Patents Represented by Attorney Michael Morris
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Patent number: 7439258Abstract: A compound of the formula I: wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl,Type: GrantFiled: May 21, 2004Date of Patent: October 21, 2008Assignee: Boehringer Ingelheim (Canada) LtdInventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Patent number: 7386398Abstract: The HCV NS5B polymerase, when complexed with certain inhibitors, adopts a conformation in which the finger loop region defined by amino acid residues 18 to 35 is displaced to expose a binding pocket defined generally by amino acid residues 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 496, 500 and 503. This newly exposed binding pocket defines a novel target in the search of further chemical entities which are capable of binding to HCV NS5B and modulating, or preferably inhibiting, the polymerase activity of HCV NS5B.Type: GrantFiled: May 7, 2004Date of Patent: June 10, 2008Assignee: Boehringer Ingelheim International GmbHInventors: René Coulombe, Pierre Beaulieu, Eric Jolicoeur, George Kukolj, Steven Laplante, Marc-André Poupart
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Patent number: 7375090Abstract: The present invention relates to glucopyranosyloxy-pyrazoles of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on sodium-dependent glucose cotransporter SGLT, the use thereof for the treatment of diseases, particularly metabolic disorders such as diabetes, and the preparation thereof.Type: GrantFiled: August 24, 2004Date of Patent: May 20, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Peter Eickelmann, Leo Thomas, Edward Leon Barsoumian
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Patent number: 7371732Abstract: The present invention relates to glucopyranosyloxy-substituted aromatic groups of general formula wherein R1 to R6 and R7a, R7b, R7c are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on the sodium-dependent glucose cotransporter SGLT2, the use thereof for the treatment of diseases, particularly metabolic disorders such as diabetes, and the preparation thereof.Type: GrantFiled: December 21, 2004Date of Patent: May 13, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Peter Eickelmann, Frank Himmelsbach, Edward Leon Barsoumian
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Patent number: 7371753Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.Type: GrantFiled: August 25, 2005Date of Patent: May 13, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Harald Engelhardt, Andreas Schoop, Martin Steegmaier, Matthias Hoffmann, Matthias Grauert
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Patent number: 7335657Abstract: Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: June 27, 2006Date of Patent: February 26, 2008Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Matthew Russell Netherton, Kevin Chungeng Qian, Mark Stephen Ralph, Lifen Wu, Zhaoming Xiong, Ronald A. Aungst, Jr.
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Patent number: 7332491Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: February 19, 2008Assignee: Boehringer Ingelheim International, GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Christian Eickmeier, Gisela Schnapp, Norbert Redemann, Flavio Solca, Jens Juergen Quant
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Patent number: 7332614Abstract: The present invention provides a process for making a compound of general formula I: wherein: R=H or C1-8alkyl X=C3-C8cycloalkyl, C3-C8aryl or C3-C8alkyl; Y=heteroaryl or aryl; Z=H, HO2C—, C1-8alkyl O2C—, C1-6alkyl HNC(O)—, and as described herein.Type: GrantFiled: March 7, 2005Date of Patent: February 19, 2008Assignee: Boehringer Ingelheim International, GmbHInventors: Ahmad Khodabocus, Guisheng Li, Zhi-Hui Lu, Frank Roschangar, Chris Hugh Senanayake, Ming Shen
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Patent number: 7326719Abstract: This invention relates to peptidyl compounds of the formulas (I) and (II) active as cathepsin S, a cysteine protease, inhibitors. The compounds are selective, reversible inhibitors of the cathepsin S are therefore useful in the treatment of autoimmune and other diseases.Type: GrantFiled: March 1, 2004Date of Patent: February 5, 2008Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Eugene R. Hickey, Weimin Liu, Sanxing Sun, Yancey David Ward, Erick Richard Roush Young
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Patent number: 7322810Abstract: Method for identifying compounds useful for the therapy of cancers in which the activity of Myc is causally involved. The method is based on measuring the activity of the E3 ligase HectH9, which is required for ubiquitination and activation of Myc.Type: GrantFiled: May 13, 2005Date of Patent: January 29, 2008Assignee: Boehringer Ingelheim International GmbHInventor: Martin Eilers
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Patent number: 7323470Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: April 17, 2006Date of Patent: January 29, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Marc-André Poupart, Pierre Louis Beaulieu, Jean Rancourt
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Patent number: 7323567Abstract: Compounds or enantiomers of formula (I) or a salt thereof: wherein R1, R2, R3, R4 and R5 are as defined herein, are useful for the manufacture of a medicament for the treatment or prevention of respiratory syncytial virus infection in a mammal.Type: GrantFiled: October 28, 2004Date of Patent: January 29, 2008Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Bruno Simoneau, Josee Bordeleau, Gulrez Fazal, Serge Landry, Steve Mason, Jean Rancourt
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Patent number: 7312030Abstract: A method for determining the capability of an arterivirus to replicate in a permissive cell is disclosed. The method includes determining an amino acid at a position that corresponds to an amino acid of a protein of a porcine reproductive and respiratory syndrome virus. The invention also discloses a method for determining the capability of an arterivirus to replicate in a green monkey cell line. The invention further discloses a method for producing arterivirus in a green monkey cell line wherein the virulence of the arterivirus is maintained and the virus yield is increased. Methods for determining the attenuation of an arterivirus and for attenuating the virulence of the arterivirus by changing amino acids are further disclosed.Type: GrantFiled: April 4, 2003Date of Patent: December 25, 2007Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Petrus Antonius van Rijn, Johanna Jacoba M. Meulenberg
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Patent number: 7312211Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.Type: GrantFiled: August 26, 2004Date of Patent: December 25, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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Patent number: 7294457Abstract: A method for identifying compounds binding to HCV polymerase comprising the steps of: contacting said HCV polymerase or an analog thereof with a probe formula I: wherein A is O, S, N, NR1, or CR1, wherein R1 is defined herein; ----- represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, wherein R3 is defined herein; with the proviso that, when A is not N, then one of A or B is either CR1 or CR3, K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; R5 is C(Y1)Z wherein Y1 is O or S; and Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herType: GrantFiled: August 2, 2002Date of Patent: November 13, 2007Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: George Kukolj, Pierre Louis Beaulieu, Ginette McKercher
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Patent number: 7291733Abstract: Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents.Type: GrantFiled: October 7, 2004Date of Patent: November 6, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Charles Lawrence Cywin, Roman Wolfgang Fleck, Eugene Richard Hickey, Weimin Liu, Tina Marie Morwick, John Robert Proudfoot, Denice M. Spero
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Patent number: 7285545Abstract: Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 29, 2005Date of Patent: October 23, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Daniel R. Goldberg, Ming-Hong Hao, Zhaoming Xiong, Ronald A. Aungst, Amy L. Davis
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Patent number: 7279475Abstract: Disclosed are compounds of formula(I): wherein R1, R2, W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: September 14, 2004Date of Patent: October 9, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, Victor Kamhi, Neil Moss, Paul S Riska, Christopher Pargellis
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Patent number: 7276491Abstract: Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors.Type: GrantFiled: December 10, 2004Date of Patent: October 2, 2007Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Chester C. Wood, Thomas van der Poll
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Patent number: RE40525Abstract: A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted with C1-6 alkyl; C1-6 alkoxy; C1-6 alkanoyl; hydroxy; hydroxyalkyl; halo; haloalkyl; nitro; cyano; cyanoalkyl; amino optionally substituted with C1-6 alkyl; amido; or (lower alkyl)amide; or B is an acyl derivative of formula R4—C(O)—; a carboxyl derivative of formula R4—O—C(O)—; an amide derivative of formula R4—N(R5)—C(O)—; a thioamide derivative of formula R4—N(R5)—C(S)—; or a sulfonyl of formula R4—SO2; R5 is H or C1-6 alkyl; and Y is H or C1-6 alkyl; R3 is C1-8 alkyl, C3-7 cycloalkyl, or C4-10 alkylcycloalkyl, all optionally substituted with hydroxy, C1-6 alkoxy, C1-6 thioalkyl, amido, (lower alkyl)amido, C6 or C10 aryl, or C7-16 aralkyl; R2 is C2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl or C4-10 (alkylcycloalkyl), all of which being optionally mono-, di- or tri-Type: GrantFiled: September 30, 2005Date of Patent: September 30, 2008Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Anne-Marie Faucher, Elise Ghiro, Nathalie Goudreau, Teddy Halmos, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Dominik M. Wernic