Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
  • Pyrrolotriazine compounds as kinase inhibitors
    Patent number: 7297695
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: November 20, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
  • Use of 2-alkoxyphenyl-substituted imidazotriazinones
    Patent number: 7276504
    Abstract: The present invention relates to the use of known 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position and cGMP PDE-inhibitory properties for the production of medicaments for the treatment of cardiac insufficiency, psoriasis, female infertility, cancer, diabetes, ophthalmic disorders such as glaucoma, disorders of gastric motility, cystic fibrosis, premature labour, pulmonary hypertension, bladder disorders, prostate hyperplasia, nitrate-induced tolerance, pre-eclampsia, alopecia, Parkinson's disease, pain, tinnitus or the renal syndrome.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: October 2, 2007
    Assignee: Bayer HealthCare AG
    Inventors: Maria Theresia Niewohner, legal representative, Erwin Bischoff, Helmut Haning, Afssaneh Rahbar, Tiemo-Joerg Bandel, Wolfgang Barth, Ulrich Niewohner, deceased
  • Anticoagulant and fibrinolytic therapy using p38 MAP kinase inhibitors
    Patent number: 7276491
    Abstract: Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: October 2, 2007
    Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Chester C. Wood, Thomas van der Poll
  • PYRROLOTRIAZINE ANILINE PRODRUG COMPOUNDS USEFUL AS KINASE INHIBITORS
    Publication number: 20070213300
    Abstract: Compounds having the Formula (I), including pharmaceutically acceptable salts thereof, wherein at least one of X1, X2 or X3 is and any remaining X1, X2 or X3 is hydrogen, which are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, A1, A2 and m are as described herein.
    Type: Application
    Filed: March 6, 2007
    Publication date: September 13, 2007
    Inventors: Chunjian Liu, Katerina Leftheris, Vivekananda M. Vrudhula, James Lin
  • Inhibitors of kinases
    Patent number: 7265113
    Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: January 13, 2005
    Date of Patent: September 4, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rajeev S. Bhide, Zhen-Wei Cai, Ligang Qian, Stephanie Barbosa, Louis Lombardo, Jeffrey Robl
  • Tricyclic-heteroaryl compounds useful as kinase inhibitors
    Patent number: 7253167
    Abstract: The present invention relates to compounds having the formula, wherein, Q is optionally substituted aryl or heteroaryl, R1 is hydrogen or C1-4alkyl, and R2, R3, R4 and R5 are hydrogen or optional substituents as defined in the specification.
    Type: Grant
    Filed: June 29, 2005
    Date of Patent: August 7, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: James Lin, Stephen T. Wrobleski, Chunjian Liu, Katerina Leftheris
  • Pyrrolotriazine inhibitors of kinases
    Patent number: 7244733
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: February 2, 2006
    Date of Patent: July 17, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: John T. Hunt, Rajeev S. Bhide, Robert Michael Borzilleri, Ligang Qian
  • 3-furanyl analogs of toxoflavine as kinase inhibitors
    Patent number: 7241763
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein, the use of such compounds as inhibitors of cyclin-dependent serine/threonine kinases (Cdks), as well as kinases and phosphatases involved in cell cycle regulation such as the tyrosine kinases Wee1, Mik1 and Myt1 or the tyrosine dephosphatases such as Cdc25 and Pyp3. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating cell proliferative disorders such as atherosclerosis, restenosis and cancer.
    Type: Grant
    Filed: July 8, 2003
    Date of Patent: July 10, 2007
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean Fernand Armand LaCrampe, Richard William Connors, Chih Yung Ho, Alan Richardson, Eddy Jean Edgard Freyne, Peter Jacobus Johannes Buijnsters, Annette Cornelia Bakker
  • Intermediates useful in preparing certain pyrrolotriazine compounds and process for making such intermediates
    Patent number: 7232901
    Abstract: Described herein is at least one pyrrolo[1,2-f][1,2,4]triazine-2,4(1H,3H)-dione, which is an intermediates useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and at least one method for making such intermediate.
    Type: Grant
    Filed: June 27, 2006
    Date of Patent: June 19, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Harold Mastalerz, Guifen Zhang
  • Reverse-turn mimetics and method relating thereto
    Patent number: 7232822
    Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
    Type: Grant
    Filed: March 17, 2004
    Date of Patent: June 19, 2007
    Assignee: Choongwae Pharma Corporation
    Inventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
  • N-[4-(heteroarylmethyl)phenyl]-heteroarylamines
    Patent number: 7205312
    Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
    Type: Grant
    Filed: November 2, 2004
    Date of Patent: April 17, 2007
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Marc Gaston Venet, Dominique Jean-Pierre Mabire, Jean Fernand Armand Lacrampe, Gerard Charles Sanz
  • Substituted imidazotriazines
    Patent number: 7202243
    Abstract: The invention relates to new substituted imidazotriazines, processes for their preparation and their use for the production of medicaments for the treatment and/or prophylaxis of cancer and neurodegenerative disorders, in particular of Parkinson's disease and of schizophrenia.
    Type: Grant
    Filed: June 25, 2003
    Date of Patent: April 10, 2007
    Assignee: Bayer HealthCare AG
    Inventors: Martin Hendrix, David Brückner, Arno Friedl, Irene Gerlach, Volker Hinz, Jörg Keldenich, Frank Mauler, Maria Niewöhner, legal representative, Dagmar Karthaus, Karl-Heinz Schlemmer, Adrian Tersteegen, Özkan Yalkinoglu, Ulrich Niewöhner, deceased
  • Protein tyrosine phosphatase inhibitor
    Patent number: 7199121
    Abstract: Use of a compound of formula (I): wherein each R, which are the same or different, is H or C1–C6 alkyl, and X completes a ring which is a substituted triazine having one of the following formulae (II) to (IV): wherein R? is H or C1–C6 alkyl; or an enol tautomer of a compound of formula (I) in which any of the groups R or R? is hydrogen; in the manufacture of a medicament for use as a protein tyrosine phosphatase (PTP) inhibitor. Formula (I) embraces 2-methylfervenulone, which can be produced by fermentation of a novel microbial strain. Fermentation of the said strain also produces novel precursors to 2-methylfervenulone having utility as prodrugs.
    Type: Grant
    Filed: September 7, 2001
    Date of Patent: April 3, 2007
    Assignee: Institute of Molecular and Cell Biology
    Inventors: Catherine J. Pallen, Haishan Wang, Kah Leong Lim, Su Ling Yeo, Yue Wang, Yin Hwee Tan
  • Heteropolycyclic inhibitors of protein kinases
    Patent number: 7196083
    Abstract: A method of inhibiting tumor growth is provided, comprising administering an effective dose of a compound of the formula wherein, independently at each occurrence, w is C or N, v and x are N with H substitution as needed to fulfill open valence sites; y and z are selected from N and C, with H substitution as needed to fulfill open valence sites, with the proviso that each of w, v, x, y and z is not simultaneously C; the ring formed from v, w, x, y and z may be saturated or unsaturated; and R1, R2, R3 and R4 are selected from hydrogen, alkyl, aryl, alkaryl, aralkyl, heteroalkyl, and heteroaryl; wherein any adjacent two of R1, R2, R3 and R4 may join together to form a 5, 6 or 7-membered carbocyclic ring or a 5, 6 or 7-membered heterocyclic ring containing at least one atom selected from nitrogen, oxygen and sulfur.
    Type: Grant
    Filed: December 4, 2002
    Date of Patent: March 27, 2007
    Assignee: OLT Inc.
    Inventors: Zaihui Zhang, Xinyao Du, Serguei Sviridov, Greg Chopiuk
  • (Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds
    Patent number: 7196095
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis
    Type: Grant
    Filed: June 21, 2002
    Date of Patent: March 27, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Richard Beresis, Richard Berger, Steven L. Colletti, James B. Doherty, Dennis D. Feng, Gui-Bai Liang, Dennis M. Schmatz, Xiaoxia Qian, David A. Claremon, Nigel J. Liverton, Charles J. McIntyre, Ernest W. Kovacs
  • Imidazo-triazine derivatives as ligands for gaba receptors
    Patent number: 7176203
    Abstract: A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
    Type: Grant
    Filed: May 1, 2003
    Date of Patent: February 13, 2007
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Robert James Maxey, Michael Geoffrey Neil Russell, Leslie Joseph Street
  • Pyrrolotriazine kinase inhibitors
    Patent number: 7173031
    Abstract: In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.
    Type: Grant
    Filed: June 24, 2005
    Date of Patent: February 6, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhong Chen, John T. Hunt, Tram Huynh, Michael A. Poss, Gretchen M. Schroeder, Wayne Vaccaro, Tai W. Wong, Xiao-Tao Chen, Kyoung S. Kim
  • Pyrrolo-triazine aniline compounds useful as kinase inhibitors
    Patent number: 7160883
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: January 9, 2007
    Assignee: Bristol-Myers-Squibb Company
    Inventors: Alaric Dyckman, John Hynes, Katerina Leftheris, Chunjian Liu, Stephen T. Wrobleski
  • Devices and methods for eliminating termite colonies
    Patent number: 7157078
    Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing a) a termiticide selected such that the termiticide causes death to about 50 to about 100% of termites within about 24 to about 84 days after the termites begin to ingest the termiticide or the bait matrix comprising the termiticide, b) a cellulose containing material, and c) water. The termiticidal bait matrix can be used in a bait station installed in the ground. The kits are suitable to be used by consumers in their homes.
    Type: Grant
    Filed: February 2, 2004
    Date of Patent: January 2, 2007
    Assignee: The University of Florida Research Foundation, Inc.
    Inventors: Philip Frederick Brode, III, Garry Steven Garren, Leo Timothy Laughlin, Randall Stryker Matthews, Dale Edwin Barker, Daniel James Kinne, Gary Eugene McKibben, Christopher Miles Miller, Timothy Robert Probst
  • Pyrrolotriazine compounds
    Patent number: 7151176
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: October 19, 2005
    Date of Patent: December 19, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Wen-Ching Han, Yufen Zhao, Ping Chen
  • C-6 modified indazolylpyrrolotriazines
    Patent number: 7148220
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: December 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Gregory D. Vite, Ashvinikumar V. Gavai, Brian E. Fink, Harold Mastalerz, John F. Kadow
  • Process for preparing pyrrolotriazine aniline compounds useful as kinase inhibitors
    Patent number: 7148348
    Abstract: A process is provided for the process for preparing a pyrrolotriazine aniline p38 kinase inhibitor such as amide II by the direct aminolysis of the ester I wherein ester I is reacted with a strong organometallic base, such as hexyllithium or n-butyllithium and the desired amine such as n-propylamine to form the amide II.
    Type: Grant
    Filed: August 9, 2005
    Date of Patent: December 12, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Reginald O. Cann, Edward J. Delaney, Junying Fan, Luca Parlanti
  • Pyrrolotriazine compounds as kinase inhibitors
    Patent number: 7141571
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: November 28, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brian E. Fink, Ashvinikumar V. Gavai, Gregory D. Vite, Ping Chen, Harold Mastalerz, Derek J. Norris, John S. Tokarski, Yufen Zhao, Wen-Ching Han
  • Methods of synthesizing 3-amino-1,2,4-benzotriazines
    Patent number: 7129349
    Abstract: An improved method of producing 3-amino-1,2,4-benzotriazines using nitrobenzene or a derivative thereof, a guanidine salt and a base as reactants is provided. The method is carried out at a moderate reaction temperature without producing halide wastes derived from nucleophilic substitution and acid byproducts.
    Type: Grant
    Filed: October 8, 2003
    Date of Patent: October 31, 2006
    Assignee: Trustees of Dartmouth College
    Inventors: Nikolai V. Moskalev, Gordon W. Gribble
  • Triazolotriazine compounds and uses thereof
    Patent number: 7122548
    Abstract: The present invention relates to compounds of the Formula (I), and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: June 24, 2004
    Date of Patent: October 17, 2006
    Assignee: Sugen, Inc.
    Inventors: Fang-Jie Zhang, Tomas Vojkovsky, Ping Huang, Congxin Liang, Steven Huy Do, Marcel Koenig, Jingrong Cui
  • 2-Phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
    Patent number: 7122540
    Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
    Type: Grant
    Filed: August 20, 2004
    Date of Patent: October 17, 2006
    Assignee: Bayer HealthCare AG
    Inventors: Maria Niewöhner, legal representative, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Semo, Marc Nowakowski, Ulrich Niewöhner, deceased
  • Heterocycles 3
    Patent number: 7115602
    Abstract: The invention relates to 7-(4-tert butyl-cyclohexyl)-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: October 3, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Cristina Alonso-Alija, Heike Gielen, Martin Hendrix, Maria Niewöhner, Dagmar Schauss, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel J. Cuthbert, Mary F. Fitzgerald, Graham Sturton, Ulrich Niewöhner
  • A-pyrrolines
    Patent number: 7115603
    Abstract: This invention relates to novel ?1-pyrrolines of formula(I) in which R1, R2, Y and R3 are as defined in the disclosure, to a number of processes for preparing these substances, and to their use for controlling pests.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: October 3, 2006
    Assignee: Bayer CropScience AG
    Inventors: Thomas Seitz, Martin Füsslein, Johannes-Rudolf Jansen, Udo Kraatz, Angelika Lubos-Erdelen, legal representative, Andreas Turberg, Olaf Hansen, Christoph Erdelen, deceased
  • Pyrrolotriazine inhibitors of kinases
    Patent number: 7112675
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: September 26, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: John T. Hunt, Rajeev S. Bhide, Robert Michael Borzilleri, Ligang Qian
  • Pyrrolotriazine compounds
    Patent number: 7102003
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: June 21, 2005
    Date of Patent: September 5, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Harold Mastalerz, Jean-Paul Daris, Pierre Dextraze, Philippe Lapointe, Edward H. Ruediger, Dolatrai M. Vyas, Guifen Zhang
  • Pyrrolotriazine kinase inhibitors
    Patent number: 7102002
    Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: September 5, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Zhen-wei Cai, Louis J. Lombardo, Rajeev S. Bhide, Ligang Qian, Donna D. Wei, Stephanie Barbosa
  • Imidazotriazinones and the use thereof
    Patent number: 7098207
    Abstract: Novel imidazotriazinones of general formula a method for the production and the pharmaceutical use thereof are disclosed.
    Type: Grant
    Filed: January 5, 2005
    Date of Patent: August 29, 2006
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Maria Niewohner, legal representative, Mazen Es-Sayed, Thomas Lampe, Helmut Haning, Gunter Schmidt, Karl-Heinz Schlemmer, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Ulrich Niewohner, deceased
  • 5-Ethyl-imidazotriazinones
    Patent number: 7087605
    Abstract: The invention relates to novel 5-Ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
    Type: Grant
    Filed: May 21, 2002
    Date of Patent: August 8, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Cristina Alonso-Alija, Heike Gielen, Martin Hendrix, Maria Theresia Niewohner, legal representative, Dagmar Schauss, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel J. Cuthbert, Mary F. Fitzgerald, Richard Graham Sturton, Martin Michels, Ulrich Niewohner, deceased
  • 5-ethylimidarotriazones
    Patent number: 7074790
    Abstract: The invention relates to novel 5-ethyl-imidazotriazinones, processes for their preparation and their use in medicaments, esp. for the treatment and/or prophylaxis of inflammatory processes and/or immune diseases.
    Type: Grant
    Filed: May 5, 2003
    Date of Patent: July 11, 2006
    Inventors: Cristina Alonso-Alija, Heike Gielen-Haertwig, Martin Michels, Dagmar Karthaus, Hilmar Bischoff, Nils Burkhardt, Volker Geiss, Karl-Heinz Schlemmer, Nigel Cuthbert, Mary F. Fitzgerald, Graham Sturton, Maria Theresia Niewöhner, legal representative, Ulrich Niewöhner, deceased
  • Di-substituted pyrrolotriazine compounds
    Patent number: 7064203
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: June 20, 2006
    Assignee: Bristol Myers Squibb Company
    Inventors: Ashvinikumar V. Gavai, Wen-Ching Han, Ping Chen, Edward H. Ruediger, Harold Mastalerz, Brian E. Fink, Derek J. Norris
  • Tetracyclic compounds as c-Met inhibitors
    Patent number: 7037909
    Abstract: The present invention relates to compounds of the Formulae (I) and (II), wherein R1-R10 and G are defined herein, and their pharmaceutically acceptable salts. These compounds modulate the activity of c-Met and are therefore expected to be useful in the prevention and treatment of c-Met related disorders such as cancer.
    Type: Grant
    Filed: June 29, 2004
    Date of Patent: May 2, 2006
    Assignee: Sugen, Inc.
    Inventors: Tomas Vojkovsky, Marcel Koenig, Fang-Jie Zhang, Jingrong Cui
  • Azabicyclic heterocycles as cannabinoid receptor modulators
    Patent number: 7037910
    Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, and R4 are described herein.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: May 2, 2006
    Assignee: Bristol-Myers Squibb
    Inventors: William R. Ewing, Guixue Yu, Bruce A. Ellsworth
  • Pyrrolotriazinone compounds and their use to treat diseases
    Patent number: 7030118
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: April 18, 2006
    Assignee: Bristol-Myers Squibb Company
    Inventors: Louis J. Lombardo, Rajeev S. Bhide, Kyoung S. Kim, Songfeng Lu
  • Imidazo-triazine derivatives as ligands for gaba receptors
    Patent number: 7005431
    Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
    Type: Grant
    Filed: May 1, 2003
    Date of Patent: February 28, 2006
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Michela Bettati, Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Michael Geoffrey Neil Russell, Leslie Jospeh Street
  • Substituted imidazotriazinones
    Patent number: 6998402
    Abstract: The invention relates to novel substituted imidazotriazinones, to a method for their production and to the use thereof for producing medicaments, in particular to improve perception, powers of concentration, learning capacity and/or memory retentiveness.
    Type: Grant
    Filed: February 11, 2002
    Date of Patent: February 14, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Maria Theresia Niewöhner, legal representative, Dagmar Schauss, Gerhard König, Martin Hendrix, Frank-Gerhard Böss, Franz-Josef van der Staay, Rudy Schreiber, Karl-Heinz Schlemmer, Toshiya Moriwaki, Ulrich Niewöhner, deceased
  • Heterocyclic topoisomerase poisons
    Patent number: 6995154
    Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: February 7, 2006
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
  • Pharmaceutical formulations of antineoplastic agents and processes of making and using the same
    Patent number: 6987108
    Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: January 17, 2006
    Assignee: Schering Corporation
    Inventors: Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
  • Carboline derivatives as PDE5 inhibitors
    Patent number: 6984641
    Abstract: Selective inhibitors of cGMP-specific PDE, and use of the compounds and salts and solvates thereof as therapeutic agents, are disclosed.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: January 10, 2006
    Assignee: Lilly Icos LLC.
    Inventors: Mark W. Orme, Jason S. Sawyer, Alain C. Daugan, Agnes Bombrun, Françoise Gellibert, Lisa M. Schultze, Raymond F. Brown, Romain L. Gosmini
  • Pyrrolotriazine inhibitors of kinases
    Patent number: 6982265
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: May 18, 2000
    Date of Patent: January 3, 2006
    Assignee: Bristol Myers Squibb Company
    Inventors: John T. Hunt, Rajeev S. Bhide, Robert Michael Borzilleri, Ligang Qian
  • Azaisoquinoline derivatives as matrix metalloproteinase inhibitors
    Patent number: 6977261
    Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, Y, R2, R3, R4, R5, and n are as defined in the specification. The invention also provides pharmaceutical compositions comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, as defined in the specification, together with a pharmaceutically acceptable carrier, diluent, or excipient. The invention also provides methods of inhibiting an MMP-13 enzyme in an animal, comprising administering to the animal a compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention also provides methods of treating a disease mediated by an MMP-13 enzyme in a patient, comprising administering to the patient a compound of Formula I, or a pharmaceutically acceptable salt thereof, either alone or in a pharmaceutical composition.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: December 20, 2005
    Assignee: Warner-Lambert Company LLC
    Inventors: Amy Mae Bunker, Joseph Armand Picard
  • Azaindole kinase inhibitors
    Patent number: 6969717
    Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: November 29, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rajeev S. Bhide, Rejean Ruel, Carl Thibault, Alexandre L'Heureux
  • Pyrazolotriazines as CRF antagonists
    Patent number: 6960583
    Abstract: The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.
    Type: Grant
    Filed: March 18, 2004
    Date of Patent: November 1, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Paul J. Gilligan, Richard G. Wilde
  • Pyrrolotriazine kinase inhibitors
    Patent number: 6951859
    Abstract: The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
    Type: Grant
    Filed: August 4, 2003
    Date of Patent: October 4, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rajeev S. Bhide, Robert M. Borzilleri
  • Substituted pyrazoles
    Patent number: 6951851
    Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.
    Type: Grant
    Filed: March 28, 2003
    Date of Patent: October 4, 2005
    Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
  • 7-Alkyl and cycloalkyl-substituted imidazotriazinones
    Patent number: 6943163
    Abstract: The present invention relates to 7-alkyl- and cycloalkyl-substituted imidazotriazinones, to processes for their preparation and to their use as medicaments, in particular as inhibitors of cGMP-metabolizing phosphodiesterases.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: September 13, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Gunter Schmidt, Karl-Heinz Schlemmer, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn