Patents Represented by Attorney, Agent or Law Firm T. X. Witkowski
  • Patent number: 6682747
    Abstract: The present invention relates to orally administered suspensions of pharmaceutical active substances of the NSAID type, particularly the antirheumatic agent Meloxicam, which are stabilized by the addition of small amounts of highly dispersed silicon dioxide using high shear forces and adding small amounts of hydrophilic polymers to form a three-dimensional siloid structure, and a process for the preparation thereof.
    Type: Grant
    Filed: November 7, 2000
    Date of Patent: January 27, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Dietrich Türck, Veit Schmelmer
  • Patent number: 6660772
    Abstract: A method of treating urinary incontinence in a patient in need thereof, the method comprising administering to the patient an effective amount of 2-amino-1-(4-hydroxy-2-methanesulfonamidophenyl)ethanol or a pharmacologically acceptable salt thereof, and pharmaceutical compositions.
    Type: Grant
    Filed: January 30, 2002
    Date of Patent: December 9, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Pascale Pouzet, Franz Esser, Hisato Kitagawa, Naoki Ishiguro, Ikunobu Muramatsu
  • Patent number: 6653305
    Abstract: A compound of formula (I) wherein: Ra is a benzyl or 1-phenylethyl group or a phenyl group substituted by the groups R1 and R2, wherein: R1 is a hydrogen, fluorine, chlorine, or bromine atom, or a methyl, trifluoromethyl, cyano, or ethynyl group, and R2 is a hydrogen or fluorine atom; Rb is an R3O—CO—CH2—N—CH2—CH2—OH group optionally substituted at the methylene groups by 1 or 2 methyl or ethyl groups, wherein R3 is a hydrogen atom or a C1-4-alkyl group, a 2-oxomorpholin-4-yl group optionally substituted by 1 or 2 methyl or ethyl groups, or a N-[(1,3-dioxolan-2-yl)methyl]methylamino group; Rc is a hydrogen atom, or a methoxy, ethoxy, 2-methoxyethoxy, 2-ethoxyethoxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy, cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, cyclohexylmethoxy, tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy, tetrahydropyran-4-yloxy, tetrahydrofuranylmethoxy, or tetrahydropyranylmethoxy group; and n is 1, 2, or 3
    Type: Grant
    Filed: August 15, 2001
    Date of Patent: November 25, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
  • Patent number: 6576669
    Abstract: Medicaments and pharmaceutical kits comprising an LTB4 antagonist of formula (I) a tautomer thereof or a pharmaceutically acceptable salt thereof, and methods of treating or preventing cystic fibrosis, diseases caused by increased expression of mucin genes in the bronchial or gastrointestinal epithelium, or hyperplasia of goblet cells induced by toxins of products of pathogenic bacteria in a patient in need of such treatment, the method comprising administering to the patient a therapeutically effective amount of an LTB4 antagonist of formula (I).
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: June 10, 2003
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Christopher J. Montague Meade, Franz Birke, Hans Michael Jennewein, Birgit Jung
  • Patent number: 6403790
    Abstract: A process for preparing epinastine hydrochloride of formula (I) the process comprising: (a) suspending and dissolving an epinastine base of formula (II)  in water by the addition of aqueous hydrochloric acid at a pH of ≧7; (b) extracting the aqueous solution obtained from step (a) with an organic, water-immiscible solvent; (c) removing the organic, water-immiscible solvent from the aqueous solution obtained from step (b); and (d) adjusting the pH of the aqueous solution of step (c) to ≦6 using hydrochloric acid to precipitate the product of formula (I), and then drying the product.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: June 11, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventor: Rolf Dach
  • Patent number: 6369271
    Abstract: The invention relates to a process for large-scale industrial production of biphenyl-2-carboxylic acid derivatives (I) wherein R1 and R2 may have the meanings given in the specification and claims.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: April 9, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventor: Heinrich Schneider
  • Patent number: 6353007
    Abstract: 1-(4-Aminophenyl) indoles optionally substituted on the 2-,4-,5-,6- and 7-positions of the indole ring and on the amino group on the 4-position of the phenyl ring, which indoles inhibit IL-2 production in T-lymphocytes.
    Type: Grant
    Filed: July 13, 2000
    Date of Patent: March 5, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Rajiv Sharma
  • Patent number: 6346545
    Abstract: The present invention relates to urethanes and the thio and dithio analogues thereof of general formula wherein m, n, A, X, Y and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: March 24, 1999
    Date of Patent: February 12, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Roland Maier, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Peter Mueller, Gebhard Adelgoss, Gebhard Schilcher
  • Patent number: 6323207
    Abstract: Novel benzoylguanidine derivatives of general formula I useful for the treatment or reduction of tissue damage due to ischaemia.
    Type: Grant
    Filed: September 15, 1999
    Date of Patent: November 27, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Christian Eickmeier, Erich Buerger, Stefan Matthias Blech, Otto Roos
  • Patent number: 6314796
    Abstract: Apparatus and process for non-destructively testing a fluid-filled container for leaktightness, the process comprising: (a) subjecting the fluid-filled container to a vacuum or near vacuum environment; (b) utilizing electrical equipment to form an electrical discharge in the vacuum or near vacuum environment sufficient to stimulate spectral light emissions from volatile fluid-filled container contents present in the vacuum or near vacuum environment; (c) detecting the spectral light emissions from the volatile fluid-filled container contents produced in step (b); and (d) evaluating the spectral light emissions detected in step (c) to determine the amount of volatile fluid-filled container contents present in the vacuum or near vacuum environment by comparing: (i) the measured brightness level of the spectral light emissions obtained from step (c), to (ii) a base brightness level obtained by measuring the brightness level of the spectral emissions due to the presence of residual gas or air molecules in the
    Type: Grant
    Filed: August 2, 1999
    Date of Patent: November 13, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Juergen Wittekind, Gerhard Poss, Andreas Kuehnel
  • Patent number: 6313097
    Abstract: Compounds of the formula (I) wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compositions containing these compounds, and their use in the selective antagonization of calcitonin gene-related peptide (CGRP) and in the treatment or prophylaxis of migraine or cluster headaches, non-insulin-dependent diabetes mellitus, inflammation, allergic rhinitis, asthma, morphine tolerance, menopausal hot flashes, and diseases characterized by excessive vasodilatation and consequent reduction in blood-flow.
    Type: Grant
    Filed: March 10, 2000
    Date of Patent: November 6, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
  • Patent number: 6300342
    Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: October 9, 2001
    Assignee: Boehringer Ingelheim Pharm KG
    Inventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
  • Patent number: 6288277
    Abstract: The present invention relates to new phenylamine derivatives, processes for preparing them and their use as pharmaceutical compositions.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: September 11, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Hans Michael Jennewein, Christopher John Montague Meade
  • Patent number: 6281218
    Abstract: Compounds of general formula (I) wherein R1, R2, R3, and R4 denote hydrogen or hydroxy with the proviso that R1, R2, R3, and R4 cannot simultaneously represent hydrogen, processes for their preparation of the compounds of general formula (I), and their use as pharmaceuticals.
    Type: Grant
    Filed: August 8, 2000
    Date of Patent: August 28, 2001
    Assignee: Ingelheim Italia S.p.A.
    Inventors: Enzo Cereda, Maura Bignotti, Giovanni Battista Schiavi
  • Patent number: 6268389
    Abstract: The present invention relates to the use of &agr;lL-agonists for treating urinary incontinence.
    Type: Grant
    Filed: January 11, 1999
    Date of Patent: July 31, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Franz Esser, Helmut Staehle, Sven Luettke, Ikunobu Muramatsu, Hisato Kitagawa, Shuji Uchida
  • Patent number: 6255329
    Abstract: The present invention relates to the use of 2-amino-4,5,6,7-tetrahydro-6-n-propylamino-benzothiazole (pramipexole), the (+)- or (−)- enantiomer thereof, or one of the pharmacologically acceptable salts thereof, in conjunction with sertraline for the improved treatment of depression and depressive states.
    Type: Grant
    Filed: July 6, 1999
    Date of Patent: July 3, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventor: Jerzy Maj
  • 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: 6242466
    Abstract: Phenylamidines of the formula (I) wherein: R6 is a C5-12-alkyloxycarbonyl group, and R7 is a hydrogen atom, or a C1-8-alkyl, C4-7-cycloalkyl, phenyl-C1-4-alkyl, or R8—CO—OCHR9— group, wherein R8 is a C1-4-alkyl, C1-4-alkoxy, C3-7-cycloalkyl, or C4-7-cycloalkoxy group, and R9 is a hydrogen atom or a C1-4-alkyl group, or a tautomer or pharmaceutically acceptable salt thereof. These compounds inhibit cell aggregation and are useful for the treatment or prevention of thrombosis, inflammation, bone degradation, tumors and tumor metastasis.
    Type: Grant
    Filed: July 14, 1999
    Date of Patent: June 5, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Frank Himmelsbach, Brian Guth, Hans-Dieter Schubert
  • Patent number: 6235738
    Abstract: The invention relates to novel diphenyl-substituted heterocycles with 6-membered ring of general formula (I) in which A, X and the residues R1, R2, R3, R4 and R5 are as defined in the claims, processes for the preparation thereof and the use thereof as medicaments.
    Type: Grant
    Filed: April 12, 1999
    Date of Patent: May 22, 2001
    Assignees: Boehringer Ingelheim Pharma KG, Boehringer Ingelheim Italia S.p.A.
    Inventors: Michael Brenner, Rainer Palluk, Marion Wienrich, Thomas Weiser, Enzo Cereda, Maura Bignotti, Carlo Maria Pellegrini, Giovanni Battista Schiavi, Raffaele Cesana
  • Patent number: 6218575
    Abstract: An improved process for preparing adrenaline, or an addition salt thereof, on an industrial scale, with asymmetric hydrogenation as a key step and a special sequence of successive steps, using [Rh(COD)Cl]2 as catalyst and a chiral, bidentate phosphine ligand such as (2R,4R)-4-(dicyclohexylphosphino)-2-(diphenylphosphinomethyl)-N-methylaminocarbonylpyrrolidine as the catalyst system.
    Type: Grant
    Filed: July 26, 2000
    Date of Patent: April 17, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Franz Dietrich Klingler, Lienhard Wolter