Abstract: The present invention is directed to new 4,7-dihydro-pyrazolo[3,4-b]pyridines. The compounds possess Ca.sup.2+ -antagonist, antihypertensive, vasodilating and antiangina activity. A process for producing them as well as pharmaceutical compositions containing them are also described.
Abstract: There are disclosed new naphthyridine- and quinoline-carboxylic acids having a 1-tertiary-alkyl substituent, compositions containing them, and their use in treating bacterial infections in warm-blooded animals. Also disclosed are novel amines and intermediates used in the preparation of the naphthyridine- and quinoline-carboxylic acids.
Type:
Grant
Filed:
December 19, 1988
Date of Patent:
September 4, 1990
Assignee:
Bristol-Myers Company
Inventors:
Abraham Weber, Daniel Bouzard, Munir Essiz, Pierre Di Cesare, Jean-Pierre Jacquet, Philippe Remuzon
Abstract: Bicyclo[3.3.1]nonane derivatives of the general formula (I) ##STR1## where n is an integer from 1 to 70,R.sup.1 is hydrogen,R.sup.2 is hydrogen or hydroxyl, or the radical ##STR2## R.sup.3 and R.sup.4 are each independently of the other phenyl or 1- or 2-naphthyl, which phenyl or naphthyl may each be substituted by 1, 2 or 3 C.sub.1 -C.sub.12 -alkyls, C.sub.1 -C.sub.12 -alkoxys, chlorines, bromines, fluorines, trifluoromethyls or cyanos, in the case of 2 or 3 substituents these substituents being identical or different,A and B are each independently of the other a chemical bond, C.sub.1 -C.sub.22 -alkylene, cycloalkylene ##STR3## where m and o are each from 1 to 20 andR.sup.10 is hydrogen, C.sub.1 -C.sub.22 -alkyl, C.sub.5 -C.sub.12 -cycloalkyl, C.sub.7 -C.sub.18 -phenylalkyl, phenyl or C.sub.2 -C.sub.22 -cyanoalkyl,M is a radical of the formula ##STR4## which may be bonded to A not only via the nitrogen atom but also via the carbon atom, andR.sup.11, R.sup.12, R.sup.13 and R.sup.
Type:
Grant
Filed:
December 10, 1988
Date of Patent:
July 24, 1990
Assignee:
BASF Aktiengesellschaft
Inventors:
Alexander Aumueller, Peter Neumann, Hubert Trauth
Abstract: The two enantiomers of the anti-depressant drug of the formula I ##STR1## are disclosed. Methods for resolving intermediates and their steroselective conversion to a corresponding enatiomer of I are also disclosed.
Abstract: Novel 1-alkyl substituted benzimidazole derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.
Type:
Grant
Filed:
February 6, 1989
Date of Patent:
July 24, 1990
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Frans E. Janssens, Gaston S. M. Diels, Joseph L. G. Torremans, Francois M. Sommen
Abstract: A process is disclosed for increasing the recovery of maleic anhydride from the product condenser. Maleic anhydride is added to the oxidation reactor gaseous effluent. Maleic acid buildup in the condenser is reduced; condenser plugging is reduced; and process run time required to build up to production rates after periodic cleaning can be reduced.
Type:
Grant
Filed:
August 23, 1989
Date of Patent:
July 17, 1990
Assignee:
Amoco Corporation
Inventors:
Stephen C. Ceisel, James F. Conrad, Elizabeth M. Lestan, Allen P. Nelson
Abstract: Compounds of the formula I: ##STR1## wherein X is the residue of an unsubstituted 6-membered aromatic ring having 3 carbon atoms and one nitrogen atom;R.sup.1 is C.sub.1-6 primary alkyl (free of asymmetric carbon atoms), or isopropyl;R.sup.2 is substituted or unsubstituted phenyl, primary or secondary C.sub.1-6 alkyl (free of asymmetric carbons),C.sub.3-6 cycloalkyl or phenalkyl as defined in the Specification ##STR2## in which R.sup.8 is hydrogen, R.sup.9 or M, whereinR.sup.9 is a physiologically acceptable and hydrolyzable ester group, andM is a pharmaceutically acceptable cation;are obtained by multi-step processes and are useful as cholesterol biosynthesis inhibitors.
Type:
Grant
Filed:
March 8, 1989
Date of Patent:
July 3, 1990
Assignee:
Sandoz Pharm. Corp.
Inventors:
Paul L. Anderson, Faizulla G. Kathawala, Nicholas A. Paolella, Sompong Wattanasin
Abstract: Substituted 4-aminothienopyridine derivatives which are inhibitors of gastric acid secretion. A compound of the invention is 6-butyryl-7-(2-isopropylphenylamino)-thieno[3,2-b]pyridine.
Type:
Grant
Filed:
February 23, 1989
Date of Patent:
June 19, 1990
Assignee:
SmithKline Beckman Intercredit B.V.
Inventors:
Robert J. Ife, Thomas H. Brown, Colin A. Leach
Abstract: Sulfoxide derivatives having the formula (I) or (V) show a gastric acid-secretion inhibitory effect: ##STR1## wherein each of R.sup.1 and R.sup.2 is hydrogen, lower alkyl, hydroxyalkyl, phenyl, phenylalkyl or cycloalkyl, R.sup.1 and R.sup.2 may form together with the adjacent N atom a heterocyclic group; each of R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 is hydrogen, halogen, lower alkoxy, lower alkyl, trifluoromethyl, or fluorine atom-containing lower alkoxy; Y is CH or N; and Z is unsubstituted or substituted 2-pyridine or 2-aminophenyl.
Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
Type:
Grant
Filed:
January 30, 1989
Date of Patent:
June 12, 1990
Assignee:
Merck Frosst Canada, Inc.
Inventors:
Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
Abstract: A fogged direct positive photographic silver halide emulsion containing a sensitizing amount of at least one cyanine dye defined above, e.g., cyanine dye containing a 1-phenylindole nucleus substituted in the 2-position with the 3-pyridyl group. The said cyanine dye is also covered. The dye useful in sensitizing the silver halide emulsion useful for fogged direct-positive films.
Abstract: The invention relates to new heterocyclic substituted bicyclic triazoles of general formula I ##STR1## in which X, Y, Z, R.sup.1, n and m have the meanings given in the description, processes for their preparation and their use as herbicides.
Type:
Grant
Filed:
November 28, 1988
Date of Patent:
May 15, 1990
Assignee:
Schering Aktiengesellschaft
Inventors:
Friedhelm Blume, Gabriele Dorfmeister, Wilfried Franke, Richard Rees, Gerhard Johann, Friedrich Arndt
Abstract: The disclosure deals with a pyrazolopyridine compound of the formula ##STR1## wherein the variables are defined in the specification. The compounds are useful as a diuretic, antihypertensive agent, etc.
Abstract: The present invention relates to novel compounds of the following formula: ##STR1## individual isomers and pharmaceutically acceptable acid addition salts thereof, whereinR.sup.1 is hydrogen, alkyl or phenyl-lower alkyl, in which the phenyl group may be substituted with halogen, lower alkyl or lower alkoxy;R.sup.2 is alkyl, alkenyl, alkynyl, branched or unbranched, with 1-6 carbon atoms inclusive, which group may be optionally substituted with fluoro, hydroxy or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy;R.sup.3 and R.sup.4 are the same or different, and each represents hydrogen, alkyl(1-6 C-atoms), cycloalkyl (3-6 C-atoms), phenyl optionally substituted with halogen trifluoromethyl, lower alkyl, hydroxy or lower alkoxy, or phenyl-lower alkyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy.
Type:
Grant
Filed:
March 13, 1989
Date of Patent:
May 8, 1990
Assignee:
H. Lundbeck A/S
Inventors:
Povl Krogsgaard-Larsen, Erik Falch, Henrik Pedersen
Abstract: Process for obtaining maleic anhydride that is not prone to discolor by treating crude maleic anhydride with oxygen, a gas mixture containing oxygen, or a substance that releases oxygen before or while it is distilled.
Type:
Grant
Filed:
January 4, 1989
Date of Patent:
May 1, 1990
Assignee:
BASF Aktiengesellschaft
Inventors:
Gerhard Michl, Rolf Seubert, Johannes E. Schmidt
Abstract: The invention relates to an imidazopyridine compound of the following formula: ##STR1## wherein R.sup.1 is lower alkynyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl, R.sup.4 is amino or acylamino, R.sup.5 is hydrogen; lower alkyl which may be substituted by halogen, halogen; nitro; amino; acylamino; esterified carboxy; or N,N-di(lower)alkylsufamoyl, and A is lower alkylene, and pharmaceutically acceptable salts thereof, useful in the treatment of ulcers.
Abstract: The present invention provides ketones of the general formula (I): ##STR1## and physiologically acceptable salts and solvates thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, each represents a hydrogen atom or a C.sub.1-6 alkyl group; Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.3, R.sup.4 and R.sup.5 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenyl C.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and an aromatic or heteroaromatic group as defined in the specification.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.
Type:
Grant
Filed:
April 13, 1988
Date of Patent:
April 17, 1990
Assignee:
Glaxo Group Limited
Inventors:
Alexander W. Oxford, David J. Cavalla, Peter C. North