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
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.
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
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
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
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
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
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
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.
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
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.
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
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
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
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
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.
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