Additional Nitrogen Containing Hetero Ring (e.g., Thiazole, Etc.) Patents (Class 544/82)
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Patent number: 5658854Abstract: Acylated aminophenylureas, preparation and use as herbicides and plant growth regulatorsThe compounds of the formula I or their salts ##STR1## in which G is a radical G1, G2 or G3 ##STR2## R.sup.1 is H or alkyl, R.sup.2 is COOH, CSOH or a derivative of the carboxyl or thiocarboxyl group, of 1 to 20 carbon atoms, or acyl of the type CO-R.degree. of 1-12 carbon atoms, or an imino, hydrazone or oxime derivative of the group CO-R.degree., and R.degree. , R.sup.3a, R.sup.4a, R.sup.3b, R.sup.4b, W, X, Y and Z are as defined in claim 1, are suitable as selective herbicides and plant growth regulators in crops.The preparation is carried out in analogy to known processes (see claim 5) by way of intermediates, some of which are new, from the group consisting of benzene-sulfonamides (II), benzenesulfonyl isocyanates (IV) and benzesulfonyl chlorides (VI) and heterocyclically substituted carbamates (III), amines (V) and/or (thio)-isocyanates (XIX).Type: GrantFiled: June 30, 1994Date of Patent: August 19, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 5641777Abstract: The invention relates to neurokinin receptor antagonist compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycleAPPLICATION: Neurokinin receptor antagonists.Type: GrantFiled: January 30, 1996Date of Patent: June 24, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5616537Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## (wherein R is a hydroxyl group, R.sup.3 or R.sup.4 is an alkoxy group, W is an oxygen atom, Yn is a hydrogen atom, Z is a methine group, and A is a 5- or 6-membered heterocyclic ring which may be substituted, and a herbicide, are presented. When used for paddy field treatment, upland soil treatment and foliage treatment, the condensed heterocyclic derivative of the present invention exhibits excellent herbicidal activities against gramineous and non-gramineous weeds without adversely affecting crop plants.Type: GrantFiled: March 1, 1994Date of Patent: April 1, 1997Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Sumio Yokota, Masafumi Matsuzawa, Nobuyuki Ohba, Toshihiro Nagata, Shigehiko Tachikawa, Takeshige Miyazawa, Katsutada Yanagisawa
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Patent number: 5612337Abstract: The present invention relates to compounds of formula (I), wherein R.sup.1 is hydrogen, halogen, C.sub.1-6 C alkyl, C.sub.1-6 alkoxy, CF.sub.3, NO.sub.2, CN, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl or C.sub.1-4 alkyl substituted by C.sub.1-4 alkoxy, where R.sup.a and R.sup.b are hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halogen, C .sub.1-6 alkyl, C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy or CF.sub.3 ; R.sup.3 is hydrogen, halogen or CF.sub.3 ; R.sup.4 is selected from the definitions of R.sup.1 ; R.sup.5 is selected from the definitions of R.sup.2 ; R.sup.6 is a 5-membered or 6-membered heterocyclic ring containing 2 or 3 nitrogen atoms optionally substituted by .dbd.O, .dbd.S or a C.sub.1-4 alkyl group, and optionally substituted by an aminoalkyl group; R.sup.9a and R.sup.9b are hydrogen or C.sub.1-4 alkyl, or R.sup.9a and R.sup.9b are joined to form a C.sub.5-7 ring; X is C.sub.Type: GrantFiled: June 13, 1996Date of Patent: March 18, 1997Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Timothy Harrison, Angus M. MacLeod, Andrew P. Owens, Eileen M. Seward, Christopher J. Swain, Martin R. Teall
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Patent number: 5556985Abstract: A novel pyrazolonoxonol compound represented by formula (A) and a silver halide photographic material comprising such a pyrazolonoxonol compound: ##STR1## wherein R.sub.1 and R.sub.2 each represents a hydrogen atom, an alkyl group or an aryl group, and the alkyl groups represented by R.sub.1 and R.sub.2 may bond each other to form a saturated 5- or 6-membered ring; R.sub.3 represents a hydrogen atom, an alkyl group, an aryl group, a heterocyclic group, a hydroxyl group, an alkoxy group, a carboxyl group, an ester group, a carbamoyl group, an amino group, an acylamino group, an ureide group, an urethane group or a cyano group; L.sub.1, L.sub.2, L.sub.3, L.sub.4 and L.sub.5 each represents a methine group, and the methine groups which are not adjacent to each other may bond each other to form a 5- or 6-membered ring; M represents a hydrogen atom or a monovalent cation; and m and n each represent an integer 0 or 1.Type: GrantFiled: January 27, 1995Date of Patent: September 17, 1996Assignee: Fuji Photo Film Co., Ltd.Inventors: Koji Wariishi, Mario Aoki
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Patent number: 5541186Abstract: A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.Type: GrantFiled: June 27, 1994Date of Patent: July 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael L offler, Marcel M uller, Werner Neidhart, Henri Ramuz
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Patent number: 5521063Abstract: The present invention describes an assay system wherein target polynucleotide molecules are captured on a support by base-specific binding to support-bound polymers, which are themselves substantially uncharged, and the target polynucleotides can be detected on the basis of their backbone charge. The assay system may also include polycationic reporter molecules which are designed to bind to the fully charged analyte backbone, but not the uncharged (or substantially uncharged) polymer backbone. In one embodiment, the reporter molecules are composed of a polycationic moiety or tail designed to bind electrostatically to a fully charged polynucleotide, under conditions where the reporter does not bind to the less charged or uncharged binding polymer carried on the diagnostic reagent.Type: GrantFiled: February 9, 1993Date of Patent: May 28, 1996Assignee: Antivirals Inc.Inventors: James E. Summerton, Dwight D. Weller
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Patent number: 5496943Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.Type: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
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Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5466800Abstract: 2,5-Disubstituted pyridines of the formula ##STR1## can be prepared by reacting enamines of the formula ##STR2## with .beta.-amino-acrylonitriles of the formula ##STR3## and treating the open-chain intermediate, which represents a R-R.sup.1 -5-amino-penta-2,4-dienonitrile, with protic acids or with ammonia.Type: GrantFiled: July 6, 1993Date of Patent: November 14, 1995Assignee: Bayer AktiengesellschaftInventor: Helmut Kraus
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Patent number: 5420099Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventor: Trevor W. Newton
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Patent number: 5420155Abstract: A class of 4-hydroxy-2(1H)-pyrrolone 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: May 10, 1993Date of Patent: May 30, 1995Assignee: Merck Sharp & Dohme Ltd.Inventors: Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer
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Patent number: 5405845Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.Type: GrantFiled: May 25, 1994Date of Patent: April 11, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: David G. Wettlaufer, Peter A. Nemoto
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Patent number: 5397781Abstract: The present invention relates to novel 5-(.omega.-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.Type: GrantFiled: February 11, 1993Date of Patent: March 14, 1995Assignee: Mochida Pharmaceutical Company, LimitedInventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
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Patent number: 5324710Abstract: Compounds of the formula I or their salts ##STR1## in which R.sup.1 to R.sup.6, W, X, a and b are as defined in claim 1 and L is a heterocyclic or isocyclic aromatic radical having 5 to 6 ring atoms, which can be condensed with an aromatic or non-aromatic 5- or 6-membered ring, where the radical can be unsubstituted or substituted, and a, b and c independently of one another are 0 or 1, are suitable as herbicides, plant growth regulators and fungicides. They can be prepared by the processes defined herein, it being possible in some cases to use novel intermediates.Type: GrantFiled: April 21, 1992Date of Patent: June 28, 1994Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
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Patent number: 5292740Abstract: The novel sulfonamides of formula I, ##STR1## in which the symbols R.sup.1 -R.sup.9, R.sup.a, R.sup.b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.Type: GrantFiled: June 9, 1992Date of Patent: March 8, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Kaspar Burri, Martine Clozel, Walter Fischli, Georges Hirth, Bernd-Michael Loffler, Werner Neidhart, Henri Ramuz
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Patent number: 5250530Abstract: Aminopyrimidine derivatives, their preparation, and agents containing them, and their use as fungicides comprising ##STR1## in which R.sup.1 is alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, substituted aminoalkyl, phenyl, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl or phenoxyphenoxyalkyl, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, or phenyl, R.sup.5 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, R.sup.7 R.sup.8 N-,alkylthioalkyl, R.sup.7 R.sup.8 N-alkyl, halogen, alkenyl, alkynyl, phenyl, phenoxy, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl, phenylmercapto, phenylalkoxy or phenylalkylthio, R5 is H, alkyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, halogen, or phenyl or R.sup.5 and R.sup.6 together form a chain, and R.sup.7 and R.sup.8 are H, alkyl, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, alkenyl, substituted formyl, phenyl or phenylalkyl, or R.sup.7 or R.sup.Type: GrantFiled: July 9, 1990Date of Patent: October 5, 1993Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Giencke, Burkhard Sachse, Heinrich Wicke
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Patent number: 5250533Abstract: Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the two radicals may, together with the nitrogen to which they are bonded, form a 5- to 7-membered, saturated or unsaturated ring which optionally contains a further hetero atom and which is optionally substituted by 1 or 2 alkyl groups; orR.sup.1 represents in each case optionally substituted aryloxy, arylthio, aralkyloxy or aralkylthio,R.sup.2 and R.sup.3 are independent of one another and are identical or different and in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio or alkoxycarbonyl,orR.sup.2 and R.sup.3 together represent anaylene chain having 3 to 6 carbon atoms which are linked via the ring positions 3 and 4 or 4 and 5,R.sup.Type: GrantFiled: March 2, 1992Date of Patent: October 5, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
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Patent number: 5245030Abstract: An IR-ray absorptive compound represented by the formula (1) or (2): ##STR1## and an optical recording medium having a substrate and an organic dye thin film, comprising the formulae (1) and/or (2).Type: GrantFiled: January 31, 1992Date of Patent: September 14, 1993Assignee: Canon Kabushiki KaishaInventors: Tetsuro Fukui, Yoshihiro Oguchi, Hiroyuki Sugata, Kyo Miura
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Patent number: 5235033Abstract: Alpha-morpholino subunits and polymer compositions composed of alpha-morpholino subunits are disclosed. These subunits can be linked together by uncharged linkages, one to three atoms in length, joining the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide. The polymers of the present invention can be used in place of standard RNA or DNA oligomers for a number of standard laboratory procedures, for example, as probes in solid-phase systems and nucleic acid hybridization analyses. Further, the polymers of the present invention have potential use as therapeutic agents in anti-sense-type technologies.Type: GrantFiled: December 20, 1989Date of Patent: August 10, 1993Assignee: Anti-Gene Development GroupInventors: James E. Summerton, Dwight D. Weller, Eugene P. Stirchak
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Patent number: 5231095Abstract: A novel compound and compositions containing S-(-)-3-morpholino-4-(3-tert-butylamino-2-hydroxypropoxy)-1,2,5 thiadiazole hemihydrate useful for administration to a patient particularly for topical administration as a pharmaceutical agent for treating known conditions and disorders treatable with timolol.Type: GrantFiled: April 19, 1991Date of Patent: July 27, 1993Assignee: Leiras OyInventor: Markku Peralampi
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Patent number: 5223505Abstract: This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.Type: GrantFiled: April 20, 1990Date of Patent: June 29, 1993Assignee: Imperial Chemical Industries PlcInventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
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Patent number: 5204236Abstract: The improved silver halide photographic material is provided which contains a compound of the general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 each represents a hydrogen atom, an alkyl group, an aryl group, an alkenyl group or a heterocyclic group; Z.sub.1 and Z.sub.2 each represents a non-metallic atomic group necessary for forming a 5- to 7-membered ring; X.sub.1 and X.sub.2 each represents an oxygen atom, a sulfur atom or .dbd.N-R.sub.3 ; R.sub.3 is a hydrogen atom, an alkyl group, an aryl group, an alkenyl group, a heterocyclic group or --OR.sub.4 ; R.sub.4 represents a hydrogen atom, an alkyl group, an aryl group, an alkenyl group or a heterocyclic group; L.sub.1 to L.sub.5 each represents a methine group; and n.sub.1 and n.sub.2 each represents an integer of 0, 1 or 2.Type: GrantFiled: February 27, 1992Date of Patent: April 20, 1993Assignee: Konica CorporationInventors: Yasuhiko Kawashima, Reiko Yamauchi
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Patent number: 5204463Abstract: Pyridazinones of the following formula (I): ##STR1## where R.sup.1 -R.sup.4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).Type: GrantFiled: September 4, 1991Date of Patent: April 20, 1993Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
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Patent number: 5204480Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen is loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.Type: GrantFiled: February 21, 1992Date of Patent: April 20, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, David M. Fink
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Patent number: 5185444Abstract: A polymer composition is disclosed composed of morpholino subunit structures linked together by uncharged, chiral linkages, one-three atoms in length. These chiral linkages join the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide.Type: GrantFiled: November 21, 1991Date of Patent: February 9, 1993Assignee: Anti-Gene Deveopment GroupInventors: James E. Summerton, Dwight D. Weller
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Patent number: 5182282Abstract: Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having anti-arhythmic activity.Type: GrantFiled: October 11, 1991Date of Patent: January 26, 1993Assignee: Roussel UclafInventors: Francois Clemence, Jacques Guillaume, Gilles Hamon
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Patent number: 5180717Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.Type: GrantFiled: May 7, 1991Date of Patent: January 19, 1993Assignee: The Upjohn CompanyInventors: Ronald B. Gammill, Frank P. Bell
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Patent number: 5162325Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.Type: GrantFiled: May 7, 1991Date of Patent: November 10, 1992Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
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Patent number: 5129943Abstract: Disclosed herein are 2- or 6-fluoromethyl-3-pyridinecarboxylate derivatives with 5-[(heterocyclic)ylidene]amino substitution useful as herbicides and herbicide intermediates.Type: GrantFiled: May 20, 1991Date of Patent: July 14, 1992Assignee: Monsanto CompanyInventors: Shridhar G. Hegde, Len F. Lee, Robert D. Bryant
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Patent number: 5130317Abstract: Pyrimidine-4,6-dicarboxylic acid diamides, processes for the use thereof, and pharmaceuticals based on these compoundsThe invention relates to pyrimidine-4,6-dicarboxylic acid diamides of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The compounds according to the invention inhibit proline hydroxylase and lysine hydroxylase and can be employed as fibrosuppressants and immunosuppressants.Type: GrantFiled: September 19, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
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Patent number: 5120843Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).Type: GrantFiled: October 23, 1989Date of Patent: June 9, 1992Assignee: UpjohnInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
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Patent number: 5100890Abstract: Arylmethylazoles of the formula I ##STR1## in which Aryl is (substituted) phenyl or naphthyl;Z is CH or N;R.sup.1 and Q are H or alkyl;R.sup.2 is H, alk(en)yl or alkynyl;R.sup.3 and R.sup.4 are H, alkyl or other hydrocarbons; orR.sup.3 and R.sup.4 together are a--(CH.sub.2).sub.2-11 chain or a bridged--(CH.sub.2).sub.4-5 chain,and their acid addition salts, stereoisomers and optically active enantiomers possess outstanding antimycotic and antidepressant activity.They are obtained, inter alia, from arylmethylazoles II ##STR2## which are reacted with a strong base and then with a carbonyl compound III O.dbd.CR.sup.3 R.sup.4 ; thereafter, the product is reacted with the protic acid or with an alkyl halide IV R.sup.2 Hal.If desired, the products are converted to the acid addition salts, or the stereoisomers or optically active enantiomes are resolved.Type: GrantFiled: September 25, 1989Date of Patent: March 31, 1992Assignee: Hoechst AktiengesellschaftInventors: Herbert Siegel, Klaus-Dieter Kampe, Hans-Georg Alpermann, Hermann J. Gerhards, Patricia Usinger, Ulrich Schacht, Margret Leven, Wolfgang Raether, Walter Dittmar, Burkhard Sachse
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Patent number: 5099019Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: August 8, 1988Date of Patent: March 24, 1992Assignee: Upjohn CompanyInventors: John M. McCall, Donald E. Ayer, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
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Patent number: 5098900Abstract: A 3(2H)pyridazinone of the formula: ##STR1## wherein R.sub.1 is C.sub.2 -C.sub.5 alkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.3 alkyl, chlorine or bromine; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; and each of Y.sub.1, Y.sub.2 and Y.sub.3 which may be the same or different, is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, halogen, --(CH.sub.2).sub.l A [wherein A is substituted amino of the formula --N(R.sub.4) (R.sub.5) (wherein each of R.sub.4 and R.sub.5 which may be the same or different, is C.sub.1 -C.sub.4 alkyl, or R.sub.4 and R.sub.5 together form C.sub.4 -C.sub.6 alkylene), morpholino, 4-R.sub.6 -piperazin-1-yl (wherein R.sub.6 is C.sub.1 -C.sub.3 alkyl) or --OR.sub.7 (wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.3 alkyl), and l is an integer of 0 to 3], --OR.sub.8 [wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.5 alkenyl, benzyl or --(CH.sub.2).sub.q --R.sub.9 [wherein R.sub.9 is CO.sub.2 R.sub.3 (wherein R.sub.3 is as defined above), --CONHR.sub.3 (wherein R.Type: GrantFiled: April 11, 1988Date of Patent: March 24, 1992Assignee: Nissan Chemical Industries Ltd.Inventors: Motoo Mutsukado, Keizo Tanikawa, Ken-ichi Shikada, Ryozo Sakoda
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Patent number: 5091405Abstract: Pyrazolines and their intermediates, including all geometric and stereoisomers of the pyrazolines and intermediates, agricultural compositions containing the pyrazolines, and methods for use as insecticides.Type: GrantFiled: May 12, 1989Date of Patent: February 25, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thomas M. Stevenson
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Patent number: 5078780Abstract: 1,5-diphenylpyrazole-3-carboxylic acid derivatives of the formula ##STR1## are capable of antagonising specifically the phytotoxic action of phenoxypropionic acid ester herbicides of the formula II ##STR2## in which G represents ##STR3## Compositions, containing those compositions, as selective herbicides and the use of those two active ingredients for controlling weeds in crops of useful plants are described, as are also novel 1,5-diphenylpyrazole-3-carboxylic acid derivatives corresponding to the formula I and the preparation thereof.Type: GrantFiled: October 16, 1987Date of Patent: January 7, 1992Assignee: Ciba-Geigy CorporationInventors: Hans Moser, Beat Bohner, Werner Fory
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Patent number: 5066651Abstract: New pyrrolidone compounds of the formula: ##STR1## in which: R is OR", SR" or N (R.sub.3 R.sub.4)R' is optionally substituted alkyl or aryl, andthe carbon in the 5-position of the pyrrolidone ring, which is substituted by CH.sub.2 R has the R or S configuration.These new compounds and their physiologically tolerable salts may be used therapeutically especially in the treatment of asthenias, ischaemic syndromes and nervous disorders associated with normal or pathological ageing.Type: GrantFiled: May 17, 1990Date of Patent: November 19, 1991Assignee: Adir et CompagnieInventors: Gilbert Regnir, Alain Dhainaut, Jean Lepagnol, Jean Lepagnol
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Patent number: 5053072Abstract: Compounds of the formula I or salts thereof ##STR1## where R.sup.1 is H or an aliphatic radical; R.sup.2 and R.sup.3 are H, alkyl or phenyl; W is O, S, NR.sup.4 or NOR.sup.4 ; X is CHR.sup.2, O or NR.sup.4 ; L is a (substituted) phenyl, naphthyl or monocyclic heteroaryl radical, A is a (substituted) pyrimidyl, triazinyl, triazolyl or bicyclic heteroaryl radical, and m and n are 0 or 1, have advantageously herbicidal or plant growth-regulating properties.Type: GrantFiled: July 31, 1989Date of Patent: October 1, 1991Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz
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Patent number: 5051504Abstract: Triphenylmethane dyes of the formula ##STR1## where each R.sup.1 is independently of the others hydrogen or substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl, or two R.sup.1 radicals together with the nitrogen atom joining them form a heterocyclic radical,R.sup.2 and R.sup.5 is independently of the others hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.3 and R.sup.4 is independently of the others hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or halogen,An.sup..crclbar. is one equivalent of an anion, andn is 1 or 2,preparable from piperazine derivatives as intermediates, are useful for coloring paper.Type: GrantFiled: May 10, 1990Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Erwin Hahn, Walter Breitschaft, Udo Mayer, Gunter-Rudolf Schroeder
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Patent number: 5041548Abstract: Triethylene diamines are prepared in a high yield with an amine compound having a specific group as the starting material by bringing the same into contact with a catalyst formed of a crystalline metal silicate of which the molar ratio (SiO.sub.2 /M.sub.2 O.sub.3) of silicon dioxide (SiO.sub.2) to the oxide of a tervalent metal (M.sub.2 O.sub.3, M being the tervalent metal) is at least 12. Particularly high efficiency can be obtained by using a crystalline metal silicate crystallized in the presence of an organic crystallizing agent.Type: GrantFiled: June 17, 1987Date of Patent: August 20, 1991Assignee: Idemitsu Kosan Company LimitedInventors: Haruhito Sato, Masanori Tsuzuki
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Patent number: 5006524Abstract: Triphenylpyrazoline compounds, including all of their geometric isomers, stereoisomers and agriculturally suitable salts; agricultural compositions containing them; and use of such compounds as insecticides.Type: GrantFiled: January 2, 1990Date of Patent: April 9, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: George P. Lahm
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Patent number: 5001137Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.Type: GrantFiled: September 14, 1989Date of Patent: March 19, 1991Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
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Patent number: 4999368Abstract: A pyrazoline having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are selected independently from a group consisting of hydrogen with the proviso that only one of R.sup.1 and R.sup.2 can be hydrogen, substituted or unsubstituted alkyl of from 1-20 carbon atoms and substituted or unsubstituted aryl of 6 to 20 carbons, or R.sup.1 and R.sup.2 can together comprise the atoms necessary to complete a heterocyclic group of 5 to 6 nuclear carbon and hetero atoms;R.sup.3 and R.sup.4 are selected independently from a group consisting of hydrogen, substituted or unsubstituted alkyl of from 1-20 carbon atoms, substituted or unsubstituted aryl of 6-20 carbon atoms, alkoxy, alkylthio, cycloalkyl or heterocyclyl of 5 to 6 nuclear carbon and hetero atoms, or R.sup.3 and R.sup.4 together are an alkylene group of 4 to 5 carbon atoms.R.sup.Type: GrantFiled: February 12, 1990Date of Patent: March 12, 1991Assignee: Eastman Kodak CompanyInventor: John J. Delany
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Patent number: 4996318Abstract: The amino-9,10-secosteroids ##STR1## of the present invention contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain and are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc.Type: GrantFiled: September 19, 1989Date of Patent: February 26, 1991Assignee: The Upjohn CompanyInventors: Martin Gall, Robert I. Higuchi
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Patent number: 4980355Abstract: Novel substituted isonicotinic acid amides of the general formula ##STR1## in which X in ortho/ortho'-position are equal and represent fluorine, chlorine, bromine or iodine;Q.sub.1 is unsubstituted pyridimin-4-yl, or pyrimidin-4-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.2 is unsubstituted pyrimidin-2-yl, or pyrimidin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.3 is unsubstituted pyrimidin-5-yl, or pyrimidin-5-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.4 is pyridin-2-yl, pyridin-3-yl or pyridin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.5 is pyridazin-3-yl or pyridazin-4-yl each of which is unsubstituted or substituted by R.sub.1, R.sub.2 and R.sub.3 ;Q.sub.6 is unsubstituted pyrazin-2-yl, or pyrazin-2-yl substituted by R.sub.1, R.sub.2 and R.sub.3 ;R.sub.1, R.sub.2, R.sub.3 are hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl having from 1 to 3 halogen atoms, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.Type: GrantFiled: March 3, 1989Date of Patent: December 25, 1990Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Alfred Meyer, Wolfgang Eckhardt, Walter Kunz
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Patent number: 4978663Abstract: There are described compounds of the formula ##STR1## where n is 1,2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR5## taken as a whole is ##STR6## R.sub.3 is hydrogen or loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.Type: GrantFiled: August 16, 1989Date of Patent: December 18, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, David M. Fink
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Patent number: 4975433Abstract: A compound of the formula: ##STR1## wherein: R and R.sub.1 may be the same or different and are selected from the group consisting of H; cycloalkyl groups having up to 10 carbon atoms; or straight or branched chain alkyl, alkenyl or alkynyl of 1 to 10 carbon atoms;R.sub.2 and R.sub.3 together with the nitrogen atom to which they are bonded form a pyrrolidine, piperidine, N-methyl piperazine, piperazine or morpholine ring;or a non-toxic pharmaceutically acceptable salt, adduct, oxide or other derivative thereof; and pharmaceutical compositions adapted for topical administration to a human or non-human animal and methods of topically administering the compositions to humans and non-human animals.Type: GrantFiled: January 31, 1989Date of Patent: December 4, 1990Assignee: University of FloridaInventor: Kenneth B. Sloan
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Patent number: 4968714Abstract: Fungicidal substituted 3-amino-2-pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 represents unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, or unsubstituted or substituted cycloalkyl or cycloalkenyl,R.sup.2 represents hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or alkinyl, unsubstituted or substituted cycloalky or cycloalkenyl, unsubstituted or substituted aryl or unsubstituted or substituted heterocyclyl, or represents one of the radicals --CX--YR.sup.3, --CXNR.sup.4 R.sup.5, ##STR2## --SO.sub.2 NR.sup.4 R.sup.5 or --SO.sub.2 R.sup.7, R.sup.3 represents unsubstituted or substituted alkyl or unsubstituted or substituted alkenyl or alkinyl,R.sup.4 and R.sup.Type: GrantFiled: February 16, 1990Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Gerd Hanssler
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Patent number: RE35053Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.Type: GrantFiled: October 9, 1992Date of Patent: October 10, 1995Assignee: The Upjohn CompanyInventors: John M. McCall, E. Jon Jacobsen