Patents Represented by Attorney, Agent or Law Firm Philip I. Datlow
  • Patent number: 6828301
    Abstract: Disclosed are pharmaceutical compositions of hepatitis C viral protease inhibitors having improved bioavailability, and methods of using these compositions for inhibiting the replication of the hepatitis C virus (HCV) and for the treatment of an HCV infection. These compositions include co-solvent systems, lipid based systems, solid dispersions and granulations, and all comprise the hepatitis C viral protease inhibitor, at least one pharmaceutically acceptable amine and optionally one or more additional ingredients.
    Type: Grant
    Filed: February 4, 2003
    Date of Patent: December 7, 2004
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Shirlynn Chen, Xiaohui Mei
  • Patent number: 6794158
    Abstract: This invention is directed to a fluorescence polarization assay useful in the detection and evaluation of soluble epoxide hydrolase (sEH) inhibitors. This invention also relates to novel fluorescent probes used in the fluorescence polarization assay, and methods of manufacturing such fluorescent probes. This fluorescent probe of the invention is a compound having the following formula (I): X-spacer-R1-Y  (I) wherein X is the radical of compound that binds to the active site of soluble epoxide hydrolase, Y is a fluorescent label, and “spacer” and R1 are as defined herein.
    Type: Grant
    Filed: March 28, 2002
    Date of Patent: September 21, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Richard Harold Ingraham, Mario G. Cardozo, Christine Anne Grygon, Rachel Rebecca Kroe, John Robert Proudfoot
  • Patent number: 6794404
    Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: September 21, 2004
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
  • Patent number: 6770639
    Abstract: Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases associated with such kinases, for example, diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are processes for preparing these compounds, novel intermediates useful in these processes and compositions comprising compounds of the formula (I).
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: August 3, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, III, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
  • Patent number: 6770762
    Abstract: Disclosed is a process which can be used on an industrial scale for preparing and purifying 1,7′-dimethyl-2′-propyl-2,5′-bi-1H-benzimidazole in which the crude product is subjected to charcoal treatment.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: August 3, 2004
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Werner Belzer, Rolf Dach, Volker Fachinger, Markus Heitzmann, Hartmut Schmidt
  • Patent number: 6767991
    Abstract: Disclosed herein are hepatitis C viral protease inhibitors of formula (I): wherein a is 0 or 1; b is 0 or 1; Y is H or C1-6 alkyl; B is H, an acyl derivative or a sulfonyl derivative; R6, when present, is C1-6 alkyl substituted with carboxyl; R5, when present, is C1-6 alkyl optionally substituted with carboxyl; R4 is C1-10 alkyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); R3 is C1-10 alkyl optionally substituted with carboxyl, C3-7 cycloalkyl or C4-10 (alkylcycloalkyl); R2 is CH2—R20, NH—R20, O—R20 or S—R20; wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkyl cycloalkyl) being optionally mono-, di- or tri-substituted with R21, or R20 is a C6 or C10aryl, C7-16 aralkyl, Het or (lower alkyl)-Het, all optionally mono-, di- or tri-substituted with R21, wherein R21 is as defined herein; R1 is C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl, all optionally substituted with halogen; and W is hydroxy or a N-substituted amino: or W taken together with t
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: July 27, 2004
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale Cameron, Elise Ghiro, Nathalie Goudreau, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Bruno Simoneau, Dominik M. Wernic
  • Patent number: 6759409
    Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: wherein: A,; X, W, R1, Y; R3; and R4 are as defined herein. The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.
    Type: Grant
    Filed: December 17, 2001
    Date of Patent: July 6, 2004
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Christiane Yoakim, Bruno Haché, William W. Ogilvie, Jeffrey O'Meara, Peter White, Nathalie Goudreau
  • Patent number: 6747044
    Abstract: The invention relates to new compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1 denotes 3-hydroxypropyl, 1,3-dihydroxyprop-2-yl or C3-C6-cycloalkylmethyl, and R2, R3, R4 and Ar have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: June 8, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Horst Dollinger, Franz Esser, Birgit Jung, Kurt Schromm, Georg Speck
  • Patent number: 6739333
    Abstract: The present invention relates to corrosion resistant stainless steel canisters for propellant-containing aerosol forumlations for use in propellant gas-operated inhalers.
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: May 25, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Hubert Hoelz, Richard Thomas Lostritto, Juergen Nagel, Julio César Vega
  • Patent number: 6689804
    Abstract: A method for treating inflammatory and immune cell-mediated diseases by the administration of compounds of the formula I Exemplary are:
    Type: Grant
    Filed: July 16, 2002
    Date of Patent: February 10, 2004
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jiang-Ping Wu, Terence Alfred Kelly, Rene Lemieux, Daniel R. Goldberg, Jonathan Emilian Emeigh, Ronald John Sorcek
  • Patent number: 6683089
    Abstract: The present invention relates to 1,2,3,4,5,6-hexahydro-2,6-methano-3 -benzazocin-10-ols of general formula 1 wherein the groups R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as set forth herein, processes for preparing them, pharmaceutical compositions thereof and their use in treating or preventing a disease or disorder by blocking the voltage-dependent sodium channel.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: January 27, 2004
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Adrian Carter, Helmut Ensinger, Matthias Grauert, Detlef Andre Stiller, Thomas Weiser
  • Patent number: 6664253
    Abstract: The invention relates to new compounds of formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, X and Ar1 have the meanings given in the specification, as well as the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: December 16, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Horst Dollinger, Franz Esser, Birgit Jung, Gerd Schnorrenberg, Kurt Schromm, Georg Speck
  • Patent number: 6663889
    Abstract: The present invention relates to a new tablet for sucking containing the active substance ambroxol and having improved properties.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: December 16, 2003
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frieder Ulrich Maerz, Holger Hans-Hermann Von Der Heydt, Horst Schmitt
  • Patent number: 6642204
    Abstract: Disclosed herein are compounds of formula (1): wherein R1 is hydroxy or NHSO2R1A wherein R1A is (C1-8)alkyl, (C3-7)cycloalkyl or {(C1-6)alkyl-(C3-7)cycloalkyl}, which are all optionally substituted from 1 to 3 times with halo, cyano, nitro, O—(C1-6)alkyl, amido, amino or phenyl, or R1A is C6 or C10 aryl which is optionally substituted from 1 to 3 times with halo, cyano, nitro, (C1-6)alkyl, O—(C1-6) alkyl, amido, amino or phenyl; R2 is (C4-6)cycloalkyl; R3 is t-butyl or (C5-6) cycloalkyl and R4 is (C4-6)cycloalkyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of HCV NS3 protease.
    Type: Grant
    Filed: January 29, 2003
    Date of Patent: November 4, 2003
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Montse Llinas-Brunet, Vida J. Gorys
  • Patent number: 6617325
    Abstract: The present invention relates to biphenyl derivatives of general formula wherein Ra to Rg and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: September 9, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Patent number: 6610624
    Abstract: Methods for removing soluble material from confined spaces within substrates such as containers, capsules and porous powders comprising extraction with supercritical fluids, the pressure of which is preferably modulated between an upper level and a lower level within a relatively narrow range of fluid pressure and density. The method permits enhanced extraction efficiency, catalytic reaction rates and ability to maintain catalyst activity.
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: August 26, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Stephen T. Horhota, Said Saim
  • Patent number: 6608027
    Abstract: The present invention covers macrocyclic compounds of formula I active in-vitro and in cellular assays against the NS3 protease of the hepatitis C virus. wherein W, R21, R22, R3, R4, D and A are as defined herein, or a pharmaceutically acceptable salts or ester thereof.
    Type: Grant
    Filed: January 16, 2001
    Date of Patent: August 19, 2003
    Assignee: Boehringer Ingelheim (Canada) Ltd
    Inventors: Youla S. Tsantrizos, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Montse Llinas-Brunet
  • Patent number: 6593355
    Abstract: Novel benzimidazoles having antithrombotic activity. Exemplary are: (a) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, (b) 2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, and (c) (R)-2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(isobutyloxycarbonylmethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole.
    Type: Grant
    Filed: July 3, 2002
    Date of Patent: July 15, 2003
    Assignee: Boehringer Ingelehim Pharma KG
    Inventors: Uwe Ries, Iris Kaufmann-Hefner, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
  • Patent number: 6585959
    Abstract: The invention relates to a new process for producing powdered preparations for inhalation.
    Type: Grant
    Filed: October 11, 2001
    Date of Patent: July 1, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Michael Walz, Georg Boeck
  • Patent number: 6583285
    Abstract: The invention relates to a process for preparing a compound of formula (I) wherein a compound of formula (II),  wherein R1 denotes chlorine, bromine, iodine, —O—COCH3, tosylate or mesylate, is reacted with a compound of formula (III),  optionally in a suitable diluent and/or in the presence of a suitable added reagent or catalyst, the reaction being carried out in a temperature range from 20 to 80° C.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: June 24, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Markus Sauter, Wolfgang Wohlleben