Ring Nitrogen Is Shared By The Two Cyclos Patents (Class 546/121)
  • PHARMACEUTICAL FORMULATIONS USEFUL IN THE TREATMENT OF INSOMNIA
    Publication number: 20130230589
    Abstract: There is provided a formulation suitable for transmucosal administration comprising a short acting hypnotic drug, which formulation provides a measurable plasma concentration of drug within 10 minutes of administration. The formulation is capable of providing sleep on demand, and preferably comprises particles of drug, for example zolpidem or a pharmaceutically-acceptable salt thereof and a mucoadhesion promoting agent, such as sodium carboxymethylcellulose, which particles of drug and mucoadhesive are presented upon the surface of larger carrier particles.
    Type: Application
    Filed: April 25, 2013
    Publication date: September 5, 2013
    Applicant: Orexo AB
    Inventors: Anders Pettersson, Christer Nystrom, Susanne Bredenberg
  • Bicyclic Heteroaryl Compounds
    Publication number: 20130231337
    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: September 5, 2013
    Applicant: 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 THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20130231344
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 4, 2013
    Publication date: September 5, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • COMPOUNDS AND COMPOSITIONS FOR MITIGATING TISSUE DAMAGE AND LETHALITY
    Publication number: 20130231518
    Abstract: Embodiments of the present invention provide compounds and compositions thereof, which are effective for mitigating tissue damage or lethality induced by an agent, and methods of making and using the same.
    Type: Application
    Filed: August 3, 2011
    Publication date: September 5, 2013
    Applicant: The Regents of the University of California
    Inventors: Robert H. Schiestl, Yelena O. Rivina, Michael E. Jung, Robert Damoiseaux
  • NOVEL CONJUGATES OF CC-1065 ANALOGS AND BIFUNCTIONAL LINKERS
    Publication number: 20130224227
    Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Application
    Filed: April 21, 2011
    Publication date: August 29, 2013
    Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgersma, Wiro Michael Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus de Groot
  • NEW BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND BETA-LACTAMASE INHIBITORS
    Publication number: 20130225554
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Application
    Filed: November 30, 2012
    Publication date: August 29, 2013
    Applicant: NAEJA PHARMACEUTICAL INC.
    Inventor: Naeja Pharmaceutical Inc.
  • IMIDOTHIAZOLE KINASE INHIBITORS
    Publication number: 20130225591
    Abstract: The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 29, 2013
    Inventors: Michelle R. Machacek, Sean P. Ahearn, Eric Romeo, Tony Siu, Stephanie Chichetti, Gabriela de Almeida, Alexey A. Rivkin
  • 5-Alkynyl Pyridine
    Publication number: 20130225567
    Abstract: 5-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.
    Type: Application
    Filed: February 19, 2013
    Publication date: August 29, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Ulrich REISER, Gerd BADER, Walter SPEVAK, Andreas STEFFEN, Alastair L. PARKES
  • Pyrazolo[1,5-a]pyridines as MARK inhibitors
    Patent number: 8518911
    Abstract: The invention encompasses pyrazolo[1,5-a]pyridine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason D. Katz, Sandra L. Knowles, James P. Jewell, David L. Sloman, Matthew G. Stanton, Njamkou Noucti
  • 2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
    Patent number: 8518943
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: August 27, 2013
    Assignee: UCB Pharma, S.A.
    Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
  • IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR 2 MODULATORS
    Publication number: 20130217720
    Abstract: The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2).
    Type: Application
    Filed: February 12, 2013
    Publication date: August 22, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Imidazo[1,2-a]pyridine compounds for use in treating cancer
    Patent number: 8513276
    Abstract: The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: August 20, 2013
    Assignee: Astex Therapeutics Limited
    Inventors: Valerio Berdini, Gilbert Ebai Besong, Owen Callaghan, Maria Grazia Carr, Miles Stuart Congreve, Adrian Liam Gill, Charlotte Mary Griffiths-Jones, Andrew Madin, Christopher William Murray, Rajdeep Kaur Nijjar, Michael Alistair O'Brien, Andrew Pike, Gordon Saxty, Richard David Taylor, Emma Vickerstaffe
  • IMIDAZOPYRIDINES SYK INHIBITORS
    Publication number: 20130210802
    Abstract: Certain imidazopyridines (I) and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.
    Type: Application
    Filed: March 11, 2011
    Publication date: August 15, 2013
    Applicant: Gilead Connecticut, Inc
    Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
  • Novel Heterocyclic Compounds and Uses Thereof
    Publication number: 20130210818
    Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 15, 2013
    Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
  • FUSED-IMIDAZOYL COMPOUNDS USEFUL AS ANTIMICROBIAL AGENTS
    Publication number: 20130210816
    Abstract: The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined herein. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and methods of using the compound of Formula (I) to treat microbial infections.
    Type: Application
    Filed: July 28, 2011
    Publication date: August 15, 2013
    Inventors: Tin-Yau Chan, Henry M. Vaccaro
  • Bicyclic pyridinylpyrazoles
    Patent number: 8507472
    Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: April 5, 2011
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Amos Mattes, Hendrik Helmke, Stefan Hillebrand, Gorka Peris, Alexander Sudau, Lars Rodefeld, Stefan Gauger, Jürgen Benting, Peter Dahmen, Ruth Meissner, Ulrike Wachendorff-Neumann, Hiroyuki Hadano
  • Polysubstituted 2-aryl-6-phenylimidazo[1,2-A]pyridine derivatives, and preparation and therapeutic use thereof
    Patent number: 8507520
    Abstract: Compounds of formula (I): wherein R, R1, R2, R3, R4, and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
    Type: Grant
    Filed: September 14, 2010
    Date of Patent: August 13, 2013
    Assignee: Sanofi
    Inventors: Danielle De Peretti, Yannick Evanno, Patrick Lardenois, Nathalie Rakotoarisoa, Antonio Almario Garcia, André Malanda
  • Compounds having affinity for amyloid
    Patent number: 8506930
    Abstract: The present invention provides a compound which has affinity with amyloid, shows sufficiently rapid clearance from normal tissues and is suppressed in toxicity such as mutagencity. Provided is a compound represented by the following formula (1) or a salt thereof: wherein A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a halogen substituent; R2 is a halogen substituent; and m is an integer of 0 to 2, provided that at least one of R1 and R2 is a radioactive halogen substituent, at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4 as well as a low-toxic diagnostic agent comprising a compound represented by the preceding formula or a salt thereof.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: August 13, 2013
    Assignee: Nihon Medi-Physics Co., Ltd.
    Inventors: Shigeyuki Tanifuji, Daisaku Nakamura, Shinya Takasaki, Yuki Okumura
  • Compounds for the treatment of hepatitis C
    Patent number: 8507683
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: August 13, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kap-Sun Yeung, John F. Kadow, Rajesh Onkardas Bora, Kumaravel Selvakumar
  • INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
    Publication number: 20130203747
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: November 21, 2012
    Publication date: August 8, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • 3 -AMINO- PYRAZOLE DERIVATIVES USEFUL AGAINST TUBERCULOSIS
    Publication number: 20130203802
    Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicyclic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: GLAXO GROUP LIMITED
    Inventors: Julia Castro Pichel, Raquel Fernandez Menendez, Esther Pilar Fernandez Velando, Silvia Gonzalez Del Valle, Araceli Mallo-Rubio
  • ISOINDOLINE PDE10 INHIBITORS
    Publication number: 20130203756
    Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: October 24, 2011
    Publication date: August 8, 2013
    Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
  • 2-Aryl Imidazo[1,2-a]Pyridine-3-Acetamide Derivatives, Preparation Methods and Uses Thereof
    Publication number: 20130203754
    Abstract: Disclosed are 2-arylimidazo[1,2-a]pyridine-3-acetamide derivatives represented by formula I, their tautomer, racemate or optical isomer, their pharmaceutically acceptable salt, or their solvates, wherein R1, R2, R3 and R4 are defined as in the specification.
    Type: Application
    Filed: June 9, 2011
    Publication date: August 8, 2013
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Rifang Yang, Yunfeng Li, Yongzhen Li, Nan Zhao, Liuhong Yun, Juanjuan Qin, Zhongyao Feng, Youzhi Zhang
  • Imidazopyridines and imidazopyrimidines as HIV-1 reverse transcriptase inhibitors
    Patent number: 8501767
    Abstract: The invention provides compounds of formula A or B which are useful in the treatment of a subject infected with HIV.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: August 6, 2013
    Assignee: CSIR
    Inventors: Moira Leanne Bode, Amanda Louise Rousseau, David Gravestock, Simon Sana Moleele, Christiaan Wynand Van Der Westhuyzen
  • COMPOSITIONS TO EFFECT NEURONAL GROWTH
    Publication number: 20130195816
    Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosed.
    Type: Application
    Filed: January 17, 2013
    Publication date: August 1, 2013
    Applicant: NEURALSTEM, INC.
    Inventor: NEURALSTEM, INC.
  • Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament
    Publication number: 20130197011
    Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
  • FATTY ACID SYNTHASE INHIBITORS
    Publication number: 20130196971
    Abstract: This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer.
    Type: Application
    Filed: September 15, 2011
    Publication date: August 1, 2013
    Inventors: Christopher Joseph Aquino, Dennis Heyer, Terence John Kiesow, David Lee Musso, Cynthia A. Parrish
  • 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.
  • Substituted Imidazo[1,2-a]pyrimidines and -pyridines
    Publication number: 20130190332
    Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.
    Type: Application
    Filed: July 7, 2011
    Publication date: July 25, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stuart Ince, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer, William Scott
  • SUBSTITUTED BENZALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION
    Publication number: 20130190315
    Abstract: Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 25, 2013
    Applicants: Global Blood Therapeutics, Inc., The Regents of the University of California, Cytokinetics, Inc.
    Inventors: Global Blood Therapeutics, Inc., Cytokinetics, Inc., The Regents of the University of California
  • SUBSTITUTED HETEROARYL ALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION
    Publication number: 20130190316
    Abstract: Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 25, 2013
    Applicants: Global Blood Therapeutics, Inc., The Regents of the University of California, Cytokinetics, Inc.
    Inventors: Global Blood Therapeutics, Inc., Cytokinetics, Inc., The Regents of the University of California
  • Azaazulene compounds
    Patent number: 8492374
    Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: July 23, 2013
    Assignee: Industrial Technology Research Institute
    Inventors: On Lee, Chih-Hung Chen, Chi-Y Hung, Yow-Lone Chang, Ting-Shou Chen
  • GSK-3? inhibitor
    Patent number: 8492378
    Abstract: For the purpose of providing a GSK-3? inhibitor containing an oxadiazole compound or a salt thereof or a prodrug thereof useful as an agent for the prophylaxis or treatment of a GSK-3?-related pathology or disease, the present invention provides a GSK-3? inhibitor containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: July 23, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Fumio Itoh, Jun Kunitomo, Hiromi Kobayashi, Eiji Kimura, Morihisa Saitoh, Tomohiro Kawamoto, Hiroki Iwashita, Katsuhito Murase
  • 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
  • NOVEL ALKYNYL DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
    Publication number: 20130178631
    Abstract: The present invention relates to novel compounds of formula I wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
    Type: Application
    Filed: July 13, 2012
    Publication date: July 11, 2013
    Applicant: Addex Pharma SA
    Inventor: Béatrice Bonnet
  • ARYLETHYNYL DERIVATIVES
    Publication number: 20130178456
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Imidazo[1,2 a] pyridine-6-carboxamide derivatives, their use for the treatment of colon cancer and their method of manufacture
    Patent number: 8481740
    Abstract: This invention relates to the manufacture of novel chemical compounds which have biological activity, particularly to novel chemical compounds that are cytotoxic against colon cancer cells and colon cancer cell lines. The manufacturing of said chemical compounds displaying anti-cancer properties employs the use of multi-component chemical reactions. The object of this invention is to manufacture and isolate analogues of imidazo[1,2-a]pyridine, namely compounds of Formula 1, which are cytotoxic against colon cancer cells, while concomitantly being relatively inactive against white blood cells. wherein, R is bromo, methyl, phenyl, nitro, hydrogen or an amide functional group; R1 is benzyl, 2,6-dimethylphenyl or cyclohexyl; and R2 is methoxy, benzyloxy or hydroxy.
    Type: Grant
    Filed: April 1, 2010
    Date of Patent: July 9, 2013
    Assignee: University of the Witwatersrand, Johannesburg
    Inventors: Nurit Esperance Farkas (Nee Dahan), Hajierah Davids, Candice Langley, Charles Bernard De Koning
  • 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
  • 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
  • FATTY ACID SYNTHASE INHIBITORS
    Publication number: 20130172384
    Abstract: This invention relates to the use of triazolone and triazolethione derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones and triazolethiones in the treatment of cancer.
    Type: Application
    Filed: September 15, 2011
    Publication date: July 4, 2013
    Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Jonathan M. Ghergurovich, David Lee Musso, Cynthia A. Parrish
  • 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
  • Crystalline forms of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide sodium salt
    Patent number: 8471025
    Abstract: The present invention relates to novel crystalline forms of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) thereof. The present invention relates to compositions comprising a crystalline form of sodium salt of trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide (e.g., NXL-104) alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil). Processes for the preparation of the crystalline forms and methods of treating bacterial infections by administering the crystalline forms alone or in combination with an antibacterial agent (e.g., ceftaroline fosamil) are also described.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: June 25, 2013
    Inventors: Mahendra G. Dedhiya, Sisir Bhattacharya, Véronique Ducandas, Alexandre Giuliani, Valérie Ravaux, Alain Bonnet, Alain Priour, Peter Lionel Spargo
  • Heteroaryl Nitrile Compounds Useful as Inhibitors of Cathepsin-S
    Publication number: 20130158018
    Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
  • Heterocyclic sulfonamide derivatives
    Patent number: 8466289
    Abstract: The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: June 18, 2013
    Assignee: Novartis AG
    Inventors: Mark G. Bock, Dinesh Chikkanna, Clive McCarthy, Henrik Moebitz, Chetan Pandit
  • IMINOPROPENE COMPOUND AND USE THEREOF
    Publication number: 20130150392
    Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.
    Type: Application
    Filed: February 8, 2013
    Publication date: June 13, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: SUMITOMO CHEMICAL COMPANY, LIMITED
  • 5-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE
    Publication number: 20130150584
    Abstract: The invention relates to a method of inhibiting abnormal cell growth or treating a hyperproliferative disorder in a mammal comprising administering to said mammal a therapeutically effective amount of an imidazopyridine of formula I with anti-hyperproliferative activity.
    Type: Application
    Filed: February 5, 2013
    Publication date: June 13, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Isoquinoline derivative
    Patent number: 8461329
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.
    Type: Grant
    Filed: December 25, 2009
    Date of Patent: June 11, 2013
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
  • POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20130143880
    Abstract: The present invention is directed to benzimidazolone 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: August 5, 2011
    Publication date: June 6, 2013
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Kenneth L. Arrington, Mark E. Layton, Alexander J. Reif, Kevin J. Rodzinak, Joseph E. Pero
  • 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
  • Substituted indolin-2-one derivatives and their use as P38 mitogen-activated kinase inhibitors
    Patent number: 8450341
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: May 28, 2013
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Victor Giulio Matassa