Abstract: 4-Hydroxy[1]benzothieno[3,2-f]quinoline-2-carboxylic acids and esters thereof are prepared by the reaction of an optionally substituted 2-aminobenzothiophene with dimethyl acetylenedicarboxylate followed by ring closure. The sulfur atom of the intermediate compounds in the process can be oxidized to oxide or dioxide state, then hydrolyzed to the acids, or first hydrolyzed to the acids and then oxidized, if desired. The acids are physiologically active as anti-allergic agents in the acid form or as salts.

Abstract: The title compounds, which can casually be called 1-oxapenicillins, are produced by total synthesis. Thus 1-oxabenzylpenicillin is produced either by phenylacetylation of 2,2-dimethyl-3R-carboxy-6S-amino-1-oxa-4-aza-5R-bicyclo[3,2,0]heptan-7-one or by hydrolysis and rearrangement of 2-benzyl-6-(1'-methoxycarbonyl-2'-methylprop-1'-enyl)-1-oxa-3,6-diaza-4S, 5R-bicyclo[3,2,0]hept-2-en-7-one.

Abstract: Cephalosporin compounds having a substituted phenylglycyl substituent at the 7-position and any of a variety of groups at the 3-position are prepared by acylation of a 7-aminocephalosporanic acid. The compounds have antibacterial activity.

Abstract: 7,8-Disubstituted-5-acetylquinolines and antimicrobial compositions containing said compounds are disclosed.

Abstract: 2,6-Diamino-1,4-dihydropyridines bearing carbonyl functions in the 3- and 5-positions and being substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2,6-diamino-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an amidine with either an aldehyde or an ylidenecyanoacetoacetic acid ester.

Abstract: The preparation of dl and l compounds of the type 6-(mono and di-substituted phenyl)-5,6-dihydro or 2,3,5,6-tetrahydroimidazo[2,1-b]thiazoles and the pharmaceutically acceptable salts thereof, is described. The use of said compounds for treating helminthiasis in warm-blooded animals is also described.

Abstract: 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##STR1## IN WHICH R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, n and m independently of one another represent 0 or 1 and B represents an optionally substituted 2,6-dioxo- or 2,6-dithioxo-1,2,3,6-tetrahydro-pyrimidyl, 2-thioxo-6-oxo-1,2,3,6-tetrahydropyrimidyl, 2,6-dihydroxy- or 2,6-dimercapto-pyrimidyl, 2-mercapto-6-hydroxy-pyrimidyl, 2,6-diaminopyrimidyl, 2-amino-6-hydroxy-pyrimidyl or 2,6-dihalogenopyrimidyl radical, these radicals being bonded in the 4- or 5-position.

Abstract: The invention relates to novel semisynthetic intermediates or relay compounds of use in the production of cephalosporins and related .beta.-lactam antibiotic compounds. The novel compounds are 3-hydroxy- and 3-oxo-7-amino- and blocked amino --(6R,7R)-cephams. Process for the preparation of the novel compounds are described and exemplified.

Abstract: 3,4-Cycloalkano furoxans are produced and are found to be useful in cross-linking of polymers.

Abstract: The invention concerns a new process for the manufacture of 3-substituted thiomethyl-7-amino-3-cephem-4-carboxylic acid compounds which comprises reacting a 3-y-methyl-7-amino-3-cephem-4-carboxylic acid compound, in which Y is hydroxy or esterified hydroxy, with a mercaptane compound, if necessary, in the presence of an optionally protonic Lewis acid, particularly trifluoroacetic acid.

Abstract: The racemic mixture, and the dextrorotatory enantiomer, of a compound of the formula ##STR1## wherein R is alkyl having from one to four carbon atoms or benzyl, and R.sub.1 and R.sub.2 are each alkyl having from one to four carbon atoms, are useful as analgesic and tranquilizing agents in mammals.

Abstract: 7-Amino-(or 7-acylamido)-3-(disubstituted-amino)-3-cephem-4-carboxylic acid esters are prepared with the corresponding 3-chloro-3-cephem ester or 3-alkyl-(or aryl)-sulfonyloxy-3-cephem esters and a secondary amine, e.g., diphenylmethyl 7-[2-(2-thienyl)acetamido] -3-morpholino-3-cephem-4-carboxylate is prepared with the corresponding 3-methyl-sulfonyloxy ester and morpholine. The 3-amino-substituted cephem esters are useful intermediates undergoing reduction with diborane to the corresponding 3H-3-cephem esters, or, alternatively, they are reacted with Grignard reagents, e.g., phenylmagnesium bromide to provide, for example, the 3-phenyl-3-cephem ester.

Abstract: This invention relates to certain novel .alpha.-amino- or .alpha.-formyl-.alpha.-(p-acyloxyphenyl)acetamidocephalosporanic acids which are useful as antibacterial agents.

Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus bearing a substituent in position 1, said substituent incorporating an acid, ester or amide function therein, are disclosed. The nucleus is further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7, 8, and 9. The derivatives are useful antiinflammatory, analgesic, antibacterial and antifungal agents and methods for their preparation and use are also disclosed.

Abstract: Vinblastine, vincristine and leurosidine are converted to 3-carboxylic acids and 4-desacetyl-3-carboxylic acids, useful as intermediates to prepare aliphatic esters thereof.

Abstract: 2,5-Di-substituted 4-oxazolealkanoic acids and esters thereof of the formula: ##STR1## WHEREIN M REPRESENTS AN INTEGER OF 1 TO 2; R.sup.1 represents an alkyl group having 1 to 4 carbon atoms; n represents an integer of 1 to 2; R represents a mono- or di-substituted phenyl group (in which the substituents are selected from the group consisting of a halogen atom, a methyl group, a methoxy group, a nitro group, a trifluoromethyl group, a phenyl group, a halogen-substituted phenyl group, a phenoxy group and a halogen-substituted phenoxy group), a pyridyl group, a halogen-substituted pyridyl group, a furyl group, a halogen-substituted furyl group, a thienyl group, a halogen-substituted thienyl group, a naphthyl group or a halogen-substituted naphthyl group; when m represents an integer of 1, Y represents an hydrogen atom, an alkyl group having 1 to 2 carbon atoms, a benzyl group or a pyridylmethyl group; and when m represents an integer of 2, Y represents a trimethylene group.

Abstract: The invention relates to magnesium halide derivatives of tetrahydroquinolines and related compounds. These are intermediates useful in the preparation of anti-ulcer agents.

Abstract: Novel thiazolidines, a process for their manufacture, and odorant and/or flavorant compositions containing the novel compounds are disclosed.

Abstract: The invention relates to magnesium halide derivatives of tetrahydroquinolines and related compounds. These are intermediates useful in the preparation of anti-ulcer agents.

Abstract: Disclosed are bi-4-[1-(quinazolinyl-4)piperidyls] and bis{4-[1-(quinazolinyl-4)piperidyl]alkanes}, e.g. 1,3-bis{4-[1-(6,7-dimethylquinazolinyl-4)piperidyl]propane}, having pharmacological activity in animals and useful for example, as anti-obesity and anti-diabetic agents. Said compounds may be prepared by reacting a 4-haloquinazoline with bi-4-piperidyl or a bis(piperidyl-4)alkane.