Abstract: This invention relates to a process for the production of phthalazineacetic acid ester derivatives of the formula ##STR1## wherein R is (C.sub.1 -C.sub.4)alkyl which comprises reacting (Z)-3-oxo-1(3H)-isobenzofuranylideneacetic acid with hydrazine in the presence of a solvent; reacting the resulting mixture of the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid and 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of a solvent; and reacting the resulting 3,4-dihydro-4-oxo-phthalazineacetic acid with acid in the presence of an alcohol.This invention also relates to the novel compound 1-hydrazino-1,2,3,4-tetrahydro-4-oxo-phthalazineacetic acid of the formula ##STR2## which is an intermediate formed in the process of this invention and which is useful for the production of phthalazineacetic acid ester derivatives of formula IV. The compounds of formula IV are useful for the preparation of certain heterocyclic oxophthalazinyl acetic acids and esters thereof.

Abstract: 2-Amino and 2-thio-4-substituted-5-(hydroxy or alkoxy)-pyrimidines, which may be 6-substituted, and derivatives thereof are disclosed. The compounds are inhibitors of leukotriene synthesis and are, therefore, useful for the treatment of pulmonary, inflammatory, dermatological, allergic and cardiovascular diseases. The compounds are also cytoprotective and therefore, useful in the treatment of peptic ulcers.

Abstract: Intermediates and a stepwise process for the conversion of an alkyl 4-chloro-3R-hydroxybutyrate to optically active compounds of the formula ##STR1## wherein R is (C.sub.1 -C.sub.3) alkyl, phenyl or tolyl. The latter compounds are in turn useful as an intermediate in the preparation of penem antibiotic 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid and corresponding pharmaceutically acceptable salts and esters.

Abstract: A method of treating premature ejaculation comprising administering to a human in need of such treatment an amount of the compound (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenam ine, also known by the generic name sertraline, or a pharmaceutically acceptable salt thereof, effective in delaying ejaculation.

Abstract: A series of novel 4-arylsulfonyl-3,4-dihydro-2(1H)-quinoxalinone-1-alkanoic acid compounds have been prepared, including their lower alkyl ester derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These particular compounds are useful in therapy as agents for the control of certain chronic diabetic complications. Typical members include those compounds derived from 3,4-di-hydro-2-(1H)-quinoxalinone-1-acetic acid wherein an unsubstituted or substituted phenylsulfonyl moiety is located at the 4-position of the molecule. Ethyl 4-benzenesulfonyl-3,4-dihydro-2(1H)-quinoxalinone-1-acetate and 4-benzenesulfonyl-3,4-dihydro-2(1H)-quinoxalinone-1-acetic acid represent typical and preferred member compounds. Methods for preparing all these compounds from known starting materials are provided.

Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.

Abstract: Quinolonecarboxylic acid intermediaes useful in the preparation of antibacterial 6-fluouro-7-substituted-quinolonecarboxylic acids are prepared from 2-(iodo, bromo or chloro)-3-fluoro-4-(fluoro or chloro)-phenyl carboxylic acid or ester.

Abstract: Sequencing of the XPR2 and LEU2 genes of Yarrowia lipolytica, recombinant Yarrowia lipolytica cloning vehicles comprising heterologous DNA coding for the expression of mammalian protein and other polypeptides, including plasmids suited for transformation of Y. lipolytica hosts and incorporating a regulon homologous to the host in its untransformed state, and secretion signals for the heterologous gene; integrative expression vectors using the XPR 2 gene promoter, alkaline protease pre-proregion and XPR2 terminator region and those having the LEU2 promoter and alkaline protease secretory signal sequences capable, in a transformed Y. lipolytica cell culture, of expressing and secreting a heterologous protein outside the cell; Y. lipolytica transformants comprising said vectors and plasmids; methods for preparing vectors to direct secretion of specified heterologous proteins coded for by genes, cDNA or synthetic DNA in Y. lipolytica in their mature, functional state.

Abstract: N-demethylefrotomycin, a valuable new antibiotic substance, is produced by the microbial conversion of mocimycin using a novel, efrotomycin-producing, microbial species ATCC 53758.

Abstract: Platelet activating factor antagonists of formula (I): ##STR1## wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, aryl (C.sub.1 -C.sub.4) alkoxy, fluoro (C.sub.1 -C.sub.4) alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphonyl, hydroxy, trifluoromethyl and cyano, or is phenyl fused to a dioxole ring;R.sup.1 and R.sup.2 are each independently H or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together complete a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C.sub.1 -C.sub.4 alkyl) piperazinyl or N-(C.sub.2 -C.sub.4 alkanoyl)-piperazinyl group;orR.sup.2 is H or C.sub.1 -C.sub.4 alkyl and R.sup.1 is CN, C.sub.3 -C.sub.7 cycloalkyl, aryl, heteroaryl or a C.sub.1 -C.sub.4 alkyl group substituted by one or more substituents selected from C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxycarbonyl, aryl or heteroaryl;Z is selected from C.sub.1 -C.sub.6 alkoxy, aryl (C.sub.1 -C.sub.

Abstract: Polypeptides and derivatives thereof containing nor-statine and nor-cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.

Abstract: A method is disclosed for the containment and controlled release of and the substantial reduction of the leaching from the site of application of agricultural chemicals. In the disclosed method, the agricultural chemicals are applied to the soil dispersed in an aqueous gel-forming composition. Novel compositions of the agricultural chemicals dispersed in aqueous gel-forming compositions are also disclosed.

Abstract: Promoter-ribosome binding site (rbs) expression elements of general utility for high level heterologous gene expression; plasmids carrying said promoter-rbs expression elements and encoding genetic information for direct high level expression in bacteria of heterologous proteins, especially plasmids carrying a gene coding for prorennin or mammalian growth hormones; methods for their construction, including the use of synthetic linkers to provide desirable functional properties thereto; recombinant microorganisms comprising said plasmids; expression of said bacterial produced heterologous proteins by said recombinant microorganisms; and demonstration of the activities of the thus-produced proteins.

Abstract: A series of tetrahydrofuran-containing, macrocyclic polyether compounds. The macrocycles have a 21-membered ring, incorporating six oxygen atoms, and they have a carboxy group (or a salt thereof) directed towards the interior of the ring. Administration of the compounds of the invention to ruminant animals (e.g. cattle and sheep) modifies their digestive fermentation processes such that the volatile fatty acids produced in the rumen contain a higher proportion of propionates rather than acetates, thereby increasing the efficiency of feed utilization in said ruminant animals. Additionally, the compounds of the invention show antibacterial activity in vitro against certain gram-positive microorganisms.

Abstract: Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.

Abstract: A compression anastomosis assembly of interlocking coupling members, particularly suitable for use in achieving anastomosis of tubular organs, having an improved locking feature to prevent inadvertent disassembly of installed coupled members. The design and configuration of the members also provide for ease in placement of the assembly in a living body wherein preferably one assembly member includes a cutting guide and a cutting ring which facilitate use of a cutting implement commonly associated with a device suitable for use during assembly implantation.

Abstract: Antiparasitic milbemycin derivatives having at the C.25 position a substituted 2-propenyl group --C(CH.sub.3).dbd.CH--R.sup.2 wherein R.sup.2 is a C.sub.3 -C.sub.8 alkyl, alkenyl or alkynyl group which may optionally contain an oxygen or sulphur atom as part of the chain, or a C.sub.3 -C.sub.8 cycloalkyl or cycloalkenyl group, or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may optionally be substituted by one or more alkyl groups or halogen atoms; and process for their preparation.

Abstract: Antiparasitics comprising Avermectin derivatives of formula (I): ##STR1## wherein X represents a single or a double bond; R.sup.1 is H or OH; provided that when X is a single bond, R.sup.1 is H or OH, and when X is a double bond, R.sup.1 is absent;R.sup.2 is an alkyl group substituted by one oxo or one or more hydroxy groups or by a single oxygen atom on two adjacent carbon atoms to form an oxirane ring, or R.sup.2 is an alkyl group substituted by an alkoxycarbonyl group, said substituents on R.sub.2 being attached to either or both a terminal carbon atom and a carbon atom adjacent to a terminal carbon atom of R.sup.2 ; and R.sup.3 is H or CH.sub.3 ; or, when R.sup.2 is oxo-substituted alkyl, an alkyl acetal or ketal derivative thereof.