Abstract: An enantiomeric-resolving process for obtaining (1R,2S)-1-amino-2-vinylcyclopropyl carboxylic acid methyl ester by use of an esterase, and especially Alcalase®, is disclosed.
Abstract: This invention relates to compounds of formula (1):
wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.
Type:
Grant
Filed:
November 12, 1999
Date of Patent:
July 31, 2001
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rajashekhar Betageri, Pierre L. Beaulieu, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, Usha Patel, John R. Proudfoot, Mario Cardozo
Abstract: An aqueous pharmaceutical suspension consisting essentially of nevirapine hemihydrate having a particle size between about 1 and 150 microns in diameter.
Type:
Grant
Filed:
March 2, 2000
Date of Patent:
July 3, 2001
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
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 invention provides a process for coating a branded pharmaceutical dosage form for the purpose of covering any embossed or printed matter or any colored coating by the application of an amount of a sugar based coating which is sufficient to obscure any identifying indicia without compromising the stability or releasability of the drug that is contained in the dosage form.
Type:
Grant
Filed:
January 28, 2000
Date of Patent:
July 3, 2001
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: The invention relates to new diphenyl-substituted 5-ring heterocycles of general formula (I)
wherein A, X and the groups R1, R2, R3, R4 and R5 are defined as in the claims, processes for preparing them and their use as pharmaceutical compositions.
Type:
Grant
Filed:
April 13, 1999
Date of Patent:
July 3, 2001
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Michael Brenner, Wolf-Dietrich Bechtel, Rainer Palluk, Marion Wienrich, Thomas Weiser, Enzo Cereda, Maura Bignotti, Carlo Maria Pellegrini
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: The present invention relates to N-(5-phenyl-tetrahydrofuranyl)methyl- and N-(6-phenyl-tetrahydropyranyl)methyl-substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocin-10-ols of general formula 1, processes for preparing such compounds, pharmaceutical compositions containing such compounds and methods for using such compounds for the treatment of various diseases caused by a functional disorder resulting from overstimulation.
Type:
Grant
Filed:
February 22, 2000
Date of Patent:
June 12, 2001
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Matthias Grauert, Hans Briem, Matthias Hoffmann, Adrian Carter, Thomas Weiser, Wolf-Dietrich Bechtel, Rainer Palluk
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: A compound of formula I
wherein R1 is hydrogen, methyl, ethyl, methoxy or methylthio; R2 and R3 each independently is hydrogen or lower alkyl; R4 is hydrogen, lower alkyl, methoxy, ethoxy or benzyloxy; R5 is lower alkyl, lower cycloalkyl, (CH2)mC(O)OR6 wherein m is the integer 1 or 2 and R6 is lower alkyl, phenyl optionally substituted; optionally Het or Het(lower alkyl); or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with C(O)O-benzyl or with phenyl optionally substituted with C(O)OR7 wherein R7 is lower alkyl or (lower alkyl)phenyl; and Z is lower alkyl or optionally substituted phenyl or Het; with the proviso that when Z is (CH2)p-(Het), then R2 and R3 each is hydrogen; or a therapeutically acceptable acid addition salt thereof which compound is useful in the treatment of HCMV infections.
Type:
Grant
Filed:
October 6, 1998
Date of Patent:
June 5, 2001
Assignee:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
Christiane Yoakim, Robert Déziel, Jeffrey O'Meara, William W. Ogilvie
Abstract: Disclosed are novel aromatic polycyclo heterocyclic compounds of the formula(I) wherein A, B, C, G, Ar, L, Q and X are described herein. The compounds are useful in pharmaceutical compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes of making such compounds.
Abstract: A compound of formula 1:
wherein Y is S or O;
R1 is C1-6 alkyl; (C0-6 alkyl)aryl; (C0-6 alkyl)Het; or
R1 is an amino acid analog or dipeptide analog of the formula:
wherein R2 is H, C1-10 alkyl; or an amide or ester group;
A is C6-10 aryl, Het or CH—R3 wherein R3 is C1-6 alkyl or (C0-4 alkyl)aryl; and
Z is H, C1-6 alkyl, or an acyl;
R4 is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; and
R5 is alkyl, cycloalkyl, carboxyl group; an aryl;
Het or Het(lower alkyl); or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with phenyl or C(O)OCH2-phenyl, said phenyl ring optionally mono- or
di-substituted with among others C(O)OR7 wherein R7 is lower alkyl or phenyl(lower alkyl); or a therapeutically acceptable acid addition salt thereof which compounds are useful in the treatment of HCMV infections.
Type:
Grant
Filed:
October 6, 1998
Date of Patent:
May 29, 2001
Assignee:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
Eric Malenfant, Jeffrey O'Meara, Robert Déziel, William W. Ogilvie
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: Disclosed are compounds which are neurokinin (tachykinin)-antagonists, useful for the treatment or prevention of inflammatory and allergic disease.
Type:
Grant
Filed:
December 1, 1999
Date of Patent:
May 15, 2001
Assignee:
Boehringer Ingelheim KG
Inventors:
Franz Esser, Gerd Schnorrenberg, Hans-Peter Ignatow, Günther Giesler, Birgit Jung, Georg Speck
Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
Type:
Grant
Filed:
December 14, 1999
Date of Patent:
May 8, 2001
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
John R. Regan, Pier F. Cirillo, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
Abstract: Hard shelled capsules and dry, powdered pharmaceutical formulations are treated with supercritical fluids to remove impurities such as mold lubricants and moisture.
Type:
Grant
Filed:
September 21, 1998
Date of Patent:
May 8, 2001
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: A compound of formula I:
wherein R1 is hydrogen, methyl, ethyl, methoxy or methylthio; R2 and R3 each independently is hydrogen or C1-3 alkyl; R4 is hydrogen, lower alkyl, methoxy, ethoxy, or benzyloxy; R5 is lower alkyl, lower cycloalkyl, (CH2)mC(O)OR6 wherein m is the integer 1 or 2 and R6 is lower alkyl, phenyl optionally substituted with C(O)OR7 wherein R7 is lower alkyl or phenyl (lower alkyl); or R6 is Het or Het(lower alkyl; or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with benzyloxycarbonyl or with phenyl optionally substituted among other group with C(O)OR7 wherein R7 is lower alkyl or (lower alkyl)phenyl; X is selected from the group consisting of O, S, SO, SO2, NR8, wherein R8 is H or lower alkyl; and
Y is C1-10 non-cyclic or cyclic alkyl; [(CH2)0-1]-phenyl, said phenyl ring optionally substituted; Het or Het(lower alkyl); or when X is NR8, wherein R8 is lower alkyl and Y is lower alkyl or
Type:
Grant
Filed:
October 6, 1998
Date of Patent:
April 3, 2001
Assignee:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
Christiane Yoakim, Robert Déziel, Stephen Kawai, William W. Ogilvie, Jeffrey O'Meara, Catherine Chabot
Abstract: Quinoxazolines having antithrombotic activity. Exemplary of those disclosed are:
4-{[6-(N-carboxymethyl-quinolin-8-yl-sulphonylamino)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine,
4-{[6-(1-(N-cyclopentyl-carboxymethylcarbonylamino)-cyclo-propyl)-1-methyl-2-oxo-1,2-dihydroquinoxalin-3-yl]-methyl}-benzamidine, and
4-{[7-(N-carboxymethylaminocarbonyl-ethylamino)-4-methyl-quinolin-2-yl]-oxo}-benzamidine.
Type:
Grant
Filed:
March 29, 1999
Date of Patent:
March 13, 2001
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Uwe Ries, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen