Abstract: Provided is a novel improved process for the preparation of .alpha.-D-cellobiose octaacetate via the acetylative degradation of cellulose or cellulose acetate. The title compound is provided in high yield and quality in a facile one-pot process, amenable to large-scale synthesis.

Abstract: Certain salts of 4"-deoxy-4"-epi-methylamino avermectin Bla/Blb such as: the benzoic acid salt, gallic acid salt, citric acid salt, benzenesulfonic acid salt and salicyclic acid salt, phosphoric acid salt, tartaric acid salt or maleic acid salt, exhibit enhanced stability, a property which serves to provide greater shelf life and a product of greater safety for the user and the environment.

Abstract: Avermectin compounds are substituted at the 4a-position: the 4a-methyl group is first derivatized with a hydroxy group which is then substituted with a variety of alkyl, alkoxy alkyl, or polyalkoxy alkyl groups and derivatives thereof. The compounds are potent antiparasitic and anthelmintic agents and compositions for such uses are also disclosed.

Abstract: A novel antibiotic complex designated BU-4224V produced by fermentation of Kibdelosporangium albatum sp. nov. Strain R761-7. The complex may be separated chromatographically into bioactive components designated BU-4224V A, B.sub.1, B.sub.2, and C. The components BU-4224V B.sub.1 and B.sub.2 display both antiviral and antimicrobial activity, while component BU-4224V A has antimicrobial activity and component BU-4224V C has antiviral activity.

Abstract: This invention relates to a method for inhibiting or suppressing in an animal the contraction of vessels lined with endothelial tissue, which contractions are caused by anoxia or hypoxia. The method comprises administering to such an animal an effective therapeutic (contraction-inhibiting) amount of an avermectin class antibiotic such as ivermectin or a derivative thereof for a time period sufficient to inhibit or suppress said contractions.

Abstract: Avermectin analogs are prepared where the 23-position ring carbon atom is deleted and replaced by an oxygen atom. The compounds are prepared by opening the outer spiroketal ring to gain access to the 23-position atom, substituting the ring-opened compounds with a substituent containing the oxygen atom in the appropriate position and closing the ring to prepare the desired compounds. The compounds are potent anthelmintic agents and methods and compositions including such 23-nor-23-oxa compounds are also disclosed.

Abstract: A method is provided for preparing a cellulose ester plastic composition from waste paper (e.g. recycled paper) and/or sugar cane bagasse. The paper or bagasse is reacted with an acid anhydride in the presence of a catalyst to esterify some of the hydroxy groups on the cellulose. The resulting cellulose ester product is combined with various additives such as acetins, agricultural fillers, and carbon particles.

Abstract: There are disclosed avermectin derivatives which are avermectin modified at the 3- and 4-positions. The 3-hydroxy and 4-keto, epoxide and hydroxy (hydroxymethyl) derivatives and the 4-oxo compound are prepared from the natural avermectin by moving the 3,4-double bond exocyclic at 4 and forming a 3-hydroxy group. Osmolation gave an .alpha.,.beta.-diol across the double bond and cleavage of the diol provided the 4-oxo compound. The 4-oxo compound is epoxidized with an ylide reagent. The compounds are useful as anthelmintic agents and compositions for that use using the compounds as the active ingredient thereof are also described.

Abstract: The invention relates to elaiophylin derivatives of the formula I, II and III ##STR1## in which the substituents R(1), R(2), R(3) and R(3)' have the specified meanings. The compounds have antibacterial and antiviral activity.

Abstract: Avermectin compounds are substituted at the 4", 4' or 13-postion hydroxy group with an alkylthioalkyl group and are optionally substituted at the other reactive positions of the avermectin molecule. The compounds are prepared by reacting protected avermectins, avermectin monosaccharides or avermectin aglycones with dialkylsulfoxides. The compounds are potent antiparasitic agents and compositions for such uses are also disclosed.

Abstract: An improved process for isolating A83543 factors from fermentation broth in which they are produced which comprises:a) adding an approximately equal volume of a water miscible, polar organic solvent to the fermentation broth, including the biomass thereof;b) separating the liquid phase of the resulting mixture from the biomass;c) adjusting the pH of the separated liquid phase to between about 7 and 13;d) applying the separated liquid phase directly to a column of nonfunctional, macroreticular polymer;e) eluting the A83543 components from the column with an aqueous solution of water miscible, polar organic solvent; andf) collecting the fractions containing A83543 components.

Abstract: A method of producing a 3-deacylated derivative of a 16-membered macrolide antibiotic using a microorganism belonging to the genus Phialophora or Preussia which comprises incubating said microorganism with a 16-membered macrolide antibiotic in a medium containing nutritional sources commonly used for incubating microorganisms, isolating a 3-deacylated derivative from the incubation medium, a microorganism to be used for the above method and a novel macrolide antibiotic.

Abstract: Avermectin derivatives are disclosed wherein the 4"-hydroxy group is replaced by a substituted alkylthio or acylthio group or an iodo group. These avermectin derivatives can be further derivatized at the 5- and 23-positions as ketoximes or O-substituted ketoximes. The 4"-substituted avermectin derivatives are prepared from the 4"- and 4'-trifluoromethanesulfonyl avermectin derivatives with halo- or sulfur-containing nucleophiles. The 4"- and 4'-.alpha.- and .beta.-trifluoromethane sulfonates are prepared selectively and converted into 4"- or 4'-alkyl- or acylsulfides, or iodides using the appropriate sulfur-containing or iodine nucleophile. Substituted sulfoxy and sulfonyl substituents at the 4"- and 4'-positions are prepared from oxidation of the corresponding substituted sulfides. The new compounds are potent anti-parasitic agents; in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is a group --CH.sub.2 --X where X is hydrogen, halogen, --CN, --N.sub.3, --OC(O)R.sub.5, --S(O).sub.n R.sub.5, --SH, --OC(O)NHR.sub.5, --NHCONHR.sub.5 or --NR.sub.6 R.sub.7, where R.sub.5 is hydrogen optionally substituted C.sub.1-8 alkyl, or aryl, heteroaryl, aryl C.sub.1-4 alkyl or heteroaryl C.sub.1-4 alkyl in each of which the aromatic moiety is optionally substituted with the proviso that when X is --S(O).sub.n R.sub.5, R.sub.5 does not represent hydrogen, R.sub.6 and R.sub.7 are independently hydrogen or C.sub.116 alkyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is --formyl, C.sub.2-8 alkanoyl, dialkoxyphosphoryl, aroyl, heteroaroyl, aryl C.sub.1-4 alkanoyl, heteroaryl C.sub.1-4 alkanoyl, C.sub.1-8 alkylsulphonyl, arylsulphonyl, heteroarylsulphonyl, aryl C.sub.1-4 alkylsulphonyl or heteroaryl C.sub.1-4 alkylsulphonyl, where any aromatic moiety in R.sub.6 or R.sub.

Abstract: Avermectin compounds are glycosylated the 4' and 4"-positions by adding the avermectin compounds to the fermentation medium of Saccharapolyspora erythrea. The outer oleandrose sugar group of the avermectin compound is glycosylated with a glycosyl moiety, specifically a glucose group. In addition, other changes are effected in the avermectin moiety such as selective hydroxylation, epimerization at the 2-carbon and migration of the .DELTA. 3-double bond to a .DELTA. 2-position.

Abstract: Avermectin aglycones are glycosylated by fermentation in a medium of a non-producing mutant of Streptomyces avermitilis MA-6078. The glycosylation produces the monosaccharide and disaccharide derivatives while leaving the remainder of the molecule intact. The microorganism glycosylates with the .alpha.-L-oleandrose moiety.

Abstract: A method of treating a patient to reduce or prevent an acute or chronic inflammation or an ischaemic state which comprises administering to such patient an effective amount therefor of efomycin A, E or G.

Abstract: Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl substituent. This is accomplished by opening the outer spiroketal ring with the elimination of ring carbon atoms 23, 24 and 25 and the alkyl substituent at the 25-position and incorporation a new component, reclosing the spiroketal to a 5-membered ring with new substituents at the 24-position. The compounds are used as anti-parasitic insecticidal and anti-helmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: There are disclosed derivatives of avermectin compounds wherein one or both of the 13-oleandrose saccharide groups lack the methyl group of the 3'- or 3"-methoxy. Such compounds are potent anthelmintic and antiparasitic agents.

Abstract: The present invention, utilizing recombinant DNA technology, provides a novel method for obtaining 20-deoxotylosin from a tylosin producing microorganism. 20-deoxotylosin is useful as an antibiotic with a microbial inhibitory activity similar to tylosin.

Abstract: Avermectin analogs are prepared where the 23-position ring carbon atom is deleted and replaced by a sulfur atom. The compounds are prepared by opening the outer spiroketal ring to gain access to the 23-position atom, substituting the ring-opened compounds with a substituent containing the sulfur atom in the appropriate position and closing the ring to prepare the desired compounds. The compounds are potent anthelmintic agents and methods and compositions including such 23-nor-23-thia compounds are also disclosed.

Abstract: Disclosed is a novel process of preparing tobacco smoke filter material, wherein an acidic compound such as citric acid is dissolved in a cellulose acetate spinning solution (dope) prior to spinning the filaments of the filter material.

Abstract: The present invention is directed to the production and utilization of novel antibiotic compounds. These compounds are derivatives of the antibacterial agents tylosin and rosaramicin and exert a broad spectrum antibiotic activity toward several bacterial strains. Pharmaceutical compositions and methods of treating bacterial infections are described.

Abstract: There are disclosed new compounds with significant antiparasitic activity which are prepared by fermenting 13-epi-ivermectin aglycone in a novel microorganism identified as Streptomyces avermitilis MA-5542. The 13-epi-ivermectin aglycone compounds are modified by the microorganism by methylation at the 5-hydroxy position and the addition of an .alpha.-L-oleandrose at the 13-position hydroxy. The compounds are significant antiparasitic and anthelmintic agents and compositions for that use are also disclosed.

Abstract: Compounds of formula (1) ##STR1## wherein R represents a sugar residue or an acylated derivative thereof;R.sup.1 represents a methyl, ethyl or isopropyl group;Y.sup.1 is --CH.sub.2, Y.sup.2 is --CH-- and X represents ##STR2## [wherein R.sup.2 represents a hydrogen atom or a group OR.sup.6 (where OR.sup.6 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.0, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.7 (where R.sup.7 represents a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.7 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--; andR.sup.4 represents a group OR.sup.6 as defined above and R.sup.5 represents a hydrogen atom, or R.sup.4 and R.sup.5 together with the carbon atom to which the are attached represent >C.dbd.0 or >C.

Abstract: There are disclosed avermectin derivatives which incorporate a spacer between the disaccharide and the aglycone. The synthetic spacer-containing analogs are derived from the corresponding aglycones which in turn are prepared by chemical modification of naturally occurring avermectins. The compounds are active antiparasitic agents and compositions for that use are disclosed.

Abstract: A process for making cellulose acetate from wood pulp takes wet wood pulp and instead of converting it into dry pulp sheet which is the usual feedstock for acetate, dries and mechanically separates the pulp into a cellulose flock using a pin mill through which a hot drying gas is passed. Deactivation of the cellulose is avoided by control of the drying gas exit temperature to 80.degree. C. to 95.degree. C. and of the moisture content of the cellulose flock to 4 to 15% by weight. The flock produced may be acetylated directly without any need for reactivation treatments additional to the normal activation with acetic acid.

Abstract: Antiparasitic compounds of formula (I): ##STR1## The broken line at the 22-23 position representing an optional double bond and either R.sup.1 is H or OH and the double bond is absent or the double bond is present and R.sup.1 is absent; R.sup.2 is optionally substituted phenyl, or a group of formula (II): ##STR2## wherein X is O, S or --CH.sub.2 --, abc and d are 0-2 and a+b+c+d.ltoreq.5 R.sup.3 is H or MeR.sup.4 is H, OH or 4'-(alpha-L-oleandrosyl)-alpha-L-oleandrosyloxy.The compounds are prepared by fermentation of Streptomyces avermitilis in the presence of an N-alkanoyl cysteamine thioester containing R.sup.2.

Abstract: Compounds of formula (1) ##STR1## and their salts, wherein R.sup.1 is a methyl, ethyl or isopropyl group each substituted by a hydroxyl group or R.sup.1 is a group --(CH.sub.2).sub.n R7 or a group --CH(CH.sub.3)R.sup.7 (where n is zero or 1 and R.sup.7 l is CHO or CO.sub.2 H);Y.sup.1 is --CH.sub.2 --, Y.sup.2 is --CH-- and X represents ##STR2## [where R.sup.2 is a hydrogen atom or a group OR.sup.8 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >.dbd.O, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.9 (where R.sup.9 is a hydrogen atom or a C.sub.1-8 alkyl or C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.9 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--;R.sup.4 is a group OR.sup.8 as defined above and R.sup.5 is a hydrogen atom, or R.sup.4 and R.sup.

Abstract: Novel 12-membered lactone and 11-membered lactone derivatives of erythromycin, having antimicrobial activity against certain Gram-positive pathogens such as Steptococcus pyogenes and Gram-negative cocci such as Haemophilus influenzae, and useful as intermediates to other macrolide derivatives, are disclosed.

Abstract: Mycaminosyl tylonolide derivatives represented by the following general formula ##STR1## (wherein R.sup.1 denotes hydroxyl group, a lower alkanoyloxy group, benzoyloxy group, azido group, or amino group which may optionally be substituted with a lower alkyl or a lower alkanoyl radical; R.sup.2 stands for hydrogen atom or hydroxyl group; R.sup.3 expresses hydrogen atom or formyl group; and means a double bond or a radical represented by ##STR2## and salts thereof.

Abstract: 3-Deoxy mycaminosyl tylonolide derivatives represented by the following general formula and salts thereof: ##STR1## wherein X represents an oxygen atom or .dbd.N--OR.sup.4 (wherein R.sup.4 represents hydrogen or lower alkyl); R.sup.1 represents a hydrogen atom, an acyl group or an alkylsilyl group; R.sup.2 represents a hydrogen atom or an acyl group; and R.sup.3 represents a hydrogen atom or a hydroxyl group. The compounds of this invention of the formula (I) are novel compounds and have excellent antibacterial activity.

Abstract: The invention relates to cyclic antibiotics of formula ##STR1## wherein the prefix R represents that the substituents on the adjacent carbon atom are in the R configuration; the prefix S represents that the substituents on the adjacent carbon atom are in the S configuration;R.sub.1 is hydrogen or hydroxy and R.sub.2 is hydroxy and salts thereof, especially pharmaceutically acceptable salts.The compounds of formula I are prepared by fermentation using the strain So ce 12 (NCIB 12134) of the species Sorangium cellulosum and are effective antibiotics.

Abstract: Retinoic esters of D-desosamine have the formula ##STR1## wherein the ##STR2## radical is (all trans) retinoyl, (13 cis) retinoyl or etretinoyl, and R.sub.2 represents linear or branched alkyl having 1-24 carbon atoms; and the .alpha. and .beta. anomers, their mixtures and their salts.These esters are usefully employed in human and veterinary medicines and in cosmetic compositions.

Abstract: An angolamycin derivative represented by the following formula ##STR1## wherein X represents an acetyl, methanesulfonyl, methylthio, benzoyl or methoxy group. This compound is useful as a medicament such as antibacterial agent and an animal feed additive.

Abstract: A new antibiotic designated BMY-42448 is produced by fermentation of Micromonospora narashinoensis strain C39217-R109-7 (ATCC-53791). BMY-42448 exhibits both in vitro and in vivo antitumor activity.

Abstract: A antibiotic L53-18A and a pharmaceutically acceptable salt thereof which are useful for treatment of bacterial inventions are obtained by culturing, for example, Saccharopolyspora sp. L53-18 (FERM BP 2231) in a medium and the antibiotic accumulated therein is collected.

Abstract: Non-natural demethylavermectins useful as parasiticides and process therefor.

Abstract: This invention relates to a novel process for isolation and purification of avermectin compounds which are produced by the microorganism, Streptomyces avermitilis. The process disclosed herein involves two steps, namely, crude crystallization and recrystallization. The isolated compounds are described generically as avermectin B1 and B2 and have significant parasiticidal activity.

Abstract: Incubation of 13-deoxy ivermectin aglycone with a species of B. subtilis and of S. griseus results in the production of 13-.beta. ivermectin monoglucopyranoside as the major product and of 5-.beta. ivermectin monoglucopyranoside as the minor product.

Abstract: The carE gene of Streptomyces thermotolerans has been isolated and used to construct recombinant DNA expression vectors. The carE gene encodes 4"-O-isovaleryl acylase activity important in the biosynthesis of a number of useful antibiotics. The carE gene can be used not only to construct recombinant cells with an increased ability to produce the acylase enzyme but also to construct recombinant cells with the ability to produce novel antibiotic compounds.

Abstract: The present invention discloses a method for producing a novel antibiotic, 2"'-O-demethyltylosin. The novel antibiotic, utilizing recombinant DNA technology, can be produced from a transformed mutant of a tylosin producing microorganism. By transforming for example Streptomyces fradiae GS 16 with plasmid pHJL284, the transformant can produce 2"'-O-demethyltylosin. Streytomyces fradiae GS16 is a tylosin producing species that contain a mutation in the tylE gene found in the tylosin biosynthetic pathway. The tylE gene codes for demethylmacrocin 2"'-O-methyltransferase enzyme (DMOMT), the enzyme that methylates the 2-hydroxyl position of the 6-deoxyallose moiety. Plasmid pHJL284 contains the cloned tylF gene which codes for the macrocin 3"'-O-methyltransferase enzxyme (MOMT), the enzyme that methylates the 3"'-hydroxyl position, but it does not contain the tylE gene. Transformation of S.

Abstract: There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the perhydrooxepine derivatives. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or optionally protected hydroxy; R.sup.2 is alkoxy, optionally protected hydroxy, oxo or optionally O-substituted oximino; R.sup.3 is hydrogen, optionally protected hydroxy, or a group 4'-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrosyloxy or .alpha.-L-oleandrosyloxy wherein the terminal hydroxy group is optionally protected; one or R.sup.4 and R.sup.5 is hydrogen and the other is methyl; and one of R.sup.6 and R.sup.7 is hydrogen and the other is methyl; with the proviso that (a) when R.sup.1 is optionally protected hydroxy, R.sup.3 is hydrogen, and (b) when R.sup.2 is not methoxy or optionally protected hydroxy, R.sup.1 and R.sup.3 are both hydrogen, are new and useful as anthelmintic agents.

Abstract: There are disclosed avermectin derivatives in which position 13 of the avermectins has been inverted from the normal (alpha) stereoschemistry to the epimeric 13-beta stereochemistry. The synthetic 13-epi analogs are derived from the corresponding aglycones which in turn are prepared by chemical modification of naturally occurring avermectins. The compounds are active antiparasitic agents and compositions for that use are disclosed.

Abstract: All trans or 13-cis retinoic acid esters of macrolide and lincosamide antibiotics. These esters are useful in the therapeutic and cosmetic treatment of dermatosis and principally in the treatment of acne.

Abstract: A represents:a CH.sub.2 OH group, and in this case B represents a lower acyl group,a (CH.sub.2).sub.n CN group,a (CH.sub.2).sub.n CHO group,or a (CH.sub.2).sub.(n+1) OH groupin which n is an integer between 1 and 6, R.sub.1 and R.sub.2 being defined in the description. The macrolide compounds are useful as antibacterial agents.

Abstract: Compounds of general formula: ##STR1## where A, B, G, R.sub.2, R.sub.3, R.sub.4 and are defined in the description.Medicinal products comprising a compound of the invention and useful in the treatment of bacterial infections are also disclosed.

Abstract: There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the oleandrose 4"- or 4'-spiro-epoxide. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: 9-Dihydro-9-O-alkyldesmycosin derivatives and their salts are disclosed. The 9-dihydro-9-O-alkyldesmycosin derivatives are represented by the following formula (I), ##STR1## --wherein X represents an --O-- mycinose or a di-lower alkylamino group, R.sup.1 represents a hydrogen atom or a lower alkanoyl group, R.sup.2 represents a lower alkyl group, a cycloalkyl-lower group, or phenyl-lower alkyl group which may have a substituent, and R.sup.3 represents a hydrogen atom or a hydroxyl group. The compounds and the salts are useful as an antimicrobial agent. Unlike known desmycosin derivatives, the compounds give a high blood concentration by oral administration.