The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/253.01)
  • Patent number: 10507250
    Abstract: Method provided for labeling a nuclear medicine for imaging tracing, comprising a labeling precursor of the HDAC inhibitor BNL-26 (C22H23N3O) and the derivatives that are separated into two classes. The first class comprises a BNL-26 (C22H23N3O) and derivatives BNL-26a (C21H21N3O), BNL-26b (C22H22N2O), and other compounds of the labeling precursors which are categorized into two parts, the first part includes BNL-26-CH2CH2OTs (C31H33N3O4S), BNL-26a-CH2CH2OTs (C30H31N3O4S), and BNL-26b-CH2CH2OTs (C31H32N2O4S), which provides labeling precursor through —CH2CH2OTs structure, and the second part includes pre-BNL-26 (C28H34N3O3B), pre-BNL-26a (C27H32N3O3B), pre-BNL-26b (C28H33N2O3B), which provides labeling precursor through 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl structure. The second class includes BNL-26 (C22H23N3O) indole/indoline, which provides a series of derivative labeling precursors derived from a secondary amide bond.
    Type: Grant
    Filed: September 8, 2017
    Date of Patent: December 17, 2019
    Assignee: Institute of Nuclear Energy Research, Atomic Energy Council, Executive Yuan
    Inventors: Ming-Hsin Li, Chyng-Yann Shiue, Han-Chih Chang, Chun-Fang Feng
  • Patent number: 10450308
    Abstract: The disclosure relates to Compounds of Formula (I) and pharmaceutically acceptable derivatives thereof, where R1, R4, R8, R9, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, pain associated with osteoarthritis, osteoarthritis, UI, an ulcer, IBD, and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I) or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: October 22, 2019
    Assignees: Purdue Pharma L.P., Shionogi & Co. Ltd.
    Inventors: Shigeru Ando, Noriyuki Kurose, Laykea Tafesse
  • Patent number: 10208043
    Abstract: Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: February 19, 2019
    Assignees: Cornell University, Novita Pharmaceuticals, Inc.
    Inventors: Xin-Yun Huang, Christy Young Shue
  • Patent number: 10011595
    Abstract: The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. Such compounds are of the general structural formula I: The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: July 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Scott D. Kuduk, Nigel Liverton, Gang Zhou
  • Patent number: 9908907
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Grant
    Filed: June 28, 2016
    Date of Patent: March 6, 2018
    Assignee: Helsinn Healthcare SA
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J Stella
  • Patent number: 9546157
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general Formula I: or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: January 17, 2017
    Assignee: Helsinn Healthcare SA
    Inventors: Claudio Giuliano, Silvina Garcia Rubio, Antoine Daina, Angelo Guainazzi, Claudio Pietra
  • Patent number: 9409864
    Abstract: The invention discloses compounds of Formula (I). The compounds of formula (I) are TRPA1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of TRPA1 receptors.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: August 9, 2016
    Assignee: ARIO PHARMA LIMITED
    Inventors: Francesca Fruttarolo, Maria Giovanna Pavani, Serena Bencivenni, Raffaele Gatti, Mauro Napoletano
  • Patent number: 9358228
    Abstract: Combinations of netupitant and palonosetron, and methods of using such combinations to treat various pain states and irritable bowel syndrome, are provided.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: June 7, 2016
    Assignee: HELSINN HEALTHCARE SA
    Inventors: Claudio Pietra, Sergio Cantoreggi
  • Patent number: 9339498
    Abstract: Non-domesticated mammalian animals are sedated and immobilized by injecting an effective amount of pharmaceutically effective combination of nalbuphine hydrochloride and medetomidine hydrochloride into the animal from a dart. Azaperone tartrate may also be included, if desired.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: May 17, 2016
    Assignee: Wildlife Laboratories, Inc.
    Inventors: Lisa L. Wolfe, Michael W. Miller, William R. Lance, David K. Smith
  • Patent number: 9284275
    Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: March 15, 2016
    Assignee: CRITICAL OUTCOME TECHNOLOGIES INC.
    Inventor: Wayne R. Danter
  • Patent number: 9278954
    Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: March 8, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Niklas Heine, Martin Fleck, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 9181226
    Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, 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: July 17, 2012
    Date of Patent: November 10, 2015
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Jiezhen Li, Thomas E. Richardson, Pandi Bharathi, Brian H. Heasley, Andreas Goutopoulos
  • Patent number: 9115086
    Abstract: 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: Grant
    Filed: December 29, 2011
    Date of Patent: August 25, 2015
    Assignee: AGIOS PHARMACEUTICALS, INC.
    Inventors: Francesco G. Salituro, Jeffrey Saunders
  • Patent number: 9078894
    Abstract: The present invention relates to the treatment of severe persistent asthma, and in particular severe persistent corticosteroid-dependent or corticosteroid-resistant asthma, comprising administration a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: July 14, 2015
    Assignee: AB SCIENCE
    Inventors: Alain Moussy, Jean-Pierre Kinet
  • Patent number: 9073861
    Abstract: The present invention provides: a novel compound which has a useful pharmacological action for treating heart failure or shock without increasing heart rate; and a pharmaceutical composition using the same. The present invention relates to a diphenylmethyl piperazine derivative represented by general formula (I) (In the formula, R1 is a hydrogen atom or a hydroxy group. R2 is a hydrogen atom, a halogen atom, a hydroxy group, an alkyl group having one to five carbon atoms, or an alkoxyl group having one to five carbon atoms, excluding the case where R1 is a hydroxy group and R2 is a chlorine atom.) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: July 7, 2015
    Assignee: AETAS PHARMA CO., LTD.
    Inventor: Noboru Kaneko
  • Patent number: 9067921
    Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: June 30, 2015
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Ganfeng Cao, Taisheng Huang, Lihua Chen, Ke Zhang, Anlai Wang, David J. Meloni, Rajan Anand, Joseph Glenn, Brian W. Metcalf
  • Patent number: 9049874
    Abstract: The present invention relates to a method for the reduction of antibiotic usage in animals through the use of orally administered azaperone.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: June 9, 2015
    Assignee: Elanco Animal Health Ireland Limited
    Inventors: Rainier Johannes Hendrikus Van Gelderen, Peter Meerts
  • Patent number: 9034874
    Abstract: The invention relates to compound of the formula I or a salt thereof, wherein the substituents are as defined in the specification; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: May 19, 2015
    Assignee: NOVARTIS AG
    Inventors: Yves Auberson, Mark Gary Bock, Dario Braga, Marco Curzi, Stephanie Kay Dodd, Stefano Luca Giaffreda, Haiyang Jiang, Piotr Karpinski, Thomas J. Troxler, Tielin Wang, Xiaoyang Wang, Xuechun Zhang
  • 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
  • Publication number: 20150105386
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: October 24, 2014
    Publication date: April 16, 2015
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Muller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steven L. Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
  • Patent number: 8999989
    Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: April 7, 2015
    Assignee: R-Tech Ueno, Ltd.
    Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
  • Patent number: 8993574
    Abstract: The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: March 31, 2015
    Assignee: F2G Ltd
    Inventors: Graham Edward Morris Sibley, Robert Downham, Lloyd James Payne, Derek Law, Jason David Oliver, Mike Birch, Gareth Morse Davies, Patricia Suling Davies
  • Publication number: 20150080365
    Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 19, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 8980897
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: March 17, 2015
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli-Nollet
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8957215
    Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: February 17, 2015
    Assignee: Navidea Biopharmaceuticals, Inc.
    Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
  • Patent number: 8952012
    Abstract: Systems and methods for screening whether a candidate compound inhibits delta-6 desaturase activity are disclosed. Also disclosed is a transgenic mammal which overexpresses a gene encoding delta-6 desaturase and an animal model of a cardiometabolic disorder or disease that includes the transgenic mammal. A method of treating a cardiometabolic disorder or disease is also disclosed.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: February 10, 2015
    Assignee: Colorado State University Research Foundation
    Inventor: Adam J. Chicco
  • Patent number: 8952004
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R3, A, B, X, and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 5, 2011
    Date of Patent: February 10, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Ronald John Sorcek, Michael Robert Turner, Di Wu, Frank Wu
  • Publication number: 20150018366
    Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Inventor: Laykea TAFESSE
  • Publication number: 20150011551
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Applicant: Sanford- Burnham Medical Reseach Institute
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
  • Publication number: 20150005296
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
  • Publication number: 20140378429
    Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) (The chemical formulas should be inserted here) in which the variables are as described herein.
    Type: Application
    Filed: January 31, 2013
    Publication date: December 25, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
  • Publication number: 20140364389
    Abstract: The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.
    Type: Application
    Filed: December 12, 2013
    Publication date: December 11, 2014
    Applicant: JAPAN TOBACCO INC.
    Inventors: YUJI MATSUZAKI, WATARU WATANABE, SATORU IKEDA, MITSUKI KANO
  • Patent number: 8906924
    Abstract: The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: December 9, 2014
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Publication number: 20140356292
    Abstract: A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. An in vivo animal model for screening of a therapeutic agent for improving cognitive dysfunction by schizophrenia is provided.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: Sumitomo Dainippon Pharma Co., Ltd.
    Inventor: Takeo ISHIYAMA
  • Publication number: 20140357614
    Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xioahu Zhang
  • Patent number: 8901129
    Abstract: Disclosed are compounds and methods for treating neurological and other disorders by administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for GFR? receptor molecules, which can be mimetics of glial-derived neurotrophic factor (GDNF) family ligands (GFLs), GFR?/RET signaling pathway agonists, and/or direct RET agonists (activators).
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: December 2, 2014
    Assignee: GeneCode AS
    Inventors: Mart Saarma, Mati Karelson, Maxim Bespalov, Mehis Pilv
  • Publication number: 20140349986
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 27, 2014
    Applicant: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Publication number: 20140350012
    Abstract: The invention further 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 —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 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 C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Publication number: 20140350015
    Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 27, 2014
    Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
  • Patent number: 8895586
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: November 25, 2014
    Inventors: Luca Fadini, Peter Manini, Claudio Pietra, Claudio Giuliano, Emanuela Lovati, Roberta Cannella, Alessio Venturini, Valentino J. Stella
  • Patent number: 8895562
    Abstract: The present invention relates to piperazin-1-yl-trifluoromethyl-substituted-pyridines that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Michiel Luc Maria Van Gool
  • Patent number: 8889690
    Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: November 18, 2014
    Assignee: Purdue Pharma L.P.
    Inventor: Laykea Tafesse
  • Publication number: 20140336201
    Abstract: The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 13, 2014
    Inventors: Guenter HOELZEMANN, Dieter DORSCH, Alfred JONCZYK, Christiane AMENDT, Frank ZENKE
  • Patent number: 8877747
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 4, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Publication number: 20140323460
    Abstract: Disclosed are uses of carboxamide, sulfonamide and amine compounds for the treatment and amelioration of disorders and conditions related to oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. Also described are methods for increasing exercise endurance, exercise efficiency and aerobic workload using the compounds described herein.
    Type: Application
    Filed: July 7, 2014
    Publication date: October 30, 2014
    Inventors: Donald Payan, Yasumichi Hitoshi, Todd Kinsella
  • Patent number: 8871770
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: February 3, 2014
    Date of Patent: October 28, 2014
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Patent number: 8871768
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: October 28, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley P. Morgan, David J. Morgans, Alex Muci, Pu-Ping Lu, Erica A. Kraynack, Todd Tochimoto
  • Publication number: 20140315915
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed that have lower neurotoxicity effects than other compounds.
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. Hergenrother, Quinn Patrick Peterson, Danny Chung Hsu, Diana C. West, Timothy M. Fan, Chris J. Novotny