Abstract: (6R,7R)-7-[(Z)-2-(2-triphenylmethylaminothiazol-4-yl)-2-(2-tert.-butoxycarb onylprop-2-oxyimino)acetamido]-3-(1-pyridiniummethyl)ceph-3-em-4-carboxylat e is isolated by formation of N,N-dimethylacetamide solvates.

Abstract: Compounds of the formula ##STR1## in which Y is hydrogen or hydroxyl, useful as intermediates in the production of antibiotics, are prepared by reacting a sulfinic acid of the formula ##STR2## with an oxidizing agent.

Abstract: A-21978C cyclic peptides of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, an amino-protecting group , 8-methyldecanoyl, 10-methylundecanoyl, 10-methyldodecanoyl, the specific C.sub.10 -alkanoyl group of A-21978C factor C.sub.0 and the specific C.sub.12 -alkanoyl groups of A-21978C factors C.sub.4 and C.sub.5 ; R.sup.1 and R.sup.2 are, independently, hydrogen or an amino-protecting group, and salts thereof, are prepared by enzymatic deacylation of an antibiotic selected from A-21978C complex, A-21978C factors C.sub.0, C.sub.1, C.sub.2, C.sub.3, C.sub.4 and C.sub.5 and blocked A-21978C complex and factors C.sub.0, C.sub.1, C.sub.2, C.sub.3, C.sub.4 and C.sub.5, using an enzyme produced by the Actinoplanaceae, preferably by Actinoplanes utahensis. The A-21978C cyclic peptides and salts thereof are useful intermediates to prepare new semi-synthetic antibacterial agents.

Abstract: There is provided by this invention cell-targeting cytotoxic compositions comprising transferrin covalently coupled to vinca alkaloid.

Abstract: Improved bioconverting strain of Streptomyces thermotolerans useful in preparing tylosin esters and new antibacterial macrocin or lactenocin ester derivatives of the formula: ##STR1## wherein R is formyl or hydroxymethyl; R.sup.1 is hydrogen, acetyl or propionyl; R.sup.2 is hydrogen or ##STR2## and R.sup.3 is hydrogen, acetyl, propionyl, n-butyryl or isovaleryl; provided that one of R.sup.1 or R.sup.3 must be other than hydrogen.

Abstract: 2-Fluoro-17.beta.-estradiol is synthesized by mercurating a 17.beta.-estradiol diacylate or dietherate at C-2, replacing the mercury group with fluorine and then cleaving the acyl or ether protecting groups.

Abstract: Sexual dysfunction in mammals is treated with a trans-(.+-.)- or trans-(-)-2-amino-4-permissibly-substituted-6-loweralkyl or allyl octahydropyrimido[4,5-g]quinoline or a pharmaceutically-acceptable acid addition salt thereof.

Abstract: 7.beta.-Acylamino-3-azido-3-cephem-4-carboxylic acid esters are obtained with the corresponding 3-halo or 3-sulfonyloxy-3-cephem esters and an alkali metal azide. The 3-azido compounds as the free acids or salts are antibacterial agents while in esterified form react with alcohols and phenols to provide 2-alkoxy (or 2-phenoxy)-3amino-3-cephem esters and isomeric ring expanded 4,7-bicyclo .beta.-lactam compounds, namely [2R-(2.alpha.,7.alpha.,8.beta.)-4-alkoxy (or 4-phenoxy)-9-oxo-8-acylamino-6-thia-1,3-diazabicyclo[5.2.0]non-3-ene-2-car boxylic acids and esters and the corresponding 3-alkoxy (or 3-phenoxy) 1,4-diazabicyclo[5.2.0]non-3-ene-2-carboxylic acids and esters. These reaction products obtained with the azide possess antibacterial properties.

Abstract: 1-(1-naphthyl)piperazine, a powerful and selective peripheral vascular serotonergic receptor blocker.

Abstract: This invention provides a novel allylic chlorination process for inserting a chlorine atom on the saturated methyl group of a 3-methyl-2-but-3-enoate group on the ring nitrogen atom of a 2-azetidinone or thiazolinoazetidinone. The chloro-substituted compounds prepared thereby are novel intermediates used in preparation of cephalosporins.

Abstract: N-Aryl benzamides wherein the aryl group is a nitrogen containing heterocycle are useful as selective herbicidal agents. Compositions containing the novel benzamides and a herbicidal method of selective weed control are disclosed.

Abstract: 3-Exomethylene cepham sulfones are converted to azetidinone sulfinic acids by reaction with activated zinc, magnesium, activated magnesium or amalgamated magnesium and a protonic acid.

Abstract: This invention provides for certain naphthalenylimidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents, bronchodilators, vasodilators, and anticoagulants.

Abstract: 7.beta.-[2'-Triazepinone-2'-(oxime ether) acetamido] cephalosporin antibiotics are claimed. Also claimed are the 2'-triazepinone-2'-(oxime ether) acetic acid intermediates and the esters, salts and halides thereof.

Abstract: The present invention discloses functionally independent selectable recombinant DNA cloning vectors for use in Streptomyces.

Abstract: There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, ##STR1## in which R.sub.1 is (i) an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C.sub.3-6 alkoxy, C.sub.3-6 cycloalkyl, aryl or heteroaryl, the cycloalkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms,(ii) cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or(iii) aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C.sub.1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R.sub.

Abstract: This invention relates to certain amino-5,6-diarylpyrazines useful as activators of GABA and benzodiazepine binding.

Abstract: The present invention discloses selectable recombinant DNA cloning vectors for use in Streptomyces and related organisms.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable non-toxic acid addition salts thereof, in whichR is hydrogen, methyl, ethyl, cyclopropylmethyl, or allyl;A is a residue of a D-amino acid selected from the goup consisting of Ala, Abu, Nva, Val, Nle, Leu, Ile, Gly(Al), Gly(Cp) Met, Cys(Me), Met(O), Cys(Me) (O), Ser, Ser(Me), Thr, and Hse;R.sub.1 is hydrogen, C.sub.1 -C.sub.3 primary alkyl, cyclopropylmethyl, allyl, ethylthiomethyl, 2-fluoroethyl, or propargyl; andX is hydrogen, fluoro, bromo, iodo, chloro, hydroxy, C.sub.1 -C.sub.3 alkyl, trifluoromethyl, or C.sub.1 -C.sub.2 alkoxy; are useful analgesic agents.

Abstract: 9-(N-alkanoylaminoalkyl)-fluorenes are anti-arrhythmic agents.