Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
  • Patent number: 8927534
    Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: January 6, 2015
    Assignee: Shire Orphan Therapies GmbH
    Inventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
  • Patent number: 8921399
    Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B 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 monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: April 16, 2012
    Date of Patent: December 30, 2014
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
  • Publication number: 20140377292
    Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue
  • Patent number: 8916569
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: December 23, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Patent number: 8916594
    Abstract: This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: December 23, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kyohei Hayashi, Yuusuke Tamura, Naoki Omori
  • Patent number: 8916553
    Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: December 23, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
  • Publication number: 20140371231
    Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
  • Publication number: 20140371227
    Abstract: The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.
    Type: Application
    Filed: September 14, 2012
    Publication date: December 18, 2014
    Applicants: The Scripps Research Institute, University of Kansas
    Inventors: Jeffrey Aube, Laura Bohn, Thomas Edward Prisinzano, Frank John Schoenen, Kevin John Frankowski
  • Publication number: 20140371222
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Patent number: 8912221
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: December 16, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
  • Publication number: 20140364408
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 29, 2012
    Publication date: December 11, 2014
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Patent number: 8907099
    Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.
    Type: Grant
    Filed: April 9, 2012
    Date of Patent: December 9, 2014
    Assignee: Bial-Portela & Ca, S.A.
    Inventors: David Alexander Learmonth, Laszlo Erno Kiss, Pedro Nuno Leal Palma, Humberto Dos Santos Ferreira, Patricio Manuel Vieira Araújo Soares da Silva
  • Publication number: 20140357675
    Abstract: Compounds are provided having an excellent hypoglycemic effect and ? cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shigeo Yamanoi, Hidenori Namiki, Yuichi Ochiai, Madoka Hoshino, Koji Matsumoto
  • Patent number: 8901121
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: December 2, 2014
    Assignee: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger
  • Publication number: 20140350058
    Abstract: The present invention relates to 3-[(pyridin-2-ylmethoxyimino)(phenyl)methyl]-2-substituted-1,2,4-oxadiazol-5(2H)-one derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Application
    Filed: December 19, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Braun, Pierre-Yves Coqueron, Christophe Dubost, Helene Lachaise, Simon Maechling, Anne-Sophie Rebstock, Philippe Rinolfi, Haruko Sawada, Ulrike Wachendorff-Neumann
  • Publication number: 20140350003
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: August 12, 2014
    Publication date: November 27, 2014
    Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
  • Publication number: 20140350026
    Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.
    Type: Application
    Filed: November 9, 2012
    Publication date: November 27, 2014
    Inventors: Xianjin Luo, Weidong Ye
  • Publication number: 20140350055
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: August 31, 2012
    Publication date: November 27, 2014
    Applicant: Amakem NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
  • Publication number: 20140349848
    Abstract: The present invention provides fungicidal 4-substituted-3-{phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I) wherein A represents a pyridyl or thiazole group and X1, Y1 to Y5 represent independently different substituents.
    Type: Application
    Filed: September 10, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Braun, Haruko Sawada, Helene Lachaise, Stephane Brunet, Philippe Rinolfi, Christophe Dubost, Pierre-Yves Coqueron, Simon Maechling, Anne-Sophie Rebstock, Ulrike Wachendorff-Neumann
  • Publication number: 20140350059
    Abstract: The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Inventors: Jae Keol RHEE, Weon Bin IM, Chong Hwan CHO, Sung Hak CHOI, Tae Ho LEE
  • Publication number: 20140350057
    Abstract: There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 27, 2014
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: Domenico Russo, Laszlo Erno Kiss, Jorge Bruno Reis Wahnon, David Alexander Learmonth, Tibor Eszenyi, Axel Zimmermann, Bjoern Schlummer, Michael Kreis, Klaus Reiter
  • Publication number: 20140349973
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: December 10, 2012
    Publication date: November 27, 2014
    Applicant: Viamet Pharmaceuticals, Inc
    Inventors: William J. Hoekstra, Christopher M. Yates
  • Patent number: 8895584
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: November 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth J. Wilson
  • Patent number: 8895587
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: November 25, 2014
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Publication number: 20140343031
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joesph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140343085
    Abstract: The present invention relates to the use of compounds of formula (I), wherein the variables are as defined in the description, in the free form or in salt form, for the manufacture of a medicament for controlling ectoparasites on a warm-blooded animal, wherein said medicament is administered orally to the animal at a dose of from 0.1 to 100 mg/kg from 30 minutes before to 3 hours after feeding the animal with an animal food.
    Type: Application
    Filed: November 23, 2012
    Publication date: November 20, 2014
    Applicant: Novartis AG
    Inventors: Cyril Desevaux, Martin Jung, Caroline Kablitz, Steve Nanchen
  • Publication number: 20140341850
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Applicant: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140343046
    Abstract: The present invention relates to the pharmaceutical use of selective GABA A ?5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: Rodolfo Gasser, Maria-Clemencia Hernandez, Andrew Thomas
  • Patent number: 8889665
    Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R3 and L are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Steffen Steurer, Irene Waizenegger
  • Patent number: 8889668
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: November 18, 2014
    Assignee: Merck Serono SA
    Inventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
  • Patent number: 8889720
    Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: November 18, 2014
    Assignee: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai
  • Patent number: 8889694
    Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: November 18, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
  • Publication number: 20140336142
    Abstract: Provided is a method of treating or preventing age-related macular degeneration (AMD) in a patient subject to, or symptomatic of the disease, wherein the method comprises restoring normal lysosomal pH (pHL), or acidifying an abnormally elevated pHL, thus decreasing or preventing a damaging accumulation of lipofuscin or waste products in the retinal pigment epithelium (RPE) cells of the eye of the patient. Further, this method is achieved by modulating the action of the P2X7 and/or P2Y12 receptors of the RPE cells, specifically decreasing the acidity (pHL) of the RPE lysosomes by administering selected receptor antagonists affecting the action of the P2X7 and/or P2Y12 receptors of the RPE. Methods for selecting and quantifying the effectiveness of drugs to restore pHL and determine outer segment clearance rates is also provided using a high through-put screening protocol.
    Type: Application
    Filed: July 30, 2014
    Publication date: November 13, 2014
    Inventors: Claire Mitchell, Alan Laties
  • Publication number: 20140336198
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 13, 2014
    Applicants: MERCK PATENT GMBH, BIONOMICS LIMITED
    Inventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
  • Publication number: 20140335201
    Abstract: The present invention provides a composition comprising a combination of components A) and B), wherein component A) is a compound of formula (I) and the component (B) is a further fungicide, insecticide or herbicide.
    Type: Application
    Filed: April 9, 2012
    Publication date: November 13, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Ulrich Johannes Haas, Dietrich Hermann, Gabriel Didier Scalliet, Kurt Nebel, Long Lu, Jianzhong Yang, Qiang Lu, Thomas James Hoffman, Renaud Beaudegnies, Werner Zambach, Olivier Jacob
  • Patent number: 8883827
    Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: November 11, 2014
    Assignee: Oslo University Hospital HF
    Inventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
  • Publication number: 20140329825
    Abstract: The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical combinations thereof, and their use as medicaments, particularly for the treatment of neurodegeneration, muscle atrophy or diabetes/metabolic syndrome via inhibition of HDAC4.
    Type: Application
    Filed: November 26, 2012
    Publication date: November 6, 2014
    Applicant: NOVARTIS AG
    Inventors: Christina Hebach, Joerg Kallen, Joachim Nozulak, Marina Tintelnot-Blomley, Leo Widler
  • Publication number: 20140329797
    Abstract: The present application relates to novel substituted 5-(1,2,4-oxadiazol-5-yl)pyridin-2-ones and 6-(1,2,4-oxadiazol-5-yl)pyridazin-3-ones, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for producing medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
    Type: Application
    Filed: October 16, 2012
    Publication date: November 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Unterschemmann
  • Patent number: 8877783
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: November 4, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Patent number: 8877782
    Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: November 4, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • Publication number: 20140323485
    Abstract: A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Ra, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Application
    Filed: September 14, 2012
    Publication date: October 30, 2014
    Applicant: NOVARTIS AG
    Inventors: Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Darren Mark LeGrand, Roger John Taylor
  • Publication number: 20140323524
    Abstract: Disclosed herein are anti-proliferative compounds which find use in inhibiting the growth of cancer cells. Also provided herein are methods for using these compounds for inhibiting growth of cancer cells. Also provided herein are methods for using these compounds for treating a subject for hyperproliferative conditions, including without limitation the treatment of hematopoietic cancers.
    Type: Application
    Filed: May 15, 2012
    Publication date: October 30, 2014
    Applicant: The Board Of Trustees of the Leland Stanford Junior University
    Inventors: Michael L. Cleary, Christina Matheny
  • Publication number: 20140322193
    Abstract: Unexpectedly, disorders of the cornea and conjunctiva are found to be caused or to be exacerbated, at least in part, by extracellular ATP and P2X7 receptor activation. Therapeutic compositions for topical administration to the eye for the treatment of disorders of the cornea and conjunctiva include an entity that inhibits P2X7 receptor function, reduces the effective concentration of extracellular ATP, or both.
    Type: Application
    Filed: December 1, 2012
    Publication date: October 30, 2014
    Inventor: Michael Kaleko
  • Publication number: 20140323486
    Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 30, 2014
    Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
  • Publication number: 20140315913
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, R4, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.
    Type: Application
    Filed: March 11, 2014
    Publication date: October 23, 2014
    Inventors: Venkataiah Bollu, James Breitenbucher, Alan Kaplan, Robert Lemus, Andrew Lindstrom, Troy Vickers, Mark E. Wilson, James Zapf
  • Publication number: 20140315946
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Arun K. Ghosh
  • Publication number: 20140315903
    Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: HASSAN JULIEN IMOGAI, JOSE MARIA CID-NUNEZ, JOSE IGNACIO ANDRES-GIL, ANDRES AVELINO TRABANCO-SUAREZ, JULEN OYARZABAL SANTAMARINA, FRANK MATTHIAS DAUTZENBERG, GREGOR JAMES MACDONALD, SHRILEY ELIZABETH PULLAN, ROBERT JOHANNES LUTJENS, GUILLAUME ALBERT JACQUES DUVEY, VANTHEA NHEM, TERRY PATRICK FINN, GAGIK MELIKYAN
  • Patent number: 8859462
    Abstract: Disclosed is a pest control composition comprising at least one pyripyropene derivative of formula (I) or agriculturally and horticulturally acceptable salt thereof and at least one other pest control agent as active ingredients. The combined use of the two ingredients can provide a better insecticidal effect.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: October 14, 2014
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Ryo Horikoshi, Kazuhiko Oyama, Mitsuyuki Yabuzaki
  • Patent number: 8859768
    Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: October 14, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Courtney A. Cullis, Krista E. Granger, Jianping Guo, Masaaki Hirose, Gang Li, Miho Mizutani, Tricia J. Vos
  • Publication number: 20140302069
    Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 9, 2014
    Inventors: David Fairlie, Robert C. Reid