl;X is an anion;with the proviso that at least one of R.sub.1 and R.sub.2 is other than hydrogen, lower alkyl or C.sub.4 -C.sub.6 cycloalkyl; and with the further proviso that when R.sub.2 is dimethylamino, at least one of R.sub.1 and R.sub.3 is other than hydrogen, and intermediates used in the preparation thereof are disclosed.

Abstract: An immunoassay wherein the sample containing an immunologic substance is added to a suspension of particles coated with a second immunologic substance which is specific to the immunologic substance of the sample. The change in percentage of light transmission through the suspension undergoing the resulting agglutination is measured for a predetermined period of time and compared to a standard graph. The suspension is under constant agitation during the measurement.

Abstract: The present invention is concerned with new 3-pyrrolin-2-one derivatives which exhibit anti-hypertensive and vasodilatory action and with the preparation thereof.

Abstract: A process for the preparation of cis-(.+-.)-3,4-dihydro-N,N,2-trimethyl-2H-1-benzopyran-3-amine (I), a known antidepressant, is disclosed. The process of the invention is a multi-step process starting with 2-methyl-2H-1-benzopyran (II), which involves the production of novel intermediates (2.alpha.,3.beta.,4.alpha.)-(.+-.)-3,4-dihydro-2-methyl-4-(methylamino)-2H -1-benzopyran-3-ol (IV) and its hydrogen sulfate ester (V) as well as (1a.alpha.,2.beta.,7b.alpha.)-(.+-.)-1,1a,2,7b-tetrahydro-1,2-dimethyl[1]b enzopyrano[3,4-b]azirine (VI) and cis-(.+-.)-3,4-dihydro-N,2-dimethyl-2H-1-benzopyran-3-amine (VII). In the final step of the process, compound VII is methylated to form compound I.

Abstract: A process for the preparation of 1-hydroxyaporphine derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.3 and R.sub.4, which are the same or different, are lower alkyl, aryl or aralkyl radicals or R.sub.3 and R.sub.4 can together form a lower alkylene bridge member and R.sub.2 is a hydrogen atom or a lower alkyl, aralkyl or alkoxycarbonyl radical or an acyl radical derived from an aliphatic, aromatic or araliphatic carboxylic acid.

Abstract: This invention relates to a method for the removal of heparin from heparin-containing blood plasma test samples using an insoluble protamine reaction product, without adversely affecting subsequent testing of the plasma for clotting time. Protamine sulfate or a combination of protamine sulfate and serum albumin is cross-linked with glutaraldehyde to form an insoluble reaction product which is capable of adsorbing heparin. According to the method of this invention, excess amounts of either of the cross-linked protamine reaction products are added to blood plasma samples containing heparin and the mixture is agitated for a time sufficient to permit adsorption of substantially all heparin present. The insoluble protamine heparin complex formed is removed from the plasma along with any excess insoluble protamine reaction product. Aliquots of the heparin-free plasma may be subjected to coagulation tests in order to determine true clotting time.

Abstract: This invention relates to a tableted form of fibrous triethylaminoethyl cellulose suitable for the removal of heparin from heparin-containing blood plasma. The tablet is composed of granular microcrystalline cellulose and fibrous triethylaminoethyl cellulose in a ratio of from about 5.4:1 to about 10:1. According to the method of this invention, the triethylaminoethyl cellulose tablet, which is formulated to provide from about 5 to about 26 mg. of triethylaminoethyl cellulose per milliliter of plasma sample, is added to a heparin-containing blood plasma sample, the sample is agitated or allowed to stand for a time sufficient to permit adsorption of substantially all heparin present. The sample is then centrifuged and the remaining heparin-free plasma can be subjected to coagulation testing in order to determine the true clotting time.

Abstract: An immunoassay for the sandwich technique is disclosed in which antibody (or antigen) is bound to a plastic strip, and after reaction with a test sample and then fluorescently tagged antibody (or antigen), fluorescense is read directly from the plastic strip in a fluorometer.

Abstract: 3-cyanochromones having the following structural formula I: ##STR1## wherein R represents hydrogen, halogen or lower alkoxy, are prepared by dehydrating chromone-3-carboxamides with thionyl chloride in N,N-dimethylformamide. The compound having formula I is useful as an anti-allergic and anti-secretory agent.

Abstract: This invention relates to prostaglandin analogues of the formula: ##STR1## (wherein R represents a hydrogen atom or a methyl group, and the double bonds between C.sub.2 -C.sub.3 and C.sub.13 -C.sub.14 are trans) and cyclodextrin clathrates of such compounds and, when R represents a hydrogen atom, non-toxic salts thereof, which possess characteristic prostaglandin-like activity.

Abstract: The present invention relates to diacyloxyacids derived from the antibiotic substance, designated acid S, produced by Polyangium cellulosum var. fulvum (ATCC No. 25532), and to processes for their production. The diacyloxyacids derivatives of acid S of this invention are useful as antifungal and antibacterial agents.

Abstract: This invention relates to novel substituted indolopyrones which have utility in preventing allergic and asthmatic reactions in mammals.

Abstract: A two-stage process for the preparation of a chewing gum base utilizing solid elastomer is described wherein the solid elastomer is initially subjected to high intensity mixing under high shear conditions to masticate the solid until a substantially uniform, lump-free mass is obtained; followed by the step-wise addition of an elastomer solvent and an oleaginous plasticizer with continuous high intensity mixing until a substantially molten, uniform mass is obtained. In the second stage of the process, the remaining chewing gum base ingredients are added, step-wise, with continuous high intensity mixing until a uniform blend of ingredients is obtained. The second stage ingredients, which may include a non-toxic vinyl polymer, a hydrophobic plasticizer, additional oleaginous plasticizer and an emulsifier, are added step-wise in a sequence determined by decreasing order of viscosity. In a modification of the process, the hydrophobic plasticizer or emulsifier may be added with the stage one ingredients.

Abstract: A process for the conversion of the major antifungal antibiotic, acid S (ATCC No. 25532) isolated from the fermentation of Polyangium cellulosum var. fulvum into the minor antibiotic, acid F, from the same fermentation is described wherein acid S is methylated with diazomethane to provide acid S methyl ester which is then oxidized with silver carbonate on celite to obtain the corresponding keto ester S, which is subsequently reduced with sodium borohydride to give a mixture of acid S methyl ester and acid F methyl ester. These esters are readily separated by preparative thin layer chromatography and the acid F methyl ester is hydrolyzed with sodium hydroxide solution to provide acid F.