Abstract: 2,4-Diaminoquinazoline compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R is a pyrimidinyl, pyrazinyl, pyridazinyl or triazinyl group linked to the piperazine ring by one of its carbon atoms, and optionally substituted by hydroxy, halogen, alkyl, aralkyl, alkoxy, aralkoxy, alkylthio, aryl, aryloxy and certain amino groups; their use as an antihypertensive agent and pharmaceutical compositions containing them.

Abstract: There is presented compounds of the formula ##STR1## in which R.sup.1 represents hydrogen or methyl, as well as readily hydrolyzable esters and salts of these compounds and the hydrates thereof.Also presented are various intermediates and a process to produce the novel derivatives.The acyl derivatives have pharmacological activity as antibacterial agents.

Abstract: 7-(2-Benzothienyl)glycylamido cephalosporins have good gram positive activity and favorable pharmacokinetics and are orally effective.

Abstract: The acetoxymethyl group at the 3-position of 3-acetoxymethylcephalosporanic acids and salts thereof may be replaced by an alkoxymethyl group, by reacting the 3-acetoxymethylcephalosporanic acid or salt thereof with a C.sub.1 -C.sub.4 alkanol in the presence of halide ions.

Abstract: Novel carbostyril derivatives and their salts having antihistaminic effects and are useful as antihistaminic agents, represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkenyl group, a lower alkynyl group or a lower alkyl group which may have phenyl group(s) as the substituted group(s); R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), or a phenyl group which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, lower alkyl groups and lower alkoxy groups; R.sup.4 is a hydrogen atom, a hydroxyl group or a lower alkanoyl group; X is a halogen atom; Y is a lower alkylene group which may have hydroxyl group(s) as the substituent(s); n is 0, 1 or 2; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; provided that when R.sup.

Abstract: 1-Carboxy-(alkanoyl or aralkanoyl)-indoline-2-carboxylic acids, e.g., those of the formula ##STR1## R=H, alkyl, alkoxy, halogeno or CF.sub.3 ; R'=H or R-phenyl;m=0 or 1;p,q=0 to 2;and derivatives thereof, are antihypertensive and cardioactive agents.

Abstract: Substituted imidazo[1,5-c]pyrimidines have been found to have potent bronchodilator activity. Pharmacological methods, pharmaceutical compositions and synthetic intermediates are also disclosed.

Abstract: This invention relates to novel 7-acylaminocephalosporanic acid derivatives of high antimicrobial activity, to processes for their preparation, and to pharmaceutical compositions comprising said derivatives, said derivatives being of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is dialkanoyloxy(lower)alkyl; alkyl having one or more substituents selected from the group consisting of hydroxy, protected hydroxy, alkoxy, carboxy, protected carboxy, cycloalkylcarbonyloxy and heterocyclic group; lower alkoxycarbonyloxy(lower)alkyl; azido(lower)alkoxycarbonyloxy(lower)alkyl; aroyloxy(lower)alkyl; higher alkanoyloxy(lower)alkyl; phthalidyl; or phthalidylidene(lower)alkyl,R.sup.3 is lower alkyl,Y is thio (--S--) or sulfinyl (--S--), and the dotted line represents 2- or 3-cephem nuclei.

Abstract: 2-[2-Hydroxy-3,5-di-tert-octylphenyl]-2H-benzotriazole exhibits outstanding efficacy in protecting organic substrates from light induced deterioration as well as good resistance to loss by volatilization or exudation during the high temperature processing of stabilized compositions.

Abstract: This invention encompasses 7-(S)-acylamino-3-acetoxymethyl-3-cephem-4-carboxylic acid sulfones and the epimerization process for making them. The epimerization process employs an organic nitrogen base reagent having a pKa between about 9.0 to about 11.5. The compounds of this invention are intermediates in the synthesis of 1-oxa-.beta.-lactam antibiotics.

Abstract: Disclosed are esters of substituted 8-hydroxy-1-phenyl-2,3,4,5-tetrahydro-1-H-3-benzazepines represented by the general formula I ##STR1## wherein X is chloro, bromo or trifluoromethyl; R.sub.1 is alkyl, aralkyl, aryl, alkoxyalkyl, aryloxyalkyl, aralkoxyalkyl, cycloalkylalkyl, alkoxycarbonylalkyl, cycloalkyl, 1-adamantyl, cycloalkoxyalkyl, alkoxy, aralkoxy, cycloalkoxy or aryloxy; and the pharmaceutically acceptable acid addition salts thereof. The compounds show neuroleptic, antidepressive and antiaggressive activity.

Abstract: 2,4-Dihydroxypyrimidine (uracil) is prepared from alkali formyl acetic acid ester by reaction with thiourea, heating with chloroacetic acid, and heating with acids.

Abstract: Novel alkyloximes of 7-amino-thiazolyl-acetamido-cephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and --CH.sub.2 --SR', R' is selected from the group consisting of acyl of an alkanoic acid of 2 to 4 carbon atoms, 1-methyl-tetrazolyl and 2-methyl-1,3,4-thiadiazolyl, R.sub.1 is selected from the group consisting of hydrogen and a group easily removeable by acid hydrolysis or hydrogenolysis, R.sub.2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, an alkali metal cation, an equivalent of an alkaline earth metal or magnesium, or organic amine base cation and an ester group easily removeable by acid hydrolysis or hydrogenolysis with the proviso that when R.sub.1 is hydrogen, A is not an ester group easily removeable by hydrogenolysis or acid hydrolysis and the wavy line means that OR.

Abstract: A process for the preparation of indoles which comprises reacting aniline or a derivative thereof with a 1,2-glycol in the presence of a catalyst comprising silver supported on a carrier having a specific surface area of not less than 10 m.sup.2 /g.

Abstract: The present invention relates to derivatives of the family of cephalosporins, of formula: ##STR1## in which ##STR2## is an acid, a salt or an ester of this acid, R.sub.1 is a group of form ##STR3## in which R.sub.A and R.sub.B are H or alkyl or form a saturated cyclobutyl or cyclopentyl ring and R.sub.C is H or COOH, R.sub.2 is a thiazolium salt or a OCOCH.sub.2 R.sub.D group in which R.sub.D is a 1,3-thiazol-4-yl group.The invention also relates to a process for preparing the products of formula (I) and to drugs containing said products.

Abstract: Amides obtained by condensing aminotetrazole with optionally substituted ortho-alkoxybenzoic and ortho-methylthiobenzoic acids are potent anti-allergic agents.

Abstract: Cephalosporin compounds represented by the general formula ##STR1## wherein R represents a group shown by formula ##STR2## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group of 1-3 carbon atoms and R.sup.2 represents a hydrogen atom, a lower alkyl group of 1-3 carbon atoms, a phenyl group which may be substituted by an amino or hydroxy group, a cyano group, a carboxy group, or a carboxymethyl group; said R.sup.1 and R.sup.2 may form a cycloalkylidene group of 4-6 carbon atoms together with the carbon atom to which they are bonded) or a group shown by formula --CH.sub.2 --R.sup.3 (wherein R.sup.3 represents a hydrogen atom, a halogenomethyl group, a carbamoyl group, a carboxymethyl group, .alpha.4-carboxy-3-hydroxyisothiazol-5-yl-thiomethyl group, or .alpha.2-carboxyphenylthiomethyl group); R' represents a group shown by formula ##STR3## (wherein R.sub.a represents a carboxy group, a cyano group, or a carbamoyl group which may be substituted by a lower alkyl group of 1-3 carbon atoms and R.sub.

Abstract: There are described compounds of formula I, ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.7, which may be the same or different, each represent hydrogen, hydroxy, alkyl Cl to 6, alkoxy C1 to 6, amino, acyl C2 to 6, acylamino C2 to 6, alkenyl C2 to 6, halogen, or alkoxy C1 to 6 substituted by phenyl,X is a hydrocarbon chain of 1 to 10 carbon atoms optionally substituted by a hydroxy group,A is --Q--COOH,Q is absent or represents a straight or branched alkylene, alkenylene or alkynylene group of up to and including 6 carbon atoms,R.sub.8 and R.sub.9, which may be the same or different, each represent hydrogen or alkyl C1 to 6 or together form a single bond,D, Y and Z, which may be th same or different, each represent sulphur, oxygen or --NR.sub.10 --, andR.sub.10 is hydrogen or alkyl C1-C6,provided that(i) when D, Z and Y are all oxygen, R.sub.8 and R.sub.9 do not together form a single bond,(ii) when D is oxygen, R.sub.8 and R.sub.9 together form a single bond, X is (CH.sub.2).sub.

Abstract: A process is disclosed for the preparation of racemic cis or trans apovincaminic acid esters of the formula (I) ##STR1## and the corresponding optically active derivatives of the formulae (Ia) ##STR2## wherein R.sup.1 and R.sup.2 are identical or different alkyl groups having 1 to 6 carbon atoms. Apovincaminic acid alkyl esters are well-known vasodilating compounds.

Abstract: 7-(D-2-Naphthylglycylamido)-3-methyl-3-cephem-4-carboxylic acid tetrahydrate is a stable crystal form of a potent orally active gram positive antibiotic.