Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
  • Patent number: 10464907
    Abstract: The present invention relates to a novel compound having HSP90 inhibitory activity or a pharmaceutically acceptable salt thereof, and a medicinal use thereof, and composition comprising a dihydroxyphenyl compound or a benzamide compound, which is a novel compound having the HSP90 inhibitory activity of the present invention can effectively inhibit HSP90, and thus can be usefully used as a pharmaceutical composition for preventing or treating HSP90-mediated diseases or a health functional food for preventing or improving HSP90-mediated diseases, which selected from the group consisting of cancer diseases, degenerative neurological diseases and viral infections.
    Type: Grant
    Filed: January 31, 2017
    Date of Patent: November 5, 2019
    Assignee: INDUSTRY ACADEMIC COOPERATION FOUNDATION KEIMYUNG UNIVERSITY
    Inventor: Young Ho Seo
  • Patent number: 10463654
    Abstract: Provided are methods for treating cancer in a patient by administering at least one antibiotic selected from the group consisting of clofazimine, rifabutin and clarithromycin, in combination with an aryladamantane compound. In an embodiment, the aryladamantane compound is [3-(4-chlorophenyl)-adamantane-1-carboxylic acid (pyridin-4-ylmethyl)amide], or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: November 5, 2019
    Assignee: RedHill Biopharma Ltd.
    Inventors: Reza Fathi, Dror Ben-Asher, Danielle Abramson
  • Patent number: 10399924
    Abstract: Provided herein are deuterium substituted fumarate derivatives and pharmaceutical compositions comprising deuterium substituted fumarate derivatives. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a deuterium substituted fumarate derivative or a pharmaceutical composition comprising a deuterium substituted fumarate derivative. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: September 3, 2019
    Assignee: Biogen MA Inc.
    Inventor: Jianhua Chao
  • Patent number: 10265322
    Abstract: The present invention relates to the use of PAR1 antagonists, in particular of vorapaxar, of atopaxar and of 3-(2-chlorophenyl)-1-[4-(4-fluorobenzyl)piperazin-1-yl]propenone, or a pharmaceutically acceptable salt thereof, for preventing and/or treating pelvi-perineal functional pathological conditions, and more particularly painful bladder syndrome.
    Type: Grant
    Filed: April 25, 2018
    Date of Patent: April 23, 2019
    Assignee: Pierre Fabre Medicament
    Inventors: Bruno Le Grand, Didier Junquero, Nicolas Monjotin
  • Patent number: 9980970
    Abstract: The present invention relates to the use of PAR1 antagonists, in particular of vorapaxar, of atopaxar and of 3-(2-chlorophenyl)-1-[4-(4-fluorobenzyl)piperazin-1-yl]propenone, or a pharmaceutically acceptable salt thereof, for preventing and/or treating pelvi-perineal functional pathological conditions, and more particularly painful bladder syndrome.
    Type: Grant
    Filed: October 31, 2014
    Date of Patent: May 29, 2018
    Assignee: PIERRE FABRE MEDICAMENT
    Inventors: Bruno Le Grand, Didier Junquero, Nicolas Monjotin
  • Patent number: 9944650
    Abstract: The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: April 17, 2018
    Assignee: AstraZeneca AB
    Inventors: Robert Hugh Bradbury, Alfred Arthur Rabow, Michael James Waring, James Francis McCabe, Steven Christopher Glossop, Arshed Mahmood, Zoe Ann Cotter
  • Patent number: 9938262
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R6, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: April 10, 2018
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Andreas Goutopoulos, Thomas E. Richardson, Jiezhen Li, Brian H. Heasley, Pandi Bharathi
  • Patent number: 9908859
    Abstract: The invention relates to methods and compositions for the treatment or prevention of diseases and disorders associated with myeloproliferative disorders. In particular, the invention relates to an LSD 1 inhibitor for use in treating or preventing Philadelphia chromosome negative myeloproliferative disorders.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: March 6, 2018
    Assignee: Oryzon Genomics, S.A.
    Inventors: Jonathan Alleman Baker, Julio Castro Palomino, Matthew Colin Thor Fyfe, Tamara Maes, Marc Martinell Pedemonte
  • Patent number: 9907799
    Abstract: A tau aggregation inhibitor can sufficiently inhibit a tau protein from aggregating in cells. The inhibitor includes a 4-substituted catechol structure compound, having, at position 4 of its catechol ring, an electron-donating substituent R other than a hydrocarbon group, or a salt thereof. The 4-substituted catechol structure compound is preferably 4-aminocatechol or 1,2,4-benzenetriol. Examples of tauopathies to which this inhibitor is applicable include AD, Down's syndrome, frontotemporal dementia, cotricobasal degeneration (CBD) and progressive supranuclear palsy (PSP).
    Type: Grant
    Filed: April 2, 2014
    Date of Patent: March 6, 2018
    Assignees: THE DOSHISHA, National Center for Geriatrics and Gerontology
    Inventors: Tomohiro Miyasaka, Hachiro Sugimoto, Rie Tokizane, Yuki Shinzaki, Yohei Oe, Tetsuo Ota, Akihiko Takashima, Yoshiyuki Soeda, Yasuo Ihara, Yoshikazu Inoue
  • Patent number: 9675600
    Abstract: Methods of treating cancer related conditions using anamorelin are described.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: June 13, 2017
    Assignee: HELSINN HEALTHCARE SA
    Inventors: William Mann, John Friend, William Polvino, Suzan Allen, Ming Lu, Elizabeth Duus, Ruben Giorgino, Enrico Baroni
  • Patent number: 9637473
    Abstract: The invention relates to novel acrylamide derivatives of the formula I wherein R1, R2, R3, X, and ring A are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 2, 2017
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Hamed Aissaoui, Christoph Boss, Claire-Lise Ciana, Thierry Kimmerlin, Romain Siegrist
  • Patent number: 9289503
    Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: March 22, 2016
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Patent number: 9089532
    Abstract: The invention relates to improved and stable pharmaceutical formulations of phenylalanine derivatives and the use thereof as urokinase inhibitors, particularly for the treatment of malignant tumors and tumoral metastases.
    Type: Grant
    Filed: September 20, 2005
    Date of Patent: July 28, 2015
    Assignee: Wilex AG
    Inventors: Wolfgang Schmalix, Markus Bürgle, Klaus Koch
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150140075
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140081
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140077
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140079
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140078
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150140080
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Application
    Filed: January 30, 2015
    Publication date: May 21, 2015
    Applicant: SARCODE BIOSCIENCE INC.
    Inventors: Thomas Gadek, John Burnier
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Patent number: 9029381
    Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: May 12, 2015
    Assignee: Astrazeneca AB
    Inventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
  • Publication number: 20150126494
    Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 7, 2015
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Janet R. Sparrow, Rando Allikmets
  • Patent number: 8993577
    Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: March 31, 2015
    Assignee: Astrazeneca AB
    Inventor: Andrew Griffin
  • Publication number: 20150087629
    Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Publication number: 20150087645
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Application
    Filed: October 7, 2014
    Publication date: March 26, 2015
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Publication number: 20150079035
    Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 19, 2015
    Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
  • Publication number: 20150072984
    Abstract: Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 12, 2015
    Inventor: Xiangping Qian
  • Patent number: 8975235
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: March 10, 2015
    Assignee: InterMune, Inc.
    Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 8975399
    Abstract: A benzene sulphonamide compound of formula I or one of its addition salts with pharmaceutically acceptable acids, for its use in a method for treating a pathology linked to an excessive effect of TNF-alpha and for its use in a method for treating the human or animal body as a direct inhibitor of TNF-alpha.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: March 10, 2015
    Inventors: Jean-Francois Zagury, Matthieu Montes, Hadley Mouhsine, Helene Guillemain
  • Publication number: 20150065471
    Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
  • Patent number: 8969354
    Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: March 3, 2015
    Assignee: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
  • Publication number: 20150051144
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: September 26, 2012
    Publication date: February 19, 2015
    Inventors: Harikishore Pingali, Vrajesh Pandya
  • Publication number: 20150038493
    Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 5, 2015
    Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
  • Publication number: 20150038498
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 5, 2015
    Inventors: Timothy Allen Blizzard, Tesfaye Biftu
  • Patent number: 8946227
    Abstract: The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: February 3, 2015
    Assignee: Merck Serono SA
    Inventors: Sharad Magar, Andreas Goutopoulos, Yihua Liao, Matthias Schwarz, Russell J. Thomas
  • Publication number: 20150031635
    Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
    Type: Application
    Filed: June 30, 2014
    Publication date: January 29, 2015
    Inventors: Thomas E. Jenkins, Julie D. Seroogy, Jonathan W. Wray
  • Publication number: 20150031663
    Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.
    Type: Application
    Filed: October 13, 2014
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
  • Publication number: 20150018355
    Abstract: Compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating leukemia. In particular, compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating acute lymphoblastic leukemia (ALL) in its various forms.
    Type: Application
    Filed: March 13, 2013
    Publication date: January 15, 2015
    Inventors: Mark R. Kelley, Melissa L. Fishel, Angelo A. Cardoso
  • Publication number: 20150018335
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 7, 2013
    Publication date: January 15, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Patent number: 8933102
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
  • Publication number: 20150011565
    Abstract: The present invention relates to heterocyclic compounds useful for antagonizing angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperazine and diazepine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 8, 2015
    Inventors: Thomas David McCarthy, Alan Naylor
  • Publication number: 20140371235
    Abstract: A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing
    Type: Application
    Filed: October 10, 2012
    Publication date: December 18, 2014
    Applicant: University of Pittsburgh - Of the Commonweath System of Higher Education
    Inventors: Zhou Wang, Joel Byron Nelson, Minh Mindy Bao Nguyen, John S. Lazo, Paul A. Johnston, Peter Wipf
  • Publication number: 20140357648
    Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease and related disorders. In particular, the invention concerns compounds which, alone or in combination(s), can effectively modulate synapse function and/or angiogenesis and/or cell stress response. The invention also relates to methods of producing a drug or a drug combination for treating Alzheimer's disease and to methods of treating Alzheimer's disease or a related disorder.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: DANIEL COHEN, ILYA CHUMAKOV, SERGUEI NABIROCHKIN
  • Publication number: 20140356360
    Abstract: The present invention relates to piperazinyl derivatives of formula (I) and the use thereof as a drug, particularly for the treatment of cancer, the pharmaceutical compositions containing said derivatives, and the method for synthesising same.
    Type: Application
    Filed: December 28, 2012
    Publication date: December 4, 2014
    Inventor: Marc-Henry PITTY
  • Patent number: 8889686
    Abstract: L malate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are disclosed for decreasing the bitterness of eszopiclone dosage forms
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: November 18, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Patent number: 8889685
    Abstract: Maleate salts of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The salts are useful for treating sleep disorders.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: November 18, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: H. Scott Wilkinson, Richard Hsia, Tushar Misra, Kostas Saranteas, Patrick Mousaw
  • Publication number: 20140329833
    Abstract: The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.
    Type: Application
    Filed: May 21, 2012
    Publication date: November 6, 2014
    Applicant: ORYZON GENOMICS, S.A
    Inventors: Tamara Maes, Marc Martinell Pedemonte, Julio Castro-Palomino Laria
  • Publication number: 20140329834
    Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.
    Type: Application
    Filed: July 13, 2012
    Publication date: November 6, 2014
    Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard College
    Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
  • Publication number: 20140323467
    Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
    Type: Application
    Filed: May 23, 2014
    Publication date: October 30, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan