Patents Examined by Ben Schroeder
  • Patent number: 6358985
    Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 29, 1999
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ian M. Bell, Douglas C. Beshore, Terrence M. Ciccarone, S. Jane de Solms, Christopher J. Dinsmore, Gerald E. Stokker
  • Patent number: 6265416
    Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.
    Type: Grant
    Filed: October 28, 1999
    Date of Patent: July 24, 2001
    Assignee: Eli Lilly and Company
    Inventors: Jolie Anne Bastian, Matthew Joseph Fisher, Richard Waltz Harper, Ho-Shen Lin, Jefferson Ray McCowan, Daniel Jon Sall, Gerald Floyd Smith, Kumiko Takeuchi, Michael Robert Wiley, Minsheng Zhang
  • Patent number: 6251916
    Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.
    Type: Grant
    Filed: May 9, 2000
    Date of Patent: June 26, 2001
    Assignee: UCB, S. A.
    Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
  • Patent number: 6248770
    Abstract: The present invention relates to new benzimidazoles of general formula wherein Ra to Rc, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain a group which is negatively charged under physiological conditions, instead of a carboxy group, and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein Rc denotes one of the amidino groups mentioned in claim 1 which have valuable pharmacological properties, particularly an antithrombotic activity.
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: June 19, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Uwe Ries, Iris Kauffmann, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
  • Patent number: 6242602
    Abstract: Dihydrophenazines and bis(dihydrophenazines) are prepared in high yield under commercially viable reaction conditions by reacting a catechol with a 1,2-diaminoaryl compound, wherein either the catechol or the 1,2-diaminoaryl compound is provided in at least 50% molar stoichiometric excess. The product may be oxidized to the corresponding phenazine, but is preferably derivatized at one or both of the 5,10-positions to form a monosubstituted or disubstituted dihydrophenazine or bis(dihydrophenazine). Most preferably, 5,10-dialkyl-5,10-dihydrophenazines are prepared starting from catechol and 1,2-diaminoaryl compound in a one pot synthesis. The products are useful as dyes, and in particular as chromophores in electrochromic systems.
    Type: Grant
    Filed: March 29, 1999
    Date of Patent: June 5, 2001
    Assignee: Gentex Corporation
    Inventors: Punam Giri, Harlan J. Byker, Kelvin L. Baumann
  • Patent number: 6228810
    Abstract: Pyridine derivatives of the formula I and their salts, their preparation, and their use for controlling animal pests and harmful fungi.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: May 8, 2001
    Inventors: Franz Röhl, Volker Harries, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Arne Ptock, Hubert Sauter, Wassilios Grammenos, Thomas Grote, Herbert Bayer, Reinhard Kirstgen, Klaus Oberdorf, Bernd Müller, Ruth Müller
  • Patent number: 6221870
    Abstract: The invention provides compounds of formula I wherein R1 to R6 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
    Type: Grant
    Filed: November 23, 1999
    Date of Patent: April 24, 2001
    Assignee: Novartis AG
    Inventors: Paul Pfaeffli, Peter Neumann, Robert Swoboda, Peter Stütz
  • Patent number: 6218378
    Abstract: A method of treatment or inhibition of tumors including the steps of: (i) exchanging one or more of the eight phenyl substituents in the compound [M(dppe)2]+ where M is selected from Au(I), Ag(I) and Cu(I) by 2, 3, or 4 pyridyl substituents to provide a compound having anti-tumor activity and an octanol/water partition coefficient between 0.01 and 25.5; and (ii) administering said compound to a subject requiring treatment which compound has selective toxicity to cancer cells including cisplatin resistant human carcinoma cell lines.
    Type: Grant
    Filed: August 22, 1997
    Date of Patent: April 17, 2001
    Assignee: Griffith University
    Inventors: Susan Jane Berners-Price, Richard John Bowen, Peter Gordon Parsons
  • Patent number: 6207835
    Abstract: Arylmetal compounds are prepared by deprotonation of aromatics which have a hydrogen atom in the ortho position relative to a halogen atom or a trifluoromethoxy group, using a suitable base or by halogen-metal exchange of haloaromatics using a suitable metalating reagent. The arylmetal compounds are prepared in a continuous-flow reactor. The arylmetal compound can be further reacted with an electrophilic reagent.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: March 27, 2001
    Assignee: Merck KGaA
    Inventors: Volker Reiffenrath, Hans Christian Stiasny
  • Patent number: 6204264
    Abstract: A benzimidazole derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is —(CH2)n—NR2R3; R2 and R3 individually represent H, lower alkyl, phenyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members, or —CONR5—(CH2)n—NR2R3 may be the following Group (W): wherein R2 is H, lower alkyl, phenyl or benzyl and ring E is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, cyano, trifluoromethyl, lower alkyl and etc.; R5 is H, lower alkyl, lower acyl or lower alkylcarbamoyl; m is 0 or 1; and n is an integer of 0-5. The benzimidazole derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.
    Type: Grant
    Filed: September 17, 1999
    Date of Patent: March 20, 2001
    Assignee: Shiseido Co., Ltd.
    Inventors: Koji Kobayashi, Hirotada Fukunishi, Kenichi Umishio, Masahiro Tajima
  • Patent number: 6197729
    Abstract: Compounds of formula I where R1 is hydrogen, chlorine, fluorine or methyl, R2 and R3, which may be the same or different from each other, are hydrogen, halogen, cyano, (C1-C4)-alkyl, vinyl, ethynyl, (C1-C4)-alkoxy, (C1-C4)-alkoxy-(C1-C4)-alkyl, fluorovinyl or fluoroethyl, or R2 and R3 together with the linking carbon atoms form a benzo ring, and R4 is (C2-C4)-alkyl, (C2-C4)-alkenyl or (C3-C4)-alkinyl, each of which is substituted by at least two fluorine atoms and optionally substituted by C1-4-alkoxy, cyanomethoxy, (C3-C4)-alkenyloxy or (C3-C4)-alkinyloxy, are useful as pesticides, especially against insects, acarids and fungi. The invention includes a novel process for fluorinating certain pyrimidines.
    Type: Grant
    Filed: July 29, 1999
    Date of Patent: March 6, 2001
    Assignee: Hoechst Schering Agrevo
    Inventors: Martin Märkl, Wolfgang Schaper, Oswald Ort, Harald Jakobi, Ralf Braun, Gerhard Krautstrunk, Ulrich Sanft, Werner Bonin, Herbert Stark, Sergej Pasenok, Ivan Cabrera
  • Patent number: 6193949
    Abstract: There is variation in the sexual performance of male mammals. The purpose of this invention is to help identify high sexual performing males, particularly for livestock such as sheep. Testosterone is necessary for the normal execution of male behavior, but baseline levels are not predictive of libido. When a male mammal is given an injection of naloxone (an endorphin antagonist), his testosterone or LH response to the injection predicts whether he is a sexually active or inactive individual. This test is based on the premise that libido is more closely linked to the ability to secrete testosterone rather than baseline concentrations. Naloxone challenge may be used as a general method to predict libido in male mammals.
    Type: Grant
    Filed: May 27, 1999
    Date of Patent: February 27, 2001
    Assignees: The United States of America as represented by the Secretary of Agriculture, Carroll College
    Inventors: Anne Perkins, James A. Fitzgerald, Verne A. Lavoie, John N. Stellflug
  • Patent number: 6191129
    Abstract: A pyridobenzoxazine derivative having a bicyclic amine derivative as its substituent, represented by the formula (I): exhibiting antimcrobial activity, and useful in treating infectious diseases and preserving food and agricultural products.
    Type: Grant
    Filed: March 18, 1999
    Date of Patent: February 20, 2001
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami
  • Patent number: 6191160
    Abstract: Compounds of the general structural formula I are selective NPY Y5 receptor antagonists. The compounds and compositions of the present invention are useful in the treatment of obesity and complications associated therewith.
    Type: Grant
    Filed: November 8, 1999
    Date of Patent: February 20, 2001
    Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
    Inventors: Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
  • Patent number: 6187802
    Abstract: Compounds of Formula I including pharmaceutically acceptable salts thereof in the form of individual enantiomers, racemates, or other mixtures of enantiomers, in which Ar is phenyl, naphthyl or benzo[b]thiophenyl, each of which may be optionally substituted; R1 and R2, which may be the same or different, independently are a) H, b) an alkyl group containing 1 to 6 carbon atoms, c) an alkenyl group containing 3 to 6 carbon atoms, d) a cycloalkyl group containing 3 to 7 carbon atoms, e) a cycloalkylmethyl group in which the ring contains 3 to 7 carbon atoms, f) an aryl or heteroaryl group optionally substituted g) an arylalkyl or heteroarylalkyl group each optionally substituted; or R1 and R2 form an alkylene chain optionally substituted by one or more alkyl groups each containing 1 to 3 carbon atoms, such that, together with the atoms to which they are attached, they form a 5 or 6 membered ring; R3 is a) H, b) an aryl or heteroaryl group each optionally substituted c) an optionally
    Type: Grant
    Filed: September 14, 1999
    Date of Patent: February 13, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Sharon Crawford Cheetham, Frank Kerrigan, Colin Gerhart Pryce Jones
  • Patent number: 6187778
    Abstract: This invention provides a means of inhibiting or preventing a disease or condition associated with an excess of neuropeptide Y which comprises administering to a mammal in need of such treatment an effective amount of a compound of the formula: wherein R1 is a nitrogen containing heterocyclic compound.
    Type: Grant
    Filed: September 7, 1999
    Date of Patent: February 13, 2001
    Assignee: Pfizer Inc.
    Inventors: Robert Lee Dow, Marlys Hammond
  • Patent number: 6184225
    Abstract: The invention relates to quinazoline derivatives of formula (I) wherein: Z represents —O—, —NH— or —S—; m is an integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluorometlyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino, or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, SO2—, —NR6—, NR8CO—, —CONR9—SO2NR10— or —NR11SO2—, (wherein R7, R8, R9, R10 and R11 each represents C1-3alkyl, C1-3alkoxyC2-3alkyl); R4 represents a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or al
    Type: Grant
    Filed: August 13, 1998
    Date of Patent: February 6, 2001
    Assignee: Zeneca Limited
    Inventors: Andrew Peter Thomas, Craig Johnstone, Laurent Francois Andre Hennequin
  • Patent number: 6174901
    Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: January 16, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
  • Patent number: 6172108
    Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z  (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptor
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: January 9, 2001
    Assignee: Adir et Compagnie
    Inventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
  • Patent number: 6172005
    Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation and Q, W, X, Y, Z, and R1 through R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: January 9, 2001
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas P. Selby