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: Compounds of formula (I): ##STR1## and their pharmaceutically acceptable salts, wherein R.sup.1 and R.sub.2 are each independently Cl, Br, CH.sub.3, CH.sub.2 CH.sub.3 or CF.sub.3 ; R.sup.3 is H, CH.sub.3 or CH.sub.2 CH.sub.3 ; and X is a 5-membered heterocyclic group containing up to four nitrogen atoms, attached via a nitrogen atom, the said group being optionally substituted by C.sub.1 -C.sub.6 alkyl or (CH.sub.2).sub.n NR.sup.4 R.sup.5, wherein n is an integer from 1 to 5 and R.sup.4 and R.sup.5 are each independently H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.1 -C.sub.4 alkyl substituted by phenyl or pyridyl, or R.sup.4 and R.sup.5 are linked to form, together with the nitrogen atom to which attached, a pyrrolidine, piperidine, piperazine, N-(C.sub.1 -C.sub.4 alkyl) piperazine, morpholine or azepine group, or, when X is triazolyl, said group may optionally be benzofused, are NMDA antagonists of value in the treatment of acute neurodegenerative disorders, e.g.

Abstract: The process of this invention is directed to isolating or otherwise obtaining an olefinic macrolide producing microorganism which microorganism does not contain epoxidase enzyme activity. This invention also relates to a process for preparing said olefinic macrolide by fermenting a mutant microorganism lacking epoxidase activity, designated rosX herein, which mutant is obtained from the wild-type microorganism. This invention also relates to a rosX mutant of Micromonospora rosaria, and to any microorganism having the identifying characteristics thereof, said mutant also designated ATCC 55709. This invention also relates to a process for preparing repromicin, the compound of formula (II), ##STR1## by mutating a wild-type microorganism capable of producing rosamicin to produce a mutant microorganism lacking epoxidase activity such that repromicin is produced by said mutant microorganism.

Abstract: The present invention relates to novel fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein Q, X.sup.1, x.sup.2 and X.sup.3 are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: The invention provides antifungal compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, whereinR is phenyl substituted by 1 to 3 substituents each independently selected from halo, --CF.sub.3 and --OCF.sub.3 ;R.sup.1 is C.sub.1 -C.sub.4 alkyl;R.sup.2 is H or C.sub.1 -C.sub.4 alkyl;X is CH or N; andY is F or Cl.

Abstract: The present invention provides novel methods of treating or preventing osteoporosis comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is hydrogen or a benzyl group; or a pharmaceutically acceptable salt thereof; together with a bone resorption inhibiting polyphosphonate.

Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates (including hydrates) of either entity, wherein R.sup.1 is (a) R.sup.2 is R.sup.3 R.sup.4 C(OH)A; V is C.dbd.O or CH.sub.2 ; W is O or NR.sup.5 ; R.sup.3 and R.sup.4 are each independently selected from H and C.sub.1 -C.sub.4 alkyl; or, together with the carbon atom to which they are attached, form a 4- or 5-membered carbocyclic ring; R.sup.5 is H, benzyl, C.sub.1 -C.sub.5 alkanoyl or SO.sub.2 (C.sub.1 -C.sub.4)alkyl; A is C.sub.2 -C.sub.3 alkylene; m is 0 or 1; and n is 0 or 1; with the provisos that when n is 1 and V is C.dbd.O then W is NH, and when n is 1 and V is CH.sub.2 then W is O; are selective 5-HT.sub.1 -like agonists useful in the treatment of, inter alia, migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders.

Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents and antiatheroscierosis agents.

Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, together with pharmaceutically compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds.

Abstract: The present invention relates to compounds of the formula ##STR1## having utility as hypoglycemic and antiobesity agents, methods for their use and pharmaceutical compositions containing them. The compounds of the present invention also possess utility for increasing lean meat deposition and/or improving lean meat to fat ratio in edible animals, i.e. ungulate animals and poultry.

Abstract: The anhydrate of 7-(?1.alpha.,5.alpha.,6.alpha.!-6-amino-3-azabicyclo?3.1.0!hex-3-yl)-6-flu oro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt has advantageous stability for formulation as an antibacterial agent.

Abstract: A method of and apparatus for spectrophotometric analysis of a powder material by reflectance measurements of a near infrared beam has a sample cell 2 within which the powder 20A is compressed between a spring biased plate 13 and a window 8 to a predetermined density. Spectrophotometric analysis is effected on the powder 20A through the window 8 by scanning with the infrared beam over an area of the powder 20A which when multiplied by the density of the powder and the depth of penetration of the beam is consistent with a predetermined dosage weight--such as that at which the powder may be marketed.

Abstract: Certain 1-(benzyl or 5-benzofuranylmethyl)-1-hydroxyurea derivatives are useful as hypoglycemic and hypocholesterolemic agents.

Abstract: Derivatives of 16-membered ring 3-deoxy macrolide antibiotic derivatives of rosaramicin, repromicin, 5-mycaminosyltylonolide, desmycosin, lactenocin, O-demethyllactenocin, cirramycin A.sub.1, and 23-deoxymycaminosyltylonolide, which are useful against bacterial and mycoplasmic pathogens in animals.

Abstract: A crystalline monohydrate of (3.beta.,5.alpha.,25R)-3-?(.beta.-D-cellobiosyl)oxy!spirostan-11-one that is useful as a hypocholesterolemic or antiatherosclerosis agent.

Abstract: Polypeptides isolated from the venom of the Geolycosa riogrande spider form pores in the plasma membrane of cells and are effective in mobilizing intracellular calcium ions in cells. These polypeptides are useful in such areas as drug delivery, cancer chemotherapy and immunotherapy, as well as in the physiological study of cells.

Abstract: The invention is directed to a novel non-aqueous oral-drench composition comprising from 0.01% to 2.0% (w/v) of an avermectin compound; from 30% to 45% (w/w) of an oil, said oil being selected from the group consisting of corn oil, sunflower oil, peanut oil and safflower oil; from 0.01% to 1.0% (w/v) of an oil-soluble antioxidant; and from 50% to 70% (w/w) of a fatty acid ester, said fatty acid ester being selected from the group consisting of caprylic/capric triglyceride, octyl palmitate and propylene glycol dicaprylate/dicaprate. The invention is further directed to methods of using the non-aqueous composition to treat parasitic diseases in mammals.

Abstract: Certain novel imidazole derivatives having the ability to inhibit the lipoxygenase enzyme and having formula (I), wherein Y is hydrogen, C.sub.1 -C.sub.8 alkyl, halosubstituted C.sub.1 -C.sub.4 alkyl, phenyl, substituted phenyl, C.sub.7 -C.sub.14 phenylalkyl, C.sub.7 -C.sub.14 (substituted phenyl)alkyl, pyridyl, substituted pyridyl, C.sub.6 -C.sub.13 pyridylalkyl or C.sub.6 -C.sub.13 (substituted pyridyl)alkyl, wherein each substituent is independently halo, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halosubstituted C.sub.1 -C.sub.4 alkyl, halosubstituted C.sub.1 -C.sub.4 alkoxy, NR.sup.4 R.sup.5, CO.sub.2 R.sup.4 or CONR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 are each, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; Ar.sup.1 and Ar.sup.2 are each, independently, phenylene, mono-substituted phenylene or di-substituted phenylene, wherein the substituents are, independently, halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo-substituted C.sub.1 -C.sub.

Abstract: The present invention relates to a method treating or preventing disorders caused by a spiral urease-positive gram-negative bacterium such as Helicobacter pylori in mammals, including humans, using compounds that are substance P receptor antagonists and, specifically, using certain quinuclidine derivatives, piperidine derivatives, pyrrolidine derivatives, azanorbornane derivatives, ethylene diamine derivatives and related compounds.

Abstract: The Invention provides a process for preparing a compound of the formula: ##STR1## or a base salt thereof, wherein R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl optionally substituted by up to 3 substituents each independently selected from the group consisting of C.sub.1 -C.sub.6 alkoxy and C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6 alkoxy)-; and R.sup.3 is C.sub.1 -C.sub.6 alkyl or benzyl, said benzyl group being optionally ring-substituted by up to 2 nitro or C.sub.1 -C.sub.4 alkoxy substituents comprising reacting a compound of the formula: ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl, phenyl or benzyl or C.sub.1 -C.sub.4 alkoxy; and R.sup.2 and R.sup.3 are as previously defined for a compound of the formula (I), with hydrogen peroxide or a source of peroxide ions: said process being optionally followed by conversion of the compound of the formula (I) to a base salt thereof. The present invention also relates to novel compounds of the formula (II).