Chalcogen Bonded Directly To Ring Carbon Of Pyridine Or Partially Hydrogenated Pyridine Ring Patents (Class 546/261)
  • Patent number: 6133442
    Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.
    Type: Grant
    Filed: March 5, 1999
    Date of Patent: October 17, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 6117888
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:
    Type: Grant
    Filed: September 28, 1999
    Date of Patent: September 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip E. Sanderson, Kellie Cutrona
  • Patent number: 6110945
    Abstract: Aromatic amines of formula (1) are described: ##STR1## wherein Az is an optionally substituted monocyclic six-membered nitrogen-containing aromatic group;L.sup.1 is a linker atom or group;R is a carboxylic acid or a derivative thereof;and R.sup.5 is a group --L.sup.2 (CH.sub.2).sub.t R.sup.6 in which L.sup.2 is a --N(R.sup.7)CO-- or --N(R.sup.7)CS-- group.The compounds are able to inhibit the binding of .alpha..sub.4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: August 29, 2000
    Assignee: Celltech Therapeutics Limited
    Inventors: John Clifford Head, Graham John Warrellow, John Robert Porter, Sarah Catherine Archibald
  • Patent number: 6110871
    Abstract: The novel cyanopyridines of the general formula (I) ##STR1## (A, B, R.sup.1, R.sup.2, X, m and n are defined in the specification) show selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: August 29, 2000
    Assignee: American Cyanamid Company
    Inventors: Thomas Maier, Stefan Scheiblich, Helmut Siegfried Baltruschat
  • Patent number: 6024937
    Abstract: The present invention provides aromatic amine substituted metal chelating compounds, chelates and chelate-targeting moiety conjugates formed from the chelating compounds, and methods for making and using these compounds. Metals capable of being chelated by the chelating compounds include radionuclides, such as .sup.99m Tc and .sup.186188 Re.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 15, 2000
    Assignee: NeoRx Corporation
    Inventors: Sudhakar Kasina, Eric Yau, John M. Reno
  • Patent number: 6020335
    Abstract: An (N-(pyridinylmethyl)-heterocyclic)ylideneamine compound of the formula ##STR1## wherein R.sup.3, A, and B are as described below, and its pharmaceutically acceptable salts and prodrugs. Compounds of the formula I and their pharmaceutically acceptable salts and prodrugs are useful in the treatment of addictive disorders, such as the use of tobacco or other nicotine containing products, neurological and mental disorders such as senile dementia of the Alzheimer's type, Parkinson's disease, attentional hyperactivity disorder, anxiety, obesity, Tourette's Syndrome and ulcerative colitis.
    Type: Grant
    Filed: November 4, 1997
    Date of Patent: February 1, 2000
    Assignee: Pfizer Inc
    Inventors: Arthur A. Nagel, Steven W. Goldstein, Stanley Jung, Peter H. Dorff
  • Patent number: 5981437
    Abstract: The novel compounds of formula I: ##STR1## wherein A represents an optionally substituted 5- or 6-membered heteroaromatic group or an optionally substituted aryl group or a difluorobenzodioxolyl group;B represents an optionally substituted cyclic hydrocarbon or thienyl, an alkyl, alkenyl or alkynyl group or independently has one of the meanings of A;n represents an integer from 0 to 2;R represents a hydrogen atom, a halogen atom, an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkoxyalkyl, dialkoxyalkyl, alkoxyalkoxy, alkylthio, amino, alkylamino, dialkylamino or alkoxyamino group or a formamidino or cyano group;X.sub.1 and X.sub.2 independently represent an oxygen or sulphur atom, and the herbicidal use of these compounds.
    Type: Grant
    Filed: July 8, 1997
    Date of Patent: November 9, 1999
    Assignee: American Cyanamid Company
    Inventors: Thomas Maier, Stefan Scheiblich, Helmut Siegfried Baltruschat, Joseph Luke Pont
  • Patent number: 5962479
    Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5962682
    Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl; R.sup.2 signifies phenyl or substituted phenyl; R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ; R.sup.4 signifies hydrogen or lower-alkyl; R.sup.5 signifies hydrogen or a residue R.sup.7, and R.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; or R.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue; R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl; R.sup.a signifies hydrogen, lower-alkyl or hydroxy; R.sup.b signifies hydrogen or lower-alkyl; Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.
    Type: Grant
    Filed: August 18, 1997
    Date of Patent: October 5, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5952326
    Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.
    Type: Grant
    Filed: December 10, 1997
    Date of Patent: September 14, 1999
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
  • Patent number: 5919930
    Abstract: Process for cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates.In a process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates under palladium catalysis in the presence of at least one water-soluble complex ligand, the reaction medium comprises an aqueous and an organic phase and the palladium is added in the form of a palladium compound soluble in the organic phase.Polycyclic aromatic compounds can thus be prepared economically and in very good yields and simultaneously very high purity, in particular without contamination by the complexing ligands.
    Type: Grant
    Filed: July 26, 1995
    Date of Patent: July 6, 1999
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Steffen Haber, Javier Manero
  • Patent number: 5880140
    Abstract: The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 1, 1997
    Date of Patent: March 9, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Patent number: 5869025
    Abstract: A composition of matter having the formula ##STR1## wherein R.sub.1 -R.sub.14, M, l, m, and n are defined herein and which have application as MRI contrasting agents.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: February 9, 1999
    Assignees: Hoechst Celanese Corporation, Washington University
    Inventors: Wei-Jen Peng, David E. Reichert
  • Patent number: 5869026
    Abstract: Novel ligands for use in MRI contrast agents and which have the formula ##STR1## wherein R.sub.1 -R.sub.14, M", l, m, and n are defined herein.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: February 9, 1999
    Assignee: Hoechst Celanese Corp.
    Inventors: Wei-Jen Peng, David E. Reichert
  • Patent number: 5861407
    Abstract: A class of substituted 1,2,3,6-tetrahydropyridine derivatives are disclosed that are ligands for dopamine receptor subtypes within the body. These compounds are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.
    Type: Grant
    Filed: February 21, 1997
    Date of Patent: January 19, 1999
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Ian Michael Mawer, Mark Peter Ridgill
  • Patent number: 5861140
    Abstract: A composition of matter having the formula ##STR1## wherein R.sub.1 -R.sub.14, M, l, m, and n are defined herein and which have application as MRI contrasting agents.
    Type: Grant
    Filed: November 20, 1996
    Date of Patent: January 19, 1999
    Assignee: Hoechst Celanese Corp.
    Inventors: Wei-Jun Peng, Daniel A. Aguilar
  • Patent number: 5858329
    Abstract: A method of performing an NMR diagnostic procedure in a patient in need of the same comprising administering to the patient an effective amount of an NMR diagnostic medium and then exposing the patient to an NMR measurement step to which the diagnostic medium is responsive thereby imaging at least a portion of the patient's body, wherein the diagnostic medium comprises a composition of matter which contains a compound which has the structural formula: ##STR1## wherein R, R.sub.1 -R.sub.10 and M are defined herein.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: January 12, 1999
    Assignee: Hoechst Celanese Corporation
    Inventors: Wei-Jen Peng, Humberto Ramos, Jr.
  • Patent number: 5834492
    Abstract: There is provided a synthesis and description of diprotonated diacid derivatives of pyridoxal isonicotinoyl hydrazone (PIH) of formula (I), wherein q is 1 or 2, DPA is 2 mols of a monoprotic acid HX or 1 mol of a diprotic acid H.sub.2 Y wherein X is a monovalent anion and Y is a divalent anion and both HX and H.sub.2 Y are pharmaceutically acceptable acids. The unique properties of the PIH.DPA molecule make it particularly suitable and pharmaceutically acceptable for formulation as an oral dosage form by virtue of its ready solubility in water. There are further provided methods of utilizing such chemically unique and isolable crystalline compounds, such as PIH.2HCI, as a pharmaceutical chelator. There are further provided pharmaceutical formulations specifically for the reduction of iron overload, and related chelatable metals, in subjects susceptible to such overload.
    Type: Grant
    Filed: April 7, 1997
    Date of Patent: November 10, 1998
    Assignee: Jacobus Pharmaceutical Co.
    Inventors: Neil Lewis, Vithal Patel, Jacek Terpinski, Robert Bliss
  • Patent number: 5824288
    Abstract: Novel precursors of ligands or use in MRI contrast agents and which have the formula ##STR1## wherein R.sub.2-R.sub.10 are defined herein.
    Type: Grant
    Filed: August 21, 1997
    Date of Patent: October 20, 1998
    Assignee: Hoechst Celanese Corporation
    Inventors: Wei-Jen Peng, Humberto Ramos, Jr., Daniel A. Aguilar
  • Patent number: 5770729
    Abstract: The present invention provides an ozonide reducing agent for use in the ozonolysis reaction of an organic compound, the ozonide reducing agent finding wide applications, and being safe and inexpensive from a commercial viewpoint and easy to treat for disposal.The ozonide reducing agent of the invention is a compound wherein sulfur has, at both ends of its molecule, a hydrocarbon residue substituted by a polar functional group.
    Type: Grant
    Filed: January 22, 1996
    Date of Patent: June 23, 1998
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventors: Michio Sasaoka, Daisuke Suzuki, Takashi Shiroi
  • Patent number: 5770613
    Abstract: Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds that are derivatives of pyridine aldehydes, thioaldehyde, acetals, or thioacetals. Such compounds are characterized by the following structure: ##STR1## X.sub.1 is selected from the group consisting of oxygen, sulfur, sulfone, sulfinyl, and --NR-- where R is hydrogen, alkyl, aryl, and aralkyl. R.sub.1 is --Y.sub.n R.sub.6, in which n is an integer between 0 and 10 and each Y.sub.n for n greater than 0 independently is methylene, methine, or quarternary carbon. R.sub.6, for any value of n (i.e.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: June 23, 1998
    Assignee: Geron Corporation
    Inventors: Federico C. A. Gaeta, Elaine C. Stracker
  • Patent number: 5767278
    Abstract: Compounds for treating cancer and other diseases involving telomerase activity are characterized by the following structure: ##STR1## Such compounds include those for which X.sub.1 is oxygen, sulfur, sulfone, or sulfinyl, and R.sub.1 is --Y.sub.n R.sub.6, where n is an integer between 0 and 10 and each Y.sub.n independently is methylene, methine, or quaternary carbon. R.sub.6, is alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, alkylcarbonyl, arylcarbonyl, heteroalkylcarbonyl, heteroaralkylcarbonyl, aralkylcarbonyl, arninocarbonyl, alkylarninocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, carboxyl, carboxaldehyde, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, or arylsulfinyl. R.sub.6 can also be a linker selected from the group consisting of alkyl, aryl, and heterocycle. R.sub.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: June 16, 1998
    Assignee: Geron Corporation
    Inventors: Federico C.A. Gaeta, Elaine C. Stracker
  • Patent number: 5750470
    Abstract: Provided are a pyridine derivative represented by the formula (1): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently represent a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.1-4 haloalkyl group, a C.sub.1-4 alkoxy group, a cyano group, a nitro group or a halogen atom,Qa represents a phenyl, pyrazolyl or pyridyl which may be substituted, Qb represents an azole, and X represents oxygen, sulfur or N-R.sup.4,R.sup.4 represents hydrogen or an alkyl group, and an agricultural chemical containing the same, particularly a herbicide.
    Type: Grant
    Filed: February 24, 1997
    Date of Patent: May 12, 1998
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Katsushi Morimoto, Masatoshi Ohnari, Hiroyuki Furusawa, Takumi Terachi, Tsutomu Nawamaki, Kimihiro Ishikawa, Kunimitsu Nakahira, Chiaki Kawaguchi
  • Patent number: 5747505
    Abstract: The heterocyclic aryl-, alkyl- and cycloalklacetamides are prepared by reacting the appropriately substituted acetic acids with amines, if appropriate in complexed form. The heterocyclic aryl-, alkyl- and cycloalkylacetamides can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: May 5, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Martin Beuck, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
  • Patent number: 5736274
    Abstract: A polymer containing a recurring unit of a conjugated N-fluoropyridinium salt and an active material for a positive electrode, an electrolyte, a battery material for the positive electrode and a battery which use such a polymer. That polymer provides a battery material and a primary battery or a secondary battery which have high electromotive force, high energy density, high environmental acceptability, a low internal resistance in charging and discharging and strong recoverability of the electromotive force, and can be useful as a fluorinating agent.
    Type: Grant
    Filed: April 18, 1997
    Date of Patent: April 7, 1998
    Assignee: Daikin Industries, Ltd.
    Inventors: Teruo Umemoto, Kenji Adachi, Ginjiro Tomizawa, Sumi Ishihara, Masayuki Nagayoshi
  • Patent number: 5725806
    Abstract: A method of stabilizing non-halogen containing 3-isothiazolone microbicides against chemical degradation by the introduction of aromatic disulfide compounds (except 2,2'-dithiobisbenzoic acid) is disclosed.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: March 10, 1998
    Assignee: Rohm and Haas Company
    Inventor: Tirthankar Ghosh
  • Patent number: 5714611
    Abstract: N,N'-bridged bistetramethylpiperidinyl compounds of Formula I ##STR1## useful as light stabilizers and stabilizers for organic material which are prepared starting from tetramethylpiperidinyl compounds of Formula II ##STR2## by reacting a compound of Formula II with a cyclic carbonate of Formula III.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: February 3, 1998
    Assignee: BASF Aktiengesellschaft
    Inventor: Alexander Aumuller
  • Patent number: 5714503
    Abstract: Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: February 3, 1998
    Assignee: Medivir AB
    Inventors: John M. Morin, Jr., Robert J. Ternansky, Rolf Noreen, Peter Tomas Lind
  • Patent number: 5684022
    Abstract: There are disclosed novel ether compounds of the general formula: ##STR1## wherein R.sup.1 is halogen; A is a group of the general formula Q-1: --CH(R.sup.2)--(CH.sub.2).sub.m --CH (R.sup.3)--N(R.sup.4)--C(.dbd.Y)--X--R.sup.5, or the like; E is a group of the general formula: ##STR2## and l is an integer of 0 to 2; harmful-organism controlling agents containing them as active ingredients, and intermediates for use in their production.
    Type: Grant
    Filed: December 12, 1996
    Date of Patent: November 4, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Akira Shuto, Hirosi Kisida, Toru Tsuchiya, Yoji Takada, Hiroaki Fujimoto
  • Patent number: 5670645
    Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: metal ion-ligand coordination complexes ("MLC"), novel ligands, antibodies specific for MLC, immunoassays utiliizing the foregoing, and methods for selecting said antibodies.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: September 23, 1997
    Assignee: Abbott Laboratories
    Inventor: David K. Johnson
  • Patent number: 5654122
    Abstract: Pyridone dyes useful for thermal transfer have the formula ##STR1## where R.sup.1 is hydrogen or C.sub.1 -C.sub.4 - alkyl,R.sup.2 and R.sup.3 are identical or different and each is, independently of the other, hydrogen, substituted or unsubstituted C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridyl, substituted or unsubstituted C.sub.1 -C.sub.12 -alkanoyl, C.sub.1 -C.sub.12 -alkoxycarbonyl, substituted or unsubstituted C.sub.1 -C.sub.12 -alkylsulfonyl, C.sub.5 -C.sub.7 -cycloalkylsulfonyl, substituted or unsubstituted phenylsulfonyl, substituted or unsubstituted pyridylsulfonyl, substituted or unsubstituted benzoyl, pyridylcarbonyl or thienylcarbonyl or are together with the nitrogen atom to which they are bonded unsubstituted or C.sub.1 -C.sub.4 - alkyl-substituted succinimido, unsubstituted or C.sub.1 -C.sub.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 5, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl-Heinz Etzbach, Ernst Schefczik, Ruediger Sens, Matthias Wiesenfeldt
  • Patent number: 5624901
    Abstract: Disclosed is a series of improved metal chelating agents, which are highly effective upon both injection and oral administration; several of the most effective are of low toxicity. These chelating agents incorporate within their structure 1-hydroxy-2-pyridinone (1,2-HOPO) and 3-hydroxy-2-pyridinone (3,2-HOPO) moieties with a substituted carbamoyl group ortho to the hydroxy or oxo groups of the hydroxypyridinone ring. The electron-withdrawing carbamoyl group increases the acidity of the hydroxypyridinones. In the metal complexes of said chelating agents, the amide protons form very strong hydrogen bonds with its adjacent HOPO oxygen donor, making these complexes very stable at physiological conditions. The terminal N-substituents provides a certain degree of lipophilicity to said 3,2-HOPO, increasing oral activity.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: April 29, 1997
    Assignee: The Regents of the University of California
    Inventors: Kenneth N. Raymond, Jide Xu
  • Patent number: 5618775
    Abstract: Mixtures of optically active cyclohexenone oxime ethers having R- and S-configuration in the oxime ether moiety of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; ##STR2## X=C.sub.1-C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl; m=0-3 or 1-4 where all X's are halogen;n=0-3 or 1-5 where all X's are halogen;R.sup.2 =C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl, substituted or unsubstituted C.sub.5 -C.sub.7 -cycloalkenyl, substituted or unsubstituted 5-membered saturated heterocyclic structure, substituted or unsubstituted 6- or 7-membered heterocyclic structure, substituted or unsubstituted 5-membered heteroaromatic structure, substituted or unsubstituted phenyl or pyridyl)and their agriculturally useful salts and esters with C.sub.1 -C.sub.10 -carboxylic acids and inorganic acids.
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: April 8, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Wolfgang Ladner, Helmut Walter, Karl-Otto Westphalen, Uwe Kardorff, Matthias Gerber
  • Patent number: 5618826
    Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification; and acid addition and quaternary ammonium salts of formula (I) compounds are described. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: April 8, 1997
    Assignee: University of Florida
    Inventors: Richard H. Hammer, Nicholas S. Bodor
  • Patent number: 5614634
    Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 25, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5610318
    Abstract: This invention is directed to a process for preparing a compound containing a persalt activators and salts thereof which are derived from imidocarboxylic acids and sulfimidocarboxylic acids of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine, --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M, X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2,L is a leaving group.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: March 11, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Frank Jaekel, Gerd Reinhardt, Wolf-Dieter M uller
  • Patent number: 5595958
    Abstract: Herbicidal 3-substituted pyridine compounds and derivatives thereof of the formula: ##STR1## wherein Ar is a substituted or unsubstituted 5- or 6-membered heteroaryl group having 1, 2 or 3 ring nitrogen atoms with the remainder of the ring atoms being carbon; a substituted or unsubstituted 5-membered heteroaryl group having a ring heteroatom of oxygen or sulfur with the remainder of the ring atoms being carbon; or a substituted or unsubstituted 5-membered heteroaryl group having one ring nitrogen atom and either an oxygen or sulfur ring heteroatom with the remainder of the ring atoms being carbon. Herbicidal compositions containing such 3-substituted pyridine compounds and derivatives thereof and methods of controlling undesirable vegetation employing these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the disclosed 3-substituted pyridine derivatives.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: January 21, 1997
    Assignee: Zeneca Limited
    Inventors: Hsiao-Ling M. Chin, Nhan H. Nguyen, David B. Kanne, David L. Lee
  • Patent number: 5585327
    Abstract: 4-substituted pyridyl-3-carbinols of the formula ##STR1## wherein R is hydrogen, or an acyl, alkyl or carbamyl group exhibit desirable preemergent and postemergent herbicidal activity. Also disclosed are herbicidal compositions comprising such compounds and methods of controlling undesirable vegetation employing such compounds. The compounds wherein AR is hydroxyl serve as useful intermediates for the production of the alpha-benzyl substituted compounds as well as exhibiting herbicidal activity.
    Type: Grant
    Filed: May 2, 1994
    Date of Patent: December 17, 1996
    Assignee: Zeneca Limited
    Inventors: Hsiao-Ling Chin, Yi-Qiu Wei, Nhan H. Nguyen, Michael P. Ensminger, Linda Willitts, Derek P. Dagarin
  • Patent number: 5583147
    Abstract: This invention provides amide compounds as inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT), pharmaceutical compositions containing such compounds, processes for the preparation of such compounds, and the use of such compounds as antihypercholesterolemic and/or antiatherosclerotic agents.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: December 10, 1996
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventors: Soo S. Ko, Richard G. Wilde, Indawati DeLucca, Hui-Yin Li, Hollis S. Kezar, III, George A. Boswell, Anurag S. Srivastava
  • Patent number: 5580980
    Abstract: Pyridone dyes useful for thermal transfer have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, Y, X and Z are defined in the specification.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: December 3, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl-Heinz Etzbach, Ernst Schefczik, Ruediger Sens, Matthias Wiesenfeldt
  • Patent number: 5576440
    Abstract: Compounds of formula (I), where R.sup.1, R.sup.2, n, W, R.sup.3 and A are as defined in claim 1, are suitable for use as herbicides and plant growth regulators. They can be produced by a process similar to known processes. To produce them, new compounds of formula (II) are reacted with a carbamate of formula R*--O--CO--NR.sup.3 A, where R.sup.3 stands for phenyl or alkyl. The compounds of formula (II) can be obtained from the corresponding sulphochlorides.
    Type: Grant
    Filed: January 4, 1995
    Date of Patent: November 19, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz Kehne, Lothar Willms, Oswald Ort, Klaus Bauer, Hermann Bieringer
  • Patent number: 5567725
    Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.
    Type: Grant
    Filed: February 14, 1995
    Date of Patent: October 22, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Horst Hemmerle, Gerrit Schubert, Peter Below, Andreas Herling, Hans-J org Burger
  • Patent number: 5565465
    Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 15, 1996
    Assignee: Imperial Chemical Industries PLC
    Inventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
  • Patent number: 5559133
    Abstract: A compound represented by formula I, Ar.sub.1 --O--M--O--Ar.sub.2, wherein Ar.sub.1 and Ar.sub.2 are independently substituted phenyl or substituted pyridinyl, the substituents on said phenyl or pyridinyl being independently selected from one, two or three of (C.sub.1 -C.sub.10) alkyl, (C.sub.1 -C.sub.10) alkoxy, halogen, carbamyl, (C.sub.1 -C.sub.10) alkoxycarbonyl, oxazoyl, and (C.sub.1 -C.sub.10) alkyl substituted by halogen, (C.sub.1 -C.sub.10) alkoxy, hydroxy, or (C.sub.1 -C.sub.10) alkoxycarbonyl; ##STR1## O is oxygen; R' is (C.sub.1 -C.sub.3 alkyl or H; A is oxygen or sulfur; Q is selected from hydrogen, halogen, nitro, (C.sub.1 -C.sub.6) alkyl, (C.sub.1 C.sub.6) perhaloalkyl, (C.sub.1 -C.sub.6) alkylthio (C.sub.1 -C.sub.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: September 24, 1996
    Assignee: Schering Corporation
    Inventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Richard W. Versace, Anil K. Saksena, Patrick A. Pinto
  • Patent number: 5556990
    Abstract: This invention relates to a class of novel dicarboxy amide derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis-aryl and/or heteroaryl alkyl or cycloalkylamino dicarboxy amides. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: September 17, 1996
    Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.
    Inventors: Henry W. Pauls, Yong-Mi Choi, Robert W. Studt, Martin P. Maguire, Alfred P. Spada, Don D. Cha
  • Patent number: 5554737
    Abstract: Azo dyes of the formula ##STR1## where D is the radical of a diazo component, andX is substituted or unsubstituted C.sub.2 -C.sub.8 -alkylene, in the form of the free acid or its salts, the use thereof for dyeing or printing natural or synthetic substrates, sulfopyridones as coupling components for these dyes, and a process for preparing them.
    Type: Grant
    Filed: May 2, 1995
    Date of Patent: September 10, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Gunther Lamm, Helmut Reichelt, Matthias Wiesenfeldt
  • Patent number: 5550236
    Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boronic acids with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium, if desired applied to a support material, as catalyst, wherein the coupling is carried out in the presence of a ligand and a base. The process of the invention allows the yield of polycyclic aromatic compounds to be significantly increased in comparison with processes not using a ligand and thus allows a yield optimum for the Pd(0)-catalyzed cross-coupling of aromatic boronic acids with aromatic halogen compounds to be achieved.
    Type: Grant
    Filed: April 24, 1995
    Date of Patent: August 27, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hubert Schlosser, Rainer Wingen, Javier Manero
  • Patent number: 5548078
    Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: August 20, 1996
    Assignee: Shionogi Seiyaku Kabushiki Kaisha
    Inventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
  • Patent number: 5545835
    Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pylidinedicarboxylic acids.
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: August 13, 1996
    Assignee: American Cyanamid Company
    Inventor: Henry L. Strong
  • Patent number: 5530015
    Abstract: There is disclosed a dihalopropene compound of the formula I: ##STR1## wherein l is an integer of 1 to 5; m is an integer of 1 to 4; R.sup.1 's and R.sup.2 's are the same or different and are independently halogen or various other groups; D is oxygen; X's are the same or different and are independently chlorine or bromine; Y is oxygen; Z, P and Q are the same or different and are independently nitrogen or CH, provided that P and Q are not simultaneously nitrogen, and when Y is sulfur, Z is CH. Also disclosed is an insecticide/acaricide comprising the dihalopropene compound as an active ingredient. The dihalopropene compound exhibits excellent insecticidal/acaricidal action. Further disclosed is an intermediate compound for use in the production of the dihalopropene compound.
    Type: Grant
    Filed: October 19, 1994
    Date of Patent: June 25, 1996
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noriyasu Sakamoto, Masaya Suzuki, Toshio Nagatomi, Kazunori Tsushima, Kimitoshi Umeda