Abstract: N-Alkyl allylic tertiary amines are dealkylated as illustrated by treatment of (-)-1-(p-methoxybenzyl)-2-methyl-1,2,3,4,5,6,7,8-octahydroisoquinoline in cold methylene chloride with m-chloroperbenzoic acid followed by the addition of aqueous ferrous chloride to provide a good yield of (+)-1-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline with substantial if not complete retention of optical activity. The product is an intermediate in a synthesis of the analgesic known as butorphanol.

Abstract: 7-(D-.alpha.-Hydroxy-2-arylacetamido)-3-(2-carboxyalkyl-2,3-dihydro-s-triaz olo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acids and derivatives containing blocking groups on the .alpha.-hydroxy group and their nontoxic, pharmaceutically acceptable salts are valuable as antibacterial agents and are particularly valuable as therapeutic agents in poultry and in animals, including man, in the treatment of infectious diseases caused by many Gram-positive and Gram-negative bacteria. A preferred compound is 7-(D-mandelamido)-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin -3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acid.

Abstract: There are disclosed two new antibiotics formerly denominated MC916-A and MC916-B and now called neothramycin A and neothramycin B which are potent inhibitors of the growth of leukemia cells, e.g. Leukemia L-1210 cells in mice. They are produced by controlled fermentation of Streptomyces FERM-P 2452 (A.T.C.C. 31123).

Abstract: Cephalosporins in a series having the formula ##STR1## wherein R.sup.1 is alkyl containing 1-4 carbon atoms or a nontoxic pharmaceutically acceptable salt thereof, were synthesized and found to be potent antibacterial agents especially when in the form of the syn isomers essentially free of the corresonding anti isomer.

Abstract: Cephalosporins in a series having the formula ##STR1## wherein R.sup.1 is alkyl containing 1-4 carbon atoms and n is 1 or 2 or a nontoxic pharmaceutically acceptable salt thereof, were synthesized and found to be potent antibacterial agents especially when in the form of the syn isomers essentially free of the corresponding anti isomer.

Abstract: There is provided a process for producing a stable macromomycin (hereinafter often referred to as MCR) powder which comprises adding a stablilizer selected from the group consisting of saccharides, amino acids and salts thereof, organic acid salts, inorganic acid salts and a chelating agent to a solution of macromomycin purified from fermentation broth prior to dehydration as by lyophilization.

Abstract: Increased duration of inhibition of secretion of pepsin in man by oral administration of pepstatin is achieved by the use of a formulation in which pepstatin is coated on very small granules of sodium bicarbonate to form floating minicapsules.

Abstract: Certain 7-acylamido-3-[1-carboxymethyl-(or ethyl- or propyl-)-tetrazol-5-ylthiomethyl]-3-cephem-4-carboxylic acids and their salts and easily hydrolyzed esters of the 4-carboxyl group were synthesized and found to be potent antibacterial agents which exhibited good aqueous solubility. A preferred embodiment was 7-(2-aminomethylphenylacetamido)-3-(1-carboxymethyltetrazol-5-ylthiomethyl )-3-cephem-4-carboxylic acid.

Abstract: As new semi-synthetic antibiotic derivative are provided N-methanesulfonic acid derivatives of 3',4'-dideoxykanamycin B which are less toxic than the parent antibiotic and have useful high antibacterial activity. They are produced by interacting 3',4'-dideoxykanamycin B, an aldehyde such as paraformaldehyde and sulfurous acid or an alkali metal sulfite reagent.

Abstract: Compounds having the general formula ##STR1## wherein R.sup.2 is substituted either at the 4'-position or at the 5'-position and is hydrogen, fluoro, bromo, chloro, hydroxy or lower alkyl; R.sup.3 is chloro, bromo or lower alkyl; R.sup.4 is hydroxy, amino or lower alkoxy, and Z is hydrogen or lower alkyl and the nontoxic, pharmaceutically acceptable metal salts of said compounds when Z is hydrogen exhibit strong activities in inhibiting histidine decarboxylase and anthine oxidase.

Abstract: 7-D-.alpha.-Amino-.alpha.-(p-acetoxyphenyl)acetamido-3-methyl-3-cephem-4-ca rboxylic acid is prepared in a form substantially free of the L-isomer and hydrolyzed enzymatically, preferably using wheat bran, to produce p-hydroxycephalexin (cefadroxil).

Abstract: Compounds of the formula ##STR1## wherein A is hydrogen, hydroxy, methyl or methoxy,R.sup.1 is hydrogen, sodium or potassium,R.sup.2 is carboxyl or 2-furyl or an aliphatic, aromatic or heterocyclic radical to which there is also attached a strongly acidic group in the form of its sodium or potassium salt, andR.sup.3 is tetrazol-5-yl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-2-yl, 1,3,4-oxadiazol-3-yl or 1,2,4-triazol-5-yl, each of such groups being unsubstituted or substituted with one or two lower alkyl groups of one to four carbon atoms are prepared by reacting the appropriate aldehyde with the corresponding amphoteric cephalosporin. Preferred products have the structure ##STR2## in which A is --H or --SO.sub.3 Na.

Abstract: Certain 7-acylamido-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on- 6-ylthiomethyl)-3-cephem-4-carboxylic acids and their salts and easily hydrolyzed esters of the 4-carboxyl group were synthesized and found to be potent antibacterial agents which exhibited good aqueous solubility. A preferred embodiment was 7-[o-(methylaminomethyl)phenylacetamido]-3-(2-carboxyalkyl-2,3-dihydro-s-t riazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acid.

Abstract: Compounds having the formula ##STR1## (the meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are indicated hereinafter) exhibit suppressive activity to various immune responses and can be employed in the therapy of immunological diseases, especially autoimmune diseases.

Abstract: Chemical transformation of the dihydrothiazine ring of a cephalosporin into the dihydrooxazine ring (1-oxacephem) was accomplished utilizing the novel intermediate having the structure ##STR1## wherein R is an amino-protecting group and R.sup.1 is the residue of an ester group which can be removed readily without disrupting the remainder of the molecule as illustrated by phenoxyacetyl as R and benzhydryl as R.sup.1.

Abstract: New antitumor agents named aclacinomycins A and B, which are anthracycline glycosides and inhibit the growth of various microorganisms e.g., Staphylococcus aureus, Micrococcus flavus, Corynebacterium bovis and inhibit the growth of animal tumors such as leukemia L1210 and P388 and lymphoma 6C3HED in mice and hepatomas in rats are produced by the fermentation of a microorganism belonging to the genus Streptomyces which has been designated Streptomyces galilaeus (MA144-M1 and A.T.C.C. 31133); they are recovered from the broth by conventional methods for recovering antibiotics.

Abstract: This invention relates to new processes for the production of a 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-3'-deoxy-5-O-pentofuranosylnea mine, including 3'-deoxybutirosins A and B, as a semi-synthetic antibiotic. This invention further relates to new and useful semi-synthetic antibiotics which are produced by the above new processes.

Abstract: Compounds having the structure ##STR1## wherein D is hydrogen or methoxy were synthesized and found to be antibacterial agents.

Abstract: Compounds of the formula ##STR1## wherein A is hydrogen, hydroxy, methyl or methoxy,R.sup.1 is hydrogen, sodium or potassium,R.sup.2 is carboxyl or 2-furyl or an aliphatic, aromatic or heterocyclic radical to which there is also attached a strongly acidic group in the form of its sodium or potassium salt, andR.sup.3 is tetrazol-5-yl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-2-yl, 1,3,4-oxadiazol-3-yl or 1,2,4-triazol-5-yl, each of such groups being unsubstituted or substituted with one or two lower alkyl groups of one to four carbon atoms are prepared by reacting the appropriate aldehyde with the corresponding amphoteric cephalosporin. Preferred products have the structure ##STR2## in which A is --H or --SO.sub.3 Na.

Abstract: Compounds of the formula ##STR1## wherein A is hydrogen, hydroxy, methyl or methoxy,R.sup.1 is hydrogen, sodium or potassium, andR.sup.2 is 1,2,3-triazol-5-yl, such group being unsubstituted or substituted with one or two lower alkyl groups of one to four carbon atoms are prepared by reacting the appropriate aldehyde with the corresponding amphoteric cephalosporin.