Abstract: 3,2-Benzoxazepines of the formula ##STR1## and their preparation. In formula (I), R respesents hydrogen or lower alkyl; R.sup.1 represents hydrogen, lower alkyl, lower alkenyl, hydroxy-lower alkyl, carbamyloxy-lower alkyl, acyl, amidino, carbamyl, mono- or di-substituted carbamyl; R.sup.2 may be in position 7 or 8 of the benzoxazepine ring and represents hydrogen, nitro, amino, acetamino or halo. The compounds are prepared by reacting 1,2,4,5-tetrahydro-3,2-benzoxazepine with a reactant which reacts with a secondary amino group to give substitution in the 2-position. The compounds have anti-inflammatory and central nervous system activity.

Abstract: New heterocyclic compounds represented by the following formula: ##STR1## wherein: R and R.sub.1 are independently selected from hydrogen, hydroxy, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.3-5)alkenyloxy, (C.sub.3-5)alkynyloxy, (C.sub.3-6)cycloalkyloxy, or halo or taken together represent a methylenedioxy group; the symbols W and A are defined as follows:1. W is the nitrogen atom and A is the group ##STR2## in which the carbon atom bearing the radical R.sub.2 is linked to the benzene ring and R.sub.2 is hydrogen, hydroxy, (C.sub.1-4)alkoxy or (C.sub.2-4)aliphatic acyloxy;2. W is the group =CH-- and A is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 -- or --CH=CH--.The compounds have antireproductive utility.

Abstract: The antibiotic gardimycin and process for producing said antibiotic by fermentation of strains belonging to the genus Actinoplanes.

Abstract: Compounds of the following formula ##STR1## wherein R is hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec.-butyl or tert.-butyl; R.sub.1 is hydrogen, methyl, ethyl or phenyl; R.sub.2 is hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec.-butyl or tert.-butyl; R.sub.3 is hydrogen, methoxy, trifluoromethyl, chloro, bromo or fluoro; and R.sub.4 is methyl. The new compounds are useful as CNS depressants, anticonvulsants, anti-inflammatories and inhibitors of the enzymes which promote the synthesis of prostaglandins.

Abstract: A process for preparing 6-APA and 7-ACA and derivatives therefore is disclosed wherein a penicillin or cephalosporin substrate is reacted with a molar excess of an oxalyl halide of the formula halCOCOhal whereby the COOM group of the substrate, wherein M represents hydrogen, metal or ammonium cations, is transformed into the group COOCOCOhal.

Abstract: 6-Morpholino-3-substituted phenyl triazolopyridazine compounds such as 8-methyl-6-morpholino-3-phenyl-s-triazolo[4,3-b]pyridazine or 8-methyl-6-morpholino-3-(3,4,5-trimethoxyphenyl)-s-triazolo[4,3-b]pyridazi ne are prepared by the reaction of the corresponding substituted benzoyl halide with a 3-hydrazino-6-morpholinopyridazine in the presence of a hydrogen chloride acceptor or by the reaction of a 3-halo-6-morpholinopyridazine with a corresponding substituted benzoyl hydrazide. The compounds have pharmacological activity as bronchodilators.

Abstract: Imidazolidinone derivatives of the formula ##STR1## where R, R.sub.1, R.sub.2 and R.sub.3 independently are hydrogen or lower alkyl, X represents one or two substituents selected from the group lower alkyl, halo, lower alkoxy, trifluoromethyl, and their pharmaceutically-acceptable acid salts.The compounds are prepared essentially by the method described by Wright in J. Med. Chem. 9, 852 (1966). The compounds have high depressant activity on the central nervous system.

Abstract: Pyrrolo[3,4-d]pyrimidines of the following formula: ##STR1## wherein: R is hydrogen, (C.sub.1-4)alkyl, benzyl or chloro-substituted benzyl;R.sub.1 is hydrogen, (C.sub.1-4)alkyl, phenyl or phenyl substituted with methyl, ethyl, methoxy, hydroxy, chloro, fluoro or bromo;R.sub.2 is hydrogen, (C.sub.1-4)alkyl, phenyl or amino;R.sub.3 is hydrogen or (C.sub.1-4)alkyl;D is a divalent radical selected from the groups ##STR2## wherein the carbon atoms are linked to the carbon atom of the pyrrole nucleus and R.sub.4 represents hydroxy, (C.sub.1-4)alkyl or phenyl; and a salt thereof with a pharmaceutically-acceptable acid. The compounds are useful as antiinflammatories and as prostaglandin synthetase inhibitors.

Abstract: New s-triazolo[5,1-a]isoindole derivatives of following formula I ##STR1## wherein R is selected from hydrogen, amino, lower alkyl amino, di-lower alkyl amino, acylamino, diacylamino, benzoylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R.sub.1 and R.sub.2 each independently represents hydrogen, chloro or lower alkoxy.A process for their manufacture which comprises the reaction of 2-aminophthalimidine with a reagent R-Z wherein R has the same meaning as above, and Z represents one of the following groups: ##STR2## wherein R.sub.3 is C.sub.1 -C.sub.4 alkyl. The compounds and some of the intermediates of the process are useful as antiinflammatories, analgesics, CNS depressants, antimicrobials and anti-fertility agents.

Abstract: High yields of phthalaldehydic acid from .alpha.,.alpha.,.alpha.,.alpha.',.alpha.'-pentachloro-o-xylene can be obtained in an excellent degree of purity if a mixture of said pentachloroxylene and phthalaldehydic acid in water is heated to a temperature between about 80.degree. and about 180.degree. C., and preferably at the boiling temperature of the reaction mixture. The mutual ratio of the reactants is not critical, and may vary within wide ranges, although it is usually preferred to have such a ratio between the said pentachloroxylene and phthalaldehydic acid that for each part by weight of the former at least 0.1 part by weight of the latter is present. Practically, there is no upper limit to the amount of phthalaldehydic acid which may be present, even to a large molecular excess.

Abstract: 4-Substituted-1H-2,3-benzoxazines with a chlorine atom linked to the benzene ring, and a process for their preparation, are described. The compounds are administered as sedative, hypnotic and tranquillizing agents.

Abstract: Hydrazones of 3-formylrifamycin SV of the general formula ##STR1## wherein R.sub.1 is selected from the group hydrogen; alkyl; phenyl; and benzyl; R.sub.2 is selected from the group alkyl; alkenyl; phenyl; and substituted phenyl; with the proviso that when R.sub.1 is hydrogen or alkyl having 1 to 4 carbons, R.sub.2 may not be phenyl; and the 16, 17; 18, 19; 28, 29-hexahydro and 27-demethoxy-27-hydroxy derivatives thereof.

Abstract: Substituted piperazinyliminorifamycins having the following structural formula: ##STR1## wherein Me represents a methyl group and Z represents alkenyl of 3 to 5 carbon atoms, alkynyl of 3 to 5 carbon atoms, 5- or 7-membered cycloalkenyl, cycloalkyl-(C.sub.1 -C.sub.2) alkyl wherein the cycloalkyl moiety is a 3- or 7-membered ring or cycloalkenyl-(C.sub.1 -C.sub.2)alkyl wherein the cycloalkenyl moiety is a 5- or 7-membered ring. The compounds have a broad spectrum antibacterial utility accompanied by a low toxicity.

Abstract: Novel rifamycins characterized by the following structural formula ##STR1## WHEREIN Me represents a methyl group, n represents 3, 4, 5 or 6; g represents 0, 1 or 2; and each R represents a lower alkyl group selected from methyl or ethyl substituting for a hydrogen atom of a --CH.sub.2 -- group; and wherein, when g is 2, the two lower alkyl groups may replace hydrogen atoms of two different methylene groups as well as hydrogen atoms of the same methylene group. The compounds of this invention possess a broad spectrum antibacterial utility accompanied by a low toxicity.

Abstract: Pyrrolo [3,4-d] pyrimidines of the following formula: ##SPC1##The compounds have anti-inflammatory and prostaglandin synthetase inhibitory utility.

Abstract: 2-Nitroimidazole derivatives of the general formula ##SPC1##Wherein R is a lower alkyl group and Y is a member of the group consisting of --CH.sub.2 OH, --CHO, CH.sub.3 CO--, vinyl, formylvinyl, styryl, substituted iminomethyl, 2-benzimidazolyl and 5-amino-1,3,4-thiadiazol-2-yl. The term "lower alkyl" designates aliphatic groups of from 1 to 4 carbon atoms; the term "substituted iminomethyl" designates nitrogen-containing functional derivatives of the aldehydic group. The compounds have antimicrobial activity.

Abstract: Pharmacologically active diphenylmethane derivatives of formula (I) ##SPC1##wherein: R is halo, nitro or lower alkoxy; R.sub.1 is hydrogen, halo, nitro, lower alkyl or lower alkoxy; R.sub.2 is hydrogen, lower acyl, carbamyl or substituted carbamyl; X is an --OR.sub.3 or --NHR.sub.4 group wherein R.sub.3 is hydrogen, lower alkyl, phenyl, substituted phenyl, phenyl-lower alkyl, acyl, carbamyl or substituted carbamyl; R.sub.4 is hydrogen, lower alkyl or lower acyl; and x and y are integers from zero to two, provided that the sum of x and y is at least one. The compounds are prepared by hydrogenation of an o-benzoylbenzoic acid of formula (II) to the corresponding diol of formula (III) according to the following scheme: ##SPC2##Wherein R, R.sub.1, x and y have the same meaning given above and Z is O or H.sub.2. As hydrogenating agents, a hydride or mixed metal hydrides are used. The diols of formula (III) may be subsequently coverted to other inventive compounds of formula (I) by simple chemical operations.

Abstract: Compounds with antiinflammatory, analgesic and CNS depressant activity having the following general formula ##SPC1##WhereinR represents hydrogen or methoxy;R.sub.1 represents hydrogen; lower alkyl; lower alkyl substituted with a group carboxy, carbo(lower alkoxy) or carbamyl; phenyl; benzyl, lower aliphatic acyl; benzoyl; benzoyl substituted with a halo group;R.sub.2 represents hydrogen; lower alkyl; carbo(lower alkoxy); carbamyl; phenylcarbamyl; lower aliphatic acyl; benzoyl; benzoyl substituted with a halo group,R.sub.3 represents halo; lower alkyl; lower alkyl substituted with a group selected from carboxy, carbo(lower alkoxy), carbamyl, halo, amino, mono and di-lower alkylamino, phthalimido and morpholino; phenyl; phenyl substituted with a group selected from lower alkoxy, halo, nitro, amino and acetamido;R.sub.4 represents hydrogen or lower alkyl; with the proviso that when simultaneously R.sub.1 represents hydrogen, methyl, phenyl, benzyl, acetyl or benzoyl, R.sub.

Abstract: Cephalosporin C is recovered from its fermentation broth by in situ formation of N-(p-nitrobenzoyl)cephalosporin C which is extracted therefrom and converted to 7-amino-cephalosporanic acid.

Abstract: Pyrrolo[3,4-b]pyridines which are active as antiinflammatories and prostaglandin synthetase inhibitors and have the following general formula: ##SPC1##Wherein:R is (C.sub.1-4 )alkyl, benzyl or chloro-substituted benzyl;R.sub.1 is hydrogen, (C.sub.1-4 )alkyl, phenyl or methyl-substituted phenyl;R.sub.2 and R.sub.4 independently are (C.sub.1-4 )alkyl, phenyl or hydroxy;R.sub.3 is (C.sub.1-4 )alkyl, (C.sub.1-4 )alkoxy, or phenyl;R.sub.5 is (C.sub.1-4 )alkyl; and a salt thereof with a pharmaceutically acceptable acid.