Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
Type:
Grant
Filed:
March 20, 2008
Date of Patent:
March 5, 2013
Assignee:
Genkyotex SA
Inventors:
Patrick Page, Mike Orchard, Laetitia Fioraso-Cartier, Bianca Mottironi
Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
Type:
Grant
Filed:
May 15, 2012
Date of Patent:
March 5, 2013
Assignee:
H. Lundbeck A/S
Inventors:
Hermogenes N. Jimenez, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
Type:
Grant
Filed:
May 9, 2011
Date of Patent:
February 26, 2013
Assignee:
Gilead Sciences, Inc.
Inventors:
Manoj C. Desai, Allen Yu Hong, Hongtao Liu, Randall W. Vivian, Lianhong Xu
Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are 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:
June 8, 2010
Date of Patent:
February 26, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
Type:
Grant
Filed:
December 13, 2010
Date of Patent:
February 26, 2013
Assignee:
Merck Sharp & Dohme
Inventors:
Scott D. Kuduk, Douglas C. Beshore, Christina Ng DiMarco, Thomas J. Greshock
Abstract: The document describes a process for the preparation of N-Acyl-Phosphatidyl-Ethanolamine of formula (I) on an industrial scale, In which R1, R2 and R3 are, independently from each other, saturated, monounsaturated or polyunsaturated acyls C10-C30, pure or mixed together, and X?OH or OM, where M=alkaline metal or alkaline earth, ammonium or alkylammonium. The process in question allows the conversion of lecithin of synthetic or natural origin into N-Acyl-Phosphatidyl-Ethanolamine of formula (I) of high purity, using a limited molar excess of the reagent N-acyl-ethanolamine, where the acyl is as defined above for the formula (I) through reaction of transphosphatidylation in the presence of the enzyme phospholipase D and in conditions suitable for production on an industrial scale.
Type:
Grant
Filed:
July 8, 2008
Date of Patent:
February 19, 2013
Assignee:
Chemi S.p.A.
Inventors:
Lorenzo De Ferra, Mauro Anibaldi, Ettore Ammirati
Abstract: 4-(heterocycloalkyl)benzene-1,3-diol compounds are described corresponding to general formula (I) below: Also described, are compositions including the same, processes for preparation thereof and to the use thereof in pharmaceutical or cosmetic compositions for use in the treatment or prevention of pigmentary disorders.
Abstract: The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.
Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
Type:
Grant
Filed:
December 8, 2009
Date of Patent:
February 5, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
Abstract: Compounds of formula I: in free or salt or solvate form, where R1, R2, R3 and R20 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described. These compounds are useful for the treatment of inflammatory or obstructive airways diseases such as pulmonary hypertension, pulmonary fibrosis, liver fibrosis, cancer, muscle diseases such as muscle atrophies and muscle dystrophies, and systemic skeletal disorders such as osteoporosis.
Type:
Grant
Filed:
October 15, 2008
Date of Patent:
February 5, 2013
Assignee:
Novartis AG
Inventors:
Duncan Shaw, Catherine Leblanc, Dimitrios Lizos, Cathy Ritchie, Vikki Furminger, Sarah Lewis, Benoit Hornsperger, Nikolaus Johannes Stiefl, Sven Weiler
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.
Type:
Grant
Filed:
September 23, 2011
Date of Patent:
February 5, 2013
Assignee:
Cancer Research Technology Limited
Inventors:
Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
Abstract: The present invention provides a flame-retardant hardener for epoxy resin having a compound represented by formula (I): In addition, the present invention also provides a flame-retardant resin material comprising the aforementioned flame-retardant hardener for epoxy resin. Moreover, the present invention further provides a method for manufacturing a flame-retardant hardener for epoxy resin, which can be directly applied in a resin curing process after a cooling step without additional purification. As described by the present invention, the flame-retardant hardener for epoxy resin in accordance with the present invention can replace the conventional toxic halogenated resins, and provide an environmental-friendly flame-retardant hardener for epoxy resin.
Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
Type:
Grant
Filed:
October 12, 2011
Date of Patent:
January 29, 2013
Assignee:
Panmira Pharmaceuticals, LLC
Inventors:
John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
Abstract: The present invention relates to compounds of formula a process for their production and their use in electronic devices, especially electroluminescent devices. When used as electron transport material in electroluminescent devices, the compounds of formula I, or II may provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.
Type:
Grant
Filed:
December 9, 2011
Date of Patent:
January 29, 2013
Assignee:
BASF SE
Inventors:
Thomas Schaefer, Heinz Wolleb, Christian Schildknecht, Soichi Watanabe, Christian Lennartz
Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Even more specifically, the invention provides compounds for modulating c-Kit kinase activity and methods of treating diseases mediated by c-Kit activity utilizing the compounds and pharmaceutical compositions thereof.
Type:
Grant
Filed:
August 27, 2004
Date of Patent:
January 29, 2013
Assignee:
Exelixis, Inc.
Inventors:
Wei Cheng, Erick Wang Co, Moon Hwan Kim, Rhett Ronald Klein, Donna T. Le, Amy Lew, John M. Nuss, Wei Xu, William Bajjalieh
Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
Type:
Grant
Filed:
December 16, 2011
Date of Patent:
January 22, 2013
Assignee:
Onyx Therapeutics, Inc.
Inventors:
Kevin D. Shenk, Francesco Parlati, Han-jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.
Type:
Grant
Filed:
December 20, 2011
Date of Patent:
January 22, 2013
Assignees:
University of Florida Resesarch Foundation, Inc., Smithsonian Institutution
Inventors:
Hendrik Luesch, Taori Kanchan, Valerie J. Paul
Abstract: There is provided a process for manufacture of optically-active, 2-(acyloxymethyl)-1,3-oxathiolanes of Formula I comprising a preparation of a racemic compound and an enzyme-catalyzed kinetic resolution of the enantiomers. The invention may further provide for the esterification and racemization of the by-product of the enzymatic reaction. In this manner, 2(R)-(benzoyloxymethyl)-1,3-oxathiolane is prepared as a useful intermediate for manufacture of the anti-HIV drug Apricitabine.