Patents Represented by Attorney, Agent or Law Firm Anthony P. Bottino
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Patent number: 6242453Abstract: 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: GrantFiled: February 14, 2000Date of Patent: June 5, 2001Assignee: Boehringer Ingelheim Pharmaceuticals, IncInventors: Pier F. Cirillo, Eugene R. Hickey, John R. Regan, Lin-Hua Zhang
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Patent number: 6235732Abstract: 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: GrantFiled: February 16, 1999Date of Patent: May 22, 2001Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 6228881Abstract: 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: GrantFiled: December 14, 1999Date of Patent: May 8, 2001Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: John R. Regan, Pier F. Cirillo, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
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Patent number: 6191135Abstract: 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: GrantFiled: February 8, 2000Date of Patent: February 20, 2001Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 6180645Abstract: 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: February 18, 1999Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim GmbHInventors: Walter Lösel, Otto Roos, Dietrich Arndts
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Patent number: 6156784Abstract: 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: GrantFiled: December 7, 1999Date of Patent: December 5, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, John R. Proudfoot
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Patent number: 6143507Abstract: 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: GrantFiled: October 29, 1998Date of Patent: November 7, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Marilyn R. Kehry, Steven S. Pullen, James J. Crute
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Patent number: 6103719Abstract: 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: GrantFiled: May 27, 1999Date of Patent: August 15, 2000Assignee: Boehringer Ingelheim Pharma KGInventors: Franz Esser, Gerd Schnorrenberg, Horst Dollinger, Sven Luettke, Birgit Jung, Georg Speck
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Patent number: 6093723Abstract: 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: GrantFiled: August 8, 1997Date of Patent: July 25, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Clara K Miao, Ian F. Potocki, Roger J. Snow, Karl D. Hargrave, Thomas P. Parks
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Patent number: 6093553Abstract: 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: GrantFiled: November 25, 1998Date of Patent: July 25, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Mehran Yazdanian, Barbara J. Bormann
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Patent number: 6080763Abstract: 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: GrantFiled: October 29, 1998Date of Patent: June 27, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: John R. Regan, Pier F. Cirillo, Eugene R. Hickey, Neil Moss, Charles L. Cywin, Christopher Pargellis, Thomas A. Gilmore
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Patent number: 6057451Abstract: 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: GrantFiled: December 4, 1996Date of Patent: May 2, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: James J. Crute, Anne-Marie Faucher, Christine A. Grygon, Karl D. Hargrave, Bruno Simoneau, Bounkham Thavonekham
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Patent number: 6054470Abstract: 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: GrantFiled: December 9, 1998Date of Patent: April 25, 2000Assignee: 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
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Patent number: 6040289Abstract: 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: GrantFiled: May 29, 1998Date of Patent: March 21, 2000Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
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Patent number: 5985881Abstract: 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: GrantFiled: August 2, 1997Date of Patent: November 16, 1999Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5958696Abstract: 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: GrantFiled: May 22, 1998Date of Patent: September 28, 1999Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: James J. Crute
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Patent number: 5948935Abstract: 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: GrantFiled: January 23, 1998Date of Patent: September 7, 1999Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Jean-Marie Ferland, Ingrid Guse, Eric Malenfant
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Patent number: 5947118Abstract: 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: GrantFiled: June 30, 1997Date of Patent: September 7, 1999Assignee: Boehringer Ingelheim KGInventors: Dieter Hochrainer, Ross Kinneir
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Patent number: 5925650Abstract: 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: GrantFiled: December 18, 1997Date of Patent: July 20, 1999Assignee: Boehringer Ingelheim KGInventors: Walter Losel, Otto Roos, Dietrich Arndts