Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.
Abstract: Disclosed herein are methods for measuring the particle size distribution of a pharmaceutical aerosol, including methods utilizing laser diffraction.
Type:
Grant
Filed:
October 23, 2006
Date of Patent:
August 19, 2008
Inventors:
Herbert Wachtel, Jochen Ziegler, Dieter Hochrainer, Georg Boeck, Hubert Hoelz, Christian Scheffler, Christoph Kreher
Abstract: Pharmaceutical preparations for producing powder aerosols using propellant gases which use TG 227, and possibly also TG 11, TG 12, TGH 114, propane, butane, pentane or DME.
Abstract: A method for producing a refolded, inactive form of recombinantly produced NS2/3 protease which comprises the steps of: a) purifying the protease from inclusion bodies in the presence of a chaotropic agent; and b) refolding the purified protease by contacting it with a reducing agent and lauryldiethylamine oxide (LDAO) in the presence of reduced concentration of chaotropic agent or polar additive. The invention further comprises a method for activating this refolded inactive NS2/3 protease by adding an activation detergent. This method produces large amounts of the active NS2/3 protease to allow small molecules and ligands to be screened as potential inhibitors of NS2/3 protease, which may be useful as therapeutic agents against HCV.
Type:
Grant
Filed:
December 14, 2001
Date of Patent:
November 9, 2004
Assignee:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
Diane Thibeault, Daniel Lamarre, Roger Maurice, Louise Pilote, Armin Pause
Abstract: Compounds represented by formula I:
wherein
R2 is selected from the group consisting of H, (C1-4)alkyl, halo, haloalkyl, OH, (C1-6)alkoxy, NH(C1-4alkyl) or N(C1-4alkyl)2; R4 is H or Me; R5 is H or Me; R11 is H, (C1-4)alkyl, (C3-4)cycloalkyl and (C1-4)alkyl-(C3-4)cycloalkyl; A is a connecting chain of (C1-3)alkyl; B is O or S; n is 0 or 1; wherein when n is 0:
Ring C is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted;
and E is CONR12R13; CONHNR14R15; NR16COR17; NR18SO2(C1-6)alkyl; SO2NR19R20; or SO2R21; or
when n is 1: Ring C is as defined above and E is a single bond or a connecting group; and
Ring D is 6- or 10-membered aryl or 5- or 6-membered heterocycle having from 1 to 4 heteroatoms selected from the group consisting of O, N, and S, said aryl and said heterocycle being optionally substituted with from 1 to 5 substituents;
or a salt or
Type:
Grant
Filed:
May 6, 2003
Date of Patent:
October 19, 2004
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Bruno Simoneau, Serge Landry, Eric Malenfant, Julie Naud, Jeffrey O'Meara, Bounkham Thavonekham, Christiane Yoakim
Abstract: A dietary supplement consisting essentially of a combination of Ginseng and Ginkgo to improve the speed of memory and memory quality in normal, healthy subjects and to prevent deterioration of the speed of memory in people with decreased cognitive functions, and to counteract cognitive fatigue.
Abstract: The present invention relates to substances which modulate receptors involved in inflammatory processes and whose modulated functions positively influence inflammatory diseases.
Type:
Grant
Filed:
August 31, 2001
Date of Patent:
August 10, 2004
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Birgit Jung, Norbert Kraut, Stefan Mueller, Barbara Kistler, Peter Seither, Karsten Quast, Andreas Weith
Abstract: Indolinones of the formula
having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are:
(a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone,
(b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and
(c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
Type:
Grant
Filed:
October 3, 2000
Date of Patent:
July 13, 2004
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Gerald Juergen Roth, Armin Heckel, Rainer Walter, Jacobus Van Meel, Norbert Redemann, Ulrike Tontsch-Grunt, Walter Spevak, Frank Hilberg
Abstract: A process and novel intermediates for making compounds of the formula I:
wherein:
R2 is selected from the group consisting of H, F, Cl, C1-4 alkyl, C3-4 cycloalkyl and CF3;
R4 is H or Me;
R5 is H, Me or Et, with the proviso that R4 and R5 are not both Me, and if R4 is Me then R5 cannot be Et;
R11 is Me, Et, cyclopropyl, propyl, isopropyl, or cyclobutyl; and
Q is selected from the group consisting of:
Type:
Grant
Filed:
June 19, 2003
Date of Patent:
July 6, 2004
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Carl A. Busacca, Magnus C. Eriksson, Ji-Young Kim
Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.
Type:
Grant
Filed:
May 29, 2003
Date of Patent:
June 8, 2004
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Rolf Banholzer, Gisela Bodenbach, Andreas Mathes, Helmut Meissner, Peter Specht
Abstract: Compounds of the formula
having an inhibitory effect on signal transduction mediated by tyrosine kinases, and the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract.
Type:
Grant
Filed:
August 22, 2001
Date of Patent:
May 25, 2004
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Frank Himmelsbach, Elke Langkopf, Birgit Jung, Stefan Blech, Flavio Solca
Abstract: The present invention relates to polymers characterized by novel silicon linkers based on the carbamyl piperazine moiety, methods of preparing these polymers and their use in the solid phase synthesis of compounds or libraries of compounds embracing a phenyl ring in their structure.
Type:
Grant
Filed:
January 28, 2002
Date of Patent:
May 25, 2004
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Enzo Cereda, Carlo Maria Pellegrini, Monica Quai, Walter Barbaglia
Abstract: The invention relates to a crystalline sodium salt of 4′-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid (INN: telmisartan), processes for preparing it and the use thereof for preparing a pharmaceutical composition.
Abstract: Carboxylic acid amides of general formula
which inhibit telomerase and are useful for treating tumor diseases such as carcinomas, sarcomas and leukaemias. Exemplary compounds are:
(1) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-phenyl)-amide, and,
(2) trans-3-(naphth-2-yl)-but-2-enoic acid-N-(2-carboxy-4,5-dimethoxy-phenyl)-amide.
Type:
Grant
Filed:
January 3, 2002
Date of Patent:
April 27, 2004
Assignee:
Boehringer Ingelheim Pharma KG
Inventors:
Norbert Hauel, Henning Priepke, Klaus Damm, Andreas Schnapp
Abstract: A compound of formula I:
wherein
A is a connecting chain of (C1-3) alkyl; B is O or S; R1 is H, (C1-6) alkyl, halo, CF3, or OR1a wherein R1a is H or (C1-6)alkyl; R2 is H or Me; R3 is H or Me; R4 is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl;
W is selected from
wherein,
a) one of Y is SO2 and the other Y is NR5, provided that both are not the same, wherein R5 is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR5o, COOR5p or CONR5pPR5q; and each R8 is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR8aR8b wherein R8a and R8b is H, or alkyl and J is CH2; or J is CR8aR8b and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR8aR8b or J is C(O) and E is CR8aR8b and the dotted line represents a single bond; or d) E and J are CR8aR8b and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.
Type:
Grant
Filed:
March 13, 2002
Date of Patent:
April 6, 2004
Assignee:
Boehringer Ingelheim (Canada) Ltd.
Inventors:
William W. Ogilvie, Robert Déziel, Julie Naud, Jeffrey O'Meara, Dale R. Cameron
Abstract: A unique HCV RNA molecule is provided having an enhanced efficiency of establishing cell culture replication. Novel adaptive mutations have been identified within the HCV non-structural region that improves the efficiency of establishing persistently replicating HCV RNA in cell culture. This self-replicating polynucleotide molecule contains, contrary to all previous reports, a 5′-NTR that can be either an A as an alternative to the G already disclosed and therefore provides an alternative to existing systems comprising a self-replicating HCV RNA molecule. The G→A mutation gives rise to HCV RNA molecules that, in conjunction with mutations in the HCV non-structural region, such as the G(2042)C/R mutations, possess greater efficiency of transduction and/or replication. These RNA molecules when transfected in a cell line are useful for evaluating potential inhibitors of HCV replication.
Abstract: The invention relates to a process for preparing reabsorbable polyesters by bulk polymerisation, wherein the reaction components are melted and homogenised in a stirred reactor, the reaction mixture is then transferred into a number of smaller-volume containers, the reaction mixture is polymerised in these containers and the polyester obtained is isolated by removing it from the containers, and the use of the reabsorbable polyesters thus produced for preparing reabsorbable implants.
Type:
Grant
Filed:
January 9, 2003
Date of Patent:
March 16, 2004
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Berthold Buchholz, Matthias Schellhorn, Andreas Weber
Abstract: This invention relates to Equine Herpes Viruses (EHV) wherein the protein gM is essentially absent or modified and non-functional with respect to its immunomodulatory capacity. Further aspects of the invention relate to nucleic acids coding said viruses, pharmaceutical compositions comprising these viruses or nucleic acids and uses thereof. The invention also relates to methods for improving the immune response induced by an EHV vaccine against wild type EHV infections, methods for the prophylaxis and treatment of EHV infections and methods for distinguishing wild type EHV infected animals from animals treated with EHV's according to the invention.
Type:
Grant
Filed:
February 16, 2001
Date of Patent:
March 9, 2004
Assignee:
Boehringer Ingelheim Vetmedica GmbH
Inventors:
Knut Elbers, Nikolaus Osterrieder, Christian Seyboldt