Abstract: N-Mono or N-disubstituted methyl-2-azetidinones are provided via cyclization of .beta.-hydroxy or .beta.-halo substituted acid sec-amides wherein the amide nitrogen is substituted with a mono- or di-substituted methyl group having activating substituents. Cyclization of .beta.-hydroxy acid amides is mediated by triphenylphosphine-dialkylazodicarboxylate while cyclization of .beta.-halo acid amides is mediated by strong bases e.g. lithium dialkylamides. E.g. Diethyl amino-protected L-serylaminomalonate is cyclized with 200 mole % TPP-diisopropylazodicarboxylate to N-(diethoxycarbonylmethyl)-3-protected-amino-2-azetidinone. The 2-azetidinones provided are useful intermediates.
Abstract: The present invention provides a novel moisturizing lotion which increases the rate of cell renewal on the skin without causing skin irritation and which facilitates the subsequent application of make-up.
Abstract: Methods of controlling Mycoplasma infections which comprise administering to an infected or susceptible warm-blooded animal an effective amount of a new macrocin or lactenocin ester derivative 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; or a pharmaceutically acceptable acid addition salts thereof.
Abstract: Crystalline cephalosporin hydrochloride salt represented by the formula ##STR1## wherein the oxime is in the syn configuration, is a useful pharmaceutical form of, and tool for purification of, the corresponding antibiotic free base; processes for its preparation are provided.
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 a method of producing analgesia in mammals which comprises administering dextropropoxyphene and fluoxetine or norfluoxetine. Pharmaceutical formulations useful in this method are also provided.
Abstract: 11-Thioether and certain C-20 acetal and thioacetal derivatives of tylosin and demycarosyltylosin are effective antibacterial agents. Processes for preparing, formulations containing, and methods of treating bacterial infections with these derivatives are provided.
Abstract: Octahydro-5-oxoindolizine-6-propanoic acids and octahydro-6-oxopyrido[1,2-A]pyridine-7-propanoic acids, the decarboxy and related ester and perhydro derivatives thereof inhibit angiotensin I converting enzyme and are hypotensive agents. Hydrogenation of A58365 factors A and B, obtained by culturing Streptomyces chromofuscus, provides the ACE inhibitors. Also provided are O-acyl and O-sulfonyl derivatives of A and B factors which are useful in preparing deoxy factors A and B via hydrogenolysis.
Abstract: This invention provides for a method of treating anxiety which comprises the administration of fluoxetine or norfluoxetine or pharmaceutically aceptable salts thereof.
Abstract: The present invention is directed to compounds of the formula ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, ##STR2## each of R.sup.2 and R.sup.3 is taken separately and is independently hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, C.sub.3 -C.sub.4 alkynyl, C.sub.3 -C.sub.4 cycloalkyl or C.sub.1 -C.sub.3 alkoxy, orR.sup.2 and R.sup.3 are taken together with the nitrogen atom to which they are attached and form piperidine, morpholine or pyrrolidine;each R.sup.4 independently is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -Cphd 4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy or cyano;X is 0 or S; andm is 0-3;with the provisos that when R.sup.4 is C.sub.1 -C.sub.4 alkyl, that substituent exists at other than the 2 or 6 position of the phenyl ring; and when R.sup.2 is C.sub.1 -C.sub.3 alkoxy, R.sup.3 is other than C.sub.1 -C.sub.3 alkoxy.These compounds exhibit activity as terrestrial herbicides, aquatic herbicides, and aquatic algicides.
Abstract: The present invention relates to electrochemical reduction of a 3-chlorobenzo[b]thiophene to the corresponding 3-hydrobenzo[b]thiophene compound.
Abstract: New Actinoplanes missouriensis strains CUC 014 (NRRL 15647) and CSV 558 (NRRL 15646) which operate together to cosynthesize the useful glycopeptide antibiotic CUC/CSV.
Abstract: N-methyl-S-methyl-N'-[2-(2-dimethylaminomethylthiazol-4-ylmethylthio)ethyl] isothiourea is prepared by the reaction of 2-dimethylaminomethyl-4-(2-aminoethyl)thiomethylthiazole with methylcarbonimidodithioic acid, dimethyl ester, and is a useful intermediate for the preparation of nizatidine, a pharmaceutically valuable H.sub.2 -receptor inhibitor.
Abstract: The present invention pertains to a process for preparing ketones employing a silica catalyzed oxidation of a secondary alcohol with calcium hypochlorite in acetonitrile.
Abstract: The herbicide 5-cyano-1-phenyl-N-methyl-1H-pyrazole-4-carboxamide is prepared in high yield and high purity in a two-step process without isolation of the intermediate.