Bicyclo Ring Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.04)
Isoquinolines (including hydrogenated) (Class 514/253.05)
Quinolines (including hydrogenated) (Class 514/253.06)
  • PDE-10 INHIBITORS
    Publication number: 20110178083
    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: Application
    Filed: July 9, 2009
    Publication date: July 21, 2011
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS
    Publication number: 20110178082
    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: September 22, 2009
    Publication date: July 21, 2011
    Applicant: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Melanocortin Receptor-Specific Spiro-Piperidine Compounds
    Publication number: 20110178080
    Abstract: Melanocortin receptor-specific compounds of formula I below: wherein the variables are as defined in the specification, and enantiomers, diastereomers and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders.
    Type: Application
    Filed: March 29, 2011
    Publication date: July 21, 2011
    Applicant: PALATIN TECHNOLOGIES, INC.
    Inventors: Yi-Qun Shi, John H. Dodd, Elizabeth G. Rowley, Gary L. Olson, Axel Metzger
  • PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS
    Publication number: 20110178081
    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: September 22, 2009
    Publication date: July 21, 2011
    Applicant: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Benoit Laleu, Francesca Gaggini
  • Systems and Methods for Treating Pain Using Brain Stimulation
    Publication number: 20110171325
    Abstract: The invention comprises systems and methods for treating nociceptive pain including at least one force-regulatable device in mechanical, electrical, or chemical communication with at least one brain area identified as processing nociceptive pain signals. The force-regulatable device acts to alter the nociceptive pain signals in a brain area to alleviate nociceptive pain.
    Type: Application
    Filed: March 24, 2011
    Publication date: July 14, 2011
    Inventor: Andres Lozano
  • Substituted Imidazopyridinyl-Aminopyridine Compounds
    Publication number: 20110172203
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 29, 2010
    Publication date: July 14, 2011
    Applicant: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Yuko Yamamoto
  • 3-amino-pyrazolo[3,4b]pyridines as inhibitors of protein tyrosine kinases, their production and use as pharmaceutical agents
    Patent number: 7977325
    Abstract: This invention relates to compounds of general formula I in which R1 and R2 are described in this application, the use of the compounds of general formula I as inhibitors of protein tyrosine kinases for treatment of various diseases as well as the compounds of general formulas II and III as intermediate compounds for the production of compounds of general formula I, wherein X, R1a and R2a have the meaning that is described in general formulas II and III.
    Type: Grant
    Filed: December 14, 2005
    Date of Patent: July 12, 2011
    Assignee: Bayer Schering Pharma AG
    Inventors: Wolfgang Schwede, Hermann Kuenzer, Antonius Ter Laak, Benjamin Bader, Roman Hillig, Ursula Moenning, Arndt Schmitz, Dieter Zopf
  • Phenylacetamides being FLT3 inhibitors
    Patent number: 7977338
    Abstract: Compounds of formula wherein the residues R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, salts thereof; their use, methods of their use, processes for their production, pharmaceutical compositions comprising them, their combinations with second drug substances and the use thereof and the like. The compounds are protein kinase inhibitors and can be used for the treatment of diseases mediated by protein kinase inhibitors, e.g. for the treatment of various proliferative diseases.
    Type: Grant
    Filed: October 15, 2007
    Date of Patent: July 12, 2011
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano
  • TYMPANIC MEMBRANE PERMEATING EAR DROPS AND USES THEREOF
    Publication number: 20110166060
    Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.
    Type: Application
    Filed: May 19, 2009
    Publication date: July 7, 2011
    Applicants: Massachusettes Institute of Technology, Children's Medical Center Corporation
    Inventors: Emmanuel John Simons, Todd R. Hoare, Daniel S. Kohane, Robert S. Langer
  • NOVEL COMPOSITIONS AND METHODS OF USE
    Publication number: 20110166123
    Abstract: Described herein are novel enzyme inhibitors. In some embodiments the enzyme inhibitors are integrase inhibitors, particularly HIV integrase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV integrase as a method of treating or preventing HIV, AIDS or related disorders.
    Type: Application
    Filed: January 7, 2009
    Publication date: July 7, 2011
    Applicant: AARDEA BIOSCIENCES, INC.
    Inventors: Huanming Chen, Jianlin Song, Jean-Michel Vernier, Anthony B. Pinkerton, Johnny Y. Nagasawa
  • PYRIDOPYRAZINES AND DERIVATIVES THEREOF AS ALK AND c-MET INHIBITORS
    Publication number: 20110160204
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.
    Type: Application
    Filed: February 25, 2011
    Publication date: June 30, 2011
    Applicant: CEPHALON, INC.
    Inventors: Bruce D. Dorsey, Karen L. Milkiewicz, Douglas A. Pippin, Jay P. Theroff, Ted Underiner, Linda Weinberg, Craig A. Zificsak
  • SIRTUIN MODULATING COMPOUNDS
    Publication number: 20110152254
    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: January 24, 2011
    Publication date: June 23, 2011
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • PYRROLIDINYL-ALKYL-AMIDE DERIVATIVES, THEIR PREPARATION, AND THEIR THERAPEUTIC APPLICATION AS CCR3 RECEPTOR LIGANDS
    Publication number: 20110144104
    Abstract: The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands.
    Type: Application
    Filed: January 26, 2011
    Publication date: June 16, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Agnes BEHR, Sandor BATORI, Veronika BARTANE BODOR, Zoltan SZLAVIK, Imre BATA, Katalin URBAN-SZABO, Zoltan KAPUI, Endre MIKUS
  • BICYCLIC PYRAZOLO-HETEROCYCLES
    Publication number: 20110144121
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Application
    Filed: June 16, 2010
    Publication date: June 16, 2011
    Applicant: CARA THERAPEUTICS, INC.
    Inventor: Robert Zhiyong Luo
  • 3-(imidazolyl)-pyrazolo[3,4-b]pyridines
    Patent number: 7960388
    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: November 12, 2009
    Date of Patent: June 14, 2011
    Assignee: ChemoCentryx, Inc.
    Inventors: Lianfa Li, Andrew M.K. Pennell, Penglie Zhang
  • SIRTUIN MODULATING COMPOUNDS
    Publication number: 20110130387
    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: November 29, 2010
    Publication date: June 2, 2011
    Applicant: Sirtris Pharmaceuticals, Inc.
    Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch, Thomas Salzmann, David Armistead
  • Use of 7-azaindoles in the inhibition of c-Jun N-terminal kinase
    Patent number: 7951802
    Abstract: The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: May 31, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Piotr Pawel Graczyk, Paschalis Dimopoulos, Christopher Neil Farthing, Gurpreet Singh Bhatia, Afzal Khan
  • APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
    Publication number: 20110124628
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: November 22, 2010
    Publication date: May 26, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
  • Substituted pyrazolo[4,3-c]pyridine derivatives active as kinase inhibitors
    Patent number: 7947686
    Abstract: Substituted pyrazolo[4,3-c]pyridine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: May 24, 2011
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Tiziano Bandiera, Andrea Lombardi Borgia, Paolo Polucci, Manuela Villa, Marcella Nesi, Mauro Angiolini, Mario Varasi
  • PHARMACEUTICAL FORMULATIONS OF SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES WITH PROTEASE INHIBITORS
    Publication number: 20110118279
    Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
    Type: Application
    Filed: January 14, 2011
    Publication date: May 19, 2011
    Inventors: Tao Wang, Zhongxing Zhang, Nicholas A. Meanwell, John F. Kadow, Zhiwei Yin, Qiufen May Xue, Alicia Regueiro-Ren, John D. Matiskella, Yasutsugu Ueda
  • Novel Compounds
    Publication number: 20110118246
    Abstract: The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Application
    Filed: June 3, 2009
    Publication date: May 19, 2011
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • CARBAMOYL DERIVATIVES OF BICYCLIC CARBONYLAMINO-PYRAZOLES AS PRODRUGS
    Publication number: 20110118278
    Abstract: There are provided bicyclic carbonylamino-pyrazoles of formula (I), wherein the variables are as specified in the claims, for use as medicament, in particular for the treatment of diseases due to the malfunctioning of protein kinases (PKs), such as cancer, pharmaceutical compositions comprising such carbamoyl derivatives, and their use as prodrugs of therapeutically active agents. Method of treatment and some new bicyclic carbonylamino-pyrazoles are also object of the present invention.
    Type: Application
    Filed: May 14, 2009
    Publication date: May 19, 2011
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maurizio Pulici, Paolo Polucci
  • Microsatellite Markers of Schizophrenia
    Publication number: 20110117215
    Abstract: The invention includes method of determining if a subject is at risk for developing schizophrenia (SZ), schizotypal personality disorder (SPD), or schizoaffective disorder (SD).
    Type: Application
    Filed: January 21, 2011
    Publication date: May 19, 2011
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: Mark David Brennan, Jodi Ann Condra, Amy Tabb Massey, Wei Wei, Holly Neibergs
  • APOGOSSYPOLONE DERIVATIVES AS ANTICANCER AGENTS
    Publication number: 20110112112
    Abstract: The disclosure provides compounds and methods of using Apogossypolone derivatives for treating diseases and disorders. In particular, the disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt, hydrate, or solvate thereof, and provides methods for the preparation of compounds of Formula I; and methods for treating cancer, autoimmune diseases, and inflammation by administering a compound of Formula I.
    Type: Application
    Filed: October 7, 2010
    Publication date: May 12, 2011
    Applicant: Sanford-Burnham Medical Research Institute
    Inventors: Maurizio Pellecchia, Jun Wei
  • Quinolizidinone m1 Receptor Positive Allosteric Modulators
    Publication number: 20110112077
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: January 15, 2009
    Publication date: May 12, 2011
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. KUDUK, Ronald K, CHANG
  • RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20110110889
    Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: February 27, 2009
    Publication date: May 12, 2011
    Applicants: Array Bio Pharma Inc., Grenentech ,Inc.
    Inventors: Kateri A. Ahrendt et al., Alexander J. Buckmelter, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, David Moreno, Brad Newhouse, Li Ren, Steven M. Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
  • Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase
    Patent number: 7939527
    Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: May 10, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
  • Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators and methods of use thereof
    Publication number: 20110105498
    Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Application
    Filed: April 24, 2008
    Publication date: May 5, 2011
    Applicant: Amgen Inc.
    Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
  • COMPOUNDS AND METHODS FOR TREATMENT OF CANCER
    Publication number: 20110105497
    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: Application
    Filed: October 26, 2010
    Publication date: May 5, 2011
    Inventor: Anantha Sudhakar
  • DEAZAPURINES AND USES THEREOF
    Publication number: 20110105427
    Abstract: The present invention provides compounds having formula (I): wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally.
    Type: Application
    Filed: November 2, 2010
    Publication date: May 5, 2011
    Inventors: Jane Daun, Heather A. Davis, Bruce DeCosta, Fabian Gusovsky, Ieharu Hishinuma, Yimin Jiang, Toshihiko Kaneko, Kouichi Kikuchi, Seiichi Kobayashi, André Lescarbeau, Xiang-Yi Li, Kenzo Muramoto, Norihito Ohi, Marc Pesant, Boris M. Seletsky, Motohiro Soejima, Mark Spyvee, Lynda Tremblay, Ye Yao, Hiromitsu Yokohama, Yan (Janet) Zhao, Wanjun Zheng
  • AZAINDAZOLE COMPOUNDS AND METHODS OF USE
    Publication number: 20110098308
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: July 1, 2010
    Publication date: April 28, 2011
    Applicant: Chemocentryx, Inc.
    Inventors: Penglie Zhang, Andrew M.K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu, Mark M. Gleason, Yibin Zeng, Kevin Lloyd Greenman
  • ANTAGONIST OF SMOOTHENED
    Publication number: 20110098291
    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: Application
    Filed: May 4, 2010
    Publication date: April 28, 2011
    Applicant: Alla Chem Inc.
    Inventors: Alexander KHVAT, Sergey TKACHENKO, Ilya OKUN, Borys V. ROGOVOY, Nikolay SAVCHUK, John MAY, Patrick O'CONNOR, William RIPKA, Jean-Michel VERNIER, David MATTHEWS
  • Inhibitors of Protein Tyrosine Kinase Activity
    Publication number: 20110098293
    Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.
    Type: Application
    Filed: February 27, 2009
    Publication date: April 28, 2011
    Inventors: Michael Mannion, Stephane Raeppel, Stephen William Claridge, Frederic Gaudette, Lijie Zhan, Ljubomir Isakovic, Oscar Mario Saavedra, Tetsuyuki Uno, Masashi Kishida, Arkadii Vaisburg
  • 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives
    Patent number: 7932251
    Abstract: The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
    Type: Grant
    Filed: July 15, 2008
    Date of Patent: April 26, 2011
    Assignee: N.V. Organon
    Inventors: Jiaqiang Cai, Zoran Rankovic, Philip Stephen Jones, David Jonathan Bennett, Xavier Fradera
  • PYRAZOLE [3, 4-B] PYRIDINE RAF INHIBITORS
    Publication number: 20110092479
    Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: February 27, 2009
    Publication date: April 21, 2011
    Applicants: Array BioPharma Inc., Genentech, Inc.
    Inventors: Kateri A. Ahrendt, Alexandre J. Buckmelter, Jason De Meese, Jonas Grina, Joshua D. Hansen, Ellen R. Laird, Paul Lunghofer, David Moreno, Brad Newhouse, Li Ren, Jeongbeob Seo, Hongqi Tian, Steven M. Wenglowsky, Bainian Feng, Janet Gunzner, Kim Malesky, Simon Mathieu, Joachim Rudolph, Zhaoyang Wen, Wendy B. Young
  • ORGANIC COMPOUNDS
    Publication number: 20110092505
    Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
    Type: Application
    Filed: June 12, 2009
    Publication date: April 21, 2011
    Inventors: Robin Burgis, Michael Paul Capparelli, Lucian Dipietro, Gabriel G. Gamber, Charles Francis Jewell, JR., Erik Meredith, Karl Miranda, Lauren G. Monovich, Chang Rao, Nicolas Soldermann, Taeyoung Yoon, Qingming Zhu
  • Azaindazole Compounds As CCR1 Receptor Antagonists
    Publication number: 20110086846
    Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
    Type: Application
    Filed: December 16, 2010
    Publication date: April 14, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas COOK, Darren DiSALVO, Christian HARCKEN, Daniel KUZMICH, Thomas Wai-Ho LEE, Pingrong LIU, John LORD, Can MAO, Jochen NEU, Brian Christopher RAUDENBUSH, Hossein RAZAVI, Alan David SWINAMER
  • IMIDAZOPYRIDIN-2-ONE DERIVATIVES
    Publication number: 20110082138
    Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: November 24, 2010
    Publication date: April 7, 2011
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
  • PIPERAZINYL OXOALKYL TETRAHYDROISOQUINOLINES AND RELATED ANALOGUES
    Publication number: 20110082130
    Abstract: Piperazinyl oxoalkyl tetrahydroisoquinolines and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).
    Type: Application
    Filed: August 23, 2010
    Publication date: April 7, 2011
    Applicant: LIGAND PHARMACEUTICALS, INC.
    Inventors: Yang Gao, Bingsong Han, Yuelian Xu, Timothy M Caldwell, Linghong Xie
  • NOVEL IMIDAZOPYRIDINES
    Publication number: 20110071128
    Abstract: The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
    Type: Application
    Filed: September 21, 2010
    Publication date: March 24, 2011
    Inventors: Daniela Alberati, Rubén Alvarez Sánchez, Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • 1,3-DIHYDRO-2H-PYRROLO[3,2-b]PYRIDIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USES THEREOF
    Publication number: 20110071160
    Abstract: The subject matter of the present invention are compounds corresponding to formula (I): in which: X is an unsubstituted or substituted divalent (C1-C5)alkylene radical; R1 is an —NR8R9 group; or an unsubstituted or substituted piperidin-3-yl or piperidin-4-yl radical; R2 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R3 is a hydrogen atom, a halogen atom, an Alk group or an OAlk group; R4 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group; and R5 is a hydrogen atom, a halogen atom, an Alk group, a hydroxyl or an OAlk group.
    Type: Application
    Filed: October 15, 2010
    Publication date: March 24, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Cedric COUTURIER, Loic FOULON, Claudine SERRADEIL-LE GAL, Gerard VALETTE
  • BICYCLIC ARYL AND BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
    Publication number: 20110071133
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: December 1, 2010
    Publication date: March 24, 2011
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Thilo J. Heckrodt, Joane Litvak
  • TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES AND TRIAZOLOPYRIMIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
    Publication number: 20110071162
    Abstract: The disclosure relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
    Type: Application
    Filed: November 30, 2010
    Publication date: March 24, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Luc Even, Christian Hoornaert
  • TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
    Publication number: 20110071161
    Abstract: The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
    Type: Application
    Filed: November 30, 2010
    Publication date: March 24, 2011
    Applicant: SANOFI-AVENTIS
    Inventor: Christian HOORNAERT
  • Medication Combinations for the Treatment of Alcoholism and Drug Addiction
    Publication number: 20110065628
    Abstract: The present invention provides for the use of combinations of drugs to treat addictive disorders. More specifically, the present invention provides compositions and methods for treating disorders using combinations of drugs such as topiramate, ondansetron, and naltrexone.
    Type: Application
    Filed: May 20, 2008
    Publication date: March 17, 2011
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Bankole A. Johnson, Nassima Ait-Daoud Tiouririne, Wendy J. Lynch
  • Apoptosis promoters
    Patent number: 7906505
    Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
    Type: Grant
    Filed: May 3, 2010
    Date of Patent: March 15, 2011
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    Publication number: 20110059963
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: October 18, 2010
    Publication date: March 10, 2011
    Inventors: Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Shumeye Mamo, Chao Zhang, Jiazhong Zhang, James Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak, Hanna Cho, Samuel J. Gillette, Shenghua Shi
  • DUAL ACTION ANTIBIOTICS
    Publication number: 20110059946
    Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
    Type: Application
    Filed: September 10, 2010
    Publication date: March 10, 2011
    Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische Chemie
    Inventors: Christian Hubschwerlen, Jean-Luc Specklin
  • AZAINDOLE COMPOUNDS FOR TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS
    Publication number: 20110059982
    Abstract: Azaindole derivative compounds are described. The compounds have an optionally substituted azaindole core linked to a carbocyclic ring having at least one nitrogen atom and further bound to an optionally substituted aryl ring. A process for preparing these compounds, compositions comprising them, and methods of using them to treat disorders of the central nervous system are described.
    Type: Application
    Filed: February 14, 2009
    Publication date: March 10, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Timo Heinrich, Michael Katzer
  • 2-PHENYL SUBSTITUTED IMIDAZOL [4,5B] PYRIDINE/PYRAZINE AND PURINE DERIVATIVES AS GLUCOKINASE MODULATORS
    Publication number: 20110059941
    Abstract: Compounds of Formula (I), wherein R1-R10, A and X1 to X3 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
    Type: Application
    Filed: May 19, 2006
    Publication date: March 10, 2011
    Inventors: Peter William Rodney Caulkett, Darren McKerrecher, Nicholas John Newcombe, Kurt Gordon Pike, Michael James Waring