Additional Nitrogen Containing Hetero Ring (e.g., Thiazole, Etc.) Patents (Class 544/82)
  • Patent number: 5658854
    Abstract: 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: Grant
    Filed: June 30, 1994
    Date of Patent: August 19, 1997
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 5641777
    Abstract: 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: Grant
    Filed: January 30, 1996
    Date of Patent: June 24, 1997
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5616537
    Abstract: 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: Grant
    Filed: March 1, 1994
    Date of Patent: April 1, 1997
    Assignees: 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
  • Patent number: 5612337
    Abstract: 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: Grant
    Filed: June 13, 1996
    Date of Patent: March 18, 1997
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Timothy Harrison, Angus M. MacLeod, Andrew P. Owens, Eileen M. Seward, Christopher J. Swain, Martin R. Teall
  • Patent number: 5556985
    Abstract: 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: Grant
    Filed: January 27, 1995
    Date of Patent: September 17, 1996
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Koji Wariishi, Mario Aoki
  • Patent number: 5541186
    Abstract: 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: Grant
    Filed: June 27, 1994
    Date of Patent: July 30, 1996
    Assignee: 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
  • Patent number: 5521063
    Abstract: 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: Grant
    Filed: February 9, 1993
    Date of Patent: May 28, 1996
    Assignee: Antivirals Inc.
    Inventors: James E. Summerton, Dwight D. Weller
  • Patent number: 5496943
    Abstract: 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: Grant
    Filed: March 13, 1992
    Date of Patent: March 5, 1996
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
  • Patent number: 5470975
    Abstract: 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: Grant
    Filed: January 11, 1994
    Date of Patent: November 28, 1995
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 5466800
    Abstract: 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: Grant
    Filed: July 6, 1993
    Date of Patent: November 14, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventor: Helmut Kraus
  • Patent number: 5420099
    Abstract: 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: Grant
    Filed: December 21, 1992
    Date of Patent: May 30, 1995
    Assignee: Shell Research Limited
    Inventor: Trevor W. Newton
  • Patent number: 5420155
    Abstract: 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: Grant
    Filed: May 10, 1993
    Date of Patent: May 30, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Janusz J. Kulagowski, Paul D. Leeson, Ian M. Mawer
  • Patent number: 5405845
    Abstract: 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: Grant
    Filed: May 25, 1994
    Date of Patent: April 11, 1995
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: David G. Wettlaufer, Peter A. Nemoto
  • Patent number: 5397781
    Abstract: 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: Grant
    Filed: February 11, 1993
    Date of Patent: March 14, 1995
    Assignee: Mochida Pharmaceutical Company, Limited
    Inventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
  • Patent number: 5324710
    Abstract: 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: Grant
    Filed: April 21, 1992
    Date of Patent: June 28, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
  • Patent number: 5292740
    Abstract: 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: Grant
    Filed: June 9, 1992
    Date of Patent: March 8, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kaspar Burri, Martine Clozel, Walter Fischli, Georges Hirth, Bernd-Michael Loffler, Werner Neidhart, Henri Ramuz
  • Patent number: 5250530
    Abstract: 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: Grant
    Filed: July 9, 1990
    Date of Patent: October 5, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Giencke, Burkhard Sachse, Heinrich Wicke
  • Patent number: 5250533
    Abstract: 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: Grant
    Filed: March 2, 1992
    Date of Patent: October 5, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
  • Patent number: 5245030
    Abstract: 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: Grant
    Filed: January 31, 1992
    Date of Patent: September 14, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Tetsuro Fukui, Yoshihiro Oguchi, Hiroyuki Sugata, Kyo Miura
  • Patent number: 5235033
    Abstract: 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: Grant
    Filed: December 20, 1989
    Date of Patent: August 10, 1993
    Assignee: Anti-Gene Development Group
    Inventors: James E. Summerton, Dwight D. Weller, Eugene P. Stirchak
  • Patent number: 5231095
    Abstract: 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: Grant
    Filed: April 19, 1991
    Date of Patent: July 27, 1993
    Assignee: Leiras Oy
    Inventor: Markku Peralampi
  • Patent number: 5223505
    Abstract: 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: Grant
    Filed: April 20, 1990
    Date of Patent: June 29, 1993
    Assignee: Imperial Chemical Industries Plc
    Inventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
  • Patent number: 5204236
    Abstract: 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: Grant
    Filed: February 27, 1992
    Date of Patent: April 20, 1993
    Assignee: Konica Corporation
    Inventors: Yasuhiko Kawashima, Reiko Yamauchi
  • Patent number: 5204463
    Abstract: 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: Grant
    Filed: September 4, 1991
    Date of Patent: April 20, 1993
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
  • Patent number: 5204480
    Abstract: 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: Grant
    Filed: February 21, 1992
    Date of Patent: April 20, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, David M. Fink
  • Patent number: 5185444
    Abstract: 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: Grant
    Filed: November 21, 1991
    Date of Patent: February 9, 1993
    Assignee: Anti-Gene Deveopment Group
    Inventors: James E. Summerton, Dwight D. Weller
  • Patent number: 5182282
    Abstract: Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having anti-arhythmic activity.
    Type: Grant
    Filed: October 11, 1991
    Date of Patent: January 26, 1993
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Jacques Guillaume, Gilles Hamon
  • Patent number: 5180717
    Abstract: 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: Grant
    Filed: May 7, 1991
    Date of Patent: January 19, 1993
    Assignee: The Upjohn Company
    Inventors: Ronald B. Gammill, Frank P. Bell
  • Patent number: 5162325
    Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists.
    Type: Grant
    Filed: May 7, 1991
    Date of Patent: November 10, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Malcolm MacCoss, Nathan Mantlo, Thomas F. Walsh
  • Patent number: 5129943
    Abstract: Disclosed herein are 2- or 6-fluoromethyl-3-pyridinecarboxylate derivatives with 5-[(heterocyclic)ylidene]amino substitution useful as herbicides and herbicide intermediates.
    Type: Grant
    Filed: May 20, 1991
    Date of Patent: July 14, 1992
    Assignee: Monsanto Company
    Inventors: Shridhar G. Hegde, Len F. Lee, Robert D. Bryant
  • Patent number: 5130317
    Abstract: 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: Grant
    Filed: September 19, 1990
    Date of Patent: July 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ekkehard Baader, Martin Bickel, Volkmar Gunzler-Pukall, Stephan Henke
  • Patent number: 5120843
    Abstract: 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: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer
  • Patent number: 5100890
    Abstract: 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: Grant
    Filed: September 25, 1989
    Date of Patent: March 31, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Herbert Siegel, Klaus-Dieter Kampe, Hans-Georg Alpermann, Hermann J. Gerhards, Patricia Usinger, Ulrich Schacht, Margret Leven, Wolfgang Raether, Walter Dittmar, Burkhard Sachse
  • Patent number: 5099019
    Abstract: 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: Grant
    Filed: August 8, 1988
    Date of Patent: March 24, 1992
    Assignee: Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Patent number: 5098900
    Abstract: 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: Grant
    Filed: April 11, 1988
    Date of Patent: March 24, 1992
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Motoo Mutsukado, Keizo Tanikawa, Ken-ichi Shikada, Ryozo Sakoda
  • Patent number: 5091405
    Abstract: 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: Grant
    Filed: May 12, 1989
    Date of Patent: February 25, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Thomas M. Stevenson
  • Patent number: 5078780
    Abstract: 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: Grant
    Filed: October 16, 1987
    Date of Patent: January 7, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Moser, Beat Bohner, Werner Fory
  • Patent number: 5066651
    Abstract: 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: Grant
    Filed: May 17, 1990
    Date of Patent: November 19, 1991
    Assignee: Adir et Compagnie
    Inventors: Gilbert Regnir, Alain Dhainaut, Jean Lepagnol, Jean Lepagnol
  • Patent number: 5053072
    Abstract: 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: Grant
    Filed: July 31, 1989
    Date of Patent: October 1, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz
  • Patent number: 5051504
    Abstract: 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: Grant
    Filed: May 10, 1990
    Date of Patent: September 24, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Erwin Hahn, Walter Breitschaft, Udo Mayer, Gunter-Rudolf Schroeder
  • Patent number: 5041548
    Abstract: 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: Grant
    Filed: June 17, 1987
    Date of Patent: August 20, 1991
    Assignee: Idemitsu Kosan Company Limited
    Inventors: Haruhito Sato, Masanori Tsuzuki
  • Patent number: 5006524
    Abstract: 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: Grant
    Filed: January 2, 1990
    Date of Patent: April 9, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: George P. Lahm
  • Patent number: 5001137
    Abstract: 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: Grant
    Filed: September 14, 1989
    Date of Patent: March 19, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
  • Patent number: 4999368
    Abstract: 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: Grant
    Filed: February 12, 1990
    Date of Patent: March 12, 1991
    Assignee: Eastman Kodak Company
    Inventor: John J. Delany
  • Patent number: 4996318
    Abstract: 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: Grant
    Filed: September 19, 1989
    Date of Patent: February 26, 1991
    Assignee: The Upjohn Company
    Inventors: Martin Gall, Robert I. Higuchi
  • Patent number: 4980355
    Abstract: 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: Grant
    Filed: March 3, 1989
    Date of Patent: December 25, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Alfred Meyer, Wolfgang Eckhardt, Walter Kunz
  • Patent number: 4978663
    Abstract: 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: Grant
    Filed: August 16, 1989
    Date of Patent: December 18, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, David M. Fink
  • Patent number: 4975433
    Abstract: 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: Grant
    Filed: January 31, 1989
    Date of Patent: December 4, 1990
    Assignee: University of Florida
    Inventor: Kenneth B. Sloan
  • Patent number: 4968714
    Abstract: 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: Grant
    Filed: February 16, 1990
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Winfried Lunkenheimer, Gerd Hanssler
  • Patent number: RE35053
    Abstract: 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: Grant
    Filed: October 9, 1992
    Date of Patent: October 10, 1995
    Assignee: The Upjohn Company
    Inventors: John M. McCall, E. Jon Jacobsen