Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.
Type:
Grant
Filed:
June 14, 2011
Date of Patent:
March 17, 2015
Assignee:
Bayer Cropscience AG
Inventors:
Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
Type:
Grant
Filed:
May 10, 2013
Date of Patent:
March 10, 2015
Assignee:
AbbVie Inc.
Inventors:
Todd M. Hansen, Kenton Longenecker, Howard R. Heyman, Michael L. Curtin, Richard F. Clark, Bryan Sorensen, Zhiqin Ji, Kevin Woller, George Doherty, Robin Frey
Abstract: Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
August 31, 2011
Date of Patent:
March 10, 2015
Assignees:
Genetech, Inc, Gilead Connecticut, Inc.
Inventors:
Kevin S. Currie, Xiaojing Wang, Wendy B. Young
Abstract: Provided herein are novel iso-ergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1B receptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2B receptors using the compounds and compositions disclosed herein.
Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
Abstract: There is disclosed a pyrimidinecarboxamide compound useful as a pharmaceutical agent, synthetic processes, and pharmaceutical compositions which include the pyrimidinecarboxamide compound. More specifically, there is disclosed a CXCR1/2 inhibitor useful for treating a variety of inflammatory and neoplastic disorders.
Type:
Grant
Filed:
August 2, 2013
Date of Patent:
March 3, 2015
Assignee:
Syntrix Biosystems, Inc.
Inventors:
Dean Y. Maeda, John A. Zebala, Aaron D. Schuler
Abstract: Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.
Type:
Grant
Filed:
October 8, 2013
Date of Patent:
March 3, 2015
Assignee:
Ambit Biosciences Corporation
Inventors:
Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
Type:
Grant
Filed:
September 27, 2012
Date of Patent:
March 3, 2015
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
Abstract: C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKK? and/or TBK-1: in which: R1 represents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; R2 represents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of R3 and R4 independently represents a hydrogen atom or a C1-4 alkyl group.
Type:
Grant
Filed:
July 18, 2011
Date of Patent:
February 24, 2015
Assignee:
Domainex Limited
Inventors:
Trevor Robert Perrior, Gary Karl Newton, Mark Richard Stewart, Rehan Aqil
Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 22, 2011
Date of Patent:
February 24, 2015
Assignee:
Cytokinetics, Inc.
Inventors:
Zhe Yang, Alex R. Muci, Jeffrey Warrington, Gustave Bergnes, Bradley P. Morgan, Chihyuan Chuang, Antonio Romero, Scott Collibee, Xiangping Qian, Pu-Ping Lu
Abstract: The invention relates to compounds of formula wherein the substituents are as described in claim 1. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
Type:
Grant
Filed:
January 25, 2013
Date of Patent:
February 24, 2015
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Helmut Jacobsen, Synese Jolidon, Thomas Luebbers
Abstract: A pyridazinone compound represented by the formula (I) has excellent effect on weed control and is useful as an active ingredient of herbicides.
Abstract: The invention features compounds of formula I or II: In one embodiment, the invention relates compounds and processes for conjugating ligand to oligonucleotide. The invention further relates to methods for treating various disorders and diseases such as viral infections, bacterial infections, parasitic infections, cancers, allergies, autoimmune diseases, immunodeficiencies and immunosuppression.
Type:
Grant
Filed:
September 23, 2009
Date of Patent:
February 24, 2015
Assignee:
Alnylam Pharmaceuticals, Inc.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev, Takeshi Yamada, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Shigeo Matsuda, Rajendra K. Pandey, Chang Geng Peng
Abstract: The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors.
Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
Type:
Grant
Filed:
September 11, 2012
Date of Patent:
February 17, 2015
Assignee:
IRM LLC
Inventors:
Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
Type:
Grant
Filed:
May 11, 2011
Date of Patent:
February 17, 2015
Assignee:
Amgen Inc.
Inventors:
Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.
Type:
Grant
Filed:
December 20, 2010
Date of Patent:
February 10, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2 R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
Type:
Grant
Filed:
September 7, 2010
Date of Patent:
February 10, 2015
Assignee:
E I du Pont de Nemours and Company
Inventors:
Kanu Maganbhai Patel, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
Type:
Grant
Filed:
April 2, 2013
Date of Patent:
February 10, 2015
Assignee:
Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on Behalf of Arizona State University
Inventors:
Sidney Hecht, Omar Khdour, Jun Lu, Pablo Arce