Patents Represented by Attorney, Agent or Law Firm A. R. Stempel
  • Patent number: 6663848
    Abstract: A method for crystallizing a substance, especially an inhalable medicament, comprising the following steps: (a) dissolving said substance in a solvent, to produce a solution of said substance, (b) producing a segmented stream which consists of alternating segments of said solution of the substance and of a transport medium, (c) introducing said segmented stream into the first end of a retention stretch, which retention stretch has a first end and a second end, so that said segmented stream passes from said first end to said second end of said retention stretch, and exits from the second end of the retention stretch, (d) cooling the retention stretch, to thereby bring about crystallization of the substance in the segments of solution, in the segmented stream, as said segmented stream passes through the retention stretch, and (e) separating the crystals of material from the segmented stream as it exits from the second end of the retention stretch.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: December 16, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Joerg Schiewe, Bernd Zierenberg
  • Patent number: 6660732
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 9, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashehar Betageri, Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, Thomas M. Kirrane, Monica H. Moriak, Neil Moss, Usha R. Patel, John R. Proudfoot, John R. Regan, Rajiv Sharma, Sanxing Sun, Alan D. Swinamer, Hidenori Takahashi
  • Patent number: 6656946
    Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases and their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
    Type: Grant
    Filed: August 22, 2001
    Date of Patent: December 2, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6656933
    Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.
    Type: Grant
    Filed: September 25, 2001
    Date of Patent: December 2, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Eugene R. Hickey
  • Patent number: 6638965
    Abstract: Indolinones of general formula I which are inhibitors of cell proliferation, particularly of tumour cells, and inhibitors of protein kinases. The following compounds are exemplary: (Z)-3-{1-[4-(N-(2-aminoethyl)-N-methylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, (Z)-3-{1-[4-(N-(2-dimethylaminoethyl)-N-phenylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, and (Z)-3-{1-[4-(4-methylpiperazinomethyl)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone.
    Type: Grant
    Filed: November 1, 2001
    Date of Patent: October 28, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Rainer Walter, Armin Heckel, Gerald Roth, Joerg Kley, Gisela Schnapp, Martin Lenter, Jacobus Van Meel, Walter Spevak, Ulrike Weyer-Czernilofsky
  • Patent number: 6620438
    Abstract: The present invention relates to novel pharmaceutical compositions based on anticholinergics and NK1-receptor antagonists, processes for preparing them and their use in the treatment of respiratory tract diseases.
    Type: Grant
    Filed: March 6, 2002
    Date of Patent: September 16, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Michel Pairet, Michael P. Pieper, Christopher J. M. Meade
  • Patent number: 6617329
    Abstract: Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof.
    Type: Grant
    Filed: August 23, 2001
    Date of Patent: September 9, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • 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: 6613879
    Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug having a cleavage site which is recognised by FAP&agr;, and said drug being cytotoxic or cytostatic under physiological conditions.
    Type: Grant
    Filed: April 21, 2000
    Date of Patent: September 2, 2003
    Assignees: Boehringer Ingelheim Pharma KG, Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Raymond A. Firestone, Wolfgang J. Rettig, Martin Lenter, Stefan Peters, Pilar Garin-Chesa, Juergen Mack, Dietmar Leipert, John E. Park, Leila A. Telan
  • 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: 6608054
    Abstract: The present invention relates to novel pharmaceutical compositions based on anticholinergics and endothelin antagonists, processes for preparing them and their use in the treatment of respiratory tract diseases.
    Type: Grant
    Filed: March 18, 2002
    Date of Patent: August 19, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Christopher J. M. Meade, Michel Pairet, Michael P. Pieper
  • 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: 6608055
    Abstract: The invention relates to crystalline anhydrous (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.022,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition, particularly for preparing a pharmaceutical composition with an anticholinergic activity.
    Type: Grant
    Filed: June 11, 2002
    Date of Patent: August 19, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Peter Sieger, Ulrike Werthmann
  • Patent number: 6603000
    Abstract: Disclosed is a novel method of producing heteroaryl amines of the formula(I): wherein X, Y and Z are described herein, the heteroarylamines are useful in the production of heteroaryl ureas which are key component in pharmaceutically active compounds possessing a heteroaryl urea group.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: August 5, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Nathan Yee, Suresh R. Kapadia, Jinhua J. Song
  • 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: 6593471
    Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
    Type: Grant
    Filed: December 6, 2001
    Date of Patent: July 15, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
  • Patent number: 6590099
    Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
    Type: Grant
    Filed: December 6, 2001
    Date of Patent: July 8, 2003
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
  • 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: 6583627
    Abstract: The invention relates to a process and an apparatus for detecting gas-permeable damaged points in an electrically non-conductive layer which can exist as a single layer or as a multi-layer composite with at least one conductive layer, which process can be used for containers or packaging of pharmacological preparations to determine their integrity after storage.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: June 24, 2003
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Carsten Henning, Matthias Hausmann, Juergen Wittekind, Andreas Kuehnel, Heinrich Kladders, Heiko Rengel
  • 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