Plural Rings Bonded Directly To The Same Carbon Patents (Class 562/441)
  • Patent number: 7030160
    Abstract: The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: April 18, 2006
    Assignee: Sanofi-Aventis
    Inventors: Laura Barzaghi, Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Stefano Romagnano
  • Patent number: 6979566
    Abstract: A water soluble derivative of buckministerfullerene (C50) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
    Type: Grant
    Filed: February 1, 2003
    Date of Patent: December 27, 2005
    Assignee: The Regents of the University of California
    Inventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
  • Patent number: 6924391
    Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula wherein X, Z, X1, R1, R2, Ra, Rb, R3, R4 and Y are as defined in the specification.
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: August 2, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jacques Banville, Roger Remillard, Neelakantan Balasubramanian, Gilles Bouthillier, Alain Martel
  • Patent number: 6906046
    Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-? and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
    Type: Grant
    Filed: December 11, 2001
    Date of Patent: June 14, 2005
    Assignee: Celltech R & D Inc.
    Inventors: Randy W. Jackson, Ihab Darwish, Ted A. Baughman, J. Jeffry Howbert
  • Patent number: 6809214
    Abstract: The invention relates to a method for producing derivatives of 3,3-diarylpropylamines of general formula (I) and sterically highly pure, stable intermediate products, and to their use for producing pharmaceutical compositions.
    Type: Grant
    Filed: December 9, 2002
    Date of Patent: October 26, 2004
    Assignee: Schwartz Pharma AG
    Inventor: Claus O. Meese
  • Patent number: 6806365
    Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: October 19, 2004
    Assignee: Hoffmann-La Rocher Inc.
    Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achytharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
  • Patent number: 6765098
    Abstract: A novel means for DNA compaction is provided. The object is accomplished by providing a fullerene derivative having 1 to 4 nitrogen-containing hydrophilic side chain(s) or its salt for DNA compaction. DNA compaction can be achieved effectively, and application to gene therapy is also expected.
    Type: Grant
    Filed: November 17, 2000
    Date of Patent: July 20, 2004
    Assignees: Fujisawa Pharmaceutical Co., Ltd
    Inventors: Eiichi Nakamura, Masaya Sawamura, Hiroyuki Isobe
  • Patent number: 6710205
    Abstract: An agent comprising the benzoic acid of formula (I) wherein A, B, R6, R7 are carbocyclic ring, heterocyclic ring, etc.; R1 is hydroxy etc.; R2, R3, R4 are alkyl etc.; R5, D, E are alkylene, etc.; G is oxygen etc., as active ingredient. The compound of formula (I) is considered to be useful for the treatment and/or prophylaxis of bone diseases, cancer, systemic granuloma, immunological diseases, allergy, atopy, asthma, gumboil, gingivitis, periodontitis, neurocyte death, Alzheimer's diseases, lungs injury, pulmopathy, acute hepatitis, nephritis, myocardial ischemia, Kawasaki disease, ambustion, ulcerative colitis, Crohn's disease, multiple organ failure, sleeping disorder, platelet aggregation, etc.
    Type: Grant
    Filed: August 16, 2002
    Date of Patent: March 23, 2004
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kousuke Tani, Kaoru Kobayashi, Takayuki Maruyama
  • Patent number: 6664291
    Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.
    Type: Grant
    Filed: March 28, 2001
    Date of Patent: December 16, 2003
    Assignee: Pfizer, Inc.
    Inventors: Yuan-Ching P. Chiang, Gary E. Aspnes, Kimberly G. Estep
  • Patent number: 6649656
    Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.
    Type: Grant
    Filed: April 4, 2001
    Date of Patent: November 18, 2003
    Assignee: Teijin Limited
    Inventors: Naoki Tsuchiya, Susumu Takeuchi, Takumi Takeyasu, Naoki Hase, Takao Yamori, Takashi Tsuruo
  • Patent number: 6566554
    Abstract: The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is an
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: May 20, 2003
    Assignee: Leo Pharmaceutical Products Ltd. a/s (Lovens Kemiske Fabrik Produktionsaktieselskab)
    Inventor: Erik Rytter Ottosen
  • Patent number: 6504052
    Abstract: Compounds of the formula (I) in which R1 is C1-10 allyl; C2-10 alkenyl; C2-10 alkynyl; phenyl-C2-10 alkyl or phenyl-C2-10 alkenyl; and salts and esters thereof, modulate metabotropic glutamate receptor function and are useful in treating disorders of the central nervous system
    Type: Grant
    Filed: November 16, 2001
    Date of Patent: January 7, 2003
    Assignee: Eli Lilly and Company
    Inventors: Ivan Collado Cano, Concepcion Pedregal Tercero, Alicia Marcos Llorente
  • Patent number: 6409995
    Abstract: Use of amino-substituted hydroxybenzophenones of the formula I in which the variables have the meanings explained in the description, as photostable UV filters in cosmetic and pharmaceutical preparations for protecting human skin or human hair from the sun's rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.
    Type: Grant
    Filed: April 20, 2000
    Date of Patent: June 25, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Thorsten Habeck, Frank Prechtl, Thomas Wünsch, Horst Westenfelder, Sylke Haremza, Thorsten Bach, Anja Spiegel
  • Patent number: 6380249
    Abstract: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: April 30, 2002
    Assignees: Merck & Co., Inc., Tularik Inc.
    Inventors: Steven D. Young, Melissa Egbertson, Linda S. Payne, John S. Wai, Thorsten E. Fisher, James P. Guare, Jr., Mark W. Embrey, Lekhanh Tran, Linghang Zhuang, Joseph P. Vacca, H. Marie Langford, Jeffrey Melamed, Juan C. Jaen, David L. Clark, Julio C. Medina
  • Patent number: 6310238
    Abstract: The invention relates to novel o-aminophenolcarboxylic acids or o-aminothiophenolcarboxylic acids of the following structure in which: A1 to A7 are—independently of one another—H, CH3, OCH3, CH2CH3 or OCH2CH3; T is O or S, and m is 0 or 1; Z is a carbocyclic or heterocyclic aromatic radical.
    Type: Grant
    Filed: September 24, 1998
    Date of Patent: October 30, 2001
    Assignee: Siemens Aktiengesellschaft
    Inventors: Recai Sezi, Michael Keitmann
  • Patent number: 6245938
    Abstract: A method of separating a racemic mixture of amino acid enantiomers, which entails reacting the mixture with a 4-pentenoyl compound, thereby derivatizing the enantiomers to form two diastereomers, and separating the diastereomers.
    Type: Grant
    Filed: November 14, 1997
    Date of Patent: June 12, 2001
    Assignee: University of Virginia Patent Foundation
    Inventors: Sidney Hecht, Michiel Lodder
  • Patent number: 6232467
    Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.
    Type: Grant
    Filed: June 27, 1997
    Date of Patent: May 15, 2001
    Assignee: University of Southern California
    Inventors: Nicos A. Petasis, Ilia A. Zavialov
  • Patent number: 6214876
    Abstract: Indene-1-acetamide compounds of the general formula (I) below; inhibit sPLA2 mediated release of fatty acids and are useful for treatment of conditions such as septic shock.
    Type: Grant
    Filed: July 21, 1994
    Date of Patent: April 10, 2001
    Assignees: Eli Lilly and Company, Shionogi & Company, Ltd.
    Inventors: Robert D. Dillard, Sanji Hagishita, Mitsuaki Ohtani
  • Patent number: 6204391
    Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
    Type: Grant
    Filed: September 21, 1998
    Date of Patent: March 20, 2001
    Assignee: The Regents of the University of California
    Inventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
  • Patent number: 6172058
    Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: January 9, 2001
    Assignee: Lilly, SA
    Inventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
  • Patent number: 6103743
    Abstract: Described herein are compounds having the general formula: ##STR1## Ar.sub.1 and Ar.sub.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sub.1 or Ar.sub.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sub.1 and Ar.sub.
    Type: Grant
    Filed: August 6, 1999
    Date of Patent: August 15, 2000
    Assignee: Allelix Neuroscience, Inc.
    Inventors: Stanley Charles Bell, Kathleen Da Silva, Allen Hopper, Methvin Isaac, Eric A. Meade, Vassil Ilya Ognyanov, Abdelmalik Slassi
  • Patent number: 6063815
    Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein Y is ##STR2## R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, perfluoroalkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, thienyl, furyl, phenyl or phenyl mono-, di- or tri-substituted with trifluoromethyl, chloro, methoxy, or trifluoromethoxy;R.sup.3 and R.sup.4 are each, independently, hydrogen, carboxyl, hydroxyl, hydoxyalkyl of 1-6 carbon atoms, hydroxyalkanoyl of 1-6 carbon atoms, aryloxycarbonyl of 7-13 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, perfluoroalkoxycarbonyl of 2-7 carbon atoms, alkyl of 1-6 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, aminoalkyl of 1-6 carbon atoms, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, tetrazolyl, mercapto, alkylsulfanyl of 1-6 carbon atoms, nitrile, nitro, amino, --NHSO.sub.2 CF.sub.
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: May 16, 2000
    Assignee: American Home Products Corporation
    Inventor: Paul J. Dollings
  • Patent number: 6043247
    Abstract: The present invention relates to novel substituted acrylic acids, to methods for their preparation, compositions containing them, and their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention also relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings.
    Type: Grant
    Filed: April 16, 1997
    Date of Patent: March 28, 2000
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Niels Peter Hundahl M.o slashed.ller, Peter Madsen
  • Patent number: 6013811
    Abstract: A process for the preparation of a polycyclic dye of Formula (1) which comprises steps: i) reaction of a compound of formula (2) with a compound of formula (3) or a derivative thereof to form an intermediate of formula (4) and ii) reaction of the intermediate of formula (4) with an aromatic compound of formula (5): B--H optionally in the presence of an oxidizing agent, wherein: A and B each independently is optionally substituted aryl; and X.sup.1 and X.sup.2 each independently is --H, halo, alkyl, or alkoxy.
    Type: Grant
    Filed: December 30, 1998
    Date of Patent: January 11, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: David John Milner, David Philip Devonald
  • Patent number: 5998662
    Abstract: The invention relates to novel o-aminophenolcarboxylic acids, and o-aminothiophenolcarboxylic acids of the following structure: ##STR1## where A.sup.1 to A.sup.7 are--independently of one another--H, F, CH.sub.3, CF.sub.3, OCH.sub.3, OCF.sub.3, CH.sub.2 CH.sub.3, CF.sub.2 CF.sub.3, OCH.sub.2 CH.sub.3 or OCF.sub.2 CF.sub.3, where at least one of the radicals A.sup.1 to A.sup.3 must be F or an F-containing group; T is O or S, and m is 0 or 1; and Z is a carbocyclic or heterocyclic aromatic radical.
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: December 7, 1999
    Assignee: Siemens Aktiengesellschaft
    Inventors: Recai Sezi, Michael Keitmann
  • Patent number: 5936055
    Abstract: Disclosed is an acid-funtionalized polyurethane adduct and a process for the preparation of such adduct. The adduct having a linear or preferably branched structure comprises a plurality of internal urethane linkages and one or more terminal carboxylic acid groups per molecule. Such acid-funtionalized polyurethane adducts find value in the manufacture of crosslinked aqueous rubber latexes such as might be used in paint compositions.
    Type: Grant
    Filed: February 19, 1997
    Date of Patent: August 10, 1999
    Assignee: The Dow Chemical Company
    Inventors: Michael J. Elwell, Hanno R. van der Wal, Camiel F. Bartelink, Henri J. Grunbauer
  • Patent number: 5925787
    Abstract: A method for the production of a keto acid having the general formula ##STR1## wherein R1 and R2 independently represent a straight or branched chain alkyl of 1-18 carbon atoms, a cycloalkyl of 4-8 carbon atoms or a phenyl, each of which may be substituted by at least one substituent selected from the group consisting of halogen atoms and alkyls having 1-4 carbon atoms, an aralkyl of 7-10 carbon atoms, alkoxyalkyl having 2-20 carbon atoms, tetrahydrofuryl alkyl, alkylcarboxy alkyl, alkylcarboxy benzyl, or R1 and R2 together with the adjacent nitrogen atom may form a heterocyclic ring, or one of R.sub.1 and R.sub.2 is hydrogen, but R1 and R2 may not simultaneously be methyl or ethyl or benzyl which comprises reacting a m-amino phenol having the general formula ##STR2## wherein R1 and R2 are the same as above, with phthalic anhydride, in an organic solvent in an amount of less than 0.5 parts by weight per part of m-amino phenol.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: July 20, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James Philip Taylor, William Walker, John Whitworth, Michael Heneghan
  • Patent number: 5916922
    Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.
    Type: Grant
    Filed: November 24, 1997
    Date of Patent: June 29, 1999
    Assignee: Eli Lilly and Company
    Inventors: Theodore Goodson, Jr., Richard Waltz Harper, David Kent Herron
  • Patent number: 5917086
    Abstract: A method for the purification of a keto acid having the general formula ##STR1## wherein R1 and R2 independently represent a straight or branched chain alkyl of 1-18 carbon atoms, a cycloalkyl of 4-8 carbon atoms or a phenyl both of which may be substituted by at least one substituent selected from the group consisting of halogen atoms and alkyls having 1-4 carbon atoms, an aralkyl of 7-10 carbon atoms, alkoxyalkyl having 2-20 carbon atoms, tetrahydrofuryl alkyl, alkylcarboxy alkyl, alkyl carboxy benzyl, or R1 and R2 together with the adjacent nitrogen atom may form a heterocyclic ring, or one of R.sub.1 and R.sub.2 is hydrogen, which comprises slurrying the keto acid with an alcohol solvent, maintaining the slurry at elevated temperature in a sealed vessel until the Rhodamine impurity has dissolved, cooling and isolating the pure keto acid by filtration.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: June 29, 1999
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: James Philip Taylor, John Barry Henshall, John Whitworth
  • Patent number: 5908851
    Abstract: Compounds of formula (I), ##STR1## wherein X is a --CO.sub.2 H or --CONHOH group; R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: June 1, 1999
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Raymond Paul Beckett, Andrew Miller, Zoe Marie Spavold, Mark Whittaker
  • Patent number: 5863947
    Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: January 26, 1999
    Assignee: Eli Lilly and Company Limited
    Inventors: Stephen Richard Baker, Barry Peter Clark, John Goldsworthy, John Richard Harris
  • Patent number: 5843997
    Abstract: The present invention provides novel compounds that affect excitatory amino acid receptors and are useful in the treatment of neurological disorders. This invention also provides synthetic methods for the preparation of the novel compounds.
    Type: Grant
    Filed: April 2, 1996
    Date of Patent: December 1, 1998
    Assignee: Eli Lilly and Company
    Inventors: Lawrence J. Heinz, William H.W. Lunn, Darryle Darwin Schoepp
  • Patent number: 5840939
    Abstract: Compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; ##STR1## R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: November 24, 1998
    Assignee: British Biotech Pharmaceuticals, Ltd.
    Inventors: Raymond Paul Beckett, Andrew Miller, Zoe Marie Spavold, Mark Whittaker
  • Patent number: 5811460
    Abstract: A water soluble derivative of buckministerfullerene (C.sub.60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.
    Type: Grant
    Filed: January 24, 1994
    Date of Patent: September 22, 1998
    Assignee: The Regents of the University of California
    Inventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. De Camp, Rintje P. Sijbesma, George L. Kenyon
  • Patent number: 5753700
    Abstract: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2, therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: May 19, 1998
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Yuuki Nagao, Kazuhiko Torisu, Takayuki Maruyama
  • Patent number: 5723489
    Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.
    Type: Grant
    Filed: May 7, 1996
    Date of Patent: March 3, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
  • Patent number: 5717109
    Abstract: The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.
    Type: Grant
    Filed: July 10, 1995
    Date of Patent: February 10, 1998
    Assignee: Eli Lilly and Company
    Inventors: M. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano
  • Patent number: 5679711
    Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoalkanoate salts and substituted N,N-substituted-aminoalkanoate salts.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 21, 1997
    Assignee: FHJ Scientific, Inc.
    Inventors: Delton R. Carrell, Edward J. Cragoe, Jr.
  • Patent number: 5631401
    Abstract: The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.
    Type: Grant
    Filed: January 24, 1995
    Date of Patent: May 20, 1997
    Assignee: Abbott Laboratories
    Inventors: Herman H. Stein, William R. Baker, Anthony K. L. Fung, Saul H. Rosenberg, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, William J. McClellan, Stephen J. O'Connor, Rajnandan Prasad, Wang Shen, Gerard M. Sullivan
  • Patent number: 5589501
    Abstract: A pharmaceutical compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,Y is --CH.dbd.CH--, andZ is(i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or(iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.
    Type: Grant
    Filed: November 22, 1994
    Date of Patent: December 31, 1996
    Assignees: Eli Lilly and Company, Universite Louis Pasteur, Lilly, S.A.
    Inventors: Jesus E. Carrera, Almudena R. Esteban, Andr e Mann, Ang ele Schoenfelder, Darryle D. Schoepp, Concepcion P. Tercero, Camille-Georges Wermuth
  • Patent number: 5585391
    Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoacetate salts and substituted N,N-substituted-aminoacetate salts.
    Type: Grant
    Filed: October 8, 1993
    Date of Patent: December 17, 1996
    Assignee: FHJ Scientific, Inc.
    Inventors: Delton R. Carrell, Edward J. Cragoe, Jr.
  • Patent number: 5530157
    Abstract: Novel benzoic acid derivatives have the formula: ##STR1## wherein --X-- represents C.sub.1 to C.sub.6 alkylene, C.sub.2 to C.sub.6 alkenylene or a divalent moiety having the structure --(CH.sub.2).sub.m --Z-- in which m is an integer from 0 to 3 and Z represents --O--, --S-- or --NH--;--Y-- represents a direct bond, C1 to C.sub.6 alkylene, C.sub.2 to C.sub.6 alkenylene or a divalent moiety having the structure --(CH.sub.2).sub.m --Z--(CH.sub.2).sub.n in which m and n are each, independently, an integer from 0 to 3 and --Z-- represents --O--, --S-- or --NH--;R represents a 5- or 6-membered carbocyclic or heterocyclic ring or a carbocyclic or heterocyclic fused ring system containing up to 10 members in the ring, which carbocyclic, heterocyclic or fused ring system may be saturated or unsaturated and may contain up to two substituents selected from lower alkyl, methoxy, halo and trifluoromethyl; andR.sup.1 and R.sup.
    Type: Grant
    Filed: February 16, 1995
    Date of Patent: June 25, 1996
    Assignee: Scios Nova Inc.
    Inventors: Richard Mewshaw, Gregory S. Hamilton
  • Patent number: 5514808
    Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoacetate salts and substituted N,N-substituted-aminoacetate salts.
    Type: Grant
    Filed: August 25, 1994
    Date of Patent: May 7, 1996
    Assignee: FHJ Scientific, Inc
    Inventors: Delton R. Carrell, Edward J. Cragoe, Jr.
  • Patent number: 5463107
    Abstract: Triterpene derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydrogen or metabolic ester residue; and R.sup.2 is hydrogen or --R.sup.3 --R.sup.4 wherein R.sup.3 is --SO.sub.3 --, --CH.sub.2 COO--, --COCOO--, or --COR.sup.5 COO-- (R.sup.5 is lower alkylene or lower alkenylene), and R.sup.4 is hydrogen or metabolic ester residue or a pharmaceutically acceptable salt thereof, which have anti-endothelin activities and are useful in prophylaxis and treatment of diseases caused by excessive secretion of endothelin.
    Type: Grant
    Filed: June 10, 1994
    Date of Patent: October 31, 1995
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiro Konoike, Yoshitaka Araki, Tetsuyoshi Hayashi, Kensuke Sakurai, Takehiko Tozyo
  • Patent number: 5385917
    Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: January 31, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Hiroaki Ueno, Masahiko Morioka, Fumiko Hatanaka
  • Patent number: 5374724
    Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.
    Type: Grant
    Filed: November 2, 1992
    Date of Patent: December 20, 1994
    Assignee: Zeneca, Limited
    Inventors: Nigel Hall, Nigel Hughes, Prakash Patel
  • Patent number: 5371285
    Abstract: In a method of producing a keto acid having the general formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl of 1-6 carbons or a cycloalkyl of 4-8 carbons, by reacting an m-aminophenol having the general formula ##STR2## wherein R.sup.1 and R.sup.2 are the same as above, with phthalic anhydride, in an organic solvent, the improvement comprising effecting the reaction in an amount of the organic solvent which is insufficient to dissolve the keto acid produced in the reaction, so that at least a portion of the resultant keto acid crystallizes out of the solvent and allowing the reaction to proceed in a heterogeneous system.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: December 6, 1994
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Masahiro Kondo, Michio Tanaka, Naoya Sakamoto, Hajime Ooyoshi
  • Patent number: 5324833
    Abstract: Compounds of the formula I, ##STR1## in which 'R.sub.1 is an amino protective group, and n stands for 1 or 2, R.sub.1 denotes hydrogen or an amino protective group, R.sub.2 denotes hydrogen or a carboxyl protective group and R.sub.3 denotes triphenylmethyl, 4-monomethoxy-trityl or 4,4'-dimethoxy-trityl, and reactive carboxylic acid derivatives of such compounds of the formula I in which R.sub.2 stands for hydrogen, are described.These compounds can be used as starting materials for the preparation of peptides. They are more suitable for this than are analogous compounds of the formula I in which R.sub.3 denotes hydrogen or one of the carbamoyl protective groups hitherto customary.
    Type: Grant
    Filed: April 13, 1990
    Date of Patent: June 28, 1994
    Assignee: Novabiochem AG
    Inventors: Peter Sieber, Bernhard Riniker
  • Patent number: 5288914
    Abstract: The invention is a poly(arylcyclobutene) comprising arylcyclobutene moieties connected by a bridging member, wherein the bridging member is (a) a direct bond, (b) a polyvalent inorganic radical or (c) a polyvalent organic radical which contains (1) one or more heteroatoms comprising oxygen, sulfur, nitrogen or phosphorus or (2) one or more aromatic radicals, and wherein one or more cyclobutene rings are fused to one of the aryl rings.
    Type: Grant
    Filed: December 26, 1989
    Date of Patent: February 22, 1994
    Assignee: The Dow Chemical Company
    Inventor: Robert A. Kirchhoff
  • Patent number: 5264577
    Abstract: Novel cyclic amino acids which are useful in preparing biologically active peptides as well as a process for the preparation of D and L enantiomers of the cyclic amino acids are described where an N-protected derivative of the racemic cyclic amino acid is treated with (-)cinchonidine and the resulting salt resolved into the desired enantiomers, as well as derivatives thereof and valuable intermediates used in the process.
    Type: Grant
    Filed: April 22, 1992
    Date of Patent: November 23, 1993
    Assignee: Warner-Lambert Company
    Inventors: Vladimir Beylin, Huai G. Chen, Om P. Goel, Mark E. Marlatt, John G. Topliss