Patents Examined by Catherine S. Kilby Scalzo
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Patent number: 5426106Abstract: A class of 4-hydroxy-pyrrolo[1,2-b]pyridazin-2(1H)-one derivatives, substituted at the 3-position by an optionally substituted aryl substituent, are selective non-competitive antagonists of NMDA receptors and/or are antagonists of AMPA receptors, and are therefore of utility in the treatment of conditions, such as neurodegenerative disorders, convulsions or schizophrenia, which require the administration of an NMDA and/or AMPA receptor antagonist.Type: GrantFiled: March 16, 1993Date of Patent: June 20, 1995Assignee: Merck Sharp & Dohme LimitedInventors: Janusz J. Kulagowski, Paul D. Leeson
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Patent number: 5424330Abstract: Benzofurancarboxamides having basic substituents, of the formula I ##STR1## in which R.sup.1 and X have the meanings stated in the description, a process for the preparation thereof, and therapeutic agents containing them.Type: GrantFiled: May 24, 1994Date of Patent: June 13, 1995Assignee: BASF AktiengesellschaftInventors: Rainer Schlecker, Hans-Juergen Teschendorf, Liliane Unger
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Patent number: 5420134Abstract: Trans-hexahydrobenzo[a]phenanthridine of the formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 is hydrogen or a phenoxy protecting group, X is fluoro, chloro, bromo, iodo or a group of the formula--OR.sub.5, and R.sub.2, R.sub.3, and R.sub.4 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, fluoro, chloro, bromo, iodo, or a group --OR.sub.1 provided that at least one of R.sub.2, R.sub.3, and R.sub.4 are other than hydrogen, are novel ligands for dopamine receptors.Type: GrantFiled: September 30, 1993Date of Patent: May 30, 1995Assignees: Purdue Research Foundation, University of North Carolina at Chapel HillInventors: David E. Nichols, Richard B. Mailman
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Patent number: 5420146Abstract: This invention relates to novel 2-[4-(5-substituted-1,2,4-oxadiazol-3-ylmethoxy)benzyl]-1,2,5-oxadiazolidi ne-3,5-diones which have demonstrated antihyperglycemic activity in diabetic (ob/ob and db/db) mice, genetic animal models of non-insulin dependent diabetes mellitus (NIDDM or Type II diabetes). These compounds are represented by Formula I below: ##STR1## wherein R.sup.1 is C.sub.6 -C.sub.10 aryl, optionally substituted by one to three substituents independently selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.3 trifluoroalkyl or C.sub.1 -C.sub.3 trifluoroalkoxy; andR.sup.2 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.3 trifluoroalkyl, and C.sub.1 -C.sub.3 trifluoroalkoxy,or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 10, 1994Date of Patent: May 30, 1995Assignee: American Home Products CorporationInventors: Michael S. Malamas, Cynthia L. Palka, Iwan Gunawan
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Patent number: 5411966Abstract: Compounds of formula I and their acid addition salts ##STR1## in which R.sup.2 R.sup.6 R.sup.13 and X have the meanings defined herein are described as well as a process and intermediates for their production, and pharmaceutical agents containing these compounds.Type: GrantFiled: September 27, 1993Date of Patent: May 2, 1995Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Bernd Schroter, Thomas Brumby, Helmut Wachtel, Peter A. Loschmann
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Patent number: 5411963Abstract: Substituted quinazolines of the formula (1): ##STR1## wherein: R.sup.1 to R.sup.4 are independently H, halo, (C.sub.1 -C.sub.4) alkyl, branched (C.sub.3 -C.sub.4) alkyl, halo (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, NO.sub.2, or NH.sub.2,provided thatat least two of R.sup.1 to R.sup.4 are H;Y is H, Cl, X--W--Ar, or O--Alk;X is O, NR.sup.7, or CR.sup.8 R.sup.9 ;Z is H, Cl, OCH.sub.3, CH.sub.3, or --NR.sup.7 --W--Ar, provided that Z can be --NR.sup.7 --W--Ar only if Y is H, Cl, or NR.sup.7 --W--Ar and Z must be --NR.sup.7 --W--Ar if Y is H or Cl, which are plant fungicides, miticides, and insecticides.Type: GrantFiled: July 19, 1993Date of Patent: May 2, 1995Assignee: DowElancoInventors: Barry A. Dreikorn, Glen P. Jourdan, Robert G. Suhr
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Patent number: 5407940Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification, and medicaments.Type: GrantFiled: October 1, 1993Date of Patent: April 18, 1995Assignee: ADIR et CompagnieInventors: E. Bisagni, R. Jasztold-Howorko, G. Atassi, A. Pierre
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Patent number: 5405843Abstract: Heterocyclic compounds useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells are disclosed, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.Type: GrantFiled: September 9, 1993Date of Patent: April 11, 1995Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Nobuyuki Fukazawa, Makoto Odate, Tsuneji Suzuki, Kengo Otsuka, Takashi Tsuruo, Wakao Sato
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Patent number: 5403859Abstract: The invention concerns a heterocyclic derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (1-6C)alkenylene, (3-6C)alkynylene or cyclo-(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X--A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 7 ring atoms, wherein A.sup.2 and A.sup.3 is (1-4C)alkylene and X is oxy;or a pharmaceutically-acceptable salt thereof.These compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: April 29, 1993Date of Patent: April 4, 1995Assignees: Imperial Chemical Industries plc, ICI PharmaInventors: Philip N. Edwards, Jean-Marc M. M. Girodeau
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Patent number: 5399563Abstract: The invention relates to benzylidene-quinuclidinone derivatives of the formula I ##STR1## in which R.sup.1 is A;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are in each case independently of one another H, A, OA or OH; andA is a straight-chain or branched alkyl radical having 1 to 10 C atomsand processes for their preparation and their use in cosmetic and/or pharmaceutical preparations.Type: GrantFiled: July 1, 1993Date of Patent: March 21, 1995Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Ingeborg Stein, Roland Martin, Michael Casutt, Ulrich Heywang, Henning Bottcher, Gunther Holzemann
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Patent number: 5391558Abstract: A composition for accelerating healing of a wound is disclosed, comprising as an active ingredient a compound represented by formula (I): ##STR1## wherein R represents a hydrogen atom, a phenyl group or a phenyl group substituted with a halogen atom, a C.sub.1 -C.sub.6 alkyl group, a hydroxyl group or a C.sub.1 -C.sub.6 alkoxy group; and X represents a 1-imidazolyl group or a 1,2,4-triazol-1-yl group.Type: GrantFiled: August 25, 1993Date of Patent: February 21, 1995Assignee: Nihon Nohyaku Co., Ltd.Inventors: Akira Seo, Kunikazu Hiraga, Hiroyasu Koga, Yoshimi Niwano
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Patent number: 5387691Abstract: 2-(Benzotriazol-2-yl)-4-alkyl-6-(2-hydroxy-3-benzoyl-6-alkoxybenzyl)phenols am prepared by reacting a Mannich base of a 2-(2-hydroxy-5-alkylphenyl)-2H-benzotriazole with a 2-hydroxy-4-alkoxybenzophenone. The hybrid products exhibit outstanding efficacy in protecting organic substrates from light-induced deterioration as well as good resistance to loss by volatilization or exudation during the processing of stabilized compositions at elevated temperatures.Type: GrantFiled: March 5, 1993Date of Patent: February 7, 1995Assignee: Ciba-Geigy CorporationInventors: Robert A. Falk, John J. Luzzi, Gregory R. Coughlin
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Patent number: 5387682Abstract: Radiation-sensitive organo-halogen compounds having a photo-labile halomethyl-1,3,5-triazine moiety and at least one polymerizable moiety within one molecule. The compounds of this invention have at least one halomethyl substituent attached to a carbon atom of the triazine moiety and at least one polymerizable monomeric moiety attached to another atom of the triazine moiety. The compounds of this invention can be used to prepare polymers having 1,3,5-triazine substituents attached thereto. The compounds of this invention are good photoinitiators, and compositions containing them can be used in printing, duplicating, copying, and other imaging systems. The compounds of this invention are capable of stimulation by actinic radiation at a wavelength of about 250 to 900 nanometers to generate free radicals.Type: GrantFiled: April 19, 1993Date of Patent: February 7, 1995Assignee: Minnesota Mining and Manufacturing CompanyInventors: James A. Bonham, Mithcell A. Rossman, Richard J. Grant
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Patent number: 5385912Abstract: This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.The compounds of this invention are described by the formula ##STR1## where Ar I is phenylene or naphthylene, Ar II is phenyl or naphthyl and A is 1-azabicyclo[2.2.2]octan-3-yl.Type: GrantFiled: October 13, 1992Date of Patent: January 31, 1995Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Kent Neuenschwander, Dilip Amin, Anthony C. Scotese, Robert L. Morris
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Patent number: 5385911Abstract: Certain Castanospermine ester derivatives of the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1-14 alkanoyl, C.sub.1-14 alkenoyl, cyclohexanecarbonyl, C.sub.1-8 alkoxyacetyl, ##STR2## naphthalenecarbonyl optionally substituted by methyl or halogen; phenyl (C.sub.2-6 alkanoyl) wherein the phenyl is optionally substituted by methyl or halogen; cinnamoyl; pyridinecarbonyl optionally substituted by methyl or halogen; dihydropyridine carbonyl optionally substituted by C.sub.1 -C.sub.10 alkyl; thiophenecarbonyl optionally substituted by methyl or halogen; or furancarbonyl optionally substituted by methyl or halogen; Y is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylmercapto, cyano or dimethylamino; Y' is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or it is combined with Y to give 3,4-methylenedioxy; Y" is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen; with R, R.sub.1 and R.sub.Type: GrantFiled: April 1, 1993Date of Patent: January 31, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Sai P. Sunkara, Paul S. Liu, A. Stanley Tyms, Debra L. Taylor
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Patent number: 5382669Abstract: The invention provides a process for the preparation of ergoline derivatives of the formula I ##STR1## the process comprising reacting an ergoline amide of the formula II with an isocyanate of formula III ##STR2## in presence of a metal catalyst and of a phosphorus compound. The compounds of the formula I are useful antiprolactinic and antiparkinson agents.Type: GrantFiled: March 9, 1993Date of Patent: January 17, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Ilaria Candiani, Walter Cabri, Angelo Bedeschi, Franco Zarini
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Patent number: 5371090Abstract: The invention relates to naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by an optionally partially hydrogenated azaisoindolinyl ring, to processes for their preparation, and to antibacterial agents and feed additives containing them.Type: GrantFiled: February 18, 1994Date of Patent: December 6, 1994Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Andreas Krebs, Thomas Schenke, Klaus Grohe, Klaus-Dieter Bremm, Rainer Endermann, Karl-Georg Metzger, Hans-Joachim Zeiler
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Patent number: 5371225Abstract: The present invention relates to novel tetracyclic compounds represented by formula (I) ##STR1## (wherein each of X.sup.1 and X.sup.2 independently represents hydrogen or lower alkyl; n represents an integer of 1 to 4), or a pharmaceutically acceptable salt thereof, which are useful as immunosuppressive agents.Type: GrantFiled: December 22, 1993Date of Patent: December 6, 1994Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Fumio Suzuki, Yoshisuke Nakasato, Hiroshi Tsumuki, Kenji Ohmori, Hiroshi Nakajima, Tadafumi Tamura, Soichiro Sato
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Patent number: 5366509Abstract: A method for bleaching a cloth dyed with an indigo dye by using a processing solution containing a bleaching agent, wherein said processing solution is an aqueous solution of a dichloroisocyanuric acid salt, is disclosed. According to the invention, the degree of bleaching can be easily controlled and, after the bleaching, neither yellowing nor deterioration of fibers occurs.Type: GrantFiled: December 11, 1992Date of Patent: November 22, 1994Assignee: Nissan Chemical Industries, Ltd.Inventors: Masanori Ota, Masashi Nakamura, Takashi Kamiyama
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Patent number: 5364854Abstract: Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R.sub.3 represents ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, which are useful in the treatment of CNS disorders, gut motility disorders, emesis and migraine, as cognition activators, anti-drug addiction agents and analgesic.Type: GrantFiled: June 3, 1993Date of Patent: November 15, 1994Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Franco Heidempergher, Claudio Arrigoni, Carla Caccia