Abstract: The present invention is directed to quinolone compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is 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 the neuropeptide S receptor is involved.
Type:
Grant
Filed:
November 3, 2009
Date of Patent:
March 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
James C. Barrow, Mark T. Bilodeau, Christopher D. Cox, John C. Hartnett, Nathan R. Kett, Yiwei Li, Peter J. Manley, Jeffrey Melamed, William D. Shipe, B. Wesley Trotter, Amy Zartman
Abstract: Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
Type:
Grant
Filed:
July 21, 2010
Date of Patent:
February 26, 2013
Assignee:
Merck Canada Inc.
Inventors:
Jean-Philippe Leclerc, Chun-Sing Li, Oscar Miguel Moradei
Abstract: The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.
Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof; wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen; R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy; R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidized forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; and R3 is a group D: wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopro
Abstract: Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals.
Type:
Grant
Filed:
December 17, 2009
Date of Patent:
February 26, 2013
Assignee:
Novartis AG
Inventors:
Steve Nanchen, Noëlle Gauvry, Thomas Goebel
Abstract: Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals.
Type:
Grant
Filed:
December 17, 2009
Date of Patent:
February 19, 2013
Assignee:
Novartis AG
Inventors:
Steve Nanchen, Noëlle Gauvry, Francois Pautrat
Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
September 22, 2009
Date of Patent:
February 12, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Monika Ermann
Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.
Abstract: The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p, R1, R2, R3, R4, R5 and R6 are defined in the specification. The invention further provides pharmaceutical compositions including the compounds of the invention as well as methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various conditions and disorders, such as Crohn's disease and ulcerative colitis.
Type:
Grant
Filed:
April 27, 2010
Date of Patent:
February 5, 2013
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Ying-zi Xu, Shendong Yuan, David Wone, Andrei Konradi
Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.
Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
August 25, 2011
Date of Patent:
January 29, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Markus Ostermeier, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
Abstract: The invention relates to the compounds of the general formula (I): in which A, D, R, R1 and X are as defined in the description, to a process for the preparation thereof and to the therapeutic use thereof in the treatment of pathologies associated with insulin resistance syndrome.
Type:
Grant
Filed:
July 7, 2006
Date of Patent:
January 29, 2013
Assignee:
Merck Patent Gesellschaft mit beschränkter Haftung
Inventors:
Gérard Moinet, Gérard Botton, Annick Arbellot de Vacqueur
Abstract: The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, A? protein or ?-synuclein protein aggregation.
Type:
Grant
Filed:
November 19, 2007
Date of Patent:
January 29, 2013
Assignee:
Treventis Corporation
Inventors:
Michael D. Carter, Donald F. Weaver, Sheila Marie H. Jacobo, Erhu Lu, Fuye Gao
Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Type:
Grant
Filed:
March 15, 2011
Date of Patent:
January 29, 2013
Assignee:
Exelixis, Inc.
Inventors:
Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
Abstract: A process for the preparation of pure Duloxetine hydrochloride comprises the steps of: a) reacting 1-(thiophen-2-yl)ethanone with dimethylamine hydrochloride, b) purifying the component in a solvent, c) reducing the component with an alkali metal borohydride, d) resolving the compound with a chiral acid, and treating the obtained compound with weak inorganic base, e) reacting the compound to give Duloxetine oxalate salt and f) converting the Duloxetine salt into its hydrochloride salt. Further the purifications of the obtained compound and of two intermediate products are described.
Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
Type:
Grant
Filed:
March 2, 2011
Date of Patent:
January 22, 2013
Assignee:
Janssen Pharmaceutica NV
Inventors:
Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
Abstract: The present invention provides benzoxazole compounds and pharmaceutically acceptable salts thereof and pharmaceutical compositions including the same. The present invention further provides methods of use as described herein.
Type:
Grant
Filed:
September 25, 2009
Date of Patent:
January 15, 2013
Assignee:
Eisai R&D Co., Ltd.
Inventors:
Wanjun Zheng, Mark Spyvee, Fabian Gusovsky, Sally T. Ishizaka
Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
Type:
Grant
Filed:
January 27, 2012
Date of Patent:
January 15, 2013
Assignee:
4SC Discovery GmbH
Inventors:
Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
Abstract: Embodiments of the present invention comprises a compound of formula I or its enantiomer, diastereomer, stereoisomer or its pharmaceutically acceptable salt, methods of use and methods of synthesis.
Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
September 21, 2011
Date of Patent:
January 8, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi