Four Or More Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 544/184)
  • Publication number: 20090163468
    Abstract: Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
    Type: Application
    Filed: December 2, 2008
    Publication date: June 25, 2009
    Inventors: Xin Chen, Heather Coate, Andrew Philip Crew, Han-Qing Dong, Ayako Honda, Mark Joesph Mulvihill, Paula A.R. Tavares, Jing Wang, Douglas S. Werner, Kristen Michelle Mulvihill, Kam W. Siu, Bijoy Panicker, Apoorba Bharadwaj, Lee D. Arnold, Meizhong Jin, Brian Volk, Qinghua Weng, James David Beard
  • Publication number: 20090156594
    Abstract: The present disclosure provides heterocyclic protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.
    Type: Application
    Filed: May 21, 2008
    Publication date: June 18, 2009
    Applicant: SGX Pharmaceuticals, Inc.
    Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth A. Jefferson, Jorg Hendle, Patrick S. Lee, Angelina Marie Thayer, Gavin Charles Hirst
  • Publication number: 20090156604
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Application
    Filed: August 14, 2008
    Publication date: June 18, 2009
    Inventors: Swen HOLDER, Armin Zulch, Thomas Bar, Thomas Maier, Astrid Zimmermann, Thomas Beckers, Volker Gekeler, Hemant Joshi, Yogesh Munot, Umesh Bhise, Sunil Chavan, Sachin Shivatare, Sarvesh Patel, Vikas Gore
  • Publication number: 20090143356
    Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.
    Type: Application
    Filed: October 26, 2006
    Publication date: June 4, 2009
    Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Publication number: 20090124609
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: January 15, 2008
    Publication date: May 14, 2009
    Applicant: Amgen Inc.
    Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie Springer, Markian Stec, Ning Xi, Kevin Yang
  • Publication number: 20090082564
    Abstract: Magenta chromophore dyes which are stabilized by adding steric hindering groups to protect the imino carbons; nonlimiting examples of the steric hindering groups being phenyl, methyl, ethyl, isopropyl, fluoride, chloride, bromide and iodide groups.
    Type: Application
    Filed: September 24, 2008
    Publication date: March 26, 2009
    Inventor: Larrie A. Deardurff
  • Publication number: 20090082354
    Abstract: A pyrazolo[5,1-c][1,2,4]triazine compound of formula A: and pharmaceutically acceptable sats thereof. The multiply-substituted pyrazolo[5,1-c][1,2,4]triazine compounds of the invention selectively inhibit B-Raf kinase activity and are useful for treating disorders mediated by B-Raf kinase.
    Type: Application
    Filed: September 19, 2008
    Publication date: March 26, 2009
    Applicant: Wyeth
    Inventors: Dan Maarten Berger, Minu Dhanjisha Dutia, Darrin William Hopper, Nancy Torres
  • Patent number: 7507734
    Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
    Type: Grant
    Filed: November 16, 2006
    Date of Patent: March 24, 2009
    Assignee: Aventis Pharma S.A.
    Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
  • Patent number: 7473669
    Abstract: This invention relates to substituted dihydrotriazinones, triazinones and related compounds, compositions comprising such compounds and an agronomically acceptable carrier, and the use thereof as broad spectrum fungicides. This invention also teaches methods of preparing these compounds as well as methods of using the compounds as fungicides.
    Type: Grant
    Filed: May 3, 2006
    Date of Patent: January 6, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Steven Howard Shaber, Maurice Chee Hoong Yap, Kevin Gerald Meyer, Noormohamed Mohamed Niyaz, Brent Jeffrey Rieder, Michael Thomas Sullenberger, William Randal Erickson, Frisby Davis Smith
  • Patent number: 7470689
    Abstract: Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: December 30, 2008
    Assignee: Aventis Pharma S.A.
    Inventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Günter Müller, Cécile Combeau, Christine Delaisi, Anke Steinmetz, Ingrid Sassoon
  • Publication number: 20080312218
    Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.
    Type: Application
    Filed: September 21, 2006
    Publication date: December 18, 2008
    Inventors: Duane A. Burnett, Wen-Lian Wu
  • Patent number: 7462615
    Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.
    Type: Grant
    Filed: December 8, 2005
    Date of Patent: December 9, 2008
    Assignee: Hybrigenics SA
    Inventors: Philippe Guedat, Guillaume Boissy, Catherine Borg-Capra, Frédéric Colland, Laurent Daviet, Etienne Formstecher, Xavier Jacq, Jean-Christophe Rain, Rémi Delansorne, Ilaria Peretto, Stefano Vignando
  • Patent number: 7462614
    Abstract: The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
    Type: Grant
    Filed: March 29, 2004
    Date of Patent: December 9, 2008
    Assignee: Smithkline Beecham Corporation
    Inventors: Mui Cheung, Nigel Paul King, Kevin Wayne Kuntz, Robert Anthony Mook, Jr., Mark Andrew Pobanz, James Michael Salovich, Brian John Wilson
  • Publication number: 20080293723
    Abstract: There are provided spiroindolinone derivatives of the formula and pharmaceutically acceptable salts and esters thereof wherein R1, R2, R3, R4 and R are as herein described. The compounds exhibit anticancer activity.
    Type: Application
    Filed: April 11, 2008
    Publication date: November 27, 2008
    Inventors: Jin-Jun Liu, Zhuming Zhang
  • Publication number: 20080269110
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I where R1, R1a, R1b, A, R3, R4, R5, R5b and R6 are as defined herein.
    Type: Application
    Filed: April 25, 2008
    Publication date: October 30, 2008
    Inventors: William N. Washburn, Saleem Ahmad, Andres S. Hernandez
  • Patent number: 7419978
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.
    Type: Grant
    Filed: October 21, 2004
    Date of Patent: September 2, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, John Hynes, Katerina Leftheris, Shuqun Lin, Stephen T. Wrobleski, Hong Wu
  • Publication number: 20080176844
    Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or pharmaceutically acceptable salt, stereoisomer, or hydrate thereof, wherein R1 is lower alkyl, R2 and R3 are independently selected from lower alkyl, and lower alkenyl and lower alkynyl, wherein the lower alkyl, lower alkenyl, and lower alkynyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio, A is N or C—H, B is N, C—H, C—(SO2—R4), or C—CO—R4, D is N, C—H, C—(SO2—R4) or C—CO—R4, E is N or C—H, wherein only one of A, B or E may be N, and one of B or D is C—(SO2—R4) or C—CO—R4, R4 is a group having the formula: in which each R5, R6, R7 and R8 are independently selected from H and lower alkyl, wherein the lower alkyl may be optionally substituted with one or more halogen, lower alkoxy, hydroxy, CN, NO2, amino, acylamino, amido, carbonyl, and alkylthio; and additionally or alternatively R6 and R5
    Type: Application
    Filed: February 21, 2006
    Publication date: July 24, 2008
    Inventors: Stewart Campbell, David Duffy, Michael Grogan, Steven Kates, Emanuele Ostuni, Olivier Schueller, Paul Sweetnam
  • Publication number: 20080167287
    Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
    Type: Application
    Filed: November 19, 2007
    Publication date: July 10, 2008
    Applicant: INCYTE CORPORATION
    Inventors: Jincong Zhuo, Meizhong Xu, Chunhong He, Colin Zhang, Ding-Quan Qian, David M. Burns, Yun-Long Li, Brian Metcalf, Wenqing Yao
  • Publication number: 20080167304
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.
    Type: Application
    Filed: March 13, 2008
    Publication date: July 10, 2008
    Inventors: Jagabandhu Das, John Hynes, Katerina Leftheris, Shuqun Lin, Stephen T. Wrobleski, Hong Wu
  • Patent number: 7388019
    Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: June 17, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Charles G. Caldwell, Joseph L. Duffy, Robert J. Mathvink, Liping Wang, Ann E. Weber
  • Publication number: 20080103149
    Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use wherein R3, R4, R5, R6, Y, Het1, T, U, V, W, X, Ru, Rv and Rw are as defined in claim 1
    Type: Application
    Filed: October 30, 2006
    Publication date: May 1, 2008
    Inventors: Philippe GUEDAT, Xavier Jacq, Frederic Colland, Laurent Daviet, Etienne Formstecher, Jean-Christophe Rain, Matteo Colombo
  • Publication number: 20080096880
    Abstract: The invention relates to novel uses of imidazo[1,2,4]triazinones for producing a medicament for the treatment and/or prophylaxis of coronary cardiopathy, heart failure, pulmonary hypertension, bladder complaints, prostatic hyperplasia, nitrate-induced tolerance, or diseases of the eye, such as glaucoma, for the treatment or prophylaxis of central, retinal or posterior ciliary artery occlusion, central retinal vein occlusion, optical neuropathy, such as anterior ischaemic optical neuropathy and glaucomatous optical neuropathy, in addition to macular degeneration, diabetes, in particular diabetic gastroparesis, for the treatment of dysperistalsis of the stomach and oesophagus, female infertility, premature contractions, pre-eclampsia, alopecia, psoriasis associated with renal syndrome, cystic fibrosis, cancer and for improving cognition, powers of concentration, learning skills or hypermnesia, in particular if the disorder is a symptom of dementia.
    Type: Application
    Filed: June 24, 2003
    Publication date: April 24, 2008
    Applicant: Bayer Heakthcare AG
    Inventors: Helmut Haning, Erwin Bischoff, Ulrich Niewohner, Maria Niewohner
  • Publication number: 20080076921
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Application
    Filed: March 28, 2007
    Publication date: March 27, 2008
    Applicant: PHARMACYCLICS, INC.
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 7326475
    Abstract: The present invention provides: an organic EL element exhibiting high luminance, a high external quantum efficiency and a long high temperature driving life at 50° C.; an illuminator and a display device employing the organic EL element; and a material preferably used for the organic EL element.
    Type: Grant
    Filed: April 20, 2004
    Date of Patent: February 5, 2008
    Assignee: Konica Minolta Holdings, Inc.
    Inventors: Eisaku Katoh, Hiroshi Kita, Tomohiro Oshiyama, Mitsuhiro Fukuda, Yoshiyuki Suzuri, Noriko Ueda
  • Patent number: 7317012
    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 Formulas I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein B, R1, R2, R3 and x are described herein.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: January 8, 2008
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chongqing Sun, Yanting Huang, Doree F. Sitkoff, Guixue Yu, Amarendra Mikkilineni, William R. Ewing
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • Patent number: 7022847
    Abstract: The invention relates to a method for the production of 2-phenyl-substituted imidazotriazinones of general formula (I), comprising the reaction of compounds of formula (II) with compounds of formula (III) and subsequent reaction with iodine or bromine, then with a metal cyanide and reaction with an acid.
    Type: Grant
    Filed: December 5, 2001
    Date of Patent: April 4, 2006
    Assignee: Bayer HealthCare Aktiengesellschaft
    Inventors: Marc Nowakowski, Alexander Vetter
  • 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
  • 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
  • Patent number: 6998483
    Abstract: The present invention relates to a process for the preparation of sulphonamide-substituted imidazotriazinones of the general formula (I) characterized in that compounds of the formula (II) are reacted with sulphuric acid and the products obtained are then reacted with thionyl chloride and converted in situ in an inert solvent using an amine into the compounds according to the invention and, if appropriate, reacted to give the corresponding salts, hydrates or N-oxides.
    Type: Grant
    Filed: May 5, 2005
    Date of Patent: February 14, 2006
    Assignee: Bayer HealthCare Aktiengesellschaft
    Inventors: Marc Nowakowski, Reinhold Gehring, Werner Heilmann, Karl-Heinz Wahl
  • 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
  • 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
  • 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
  • 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
  • Patent number: 6943158
    Abstract: Compounds of formula I are p38 inhibitors: or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen or alkyl; R2 alkyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkyl, cyanoalkyl, heterocyclyl, heterocyclylalkyl, or —Y1—C(O)—Y2—R11 (where Y1 and Y2 are independently either absent or an alkylene group and R11 is hydrogen, alkyl, haloalkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino); R3 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterosubstituted cycloalkyl, heterocyclyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(?O)—R4 (where R4 is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino), or acyl; Ar1 is aryl; X1 is O, NR5 or S, where R5 is hydrogen or alkyl; and X2 is a bond, O, NR6, S or CH2, where R6 is hydrogen or alkyl.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: September 13, 2005
    Assignees: Roche Palo Alto LLC, Hoffmann-La Roche Inc.
    Inventors: Jian Jeffrey Chen, Kin-Chun Thomas Luk
  • 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