Patents Represented by Attorney Robert P. Raymond
  • Patent number: 7012151
    Abstract: The present invention relates to a process for the highly regioselective aromatic nitration of alkyl 4-alkanoylamino-3-alkyl-benzoates in the 5-position in a mixture containing nitric acid and the use of the resulting products for preparing, in particular, pharmaceutically active benzimidazole derivatives.
    Type: Grant
    Filed: April 12, 2000
    Date of Patent: March 14, 2006
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Margarete Schneider, Heinrich Schneider
  • Patent number: 6916814
    Abstract: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.
    Type: Grant
    Filed: July 1, 2002
    Date of Patent: July 12, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Neil Moss, John Robinson Regan
  • Patent number: 6908928
    Abstract: Crystalline monohydrate of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.
    Type: Grant
    Filed: September 24, 2001
    Date of Patent: June 21, 2005
    Assignee: BI Pharma KG.
    Inventors: Rolf Banholzer, Peter Sieger, Christian Kulinna, Michael Trunk, Manfred Graulich, Peter Specht, Helmut Meissner, Andreas Mathes
  • Patent number: 6905239
    Abstract: The invention relates to a new process for producing powdered preparations for inhalation wherein a substance having a smaller particle size distribution is metered continuously through a suitable feed device onto a moving bed of a powdered substance having a larger particle size distribution.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: June 14, 2005
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Georg Boeck, Michael Walz
  • Patent number: 6903215
    Abstract: Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: March 21, 2003
    Date of Patent: June 7, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashehar Betageri, Thomas A. Gilmore, Christian Hanke Justus Joachim Harcken, Daniel Kuzmich, Doris Riether, David S. Thomson, Ji Wang, Hossein Razavi
  • Patent number: 6894173
    Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Grant
    Filed: February 10, 2003
    Date of Patent: May 17, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Lin-Hua Zhang, Lei Zhu
  • Patent number: 6872399
    Abstract: The present invention relates to the preparation of universal inactivated vaccines and their use in preparing compositions for the prophylaxis and therapy of dermatomycosis. Vaccines according to the present invention have the advantage of conferring immunity against all important causes of dermatomycosis in animals and are characterized by stable immunogenic properties, easy preparation, high content of microconidia and lack of side reactions in animals.
    Type: Grant
    Filed: February 28, 2002
    Date of Patent: March 29, 2005
    Assignee: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Igor Dimitriesich Polyakov, Ludmilla Ivanova
  • Patent number: 6869948
    Abstract: The invention relates in its first aspect to a rapidly decomposing tablet for pain therapy containing meloxicam [4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide] in the form of a salt with an inorganic or organic base providing rapid absorption of the active substance, the process of its preparation by direct tabletting, and furthermore relates in a second aspect to the crystalline meloxicam meglumin salt mono- and dihydrate and the preparation thereof.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: March 22, 2005
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Thomas Bock, Paul Saegmueller, Peter Sieger, Dietrich Tuerck
  • Patent number: 6861547
    Abstract: The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) wherein: R1 denotes a group selected from among methyl, ethyl, propyl, cyclopentyl, cyclohexyl, phenyl, benzyl and —C(Me2)phenyl, each of which is optionally mono-, di- or trisubstituted by hydroxy; and, R2 denotes a group selected from among methyl, ethyl, propyl and benzyl.
    Type: Grant
    Filed: May 5, 2002
    Date of Patent: March 1, 2005
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Joerg Brandenburg, Rolf Schmid, Rainer Soyka, Ralf Anderskewitz, Rolf Bauer, Rainer Hamm, Jutta Kroeber
  • Patent number: 6858594
    Abstract: The present invention relates to the use of ?1L-agonists for treating urinary incontinence.
    Type: Grant
    Filed: November 15, 2002
    Date of Patent: February 22, 2005
    Assignee: Boehringer Ingelheim Pharma GmbH & Co KG.
    Inventors: Franz Esser, Helmut Staehle, Sven Luettke, Ikunobu Muramatsu, Hisato Kitagawa, Shuji Uchida
  • Patent number: 6858641
    Abstract: The present invention relates to indolinones substituted in the 6-position of general formula wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: April 4, 2002
    Date of Patent: February 22, 2005
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Gerald Juergen Roth, Armin Heckel, Thorsten Lehmann-Lintz, Joerg Kley, Frank Hilberg, Jacobus Van Meel
  • Patent number: 6858627
    Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, X, Y, and n are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: August 12, 2003
    Date of Patent: February 22, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Thomas Gilmore, Denice Mary Spero, Hidenori Takahashi, David S. Thomson, Ji Wang
  • Patent number: 6852748
    Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: October 15, 2003
    Date of Patent: February 8, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux, Matt Aaron Tschantz
  • Patent number: 6852717
    Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: February 8, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, John Robinson Regan
  • Patent number: 6852728
    Abstract: A compound of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R1 and R2 are each independently a C1-C4-alkyl optionally substituted with hydroxy or halogen; and R3, R4, R5, R6, R7, and R8 are each independently hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, CF3, CN, NO2, or halogen, with the proviso that at least one of the groups R3, R4, R5, R6, R7, and R8 is not hydrogen, processes for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as pharmaceutical compositions.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: February 8, 2005
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Helmut Meissner, Gerd Morschhaeuser, Michael Paul Pieper, Gerald Pohl, Richard Reichl, Georg Speck
  • Patent number: 6846643
    Abstract: The present invention relates generally to a method for identifying molecules that bind the R7.1 epitope of LFA-1 or bind LFA-1 such that the R7.1 epitope is modified. The present invention further relates to a method for determining occupancy of the LFA-1 receptor by molecules that bind to the R7.1 epitope or bind LFA-1 such that the R7.1 epitope is modified after administration to a subject. The present invention further relates to molecules useful in the methods of the invention.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: January 25, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Joseph R. Woska, Jr., Robert Rothlein, Rene M. Lemieux, Hans C. Reiser, Gary O. Caviness, Takashi Kishimoto, Kathleen Last-Barney
  • Patent number: 6844360
    Abstract: Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
    Type: Grant
    Filed: October 15, 2003
    Date of Patent: January 18, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Terence Alfred Kelly, Jin Mi Kim, René Marc Lemieux
  • Patent number: 6841571
    Abstract: 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: Grant
    Filed: October 24, 2002
    Date of Patent: January 11, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
  • Patent number: 6841566
    Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein R1 is selected from: H, haloalkyl, (C1-6)alkyl, (C2-6)alkenyl, (C3-7)cycloalkyl, (C2-6)alkynyl, (C5-7)cycloalkenyl, 6 or 10-membered aryl, Het all optionally substituted; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C6-10)bicycloalkyl, 6- or 10-membered aryl, or Het all optionally substituted; B is N or CR5, wherein R5 is H, halogen, haloalkyl, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; X is N or CR5; D is N or CR5; each of Y1 and Y2 is independently O or S; Z is O, N, or NRZ wherein RZ is H, (C1-6)alkyl, (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl; R3 and R4 are each independently H, (C1-6)alkyl, first (C3-7)cycloalkyl or 6- or 10-membered aryl, Het (C1-6)alkyl-6- or 10-membered aryl, (C1-6)alkyl-Het; or each R3 and R4 are independently covalently bonded together to form second (C3-7)cycloalkyl, or heterocycle, all optionally substituted; or when Z is N, either R3 or R4
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: January 11, 2005
    Assignee: Boehringer Ingelheim, Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos
  • Patent number: 6838565
    Abstract: Carboxylic acid amides of general formula having an antithrombotic activity and a factor Xa-inhibiting activity. Exemplary are: (a) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-4-(2,5-dihydro-pyrrol-1-yl-carbonyl)-3-methyl-benzamide, (b) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, (c) N-[1-(5-amidino-2-hydroxy-phenyl)-2-phenyl-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide, and (d) N-[1-(5-amidino-2-hydroxy-phenyl)-2-(pyridin-3-yl)-ethyl]-3-methyl-4-(pyrrolidin-1-yl-carbonyl)-benzamide.
    Type: Grant
    Filed: July 21, 2003
    Date of Patent: January 4, 2005
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Uwe Ries, Henning Priepke, Wolfgang Wienen, Herbert Nar, Sandra Handschuh