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:
September 23, 1997
Assignee:
Eli Lilly and Company
Inventors:
Anita Melikian-Badalian, Paul L. Ornstein
Abstract: This invention relates to hexa- and octaahydrobenzo?f!quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
Type:
Grant
Filed:
April 17, 1996
Date of Patent:
September 23, 1997
Assignee:
Eli Lilly and Company
Inventors:
James E. Audia, Kenneth S. Hirsch, Charles D. Jones, David E. Lawhorn, Loretta A. McQuaid, Leland O. Weigel
Abstract: Compounds having the formula ##STR1## wherein W and Y are independently selected from optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, and optionally substituted naphthyl with the proviso that W and Y are not simultaneously the same substituent; R.sup.1 and R.sup.2 are independently hydrogen, alkyl, haloalkyl, alkoxy, or halogen; R.sup.3 is hydrogen or alkyl; X is absent or is alkylene, alkenylene, or alkynylene; and M is selected from (a) a pharmaceutically acceptable metabolically cleavable group, (b) --OR.sup.4 wherein R.sup.4 is hydrogen or alkyl; and (c) --NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from hydrogen, alkyl, hydroxy and alkoxy are disclosed. These compounds inhibit leukotriene biosynthesis and are useful in the treatment of allergic and inflammatory disease states.
Type:
Grant
Filed:
July 26, 1996
Date of Patent:
September 16, 1997
Assignee:
Abbott Laboratories
Inventors:
Clint D.W. Brooks, Teodozyj Kolasa, David E. Gunn
Abstract: Disclosed is a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: AR.sup.1 represents ##STR2## AR.sup.2 represents ##STR3## or a five-membered heterocyclic aromatic group selected from the group consisting of Formulas I to XII, wherein the substitutable carbon atoms of the five-membered heterocyclic group can optionally be substituted with a group R.sup.1.Also disclosed are pharmaceutical compositions containing compounds of Formula 1.0.Further disclosed is a method for treating asthma, allergy and inflammation by administering an anti-asthmatic, anti-allergic or anti-inflammatory, respectively, effective amount of a compound of Formula 1.0.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
September 9, 1997
Assignee:
Schering Corporation
Inventors:
Richard Friary, John J. Piwinski, Jesse K. Wong
Abstract: The invention concerns compounds of formula: ##STR1## in which Am.sup.+ represents a substituted 1-pyridylium radical, a substituted 3-thiazolylium radical, a substituted 1-pyridazinylium radical or a substituted 3-imidazolylium radical, and their salts with mineral or organic acids, whether in their optically pure or racemic form. The invention also concerns a process for the preparation of these compounds and pharmaceutical compositions containing them. Activity: antagonists of neurokinin receptors.
Type:
Grant
Filed:
November 24, 1995
Date of Patent:
September 9, 1997
Assignee:
Sanofi
Inventors:
Nathalie Chabert, Xavier Emonds-Alt, Vincenzo Proietto, Didier Van Broeck
Abstract: Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R.sup.1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
Type:
Grant
Filed:
May 31, 1994
Date of Patent:
August 12, 1997
Assignee:
Pfizer Inc.
Inventors:
George Chang, Ernest S. Hamanaka, Peter A. McCarthy, Thien V. Truong, Frederick J. Walker
Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and --N(R.sup.7)--CH(R.sup.8)(R.sup.9) are as claimed herein or their pharmaceutically acceptable acid addition salts inhibit proteases of viral origin and can be used as medicaments for the treatment of viral infections. They can be manufactured according to generally known procedures.
Type:
Grant
Filed:
April 6, 1995
Date of Patent:
July 29, 1997
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Balraj Krishan Handa, Peter James Machin, Joseph Armstrong Martin, Sally Redshaw, Gareth John Thomas
Abstract: The subject invention provides for novel compounds for inactivating viruses. These compounds include 6-nitroso-1,2-benzopyrone, 3-nitrosobenzamide, 5-nitroso-1(2H)-isoquinolinone, 7-nitroso-1(2H)-isoquinolinone, 8-nitroso-1(2H)-isoquinolinone. The invention also provides for compositions containing one or more of the compounds, and for methods of treating viral infections, cancer, infectious virus concentration with the subject compounds and compositions.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
July 29, 1997
Assignee:
Octamer, Inc.
Inventors:
Ernest Kun, Jerome Mendeleyev, William C. Rice
Abstract: Disclosed herein are substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes or pharmaceutically acceptable salts thereof that have high binding to the glycine receptor and are usefully administered to animals for the treatment or prevention of the adverse consequences of the hyperactivity of the excitatory amino acids, or neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, for the treatment of anxiety, chronic pain, convulsions, and neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome; and for the inducement of anesthesia.
Type:
Grant
Filed:
September 29, 1995
Date of Patent:
July 29, 1997
Assignees:
The Regents of the University of California, State of Oregon, acting by and through the Oregon State Board of Higer Education, acting for and on behalf of the Oregon Health Sciences University, University of Oregon
Inventors:
Sui Xiong Cai, John F. W. Keana, Eckard Weber
Abstract: Unsubstituted or substituted halo nitro and nitroso compounds and their metabolites are potent, selective and non-toxic inhibitors and supressants of cancer growth and vital infections in a mammalian host. The compounds are particularly useful for treatment and supression of tumors and viruses associated with breast cancer, AIDS, herpetic episodes and cytomegaloviral infections. The methods of treatment of tumorigenic and vital diseases by halo nitro and nitroso compounds and their metabolites are described.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
July 29, 1997
Inventors:
Ernest Kun, Jerome Mendeleyev, Eva Kirsten
Abstract: 2,3-Difluoro-5-halopyridines of the formula I ##STR1## wherein X is Cl or Br are prepared by a process which comprises reacting a starting 2,3,5-trihalopyridine of the formula II ##STR2## wherein each X is individually Br or Cl and Y is F, Cl or Br with an effective amount of potassium fluoride in the presence of a mixture of sulfolane and a tetralkylurea and/or a dialkyl-alkyleneurea as diluent, at an effective temperature up to the boiling point of the diluent, optionally in the presence of a phase-transfer catalyst such as a crown ether or polyglycol ether. The compounds are useful as intermediates to prepare herbicides.
Abstract: Novel fibrinogen receptor antagonists of the formula:X--Y--Z--Aryl--A--Bare provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
July 15, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Melissa S. Egbertson, Laura M. Vassallo, George D. Hartman, Wasyl Halczenko, David B. Whitman, James J. Perkins, Amy E. Krause, Nathan Ihle, David Alan Claremon, William Hoffman, Mark E. Duggan
Abstract: The present invention relates to a process for the preparation of 5-substituted 2-chloropyridines of the formula (I) ##STR1## by reaction of acetenamides of the formula (II) ##STR2## with Vilsmeier reagent, which is prepared by reaction of dialkylformamides of the formula (III) ##STR3## with a chlorinating agent, the excess of which is removed from the reaction mixture by distillation or by addition of dialkylformamide after completion of the reaction of the Vilsmeier reagent with the acetenamide of the formula (II), wherein in the formulae (I)-(III):R represents optionally substituted alkyl or aralkyl,R.sup.1 represents C.sub.1 -C.sub.4 -alkyl or aryl-C.sub.1 -C.sub.4 -alkyl,R.sup.2 and R.sup.3 represent straight-chain, branched or cyclic C.sub.4 -C.sub.8 -alkyl.
Type:
Grant
Filed:
January 11, 1996
Date of Patent:
July 15, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Klaus Jelich, Hans Lindel, Christoph Mannheims, Reinhard Lantzsch, Walter Merz
Abstract: Process for the preparation of antibacterial compounds of the formula ##STR1## comprises condensing an oxo compound of the formula ##STR2## with an amino compound of the formula ##STR3## to produce a compound of the formula ##STR4## reacting the compound of the formula (III) with a compound of the formula ##STR5## to give a compound of the formula ##STR6## and then eliminating the amino-protective group ##STR7##
Type:
Grant
Filed:
June 19, 1991
Date of Patent:
July 15, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Uwe Petersen, Andreas Krebs, Thomas Schenke, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl Georg Metzger, Rainer Endermann, Hans-Joachim Zeiler
Abstract: The invention relates to antimicrobial 5-(N-heterosubstituted amino) quinolone compounds having a structure according to Formula (I) or (II): ##STR1## wherein (1) R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and(2)(a) R.sup.4 and R.sup.5 are, independently, hydrogen; lower alkyl; cycloalkyl; heteroalkyl; or --C(.dbd.O)--X--R.sup.8, where X is a covalent bond, N, O, or S, and R.sup.8 is lower alkyl, lower alkenyl, arylalkyl, a carbocylic ring, or a heterocyclic ring; or(b) R.sup.4 and R.sup.5 together comprise a heterocyclic ring that includes the nitrogen to which they are bonded;and the pharmaceutically-acceptable salts, biohydrolyzable esters, biohydrolyzable amides, and solvates thereof.
Type:
Grant
Filed:
April 28, 1994
Date of Patent:
July 8, 1997
Assignee:
The Procter & Gamble Company
Inventors:
Thomas Prosser Demuth, Jr., Ronald Eugene White
Abstract: Compound of general formula I ##STR1## wherein A is a benzo or thieno group;R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
July 1, 1997
Assignee:
Boehringer Ingelheim KG
Inventors:
Dietrich Arndts, Walter Losel, Otto Roos
Abstract: The present invention provides a novel quinoline derivative useful as an anti-inflammatory agent, particularly an agent for treating arthritis, or a salt thereof. The present invention also provides a composition, particularly an anti-inflammatory composition for pharmaceutical use, comprising the novel quinoline compound of formula (I): ##STR1## wherein G is an acyl group, optionally protected hydroxyalkyl group, amidated carboxyl group or halogen atom;X is an oxygen atom, optionally oxidized sulfur atom or --(CH.sub.2).sub.q -- in which q is an integer of 0 to 5;R is an optionally substituted amino group or optionally substituted heterocyclic group;each of the ring A and ring B may optionally be substituted; andk is 0 or 1.
Type:
Grant
Filed:
June 2, 1995
Date of Patent:
June 24, 1997
Assignee:
Takeda Chemical Industries, Ltd.
Inventors:
Takashi Sohda, Haruhiko Makino, Atsuo Baba
Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts and prodrugs thereof, wherein X.sup.1, Ar, X, Y.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.5 and n are defined below, which are inhibitors of the production of leukotrienes and/or blockers of leukotriene receptors, methods for preparing said compounds and intermediates useful in the preparation thereof, pharmaceutical compositions thereof methods of treatment therewith. The compounds of the above formula are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related diseases in mammals.
Abstract: The present invention relates to a one-pot process for the preparation of 7-heterocyclyl-substituted 3-quinolonecarboxylic acid derivatives. They possess a strong anti-microbial effect. They include active compounds such as, for example, ofloxacin, ciprofloxacin or enrofloxacin.
Type:
Grant
Filed:
December 2, 1994
Date of Patent:
June 17, 1997
Assignee:
Bayer Aktiengesellschaft
Inventors:
Rudolf Zerbes, Paul Naab, Gerhard Franckowiak, Herbert Diehl