Abstract: A method for synthesizing .DELTA..sup.3 -7-substituted amino desacetoxy cephalosporanic acid from a penicillin sulfoxide or its alkylsilylated ester derivative is provided. According to the method, penicillin sulfoxide is heated in the presence of an organic ammonium salt catalyst and a copolymer composed of dimethylsilane and urea units until formation of the cephalosporanic acid occurs by ring expansion reaction. The copolymer functions both as a dehydrating agent for removing the water by-product generated from the reaction as well as an esterifying agent for converting penicillin sulfoxide into its dimethylsilyl ester derivative. The method of the invention produces high yields of the cephalosporanic acid and avoids the need for excess dimethylsilyating agents.

Abstract: For binding 5-HT.sub.

Abstract: This invention describes Cu complexes of bis-oxazolines and their use. These compounds have the following formulas: ##STR1##This project is supported in part by N. I. H. grant GM-35879.

Abstract: The present invention provides a compound having the structure: ##STR1## The present invention also provides a method for synthesizing a compound having the above-identified structure as well as the intermediate compounds produced according to that method. The present invention further provides a pharmaceutical composition comprising the above compounds. Lastly, the present invention provides a method of inhibiting growth of tumor cells.

Abstract: An ester of 7-acylamido-3-acylthio-3- or -2-cephem-4-carboxylic acid represented by general formula (1) ##STR1## wherein R.sup.1 is an acyl group, R.sup.2 is a carboxyl-protecting group, R.sup.3 is a lower alkyl group, an aryl group or a substituted aryl group, or a mixture of two or more of said ester is used as the starting compound and is reacted wit a tertiary amine and also a secondary amine. Then the tertiary amine salt compound as formed as the reaction product is reacted with a compound of formula (4)R.sup.4 --X (4)wherein R.sup.4 is a lower alkyl group, a cycloalkyl group or a heterocyclic group or a heterocyclic group-substituted methyl group and X is a leaving group, whereby the desired ester of 7-acylamido-3-substituted thio-3-cephem-4-carboxylic acid of formula (5) ##STR2## can be produced preferentially, conveniently and efficiently.

Abstract: .alpha.-Fluoro-substituted N-acryloylamino acid derivatives of the formula ##STR1## are used to make polymers optionally for chromatographic resolution of racemates into their enantiomers. The fluorine atom improves performance in many instances.

Abstract: The present invention relates to a cephalosporin compound including the pharmaceutically acceptable non-toxic salts, physiologically hydrolyzable esters, hydrates and solvates thereof of the formula(I) and its isomers: ##STR1## wherein: R.sup.1 is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl or --C(R.sup.3)(R.sup.4)COOH wherein R.sup.3 and R.sup.4, which may be the same or different, are hydrogen, C.sub.1-4 alkyl group, or constitute a C.sub.3-7 cycloalkyl group with the carbon atoms to which R.sup.3 and R.sup.4 are attached;R.sup.2, which may be attached to N.sup.a or N.sup.b, is a C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-7 cycloalkyl, aryl or amino group; andQ.sub.1 and Q.sub.2, which may be the same or different, are CH or N.

Abstract: Water-insoluble naphthalic acid imide dyestuffs of the following formula: ##STR1## wherein D is ##STR2## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl which may be substituted, R.sup.2 is hydrogen, halogen, lower alkyl, lower alkoxy or cyano, X is oxygen or sulfur, and m is 0 or 1; A is phenylene, alkylene, aralkylene or --C.sub.2 H.sub.4 OC.sub.2 H.sub.4 --; B is oxygen, sulfur or ##STR3## wherein R.sup.3 is hydrogen or lower alkyl; Y is a 6-membered nitrogen-containing heterocyclic ring having at least one active halogen atom; and n is 0 or 1.

Abstract: The present invention provides a thiazolinoazetidinone derivative represented by the formula ##STR1## wherein R.sup.1 is phenyl having or not having substituent(s), methyl having or not having substituent(s) or ##STR2## group, R.sup.3 being phenyl having or not having substituent(s), and R.sup.2 is a hydrogen atom or carboxylic acid protective group, and a process for preparing the same.The present invention further provides a process for preparing a 2-exo-methylenepenam derivative characterized by hydrolyzing the thiazoline ring of a thiazolinoazetidinone derivative of the above formula (1) to effect recyclization and obtain a 2-exo-methylenepenam derivative represented by the formula ##STR3## wherein R.sup.1 and R.sup.2 are as defined above.

Abstract: A particulate composition comprising an isothiazolinone or isothiazolothione or a salt or complex thereof and a water soluble metal salt. The salt is typically a metal salt, for example the sodium salt of 1,2-benzisothiazolin-3-one and the water soluble metal salt is particularly an alkali metal salt such as disodium hydrogen phosphate. A preferred composition can be obtained by stirring together an isothiazolinone or isothiazolothione, a base and an alkali metal phosphate in the presence of water until a dry particulate product is obtained. The particulate product is typically highly and rapidly soluble in water and may be stored in a container formed from a water soluble material, for example a bag formed from polyvinyl alcohol.

Abstract: A method of crystallizing (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio- 6[(R)-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate (hereinafter simply referred to as L-627), which is characterized by maintaining an aqueous solution of L-627 at temperatures ranging from the eutectic temperature of the solution to temperatures lower than 0.degree. C.The method provides some advantages that loss of L-627 accompanied by crystallization is less, number of steps in the preparation of vial formulations is less and maintenance of these steps under sterile and dust-free conditions can be performed easily, dispensation of the drug can be conducted with quantitative accuracy, and the crystals dissolve in a solvent promptly at the time of use.

Abstract: The present invention relates to a process for the preparation of 5-aryl tetrazoles of the formula: ##STR1## or a salt thereof comprising reacting an aryl nitrile with a trisubstituted silyl azide and a disubstituted tin oxide.

Abstract: The present invention provides a method for treating osteoporosis in a mammal comprising administering to said mammal a therapeutically-effective amount of a compound of Formula I: ##STR1##

Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.5 is hydrogen, alkyl of 1-6 carbon atoms, benzyl, triphenylmethyl, or Sn(alkyl of 1-6 carbon atoms).sub.3 ;n is 1 to 3;Y is ##STR5## wherein R.sup.3 is hydrogen, perfluoro alkyl of 1-6 carbon atoms, trifluoromethylalkyl of 1-6 carbon atoms, or alkyl of 1-6 carbon atoms; and R.sup.4 is hydrogen or alkyl of 1-6 carbon atoms;with the proviso that when R.sup.1 is ##STR6## then R.sup.2 cannot be ##STR7## wherein X is as defined above; and the pharmaceutically acceptable salts thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure.

Abstract: Novel semi-synthetic cephalosporin derivatives having a fused pyridiniummethyl at 3-position of the cephem nucleus, pharmaceutically acceptable salts, physiologically hydrolizable esters or solvates thereof are disclosed. Also disclosed is a process for preparing the cephalosporin derivatives which comprises introducing a fused pyridiniummethyl substituent at 3-position of 7-.beta.-[(Z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetamido]-3-cephem-ca rboxylic acid derivatives. The compounds of the present invention show potent antibacterial activities and a broad spectrum against both gram-positive and gram-negative bacteria.

Abstract: The invention herein relates to titled compounds having the structure ##STR1## wherein the R.sub.1 -(R.sub.4).sub.n members are as defined in the claims. Characteristic features of these compounds are the haloalkyl R.sub.2 radical and cyclization of two R.sub.4 members at the meta and para positions of the phenyl ring to form a substituted benzoxazinone ring fused to the phenyl or benzthiazinone ring. Such compounds are useful as active ingredients in herbicidal compositions to control undesirable weeds in various crops.

Abstract: The invention relates to a novel stable form of cephradine, processes for its production and intermediates used therein.

Abstract: 7 .alpha.-formamido cephalosporin derivatives having a 3[N-(optionally substituted)aminothiopyridinium thiomethyl] substituent have anti-bacterial activity and are of use in anti-bacterial therapy. Processes for the preparation thereof and intermediates for use in these processes are also disclosed.

Abstract: The invention relates to new 3-substituted cephalosporins, to a process for their preparation and to their use as medicaments, in particular as medicaments having antibacterial activity.The invention relates to compounds of the general formula (I) ##STR1## in which X, Y, R.sup.1 and R.sup.2 have the meaning indicated in the description.

Abstract: Antimicrobial quinolnyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A, R.sup.6, R.sup.7, and R.sup.8 form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.