Patents Represented by Attorney, Agent or Law Firm Anthony P. Bottino
  • Patent number: 6242453
    Abstract: Disclosed are novel aromatic polycyclo heterocyclic compounds of the formula(I) wherein A, B, C, G, Ar, L, Q and X are described herein. The compounds are useful in pharmaceutical compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes of making such compounds.
    Type: Grant
    Filed: February 14, 2000
    Date of Patent: June 5, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc
    Inventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
  • Patent number: 6235732
    Abstract: The invention relates to new compounds of general formula I and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: May 22, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 6228881
    Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Grant
    Filed: December 14, 1999
    Date of Patent: May 8, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: John R. Regan, Pier F. Cirillo, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
  • Patent number: 6191135
    Abstract: The invention relates to new compounds of general formula and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R1, R2, R3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: February 8, 2000
    Date of Patent: February 20, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 6180645
    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: February 18, 1999
    Date of Patent: January 30, 2001
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Walter Lösel, Otto Roos, Dietrich Arndts
  • Patent number: 6156784
    Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I).
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: December 5, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashekhar Betageri, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, John R. Proudfoot
  • Patent number: 6143507
    Abstract: Disclosed is a high throughput compatible assay that is useful for the identification of specific antagonists of TRAF-receptor interactions. The modular flexibility of the assay makes it possible to introduce simple modifications in order to measure the interaction of any TNF receptor cytoplasmic domain (or TRAF-binding protein) with any of the six TRAF proteins, TRAF1, TRAF2, TRAF3, TRAF4, TRAF5 and TRAF6.
    Type: Grant
    Filed: October 29, 1998
    Date of Patent: November 7, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Marilyn R. Kehry, Steven S. Pullen, James J. Crute
  • Patent number: 6103719
    Abstract: The invention relates to new compounds of general formula I ##STR1## or the pharmaceutically acceptable salts thereof, wherein X=N--R.sup.3 or CH--R.sup.4,Y=CH.sub.2 or (CH.sub.2).sub.2,Z=O or H.sub.2 ;and R.sup.1, R.sup.2, R.sup.3, R.sup.4 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 27, 1999
    Date of Patent: August 15, 2000
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Sven Luettke, Birgit Jung, Georg Speck
  • Patent number: 6093723
    Abstract: This invention relates to 4-substituted .beta.-carbolines and .beta.-carboline analogs that inhibit Ca.sup.+2 influx and interleukin-2 (IL-2) production. The 4-substituted .beta.-carbolines and .beta.-carboline analogs of this invention are represented by formula (I): ##STR1## wherein Q, n, R, R', R" and R.sub.1 -R.sub.4 are as defined herein. This invention also relates to methods for producing .beta.-carbolines. Because of their selective immunomodulating properties, the compounds and pharmaceutical compositions of this invention are particularly well suited for preventing and treating immune disorders, including autoimmune disease, inflammatory disease, organ transplant rejection and other disorders associated with IL-2 mediated immune response.
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: July 25, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Clara K Miao, Ian F. Potocki, Roger J. Snow, Karl D. Hargrave, Thomas P. Parks
  • Patent number: 6093553
    Abstract: A brain microvessel endothelial cell having a Middle-T antigen gene from papovirus is disclosed. The brain microvessel endothelial cell exhibits normal cell phenotype, maintains the phenotype in culture and forms monolayers substantially impermeable to low molecular weight molecules. The cells are useful for in vitro studies involving the blood brain barrier. Also disclosed, are methods of using and processes of making these cells.
    Type: Grant
    Filed: November 25, 1998
    Date of Patent: July 25, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Mehran Yazdanian, Barbara J. Bormann
  • Patent number: 6080763
    Abstract: Novel aromatic heterocyclic compounds inhibit cytokines production involved in immunoregulation and inflammation such as interleukin-1 and tumor necrosis factor production. The compounds are therefore useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
    Type: Grant
    Filed: October 29, 1998
    Date of Patent: June 27, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: John R. Regan, Pier F. Cirillo, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
  • Patent number: 6057451
    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: December 4, 1996
    Date of Patent: May 2, 2000
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: James J. Crute, Anne-Marie Faucher, Christine A. Grygon, Karl D. Hargrave, Bruno Simoneau, Bounkham Thavonekham
  • Patent number: 6054470
    Abstract: This invention relates to compounds of formula (1): ##STR1## 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: December 9, 1998
    Date of Patent: April 25, 2000
    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
  • Patent number: 6040289
    Abstract: The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: March 21, 2000
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
  • Patent number: 5985881
    Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.
    Type: Grant
    Filed: August 2, 1997
    Date of Patent: November 16, 1999
    Assignee: Boehringer Ingelheim KG
    Inventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
  • Patent number: 5958696
    Abstract: This invention relates to a solid phase helicase assay for identifying helicase inhibitors. The assay having a model helicase substrate adsorbed on a solid support, the model helicase substrate being an immobilized extended single-stranded nucleic acid polymer hybridized to a labeled helicase reaction product. The presence of the labeled helicase reaction product is detectable in solution on helicase activity. Also described is a method for measuring the helicase inhibiting ability of test substances thus, making the assay useful for identifying pharmaceutically important helicase inhibitors.
    Type: Grant
    Filed: May 22, 1998
    Date of Patent: September 28, 1999
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: James J. Crute
  • Patent number: 5948935
    Abstract: Disclosed herein is a process for preparing (S)-.alpha.-amino-1-carboxycyclopentaneacetic acid which is a useful intermediate for preparing peptidomimetic inhibitors of herpes viral ribonucleotide reductase. The process comprises the preparation of the key intermediate ##STR1## and its subsequent conversion to the desired product.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: September 7, 1999
    Assignee: Boehringer Ingelheim (Canada) Ltd.
    Inventors: Jean-Marie Ferland, Ingrid Guse, Eric Malenfant
  • Patent number: 5947118
    Abstract: A capsule holder for the insertion and fixing of pharmaceutical capsules consists of a plate (2) with a recess (1) in which there are at least three ribs (3) arranged parallel to the central axis and at unequal spacings from one another, between which the capsules can be clamped both by their upper part and by their lower part in such a way that they do not fall out during normal handling but can readily be removed.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: September 7, 1999
    Assignee: Boehringer Ingelheim KG
    Inventors: Dieter Hochrainer, Ross Kinneir
  • Patent number: 5925650
    Abstract: A compound of formula I ##STR1## wherein A denotes a benzo, indolo or thieno group;R.sup.1 denotes thienyl or the group ##STR2## wherein R.sup.7, R.sup.8 and R.sup.9 independently of one another may represent methyl, ethyl, propyl, phenyl or benzyl, whilst not more than 2 of the substituents can simultaneously represent phenyl or benzyl;R.sup.2, m, R.sup.3 and R.sup.4 are defined as in the specification, as well as pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
    Type: Grant
    Filed: December 18, 1997
    Date of Patent: July 20, 1999
    Assignee: Boehringer Ingelheim KG
    Inventors: Walter Losel, Otto Roos, Dietrich Arndts