Abstract: 6,11'-Cyclyl-1,2,3,4,5,6,11,11a-octahydrobenzo[b]quinolizine derivatives, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
Type:
Grant
Filed:
October 7, 1994
Date of Patent:
July 18, 1995
Assignee:
Sterling Winthrop Inc.
Inventors:
Diane L. DeHaven-Hudkins, William G. Earley, John P. Mallamo, Garry M. Pilling
Abstract: An asymmetric synthesis of (S)-(-)-6-chloro-4-cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-qu inazolinone comprises the chiral addition of 2-pyridylacetylide to N.sup.1 -protected 6-chloro-4-cyclopropyl-2-quinazolinone followed by removal of the protecting group.
Type:
Grant
Filed:
November 8, 1993
Date of Patent:
July 18, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Mark A. Huffman, Nobuyoshi Yasuda, Ann E. DeCamp, Edward J. J. Grabowski
Abstract: The invention relates to cyclic imino derivatives of general formula ##STR1## wherein A to G, R.sub.1, Z.sub.1 to Z.sub.6, X and Y are defined as in claim 1, the tautomers, stereoisomers and mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting properties, pharmaceutical compositions which contain these compounds and processes for preparing them.
Type:
Grant
Filed:
August 28, 1992
Date of Patent:
July 18, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Volhard Austel, Helmut Pieper, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
Abstract: A series of novel alkoxypyridin-4-yl and alkoxypyrimidin-4-yl derivatives of indol-3-ylalkylpiperazines of Formula I are intended to be useful agents ##STR1## for alleviation of vascular headache on the basis of their potent affinity and agonist activity at 5-HT1D binding sites.
Type:
Grant
Filed:
April 26, 1994
Date of Patent:
July 18, 1995
Assignee:
Bristol-Myers Squibb Company
Inventors:
David W. Smith, Joseph P. Yevich, Andrew Williams, Edward H. Ruediger, Keith D. Combrink, Bradley C. Pearce
Abstract: 6,11-Substituted-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
Type:
Grant
Filed:
October 25, 1994
Date of Patent:
July 4, 1995
Assignee:
Sterling Winthrop Inc.
Inventors:
Diane L. DeHaven-Hudkins, William G. Earley, John P. Mallamo, Matthew S. Miller
Abstract: A 5-aminoquinolone carboxylic acid derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 means a hydrogen atom, an amino group, a linear or branched alkyl group having 1-5 carbon atoms and an alkylamino group containing a linear or branched alkyl group having 1-5 carbon atoms, R.sup.2 denotes a hydrogen atom or a linear or branched alkyl group having 1-5 carbon atoms, X stands for a halogen atom, Y means CH.sub.2, NH, CHR.sup.3 NR.sup.3, (R.sup.3 denoting a linear or branched alkyl group having 1-5 carbon atoms) or an oxygen atom, and Z stands for an oxygen atom or 2 hydrogen atoms, or a salt thereof, and an antibacterial agent containing such a derivative or salt as an active ingredient.The derivative or salt thereof exhibits strong anti-bacterial activities against Grampositive bacteria including tolerant bacteria, and is satisfactorily absorbed in a living body.
Abstract: Apparatus and process for sorting used batteries and accumulators on the basis of their chemical constitution based on the analysis of the inductive effect produced by the substances which are contained in the battery or accumulator, and whose ferromagnetic properties differ according to their chemical constitution. The measurement process in which the apparatus is used is based on the consecutive application to the excitation circuit of at least two different voltage amplitudes at the same frequency or two different frequencies at the same voltage amplitude.
Type:
Grant
Filed:
September 25, 1992
Date of Patent:
July 4, 1995
Assignees:
Titalyse SA, Detra SA
Inventors:
Mai Tu Xuan, Thinh T. Nguyen, Jean P. Wia, Michel Schwab
Abstract: Disclosed is a novel spirooxazine compound having excellent durability which changes into a colored form upon irradiation with the light containing ultraviolet rays such as of sunrays or the light from a mercury lamp, the change being reversible.
Abstract: Novel therapeutic agents useful as inhibitors of HLE are provided. The compounds have the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.9, m, n and p are as defined herein. Methods of using the compounds of formula (I) to inhibit serine proteases and to treat physiological conditions and disease states associated with elevated HLE levels are also provided, as are pharmaceutical compositions containing the compounds.
Type:
Grant
Filed:
January 27, 1994
Date of Patent:
June 27, 1995
Assignee:
SRI International
Inventors:
Charles K. Hiebert, Alan Laibelman, Kenneth J. Ryan
Abstract: There are disclosed compounds of the formula (I): ##STR1## in which the variables R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and X are defined in the specification. The compounds are useful as pharmaceuticals, especially as anti-inflammatory agents.
Type:
Grant
Filed:
October 15, 1993
Date of Patent:
June 27, 1995
Assignee:
Fisons plc
Inventors:
John R. Bantick, David N. Hardern, Richard A. Appleton, John Dixon, David J. Wilkinson
Abstract: The specification describes a process for producing synthetic rutile from a titaniferous ore or concentrate. The process involves three basic steps which are reduction, removal or iron by leaching or aeration and removal of other impurities by leaching in a solution of a strong mineral acid such as hydrochloric acid or sulphuric acid. The conditions of reduction are controlled to promote the formation of metallic iron, a major rutile phase and a minor impurity bearing phase. The minor impurity phase may be a metatitanate, an anosovite or a pseudobrookite. However, formation of a metatinatate is normally preferred. Suitable reductants include carbonaceous materials or hydrogen bearing gases such as natural gas or synthesis gas. The process is capable of removing more than 80% of each of the contained iron magnesium and manganese remaining as oxides after reduction. Substantial proportions of contained aluminum can also be removed.
Type:
Grant
Filed:
November 2, 1992
Date of Patent:
June 27, 1995
Assignee:
Wimmera Industrial Minerals Pty. Ltd.
Inventors:
Michael J. Hollitt, Brian A. O'Brien, Ian E. Grey
Abstract: Compounds of the formula I ##STR1## and their tautomeric form of the formula Ia ##STR2## in which the substituents R.sup.1 to R.sup.5 and V, W, Y and Z have the stated meanings, display an effect against viruses.
Type:
Grant
Filed:
September 23, 1993
Date of Patent:
June 13, 1995
Assignee:
Hoeschst Aktiengesellschaft
Inventors:
Uta-Maria Billhardt-Troughton, Manfred Rosner, Rudolf Bender, Christoph Meichsner
Abstract: A process for producing pharmacologically active 1-unsubstituted 3-aminopyrroles of the formula ##STR1## by ring transformation of a corresponding 1,2-thiazolium pyrrole in a single step, without producing harmful byproducts.
Type:
Grant
Filed:
August 11, 1993
Date of Patent:
May 9, 1995
Assignee:
Arzneimittelwerk Dresden GmbH
Inventors:
Andreas Rolfs, Jurger Liebscher, Klaus Unverferth, Gottfried Faust
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted purinyl group including pharmaceutically acceptable salts are useful as antiviral agents.
Type:
Grant
Filed:
February 22, 1994
Date of Patent:
May 9, 1995
Assignee:
Bristol-Myers Squibb Co.
Inventors:
Joseph A. Tino, Gregory S. Bisacchi, Saleem Ahmad
Abstract: The invention relates to thiadiazinecarboxamide derivatives of the general formula I ##STR1## to processes for their preparation, and to pharmaceuticals comprising them.
Type:
Grant
Filed:
September 16, 1993
Date of Patent:
May 2, 1995
Assignee:
Luitpold Pharma GmbH
Inventors:
Rupert Strasser, Peter Zeiller, Rainer J. Klauser
Abstract: A battery charging system (200) comprises a battery (206) and charger (202). Battery 206 includes a thermistor (112) for determining the temperature of battery (206) and a resistor (214), for informing charger (202) of the current capacity of battery (206). Charger (202) includes a transistor (220) for effectively switching between measuring thermistor (112) and resistor (214) at charger input terminal (240). This effectively reduces the number of battery and charger contacts required as compared to the prior art.
Abstract: Novel quinazolinone compounds of the formula: ##STR1## wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8, R and X are defined in the specification, which have angiotensin II (AII) antagonizing activity, intermediates useful in the preparation of the compounds, methods of producing and using the compounds to alleviate angiotensin induced hypertension and treat congestive heart failure in mammals.
Type:
Grant
Filed:
October 29, 1993
Date of Patent:
April 11, 1995
Assignee:
American Cyanamid Company
Inventors:
Aranapakam M. Venkatesan, Jeremy I. Levin
Abstract: Described are novel reversible photochromic spiro(indoline) naphthoxazine compounds of improved photocolorability that may be graphically represented by the formula, ##STR1## In preferred embodiments, R.sub.1 is allyl, alkoxyalkyl, and alkyl; each R.sub.2 is alkyl or alkoxy; R.sub.3 and R.sub.4 are alkyl; R.sub.5 is alkoxycarbonyl; and R.sub.6 is hydroxy, alkoxy, or carboxy, e.g., acetoxy. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the naphthoxazine compounds or combination thereof with complementary photochromic compounds, e.g., naphthopyran or benzopyran compounds, are also described.
Abstract: Novel compounds of the formula ##STR1## where the phenyl ring can also contain a nitrogen atom instead of a CH group, R.sub.1 is C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.3 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkanoyloxy, benzoyloxy, morpholinocarbonyloxy, C.sub.1 -C.sub.6 -alkyloxycarbonyloxy, C.sub.1 -C.sub.6 -alkylaminocarbonyloxy, C.sub.1 -C.sub.6 -dialkylaminocarbonyloxy or the group -Alk-A, where Alk represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -hydroxyalkyl or C.sub.3 -C.sub.6 -cycloalkyl and the symbol A represents hydrogen or other substituents.R.sub.2, R.sub.3 and R.sub.4 represent various substituents, where R.sub.1 may also be hydrogen, when R.sub.2 is the group ##STR2## and R.sub.5 represents phenyl, C.sub.1 -C.sub.4 -alkoxyphenyl or diphenylmethyl and R.sub.3 and R.sub.4 are hydrogen and their salts. The compounds provide anti-allergic, anti-asthmatic, anxiolytic and hypotensive effects.
Type:
Grant
Filed:
August 24, 1993
Date of Patent:
April 11, 1995
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Hans-Reinhold Dieter, Jurgen Engel, Karl-Heinz Klingler, Bernhard Kutscher, Stefan Szelenyi, Ute Achterath-Tuckermann, Jurgen Schmidt, Peter Metzenauer
Abstract: The invention relates to benzopyranone and benzothiopyranone compounds, compositions and methods of use which have adrenergic and serotonergic activity.
Type:
Grant
Filed:
May 26, 1992
Date of Patent:
April 4, 1995
Assignee:
Recordati S.A., Chemical and Pharmaceutical Company
Inventors:
Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa