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
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
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.
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
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
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
Abstract: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.
Abstract: The present invention relates to substituted indolinones of general formula
wherein
R1 to R5, and X are defined as in claim 1, the isomers thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, particularly an inhibitory effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells, pharmaceutical compositions containing these (compounds, their use and processes for preparing them.
Type:
Grant
Filed:
April 6, 1999
Date of Patent:
January 2, 2001
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Armin Heckel, Rainer Walter, Wolfgang Grell, Jacobus C. A. van Meel, Norbert Redemann
Abstract: The present invention relates to a phosphoric acid salt of N-methyl-o-phenylenediamine and processes for making the same. In preferred embodiments of the invention, the phosphoric acid salt of N-methyl-o-phenylenediamine has the general Formula I
wherein n is a number between 0.5 and 1.0, between 0.7 and 0.8, or between 0.75 and 0.78. The process for making the phosphoric acid salt of N-methyl-o-phenylenediamine comprises (a) dissolving the N-methyl-o-phenylenediamine in a first solvent, and (b) reacting the dissolved N-methyl-o-phenylenediamine with crystalline phosphoric acid or phosphoric acid dissolved in a second solvent.
Abstract: An otoscope having (a) a gripping body; (b) a hollow ear speculum, having an outer end adapted to be placed in the ear canal of a patient, said ear speculum being connected to a top end of the gripping body; (c) a viewing port connected to the top end of said gripping body to provide a line of sight through the ear speculum; (d) a light source which is directed through said ear speculum; and (e) a dispenser which is integral with said otoscope for ejecting medicament through the ear speculum.
Type:
Grant
Filed:
March 1, 1999
Date of Patent:
November 28, 2000
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: The present invention relates to a formoterol active substance concentrate suitable for storage, in the form of a solution or suspension for use in inhalers for inhalation or nasal therapy.
Abstract: The invention relates to new amino acid derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, wherein group R.sup.5 is ##STR1## and R.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, Z, t and u have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.
Type:
Grant
Filed:
July 8, 1998
Date of Patent:
November 14, 2000
Assignee:
Boehringer Ingelheim KG
Inventors:
Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Birgit Jung, Erich Burger
Abstract: The present invention relates to new processes for preparing norbenzomorphan, the central intermediate step in the preparation of pharmaceutically useful benzomorphan derivatives of general formula 1 ##STR1## especially (-)-(1R,5S,2"R)-3'-hydroxy-2-(2-methoxypropyl)-5,9,9-trimethyl-6,7-benzomo rphan or [(-)-(2R, 6S,2'R)-3-(2-methoxypropyl)-6,11,11-trimethyl-1,2,3,4,5,6-hexahydro-2,6-me thano-benzo[.alpha.]oxacin-9-ol] (BIII 277).
Type:
Grant
Filed:
November 18, 1999
Date of Patent:
October 24, 2000
Assignee:
Boehringer Ingelheim KG
Inventors:
Matthias Grauert, Herbert Merz, Hanfried Baltes
Abstract: The invention refers to a transcorneal system for the actively controlled transcorneal delivery of a medicament into a subject comprising an active substance reservoir and a device provided with a plurality of micro-pins or micro-blades adapted in use to penetrate the stratum corneum of the subject and connected with reservoir via a liquid conveying connection and thereby allow active substance to pass from the reservoir through capillary openings of the micro-pins or along the micro-blades into the subject.
Abstract: Novel disubstituted bicyclic heterocycles, of which the following are exemplary:(a) 1-methyl-2-[(4-amidinophenyl)-oxymethyl]-5-[N-(hydroxycarbonylmethyl)-quin oline-8-sulphonylamino]-benzimidazole,(b) 1-methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(N-(hydroxycarbonylmethyl)-ami nocarbonylmethyl)-quinoline-8-sulphonylamino]-benzimidazole,(c) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-benzimidazole and(d) 1-methyl-2-[N-(4-amidinophenyl)-aminomethyl]-5-[N-(hydroxycarbonylmethyl)- quinoline-8-sulphonylamino]-indole.These are useful for the treatment of thrombotic disease.
Type:
Grant
Filed:
July 22, 1999
Date of Patent:
September 19, 2000
Assignee:
Boehringer Ingelheim KG
Inventors:
Norbert Hauel, Uwe Ries, Henning Priepke, Gerhard Mihm, Wolfgang Wienen, Jean Marie Stassen, Klaus Binder, Rainer Zimmermann
Abstract: Phenylacetic acid benzylamides having the following general structure
wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.
Type:
Grant
Filed:
October 7, 1997
Date of Patent:
January 30, 2001
Assignee:
Boehringer Ingelheim KG
Inventors:
Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht