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: A new piperidine derivative represented by the formula: ##STR1## wherein X is oxygen, sulfur, carbonyl, hydroxymethylene or methylene; R.sub.1 is straight-chain alkylene having 1-4 carbon atoms with or without lower alkyl substituent(s); (A).sub.m and R.sub.2 are usually used substituents; and Y is a monovalent group or a divalent group and is one of the following three groups: ##STR2## wherein when p is 0, B is --N.dbd.N--, ##STR3## and when p is 1, B is ##STR4## wherein (R.sub.3).sub.n is a usually used substituent, has hypotensive activity.
Abstract: Novel N-(heterocyclicaminocarbonyl)carbonyl-substituted benzothiophene- and benzofuransulfonamides are useful as herbicides. The invention also includes novel sulfonamides and sulfonyl isocyanates useful in preparing such compounds.
Abstract: A 5,10-dihydroimidazo[2,1-b]quinazoline in which at least one ring carbon atom, other than the carbon atom in the 2-position, bears a substituent, or a pharmaceutically acceptable acid addition salt thereof is a useful cardiotonic agent and vasodilator in heart insufficiency and a blood platelet aggregation inhibitor.
Abstract: Novel pyrimidine derivatives of the formula; ##STR1## ps wherein Ar is phenyl or naphthyl, which may be substituted by lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, halogen, nitro, trifluoromethyl or di-lower alkylamino; R.sup.1 is lower alkyl, lower cycloalkyl, trifluoromethyl, lower alkoxycarbonyl, phenyl or benzyl, and the phenyl may be substituted by halogen; R.sup.2 is hydrogen or lower alkyl; R.sup.3, R.sup.4 and R.sup.5 are hydrogen,lower alkyl, lower alkenyl or lower alkoxy, or R.sup.3 and R.sup.4 or R.sup.4 and R.sup.5 combine with each other to represent trimethylene, tetramethylene or butadienylene, or salts of them, are excellent antimicrobial agents.
Abstract: Compounds of the formula ##STR1## wherein A is .dbd.CH-- or .dbd.N--;R.sub.1 is (a) hydrogen, lower alkyl, lower alkoxy or a fused benzene ring, or (b) --CO--R.sub.4, tetrazol-5-yl or cyano in the 4- or 5-position;R.sub.2 is --CO--R.sub.4, tetrazol-5-yl, cyano or, when R.sub.1 has one of the meanings included in (b), also hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;R.sub.3 is hydrogen or lower alkanoyl; andR.sub.4 is hydroxyl, amino, hydroxy-amino, tetrazol-5-yl-amino or lower alkoxy;internal salts thereof, and non-toxic salts thereof formed with a basic substance. The compounds as well as their salts are useful as antiallergics.
Type:
Grant
Filed:
August 7, 1979
Date of Patent:
December 23, 1980
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner, Volker Jacobi
Abstract: Tricyclic quinazolines of the formula, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined in the specification, such as 4,5-dihydro-5-arylimidazo[1,2-a]quinazolines, 4,5-dihydro-5-aryl-s-triazolo[4,3-a]quinazolines and 4,5-dihydro-5-aryltetrazolo[1,5-a]quinazolines having anti-inflammatory and analgesic activity are, for example, prepared by reducing the corresponding 4,5-unsaturated compounds, and then, if necessary, by alkylating the thus produced compounds.
Abstract: Dyes for application to hair to impart rich color nuances thereto, include diazamerocyanines, the mesomeric forms thereof and the salts thereof, of the formulaA.dbd.N--N.dbd.
Abstract: The known blood platelet antiaggregative agent 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-one is prepared in high yield via an improved process involving a novel intermediate of the Formula ##STR1## in which R.sup.1 is (lower)alkyl and X is bromo, chloro or iodo.
Type:
Grant
Filed:
April 10, 1978
Date of Patent:
March 27, 1979
Assignee:
Bristol-Myers Company
Inventors:
Thomas A. Jenks, Warren N. Beverung, Jr., Richard A. Partyka
Abstract: An improved and novel process is provided for the reduction of isocyanate groups in organic compounds to formamide groups by catalytic hydrogenation with a noble metal catalyst. The process allows preparation of formamides in consistently high yields from all types of isocyanates.
Abstract: The present invention is concerned with the preparation of chemical intermediates, namely, beta-amino-acrylic acid ester derivatives of nitrogen heterocycles, i.e. pyridine, quinoline, quinoxaline, pyrazine, pyrimidine and the like. Said intermediates are cyclized to form pyrido-pyrimidine type final products possessing analgesic activity.
Type:
Grant
Filed:
September 17, 1975
Date of Patent:
May 16, 1978
Assignee:
Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
Inventors:
Zoltan Meszaros, Jozsef Knoll, Istvan Hermecz, Piroska Simon, Peter Szentmiklosy, Lelle Vasvari, Agnes Horvath, Gabor Horvath, Peter Dvortsak