Abstract: Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
Type:
Grant
Filed:
February 8, 2008
Date of Patent:
January 20, 2015
Assignees:
Medivir AB, Janssen R&D Ireland
Inventors:
Pierre Jean-Marie Bernard Raboisson, Anna Karin Gertrud Linnea Belfrage, Björn Olof Classon, Karin Charlotta Lindquist, Karl Magnus Nilsson, Åsa Annica Kristina Rosenquist, Bertil Bengt Samuelsson, Horst Jürgen Wähling
Abstract: This invention relates to certain metabolites of N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide In particular, the present invention relates to pharmaceutical compositions comprising these metabolites, as well as processes for their preparation and their use in the treatment of diseases.
Abstract: Compound of Table I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
Type:
Application
Filed:
December 26, 2012
Publication date:
January 15, 2015
Applicant:
IRONWOOD PHARMACEUTICALS, INC.
Inventors:
Charles Kim, Takashi Nakai, Joel Moore, Nicholas Robert Perl, G-yoon Jamie Im, Timothy Claude Barden, Rajesh R. Iyengar, Daniel P. Zimmer, Angelika Fretzen, Paul Allan Renhowe
Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
Abstract: Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.
Abstract: Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.
Type:
Application
Filed:
July 8, 2014
Publication date:
January 8, 2015
Applicant:
MILLENNIUM PHARMACEUTICALS, INC.
Inventors:
Ashley Sue McCarron, Todd B. Sells, Matthew Stirling, Stephen G. Stroud
Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
Type:
Grant
Filed:
May 18, 2010
Date of Patent:
January 6, 2015
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1-R5, B and Z have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.
Type:
Application
Filed:
January 4, 2013
Publication date:
January 1, 2015
Inventors:
Koen Vandyck, Geerwin Yvonne Paul Haché, Geert Rombouts, Wim Gaston Verschueren, Pierre Jean-Marie Raboisson
Abstract: An arylalkyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group, a dioxolane group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; Y is CH or a nitrogen atom; q is an integer of 1 to 3; m is an integer of 0 to 5; and n is 0 or 1 or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.
Abstract: Provided are N-[(4-hydroxypiperidin-4-yl)methyl]pyridin-2(1H)-one derivatives represented by formula I, stereoisomers, pharmaceutically acceptable salts or solvates thereof. The above compounds have the dual activities of 5-hydroxytryptamine 1A receptor ligand and selective serotonin reuptake inhibitor. The preparation methods of the above compounds, the uses of these compounds for the prevention or treatment of nervous system diseases related to 5-hydroxytryptamine system dysfunction and the pharmaceutical compositions containing these compounds are also provided.
Type:
Grant
Filed:
April 8, 2011
Date of Patent:
December 30, 2014
Assignee:
Institue of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A., China
Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.
Abstract: Provided are an extended release preparation for oral administration of bosentan including bosentan, a pharmaceutically acceptable salt thereof or a solvate thereof as an active ingredient and a hydrophilic polymer as a sustained release excipient, and a method of manufacturing the same. Accordingly, the number of administrations of the bosentan, a pharmaceutically acceptable salt thereof or a solvate thereof may be reduced, thereby enhancing ease of administration and patient compliance. In addition, the extended release preparation for oral administration of bosentan may be effectively manufactured.
Type:
Application
Filed:
May 10, 2013
Publication date:
December 25, 2014
Inventors:
Sung Wuk Kim, Seong Choon Choi, Ja Seong Koo, Sang Ouk Sun, Na Young Lee
Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1 and R2 are as defined in the description, and the active compound groups (2) to (24) listed in the description have very good fungicidal properties.
Type:
Application
Filed:
September 3, 2014
Publication date:
December 18, 2014
Inventors:
Ulrike WACHENDORFF-NEUMANN, Peter DAHMEN, Ralf DUNKEL, Hans-Ludwig ELBE, Heiko RIECK, Anne SUTY-HEINZE
Abstract: The present invention relates to Pyrimidine Ether Derivatives, compositions comprising a Pyrimidine Ether Derivative, and methods of using the Pyrimidine Ether Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
Type:
Grant
Filed:
November 16, 2010
Date of Patent:
December 16, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Santhosh Francis Neelamkavil, Andrew Stamford, Samuel Chackalamannil, William J. Greenlee
Abstract: The present invention is directed to the provision of a multi-dose topical ophthalmic composition containing a 1H-indole-1-carboxamide and use thereof for treatment of ophthalmic disease. More specifically the present invention is directed to a multi-dose aqueous ophthalmic composition (e.g., a solution, a suspension, an emulsion or the like) containing a 1H-indole-1-carboxamide (e.g., N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino) methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide) and use thereof for treatment of an ophthalmic disease at the back of the eye such as age related macular degeneration (AMD).
Type:
Application
Filed:
May 30, 2014
Publication date:
December 11, 2014
Applicant:
Novartis AG
Inventors:
Malay Ghosh, Christopher Michael Adams, Stephanie Kay Dodd, Stephen Hedrick Poor
Abstract: The present disclosure describes a formulation including a nanoparticle including a polymer-associated strobilurin compound with an average diameter of between about 1 nm and about 500 nm; wherein the polymer is a polyelectrolyte, and a dispersant or a wetting agent. The disclosure describes various formulations and formulating agents that can be included in the formulations. Additionally, the disclosures describes application to various plants and fungi as well as advantages of the disclosed formulations.
Type:
Application
Filed:
August 23, 2012
Publication date:
December 11, 2014
Applicant:
VIVE CROP PROTECTION INC.
Inventors:
Fugang Li, Hung Hoang Pham, Rachel Gong, Henry Galas
Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
Type:
Grant
Filed:
August 5, 2010
Date of Patent:
December 9, 2014
Assignee:
Katholieke Universiteit Leuven
Inventors:
Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
Type:
Grant
Filed:
October 20, 2008
Date of Patent:
December 9, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Yan Xia, Craig D. Boyle, William J. Greenlee, Samuel Chackalamannil, Charles Lee Jayne
Abstract: Methods for therapeutic renal denervation are disclosed herein. One aspect of the present application, for example, is directed to methods that block, reduce and/or inhibit renal sympathetic nerve activity to achieve a reduction in central sympathetic tone. Renal sympathetic nerve activity may be altered or modulated along the afferent and/or efferent pathway. The achieved reduction in central sympathetic tone may carry several therapeutic benefits across many disease states.
Type:
Application
Filed:
June 6, 2014
Publication date:
December 4, 2014
Inventors:
Neil Barman, Howard Levin, Paul Sobotka, Mark Gelfand
Abstract: In one aspect, the invention relates to substituted N-phenylpyrimidin-2-amine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of Axl kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the Axl kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
March 31, 2012
Date of Patent:
December 2, 2014
Assignee:
University of Utah Research Foundation
Inventors:
David J. Bearss, Hariprasad Vankayalapati, Alexis Mollard, Steven L. Warner, Sunil Sharma
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
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.
Type:
Grant
Filed:
February 13, 2013
Date of Patent:
November 25, 2014
Assignee:
Janssen Pharmaceutica, NV
Inventors:
Steven J Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A Miskowski, Scott L. Dax, Henry J Breslin, Bart L. De Corte, Wei He
Abstract: This disclosure is directed to: (a) processes for preparing a compound and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.
Type:
Grant
Filed:
July 15, 2011
Date of Patent:
November 25, 2014
Inventors:
Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
Abstract: A benzyloxypyrimidine derivative represented by the formula (I) wherein R1 is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, an alkoxyalkyl group and the like; R2 and R3 are each a hydrogen atom, an alkyl group and the like; X is an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, a haloalkyl group, a haloalkenyl group, a haloalkynyl group, a trialkylsilyl group and the like; A is a oxygen atom and the like, and m is an integer of 0-5, or a salt thereof, and an agrohorticultural insecticide containing the compound as an active ingredient and a method of use thereof.
Abstract: The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Application
Filed:
September 12, 2012
Publication date:
November 20, 2014
Applicant:
MERCK PATENT GMBH
Inventors:
Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Lizbeth Celeste Deselm, Hui Qiu, Constantin Neagu, Donald Bankston, Christopher Charles Victor Jones
Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.
Type:
Application
Filed:
May 12, 2014
Publication date:
November 20, 2014
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
Abstract: Combinations, compositions and methods of use for modulating plant pathogen infection using plant extracts containing anthraquinone derivatives which induce resistance to plant phytopathogens and an antimicrobial agent, a biological control agent and/or a surfactant having fungicidal activity.
Type:
Grant
Filed:
July 29, 2010
Date of Patent:
November 18, 2014
Assignee:
Marrone Bio Innovations, Inc.
Inventors:
Hai Su, Marja Koivunen, Pamela G Marrone
Abstract: The present invention is directed to aryloxymethyl cyclopropane derivatives which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). 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:
Application
Filed:
May 21, 2012
Publication date:
November 13, 2014
Inventors:
Michael J. Breslin, Christopher D. Cox, Timothy J. Hartingh, Joseph Pero, Izzat T. Raheem, Michael Rossi, Laura Vassallo
Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
Type:
Application
Filed:
July 9, 2014
Publication date:
November 13, 2014
Inventors:
Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER
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
Abstract: A fungicidal composition containing a fungicidally effective amount of a compound of Formula I-V and at least one fungicide selected from the group consisting of epoxiconazole, prothioconazole, azoxystrobin, pyraclostrobin, penthiopyrad, isopyrazam, bixafen, boscalid, prochloraz, and chlorothalonil provides synergistic control of selected fungi.
Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
Type:
Application
Filed:
December 5, 2013
Publication date:
November 6, 2014
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Christopher Blackburn, Kenneth M. Gigstad, He Xu
Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Type:
Application
Filed:
July 26, 2012
Publication date:
November 6, 2014
Inventors:
Celia Dominguez, Leticia M. Toledo-Sherman, Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson
Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
Type:
Application
Filed:
May 3, 2014
Publication date:
November 6, 2014
Applicant:
INSCENT, INC.
Inventors:
Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
Abstract: This invention relates to aminopyrimidinone compounds of Formula (I) that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment or prevention of inflammatory diseases, including rheumatoid arthritis and inflammatory bowel disease.
Type:
Application
Filed:
October 26, 2012
Publication date:
November 6, 2014
Inventors:
W. Michael Seganish, Stephanie Nicole Brumfield, Jongwon Lim, Julius J. Matasi, William T. Mcelroy, Deen B. Tulshian, Brian J. Lavey, Michael D. Altman, Criag R. Gibeau, John William Lampe, Joey Methot, Liang Zhu
Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
Type:
Application
Filed:
May 3, 2014
Publication date:
November 6, 2014
Applicant:
INSCENT, INC.
Inventors:
Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
Abstract: Provided are novel selenyl-methyluracil compounds and a pharmaceutical composition for enhancing the effect of radiation treatment. The composition contains at least one compound selected from the group consisting of the selenyl-methyluracil compounds or pharmaceutically acceptable salts thereof, as an active ingredient.
Type:
Grant
Filed:
December 23, 2010
Date of Patent:
November 4, 2014
Assignee:
Kongju National University Industry-University Cooperation Foundation
Inventors:
In Seok Hong, Sung Hee Hong, Marc M. Greenberg
Abstract: The present invention relates to novel crystalline polymorphic and amorphous forms of the compound methyl (E)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxyacrylate (azoxystrobin). Infrared Raman spectra, X-Ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops.
Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
December 8, 2009
Date of Patent:
November 4, 2014
Assignee:
Merck Patent GmbH
Inventors:
Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
Abstract: The present invention provides methods to reduce or inhibit weight gain by administering inhibitors of the SirT1 protein to a subject. Methods to identify such inhibitors are also disclosed.
Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
Type:
Application
Filed:
April 29, 2014
Publication date:
October 30, 2014
Applicant:
Ironwood Pharmaceuticals Inc.
Inventors:
Charles KIM, Takashi NAKAI, Thomas Wai-Ho LEE, Joel MOORE, Nicholas Robert PERL, Jason ROHDE, Rajesh R. IYENGAR, Ara MERMERIAN, Angelika FRETZEN
Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.
Type:
Grant
Filed:
December 10, 2009
Date of Patent:
October 28, 2014
Assignees:
Topharman Shanghai Co., Ltd., Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Topharman Shandong Co., Ltd.
Abstract: Compounds of formula (I) and their use as pharmaceutical.
Type:
Application
Filed:
December 17, 2012
Publication date:
October 23, 2014
Inventors:
Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernandez-Montalvan, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuße
Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Type:
Application
Filed:
April 7, 2014
Publication date:
October 23, 2014
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
Type:
Application
Filed:
March 14, 2014
Publication date:
October 23, 2014
Applicant:
Deciphera Pharmaceuticals, LLC
Inventors:
Daniel L. Flynn, Michael D. Kaufman, Thiwanka Samarakoon, Timothy Malcolm Caldwell, Lakshminarayana Vogeti, YuMi Ahn, William C. Patt, Karen M. Yates
Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
Type:
Application
Filed:
April 17, 2014
Publication date:
October 23, 2014
Applicant:
PFIZER LIMITED
Inventors:
Robert McKenzie Owen, Robert Ian Storer
Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
Type:
Grant
Filed:
October 6, 2010
Date of Patent:
October 21, 2014
Assignee:
Siena Biotech S.p.A.
Inventors:
Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno