Chalcogen Or Nitrogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/407)
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Patent number: 6020364Abstract: 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: GrantFiled: February 22, 1999Date of Patent: February 1, 2000Assignee: Warner-Lambert CompanyInventors: David Thomas Connor, Stephen Joseph Johnson, Suzanne Ross Kesten, Steven Robert Miller, Paul Charles Unangst, Lawrence David Wise
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Patent number: 6005007Abstract: 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: GrantFiled: July 18, 1997Date of Patent: December 21, 1999Inventors: Luc J. Farmer, Lin Zhi
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Patent number: 5925673Abstract: 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: GrantFiled: December 19, 1997Date of Patent: July 20, 1999Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Abdelmoula Namil, Jon C. Nixon
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Patent number: 5919814Abstract: 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: GrantFiled: April 24, 1998Date of Patent: July 6, 1999Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Isabelle Charton, Ahmed Mamai, Pierre Renard, Bruno Pfeiffer, Philippe Delagrange, Beatrice Guardiola
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Patent number: 5910508Abstract: Novel pharmaceutically/cosmetically-active polycyclic polyenic compounds have the structural formula (I): ##STR1## and are useful for modulating cellular hormone receptors.Type: GrantFiled: September 2, 1997Date of Patent: June 8, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventors: Etienne Thoreau, Braham Shroot
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Patent number: 5908939Abstract: 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: GrantFiled: October 16, 1997Date of Patent: June 1, 1999Assignee: Roche Vitamins Inc.Inventors: Marcel Baak, Werner Bonrath, Horst Pauling
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Patent number: 5908860Abstract: 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: GrantFiled: July 6, 1995Date of Patent: June 1, 1999Assignees: SmithKline Beecham plc,, SmithKline Beecham CorporationInventors: Mervyn Thompson, John Morris Evans, Neil Upton, Wai Ngor Chan, Kuok Keong Vong, Robert Nicholas Willette
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Patent number: 5889045Abstract: 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: GrantFiled: November 25, 1997Date of Patent: March 30, 1999Assignee: Adir et CompagnieInventors: Timothee Muller, Claudie Moulin, Muriel Duflos, Sylvie Robert-Piessard, Guillaume Le Baut, Alain Tonnerre, Daniel-Henri Caignard, Dominique Manechez, Pierre Renard
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Patent number: 5846956Abstract: 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: GrantFiled: July 7, 1997Date of Patent: December 8, 1998Assignee: Societe Civile BioprojetInventors: Jean-Christophe Plaquevent, Denis Danvy, Thierry Monteil
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Patent number: 5817836Abstract: 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: GrantFiled: May 12, 1997Date of Patent: October 6, 1998Assignee: AllerganInventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5814669Abstract: 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: GrantFiled: December 20, 1996Date of Patent: September 29, 1998Assignee: Bayer AktiengesellschaftInventors: Uwe Stelzer, Carl Casser, Thomas Seitz
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Patent number: 5811448Abstract: 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: GrantFiled: December 4, 1996Date of Patent: September 22, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinrich Christian Englert, Uwe Gerlach, Dieter Mania, Wolfgang Linz, Heinz Gogelein, Erik Klaus, Peter Crause
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Patent number: 5811438Abstract: 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: GrantFiled: June 4, 1997Date of Patent: September 22, 1998Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Gustav Graff, Daniel A. Gamache, Jon C. Nixon, William H. Garner
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Patent number: 5786491Abstract: 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: GrantFiled: December 6, 1996Date of Patent: July 28, 1998Assignee: Eastman Chemical CompanyInventors: Michael David Hamlin, Richard Wayne Connelly
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Patent number: 5780647Abstract: 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: GrantFiled: February 25, 1997Date of Patent: July 14, 1998Assignee: AllerganInventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
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Patent number: 5767132Abstract: 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: GrantFiled: October 16, 1995Date of Patent: June 16, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Henning Bottcher, Ralf DeVant, Hartmut Greiner, Gerd Bartoszyk, Jean-Jacques Berthelon, Marc Noblet, Jean-Jacques Zeiller, Michel Brunet
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Patent number: 5747528Abstract: 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: GrantFiled: January 24, 1997Date of Patent: May 5, 1998Assignee: Warner-Lambert CompanyInventor: Bharat Kakidas Trivedi
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Patent number: 5739374Abstract: 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: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5731324Abstract: 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: GrantFiled: January 19, 1995Date of Patent: March 24, 1998Assignee: Eli Lilly and CompanyInventors: 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
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Patent number: 5728696Abstract: 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: GrantFiled: June 5, 1995Date of Patent: March 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5719186Abstract: 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: GrantFiled: November 8, 1996Date of Patent: February 17, 1998Assignee: Glaxo Wellcome Inc.Inventors: Barrett Randoph Cooper, James Leroy Kelley, David Lee Musso, Jeffrey Leaman Selph
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Patent number: 5717106Abstract: 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: GrantFiled: September 16, 1996Date of Patent: February 10, 1998Assignee: Eastman Kodak CompanyInventors: Charles David DeBoer, Douglas Robert Robello, Lee William Tutt
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Patent number: 5703115Abstract: 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: GrantFiled: April 15, 1996Date of Patent: December 30, 1997Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Walter Jacobus Joseph Janssens
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Patent number: 5688952Abstract: 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: GrantFiled: April 15, 1996Date of Patent: November 18, 1997Assignee: Janssen Pharmaceutica, N.V.Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Walter Jacobus Joseph Janssens
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Patent number: 5684039Abstract: 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: GrantFiled: July 19, 1996Date of Patent: November 4, 1997Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5670667Abstract: 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: GrantFiled: April 10, 1996Date of Patent: September 23, 1997Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5668180Abstract: 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: GrantFiled: May 30, 1996Date of Patent: September 16, 1997Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Patrick Depreux, Veronique Leclerc, Philippe Delagrange, Pierre Renard
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Patent number: 5663194Abstract: 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: GrantFiled: July 19, 1996Date of Patent: September 2, 1997Inventor: Richard E. Mewshaw
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Patent number: 5658941Abstract: 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: GrantFiled: December 13, 1995Date of Patent: August 19, 1997Assignee: Bristol-Myers Squibb CompanyInventors: John D. Catt, Ronald J. Mattson
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Patent number: 5659051Abstract: 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: GrantFiled: July 11, 1994Date of Patent: August 19, 1997Assignee: Sumitomo Chemical Company, LimitedInventors: Takayuki Higashii, Hideki Ushio, Yukari Fujimoto, Tsutomu Matsumoto, Masayoshi Minai, Katsuichi Yasunaga, Hiroshi Sogabe, Takahiro Kotera
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Patent number: 5646308Abstract: 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: GrantFiled: July 18, 1994Date of Patent: July 8, 1997Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hiroyuki Nabata
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Patent number: 5646121Abstract: 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: GrantFiled: September 7, 1994Date of Patent: July 8, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Thomas-J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
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Patent number: 5641789Abstract: 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: GrantFiled: March 31, 1995Date of Patent: June 24, 1997Assignee: Pfizer Inc.Inventor: Anthony Marfat
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Patent number: 5633371Abstract: 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: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5633231Abstract: 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: GrantFiled: September 7, 1994Date of Patent: May 27, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Thomas J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
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Patent number: 5607966Abstract: 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: GrantFiled: December 23, 1994Date of Patent: March 4, 1997Assignee: Alcon Laboratories, Inc.Inventors: Mark R. Hellberg, Gustav Graff
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Patent number: 5569669Abstract: 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: GrantFiled: March 10, 1995Date of Patent: October 29, 1996Assignee: Adir et CompagnieInventors: G erald Guillaumet, Marie-Claude Viaud, Pierre Renard, G erard Adam, Daniel-Henri Caignard, B eatrice Guardiola-Lemaitre, Marie-Claire Rettori
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Patent number: 5556996Abstract: Compounds of the formula ##STR1## wherein all the symbols in the formula are as defined in the specification, have retinoid-like activity.Type: GrantFiled: December 29, 1994Date of Patent: September 17, 1996Assignee: AllerganInventors: Richard L. Beard, Roshantha A. Chandraratna
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Patent number: 5545660Abstract: 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: GrantFiled: October 6, 1994Date of Patent: August 13, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
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Patent number: 5538847Abstract: 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: GrantFiled: May 7, 1993Date of Patent: July 23, 1996
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Patent number: 5516917Abstract: 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: GrantFiled: June 8, 1994Date of Patent: May 14, 1996Assignee: G. D. Searle & Co.Inventors: Steven W. Djuric, Stella S. Yu
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Patent number: 5508450Abstract: 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: GrantFiled: September 30, 1994Date of Patent: April 16, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5500444Abstract: 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: GrantFiled: September 27, 1994Date of Patent: March 19, 1996Assignee: Hoechst Marion Roussel, Inc.Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
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Patent number: 5496853Abstract: 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: GrantFiled: April 26, 1995Date of Patent: March 5, 1996Assignee: Teijin LimitedInventors: Tatsuki Shiota, Takumi Takeyasu, Kenichiro Kataoka, Tsutomu Mochizuki, Hirofumi Tanabe, Mikio Ota, Masatoshi Kano, Hisao Yamaguchi
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Patent number: 5484810Abstract: 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: GrantFiled: February 28, 1995Date of Patent: January 16, 1996Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: J. Martin Grisar, Margaret A. Petty, Frank Bolkenius
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Patent number: 5482942Abstract: 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: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5480645Abstract: 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: GrantFiled: December 29, 1993Date of Patent: January 2, 1996Assignee: LifeGroup S.p.A.Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
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Patent number: 5481021Abstract: 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: GrantFiled: December 22, 1994Date of Patent: January 2, 1996Assignee: G. D. Searle & Co.Inventors: Robert B. Garland, Masateru Miyano, Jeffery A. Zablocki, Lori A. Schretzman
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5472984Abstract: 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: GrantFiled: December 29, 1993Date of Patent: December 5, 1995Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5468882Abstract: 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: GrantFiled: March 22, 1994Date of Patent: November 21, 1995Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe-Loop, Hans-Georg Heine, Bodo Junge, Thomas Glaser, Jean M. V. De Vry, Wolfgang Dompert, Henning Sommermeyer