Abstract: Method of blocking 5HT.sub.2 without effect on alpha receptors with 1-loweralkyl-6-methyl-8.beta.-(hydroxy)alkoxy carbonyl-5R-ergolines.

Abstract: 3-Azido-3-cephem esters are reacted with electron rich olefins, e.g., enamines and cyclic enol ethers, to provide C.sub.3 amidines and imidates having antibacterial activity in the free acid form. For example, 3-azido-3-cephem esters react with ethyl vinyl ether to provide 3-[1-(ethoxyethylidene)amino]-3-cephem esters. The latter are deesterified to provide the free acid antibacterials.

Abstract: This invention provides certain isoxazole and isothiazole derivatives, their pharmaceutical formulations, and their use in inhibiting aromatase and treating or preventing estrogen-dependent diseases in mammals.

Abstract: A new antibiotic of the rifamycin class, A39079 factor S-1, which has the structure ##STR1## is an effective broad-spectrum antibiotic and increases feed-utilization efficiency in animals.

Abstract: A folder for a sampler perfume vial is provided in which the front and back panels of flexible sheet material having cutouts extending to their distal edges are folded to effect a gripping relationship with a protuberance on the vial.

Abstract: The present invention relates to a novel transcriptional and translational activating sequence. The novel activating sequence can be either chemically synthesized or isolated on a 0.17 kb PstI-SacI restriction fragment from plasmid pKC203, a plasmid of E. coli JR225 (ATCC 31912). The activating sequence directs expression of the aminoglycoside acetyltransferase aac(3)IV and hygromycin phosphotransferase aph(4) genes present on plasmid pKC203. A series of expression vectors have been constructed in which the activating sequence directs the expression of beta-galactosidase or hygromycin phosphotransferase. These vectors can be readily modified and have been designed to facilitate the subsequent cloning and expression of any gene of research or commercial interest. The expression and cloning vectors have been transformed into E. coli and other host cells in which the activating sequence functions.

Abstract: A method for expressing a functional polypeptide in Streptomyces comprises transforming a Streptomyces host cell with a recombinant DNA expression vector and then culturing the transformed cell under conditions suitable for cell growth. The recombinant DNA expression vector comprises the veg or any other homologous Bacillus promoter, a naturally occurring or modified ribosome binding site-containing DNA sequence and a gene that codes for a functional polypeptide such as human pre-proinsulin. The method is specifically exemplified by use of expression plasmids pOW529, pOW539 and transformants, Streptomyces ambofaciens/pOW529 and Streptomyces ambofaciens/pOW539. The method is broadly applicable and is particularly useful in economically important Streptomyces taxa.

Abstract: New macrocin and 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; and the acid addition salts thereof; prepared by bioconversion of macrocin or lactenocin with an acylating enzyme system produced by Streptomyces thermotolerans strains, have improved activity against Mycoplasma species.

Abstract: Antibiotic A41030, a complex of 7 individual factors, is produced by submerged, aerobic fermentation of new Streptomyces virginiae NRRL 12525, and Streptomyces virginiae NRRL 15156. The antibiotic factors are separated and possess antibacterial activity against Staphylococcus and Streptococcus species which are penicillin resistant. In addition, the antibiotic factors have shown inhibition of Streptococcus pneumonia Park I. The complex and the individual factors enhance feed efficiency in ruminant animals, and are growth promoters in chickens and swine, and are especially valuable in milk production in dairy cattle.

Abstract: 3-Acetoxymethylcephalosporins are converted to 3-exomethylene cephalosporins by reaction with a metal and a bound proton source.

Abstract: Antibiotic A4696 factor H is isolated from the purified antibiotic complex produced by Actinoplanes missouriensis ATCC 31683 and exhibits excellent activity vs. gram-positive bacteria.

Abstract: There is described a process for preparing a sulphoxide of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4, taken individually, are alkyl, alkoxy or aryl groups, X is an alkylene group, R.sup.5 is a carboxylic acid protecting group and Y is a linking group through one or two carbon atoms forming a penam or cephem nucleus, which comprises reacting a compound of formula ##STR2## with an oxidizing agent. .alpha.-Sulphoxide compounds of formula (I) are also provided as novel intermediates.

Abstract: The novel glycopeptide antibiotic A-51568B is produced by submerged, aerobic fermentation of Nocardia orientalis NRRL 15232. A-51568B demonstrates antibiotic activity against gram-positive bacteria.

Abstract: Stable, biologically available, orally active 1,5-naphthalenedisulfonate salt of vinzolidine.

Abstract: Antibiotic A-51568 is produced by submerged, aerobic fermentation of new Nocardia orientalis NRRL 15232. The antibiotic is effective against gram-positive organisms.

Abstract: Desvancosaminyl- and des(vancosaminyl-O-glucosyl) glycopeptides, and methods for their preparation by treating a glycopeptide selected from vancomycin, A51568A, A51568B, M43A and M43D with trifluoroacetic acid under controlled conditions, are provided. The new glycopeptides are useful antibacterial agents.

Abstract: Ethers of ascorbic and isoascorbic acid and ketals and acetals thereof, angiogenesis inhibitors.

Abstract: Antibiotic compositions comprising a 1-oxa .beta.-lactam antibiotic compound of the formula ##STR1## or pharmaceutically acceptable salts thereof and either tobramycin, amikacin or piperacillin exhibit synergistic activity against multiple-antibiotic-resistant organisms. The 1-oxa compound can be used in conjunction with tobramycin, amikacin or piperacillin in a method of treating infections caused by resistant organisms.

Abstract: This invention provides for certain lactam derivatives, their pharmaceutical formulations, and a method of treating hypertension.

Abstract: N,N-Disubstituted heterocyclic amines are useful as fungicides.