The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/362)
Quinoline or isoquinoline (including hydrogenated) (Class 544/363)
  • POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20130210768
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2H-imidazo[4,5-b]pyridine-2-one derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. 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 metabotropic glutamate receptors are involved, such as schizophrenia.
    Type: Application
    Filed: June 6, 2011
    Publication date: August 15, 2013
    Inventors: Kenneth L. Arrington, Vadim Dudkin, Mark E. Layton, Joseph E. Pero, Alexander J. Reif
  • METHODS FOR THE PREPARATION OF HIV ATTACHMENT INHIBITOR PIPERAZINE PRODRUG COMPOUND
    Publication number: 20130203992
    Abstract: A method for making the compound is set forth utilizing the starting material
    Type: Application
    Filed: February 6, 2013
    Publication date: August 8, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • BICYCLIC HETEROARYL KINASE INHIBITORS AND METHODS OF USE
    Publication number: 20130203755
    Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
    Type: Application
    Filed: May 24, 2011
    Publication date: August 8, 2013
    Applicant: UNIVERSITY OF ROCHESTER
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
  • Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
    Patent number: 8501936
    Abstract: This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: August 6, 2013
    Assignee: Cephalon, Inc.
    Inventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
  • Bicyclic Heteroaryl Compounds
    Publication number: 20130196979
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: ARIAD Pharmaceuticals, Inc.
  • HETERO RING-FUSED IMIDAZOLE DERIVATIVE HAVING AMPK ACTIVATING EFFECT
    Publication number: 20130184240
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Application
    Filed: September 8, 2011
    Publication date: July 18, 2013
    Applicant: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • 3-(IMIDAZOLYL)-PYRAZOLO[3,4-B]PYRIDINES
    Publication number: 20130184289
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 3-imidazoyl-pyrazolo[3,4-b]pyridine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: January 4, 2013
    Publication date: July 18, 2013
    Applicant: ChemoCentryx Inc.
    Inventor: ChemoCentryx Inc.
  • Antagonist of smoothened
    Patent number: 8486936
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary diseases and disorders.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: July 16, 2013
    Assignee: AllaChem, LLC
    Inventors: Alexander Khvat, Sergey Tkachenko, Ilya Okun, Borys Rogovoy, Nikolay Savchuk, John May, Patrick O'Connor, William Ripka, Jean-Michel Vernier, David Matthews
  • 3-(imidazolyl)-pyrazolo[3,4-b] pyridines
    Patent number: 8481545
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 3-imidazoyl-pyrazolo[3,4-b]pyridine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: July 9, 2013
    Assignee: ChemoCentryx, Inc.
    Inventors: Lianfa Li, Andrew M. K. Pennell, Penglie Zhang
  • Bicyclic heterocyclyl derivatives as FGFR kinase inhibitors for therapeutic use
    Patent number: 8481531
    Abstract: The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: July 9, 2013
    Assignee: Astex Therapeutics Ltd
    Inventors: Gordon Saxty, Valerio Berdini, Eddy Jean Edgard Freyne, Alexandra Papanikos, Pascal Benderitter, Werner Constant Johan Embrechts, Berthold Wroblowski, Rhalid Akkari
  • PDE-10 inhibitors
    Patent number: 8481532
    Abstract: Vicinal substituted cyclopropyl 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, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT
    Publication number: 20130172360
    Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
    Type: Application
    Filed: January 27, 2012
    Publication date: July 4, 2013
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot, Anna Kruczynski, Philippe Schmitt, Michel Perez, Nicolas Rahier
  • Heteroaryl amide derivatives
    Publication number: 20130172549
    Abstract: Heteroaryl amide derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: January 29, 2013
    Publication date: July 4, 2013
    Applicant: H. Lundbeck A/S
    Inventor: H. Lundbeck A/S
  • QUINUCLIDINE ESTERS OF 1-AZAHETEROCYCLYLACETIC ACID AS ANTIMUSCARINIC AGENTS, PROCESS FOR THEIR PREPARATION AND MEDICINAL COMPOSITIONS THEREOF
    Publication number: 20130172302
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 4, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS
    Publication number: 20130172363
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Galderma Research & Development
  • SUBSTITUTED N- [1-CYANO-2- (PHENYL) ETHYL] -2-AZABICYCLO [2.2.1] HEPTANE-3-CARBOXAMIDE INHIBITORS OF CATHEPSIN C
    Publication number: 20130172327
    Abstract: Disclosed are N-1-cyano-2-(phenyl)ethyl)-2-azabicyclo[2.2.1]heptane-3-carboxamides of formula I and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory diseases.
    Type: Application
    Filed: September 14, 2012
    Publication date: July 4, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Marc GRUNDL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Doris RIETHER, Wolfgang WIENEN
  • NOVEL HETEROCYCLIC COMPOUND, AND COMPOSITION FOR TREATING INFLAMMATORY DISEASES USING SAME
    Publication number: 20130165652
    Abstract: The heterocyclic compound according to the present invention may treat and prevent inflammatory diseases and heal skin wounds, and particularly, have effects of recovering damaged skin barrier, reducing inflammation and pruritus in inflammatory skin diseases. In addition, the composition containing the compound according to the present invention as an active ingredient may be used to alleviate various inflammatory diseases and diseases in which PAR-2 is excessively expressed, and particularly, the composition may inhibit activity of PAR-2 in skin, such that the composition may be used as a composition having anti-inflammatory function in inflammatory skin diseases including atopic dermatitis, or the like.
    Type: Application
    Filed: August 25, 2011
    Publication date: June 27, 2013
    Applicant: NEOPHARM CO.,LTD.
    Inventors: Hyung Sub Gwak, Yong Zu Kim, Uk Il Kim, Byeong Deog Park, Tae Kyo Park, Sung Ho Woo, Joung Yul Yun, Dae Yon Lee, Hyang Sook Lee, Jeong Eun Jeon, Se Kyoo Jeong, Hyung Mook Choi
  • IMIDAZOPYRIDINE, IMIDAZOPYRIMIDINE AND IMIDAZOPYRAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS
    Publication number: 20130165426
    Abstract: Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 receptors.
    Type: Application
    Filed: July 5, 2011
    Publication date: June 27, 2013
    Applicant: UNIVERSITÉ DE MONTRÉAL
    Inventors: Réjean Ruel, Yves Chantigny, Anne Marinier, Patricia Rene, Michel Bouvier
  • CHEMICAL COMPOUNDS
    Publication number: 20130165439
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R5 are defined as in claim 1, which are suitable for treating diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: February 25, 2013
    Publication date: June 27, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Darryl MCCONNELL, Lars van der VEEN, Tobias WUNBERG
  • Substituted acetylenic imidazo[1,2-A]pyridine compounds as kinase inhibitors
    Patent number: 8470851
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: June 25, 2013
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
  • Compounds and methods for treatment of cancer
    Patent number: 8470817
    Abstract: Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using the compounds together with another chemotherapy, radiation therapy, hormonal therapy, biological therapy, or immunotherapy. Pharmaceutical compositions suitable for use in the methods are also disclosed.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: June 25, 2013
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventor: Anantha Sudhakar
  • Anellated pyridine compounds
    Patent number: 8470828
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: June 25, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Inhibitors of VEGF receptor and HGF receptor signalling
    Patent number: 8470850
    Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: June 25, 2013
    Assignee: MethylGene Inc.
    Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
  • NOVEL COMPOUNDS
    Publication number: 20130158042
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
    Type: Application
    Filed: December 10, 2012
    Publication date: June 20, 2013
    Inventors: Annekatrin HEIMANN, Georg DAHMANN, Marc GRUNDL, Stephan Georg MUELLER, Bernd WELLENZOHN
  • Substituted Triazolopyridines
    Publication number: 20130156756
    Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.
    Type: Application
    Filed: June 14, 2011
    Publication date: June 20, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Marcus Koppitz, Detlef Stöckigt, Olaf Prien
  • POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20130158002
    Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: February 28, 2011
    Publication date: June 20, 2013
    Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
  • AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES
    Publication number: 20130157941
    Abstract: The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances.
    Type: Application
    Filed: June 17, 2011
    Publication date: June 20, 2013
    Applicant: Sanofi
    Inventors: Stefan Petry, Norbert Tennagels, Karl-Heinz Baringhaus
  • THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
    Publication number: 20130150573
    Abstract: Novel processes for the preparation of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety and intermediates thereto are provided. The compounds prepared by the present processes may be useful, for example, as selective inhibitors of human MEK (MAPKK) enzymes, and are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.
    Type: Application
    Filed: February 6, 2013
    Publication date: June 13, 2013
    Applicant: UCB Pharma S.A.
    Inventor: UCB Pharma S.A.
  • 6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
    Publication number: 20130150340
    Abstract: The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 25, 2012
    Publication date: June 13, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • KINASE INHIBITORS
    Publication number: 20130150343
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • KINASE INHIBITORS
    Publication number: 20130150361
    Abstract: Compounds of formula (I): wherein R2, W, A, Y, and R1 are as defined in the specification, and pharmaceutically acceptable salts thereof, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
    Patent number: 8455485
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: June 4, 2013
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Selected inhibitors of protein tyrosine kinase activity
    Patent number: 8455484
    Abstract: The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: June 4, 2013
    Assignee: MethylGene Inc.
    Inventors: Stéphane Raeppel, Lijie Zhan, Stephen William Claridge, Franck Raeppel, Frédéric Gaudette, Arkadii Vaisburg
  • Therapeutic compounds
    Patent number: 8455477
    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: Grant
    Filed: July 27, 2009
    Date of Patent: June 4, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
  • Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
    Patent number: 8455486
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: June 4, 2013
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Novel Functionally Selective Ligands of Dopamine D2 Receptors
    Publication number: 20130137679
    Abstract: The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 30, 2013
    Inventors: Jian Jin, Bryan Roth, Stephen Frye
  • Thienopyridine Derivatives for the Treatment and Prevention of Dengue Virus Infections
    Publication number: 20130129677
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Application
    Filed: December 7, 2012
    Publication date: May 23, 2013
    Applicant: Siga Technologies, Inc.
    Inventor: Siga Technologies, Inc.
  • Azetidinyl diamides as monoacylglycerol lipase inhibitors
    Patent number: 8445477
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: May 21, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Pyrazolo Pyridine Derivatives as NADPH Oxidase Inhibitors
    Publication number: 20130123256
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: January 4, 2013
    Publication date: May 16, 2013
    Applicant: GENKYOTEX SA
    Inventor: Genkyotex Sa
  • HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THERAPEUTIC APPLICATION
    Publication number: 20130123271
    Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder.
    Type: Application
    Filed: June 22, 2011
    Publication date: May 16, 2013
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: David Middlemiss, Caroline Leriche
  • AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS
    Publication number: 20130123232
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: May 16, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventor: JANSSEN PHARMACEUTICA NV
  • NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS
    Publication number: 20130123237
    Abstract: Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: February 23, 2012
    Publication date: May 16, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Rajan Anand, James M. Apgar, Tesfaye Biftu, Ping Chen, Lin Chu, Vincent J. Colandrea, Guizhen Dong, James F. Dropinski, Danqing Feng, Jacqueline D. Hicks, Jinlong Jiang, Alexander J. Kim, Kenneth J. Leavitt, Bing Li, Xiaoxia Qian, Iyassu Sebhat, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • BICYCLIC PIPERAZINE COMPOUNDS
    Publication number: 20130116262
    Abstract: Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Imidazopyridin-2-one derivatives
    Patent number: 8436012
    Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: May 7, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
  • Pyrrolopyridine inhibitors of kinases
    Patent number: 8435980
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: May 7, 2013
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Jane Gong, Magdalena Przytulinska, Douglas Steinman, James Holms, Chunqiu Lai, Gui-Dong Zhu, Keith Woods
  • Heterocyclic compounds for the treatment of neurological and psychological disorders
    Patent number: 8431576
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: April 30, 2013
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Compounds that interact with glucokinase regulatory protein for the treatment of diabetes
    Patent number: 8431563
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: April 30, 2013
    Assignee: Amgen Inc.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • OXAZOLE TYROSINE KINASE INHIBITORS
    Publication number: 20130102592
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: December 5, 2012
    Publication date: April 25, 2013
    Applicant: SAREUM LIMITED
    Inventor: Sareum Limited
  • New Enzyme Inhibitor Compounds
    Publication number: 20130102587
    Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.
    Type: Application
    Filed: March 14, 2011
    Publication date: April 25, 2013
    Applicant: PROXIMAGEN LIMITED
    Inventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
  • ANTICANCER AGENT
    Publication number: 20130102776
    Abstract: An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6 alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6 alkyl group and the like; R4 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6 alkyl group and the like; R8 represents hydrogen atom, a C1-6 alkyl group and the like; A represents —O—, —S—, or —CH2—; D represents —C? or —N?; X represents methylene group, —O—, or —CO—; Q represents —N? or —C(R8)?; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.
    Type: Application
    Filed: April 28, 2011
    Publication date: April 25, 2013
    Applicants: RIKEN, THE UNIVERSITY OF TOKYO
    Inventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Nae Saito, Hirofumi Nakano, Masanao Abe, Akiko Tanaka, Teruki Honma, Shigeyuki Yokoyama, Keiko Tsuganezawa, Hitomi Yuki