Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/142)
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Patent number: 5529978Abstract: Certain N-acetonyl-substituted-amides of the formula: ##STR1## wherein A is a heterocycle, a phenylalkyl, a phenylalkoxy, naphthyl, cycloalkyl, alkoxyalkyl, alkyl, haloalkyl or alkenyl group; X, Y and Z are selected from the group consisting of hydrogen, halo, cyano, thiocyano, isothiocyano, methylsulfonyloxy, thio(C.sub.1 -C.sub.2)alkyl, (C.sub.1 -C.sub.2)alkoxy, carbamoyl, dithiocarbamoyl, hydroxy, azide, trifluoromethylcarboxy, (C.sub.1 -C.sub.4)alkylcarbonyloxy, phenylcarbonyloxy, phenoxy, thiophenyl, imidazolyl or triazolyl group as described herein; R.sup.1 and R.sup.2 are each independently a hydrogen atom or a (C.sub.1 -C.sub.6)alkyl group; and compositions containing these amides are fungicidally active, particularly against phytopathogenic fungi.Type: GrantFiled: May 3, 1994Date of Patent: June 25, 1996Assignee: Rohm and Haas CompanyInventor: Ashok K. Sharma
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Patent number: 5527811Abstract: Compounds represented by the formula: ##STR1## wherein the ring A and the ring B each stand for an optionally substituted benzene ring; Ar stands for an optionally substituted aryl group or an optionally substituted heterocyclic group; Q stands for an oxygen atom or a sulfur atom; R stands for a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted hydroxyl group or an optionally substituted amino group; X stands for --O-- or --NR.sup.1 -- wherein R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon group; Y stands for --O--, --NR.sup.2 -- wherein R.sup.2 stands for a hydrogen atom or an optionally substituted hydrocarbon group, or a bond; m denotes 1, 2 or 3, and n denotes 0, 1 or 2, and salts thereof which have excellent calcium- or substance P receptor-antagonistic activity, being useful for treating a cerebralvascular disorder in mammals such as cerebralischemia, cerebral edema and neuronal damage, their production and use.Type: GrantFiled: July 13, 1994Date of Patent: June 18, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Tetsuji Imamoto, Yuzo Ichimori
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Patent number: 5506240Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## The compounds and their pharmaceutically acceptable salts can be used as antihypertensives, agents for the treatment of glaucoma, or for increasing the flow of the retinal ocular fluid.Type: GrantFiled: July 27, 1993Date of Patent: April 9, 1996Assignee: Ciba-Geigy CorporationInventors: Tibur Schmidlin, Paul Zbinden, Peter Buhlmayer
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Patent number: 5491232Abstract: Sulfur compounds of the formula ##STR1## where n is 0 or 2,R.sup.1 and R.sup.2 are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, nitro, amino, hydroxysulfonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl or unsubstituted or substituted carbamoyl,A is methylene, carbonyl, sulfonyl or a radical of the formula CH.sub.2 --CO or CH.sub.2 --SO.sub.2,is a direct bond or unsubstituted or substituted C.sub.1 -C.sub.8 -alkylene andY is vinyl or a radical of the formula C.sub.2 H.sub.4 Q, where Q is hydroxyl or a group which can be removed under alkaline reaction conditions,and a process for their preparation are described.Type: GrantFiled: April 18, 1995Date of Patent: February 13, 1996Assignee: BASF AktiengesellschaftInventors: Manfred Patsch, Ernst Schefczik
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Patent number: 5491148Abstract: 5-HT.sub.3 receptor antagonist compounds of Formula I: ##STR1## in which X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino;R.sup.1 is hydrogen, lower alkyl, phenyl or halogen;R.sup.Type: GrantFiled: April 26, 1991Date of Patent: February 13, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: Jacob Berger, Robin D. Clark
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Patent number: 5488057Abstract: The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.Type: GrantFiled: August 23, 1994Date of Patent: January 30, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Antonio Longo, Maristella Colombo
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Patent number: 5470978Abstract: 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: GrantFiled: November 18, 1992Date of Patent: November 28, 1995Assignee: Eli Lilly and CompanyInventors: Anita Melikian-Badalian, Paul L. Ornstein
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Patent number: 5434162Abstract: Compounds characterized as quinolinyl- or isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension and are of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; X is selected from oxygen atom and methylene; G is a quinolinyl or isoquinolinyl group; R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; R.sub.2 is phenylmethyl; each of R.sub.3 and R.sub.5 is hydrido; R.sub.4 is--(CH.sub.2).sub.q --C--V;V is selected from hydrido and methyl; R.sub.6 is cyclohexylmethyl; R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; q is a number selected from zero through three, inclusive; and n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: September 13, 1993Date of Patent: July 18, 1995Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, Robert E. Manning
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Patent number: 5410054Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.Type: GrantFiled: July 20, 1993Date of Patent: April 25, 1995Assignee: Merck Frosst Canada, Inc.Inventors: Rick Friesen, Robert N. Young, Yves Girard, Marc Blouin, Daniel Dube
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Patent number: 5407942Abstract: Biphenylmethyl-substituted pyridones are prepared by reaction of pyridones with appropriate biphenylmethyl compounds.The biphenylmethyl-substituted pyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hypertension and atherosclerosis.Type: GrantFiled: May 5, 1993Date of Patent: April 18, 1995Assignee: Bayer AktiengesellschaftInventors: Jurgen Dressel, Peter Fey, Rudolf H. Hanko, Walter Hubsch, Thomas Kramer, Ulrich E. Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch
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Patent number: 5401751Abstract: The invention concerns a heterocycle of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents orAr is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;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;and R.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.Type: GrantFiled: May 24, 1993Date of Patent: March 28, 1995Assignees: Zeneca Limited, Zeneca PharmaInventors: Graham C. Crawley, Philip N. Edwards, Jean-Marc M. M. Girodeau
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Patent number: 5391761Abstract: Cyclic amido alcohols of formula I are useful in the treatment of neurological and psychiatric disorders.Type: GrantFiled: July 8, 1993Date of Patent: February 21, 1995Assignee: Centre d'Etudes Experimentals et Cliniques de Pharmacologie et d'Eutonologie (CEPBEPE)Inventors: Henri Laborit, Robert Zerbib, Philippe Dostert
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Patent number: 5362612Abstract: A photographic material is disclosed comprising a support, at least one silver halide emulsion layer, and optionally one or more non-photosensitive hydrophylic layer(s), characterized in that at least one of said emulsion layer(s) and/or non-photosensitive layer(s) contains a triphenylmethane dye, absorbing around 670 nm, represented by general formula (ID): ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen unsubstituted or substituted alkyl, or unsubstituted or substituted aryl, R.sup.3 represents an electron-withdrawing group, and the substance contains at least two water-solubilizing groups, and X.sup.- represents an anion, or an intramolecular anionic group.The triphenylmethane dyes can serve as filter dye, acutance dye, or anti-halation dye. The claimed photographic materials are especially suited for exposure by a laser diode emitting at 670 nm.Type: GrantFiled: February 10, 1994Date of Patent: November 8, 1994Assignee: Agfa-Gevaert, N.V.Inventors: Eric Kiekens, Paul Callant, Roland Claes
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Patent number: 5354749Abstract: Sulfonylbenzyl-substituted benzo- and pyridopyridones are prepared by reacting corresponding benzo- and pyridopyridones with sulphonylbenzyl compounds. The sulphonylbenzyl-substituted benzo- and pyridopyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hyper tension and atherosclerosis.Type: GrantFiled: May 5, 1993Date of Patent: October 11, 1994Assignee: Bayer AktiengesellschaftInventors: Jurgen Dressel, Peter Fey, Rudolf H. Hanko, Walter Hubsch, Thomas Kramer, Ulrich E. Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch
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Patent number: 5334600Abstract: The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 (sulfonyl) or CO (carbonyl); A represents .sub.0 (oxygen), S (sulfur), or a direct bond; B represents lower alkylene; or B represents lower alkenylene or lower alkynylene provided that A represents a direct bond; X represents oxygen or sulfur, R.sub.Type: GrantFiled: February 1, 1993Date of Patent: August 2, 1994Assignee: Ciba-Geigy CorporationInventors: John H. Van Duzer, Dennis M. Roland
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Patent number: 5306720Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.Type: GrantFiled: December 20, 1991Date of Patent: April 26, 1994Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5296483Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: September 27, 1991Date of Patent: March 22, 1994Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 5260316Abstract: The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl; C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 or CO; A represents O, S, or a direct bond; B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond; X represents oxygen or sulfur; R.sub.Type: GrantFiled: June 3, 1992Date of Patent: November 9, 1993Assignee: Ciba-Geigy CorporationInventors: John H. Van Duzer, Dennis M. Roland
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Patent number: 5242931Abstract: Novel Tricyclic compound represented by formula ##STR1## possess a TXA.sub.2 biosynthesis inhibiting act and/or a TXA.sub.2 receptor antagonizing activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: March 23, 1992Date of Patent: September 7, 1993Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 5242939Abstract: This invention relates to anilide derivatives of Formula I ##STR1## which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart failure, glaucoma, and hyperaldosteronism. Methods of making the compounds, novel intermediates useful in the preparation of the compounds, compositions containing the compounds and methods of using them are also covered.Type: GrantFiled: September 13, 1991Date of Patent: September 7, 1993Assignee: Warner-Lambert CompanyInventor: Ila Sircar
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Patent number: 5240941Abstract: The invention concerns a thioxo heterocycle of the formula I ##STR1## wherein Q is a 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's which bears 1 or 2 thioxo substituents and which is optionally further substituted;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 11, 1991Date of Patent: August 31, 1993Assignees: ICI Pharma, Imperial Chemical Industries PLCInventor: Pierre A. R. Bruneau
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Patent number: 5221677Abstract: The invention concerns a heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: September 21, 1990Date of Patent: June 22, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Philip N. Edwards
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Patent number: 5198462Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.degree. stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.Type: GrantFiled: October 16, 1991Date of Patent: March 30, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Hiroyuki Tawada, Hitoshi Ikeda
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Patent number: 5194446Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.Type: GrantFiled: July 24, 1991Date of Patent: March 16, 1993Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Joseph C. Nolan, William J. Welstead, Jr., David A. Walsh, Dwight A. Shamblee, Ibrahim M. Uwaydah
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Patent number: 5189044Abstract: This invention relates to isoquinoline-1,3-dione acetyl carbamates and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus complications and associated conditions.Type: GrantFiled: March 20, 1992Date of Patent: February 23, 1993Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5169948Abstract: This invention relates to a process for producing spiro-isoquinolinepyrrolidines. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.Type: GrantFiled: January 2, 1992Date of Patent: December 8, 1992Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5162340Abstract: Substituted 1-(2H)-isoquinolinones of the structural formula: ##STR1## are angiotensin II antagonists which are useful in the treatment of hypertension and congestive heart failure.Type: GrantFiled: May 10, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett, Dooseop Kim
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Patent number: 5158954Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.Type: GrantFiled: October 15, 1990Date of Patent: October 27, 1992Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
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Patent number: 5145966Abstract: Cyclic amides of the general formula I ##STR1## where A is a group of the formula ##STR2## where in each case the left-hand free bond is linked to the amide nitrogen and the right-hand free bond, depending on the group, is a single or double bond, and where R.sup.7 to R.sup.12 are hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl, and R.sup.13 is one of the radicals R.sup.7 to R.sup.12 or hydroxyl,R.sup.1 to R.sup.4 are C.sub.1 -C.sub.4 -alkyl, where R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 may in each case be linked to form a 5- or 6-membered ring,R.sup.5 is hydrogen or C.sub.1 -C.sub.3 -alkyl, andR.sup.6 is hydrogen, C.sub.1 -C.sub.4 -alkyl which may additionally be substituted by cyano, hydroxyl, amino or phenyl, or is C.sub.1 -C.sub.4 -acyl.are described and are used as stabilizers for organic materials.Type: GrantFiled: October 12, 1990Date of Patent: September 8, 1992Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Hubert Trauth
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Patent number: 5130425Abstract: This invention relates to spiro-lactams and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.Type: GrantFiled: July 12, 1991Date of Patent: July 14, 1992Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5128348Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.Type: GrantFiled: September 12, 1990Date of Patent: July 7, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Gregory S. Basarab
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Patent number: 5125954Abstract: The present invention relates to novel bicyclo ether derivatives, to compositions containing them, and to their method of use especially to control the growth of undesired vegetation in rice.Type: GrantFiled: November 2, 1990Date of Patent: June 30, 1992Assignee: E.I. Du Pont de Nemours and CompanyInventors: James E. Powell, Richard B. Phillips
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Patent number: 5122537Abstract: The invention relates to new arylvinylamide derivatives of formula ##STR1## wherein Y is a bicyclic ring system chosen from (A), (B), (C), (D), and (E); ##STR2## in which m is zero, 1 or 2; R is hydrogen, a C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl group;R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl; andn is an integer of 1 to 3; and wherein each of the substituents --CH.dbd.CHNHCOR.sub.1, OR and R.sub.2 may be independently on either of the aryl and heteroaryl moieties of the bicyclic ring system (A), (C), (D) and (E); whereas only the benzene ring may be substituted in the bicyclic ring system (B),which are useful as tyrosine kinase inhibitors.Type: GrantFiled: November 2, 1990Date of Patent: June 16, 1992Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Franco Buzzetti, Angelo Crugnola
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Patent number: 5120745Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles of the formula ##STR1## wherein the substituents are as defined herein, compositions containing those compounds and methods of use.Type: GrantFiled: September 27, 1990Date of Patent: June 9, 1992Assignee: Shell Internationale Research Maatschappij B.V.Inventors: Richard M. Jacobson, Luong T. Nguyen, Muthuvelu Thirugnanam
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Patent number: 5118684Abstract: A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: April 3, 1991Date of Patent: June 2, 1992Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5102886Abstract: This invention relates to 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones of structural formula (I) ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alkoxy containing 1 to 6 carbon atoms, trifluoromethyl, nitro, aryl or aryl(lower alkyl)oxy wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms;R.sup.3 is lower alkyl containing 1 to 6 carbon atoms, aryl, aryl(lower alkyl) or dihalogen substituted aryl (lower alkyl) wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms;R.sup.4 and R.sup.Type: GrantFiled: October 12, 1990Date of Patent: April 7, 1992Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5093496Abstract: This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneificial for the prevention or treatment of diabetes mellitus associated complications.Type: GrantFiled: April 4, 1991Date of Patent: March 3, 1992Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5082853Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: April 4, 1990Date of Patent: January 21, 1992Inventor: Nicholas S. Bodor
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Patent number: 5081126Abstract: The invention relates to dithioacetal compounds having 5-lipoxygenase-inhibiting activity, of the formula: ##STR1## wherein R.sup.1 is lower alkyl, di-(lower)alkylamino, aryl, or heterocyclic group which may have one or more substitutents selected from halogen, lower alkyl, lower alkoxy and phenyl,R.sup.2 and R.sup.3 are each lower alkyl, aryl or ar-(lower)alkyl, or R.sup.2 and R.sup.3 are together to form 1,3-dithian ring,R.sup.4 is hydrogen or lower alkoxy, andn is 0 or an integer 1 to 4 and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 15, 1990Date of Patent: January 14, 1992Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Yoshio Kawai, Hiroshi Kayakiri, Kazuyoshi Kuratani, Masashi Hashimoto
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Patent number: 5071860Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.Type: GrantFiled: March 7, 1990Date of Patent: December 10, 1991Assignee: Bayer AktiengesellschaftInventors: Bernd Alig, Wilhelm Stendel, Michael Londershausen
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Patent number: 5061714Abstract: The use of isoquinoline derivatives for the treatment of glaucoma or ocular hypertension. The isoquinoline derivatives are of formula I ##STR1## wherein R.sub.1 is a hydrogen or a C.sub.1 -C.sub.6 alkyl group and R.sub.2 is a C.sub.1 -C.sub.6 alkyl group. The stability of the isoquinoline derivatives when used in the form of a solution is improved by incorporating therein compounds having a phenolic hydroxyl group and/or glycols serving as a stabilizer.Type: GrantFiled: March 4, 1991Date of Patent: October 29, 1991Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toyohiro Tadokoro, Kiyoshi Sato, Shigeki Hatakeyama, Shigeo Kawase, Masao Ueno
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Patent number: 5053071Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.Type: GrantFiled: May 2, 1990Date of Patent: October 1, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph E. Semple
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Patent number: 5047412Abstract: The invention describes novel (2-styryl-, 2-naphthyl- and 2-phenethyl-4-o-hydroxyphenyl-1,3-dioxan-5-yl)alkenoic acids and related tetrazoles and sulphonamides, of the formula I wherein Q completes a benzene or pyridine ring, Y is vinylene, Z is carboxy, 1(H)-tetrazol-5-yl or a group of the formula --CO.NHSO.sub.2 R.sup.6, and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A.sup.1, A.sup.2, n and m have the meanings defined in the specification, and pharmaceutically acceptable salts thereof, for use in conjunction with their pharmaceutical compositions in treating certain pulmonary and/or vascular disorders. The invention also describes various processes and intermediates for the manufacture of the novel compounds.Type: GrantFiled: February 1, 1989Date of Patent: September 10, 1991Assignee: Imperial Chemical Industries PLCInventors: George R. Brown, Michael J. Smithers
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Patent number: 5045544Abstract: This invention relates to N'-alkyl-spiro-isoquinoline-pyrrolidine tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical perparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes melitus associated complications.Type: GrantFiled: May 21, 1990Date of Patent: September 3, 1991Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5043443Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.Type: GrantFiled: July 24, 1990Date of Patent: August 27, 1991Assignee: Du Pont Merck Pharmaceutical CompanyInventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
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Patent number: 5041452Abstract: Novel diamides having a nitrogen-containing heterocyclic moiety such as pyridyl are disclosed that are useful for improving feed utilization efficiency of ruminants and for improving lactation of lactating ruminants.Type: GrantFiled: September 28, 1989Date of Patent: August 20, 1991Assignee: Eastman Kodak CompanyInventor: Alan W. White
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Patent number: 5039681Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: February 14, 1990Date of Patent: August 13, 1991Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5021438Abstract: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.Type: GrantFiled: March 15, 1989Date of Patent: June 4, 1991Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber
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Patent number: 5017708Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen, hydroxy, oxo, halogen, azido, amino, C.sub.1 -C.sub.3 alkylamino, or aminomethyl, in which said amino, C.sub.1 -C.sub.3 alkylamino and aminomethyl each is optionally substituted by one or two members selected from the group consisting of C.sub.1 -C.sub.3 alkyl and amino-protecting group; n is an integer of 1 to 3; p and q each is an integer of 0 to 3 with proviso that p+q=1 to 4 or acid-addition salts thereof, being useful materials for preparing side chains of antibacterial quinolonecarboxylic acids, cephalosporines, or other antibiotics.Type: GrantFiled: September 8, 1989Date of Patent: May 21, 1991Assignee: Shionogi & Co., Ltd.Inventors: Masaru Ogata, Hiroshi Matsumoto, Sumio Shimizu, Shiro Kida