Additional Hetero Ring Containing Patents (Class 514/336)
The additional hetero ring is one of the cyclos in a polycyclo ring system (Class 514/337)
Ring nitrogen in the additional hetero ring (e.g., oxazole, etc.) (Class 514/340)
  • ULTRA LOW DOSE DOXEPIN AND METHODS OF USING THE SAME TO TREAT SLEEP DISORDERS
    Publication number: 20140107084
    Abstract: The invention relates to doxepin, pharmaceutically acceptable salts and prodrugs of doxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.
    Type: Application
    Filed: October 3, 2013
    Publication date: April 17, 2014
    Applicants: ProCom One, Inc., Somaxon Pharmaceuticals, Inc.
    Inventors: Philip Jochelson, Neil B. Kavey
  • INSECTICIDAL COMPOUNDS BASED ON ARYLTHIOACETAMIDE DERIVATIVES
    Publication number: 20140107161
    Abstract: The present invention provides compounds of formula (I) wherein R1, R2, 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: Application
    Filed: May 12, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
  • Pyridine derivatives as sphingosine 1-phosphate (S1P) receptor modulators
    Patent number: 8697733
    Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: June 20, 2013
    Date of Patent: April 15, 2014
    Assignee: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
  • COMPOUNDS AS TYROSINE KINASE MODULATORS
    Publication number: 20140100212
    Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 10, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Xialing Guo, Zhen Zhu
  • AQUAPORIN MODULATORS AND METHODS OF USING THEM FOR THE TREATMENT OF EDEMA AND FLUID IMBALANCE
    Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Aurora kinase modulators and method of use
    Patent number: 8686155
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
  • Thiazole derivatives as pesticides
    Patent number: 8686156
    Abstract: The present application relates to novel heterocyclic compounds, to their use for controlling animal pests including arthropods and in particular insects, and to processes for preparing the novel compounds.
    Type: Grant
    Filed: May 3, 2011
    Date of Patent: April 1, 2014
    Assignee: Bayer CropScience AG
    Inventors: Martin Füβlein, Thomas Bretschneider, Reiner Fischer, Peter Jeschke, Adeline Köhler, Joachim Kluth, Friedrich August Mühlthau, Arnd Voerste, Yoshitaka Sato
  • PHENICOL ANTIBACTERIAL AGENTS
    Publication number: 20140088046
    Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Application
    Filed: September 5, 2013
    Publication date: March 27, 2014
    Applicant: ZOETIS LLC
    Inventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
  • PRODRUGS OF DHODH INHIBITORS AND THEIR USES
    Publication number: 20140080768
    Abstract: The invention generally relates to Pro-Drugs of dihydroorotate dehydrogenase (DHODH) inhibitors and methods of use thereof. In certain embodiments, the invention provides a DHODH inhibitor compound including a cleavable functional group that increases bioavailability as compared to a form of the DHODH inhibitor without the functional group, rendering the former more suitable for therapeutic use.
    Type: Application
    Filed: September 19, 2012
    Publication date: March 20, 2014
    Inventors: Alan Palmer, Michael J. Hudson, Richard Todd, Patrick Camilleri
  • Epoxide inhibitors of cysteine proteases
    Patent number: 8673904
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: March 18, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • BRADYKININ B1 ANTAGONISTS
    Publication number: 20140073627
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Application
    Filed: November 7, 2013
    Publication date: March 13, 2014
    Applicant: EVOTEC AG
    Inventors: James MADDEN, David James HALLETT, Alastair PARKES, Ali RAOOF, Xiaolu WANG
  • COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRIDAE VIRAL INFECTIONS
    Publication number: 20140065103
    Abstract: A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 14, 2013
    Publication date: March 6, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: VERTEX PHARMACEUTICALS INCORPORATED
  • Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
    Patent number: 8664227
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: March 4, 2014
    Assignee: Theravance, Inc.
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
    Publication number: 20140057926
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM
  • FLUORO-PYRIDINONE DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS
    Publication number: 20140057919
    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: October 31, 2013
    Publication date: February 27, 2014
    Applicant: Pfizer Inc.
    Inventors: Usa Reilly, Michael Joseph Melnick, Matthew Frank Brown, Mark Stephen Plummer, Justin Ian Montgomery, Ye Che, Loren Michael Price
  • SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
    Publication number: 20140057920
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • SUBSTITUTED 4-PYRIDONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
    Publication number: 20140057916
    Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
  • Methods for treatment of kallikrein-related disorders
    Patent number: 8658685
    Abstract: We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: February 25, 2014
    Assignees: Activesite Pharmaceuticals, Inc., Joslin Diabetes Center
    Inventors: Lloyd P. Aiello, Tamie Jo Chilcote, Sukanto Sinha, Edward P. Feener
  • PYRIDONYL GUANIDINE F1F0-ATPASE INHIBITORS AND THERAPEUTIC USES THEREOF
    Publication number: 20140051727
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 20, 2014
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • 3-Arylamino Pyridine Derivatives
    Publication number: 20140051686
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: July 11, 2013
    Publication date: February 20, 2014
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • NOVEL 1,2- BIS-SULFONAMIDE DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS
    Publication number: 20140051682
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 24, 2013
    Publication date: February 20, 2014
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, Xiaoxia Liu, John E. Donello, Veena Viswanath
  • ACTIVE COMPOUND COMBINATIONS COMPRISING A (THIO)CARBOXAMIDE DERIVATIVE AND AN INSECTICIDAL OR ACARICIDAL OR NEMATICIDAL ACTIVE COMPOUND
    Publication number: 20140051576
    Abstract: The present invention relates to active compound combinations, in particular within an insecticide or fungicide composition, which comprises (A) a N-cyclopropyl-N-[substituted-benzyl]-3-(difluoromethyl)-5-fluoro-1-methyl-1H-pyrazole-4-carboxamide or thiocarboxamide derivative and a further insecticidally and/or acaricidally and/or nematicidal active compound (B). Moreover, the invention relates to a method for controlling animal pests such as insects and/or unwanted acarids and/or nematodes, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Application
    Filed: April 18, 2012
    Publication date: February 20, 2014
    Inventors: Peter Dahmen, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Elke Hellwege, Hendrik Helmke, Heike Hungenberg, Ulrike Wachendorff-Neumann
  • Active compound combination comprising azadirachtin and a substituted enaminocarbonyl compound
    Patent number: 8653110
    Abstract: Disclosed are novel active compound combinations comprising at least one substituted enaminocarbonyl compound and azadirachtin, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids. Methods of controlling insects and acarids are also disclosed.
    Type: Grant
    Filed: February 4, 2011
    Date of Patent: February 18, 2014
    Assignee: Bayer CropScience AG
    Inventors: Michael Kilian, Margit Doth
  • OLIGOMER-PROTEASE INHIBITOR CONJUGATES
    Publication number: 20140045770
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the small molecule drug not attached to the water-soluble oligomer.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Jennifer RIGGS-SAUTHIER, Lin Cheng, Tacey X. Viegas, Xuyuan Gu, Franco J. Duarte, Wen Zhang
  • NEW POSITIVE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTOR
    Publication number: 20140044806
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 13, 2014
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Compounds
    Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • INHIBITORS OF FLAVIVIRIDAE VIRUSES
    Publication number: 20140030223
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: September 25, 2013
    Publication date: January 30, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Martzman, Philip Anthony Morganelli, William J. Watkins, Hong Ye
  • CYCLIC SULFONIUM SALT, PROCESS FOR PRODUCTION OF SAME, AND alpha-GLUCOSIDASE INHIBITOR COMPRISING SAME
    Publication number: 20140031394
    Abstract: Provided is a novel cyclic sulfonium salt compound which is useful for the prevention or treatment of diabetes and the like. The present invention relates to a novel cyclic sulfonium salt compound represented by general formula (I) or (II), an isomer or solvate of the compound, or a pharmaceutically acceptable salt of the compound or the isomer or solvate. The present invention also relates to an ?-glucosidase inhibitor, a pharmaceutical composition for preventing or treating diabetes, and an anti-diabetes food, each of which comprises the compound represented by general formula (I) or (II) and the like.
    Type: Application
    Filed: January 31, 2012
    Publication date: January 30, 2014
    Applicants: DIABETYM CO., LTD., KINKI UNIVERSITY
    Inventors: Osamu Muraoka, Genzoh Tanabe
  • Heterocycle phenyl amide T-type calcium channel antagonists
    Patent number: 8637513
    Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Heteroaryl diamide compounds useful as MMP-13 inhibitors
    Patent number: 8637550
    Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
    Type: Grant
    Filed: November 5, 2009
    Date of Patent: January 28, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Sabine Schlyer, Lana Louise Smith Keenan, Steven John Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Zhaoming Xiong, Qiang Zhang
  • AMINOPYRIDINE COMPOUNDS AND THEIR USES
    Publication number: 20140024621
    Abstract: The invention generally relates to aminopyridines and methods of use thereof. In certain embodiments, the invention provides an aminopyridine or a pharmaceutically-acceptable salt thereof, in which the aminopyridine or the salt thereof includes a cleavable functional group that substantially prevents extra-hepatic hydrolysis.
    Type: Application
    Filed: July 23, 2012
    Publication date: January 23, 2014
    Applicant: MS THERAPEUTICS LIMITED
    Inventors: Michael J. Hudson, Alan Palmer, Richard Todd, Patrick Camilleri
  • ORGANIC COMPOUNDS
    Publication number: 20140024583
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: July 15, 2013
    Publication date: January 23, 2014
    Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
  • Compounds, Compositions, and Methods for Cancer Therapy
    Publication number: 20140024639
    Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.
    Type: Application
    Filed: July 19, 2013
    Publication date: January 23, 2014
    Inventors: Drew Adams, Mingji Dai, Stuart Schreiber, Mahmud Mustaqim Hussain, Zarko Boskovic
  • COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT
    Publication number: 20140023611
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: January 4, 2013
    Publication date: January 23, 2014
    Inventor: ARDELYX, INC.
  • Controlled Release Auris Sensory Cell Modulator Compositions and Methods for the Treatment of Otic Disorders
    Publication number: 20140018395
    Abstract: Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with auris sensory cell modulating agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).
    Type: Application
    Filed: June 26, 2013
    Publication date: January 16, 2014
    Applicants: The Regents of the University of California, Otonomy, Inc.
    Inventors: Jay Lichter, Andrew M. Trammel, Fabrice Piu, Qiang Ye, Michael Christopher Scaife, Benedikt Vollrath, Sergio G. Durón, Luis A. Dellamary, Carl Lebel, Jeffrey P. Harris
  • Methods for treating cognitive disorders
    Patent number: 8629165
    Abstract: Disclosed herein are methods of treating a patient suffering a cognitive disorder.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: January 14, 2014
    Assignees: Allergan, Inc., Exonhit Therapeutics SA
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • New positive allosteric modulators of nicotinic acetylcholine receptor
    Publication number: 20140010897
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 9, 2014
    Inventors: Anette Graven Sams, Jorgen Eskildsen, Ask Püschl
  • New positive allosteric modulators of nicotinic acetylcholine receptor
    Publication number: 20140010898
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 9, 2014
    Inventors: Jorgen Eskildsen, Anette Graven Sams, Ask Püschl
  • PHENOXY THIOPHENE SULFONAMIDES AND OTHER COMPOUNDS FOR USE AS INHIBITORS OF BACTERIAL GLUCURONIDASE
    Publication number: 20130345196
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.
    Type: Application
    Filed: May 24, 2012
    Publication date: December 26, 2013
    Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • INHIBITORS OF PROTEIN KINASES
    Publication number: 20130345233
    Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.
    Type: Application
    Filed: August 27, 2013
    Publication date: December 26, 2013
    Applicant: Ingenium Pharmaceuticals GmbH
    Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
  • Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
    Patent number: 8614206
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: December 24, 2013
    Assignee: F. Hoffmann-La Roche AG
    Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
  • HETEROARYLCARBOXYLIC ACID ESTER DERIVATIVE
    Publication number: 20130338132
    Abstract: Compounds represented by the following formula (I), are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: June 14, 2012
    Publication date: December 19, 2013
    Applicant: Ajinomoto Co., Inc.
    Inventors: Takahiro Koshiba, Munetaka Tokumasu, Taisuke Ichimaru, Koji Ohsumi, Tadakiyo Nakagawa, Tatsuhiro Yamada, Kayo Matsumoto, Tamotsu Suzuki
  • Pyridine compounds for controlling invertebrate pests I
    Patent number: 8609700
    Abstract: The present invention relates to novel pyridine compounds of the formulae I and II, to their salts, to their tautomers, to their N-oxides, and to the salts of these N-oxides or tautomers. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The invention further relates to plant propagation material and to agricultural compositions comprising said compounds. wherein A is a radical of the formulae A1 or A2 # denotes the binding site to the remainder of formulae I or II; n is 0, 1, 2 or 3; Z is O, S or N—RN; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and RA and RN, are as defined in claim 1.
    Type: Grant
    Filed: September 12, 2011
    Date of Patent: December 17, 2013
    Assignee: BASF SE
    Inventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh
  • HETEROARYL DERIVATIVES AS ALPHA7 NACHR MODULATORS
    Publication number: 20130331387
    Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: February 22, 2012
    Publication date: December 12, 2013
    Applicant: Lupin Limited
    Inventors: Neelima Sinha, Gourhari Jana, Sachchidanand Sachchidanand, Sanjay Pralhad Kurhade, Navnath Popat Karche, Anil Kashiram Hajare, Ajay Ramchandra Tilekar, Venkata P. Palle, Rajender Kumar Kamboj
  • SMALL MOLECULE INHIBITORS OF AGBL2
    Publication number: 20130331328
    Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.
    Type: Application
    Filed: February 14, 2012
    Publication date: December 12, 2013
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
  • INSECTICIDAL MIXTURES WITH IMPROVED PROPERTIES
    Publication number: 20130331417
    Abstract: The present invention relates to novel pesticidal compositions comprising the crystalline modification I of 4-{[(6-chloropyrid-3-yl)methyl](methyl)amino} furan-2(5H)-one and a insecticide, acaricide or nematicide that show surprisingly good insecticidal, acaricidal, nematicidal and fungicidal activities. In particular, these compositions are suited for the treatment of seed.
    Type: Application
    Filed: December 5, 2011
    Publication date: December 12, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Peter Jeschke, Robert Velten, Britta Olenik, Heike Hungenberg
  • Nanometer-sized prodrugs of NSAIDs
    Patent number: 8603531
    Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: December 10, 2013
    Assignee: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Anti-shock agent comprising diaminotrifluoromethylpyridine derivative
    Patent number: 8604212
    Abstract: Septic shock is known to lead to, at the end stage, systematic inflammatory reaction syndrome and multiple organ failure (MOF) and cause the patients' death. In both diseases, the patient dies finally of MOF, and the infiltration by inflammatory cells plays a key role for MOF. Thus, development of therapeutic agents for septic shock by suppressing the infiltration by inflammatory cells has been desired. To provide a therapeutic or preventive agent for shock, comprising as an active ingredient a diaminotrifluoromethylpyridine derivative represented by the formula (I) or its salt: wherein X is a cycloalkylcarbonyl group, an alkenylcarbonyl group, a thiophenecarbonyl group or a benzoyl group which may be substituted by a halogen atom; and Y is an alkylsulfonyl group.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: December 10, 2013
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Shuichi Yotsuya, Hiroshi Shikama
  • Alkaloid ester and carbamate derivatives and medicinal compositions thereof
    Patent number: 8604015
    Abstract: Compounds according to formula (I) are effective for the treatment of broncho-obstructive and inflammatory diseases.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: December 10, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Mauro Riccaboni, Daniele De Zani
  • COMPOUNDS USEFUL AS MODULATORS OF TRPM8
    Publication number: 20130324557
    Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
    Type: Application
    Filed: November 4, 2011
    Publication date: December 5, 2013
    Applicant: SENOMYX, INC.
    Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung