Abstract: The present invention relates to novel DNA sequences that encode for the branched-chain alpha-ketoacid dehydrogenase complex of an organism belonging to the genus Streptomyces and to novel polypeptides produced by the expression of such sequences. It also relates to novel methods of enhancing the production of natural avermectin, of producing a Streptomyces avermitilis bkd mutant and of producing novel avermectins through fermentation.

Abstract: The generation of transgenic animal models for testing various treatments of Type II Diabetes Mellitus are described. The DNA construct allows pancreatic &bgr; cell-specific expression of human islet associated polypeptide (IAPP) under the regulation of the rat insulin II promoter in both cell lines and transgenic animals. The DNA construct is introduced into animal embryos by microinjection as one or multiple copies or into established cell lines by electroporation. The transgenic animals develop amyloid plaque deposits in the islets of Langerhans in the pancreas, fasting hyperglycemia, glycouria and diabetic glomerulosclerosis at 3 to 5 months of age. The cell lines can be screened for treatments that inhibit expression of human IAPP; the transgenic animals can be screened for treatments that either enhance or inhibit the progression of this disease phenotype.

Abstract: The present invention relates to the use of microorganisms of the Monosporium and Thamostylum genera to diastereoselectively O-demethylate pharmaceutical intermediates, to produce compounds of the formulae:

Abstract: This invention relates to a method for evaluating the susceptibility of pharmaceutical drugs to metabolism by a specific cytochrome P-450 isozyme, which comprises contacting the sample compound with a reagent composition prepared by adding the specific cytochrome P-450 isozyme to liver microsomes lacking said specific cytochrome P-450 isozyme in a carrier material. More particularly, this invention relates to a useful in vitro quantitative assay for drug metabolism by P-450 isozymes such as CYP2D6, CYP2C19, and CYP2A6. This invention also relates to a reagent composition which is useful for said in vitro assay.

Abstract: Benzylidene intermediates, useful in the preparation of dihydropyridines such as nifedipine and amlodipine, are formed by reaction of a ketocarboxylic adid ester with an aldehyde in the presence of a catalytic amount of dimethylamine acetate.

Abstract: This invention relates to modified Yarrowia lipolytica LEU2 gene promoters; modified Y. lipolytica LEU2 genes comprising such modified Y. lipolytica LEU2 gene promoters; and vectors comprising such modified Y. lipolytica LEU2 genes. This invention also relates to vectors comprising a Y. lipolytica DNA sequence LEU2 genes. This invention also relates to vectors comprising a Y. lipolytica DNA sequence sufficient for integrative transformation of Y. lipolytica; vectors which comprise a nucleotide sequence coding for a polypeptide and a promoter functional in Y. lipolytica operably linked thereto; E. coli transformants which comprise vectors according to this invention; Y. lipolytica transormants which comprise an expression vector according to this invention; methods of producing Y. lipolytica transformants comprising multiple integrated expression vectors; strains of Y. lipolytica useful in the preparation of such transformants; methods of producing polypeptides with certain of the Y.

Abstract: A compound of the formulaR.sup.1 --A.sup.2 --A.sup.1 -Asp-p-nitroanilidewherein:A.sup.1 is a residue of any of the naturally occurring .alpha.-amino acids or a homolog, analog or derivative of a natural .alpha.-amino acid;A.sup.2 is a residue of a lipophilic .alpha.-amino acid;R.sup.1 is alkylcarbonyl, phenalkylcarbonyl, alkoxycarbonyl, phenalkoxycarbonyl, alkylaminocarbonyl, phenalkylaminocarbonyl or R.sup.2 --A.sup.3 whereinA.sup.3 is a residue of a lipophilic .alpha.-amino acid; andR.sup.2 is alkylcarbonyl, alkoxycarbonyl or phenylalkoxycarbonyl, anda method of detecting inhibitors of interleukin 1.beta. converting enzyme (ICE) comprising evaluating a test compound's capacity to inhibit the ICE-induced hydrolysis of a compound of the formula I. The greater the ability of a test compound to inhibit such hydrolysis, the greater its expected activity in treating inflammation as well as diseases whose pathogenesis is induced or sustained by interleukin-1.beta..

Abstract: The present invention relates to novel DNA sequences that encode for the branched-chain alpha-ketoacid dehydrogenase complex of an organism belonging to the genus Streptomyces and to novel polypeptides produced by the expression of such sequences. It also relates to novel methods of enhancing the production of natural avermectin and of producing novel avermectin through fermentation.

Abstract: The present invention relates to novel DNA sequences that encode for the branched-chain alpha-ketoacid dehydrogenase complex of an organism belonging to the genus Streptomyces and to novel polypeptides produced by the expression of such sequences. It also relates to novel methods of enhancing the production of natural avermectin, of producing a Streptomyces avermitilis bkd mutant and of producing novel avermectins through fermentation.

Abstract: This invention relates to a novel nucleic acid sequence encoding a novel human phosphodiesterase IV (hPDE IV) isozyme. It also relates to a polypeptide encoded by such sequence.This invention also relates to an assay method for detecting the presence of such novel isozyme in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozyme.

Abstract: This invention relates to a novel nucleic acid sequence encoding a novel human phosphodiesterase IV (hPDE IV) isozyme. It also relates to a polypeptide encoded by such sequence.This invention also relates to an assay method for detecting the presence of such novel isozyme in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozyme.

Abstract: A compound of the formulaR.sup.1 --A.sup.2 --A.sup.1 --Asp-p-nitroanilide Iwherein:A.sup.1 is a residue of any of the naturally occurring .alpha.-amino acids or a homolog, analog or derivative of a natural .alpha.-amino acid;A.sup.2 is a residue of a lipophilic .alpha.-amino acid;R.sup.1 is alkylcarbonyl, phenalkylcarbonyl, alkoxycarbonyl, phenalkoxycarbonyl, alkylaminocarbonyl, phenalkylaminocarbcnyl or R.sup.2 --A.sup.3 whereinA.sup.3 is a residue of a lipophilic .alpha.-amino acid; andR.sup.2 is alkylcarbonyl, alkoxycarbonyl or phenylalkoxycarbonyl, anda method of detecting inhibitors of interleukin 1.beta. converting enzyme (ICE) comprising evaluating a test compound's capacity to inhibit the ICE-induced hydrolysis of a compound of the formula I. The greater the ability of a test compound to inhibit such hydrolysis, the greater its expected activity in treating inflammation as well as diseases whose pathogenesis is induced or sustained by interleukin-1.beta..

Abstract: There is disclosed a low calorie fat substitute comprising a sorbitol fatty acid ester with a degree of substitution of about four fatty acid groups. Foodstuffs containing the sorbitol tetraester are also disclosed.

Abstract: The present invention is directed to solid salts of hop acids and to processes for their production. Preferred are solid sodium and potassium salts of isoalpha acids rho-isoalpha acids, tetrahydroisoalpha acids, hexahydroisoalpha acids and beta acids.

Abstract: Heteropolysaccharide 105-4, prepared by fermentation of a new unnamed Pseudomonas species ATCC 53923 is useful as an industrial thickening, suspending or stabilizing agent.

Abstract: A compound of the formulaR.sup.1 -A.sup.2 -A.sup.1 -Asp-p-nitroanilidewherein:A.sup.1 is a residue of any of the naturally occurring .alpha.-amino acids or a homolog, analog or derivative of a natural .alpha.-amino acid;A.sup.2 is a residue of a lipophilic .alpha.-amino acid;R.sup.1 is alkylcarbonyl, phenalkylcarbonyl, alkoxycarbonyl, phenalkoxycarbonyl, alkylaminocarbonyl, phenalkylaminocarbonyl or R.sup.2 -A.sup.3 whereinA.sup.3 is a residue of a lipophilic .alpha.-amino acid; andR.sup.2 is alkylcarbonyl, alkoxycarbonyl or phenylalkoxycarbonyl, and a method of detecting inhibitors of interleukin 1.beta. converting enzyme (ICE) comprising evaluating a test compound's capacity to inhibit the ICE-induced hydrolysis of a compound of the formula I. The greater the ability of a test compound to inhibit such hydrolysis, the greater its expected activity in treating inflammation as well as diseases whose pathogenesis is induced or sustained by interleukin-1.beta..

Abstract: There is disclosed a low calorie fat substitute comprising a sorbitol fatty acid ester with a degree of substitution of about four fatty acid groups. Foodstuffs containing the sorbitol tetraester are also disclosed.

Abstract: The present invention is directed to a method for the recovery of erythorbates from photographic solutions. In the disclosed method, the photographic solution is first acidified by passing it over an acidic cation exchange resin and the resultant solution is then passed over a weakly basic anion exchange resin.

Abstract: A composition useful in the treatment of onychomycosis comprises tioconazole, a gel-forming agent and a hydro-alcoholic vehicle.