The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/266.21)
Piperidinyl or tetrahydropyridyl (Class 514/266.22)
  • Compounds and methods of use
    Patent number: 8114893
    Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: February 14, 2012
    Assignees: Genentech, Inc., Abbott Laboratories, The Walter and Eliza Hall Medical Research Institute
    Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
  • SUBSTITUTED 2-AMINO-FUSED HETEROCYCLIC COMPOUNDS
    Publication number: 20120035194
    Abstract: The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: R1, R2, Z1, t, and ring A are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of JNK, such as diabetes, the method comprising administering to a mammal an effective amount of a compound of formula (I).
    Type: Application
    Filed: August 8, 2011
    Publication date: February 9, 2012
    Applicant: Pfizer Inc.
    Inventors: Liming Huang, Song Liu, Elizabeth A. Lunney, Simon P. Planken
  • 4,5-DIHYDRO-1H-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES
    Publication number: 20120022058
    Abstract: Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.
    Type: Application
    Filed: March 26, 2010
    Publication date: January 26, 2012
    Inventors: Graciela Barbieri Arhancet, Agustin Casimiro-Garcia, Xiangyang Chen, David Hepworth, Marvin Jay Meyers, David Walter Piotrowski, Raj Kumar Raheja
  • COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASES
    Publication number: 20120015905
    Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Inventor: Henrik C. Hansen
  • HETEROCYCLIC ANTIVIRAL COMPOUNDS
    Publication number: 20120009144
    Abstract: Compounds having the formula I wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: July 6, 2011
    Publication date: January 12, 2012
    Applicant: Roche Palo Alto LLC
    Inventors: Ryan Craig Schoenfeld, Francisco Xavier Talamas, Leanna Renee Staben
  • SUBSTITUTED QUINAZOLINE COMPOUNDS
    Publication number: 20120004210
    Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.
    Type: Application
    Filed: December 18, 2009
    Publication date: January 5, 2012
    Inventors: Caroline Leriche, Eric Auclair, Jacques Le Roux, David Middlemiss
  • Cyanoguanidines and cyanoamidines as ErbB2 and EGFR inhibitors
    Patent number: 8088766
    Abstract: Cyanoguanidine quinazoline and cyanoamidine quinazolamine derivatives that are useful in the treatment of hyperproliferative diseases are disclosed. Methods of treating hyperproliferative diseases in mammals are also disclosed.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: January 3, 2012
    Assignee: Array BioPharma Inc.
    Inventors: Eli Wallace, George Topolov, Qian Zhao, Joseph P. Lyssikatos
  • Compounds for Treating Disorders Mediated by Metabotropic Glutamate Receptor 5, and Methods of Use Thereof
    Publication number: 20110319380
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: December 17, 2010
    Publication date: December 29, 2011
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • METHODS OF TREATMENT OF BONE DEGENERATIVE DISEASES
    Publication number: 20110311519
    Abstract: Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazoline analogue such as halofuginone.
    Type: Application
    Filed: June 17, 2011
    Publication date: December 22, 2011
    Applicant: Washington University
    Inventors: Steven L. Teitelbaum, Carl J. DeSelm
  • QUINAZOLINONE, QUINOLONE AND RELATED ANALOGS AS SIRTUIN MODULATORS
    Publication number: 20110306612
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: September 29, 2009
    Publication date: December 15, 2011
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Chi B. Vu, Christopher Oalmann, Robert B. Perni, Brian White
  • PHARMACEUTICAL COMBINATIONS COMPRISING A MTOR INHIBITOR AND A RAF KINASE INHIBITOR
    Publication number: 20110301184
    Abstract: A pharmaceutical combination comprising an mTOR inhibitor and a Raf kinase inhibitor and its use.
    Type: Application
    Filed: August 11, 2011
    Publication date: December 8, 2011
    Applicant: NOVARTIS AG
    Inventor: Heidi Lane
  • 1,2-disubstituted heterocyclic compounds
    Patent number: 8071595
    Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: December 6, 2011
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASE
    Publication number: 20110294807
    Abstract: Disclosed are novel compounds that are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis. Also disclosed are pharmaceutical compositions comprising the novel compounds.
    Type: Application
    Filed: January 8, 2010
    Publication date: December 1, 2011
    Inventor: Henrik C. Hansen
  • 1H-QUINAZOLINE-2,4-DIONES
    Publication number: 20110294818
    Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.
    Type: Application
    Filed: July 28, 2011
    Publication date: December 1, 2011
    Inventors: Hans Allgeier, Yves Auberson, David Carcache, Philipp Floersheim, Christel Guibourdenche, Wolfgang Froestl, Jörg Kallen, Manuel Koller, Henri Mattes, Joachim Nozulak, David Orain, Johanne Renaud
  • METHODS AND COMPOSITIONS FOR INHIBITION OF THE TRANSITIONAL ENDOPLASMIC RETICULUM ATPASE
    Publication number: 20110288082
    Abstract: Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate.
    Type: Application
    Filed: May 6, 2011
    Publication date: November 24, 2011
    Inventors: Raymond J. Deshaies, Tsui-Fen Chou, Frank J. Schoenen, Kelin Li, Kevin J. Frankowski, Jeffrey Aube, Samuel W. Gerritz, Han-Jie Zhou
  • COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISEASES
    Publication number: 20110288077
    Abstract: This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? combinations thereof.
    Type: Application
    Filed: September 22, 2009
    Publication date: November 24, 2011
    Applicant: SCHERING CORPORATION
    Inventors: Michael K.C. Wong, Wensheng Yu, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Joseph A. Kozlowski, Seong Heon Kim, Guowei Zhou, De-Yi Yang, Razia K. Rizvi, Lei Chen, Aneta Maria Kosinski, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • LANTHIONINE SYNTHETASE COMPONENT C-LIKE PROTEINS AS MOLECULAR TARGETS FOR PREVENTING AND TREATING DISEASES AND DISORDERS
    Publication number: 20110275558
    Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.
    Type: Application
    Filed: May 4, 2011
    Publication date: November 10, 2011
    Applicant: Virginia Tech Intellectual Properties, Inc.
    Inventors: Josep BASSAGANYA-RIERA, Pinyi LU, Raquel HONTECILLAS
  • Small Molecules for Inhibition of Protein Kinases
    Publication number: 20110275645
    Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.
    Type: Application
    Filed: May 5, 2010
    Publication date: November 10, 2011
    Inventors: Renee Desai, Ketan Desai
  • HALOFUGINONE ANALOGS FOR INHIBITION OF TRNA SYNTHETASES AND USES THEREOF
    Publication number: 20110263532
    Abstract: The present invention provides novel analogs and derivatives of halofuginone. The invention also provides pharmaceutical and cosmetic compositions thereof and methods for using halofuginone analogs in treating chronic inflammatory diseases, autoimmune diseases, dry eye syndrome, fibrosis, scar formation, angiogenesis, viral infections, ischemic damage, transplant and implant rejection, neurodegenerative diseases, and cosmetic applications.
    Type: Application
    Filed: August 11, 2009
    Publication date: October 27, 2011
    Applicant: President and Fellows of Harvard College
    Inventors: Tracy Keller, Ralph Mazitschek, Malcolm Whitman, Jinbo Lee
  • NITROGEN-CONTAINING BICYCLIC HETEROARYL COMPOUNDS AND METHODS OF USE
    Publication number: 20110251199
    Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I and A1, A2, A3, A4, X, Z, Z?, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Application
    Filed: June 17, 2011
    Publication date: October 13, 2011
    Applicant: Amgen Inc.
    Inventors: Frenel F. De Morin, Jian J. Chen, Elizabeth M. Doherty, Stephen Hitchcock, Qi Huang, Joseph L. Kim, Gang Liu, Thomas Nixey, Nick A. Paras, Jeffrey Petkus, Daniel M. Retz, Adrian L. Smith, Jiawang Zhu
  • VIRAL POLYMERASE INHIBITORS
    Publication number: 20110230465
    Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 22, 2011
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
  • QUINAZOLINE INHIBITORS OF BACE 1 AND METHODS OF USING
    Publication number: 20110230505
    Abstract: Dihydroquinazoline compounds, compositions containing them, the use of the compounds and compositions for the treatment of Alzheimer's disease are described.
    Type: Application
    Filed: November 20, 2009
    Publication date: September 22, 2011
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Arun K. Ghosh
  • DI-SUBSTITUTED PHENYL COMPOUNDS
    Publication number: 20110224204
    Abstract: Di-substituted phenyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. The disclosure also relates to methods for treating neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: June 25, 2009
    Publication date: September 15, 2011
    Inventors: Richard Chesworth, Gideon Shapiro, Amy Ripka
  • Quinazolinone Compounds and Methods of Use Thereof
    Publication number: 20110217300
    Abstract: The present invention relates to quinazolinone compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising the quinazolinone compounds.
    Type: Application
    Filed: April 6, 2011
    Publication date: September 8, 2011
    Applicant: ARQULE, INC.
    Inventors: Jifeng Liu, Syed M. Ali, Mark A. Ashwell, Ping Ye, Yousheng Guan, Shi-Chung Ng, Rocio Palma, Dan Yohannes
  • Therapeutic Compounds
    Publication number: 20110207711
    Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.
    Type: Application
    Filed: July 27, 2009
    Publication date: August 25, 2011
    Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
  • PROTEIN KINASE MODULATORS AND METHOD OF USE
    Publication number: 20110201602
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
    Type: Application
    Filed: November 22, 2010
    Publication date: August 18, 2011
    Applicant: Amgen Inc.
    Inventors: Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Stuart C. CHAFFEE, Paul TEMPEST, Phillip R. OLIVIERI, Rebecca E. JOHNSON, Brian K. ALBRECHT, Vinod F. PATEL, Victor J. CEE, Joseph L. KIM, Steven BELLON, Xiaotian ZHU, Yuan CHENG, Ning XI, Karina ROMERO, Hanh Nho NGUYEN, Holly L. DEAK
  • QUINAZOLINONE DERIVATIVES USEFUL AS VANILLOID ANTAGONISTS
    Publication number: 20110195983
    Abstract: The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.
    Type: Application
    Filed: April 19, 2011
    Publication date: August 11, 2011
    Inventors: Timothy John Ritchie, Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart
  • Heterocyclic Kinase Inhibitors
    Publication number: 20110195956
    Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.
    Type: Application
    Filed: August 31, 2009
    Publication date: August 11, 2011
    Inventors: Matthew Burger, Jiong Lan
  • TRICYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20110189127
    Abstract: The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: June 10, 2009
    Publication date: August 4, 2011
    Inventors: Srikanth Venkatraman, Anilkumar Gopinadhan Nair, Kevin X. Chen, Francisco Valazquez, Qingbei Zeng, Duan Liu, Yueheng Jiang, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Stephen J. Gavalas, Patrick A. Pinto, Oleg B. Selyutin, Bancha Vibulbhan
  • Aryl-and Heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use
    Publication number: 20110190262
    Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.
    Type: Application
    Filed: November 14, 2008
    Publication date: August 4, 2011
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
  • 4-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    Patent number: 7989462
    Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: August 2, 2011
    Assignee: Myrexis, Inc.
    Inventors: Sui Xiong Cai, Mark B. Anderson, Adam Willardsen, Nilantha Sudath Sirisoma, Hong Zhang, Kazuyuki Suzuki
  • 5- AND 6-MEMBERED HETEROCYCLIC COMPOUNDS
    Publication number: 20110183976
    Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: June 25, 2009
    Publication date: July 28, 2011
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • IGF-IR antagonists as adjuvants for treatment of prostate cancer
    Patent number: 7972600
    Abstract: The present invention relates to a method of treating prostate cancer with androgen deprivation therapy and an insulin-like growth factor receptor (IGF-IR) antagonist. Although the response rate of prostate cancer to androgen deprivation therapy (ADT) is high, surviving cancer cells invariably become androgen independent (AI) and tumor growth follows. The invention inhibits or delays transition of androgen dependent cancer to androgen independent cancer, significantly decreases risk of recurrence, and improves treatment outcome.
    Type: Grant
    Filed: February 5, 2007
    Date of Patent: July 5, 2011
    Assignees: ImClone LLC, University of Washington
    Inventors: Dale L. Ludwig, Stephen R. Plymate
  • DIARYL-SUBSTITUTED FIVE-MEMBERED HETEROCYCLE DERIVATIVE
    Publication number: 20110160208
    Abstract: The present invention provides the compounds represented by formula (I): or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being useful for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.
    Type: Application
    Filed: March 7, 2011
    Publication date: June 30, 2011
    Applicant: Banyu Pharmaceutical Co., Ltd.
    Inventors: Yukari Hirata, Satoru Ito, Hiroshi Kawamoto, Toshifumi Kimura, Yasushi Nagatomi, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
  • CERTAIN CHEMICAL ENTITIES AND THERAPEUTIC USES THEREOF
    Publication number: 20110160232
    Abstract: Certain chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with PB kinase activity are described.
    Type: Application
    Filed: October 6, 2008
    Publication date: June 30, 2011
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson
  • INHIBITORS OF HUMAN METHIONINE AMINOPEPTIDASE 1 AND METHODS OF TREATING DISORDERS
    Publication number: 20110124649
    Abstract: Described herein are novel pyrimidine-pyridine compounds, methods of inhibiting methionine aminopeptidase and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, wherein a compound of the invention is administered to a subject.
    Type: Application
    Filed: November 10, 2008
    Publication date: May 26, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Jun O. Liu, Xiaoyi Hu, Xiaochun Chen, Dawei Ma, Shridhar Bhat
  • QUINAZOLIN-OXIME DERIVATIVES AS HSP90 INHIBITORS
    Publication number: 20110118258
    Abstract: Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.
    Type: Application
    Filed: May 15, 2008
    Publication date: May 19, 2011
    Inventors: Stephen Martin Courtney, Mark Whittaker, Owen Clifford Mather, Christopher John Yarnold, Oliver Robin Barker, Christian Aldo Georges Napoleon Montalbetti, Thomas Hesterkamp, Mihaly Daniel Gardiner
  • Heteroaryl sulfonamides and CCR2/CCR9
    Publication number: 20110118248
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: January 13, 2009
    Publication date: May 19, 2011
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
  • AZABICYCLOOCTYL-QUINAZOLONE DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
    Publication number: 20110112119
    Abstract: This invention relates to novel azabicyclooctyl-quinazolinone derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Application
    Filed: June 9, 2009
    Publication date: May 12, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Dan Peters, Daniel B. Timmermann, Elsebet Østergaard Nielsen, Gunnar M. Olsen, Tino Dyhring, Jeppe Kejser Christensen, Philip K. Ahring, John Paul Redrobe, Jens Damsgaard Mikkelsen
  • COMPOSITIONS AND METHODS RELATING TO HEAT SHOCK TRANSCRIPTION FACTOR ACTIVATING COMPOUNDS AND TARGETS THEREOF
    Publication number: 20110112073
    Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.
    Type: Application
    Filed: November 12, 2010
    Publication date: May 12, 2011
    Applicant: DUKE UNIVERSITY
    Inventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
  • TETRACYCLIC INDOLE DERIVATIVES AND THEIR USE FOR TREATING OR PREVENTING VIRAL INFECTIONS
    Publication number: 20110104109
    Abstract: The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: May 5, 2011
    Inventors: Frank Bennett, Qingbei Zeng, Srikanth Venkatraman, Mousumi Sannigrahi, Kevin X. Chen, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • SUBSTITUTED INDOLE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20110104110
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: May 5, 2011
    Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • INHIBITORS OF AKT ACTIVITY
    Publication number: 20110082135
    Abstract: The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.
    Type: Application
    Filed: May 27, 2009
    Publication date: April 7, 2011
    Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Yoshio Ogino, Yu Onozaki, Michael A. Rossi, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
  • C-Met Modulators and Method of Use
    Publication number: 20110077233
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Application
    Filed: October 25, 2010
    Publication date: March 31, 2011
    Applicant: Exelixis, Inc.
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
  • COMPOUNDS AS THE ESTROGEN RELATED RECEPTORS MODULATORS AND THE USES THEREOF
    Publication number: 20110071148
    Abstract: The compounds according to formula VIII, their pharmaceutically acceptable acid or base addition salts, and the uses thereof is disclosed. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for the preparing a medicament for modulating estrogen related receptor (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity, etc. The definition of the groups of the formula is defined as the description.
    Type: Application
    Filed: September 10, 2010
    Publication date: March 24, 2011
    Applicant: Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences
    Inventors: Ke Ding, Chiwai Wong, Zhanfang Kang, Xi Zhou
  • Active Compound Combinations Having Insecticidal and Acaricidal Properties
    Publication number: 20110053919
    Abstract: The novel active compound combinations comprising a compound of the formula (I) or (II) and the active compounds (1) to (6) listed in the description have very good insecticidal and acaricidal properties.
    Type: Application
    Filed: July 6, 2007
    Publication date: March 3, 2011
    Applicant: BAYER CROPSCIENE AG
    Inventors: Reiner Fischer, Wolfram Andersch, Thomas König, Anton Kraus, Emmanuel Salmon, Heike Hungenberg
  • 2-AMINOQUINAZOLINE DERIVATIVE
    Publication number: 20110039845
    Abstract: A 2-aminoquinazoline derivative represented by formula (I) {wherein R1 represents a hydrogen atom, or the like, R2 represents a hydrogen atom, R3 represents formula (II) [wherein A1 represents formula (III), or the like, R8 represents lower alkyl, or the like, and R9 represents optionally substituted aryl, or the like], R4 represents hydroxy, or the like, and R5 represents optionally substituted aryl, or the like}, or a pharmaceutically acceptable salt thereof is provided.
    Type: Application
    Filed: April 23, 2009
    Publication date: February 17, 2011
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Hajime Kashima, Tomoyuki Nishikawa, Yusuke Yamada, Toshihiro Seike, Yoshisuke Nakasato, Hiroshi Umehara
  • METHOD FOR EVALUATING PATIENTS FOR TREATMENT WITH DRUGS TARGETING RET RECEPTOR TYROSINE KINASE
    Publication number: 20110028498
    Abstract: The present invention provides a method of selection of a patient, who is a candidate for treatment with a RET drug, whereby to predict an increased likelihood of response to a RET drug. The invention provides a method for determining the sequence of RET. The method provides ARMS primers optimised for determining the sequence of RET. The invention also provides a diagnostic kit, comprising an ARMS primer.
    Type: Application
    Filed: September 6, 2007
    Publication date: February 3, 2011
    Inventors: Anderson Joseph Ryan, James Sherwood, Alan Wookey
  • QUINAZOLINONE DERIVATIVES AS TUBULIN POLYMERIZATION INHIBITORS
    Publication number: 20110028433
    Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, n, m and X have defined meanings.
    Type: Application
    Filed: March 26, 2009
    Publication date: February 3, 2011
    Applicants: JANSSEN PHARMACEUTICA NV, JANSSEN-CILAG
    Inventors: Eddy Jean Edgard Freyne, Laurence Anne Mevellec, Jorge Eduardo Vialard, Christophe Meyer, Elisabeth Thérèse Jeanne Pasquier, Xavier Marc Bourdrez, Patrick René Angibaud
  • QUINAZOLES USEFUL AS MODULATORS OF ION CHANNELS
    Publication number: 20110021495
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: January 15, 2010
    Publication date: January 27, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jesus Gonzalez, III, Dean Wilson, Andreas Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin Petzoldt, Lev T.D. Fanning, Timothy Neubert, Roger Tung, Esther Martinborough, Nicole Hilgraf