Patents Represented by Attorney, Agent or Law Firm Philip I. Datlow
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Patent number: 6534523Abstract: Racemates, diastereoisomers and optical isomers 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 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 of formula R4—O—C(O)—; an amide of formula R4—N(R5)—C(O)—; a thioamide 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 CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a saturated or unsaturated C3-7 cycloalkyl oType: GrantFiled: March 5, 2002Date of Patent: March 18, 2003Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale R. Cameron, Elise Ghiro, Nathalie Goudreau, Marc-Andre Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic
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Patent number: 6528491Abstract: The present invention relates to new pyranoside derivatives of general formula I, processes for preparing them as well as their use as medicaments:Type: GrantFiled: October 23, 2001Date of Patent: March 4, 2003Assignee: Boehringer Ingelheim Pharma KGInventors: Ralf Anderskewitz, Kurt Schromm, Franz Birke, Hans Michael Jennewein
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Patent number: 6506769Abstract: Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases associated with such kinases, for example, diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are processes for preparing these compounds, novel intermediates useful in these processes and compositions comprising compounds of the formula (I).Type: GrantFiled: August 2, 2001Date of Patent: January 14, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Roger John Snow, Mario Cardozo, Daniel Goldberg, Abdelhakim Hammach, Tina Morwick, Neil Moss, Usha R. Patel, Anthony S. Prokopowicz, III, Hidenori Takahashi, Matt Aaron Tschantz, Xiao-Jun Wang
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Patent number: 6506900Abstract: The invention relates to a new process for preparing a scopine ester useful as an intermediate in preparing (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4] nonane-bromide.Type: GrantFiled: August 19, 2002Date of Patent: January 14, 2003Assignee: Boehringer Ingelheim Pharma AGInventors: Rolf Banholzer, Manfred Graulich, Sven Luettke, Andreas Mathes, Helmut Meissner, Peter Specht, Wolfgang Broeder
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Patent number: 6503535Abstract: 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: GrantFiled: January 4, 2001Date of Patent: January 7, 2003Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Michael L. Cappola
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Patent number: 6489359Abstract: The present invention relates to new sulphoxybenzamides of general formula I, processes for preparing them as well as their use as medicaments.Type: GrantFiled: October 23, 2001Date of Patent: December 3, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Ralf Anderskewitz, Kurt Schromm, Franz Birke, Hans Michael Jennewein
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Patent number: 6486321Abstract: The invention relates to a new process for preparing (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4] nonane-bromide.Type: GrantFiled: December 19, 2001Date of Patent: November 26, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Rolf Banholzer, Manfred Graulich, Sven Luettke, Andreas Mathes, Helmut Meissner, Peter Specht, Wolfgang Broeder
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Patent number: 6479508Abstract: 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,Type: GrantFiled: November 27, 2001Date of Patent: November 12, 2002Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Patent number: 6476047Abstract: The invention relates to the use of anellated dihydropyridines according to the following formula I, and the salts thereof with physiologically acceptable acids, for the treatment of chronic pain, wherein A is benzo or thieno and Z, R1, R2, R3, R4, R5 and R6 are defined as in the specification: The inventions also relates to novel compounds of formula I and pharmaceutical compositions thereof.Type: GrantFiled: July 19, 2001Date of Patent: November 5, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Dietrich Arndts, Walter Loesel, Wolfram Gaida, Klaus Klinder, Stefan Matthias Blech, Henning Draheim
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Patent number: 6465483Abstract: A compound of formula I wherein A denotes a benzo, indolo or thieno group; R1 denotes thienyl or the group wherein R7, R8 and R9 independently of one another may represent methyl, ethyl, propyl, phenyl or benzyl, while not more than 2 of the substituents can simultaneously represent phenyl or benzyl; R2, m, R3 and R4 are defined as in the specification, as well as pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.Type: GrantFiled: October 5, 2000Date of Patent: October 15, 2002Assignee: Boehringer Ingelheim GmbHInventors: Walter Lösel, Otto Roos, Dietrich Arndts
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Patent number: 6458986Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-&agr;]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.Type: GrantFiled: February 15, 2002Date of Patent: October 1, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rogelio P. Frutos, Michael Dale Johnson
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Patent number: 6448281Abstract: 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, (CType: GrantFiled: July 3, 2001Date of Patent: September 10, 2002Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
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Patent number: 6441183Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo [1,2-&agr;]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.Type: GrantFiled: February 15, 2002Date of Patent: August 27, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rogelio P. Frutos, Michael Dale Johnson
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Patent number: 6437148Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-a]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.Type: GrantFiled: February 15, 2002Date of Patent: August 20, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rogelio P. Frutos, Michael Dale Johnson
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Patent number: 6433183Abstract: A novel process for the preparation of (R)-3-(4-Bromobenzyl)-1-(3,5-dichlorophenyl)-5-iodo-3-methyl-1-H-imidazo[1,2-&agr;]imidazol-2-one (1): This compound is useful as an intermediate in the preparation of certain small molecules that are useful in the treatment or prevention of inflammatory and immune cell-mediated diseases. The present invention also relates to certain intermediates used in this novel process.Type: GrantFiled: February 15, 2002Date of Patent: August 13, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rogelio P. Frutos, Michael Dale Johnson
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Patent number: 6423298Abstract: The present invention relates to new pharmaceutical formulations for aerosols with at least two or more active substances for administration by inhalation or by nasal route. Specifically, the invention relates to pharmaceutical preparations for propellant-driven metered dose aerosols using a fluorohydrocarbon (HFC) as propellant, which contain a combination of active substance of two or more active substances, wherein at least one active substance is present in dissolved form together with at least one other active substance in the form of suspended particles.Type: GrantFiled: June 8, 1999Date of Patent: July 23, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Daniel P. McNamara, George A. DeStefano
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Patent number: 6417190Abstract: The invention relates to the use of tricyclic nitrogen heterocycles of general formula I as pharmaceutical compositions with an inhibitory effect on PDE IV, wherein the groups R1, R2 and R3 have the meanings given in the specification and claims.Type: GrantFiled: December 10, 1999Date of Patent: July 9, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Matthias Hoffmann, Birgit Jung, Ulrike Kuefner-Muehl, Christopher John Montague Meade