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: 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: The compounds of the formula ##SPC1##In which R independently is hydrogen, lower alkyl, lower alkoxy, halo or trifluoromethyl; x is 1 to 2; n is 1 to 3, and R.sub.1 and R.sub.2 independently are hydrogen, lower alkyl or phenyl and together with the nitrogen atom form a heterocycle which may contain an oxygen atom as a hetero atom. The compounds are prepared by reacting the corresponding N-substituted-1-(arylthio)methanesulfonamide with small, incremental amounts up to substantially equimolar of 30% hydrogen peroxide in glacial acetic acid at 65.degree.-70.degree. C., to obtain the sulfinyl compound, or substantially two equimolar proportions of 30% hydrogen peroxide in glacial acetic acid at reflux temperature to obtain the sulfonyl compound, and recovering the corresponding sulfinyl or sulfonyl product.

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: Mono- and poly-phenols and derivatives thereof are ring acylated by a Friedel-Crafts acylation reaction in which the hydroxy groups are protected by prior silylation.

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: Pharmacologically active 1-substituted 4-(.beta.-2-quinolylethyl)piperazines of the formula ##SPC1##And their 1,2,3,4-tetrahydroquinolylethyl analogues, wherein R represents a lower alkyl, a phenyl, benzyl or a phenethyl group; and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof.

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.

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: 2-(Pyrrol-1-yl)amino-4,5-dihydro-1H-imidazole derivatives of the following general formula I ##SPC1##wherein R, R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are independently selected from the class consisting of hydrogen, lower alkyl, carbo-lower alkoxy, phenyl, substituted phenyl, R.sub.4 represents hydrogen or lower alkyl, n is an integer and may be 2 or 3. The corresponding pharmaceutically acceptable acid addition salts of the substances of formula I above are considered as a part of the invention. The invention compounds display very interesting anthypertensive properties.

Abstract: Antimicrobial substances of the rifamycin family corresponding to the formula ##SPC1##Wherein R is a substituted lower alkyl radical of the formula --(CH.sub.2).sub.n --A wherein n is the number 2 or 3, A stands for a hydroxyl group or for an ##EQU1## group where R.sub.3 and R.sub.4 individually may be hydrogen, lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or cycloalkyl and together with the nitrogen atom to which they are attached a heterocyclic ring; R.sub.1 is hydrogen or taken with R it may represent a lower alkylene radical to complete with the nitrogen atoms to which they are attached a heterocyclic ring; R.sub.2 is hydrogen or, when the nitrogen atom to which it is attached is a part of a heterocyclic ring a lower alkyl group. The compounds are prepared by condensing 4-guanylazo-4-deoxyrifamycin SV with a substituted aliphatic amine derivative corresponding to the formula H.sub.2 N--(CH.sub.2).sub.n --A wherein n and A have the significance previously given.

Abstract: The novel antibiotic, lipiarmycin, is prepared by cultivating Actinoplanes deccanensis A/10655, ATCC 21983, under aerobic conditions in a fermentation broth, from which it is then recovered.

Abstract: New reserpine-like compounds of the general formula ##SPC1##Wherein R is a member of the class consisting of hydrogen, lower alkyl, lower alkenyl and acyl; R.sub.1 is selected from hydrogen and lower alkyl, and R.sub.2 is hydrogen or lower alkyl. The new reserpine-like compounds are useful anti-hypertensive agents.

Abstract: Fibrinogen peptide derivatives which have biological activity as anticoagulants of blood having the dipeptide moiety prolylarginine or the tripeptide moiety glycylprolylarginine, e.g., L-prolyl-L-arginine benzyl ester p-toluenesulfonate trifluoroacetate, glycyl-L-prolyl-L-arginine benzyl ester p-toluenesulfonate trifluoroacetate, N-t-butyloxycarbonyl-L-prolyl-L-arginine benzyl ester p-toluenesulfonate methanolate, N-benzyloxycarbonyl-prolyl-L-arginine benzyl ester p-toluenesulfonate methanolate and N-t-butyloxycarbonylglycol-L-prolyl-L-arginine benzyl ester p-toluenesulfonate.

Abstract: A new class of 2,3-benzoxazepine compounds of the formula ##SPC1##In the formula, R is heterocyclic acyl or heterocyclic acetyl. The compounds have central nervous system and anti-inflammatory activity.

Abstract: A thiolsulfonate is reacted with an aminecarbodithioate salt to give an aminecarbotrithioate product. The products of this invention have biological activity, particularly in controlling microorganisms and other pests.