Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/222.8)
  • Patent number: 10687531
    Abstract: The present invention relates to compounds of formula (I) a compound of formula (1?) as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and to combat and control pests such as insect, acarine, mollusc and nematode pests.
    Type: Grant
    Filed: July 17, 2017
    Date of Patent: June 23, 2020
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Thomas Pitterna, André Jeanguenat, Fides Benfatti, Girish Rawal
  • Patent number: 10632198
    Abstract: A sterile aqueous formulation of a carbonic anhydrase inhibitor such as brinzolamide in combination with polymers like Soluplus® and a surfactant like polysorbate 80, as well as methods of preparation thereof, is disclosed. The formulation relates to the highly solubilized or an amorphous form of poorly insoluble drugs/active ingredient(s) to improve its bio-availability and manufacturability.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: April 28, 2020
    Assignee: SENTISS PHARMA PRIVATE LIMITED
    Inventors: Mandar V. Shah, Deepak Bahri
  • Patent number: 10604534
    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, R2, RA, ring A, ring C, and m are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: March 31, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Jared N. Cumming, Xing Dai
  • Patent number: 10588910
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating pulmonary arterial hypertension, which comprises an epidithiodioxopiperazine (ETP) compound or a derivative thereof, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 5, 2017
    Date of Patent: March 17, 2020
    Assignee: Vasthera Co. Ltd.
    Inventors: Sang Won Kang, Ki Hwan Kwon
  • Patent number: 10370336
    Abstract: The present invention is directed to phenylcyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: August 6, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Victoria Cofre, Antonella Converso, Kevin Rodzinak
  • Patent number: 10327446
    Abstract: The present invention relates to naphthyl- or isoquinolinyl-substituted isothiazoline compounds of formula I wherein the variables are as defined in the claims and description. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Grant
    Filed: June 23, 2014
    Date of Patent: June 25, 2019
    Assignee: BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC.
    Inventors: Pascal Bindschädler, Wolfgang Von Deyn, Karsten Körber, Deborah L. Culbertson, Koshi Gunjima, Franz Josef Braun
  • Patent number: 10314840
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: June 11, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Patent number: 10316028
    Abstract: The disclosures herein relate to novel compounds of formula wherein W, X and Y1, Y2, Y3 and Y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: June 11, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, John Andrew Christopher, Benjamin Gerald Tehan, Sukhbinder Singh Klair, Sarah Joanne Aves
  • Patent number: 10272093
    Abstract: Use of H3K9me3 modulation for enhancing cognitive function and treating anxiety related disorders is presented. A composition is administered to the subject comprising a therapeutically effective amount of a SUV39H1 inhibitor comprising analogs of ETP69. The therapeutically effective amount is effective in treating cognitive dysfunction in aging and age-related disorders.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: April 30, 2019
    Assignee: Regents of the University of California
    Inventors: Carl W. Cotman, Larry E. Overman, Shikha Snigdha
  • Patent number: 10154994
    Abstract: Ophthalmic formulations containing tyrosine kinase inhibitors, such as Nintedanib, Axitinib, Sorafenib, and Pazopanib are described. The ophthalmic formulations can contain microparticles or nanoparticles of the tyrosine kinase inhibitor. Also described are methods of using the ophthalmic formulations for treating ocular surface diseases, such pterygium, including recurrent pterygium, and hyperemia associated with pterygium.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: December 18, 2018
    Assignee: Allgenesis Biotherapeutics, Inc.
    Inventors: Tan Nguyen, Chin-yu Lai
  • Patent number: 9687015
    Abstract: The present invention includes compounds having structural formula (Ia): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: June 27, 2017
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald Karanewsky, Sara Werner, Vincent Darmohusodo, Jeff Yamamoto
  • Patent number: 9420814
    Abstract: The present invention includes compounds having structural formula (Ia): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: August 23, 2016
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald Karanewsky, Sara Werner, Vincent Darmohusodo, Jeff Yamamoto
  • Patent number: 9138013
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Grant
    Filed: August 1, 2014
    Date of Patent: September 22, 2015
    Assignee: Senomyx, Inc.
    Inventors: Catherine Tachdjian, Donald Karanewsky, Sara Werner, Vincent Darmohusodo, Jeff Yamamoto
  • Patent number: 9102688
    Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: August 11, 2015
    Assignee: Vifor (International) AG
    Inventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Christopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
  • Publication number: 20150126473
    Abstract: The present disclosure provides an isolated particle comprising very high density, ultra small, lipid depleted apo B containing particles, and may also contain cytokeratin 8. The isolated particle is useful in diagnostic assays, which are also provided.
    Type: Application
    Filed: June 14, 2012
    Publication date: May 7, 2015
    Applicant: Children's Hospital & Research Center at Oakland
    Inventors: Ronald M. Krauss, Mohmed Elfatih Ashmaig
  • Publication number: 20150126498
    Abstract: The disclosures herein relate to novel compounds of formula wherein W, X and Y1, Y2, Y3 and Y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.
    Type: Application
    Filed: July 3, 2013
    Publication date: May 7, 2015
    Inventors: Miles Stuart Congreve, John Andrew Christopher, Benjamin Gerald Tehan, Sukhbinder Singh Klair, Sarah Joanne Aves
  • Patent number: 9000151
    Abstract: The present invention includes compounds having structural formula (I): or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
    Type: Grant
    Filed: February 19, 2014
    Date of Patent: April 7, 2015
    Assignee: Senomyx, Inc.
    Inventors: Sara L. Adamski-Werner, Vincent Darmohusodo, Catherine Tachdjian, Donald S. Karanewsky
  • Publication number: 20150065492
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Application
    Filed: June 10, 2014
    Publication date: March 5, 2015
    Inventors: Peter Dragovich, Douglas E. Murphy
  • Publication number: 20150038496
    Abstract: The present invention relates to methods and pharmaceutical composition for the treatment of T-helper type 2 (Th2)-mediated diseases. More particularly, the present invention relates to an inhibitor of the Suv39h1-HP1a silencing pathway for use in the treatment of a T-helper type 2 (Th2)-mediated disease, in particular allergic asthma.
    Type: Application
    Filed: October 3, 2012
    Publication date: February 5, 2015
    Inventors: Sebastian Amigorena, Rhys Allan, Heidi Schreiber, Elina Zueva, Genevieve Almouzni
  • Publication number: 20150031684
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Application
    Filed: August 1, 2014
    Publication date: January 29, 2015
    Inventors: Catherine TACHDJIAN, Donald KARANEWSKY, Sara WERNER, Vincent DARMOHUSODO, Jeff YAMAMOTO
  • Publication number: 20150023907
    Abstract: The present invention provides new methods of treatment of lentiviral infections, more particularly to treat latent retroviral HIV infections, present in cells of the infected subject, based on the re-activation of said viruses. The invention uses a combination therapy using several agents that result in strong re-activation of the latent HIV-virus that could destroy the infected cells and elicite an immune response in the subject. This could present further spread of the infection, with the ultimate aim to eradicate the virus completely in said subject.
    Type: Application
    Filed: October 3, 2012
    Publication date: January 22, 2015
    Inventors: Carine Van Lint, Olivier Rohr, Sophie Bouchat, Jean-Stephane Gatot
  • Patent number: 8916551
    Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda
  • Publication number: 20140364424
    Abstract: The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases.
    Type: Application
    Filed: June 20, 2014
    Publication date: December 11, 2014
    Inventors: Wilm Buhr, Susanna Burckhardt, Franz Dürrenberger, Felix Funk, Peter O. Geisser, Vincent A. Corden, Stephen M. Courtney, Graham Dawson, Tara Davenport, Mark Slack, Mark P. Ridgill, Christopher J. Yarnold, Susan Boyce, Albertus A. Ellenbroek
  • Patent number: 8841292
    Abstract: Sudden cardiac arrest is treated by reducing blood temperature from about 37° C. to 33° C., following resuscitation, by injecting hypothermia inducing drugs such as a cannabinoid type into the patient's body, preferably in combination with physical surface body cooling.
    Type: Grant
    Filed: August 18, 2011
    Date of Patent: September 23, 2014
    Assignee: Weil Institute of Critical Care Medicine
    Inventors: Wanchun Tang, Shijie Sun
  • Patent number: 8835425
    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: Grant
    Filed: November 1, 2011
    Date of Patent: September 16, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rodolfo Gasser, Maria-Clemencia Hernandez, Andrew Thomas
  • Publication number: 20140243302
    Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 28, 2014
    Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
  • Patent number: 8815846
    Abstract: Compounds derived from imidazo[4,5-c][1,2,6]thiadiazine 2,2-dioxides, for use as a drug or pharmaceutical composition for treatment of parasitic diseases, preferably of diseases caused by parasites of the Trypanosoma genus, and more preferably for treatment of the Chagas disease. Furthermore, the invention also relates to the pharmaceutical compositions comprising said compounds.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: August 26, 2014
    Assignees: Universidad de la Republica de Uruguay, Consejo Superior de Investigaciones Cientificas
    Inventors: Juan Antonio Paez Prosper, Nuria Eugenia Campillo Martín, Ángela Guerra Álvarez, Maria Mercedes González Hormaizteguy, Hugo Cerecetto Meyer
  • Patent number: 8815847
    Abstract: The present invention describes [1,2,4]thiadiazine 1,1-dioxide compounds and pharmaceutically acceptable salts thereof, which are useful in lowering serum uric acid in a patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a [1,2,4]thiadiazine 1,1-dioxide compound.
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: August 26, 2014
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventor: James L. Freddo
  • Publication number: 20140234333
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases are therapeutically useful.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 21, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Kin Tso, Somasekhar Bhamidipati
  • Publication number: 20140235624
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Inventors: SARA L. ADAMSKI-WERNER, VINCENT DARMOHUSODO, CATHERINE TACHDJIAN, DONALD S. KARANEWSKY
  • Publication number: 20140235623
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Application
    Filed: November 12, 2013
    Publication date: August 21, 2014
    Applicant: SENOMYX, INC.
    Inventors: Catherine TACHDJIAN, Donald S. KARANEWSKY, Xiao-Qing TANG, Xiaodong LI, Feng ZHANG, Guy SERVANT, Qing CHEN, Vincent DARMOHUSODO, Richard FINE, Joseph R. FOTSING, Jeffrey Robert HAMMAKER, Xinshan KANG, Rachel D.A. KIMMICH, Boris KLEBANSKY, Haitian LIU, Goran PETROVIC, Marketa RINNOVA, Sara ADAMSKI-WERNER, Jeffrey YAMAMOTO, Hong ZHANG, Albert ZLOTNIK
  • Publication number: 20140221352
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • Patent number: 8785432
    Abstract: A single layer pharmaceutical composition comprising active agent(s) amlodipine or a pharmaceutically acceptable salt thereof and valsartan or a pharmaceutically acceptable salt thereof wherein the composition exhibits bioequivalence to the commercially available bilayer tablet dosage form comprising amlodipine besylate and valsartan; when administered to human subject, under the bioequivalence parameters of a 90% Confidence Interval for AUC which is between 80% and 125%, and a 90% Confidence Interval for Cmax, which is between 80% and 125%.
    Type: Grant
    Filed: February 21, 2008
    Date of Patent: July 22, 2014
    Assignee: Lupin Limited
    Inventors: Anirudha Bhagirath Kute, Nikhil Prabhakar Malewar, Makarand Krishnakumar Avachat
  • Patent number: 8778934
    Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: July 15, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda, Yasutomi Asano, Osamu Ujikawa, Michiyo Mochizuki
  • Patent number: 8754074
    Abstract: The present invention relates to the use of the vinyl quinuclidine enantiomer (R) of the following formula 2 as a synthesis intermediate in the preparation of (R)-mequitazine.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: June 17, 2014
    Assignees: Pierre Fabre Medicament, Commissariat a l'Energie Atomique et aux Energies Alternatives
    Inventors: Marc Nicolas, Laurent Larquetoux, Sébastien Leroux, Eric Doris
  • Publication number: 20140161785
    Abstract: Verticillin A is found to be a potent inhibitor of histone methyltransferases, selective for G9a, GLP, SUV39H1, SUV39H2, MLL1, and NSD2. Methods of using Verticillin A are provided. The Verticillin A can be synthetically produced or it can be isolated from natural sources. Methods if inhibiting one or more histone methyltransferases are provided. In addition, methods are provided for treating diseases or disorders related to overexpression of one or more histone methyltransferases. Exemplary diseases and disorders to be treated include cancer, asthma, HIV, and progeria.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 12, 2014
    Inventors: Feiyan Liu, Ping Wu, Kebin Liu
  • Publication number: 20140094453
    Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of modulating the sweet taste of compositions.
    Type: Application
    Filed: December 4, 2013
    Publication date: April 3, 2014
    Inventors: Catherine TACHDJIAN, Donald KARANEWSKY, Sara WERNER, Vincent DARMOHUSODO, Jeff YAMAMOTO
  • Publication number: 20140080817
    Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Application
    Filed: February 22, 2013
    Publication date: March 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masakuni KORI, Toshihiro IMAEDA, Shinji NAKAMURA, Masashi TOYOFUKU, Eiji HONDA, Yasutomi ASANO, Osamu UJIKAWA, Michiyo MOCHIZUKI
  • Publication number: 20140031345
    Abstract: A compound of formula I wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 30, 2014
    Inventors: James A. Johnson, John Lloyd, Heather Finlay, Ji Jiang, James Neels, Naveen Kumar Dhondi, Prashantha Gunaga, Abhisek Banerjee
  • Publication number: 20140023667
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of W, Z, R1H, R2, R3, R4, ring A, ring B, m, n, p, and -L1- is as defined herein. The novel compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: April 2, 2012
    Publication date: January 23, 2014
    Applicant: Merck, Sharp & Dohme Corp.
    Inventors: Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Publication number: 20140023668
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula: (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein each of ring A, ring B, ring C, R2, R3, R4, m, n, p, and -L1- is as defined herein. The novel compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: April 4, 2012
    Publication date: January 23, 2014
    Inventors: Jared N. Cumming, Eric J. Gilbert, Andrew W. Stamford
  • Patent number: 8633186
    Abstract: The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: January 21, 2014
    Assignee: Senomyx Inc.
    Inventors: Catherine Tachdjian, Donald S. Karanewsky, Xiao-Qing Tang, Xiaodong Li, Feng Zhang, Guy Servant, Qing Chen, Vincent Darmohusodo, Richard Fine, Joseph R. Fotsing, Jeffrey Robert Hammaker, Xinshan Kang, Rachel D. A. Kimmich, Boris Klebansky, Haitian Liu, Goran Petrovic, Marketa Rinnova, Sara Adamski-Werner, Jeffrey Yamamoto, Hong Zhang, Albert Zlotnik, Karen Zoller
  • Publication number: 20140011796
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • Publication number: 20130345126
    Abstract: The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
    Type: Application
    Filed: March 7, 2012
    Publication date: December 26, 2013
    Applicant: SANOFI
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
  • Publication number: 20130345128
    Abstract: The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia.
    Type: Application
    Filed: March 7, 2012
    Publication date: December 26, 2013
    Applicant: SANOFI
    Inventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Gerhard Kretzschmar, Kurt Ritter, Georg Tschank
  • Publication number: 20130338095
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: December 19, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Patent number: 8591885
    Abstract: Biocompatible intraocular drug delivery systems include a carbonic anhydrase inhibitor therapeutic agent and a polymeric component in the form of an implant, a microparticle, a plurality of implants or microparticles, and combinations thereof. The therapeutic agent is released in a biologically active form, for example, the therapeutic agent may retain its three dimensional structure when released into an eye of a patient, or the therapeutic agent may have an altered three. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy among others.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: November 26, 2013
    Assignee: Allergan, Inc.
    Inventors: James N. Chang, Patrick M. Hughes, Gerald W. Devries
  • Publication number: 20130310340
    Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.
    Type: Application
    Filed: May 15, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
  • Publication number: 20130310364
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: July 16, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Patent number: 8575154
    Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: November 5, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masakuni Kori, Toshihiro Imaeda, Shinji Nakamura, Masashi Toyofuku, Eiji Honda, Yasutomi Asano, Osamu Ujikawa, Michiyo Mochizuki