Abstract: 7-(1-Pyrrolidinyl)-3-quinolonecarboxylic acid derivatives of the formula ##STR1## in which A is CH, CCl, CF or N,R.sup.1 is hydroxyl, hydroymethyl or mercapto andR.sup.2 is hydrogen, alkyl, having 1 to 4 carbon atoms or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl,with the proviso that, when R.sup.1 is hydroxyl, A is not CF or N, or pharmaceutically acceptable hydrates, or salts thereof, are useful as antibacterials and animal feed utilization promoters.
Type:
Grant
Filed:
May 29, 1990
Date of Patent:
October 6, 1992
Assignee:
Bayer Aktiengesellschaft
Inventors:
Uwe Petersen, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
Abstract: A thienocycloheptapyridazine compound of the formula ##STR1## wherein R stands for hydrogen, a halogen or a C.sub.1-4 alkyl, Ar stands for an aryl, a heteroaryl, or an aryl or a heteroaryl having as a substituent at least a halogen, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy, nitro, amino, hydroxy, trifluoromethyl and/or a C.sub.2-5 alkanoylamino; and the bond between 4-position and 42-position represents a single bond or a double bond, which is useful as an antianxiety agent, amnesia-treating drug, a brain function-activating drug or an antidementiac drug.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, or a pharmaceutically acceptable cation;Y is cyclopropyl, ethyl or p-fluorophenyl, and X is hydrogen or fluoro, or X and Y taken together form a group ##STR2## wherein R.sup.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof. Also disclosed are antibacterial pharmaceutical compositions comprising the foregoing compounds, methods of using the compounds in treating bacterial infections, and intermediates for the preparation of the compounds.
Abstract: An imidazo [1,2-b]pyridazine compound of the formula (I): ##STR1## wherein R.sub.1 is a halogen atom or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterolcyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.k (k is zero to two), a group --.circle.A-- is a bivalent three to seven membered homocyclic or heterocyclic group optionally having substituent(s), m.sup.1 and m.sup.2 each is an integer of 0 to 4 and n is an integer of 0 or 1; or its salt, which is useful as antiasthmatics.
Abstract: An improved curing agent for use in coatings, laminates, moldings, castings and adhesives comprising the use of an amine-boron adduct component along with anhydride and epoxy component mixtures. Also provided is an improved process for the preparation of tertiary amine borane curing agents.
Abstract: A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.
Abstract: Antibacterial 5-alkylquinolonecarboxylic acids of the formula ##STR1## in which R.sup.3 is C.sub.1 -C.sub.4 -alkyl,R.sup.1 is optionally substituted alkyl or cycloalkyl, alkenyl, alkoxy, amino or alkylamino or optionally substituted phenyl,R.sup.2 is hydrogen or optionally substituted alkyl,R.sup.4 is a nitrogen-containing heterocyclic radical, andA is hydrogen, halogen, methyl, cyano or nitro, or forms a bridge with R.sup.1.and hydrates and salts thereof.
Type:
Grant
Filed:
October 1, 1990
Date of Patent:
August 18, 1992
Assignee:
Bayer Aktiengesellschaft
Inventors:
Michael Schriewer, Klaus Grohe, Andreas Krebs, Uwe Petersen, Thomas Schenke, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.
Abstract: The invention concerns a heterocycle of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl;and R.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.
Type:
Grant
Filed:
September 5, 1991
Date of Patent:
July 28, 1992
Assignees:
Imperial Chemical Industries PLC, ICI Pharma
Inventors:
Graham C. Crawley, Philip N. Edwards, Jean-Marc M. M. Girodeau
Abstract: Novel 1-phenyl-3-(1-piperazinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain, treating convulsions, and treating depression utilizing compounds or compositions thereof are disclosed.
Abstract: A fluorine-containing phosphate ester of the formula: ##STR1## wherein R.sub.f is a group containing a perfluoroalkyl polyether group of the formula:F(CF.sub.2 CF.sub.2 CF.sub.2 O).sub.m CF.sub.2 CF.sub.2 --wherein m is 2 to 200, and n is an integer of 1 to 3 is used as a rust preventive which can be homogeneously mixed with a fluorine-containing grease.
Abstract: Herbicidally active pyridyloxypyrimidines represented by the following formula [I]: ##STR1## wherein R means a formyl group or an acetal group represented by ##STR2## R.sup.1 and R.sup.2 being the same or different and individually denoting an alkyl group having 1-4 carbon atoms or R.sup.1 and R.sup.2 being coupled together and denoting an alkylene group, R.sup.3, having 2-3 carbon atoms; are prepared by reacting 2 formyl-3-hydroxypyridine or 3-hydroxy-2-pyridine carboxaldehyde acetal with 2 halogeno-4,6 dimethoxypyrimidine in the presence of a base.
Abstract: Pollen suppressants of the formula ##STR1## wherein X represents a group of the formula OR.sup.1 or NR.sup.1 R.sup.2 wherein R.sup.1 represents a C.sub.1 -C.sub.4 alkyl (optionally substituted with a C.sub.1 -C.sub.4 alkoxy group, 1 to 3 halogen atoms, or a carboxy or C.sub.1 -C.sub.4 alkylcarbonyl group), alkenyl (optionally substituted with 1 to 3 halogen atoms), or alkynyl group and R.sup.2 represents H or CH.sub.3, with the proviso that when R.sup.1 is CH.sub.3, R.sup.2 is CH.sub.3 ; Y is hydrogen, C.sub.1 -C.sub.22 linear alkyl or alkenyl containing up to four C.dbd.C double bonds, C.sub.3 -C.sub.6 branched alkyl or alkenyl, C.sub.2 -C.sub.4 alkoxyalkyl, cyclohexylmethyl, halogenated C.sub.1 -C.sub.4 alkyl, phenyl, benzyl, --(CH.sub.2 CH.sub.2 O).sub.m CH.sub.2 CH.sub.3 in which m is an integer from 1 to 5, or --CH(CH.sub.2 OR.sup.4)CH.sub.2 OR.sup.5 or --CH.sub.2 CHOR.sup.4 CH.sub.2 OR.sup.5 in which either R.sup.4 or R.sup.5 but not both represent a C.sub.1 -C.sub.
Type:
Grant
Filed:
November 16, 1990
Date of Patent:
July 14, 1992
Assignees:
Orsan, Orsem
Inventors:
Jeffrey Labovitz, William J. Guilford, Yi Liang, Lawrence Fang, Thomas G. Patterson
Abstract: New imidazo [1,2-c] quinazoline compounds useful as coronary smooth muscle relaxants and corresponding to the formula: ##STR1## in which: Y is oxygen or sulfur;R.sub.1 is (C.sub.1 -C.sub.6) alkyl optionally substituted by a phenyl itself optionally substituted, a (C.sub.3 -C.sub.6) cycloalkyl, optionally substituted phenyl, furyl, thienyl or acyl;R.sub.2 is hydrogen, a halogen or a (C.sub.1 -C.sub.6) alkyl optionally substituted by amino or dialkylamino;R.sub.3 is hydrogen, (C.sub.1 -C.sub.6) alkyl optionally substituted by an aryl, or R--CO--(CH.sub.2).sub.n -- [n being 1, 2 or 3, and R being (C.sub.1 -C.sub.6) alkoxy, amino, (alkyl or dialkyl)amino, morpholino or methylpiperazinyl]; andX is hydrogen or a halogen.These compounds and their physiologically tolerated salts can be used in medical treatment of coronary smooth-muscle dysfunctions.
Type:
Grant
Filed:
March 8, 1991
Date of Patent:
July 7, 1992
Assignee:
Adir et Compagnie
Inventors:
Jean-Jacques Bourguignon, Camille-Georges Wermuth, de la Faverie Renaud, Catherine Thollon, Alain Lombet
Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a trifluoromethoxy substituent in the 5-, 6-, 7-, or 8-position, and methods for their preparation and use, are disclosed. The derivatives are useful anti-inflammatory and analgesic agents.
Abstract: The present invention is directed to the preparation of certain phosphorothioates and phosphonoates by means of a process which employs a three-phase system for the reaction of an alkali metal or alkaline earth metal phenate, pyridinate or pyrimidinate with a phosphorochloridothioate or phosphorochloridate under alkaline conditions and in the presence of tertiary amine and quarternary ammonium salt co-catalyst, but in the absence of both a hydrocarbon or chlorinated hydrocarbon solvent and a surfactant.
Abstract: Heterocyclic-alkylene quinoxalinyloxyphenoxypropanoate compounds having the following formula: ##STR1## wherein n, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification exhibit unexpectedly desirable selective herbicidal activity. Also disclosed are compositions comprising such compounds as well as a method of controlling the growth of undesirable plants employing such compounds.
Type:
Grant
Filed:
July 11, 1989
Date of Patent:
June 9, 1992
Assignee:
Uniroyal Chemical Company, Inc.
Inventors:
Robert G. Davis, Allyn R. Bell, John A. Minatelli
Abstract: The compounds of the formula: ##STR1## in which Q is the quinoxaline nucleus; m is one of the integers 0, 1 or 2; n is one of the integers 1,2 or 3; or a pharmaceutically acceptable salt, alkyl ester or ##STR2## where R.sup.3 and R.sup.4 are, independently, hydrogen, nitro, halo or methoxy, are NMDA antagonists useful in the treatment and prevention of central nervous system related pathological conditions resulting from overstimulation by excitatory amino acids.
Type:
Grant
Filed:
February 15, 1991
Date of Patent:
June 2, 1992
Assignee:
American Home Products Corporation
Inventors:
Ivo L. Jirkovsky, Reinhardt B. Baudy, Lynne P. Greenblatt
Abstract: Novel 8-alkenyl, alkynyl, allenyl and cycloalkyl-quinolinecarboxylic acids are described as antibacterial agents as well as methods of manufacture including novel intermediates used in said manufacture.
Type:
Grant
Filed:
April 18, 1991
Date of Patent:
May 26, 1992
Assignee:
Warner-Lambert Company
Inventors:
John M. Domagala, Mark J. Suto, William R. Turner