Patents Represented by Attorney, Agent or Law Firm A. R. Stempel
  • Hepatitis C inhibitor tri-peptides
    Patent number: 6329379
    Abstract: 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 o
    Type: Grant
    Filed: September 29, 2000
    Date of Patent: December 11, 2001
    Assignee: 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
  • Hepatitis C inhibitor tri-pepitides
    Patent number: 6329417
    Abstract: Racemates, diastereolsomers 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 or
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: December 11, 2001
    Assignee: 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
  • Aromatic heterocyclic compounds as antiinflammatory agents
    Patent number: 6329415
    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 involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: June 26, 2001
    Date of Patent: December 11, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, John R. Regan
  • Hepatitis C inhibitor tri-peptides
    Patent number: 6323180
    Abstract: 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 CH2—R20, NH—R20, O—R20 or S—R20, wherein R20 is a satu
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: November 27, 2001
    Assignee: Boehringer Ingelheim (Canada) Ltd
    Inventors: Montse Llinas-Brunet, Murray D. Bailey, Dale Cameron, Elise Ghiro, Nathalie Goudreau, Marc-André Poupart, Jean Rancourt, Youla S. Tsantrizos, Anne-Marie Faucher, Teddy Halmos, Dominik M. Wernic, Bruno Simoneau
  • Benzoylguanidine derivatives
    Patent number: 6323207
    Abstract: Novel benzoylguanidine derivatives of general formula I useful for the treatment or reduction of tissue damage due to ischaemia.
    Type: Grant
    Filed: September 15, 1999
    Date of Patent: November 27, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Christian Eickmeier, Erich Buerger, Stefan Matthias Blech, Otto Roos
  • HSV primase inhibitors
    Patent number: 6323202
    Abstract: The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: wherein R1 is hydroxy or amino; R2 is hydrogen, halo, (C1-4)alkyl or (C1-4)alkoxy; R3 is hydrogen, halo, (C1-4)alkyl, (C1-4)alkoxy, amino or azido; R4 has the same significance as R2; R5 is hydrogen or (C1-4)alkyl; and R is (C1-7)alkyl, (C3-6)cycloalkyl, {phenyl(C1-7)alkyl}, {phenyl(C1-7)alkoxy}, {{(monocyclic heterocyclo)-{(C1-7)alkoxy}}, CH(W)C(O){O-(C1-4)alkyl} wherein W is hydrogen or (C1-7)alkyl, or  wherein Y is hydrogen or (C1-7)alkyl, and Z is (C1-7)alkyl, (C3-6) cycloalkyl, {(C3-6)cycloalkyl}- {(C1-7)alkyl}, phenyl(C1-7)alkyl or {{(monocyclic heterocyclo)-{(C1-7)alkyl}}, or Y and Z together with the nitrogen atom to which they are attached represent, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or 1-(4-methylpiperazinyl); with the provisos that (1) when R is CH(W
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: November 27, 2001
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Bruno Simoneau, Michele Liuzzi, Anton Mentrup
  • Substituted indolinones with kinase inhibitory activity
    Patent number: 6319918
    Abstract: Substituted indolinones of general formula having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: 3-Z-[1-(4-(N-Benzyl-N-methyl-aminomethyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone and 3-Z-[1-(4-(2,3,4,5-Tetrahydro-benzo(d)azepin-3-yl-methyl)-phenylamino)-1-methyl-methylene]-5-amido-2-indolinone.
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: November 20, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Armin Heckel, Rainer Walter, Wolfgang Grell, Jacobus C. A. van Meel, Norbert Redemann
  • Aromatic heterocyclic compound as antiinflammatory agents
    Patent number: 6319921
    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 involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: November 20, 2001
    Assignee: Boerhinger Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
  • Antagonists of calcitonin gene-related peptide
    Patent number: 6313097
    Abstract: Compounds of the formula (I) wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compositions containing these compounds, and their use in the selective antagonization of calcitonin gene-related peptide (CGRP) and in the treatment or prophylaxis of migraine or cluster headaches, non-insulin-dependent diabetes mellitus, inflammation, allergic rhinitis, asthma, morphine tolerance, menopausal hot flashes, and diseases characterized by excessive vasodilatation and consequent reduction in blood-flow.
    Type: Grant
    Filed: March 10, 2000
    Date of Patent: November 6, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
  • Succinate derivative compounds useful as cysteine protease inhibitors
    Patent number: 6313117
    Abstract: Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
    Type: Grant
    Filed: July 28, 2000
    Date of Patent: November 6, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Rajashehar Betageri, Michel Jose Emmanuel, Eugene Richard Hickey, Weimin Liu, Usha R. Patel, Denice Mary Spero, David S. Thomson, Yancey David Ward, Erick Richard Roush Young, Sanxing Sun
  • Preparation of human papillomavirus E1 having helicase activity and method therefor
    Patent number: 6306580
    Abstract: The present invention relates to a method for isolating cloned papillomavirus E1 protein from a eukaryotic expression system having demonstrable and reproducible viral helicase activity and preparation containing essentially pure E1 protein. The invention further relates to the use of this novel E1 protein preparation in a screening assay for identifying antiviral agents. More particularly a high throughput assay to screen for agents capable of inhibiting HPV DNA replication. The assay is based on measuring the effect of antiviral agents on the activity of the E1 protein and more specifically on its helicase activity.
    Type: Grant
    Filed: April 28, 1999
    Date of Patent: October 23, 2001
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Alex Pelletier, Chris M. Farnet
  • Antithrombotic phenylalkyl derivatives
    Patent number: 6300342
    Abstract: Antithrombotic phenylalkyl derivatives of the formula Exemplary compounds are: (a) 1-[3-(4-amidino-phenyl)propionyl]-6-(4-fluoro-phenylsulphonamido)-1,2,3,4-tetrahydro-quinoline, (b) 1-[3-(4-amidino-phenyl)propionyl]-6-butylsulphonamido-1,2,3,4-tetrahydro-quinoline, (c) 1-[3-(4-amidino-phenyl)propionyl]-5-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, (d) 1-[3-(4-amidino-phenyl)propionyl]-3-methyl-6-phenylsulphonamido-1,2,3,4-tetrahydro-quinoline, and, (e) 1-[3-(4-amidino-phenyl)propionyl]-6-(5-chloro-thien-2-ylsulphonamido)-1,2,3,4-tetrahydro-quinoline.
    Type: Grant
    Filed: December 9, 1999
    Date of Patent: October 9, 2001
    Assignee: Boehringer Ingelheim Pharm KG
    Inventors: Armin Heckel, Rainer Soyka, Wolfgang Grell, Eric Haaksma, Klaus Binder, Rainer Zimmerman
  • Ipratropium bromide enantiomer with prolonged duration of effect
    Patent number: 6299861
    Abstract: On account of the surprisingly powerful and long-lasting effect thereof, the salts of the L-(−)-enantiomer of (endo, syn)-(−)-3-(3-hydroxy-1-oxo-2-phenylpropoxy)-8-methyl-8-(methylethyl)-8-azoniabicyclo [3,2,1]octane are suitable as active substances for drugs administered by inhalation for respiratory tract therapy.
    Type: Grant
    Filed: August 6, 1999
    Date of Patent: October 9, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Rolf Banholzer, Richard Reichl, Bernd Disse, Georg Speck
  • Aromatic heterocyclic compounds as anti-inflammatory agents
    Patent number: 6297381
    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: February 14, 2000
    Date of Patent: October 2, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan
  • Method for extraction and reaction using supercritical fluids
    Patent number: 6294194
    Abstract: Methods for removing soluble material from confined spaces within substrates such as containers, capsules and porous powders comprising extraction with supercritical fluids, the pressure of which is preferably modulated between an upper level and a lower level within a relatively narrow range of fluid pressure and density. The method permits enhanced extraction efficiency, catalytic reaction rates and ability to maintain catalyst activity.
    Type: Grant
    Filed: March 3, 2000
    Date of Patent: September 25, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Stephen T. Horhota, Said Saim
  • Peptidomimetic inhibitors of the human cytomegalovirus protease
    Patent number: 6291640
    Abstract: A compound of formula (I) is disclosed: wherein X, z, W, Y, R1 through R5, m and n are as define herein. These compounds are peptidomimetic inhibitors of human cytomegalovirus (HCMV) protease and are useful for the treatment of human cytomegalovirus infection.
    Type: Grant
    Filed: October 19, 1998
    Date of Patent: September 18, 2001
    Assignee: Boehringer Ingelheim Ltd.
    Inventors: Murray D. Bailey, Gulrez Fazal, Pierre Lavallee, William Ogilvie, Marc-Andre Poupart
  • Antiherpes virus compounds and methods for their preparation and use
    Patent number: 6288091
    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.
    Type: Grant
    Filed: July 30, 1999
    Date of Patent: September 11, 2001
    Assignees: Boehringer Ingelheim Ltd., Boehringer Ingelheim Pharm. Inc.
    Inventors: J. James Crute, Anne-Marie Faucher, Christine Grygon, Karl D. Hargrave, Bruno Simoneau, Bounkham Thavonekham
  • Src family SH2 domain inhibitors
    Patent number: 6284768
    Abstract: This invention relates to compounds of formula (I): wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: September 4, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashekhar Betageri, Pierre L. Beaulieu, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, Usha Patel, John R. Proudfoot, Mario Cardozo
  • Oxadiazoles, processes for their preparation and their use as medicaments
    Patent number: 6277872
    Abstract: The invention relates to oxadiazole derivatives of general formula (I) wherein X, Y, Z and R1 are defined as described in the specification and claims, processes for preparing them and their use as pharmaceutical compositions.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: August 21, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Michael Brenner, Roland Maier, Marion Wienrich, Thomas Weiser, Rainer Palluk, Wolf-Dietrich Bechtel, Angelo Sagrada, Helmut Ensinger, Uwe Pschorn, Raffaele Cesana
  • Neurokinin antagonists, processes for preparing them and pharmaceutical compositions containing these compounds
    Patent number: 6277840
    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: May 9, 2000
    Date of Patent: August 21, 2001
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Sven Luettke, Birgit Jung, Georg Speck