Abstract: A system for testing systems which are in turn used to test the leaktightness of a hollow body is suggested. Instead of the hollow body, a test body (2) is placed in the system which generates a defined pressure increase in a measuring chamber (4) within a pre-determined time span. This defined pressure increase corresponds exactly to the pressure increase generated by a hollow body with a small amount of leakage, wherein the hollow body can still just be regarded as leaktight. The test body can be configured as a glass capillary which extends in a sealing manner between two chambers with different air pressure. Alternatively, the test body can comprise a material which can accept a defined amount of moisture from the ambient atmosphere during storage. A vacuum formed around the test body causes moisture to be withdrawn from the test body and at least partially evaporated in the vacuum, which again leads to an increase in pressure in the chamber.
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:
April 21, 2003
Date of Patent:
February 24, 2004
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Michel Pairet, Michael P. Pieper, Christopher J. M. Meade
Abstract: A process for making nevirapine, comprising the following steps:
(a) reacting a 2-halo-3-pyridinecarbonitrile of the formula
wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, with cyclopropylamine, to yield 2-(cyclopropylamino)-3-pyridinecarbonitrile;
(b) hydrolyzing the 2-(cyclopropylamino)-3-pyridinecarbonitrile to yield 2-(cyclopropylamino)-3-pyridine carboxylic acid;
(c) isolating the 2-(cyclopropylamino)-3-pyridine carboxylic acid from the reaction medium;
(e) treating the 2-(cyclopropylamino)-3-pyridine carboxylic acid with a chlorinating agent, to yield 2-(cyclopropylamino)-3-pyridinecarbonyl chloride;
(f) reacting the 2-(cyclopropylamino)-3-pyridine carbonyl chloride with a 2-halo-4-methyl-3-pyridinamine of the formula
wherein X is a fluorine, chlorine, bromine or iodine atom, preferably chlorine or bromine, to produce an N-(2-halo-4-methyl-3-pyridinyl)-2-(cyclopropylamino)-3-pyridinecarboxamide; and (g) cyclizing the N-
Type:
Grant
Filed:
June 5, 2003
Date of Patent:
January 20, 2004
Assignee:
Boehringer Ingelheim Chemicals, Inc.
Inventors:
Robert Frederick Boswell, Bernard Franklin Gupton, Young Sek Lo
Abstract: Compounds represented by formula I:
wherein R2 is H, halogen, NHNH2, (C1-4)alkyl, O(C1-6)alkyl, and haloalkyl; R4 is H or Me; R5 is H or (C1-4)alkyl; R11 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cycloalkyl, or (C3-7)cycloalkyl; and Q is naphthyl, fused phenyl(C4-7)cycloalkyl and fused phenyl-5, 6, or 7-membered saturated heterocycle having one to two heteroatom selected from O, N, or S, said Q being substituted with from 1 to 4 R12 substituents selected from: R13, (C1-6)alkyl, (C3-7)cycloalkyl, or (C2-6)alkenyl, said alkyl, cycloalkyl, or alkenyl being optionally substituted with R13; or a salt thereof. Compounds represented by formula I have inhibitory activity against Wild Type, single and double mutant strains of HIV.
Type:
Grant
Filed:
July 25, 2002
Date of Patent:
January 6, 2004
Assignee:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
William W. Ogilvie, Robert Déziel, Jeffrey O'Meara, Bruno Simoneau
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.
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 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: 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 a graft animal model for propagating papilloma virus and for evaluating and testing candidate therapeutic agents against papilloma virus. The animal model comprises, a recipient animal engrafted with injured skin graft infected with a host-specific papilloma virus (PV). The grafted skin, having demonstrable papillomas supports the propagation of its host-specific PV. The invention particularly relates to a xenograft animal model for hosting and propagating human papillomavirus (HPV), thereby providing a means for generating infectious and passaging HPV suspensions, and for screening candidate therapeutic agents against HPV. The invention additionally relates to a novel method for generating the xenograft human animal model.
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
Abstract: Compaction of mexiletine hydrochloride crystals is described, which provides a powder suitable for use in capsules without use of organic solvents.
Type:
Grant
Filed:
October 25, 2001
Date of Patent:
May 13, 2003
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
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: A microemulsion of pyranone protease inhibitor compounds that is substantially free of alcohol and propylene glycol comprising a pyranone protease inhibitor, one or more pharmaceutically acceptable surfactants, and a polyethylene glycol solvent having a mean molecular weight of greater than 300 but lower than 600, and a lipophilic component comprising medium chain mono- and di-glycerides, and optionally a basic amine.
Type:
Grant
Filed:
October 30, 2001
Date of Patent:
April 29, 2003
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Substituted indolinones of general formula
having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are:
3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and
3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.
Type:
Grant
Filed:
October 3, 2001
Date of Patent:
April 8, 2003
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Armin Heckel, Rainer Walter, Wolfgang Grell, Jacobus C. A. Van Meel, Norbert Redemann
Abstract: This invention relates to chimeric nucleic acids and to the therapeutic induction of apoptosis in activated inflammatory cells, or cells at a site of inflammation, by introducing into those cells the chimeric nucleic acid. The chimeric nucleic acid having at least one TNF&agr; promoter enhancer attached to a functional copy of a TNF&agr; promoter and further attached to at least one copy of an apoptosis-inducing gene, which is further attached to a 3′UTR. The apoptosis-inducing gene is Granzyme B. The invention also relates to methods of making and using self-regulated apoptosis chimeric nucleic acids and pharmaceutical compositions containing them for treating inflammatory diseases.
Type:
Grant
Filed:
January 12, 1999
Date of Patent:
March 25, 2003
Assignee:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Revati J. Tatake, Steven D. Marlin, Randall W. Barton
Abstract: A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules.
Type:
Grant
Filed:
June 12, 2002
Date of Patent:
June 3, 2003
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Terence A. Kelly, Barbara Jean Bormann, Leah Lynn Frye, Jiang-Ping Wu