Chalcogen Or Nitrogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/407)
  • Patent number: 6020364
    Abstract: This invention relates to compounds that are antagonists of dopamine D4 receptors, and to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: February 1, 2000
    Assignee: Warner-Lambert Company
    Inventors: David Thomas Connor, Stephen Joseph Johnson, Suzanne Ross Kesten, Steven Robert Miller, Paul Charles Unangst, Lawrence David Wise
  • Patent number: 6005007
    Abstract: Dienoic retinoids having activity for retinoid X receptors or are panagonists on retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their therapeutic use.
    Type: Grant
    Filed: July 18, 1997
    Date of Patent: December 21, 1999
    Inventors: Luc J. Farmer, Lin Zhi
  • Patent number: 5925673
    Abstract: Methods for treating inflammnatory pathologies are disclosed. Particularly, the methods utilize pharmaceutical compositions containing certain compounds having an anti-inflanumatory and anti-oxidant moiety covalently linked by thiol or sulfoxide or sulfone bond. The compounds are useflil in preventing and treating inflammatory disorders through several mechanisms.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: July 20, 1999
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Abdelmoula Namil, Jon C. Nixon
  • Patent number: 5919814
    Abstract: The invention relates to compound of general formula (I): ##STR1## wherein: Z represents O or CH.sub.2n is from 0 to 4R, X and Y are as defined in the description, andA represents ##STR2## wherein R.sup.1, R.sup.2, R.sup.6, R.sup.7 and T' are as defined in the description,and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: April 24, 1998
    Date of Patent: July 6, 1999
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Isabelle Charton, Ahmed Mamai, Pierre Renard, Bruno Pfeiffer, Philippe Delagrange, Beatrice Guardiola
  • Patent number: 5910508
    Abstract: Novel pharmaceutically/cosmetically-active polycyclic polyenic compounds have the structural formula (I): ##STR1## and are useful for modulating cellular hormone receptors.
    Type: Grant
    Filed: September 2, 1997
    Date of Patent: June 8, 1999
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventors: Etienne Thoreau, Braham Shroot
  • Patent number: 5908939
    Abstract: A process for the manufacture of d,1-.alpha.-tocopherol by the catalyzed condensation of trimethylhydroquinone with isophytol comprises carrying out the condensation in the presence of bis-(trifluoromethylsulphonyl)amine ?HN(SO.sub.2 CF.sub.3).sub.2 ! or a metal salt thereof of the formula Met ?N(SO.sub.2 CF.sub.3).sub.2 !.sub.n (I), wherein Met signifies a metal atom selected from the group of lithium, boron, magnesium, aluminium, silicon, scandium, titanium, vanadium, manganese, iron, cobalt, nickel, copper, zinc, yttrium, zirconium, rhodium, palladium, silver, tin, lanthanum, cerium, neodymium, praseodymium, europium, dysprosium, ytterbium, hafnium, platinum and gold and n signifies the corresponding valency (1, 2, 3, or 4) of the metal atom Met, as the catalyst or of a combination of a metal salt of formula I and a strong Bronsted acid as the catalyst system in an organic solvent. The product of the process is the most active member of the vitamin E group.
    Type: Grant
    Filed: October 16, 1997
    Date of Patent: June 1, 1999
    Assignee: Roche Vitamins Inc.
    Inventors: Marcel Baak, Werner Bonrath, Horst Pauling
  • Patent number: 5908860
    Abstract: This invention relates to the method of treatment and/or prophylaxis of anxiety and/or disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy, using compounds of the formula (Ia): ##STR1##
    Type: Grant
    Filed: July 6, 1995
    Date of Patent: June 1, 1999
    Assignees: SmithKline Beecham plc,, SmithKline Beecham Corporation
    Inventors: Mervyn Thompson, John Morris Evans, Neil Upton, Wai Ngor Chan, Kuok Keong Vong, Robert Nicholas Willette
  • Patent number: 5889045
    Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents alkyl,R.sub.2, R.sub.4 and R.sub.5, which may be identical or different, represent hydrogen or alkyl,R.sub.3 represents any one of the groups as defined in the description,X represents carbonyl or methylene,Y represents hydrogen or alkyl or aryl,A represents single bond or alkylphenyl,R.sub.6 represents any one of the groups as defined in the description, its isomers as well as its addition salts with a pharmaceutically acceptable acid or base,and medicinal productes containing the same are useful in the treatment of diabetes and complications of diabetic disease.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: March 30, 1999
    Assignee: Adir et Compagnie
    Inventors: Timothee Muller, Claudie Moulin, Muriel Duflos, Sylvie Robert-Piessard, Guillaume Le Baut, Alain Tonnerre, Daniel-Henri Caignard, Dominique Manechez, Pierre Renard
  • Patent number: 5846956
    Abstract: Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: December 8, 1998
    Assignee: Societe Civile Bioprojet
    Inventors: Jean-Christophe Plaquevent, Denis Danvy, Thierry Monteil
  • Patent number: 5817836
    Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.
    Type: Grant
    Filed: May 12, 1997
    Date of Patent: October 6, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5814669
    Abstract: The invention relates to novel amino acid derivatives, to a process for their preparation and to their use as pesticides, in particular as fungicides, and as intermediates for preparing known substituted amino acid derivatives with fungicidal activity.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: September 29, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Stelzer, Carl Casser, Thomas Seitz
  • Patent number: 5811448
    Abstract: Substituted chromanylsulfonyl(thio)ureas, processes for their preparation, their use in pharmaceutical preparations, and pharmaceutical preparations comprising themChromanylsulfonyl(thio)ureas of the formula I ##STR1## are useful pharmaceuticals for the treatment of cardiac arrhythmias and for the prevention of sudden heart death due to arrhythmia. They can be used as antiarrhythmics and are suitable for the prevention of sudden heart death, for the treatment of cardiac insufficiency and also heart failure as a result of the effects of shock.
    Type: Grant
    Filed: December 4, 1996
    Date of Patent: September 22, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Christian Englert, Uwe Gerlach, Dieter Mania, Wolfgang Linz, Heinz Gogelein, Erik Klaus, Peter Crause
  • Patent number: 5811438
    Abstract: The compounds of the present invention are of the formula (I): A--X--(CH.sub.2).sub.n --Y--(CH.sub.3).sub.m --Z wherein: A is an non-steroidal anti-inflammatory agent (NSAIA); A--X is an ester or amide linkage derived from the carboxylic acid moiety of the NSAIA, wherein X is O or NR; R is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl; Y, if present, is O, NR, C(R).sub.2, CH(OH) or S(O).sub.n' ; n is 2 to 4 and m is 1 to 4 when Y is O, NR, or S(O).sub.n' ; n is 0 to 4 and m is 0 to 4 when Y is C(R).sub.2 or is not present; n is 1 to 4 and m is 0 to 4 when Y is CH(OH); n' is 0 to 2; and Z is (a), (b), (c), (d) or (e) wherein: R' and R.sup.3 are H, C(O)R, C(O)N(R).sub.2, PO.sub.3.sup.-, or SO.sub.3.sup.- ; R" is H or C.sub.1 -C.sub.6 alkyl; and R' and R.sup.3 together may form a ring having structure: (1) or (2); and provided that when Z is (e), X is not O. The compounds of the present invention also include pharmaceutically acceptable salts of the compounds of formula (I).
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: September 22, 1998
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Gustav Graff, Daniel A. Gamache, Jon C. Nixon, William H. Garner
  • Patent number: 5786491
    Abstract: Disclosed is a process for whereby d-alpha-tocopheryl succinate (TS) can be crystallized in a short period of time by subjecting a fluid TS at particular temperature to a particular rate of shear for a particular time in order to accomplish crystallization. Then, while maintaining the crystallized TS at a temperature less than its melting point, we withdraw the crystallized TS from the region of shear flow. In a preferred embodiment of our process, crystallization is enhanced by use of a particular elongational rate for a particular time.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: July 28, 1998
    Assignee: Eastman Chemical Company
    Inventors: Michael David Hamlin, Richard Wayne Connelly
  • Patent number: 5780647
    Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.
    Type: Grant
    Filed: February 25, 1997
    Date of Patent: July 14, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5767132
    Abstract: Amino(thio)ether derivatives of formula I ##STR1## wherein R.sup.0, R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X and Z are as defined herein, and their salts, are active on the central nervous system.
    Type: Grant
    Filed: October 16, 1995
    Date of Patent: June 16, 1998
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Henning Bottcher, Ralf DeVant, Hartmut Greiner, Gerd Bartoszyk, Jean-Jacques Berthelon, Marc Noblet, Jean-Jacques Zeiller, Michel Brunet
  • Patent number: 5747528
    Abstract: Chroman derivatives of Formula I or a pharmaceutically acceptable salt thereof are inhibitors of VCAM-1 and ICAM-1 and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection ##STR1## wherein: R=Hydrogen or phenyl;R.sub.2 =Hydrogen or lower alkyl of from 1-4 carbon atoms;X=Oxygen or Sulfur;Y=(CH.sub.2).sub.n, --NR' where R' is hydrogen, alkyl of from 1 to 12 carbon atoms or aryl of from 6 to 10 carbon atoms, or Z; and Z is an alkyl or aryl containing moiety.
    Type: Grant
    Filed: January 24, 1997
    Date of Patent: May 5, 1998
    Assignee: Warner-Lambert Company
    Inventor: Bharat Kakidas Trivedi
  • Patent number: 5739374
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5731324
    Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
    Type: Grant
    Filed: January 19, 1995
    Date of Patent: March 24, 1998
    Assignee: Eli Lilly and Company
    Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, Michael John Martinelli, John Michael Morin, Jr., Michael Paal, Gerd Ruhter, Kenneth James Ruterbories, Daniel J. Sall, Theo Schotten, Marshall A. Skelton, Wolfgang Stenzel, Robert Theodore Vasileff
  • Patent number: 5728696
    Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 17, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5719186
    Abstract: Novel carbocyclic amides together with their salts, solvates and physiologically active derivatives which have a number of uses in medicine, in particular as central muscle relaxants, and in the treatment or prophylaxis of anxiety, inflammation, arthritis and pain.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: February 17, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Barrett Randoph Cooper, James Leroy Kelley, David Lee Musso, Jeffrey Leaman Selph
  • Patent number: 5717106
    Abstract: A yellow dye having the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represents hydrogen, halogen, or an alkoxy group of from 1 to about 6 carbon atoms; andZ.sup.1 and Z.sup.2 each independently represents cyano, esterified carboxy, amide, a substituted or unsubstituted benzoxazole, or alkylsulfonyl; or may be taken together to form a pyrazolone, barbituric acid or Meldrum's acid residue.
    Type: Grant
    Filed: September 16, 1996
    Date of Patent: February 10, 1998
    Assignee: Eastman Kodak Company
    Inventors: Charles David DeBoer, Douglas Robert Robello, Lee William Tutt
  • Patent number: 5703115
    Abstract: The present invention is concerned with vasoconstricive ?benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.
    Type: Grant
    Filed: April 15, 1996
    Date of Patent: December 30, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Walter Jacobus Joseph Janssens
  • Patent number: 5688952
    Abstract: The present invention is concerned with vasoconstricive ?(benzodioxan, benzofuran or benzopyran)alkylamino!alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.
    Type: Grant
    Filed: April 15, 1996
    Date of Patent: November 18, 1997
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Walter Jacobus Joseph Janssens
  • Patent number: 5684039
    Abstract: Compounds of the formula: ##STR1## in which R is a straight or branched chain alkyl group of 1 to 6 carbon atoms, hydroxyalkyl of 1 to 6 carbon atoms or a cycloalkyl group of 3 to 8 carbon atoms; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: November 4, 1997
    Assignee: American Home Products Corporation
    Inventor: Richard E. Mewshaw
  • Patent number: 5670667
    Abstract: Compounds of the formula: ##STR1## in which Z is hydrogen or a halogen; n is one of the integers 1, 2, 3, or 4; m is one of the integers 0 or 1; R is a substituted or unsubstituted aryl group in which the substituents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups; R.sup.2 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: April 10, 1996
    Date of Patent: September 23, 1997
    Assignee: American Home Products Corporation
    Inventor: Richard E. Mewshaw
  • Patent number: 5668180
    Abstract: A compound selected from those of formula (I): ##STR1## in which A, R, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description,and a medicinal product containing the same useful for treating a disorder of the melatoninergic system.
    Type: Grant
    Filed: May 30, 1996
    Date of Patent: September 16, 1997
    Assignee: Adir Et Compagnie
    Inventors: Daniel Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard
  • Patent number: 5663194
    Abstract: Described herein are compounds of the formula: ##STR1## in which n is 1, 2 or 3; m is 0 or 1; and R is a substituted or unsubstituted phenyl group in which the substitutents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups or R is alkyl of 1 to 6 carbon atoms or hydroxyalkyl of 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are inhibitors of dopamine synthesis and release, and are useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: September 2, 1997
    Inventor: Richard E. Mewshaw
  • Patent number: 5658941
    Abstract: Certain aminomethyl-benzodioxanes and benzopyrans are useful serotonergic agents. They possess anxiolytic properties with few of the side effects often associated with dopaminergic agents.
    Type: Grant
    Filed: December 13, 1995
    Date of Patent: August 19, 1997
    Assignee: Bristol-Myers Squibb Company
    Inventors: John D. Catt, Ronald J. Mattson
  • Patent number: 5659051
    Abstract: There is disclosed a process of producing a 2-cyano-4-oxo-4H-benzopyran compound of the general formula (2): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, hydroxy, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro or a group of the RCONH wherein R is C.sub.1 -C.sub.20 alkyl, phenyl, phenyl-substituted (C.sub.1 -C.sub.20) alkyl, phenyl (C.sub.1 -C.sub.20)alkoxyphenyl or (C.sub.1 -C.sub.20) alkoxyphenyl. This production process is characterized in that a carboxamide of the general formula (1): ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, is reacted with a dehydrating agent in the presence of a pyridine compound of the general formula (4): ##STR3## wherein A.sup.1 and A.sup.2 are independently hydrogen or C.sub.1 -C.sub.5 alkyl.
    Type: Grant
    Filed: July 11, 1994
    Date of Patent: August 19, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takayuki Higashii, Hideki Ushio, Yukari Fujimoto, Tsutomu Matsumoto, Masayoshi Minai, Katsuichi Yasunaga, Hiroshi Sogabe, Takahiro Kotera
  • Patent number: 5646308
    Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents .dbd.O, .dbd.S, .dbd.N--Z, etc. (Z represents a lower alkyl group, etc.); Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 each represents a hydrogen atom, a lower alkyl group, etc, are disclosed. The benzopyran derivative exhibit K.sup.+ channel opening activities and are widely applicable as antiasthmatics, antiepileptics, and the like.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: July 8, 1997
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Hiroshi Koga, Hiroyuki Nabata
  • Patent number: 5646121
    Abstract: The present invention relates to novel pseudopeptides with antiviral activity of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to a process for their preparation, and to their use as antiviral agents, especially against cytomegaloviruses.
    Type: Grant
    Filed: September 7, 1994
    Date of Patent: July 8, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Habich, Thomas-J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
  • Patent number: 5641789
    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.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: June 24, 1997
    Assignee: Pfizer Inc.
    Inventor: Anthony Marfat
  • Patent number: 5633371
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: May 27, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
  • Patent number: 5633231
    Abstract: The present invention relates to valine-containing, substituted pseudopeptides of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation, and to their use as anti-viral agents, in particular against cytomegaloviruses.
    Type: Grant
    Filed: September 7, 1994
    Date of Patent: May 27, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Habich, Thomas J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
  • Patent number: 5607966
    Abstract: Compounds having anti-inflammatory and anti-oxidant activity are disclosed. The compounds are useful in preventing and treating inflammatory disorders through several mechanisms. Methods of treatment employing these properties of the compounds and corresponding pharmaceutical compositions are disclosed.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: March 4, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Mark R. Hellberg, Gustav Graff
  • Patent number: 5569669
    Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R.sub.1, R.sub.2, R.sub.2', R.sub.2", R.sub.2'", R.sub.3 and n are as defined in the description, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable acid or base,and medicinal product containing the same useful for treating a mammal afflicted with a disorder associated to 5-HT.sub.1A or 5-HT.sub.2C receptors.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: October 29, 1996
    Assignee: Adir et Compagnie
    Inventors: G erald Guillaumet, Marie-Claude Viaud, Pierre Renard, G erard Adam, Daniel-Henri Caignard, B eatrice Guardiola-Lemaitre, Marie-Claire Rettori
  • Patent number: 5556996
    Abstract: Compounds of the formula ##STR1## wherein all the symbols in the formula are as defined in the specification, have retinoid-like activity.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: September 17, 1996
    Assignee: Allergan
    Inventors: Richard L. Beard, Roshantha A. Chandraratna
  • Patent number: 5545660
    Abstract: This invention relates to novel hydrazide acyl hydrazinium derivatives of certain 3,4-dihydro-2H-1-benzopyrans of the formula ##STR1## the stereoisomers and mixtures thereof, their inner salts, and the pharmaceutically acceptable salts thereof whereinR is H or C.sub.1-6 alkyl,R.sub.1 is C.sub.1-6 alkyl,R.sub.2 is H or --C(O)R,R.sub.3 and R.sub.4 are independently C.sub.1-6 alkyl;R.sub.5 is C.sub.1-6 alkyl, or ##STR2## with R.sub.8 being H or halogeno, n is zero, 1, 2, or 3 andis a halide, --S(O).sub.3 R.sub.6, or nothing when the inner salt is formedR.sub.6 is H, C.sub.1-6 alkyl, phenyl or 4-methylphenyl,to the intermediates, processes and techniques for their preparation, to their ability to manifest the property of being free radical scavengers, and to their end-use application in the treatment of disease conditions capable of being ameliorated by free radical scavengers.
    Type: Grant
    Filed: October 6, 1994
    Date of Patent: August 13, 1996
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
  • Patent number: 5538847
    Abstract: Spiroadamantyl dioxetanes bearing an alkoxy substituent, and an aromatic substituent of phenyl or naphthyl on the dioxetane ring can be activated to chemiluminesce if the aromatic substituent bears a moiety designated OX, wherein the X is cleaved by an enzyme with which the dioxetane is permitted to come in contact with. The T.sub. 1/2 kinetics of the chemiluminescent reaction, as well as the signal intensity, or quantum yield of the chemiluminescent reaction, can be altered by selection of an electron-withdrawing or an electron-donating group Z, at positions on the aromatic substituent other than those adjacent the point of attachment to the dioxetane. Signal strength can further be enhanced by recognized chemiluminescent enhancers.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: July 23, 1996
  • Patent number: 5516917
    Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R.sup.1 is alkyl;R.sup.2 represents alkyl from 1 to 5 carbon atoms, aryl or aryl substituted with halogen or alkyl from 1 to 5 carbon atoms;R.sup.6 is alkyl;n is 1 to 5;p is 0 to 6;x is 0 or 2; andR.sup.4 and R.sup.5 are independently hydrogen or alkyl or together with N form a cycloalkylamine.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB.sub.4.
    Type: Grant
    Filed: June 8, 1994
    Date of Patent: May 14, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Steven W. Djuric, Stella S. Yu
  • Patent number: 5508450
    Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: April 16, 1996
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
  • Patent number: 5500444
    Abstract: This invention relates to quaternary ammonium salts of certain 2H-1-benzopyran derivatives, to the intermediates and processes useful for their preparation, to their free-radical scavenger and cellular protective properties and to their end-use application as therapeutic agents.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: March 19, 1996
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
  • Patent number: 5496853
    Abstract: Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R.sub.1, R.sub.2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: March 5, 1996
    Assignee: Teijin Limited
    Inventors: Tatsuki Shiota, Takumi Takeyasu, Kenichiro Kataoka, Tsutomu Mochizuki, Hirofumi Tanabe, Mikio Ota, Masatoshi Kano, Hisao Yamaguchi
  • Patent number: 5484810
    Abstract: This invention relates to alkylated sulfonium alkylene derivatives of certain 2H-1-benzopyrans, to the intermediates and processes useful for their preparation, to their free-radical scavenger and cardioprotective properties and to their end-use application as therapeutic agents.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: January 16, 1996
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
  • Patent number: 5482942
    Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: January 9, 1996
    Assignee: American Home Products Corporation
    Inventors: Richard M. Soll, Paul J. Dollings
  • Patent number: 5480645
    Abstract: Hydroxyamines N-acyl derivatives with benzochroman or 2,3-dihydrobenzofuran carboxy acids and relative pharmaceutical composition for the therapeutic treatment of those CNS, vascular, cardiovascular, dermatologic and ophthalmic pathologies wherein it is important to associate an inflammatory modulation effect to an antioxidant activity.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: January 2, 1996
    Assignee: LifeGroup S.p.A.
    Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
  • Patent number: 5481021
    Abstract: This invention relates to phenyl amidine derivatives having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: January 2, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki, Lori A. Schretzman
  • Patent number: 5472984
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: December 5, 1995
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5468882
    Abstract: Aminomethyl-chromans are obtained by alkylation of correspondingly substituted amines or by reductive amination of correspondingly substituted aldehydes. The aminomethyl-chromans can be used as active compounds in medicaments, in particular for the treatment of diseases of the central nervous system.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: November 21, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe-Loop, Hans-Georg Heine, Bodo Junge, Thomas Glaser, Jean M. V. De Vry, Wolfgang Dompert, Henning Sommermeyer