Abstract: Cyclic imides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-(2,6-dioxo-3-piperidinyl)-4-azaisoindoline-1,3-dione.
Abstract: A process for the preparation of N-allyl compounds of the general formula I ##STR1## in which ##STR2## denotes a nitrogen-containing heterocyclic compound, R.sup.1, R.sup.3, and R.sup.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl,R.sup.2 denotes hydrogen or methyl,n is equal to 1, 2, 3, or 4, andX denotes a water-solubilizing anion,wherein a compound of formula II ##STR3## is caused to react, in aqueous medium, with a compound of formula III ##STR4## in which A denotes a radical which can be eliminated as an anion. The compounds produced by the process of the invention are very well suited for use as brighteners in nickel electroplating.
Type:
Grant
Filed:
October 19, 1994
Date of Patent:
February 25, 1997
Assignee:
BASF Aktiengesellschaft
Inventors:
Bernd Burkhart, Alfred Oftring, Rudi Widder, Ulrich Schroeder
Abstract: This invention encompasses compounds of formula (I), and pharmaceutically acceptable non-toxic salts thereof wherein X and Y am the same or different and represent oxygen or H.sub.2 with the proviso that not both X and Y are H.sub.2 ; W represents phenyl, thienyl, or pyridyl, each of which may be unsubstituted or mono or disubstituted with organic or inorganic substituents; and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables representing organic and inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorder overdose with benzodiazepine drugs, and enhancement of memory.
Abstract: This invention concerns compounds having the Z-configuration of formula: ##STR1## or salts thereof, wherein R represents an optionally substituted aryl or heteroaryl radical, R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, carboxy, hydroxy (C.sub.1 -C.sub.6)alkyl, halogen, halo(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl, optionally substituted aryl or heteroaryl or optionally substituted aralkyl or heteroarylalkyl; n represents 0, 1 or 2; R.sup.4 and R.sup.5 each independently represent hydrogen or a substituent selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl or R.sup.4 and R.sup.5 are geminal C.sub.1 -C.sub.6 alkyl substituents and R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl which possess antiinflammatory activity.
Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
Abstract: A process for the preparation of 1-substituted,4-substituted-1H-imidazo-[4,5-c]quinolines, intermediates in the preparation of such compounds, and processes for the preparation of such intermediates.
Abstract: Compounds of the formula I ##STR1## and tautomeric forms thereof, of the formula Ia, ##STR2## in which the substituents R1-R4 and X and Y have the meanings given; have an antiviral activity.
Type:
Grant
Filed:
January 13, 1995
Date of Patent:
February 11, 1997
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Uta-Maria Billhardt-Troughton, Manfred R osner, Rudolph Bender, Christoph Meichsner
Abstract: This invention concerns compounds having the Z-configuration of formula: ##STR1## or salts thereof, wherein R represents an optionally substituted aryl or heteroaryl radical, R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, carboxy, hydroxy (C.sub.1 -C.sub.6)alkyl, halogen, halo(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl, optionally substituted aryl or heteroaryl or optionally substituted aralkyl or heteroarylalkyl; n represents O, 1 or 2; R.sup.4 and R.sup.5 each independently represent hydrogen or a substituent selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl or R.sup.4 and R.sup.5 are geminal C.sub.1 -C.sub.6 alkyl substituents and R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl which possess antiinflammatory activity.
Abstract: The present invention provides methods for screening drug compounds utilizing compounds of formulas I and II, where formulas I and II are ##STR1## and the pharmaceutically acceptable salts thereof where: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent hydrogen, halogen, alkyl or alkoxy substituents;R5 is hydrogen or lower alkyl;X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; andZ is hydrogen or fluorine.The invention also provides tritium or iodine isotope radiolabeled compounds of the formulas I and II radiolabeled with tritium or isotopes of iodine.The invention further provides novel GABAa receptor subtypes which specifically bind to compounds of formulas I or II.The invention also provides GABAa receptor subtypes which are bound in situ to a compound of formula I or II.The compounds provided herein bind selectively to a novel subtype of the GABAa binding site.
Type:
Grant
Filed:
April 30, 1992
Date of Patent:
January 28, 1997
Assignee:
Neurogen Corporation
Inventors:
Kenneth Shaw, Alan Hutchison, Andrew Thurkauf, John Tallman
Abstract: 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methylaminopiperidin-1-yl )-4-oxoquinoline-3-carboxylic acid dihydrate having the following formula: ##STR1## The crystal of this dihydrate exhibits excellent stability over the other crystal forms under various pharmaceutical formulation conditions such as moisture absorption and blending in solvents and, hence, it is a most advantageous crystal form in the manufacture of pharmaceuticals.
Abstract: Substituted quinol-2-yl-methoxy-phenylacetic acid derivatives are prepared by reacting correspondingly substituted phenols with quinolylmethyl halides or by reacting unsubstituted phenols with quinolylmethyl halides and subsequent alkylation. The substituted quinol-2-yl-methoxy-phenylacetic acid derivatives may be employed as active substances in medicaments.
Type:
Grant
Filed:
August 4, 1993
Date of Patent:
January 28, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Michael Matzke, Klaus-Helmut Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Reiner M uller-Peddinghaus, Armin Hatzelmann
Abstract: Novel aminoquinoline derivatives of the general formula ##STR1## are described. Also described are methods for the treatment of malaria pathogens, particularly chloroquine-resistance malaria pathogens with compounds of formula I or the pharmaceutically acceptable salts and hydrolyzable esters thereof.
Type:
Grant
Filed:
October 26, 1994
Date of Patent:
January 21, 1997
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Werner Hofheinz, Catherine Jaquet, Syn ese Jolidon
Abstract: This invention provides a carbostyril derivative of the formula (1): ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined, or its salt. This carbostyril derivative or its salt possess an excellent matrix metalloproteinases inhibitory action.
Abstract: An improved process for the preparation of 2,3,5,6-tetrachloropyridine of the formula ##STR1## consists in that 3,3,5-trichloroglutarimide of the formule ##STR2## is reacted either a. with phosphorus trichloride or phosphorus oxytrichloride or mixtures thereof in the presence from the start of catalytic amounts of hydrogen chloride, followed by a conversion of polyphosphorous compounds formed into phosphorus oxytrichloride by supplying chlorine, optionally only after supplying further phosphorus trichloride, orb. with phosphorus trichloride and chlorine, optionally in the presence of phosphorus oxytrichloride as a solvent, followed by a dehydrochlorination of the reaction mixture and finally conversion of polyphosphorus compounds formed into phosphorus oxytrichloride by supplying chlorine, optionally only after supplying further phosphorus trichloride.Improved yields of a purer product are obtained.
Abstract: Peripheral vasodilating agents containing, as the active ingredient, carbostyril derivatives represented by the general formula: ##STR1## or a salt thereof; and novel carbostyril derivatives included within the scope of the above-mentioned general formula.
Abstract: Substituted heteroarylalkylthiopyridines of the formula (I) ##STR1## are suitable for treating conditions caused by Helicobacter bacteria, in particular the strain Helicobacter pylori.
Abstract: The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar) R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.
Type:
Grant
Filed:
May 26, 1995
Date of Patent:
December 24, 1996
Assignee:
Farmitalia Carlo Erba S.r.L.
Inventors:
Franco Buzzetti, Silvia Fustinoni, Maria G. Brasca, Sergio Penco
Abstract: The present invention relates to hitherto unknown compounds of formula; Y stands for --CH.dbd.CH--; R.sub.1 is hydrogen or halogen, preferably fluorine, chlorine or bromine; R.sub.2 is halogen, preferably fluorine, chlorine or bromine, CH.sub.3, OCH.sub.3, NO.sub.2 or CF.sub.3, and n=0-3, preferably 0, 1 or 2; A stands for an acidic group, e.g. carboxy, 1-H-tetrazolyl or a hydroxamic acid group. The present compounds are of value in the human and veterinary practice as lipoxygenase inhibitors and/or leukotriene antagonists.
Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.
Type:
Grant
Filed:
May 19, 1995
Date of Patent:
November 19, 1996
Assignee:
Eli Lilly and Company
Inventors:
Anita Melikian-Badalian, Paul L. Ornstein