Patents Examined by Robert Gerstl
  • Patent number: 6251928
    Abstract: This invention provides novel benzylidene rhodanines which are useful as agents in treating or preventing conditions associated with &bgr;-amyloid peptide. This invention further provides methods of treating or preventing Alzheimer's Disease which comprises administering to a mammal in need thereof an effective amount of one or more of the benzylidene rhodanines of the present invention.
    Type: Grant
    Filed: March 16, 1994
    Date of Patent: June 26, 2001
    Assignee: Eli Lilly and Company
    Inventors: Jill A. Panetta, Michael L. Phillips, Jon K. Reel, John K. Shadle, Sandra K. Sigmund, Richard L. Simon, Celia A. Whitesitt
  • Patent number: 6251936
    Abstract: This invention provides compounds of Formula I having the structure E is S, SO, SO2, O, or NR1c; X is hydrogen, halogen, alkyl of 1-6 carbon atoms, alkenyl of 2-7 carbon atoms, CN, aryl, aralkyl of 6-12 carbon atoms, hydroxyalkyl of 1-6 carbon atoms, hydroxyaralkyl of 6-12 carbon atoms, perfluoroalkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy; arylalkoxy, nitro, amino, NR2R2a, NR2COR2a, cycloalkylamino of 3-8 carbon atoms, morpholino, alkylsulfanyl of 1-6 carbon atoms, arylsulfanyl, pyridylsulfanyl, 2-N,N-dimethylaminoethylsulfanyl, —OCH2CO2R2b or —COR2c; Z1 and Z2 are each, independently, hydrogen, halogen, CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms, cycloalkyl of 3-8 carbon atoms, nitro, amino, —NR1R1a, —NR1COR1a, cycloalkylamino of 3-8 carbon atoms, morpholino, or OR8, or Z1 and Z2 may be taken together as a diene unit having the formula —CH═CR9—CR10═CR11—; or a pharmaceutically acceptable salt th
    Type: Grant
    Filed: May 10, 1999
    Date of Patent: June 26, 2001
    Assignee: American Home Products Corporation
    Inventors: Jay E. Wrobel, Arlene J. Dietrich, Madelene M. Antane
  • Patent number: 6251932
    Abstract: The invention relates to an immunophilin ligand of Formula I and having antiasthmatic, antiallergic, antirheumatic, immunosuppressant, antipsoriatic and neuroprotectant properties,
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: June 26, 2001
    Assignee: ASTA Medica AG
    Inventors: Dietmar Reichelt, Berhard Kutscher, István Szelényi, Hildegard Poppe, Gerhard Quinkert, Kay Brune, Holger Bang, Holger Deppe
  • Patent number: 6245927
    Abstract: According to the present invention, provided are (1) a process for the preparation of 2-chloro-5-chloromethyl-1,3-thiazole, by reacting 3- chloro-1-isothiocyanato-1-propene with a chlorinating agent, (2) a process for the preparation of 3-chloro-1-isocyanato-1-propene, by rearranging 3-chloro-1-thiocyanato-2-propene in the presence of a salt of one or more than one metal selected from the group consisting of metals belonging to Group 2A, Group 7A, Group 8 and Group 1B of the long-form periodic table, and (3) a process for the preparation of 3-chloro-1-thiocyanato-2-propene, by reacting 1,3-dichloropropene and a thiocyanate salt (a) in the presence of water, (b) in the presence of an organic solvent which is water-soluble and has a boiling point of 150° C. or lower, or (c) in an organic solvent in the presence of a phase transfer catalyst.
    Type: Grant
    Filed: April 11, 2000
    Date of Patent: June 12, 2001
    Assignee: Kuraray Co., Ltd.
    Inventors: Hideki Matsuda, Goro Asanuma, Manzo Shiono
  • Patent number: 6242493
    Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: June 5, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yves Gareau, Marc LaBelle, Helene Juteau, Michel Gallant, Nicolas LaChance, Michel Belley
  • Patent number: 6239152
    Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
    Type: Grant
    Filed: January 22, 1999
    Date of Patent: May 29, 2001
    Assignee: Pharmacia & Upjohn Company
    Inventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
  • Patent number: 6235740
    Abstract: Novel imidazoquinoxalines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: May 22, 2001
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Joel C. Barrish, Ping Chen, Jagabandhu Das, Edwin J. Iwanowicz, Derek J. Norris, Ramesh Padmanabha, Jacques Y. Roberge, Gary L. Schieven
  • Patent number: 6235895
    Abstract: A compound of formula (I) or (II), wherein: M is Pb or Sn or Bi, n is 1 to 20, each R1 is independently —SiR3 or R or —CCSiR3 or —CCR or H, each R2 is independently —CCSiR3 or —CCR or H, each X is independently H or C1 to C20 hydrocarbyl optionally including a carboxylic acid or ester group, each Y is independently H or C1 to C20 hydrocarbyl, each R is independently H or C1 to C20 hydrocarbyl, Z is C1 to C20 alkylene or arylene.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: May 22, 2001
    Assignee: The Secretary of State for Defence
    Inventors: Kenneth J McEwan, Harry Anderson
  • Patent number: 6235786
    Abstract: Compounds having the formula are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: May 22, 2001
    Assignee: Abbott Laboratories
    Inventors: Yujia Dai, Steven K. Davidsen, Michael R. Michaelides, Jamie R. Stacey, Douglas H. Steinman, Carol K. Wada
  • Patent number: 6235762
    Abstract: The present invention relates to 2-aryl-&Dgr;2-1,3,4-(oxa and thia)diazoline compounds having the structural formula and compositions and methods comprising those compounds for the control of insect and acarid pests.
    Type: Grant
    Filed: November 5, 1999
    Date of Patent: May 22, 2001
    Assignee: American Cyanamid Company
    Inventors: James Jan Takasugi, Brian Lee Buckwalter
  • Patent number: 6232344
    Abstract: 13-Oxa analogs of certain prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.
    Type: Grant
    Filed: May 21, 1999
    Date of Patent: May 15, 2001
    Assignee: Alcon Laboratories, Inc.
    Inventors: Zixia Feng, Mark R. Hellberg
  • Patent number: 6232304
    Abstract: Compositions of matter comprising a pharmaceutically acceptable salt of an aryl-heterocyclic compound, such as ziprasidone, in a cyclodextrin. Preferred cyclodextrins are SBECD and HPBCD. The composition can comprise a dry mixture, a dry inclusion complex or an aqueous solution. The salt/cyclodextrin inclusion complex preferably provides an amount of ziprasidone of at least 2.5 mgA/ml when the complex is dissolved in water at 40% w/v. A variety of ziprasidone salts are preferred, including the mesylate, esylate, besylate, tartrate, napsylate, and tosylate.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: May 15, 2001
    Assignee: Pfizer Inc.
    Inventors: Yesook Kim, Kevin C. Johnson, Ravi M. Shanker
  • Patent number: 6232498
    Abstract: There are described processes for the preparation of a compound of formula I and novel intermediates in the preparative process.
    Type: Grant
    Filed: October 1, 1999
    Date of Patent: May 15, 2001
    Assignee: Astra Zeneca UK Limited
    Inventor: Christopher Goodwin
  • Patent number: 6225288
    Abstract: Compounds represented by formula I: as well as pharmaceutically acceptable salts, esters and hydrates thereof are disclosed along with pharmaceutical compositions and methods of treatment. The compounds are useful as inhibitors of caspase-3, which is implicated in modulating apoptosis.
    Type: Grant
    Filed: March 16, 2000
    Date of Patent: May 1, 2001
    Assignee: Merk Frosst Canada & Co.
    Inventors: Yongxin Han, Andre Giroux, Erich Grimm, Renee Aspiotis, Sebastien Francoeur, Robert Zamboni, Petpiboon Prasit, Christopher Bayly, Dan McKay, Cameron Black
  • Patent number: 6225330
    Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: May 1, 2001
    Assignees: Synaptic Pharmaceutical Corporation, Novartis AG
    Inventors: Mohammad R. Marzabadi, Wai C. Wong, Walter Schilling, Stewart A. Noble
  • Patent number: 6225347
    Abstract: The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or a
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: May 1, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Bernd Buchmann, Werner Skuballa, Helmut Vorbrueggen, Bernd Raduechel, Olaf Loge, Walter Elger, Claus-Steffen Stuerzebecher, Karl-Heinz Thierauch
  • Patent number: 6222040
    Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: April 24, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Mohammad R. Marzabadi, Peter Bühlmayer, Heinrich Rüeger, Wai C. Wong, Yasuchika Yamaguchi, Stewart A. Noble
  • Patent number: 6222057
    Abstract: According to the present invention, provided are (1) a process for the preparation of 2-chloro-5-chloromethyl-1,3-thiazole, by reacting 3-chloro-1-isothiocyanato-1-propene with a chlorinating agent, (2) a process for the preparation of 3-chloro-1-isocyanato-1-propene, by rearranging 3-chloro-1-thiocyanato-2-propene in the presence of a salt of one or more than one metal selected from the group consisting of metals belonging to Group 2A, Group 7A, Group 8 and Group 1B of the long-form periodic table, and (3) a process for the preparation of 3-chloro-1-thiocyanato-2-propene, by reacting 1,3-dichloropropene and a thiocyanate salt (a) in the presence of water, (b) in the presence of an organic solvent which is water-soluble and has a boiling point of 150° C. or lower, or (c) in an organic solvent in the presence of a phase transfer catalyst.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: April 24, 2001
    Assignee: Kuraray Co., Ltd.
    Inventors: Hideki Matsuda, Goro Asanuma, Manzo Shiono
  • Patent number: 6218408
    Abstract: This invention is directed to bicyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: April 17, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Mohammad R. Marzabadi, Wai C. Wong, Stewart A. Noble
  • Patent number: 6218572
    Abstract: A process for preparing N-protected N-alkylated amino acids of the formula I: in which the substituents have the meanings stated in the description, comprises mixing a compound of the formula II with a solution of potassium tert-butanolate in a non-protic organic solvent, and subsequently adding a C1-2-alkyl halide.
    Type: Grant
    Filed: November 19, 1996
    Date of Patent: April 17, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Karl, Stefan Müller, Bernd de Potzolli