Patents Represented by Attorney, Agent or Law Firm Alan R. Stempel
  • Patent number: 6492529
    Abstract: Disclosed are aromatic heterocyclic compounds of the formula (I) wherein Ar1, Ar2, L, Q and X are described herein, and intermediate compounds useful for making such compounds. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making compounds of the formula (I), their intermediates and processes of making such intermediates, including bis pyrazole-1H-pyrazole intermediates of the formula: wherein Alk, Rx and Rz are described herein.
    Type: Grant
    Filed: February 5, 2002
    Date of Patent: December 10, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Suresh R. Kapadia, Jinhua J. Song, Nathan K. Yee
  • Patent number: 6492547
    Abstract: The present application relates to carboxylic acid amides of general formula wherein A, B and R1 to R3 are defined as in claim 1, processes for preparing them, pharmaceutical compositions containing these compounds and the use thereof and their preparation.
    Type: Grant
    Filed: December 19, 2001
    Date of Patent: December 10, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Henning Priepke, Norbert Hauel, Klaus Damm, Andreas Schnapp
  • Patent number: 6492393
    Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are 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: November 16, 2000
    Date of Patent: December 10, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Steffen Breitfelder, Pier F. Cirillo, Ming-Hong Hao, Eugene R. Hickey, Rajiv Sharma, Sanxing Sun, Hidenori Takahashi
  • Patent number: 6489365
    Abstract: Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: December 3, 2002
    Assignee: Boehringer Ingelheim KG
    Inventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Frank Himmelsbach, Franz Birke, Armin Fugner
  • Patent number: 6489359
    Abstract: The present invention relates to new sulphoxybenzamides of general formula I, processes for preparing them as well as their use as medicaments.
    Type: Grant
    Filed: October 23, 2001
    Date of Patent: December 3, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Ralf Anderskewitz, Kurt Schromm, Franz Birke, Hans Michael Jennewein
  • Patent number: 6489328
    Abstract: Disclosed are novel compounds of formula (I): wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating 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 pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.
    Type: Grant
    Filed: August 2, 2001
    Date of Patent: December 3, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Roger John Snow, Donghong A. Gao, Daniel R. Goldberg, Abdelhakim Hammach, Daniel Kuzmich, Tina Marie Morwick, Neil Moss, Anthony S. Prokopowicz, III, Robert D. Selliah, Hidenori Takahashi
  • Patent number: 6486321
    Abstract: 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: Grant
    Filed: December 19, 2001
    Date of Patent: November 26, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Rolf Banholzer, Manfred Graulich, Sven Luettke, Andreas Mathes, Helmut Meissner, Peter Specht, Wolfgang Broeder
  • Patent number: 6482429
    Abstract: An insufflation for the administration of a drug into a body cavity is described where the carrier for the drug is a finely divided powder selected from the group consisting of myoinositol, mannitol and cellobiose.
    Type: Grant
    Filed: June 20, 2001
    Date of Patent: November 19, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Frank M. Etzler
  • Patent number: 6481435
    Abstract: The invention relates to an apparatus comprising a closure-cap and a container in the form of a two-chamber cartridge in which an active ingredient and a solvent can be stored separately until the apparatus is used in a nebuliser, as well as an active substance concentrate in which the active substance is present as a solution or suspension for storage purposes.
    Type: Grant
    Filed: May 31, 2001
    Date of Patent: November 19, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Dieter Hochrainer, Bernd Zierenberg
  • Patent number: 6479524
    Abstract: Compounds that prolong thrombin time. Exemplary are: (a) rac-4-{3-[5-ethoxycarbonylmethyl-2-methyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, (b) rac-4-{3-[2,5-dimethyl-4-(2-methyl-pyrrolidinocarbonyl)-phenyl]-propargylamino}benzamidine, and (c) 4-[3-(2,5-dimethyl-4-isopropylcarbonyl-phenyl)propargyl-amino]benzamidine.
    Type: Grant
    Filed: October 18, 2001
    Date of Patent: November 12, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Henning Priepke, Iris Kauffmann-Hefner, Norbert Hauel, Uwe Ries, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
  • Patent number: 6479508
    Abstract: 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: Grant
    Filed: November 27, 2001
    Date of Patent: November 12, 2002
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel
  • Patent number: 6476023
    Abstract: Disclosed are novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: November 20, 2000
    Date of Patent: November 5, 2002
    Assignee: Boehringen Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan
  • Patent number: 6476047
    Abstract: 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: Grant
    Filed: July 19, 2001
    Date of Patent: November 5, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Dietrich Arndts, Walter Loesel, Wolfram Gaida, Klaus Klinder, Stefan Matthias Blech, Henning Draheim
  • Patent number: 6469170
    Abstract: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: October 22, 2002
    Assignee: Boehringer Ingelheim Chemicals, Inc.
    Inventors: Fang-Ting Chiu, Young S. Lo
  • Patent number: 6465483
    Abstract: 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: Grant
    Filed: October 5, 2000
    Date of Patent: October 15, 2002
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Walter Lösel, Otto Roos, Dietrich Arndts
  • Patent number: 6458959
    Abstract: This invention relates to methods for inhibiting herpes replication and for treating herpes infection in a mammal by inhibiting the herpes helicase-primase enzyme complex. This invention also relates to thiazolyphenyl derivatives that inhibit the herpes helicase-primase and to pharmaceutical compositions comprising the thiazolylphenyl derivatives, to methods of using and methods of producing the thiazolylphenyl derivatives.
    Type: Grant
    Filed: October 10, 2000
    Date of Patent: October 1, 2002
    Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim (Canada) Ltd.
    Inventors: James J. Crute, Anne-Marie Faucher, Christine A. Grygon, Karl D. Hargrave, Bruno Simoneau, Bounkham Thavonekham
  • Patent number: 6458986
    Abstract: 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: Grant
    Filed: February 15, 2002
    Date of Patent: October 1, 2002
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rogelio P. Frutos, Michael Dale Johnson
  • Patent number: 6455700
    Abstract: The invention relates to new compounds of general formula I or the pharmaceutically acceptable salts thereof, wherein X=N—R3 or CH—R4, Y=CH2 or (CH2)2, Z=O or H2; and R1, R2, R3, R4 and Ar have the meanings given in the specification, and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: September 24, 2002
    Assignee: Boehringer Ingelheim Pharma KG.
    Inventors: Sven Luettke, Andreas Mathes
  • Patent number: 6451832
    Abstract: Novel benzimidazoles having antithrombotic activity. Exemplary are: (a) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, (b) 2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(ethoxycarbonylmethylamino)-1-(2,5-dihydropyrrolocarbonyl)-ethyl]-benzimidazole, and (c) (R)-2-[4-(N-phenylcarbonylamidino)-phenylaminomethyl]-1-methyl-5-[1-(isobutyloxycarbonylmethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole.
    Type: Grant
    Filed: December 12, 2000
    Date of Patent: September 17, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Uwe Ries, Iris Kaufmann-Hefner, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
  • Patent number: 6448281
    Abstract: 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, (C
    Type: Grant
    Filed: July 3, 2001
    Date of Patent: September 10, 2002
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Pierre Louis Beaulieu, Gulrez Fazal, James Gillard, George Kukolj, Volkhard Austel