Abstract: The present invention relates to the use of the polyadenylation signal from the gene for bovine growth hormone to achieve a high level of expression of peptides in eukaryotic cells. Accordingly, the present invention provides a recombinant DNA compound comprising: a first nucleotide sequence which contains a promoter capable of initiating transcription of a gene; a second nucleotide sequence which encodes a gene for a polypeptide other than bovine growth hormone, including genomic and other intron containing forms thereof; a third nucleotide sequence which contains a bovine growth hormone polyadenylation signal; and a fourth nucleotide sequence which optionally contains a selectable marker. The first, second and third sequences are operably linked in sequence to form a functional genetic unit capable of being expressed. The fourth sequence, which is optionally provided, is useful for determining whether or not the DNA of the present invention has been incorporated into a living cell.

Abstract: An improved, more bioavailable formulation of glyburide is provided which consists preponderantly by weight of spray-dried lactose is described. This formulation utililzes micronized glyburide, but is more economically manufacatured than heretofore known micronized glyburide formulations.

Abstract: 1-Substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula (III): ##STR1## wherein R is selected from the group consisting of hydroxy, esters thereof, and alkoxy, in which the alkyl group is of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoylamino, and dialkylamino in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are produced by condensing a 1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-thione of the formula (I): ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.

Abstract: The present invention relates to certain 1,2-dihydro-2-oxo-6-alkyl-3-pyridine carboxylic acids, carboxylate esters, and methanols, their preparation and their use as antihyperglycemic agents.

Abstract: The present invention comprises certain aromatic and inter-oxa analogs of the prostaglandins in which the C-1 carboxyl is replaced by a primary alcohol. These prostaglandin F.alpha. analogs exhibit prostaglandin F.alpha. activity and are accordingly useful for the same pharmacological purposes as the corresponding prostaglandins.

Abstract: The present invention relates to analogs of lipoxin B (LX-B) and discloses the anti-inflammatory uses for these analogs. Particularly, the present invention relates to analogs of 5D,14,15-trihydroxy-6,8,10,12-eicosatetraenoic acid, including certain 5-epi-, 8,9-didehydro-, 6-iso, 6,7-dihydro-7.alpha.-hydroxy, and 6,7-dihydro-7.beta.-hydroxy derivatives.

Abstract: The present invention provides novel lipoxins A and B and a method of stimulating with lipoxin A compounds and attenuating with lipoxin B compounds the activation of neutrophils by exposure to an effective concentration of lipoxins or a derivative thereof. Also provided in the present disclosure are methods and compositions for preventing or treating inflammation, inflammatory responses, or inflammatory diseases and conditions in mammals, including humans, by administration of lipoxin B compounds. Lipoxins are novel trihydroxy-tetraene derivatives of arachadonic acid related to the leukotrienes.

Abstract: Isocyanate compositions are disclosed which yield aqueous emulsions on admixture with water. The emulsions are sufficiently stable to permit employment as particle board binders and like uses. The compositions of the invention are derived by reaction of a polymethylene polyphenyl polyisocyanate with a particular group of polyethylene glycols which have been capped with a block of propylene oxide residues.

Abstract: The present invention provides a process for the preparation of 11.alpha.-alkylprostaglandin E compounds from corresponding prostaglandin A compounds via reaction with alkyllithium complexes, and novel 11-deoxy-11.alpha.-alkylprostaglandin E compounds useful for the same pharmacological purposes as the natural PGE compounds, e.g., antiulcer and antisecretory effects.

Abstract: Copolyamide-imides characterized by thermoplasticity, high heat resistance and high impact resistance are derived by the reaction of 4,4'-methylenebis(phenyl isocyanate), optionally in admixture with a minor amount (up to 10 mole percent) of toluene diisocyanate (2,4-, 2,6-isomers and mixtures), with a mixture of trimellitic acid or anhydride (30-40 mole percent), isophthalic acid (26-44 mole percent) and a C.sub.7-10 aliphatic dicarboxylic acid (balance of 100 mole percent but not greater than 32 mole percent). These polymers are useful as engineering plastics.

Abstract: Addition of controlled amounts of water to the reaction mixture produced by phosgenation of a mixture of polymethylene polyphenyl polyamines (and like polyamines produced by condensation of formaldehyde and aromatic amines) prior to complete removal of excess phosgene gives rise to the corresponding polymethylene polyphenyl polyisocyanates having significantly improved properties. Not only is the color of the product, and of polyurethane foams prepared therefrom, significantly lighter but the proportion of higher molecular weight products is significantly less and the viscosity is less. No undesirable by-products are introduced into the polyisocyanate as a result of the process.

Abstract: The present invention provides novel 1-(6-hydroxy-4- or 7-methoxy or 4,7-dimethoxy-5-benzofuranyl)-4-substituted-1,3-butanediones which are useful as intermediates in the synthesis of khellin and related anti-atherosclerotic furochromones.

Abstract: This invention comprises certain analogs PGE or 11-deoxy-PGE compounds in which the carbonyl at C-9 is replaced by methylene. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.

Abstract: The present invention provides a total synthesis of known intermediates useful in the synthesis of khellin and antiatherosclerotic analogs thereof from pyrogallol. Pyrogallol is converted to 3,6,7-benzofurantriol triacetate using zinc chloride and chloracetanitrile, then catalytically reduced and deactoxylated at the 3 position to yield the corresponding 2,3-dihydrofuran. This substance is subjected to a Fries rearrangement to the corresponding diol, the phenolic hydroxyl group of which is then selectively alkylated. This yields 6-hydroxy-7-alkoxy-5-benzofuranyl methyl ketone, a known intermediate for the production of 4-desmethoxy khellin and analogs thereof. This compound is then selectively alkoxylated at the 4 position using lead tetraacetate or thallium (III) nitrate in an alkanol solvent to yield known chemical intermediates in the preparation of khellin and analogs thereof.

Abstract: This specification concerns the use to treat hypertension in mammals of novel and known 4H-s-triazolo[4,3-a][1,4]benzodiazepines, known 4H-s-triazolo[4,3-a][1,3,4]benzotriazepines and 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-ones, and novel 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-thiones.

Abstract: Described are compounds characterized by the following formula: ##STR1## wherein C.sub.n H.sub.2n is alkylene from 2 to 12 carbon atoms and C.sub.m H.sub.2m is alkylene from 2 to 20 carbon atoms. Each of the alkylene groups can, optionally, be substituted by inert substituents. The compounds contain a free isocyanato group and a masked isocyanate group, namely, the cyclic urea moiety, which, when the compounds are heated, preferably in the presence of a catalyst, opens to give the group OCN--C.sub.n H.sub.2n --. Thus, the compounds can be reacted via the free isocyanate group with active hydrogen-containing monomers or polymers to form storage stable compositions which, upon heating, are curable via reaction with the cyclic urea group.

Abstract: The present specification provides novel analogs of khellin, a natural product, which are useful in the treatment and prevention of atherosclerosis. Particularly, the present disclosure provides novel 5H-furo[3,2-g]-benzopyran-5-one substituted at the four and nine positions by methoxy or optionally substituted at the four position by hydroxy or alkoxy groups other than methoxy, certain 7-(N,N-dialkylaminoethen-2-yl substituted compounds. Also provided are certain novel antiatherosclerotic 7H-furo[3,2-g][1]benzopyrans.

Abstract: The present specification provides a total synthesis of known intermediates useful in the synthesis of khellin and antiatherosclerotic analogs thereof. 3-Furoic acid is treated with succinic anhydride and diesterified to 3-carboxy-.delta.-oxo-2-furanbutanoic acid bis (alkyl ester). Following amination, cyclization and bis methylation, 6-formyl-4,7-dimethoxy-5-benzofurancarboxcyclic acid alkyl ester is prepared. This compound is then converted to known intermediates in the synthesis of khellin and analogs. Further, the present invention provides numerous novel anti-atherosclerotic 4,9-di-(C.sub.2 -C.sub.4)-alkoxyfurochromones.

Abstract: The present invention provides novel methods for the stabilization of aqueous solutions of prostacyclin and related prostacyclin analogs comprising the addition of neutral or cationic surfactants to such aqueous solutions. Additionally, the novel surfactant-containing solutions of prostacyclin and related compounds are described. Finally there are provided novel pharmaceutical compositions comprising surfactant-containing aqueous solutions of prostacyclin and related compounds.

Abstract: Polyurethane polyether-based elastomers are described which are thermoplastic, recyclable and have increased high temperature resistance which permits fabrication by injection molding. The elastomers are the product of reaction of 4,4'-methylenebis(phenyl isocyanate), a particular group of polypropylene oxide-polyethylene oxide block copolymers and an extender [straight chain aliphatic diols C.sub.2-6 or the bis(2-hydroxyethyl ether) of hydroquinone or resorcinol]. The block copolymers have at least 50 percent primary hydroxyl groups, a pH in the range of 4.5 to 9, a content of alkali metal ion less than 25 ppm and a molecular weight of 1000 to 3000. The minimum ethylene oxide (E.O.) residue content (percent by weight) of the polyether for any molecular weight (M.W.) is governed by the equation: ##EQU1## In a particularly preferred embodiment the elastomers are prepared by replacing up to 25 percent by equivalents of the extender by certain diols (polyethylene glycols up to 1500 M.W. preferred).