Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
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Patent number: 11376248Abstract: The present invention provides methods for detecting and/or treating a subject having an aneurysm or at risk for developing an aneurysm. It has been discovered that a key metabolite of the kynurenine (Kyn) pathway, a major route for the metabolism of essential amino acid tryptophan (Trp) into nicotinamide adenine dinucleotide (NAD+), plays a critical role in the formation of aneurysms, for example abdominal aortic aneurysms. In particular, it has been discovered that 3-Hydroxyanthranilic acid (3-HAA), a product of kynureninase (KYNU), plays a causative role in the formation of aneurysms by, for example exerting pro-inflammatory effects on vascular smooth muscle cells. It has further been discovered that elevated levels of 3-HAA are indicative of the presence and/or progression of an aneurysm, and 3-HAA levels correlate with the size (aortic diameter) of the aneurysm.Type: GrantFiled: December 20, 2019Date of Patent: July 5, 2022Assignee: Georgia State University Research Foundation, Inc.Inventor: Ming-Hui Zou
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Patent number: 11357856Abstract: Compounds are provided having the following structure: Formula (I) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R1, R2, G1, G2 and n are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.Type: GrantFiled: April 13, 2018Date of Patent: June 14, 2022Assignee: ACUITAS THERAPEUTICS, INC.Inventors: Steven M. Ansell, Xinyao Du
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Patent number: 11332433Abstract: Processes for preparing latanoprostene bunod and an intermediate prepared from the process. Also latanoprostene bunod compositions having high-purity latanoprostene bunod.Type: GrantFiled: July 24, 2020Date of Patent: May 17, 2022Assignee: CHIROGATE INTERNATIONAL INC.Inventors: Shih-Yi Wei, Ming-Kun Hsu, Tzyh-Mann Wei
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Patent number: 10980779Abstract: The present invention relates to methods and pharmaceutical compositions useful for the treatment of hyperglycemia. Thorough multiple analyses, inventors demonstrated that Gfi1 is expressed in pancreatic acinar cells, starting from the first stages of pancreatic embryonic development. Furthermore, they observed that Gfi1 mRNA levels remain steady throughout embryonic development, while they significantly increase during the first days of life. They challenged conditional mutant mice with high fat diet for 5 months and monitored their weight and glycemia weekly. All the animals displayed a rapid increase in body mass as expected. While control mice rapidly developed a massive hyperglycemia, mutant mice remained normoglycemic throughout the entire experiment. A similar protection from induced diabetes was observed upon treatment with a high dose of Streptozotocin.Type: GrantFiled: March 26, 2018Date of Patent: April 20, 2021Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), UNIVERSITE NICE SOPHIA ANTIPOLIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE—CNRSInventors: Patrick Collombat, Tiziana Napolitano, Fabio Avolio
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Patent number: 10927070Abstract: Provided herein are compositions and methods for treating, inhibiting and/or reducing the severity of cancer in subjects in need thereof. The methods include providing an agent that inhibits expression or activity of ONECUT2 and administering a therapeutically effective amount of the agent so as to treat, inhibit and/or reduce the severity of cancer in the subject.Type: GrantFiled: May 26, 2017Date of Patent: February 23, 2021Assignee: Cedars-Sinai Medical CenterInventors: Michael Freeman, Mirja Rotinen, Ramachandran Murali, Sungyong You
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Patent number: 10894777Abstract: There are provided Tissue Transglutaminase (TG2) inhibitor compounds, and compositions and methods of use thereof for the prevention or treatment of a cancer.Type: GrantFiled: April 13, 2017Date of Patent: January 19, 2021Assignees: UNIVERSITY OF OTTAWA, UNIVERSITY OF MARYLAND, BALTIMORE, UNIVERSITY OF ROCHESTERInventors: Jeffrey W. Keillor, Abdullah Akbar, Richard L. Eckert, Matthew Fisher, Gail V. W. Johnson
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Patent number: 10766905Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.Type: GrantFiled: August 1, 2019Date of Patent: September 8, 2020Assignee: AstraZeneca ABInventors: Robert Hugh Bradbury, Alfred Arthur Rabow, Michael James Waring, James Francis McCabe, Steven Christopher Glossop, Arshed Mahmood, Zoe Ann Cotter
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Patent number: 10633378Abstract: The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.Type: GrantFiled: March 25, 2014Date of Patent: April 28, 2020Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Dorothée Bardiot, Gunter Carlens, Kai Dallmeier, Suzanne Kaptein, Mohamed Koukni, Arnaud Marchand, Johan Neyts, Wim Smets
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Patent number: 10550123Abstract: The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.Type: GrantFiled: September 26, 2012Date of Patent: February 4, 2020Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Dorothée Bardiot, Gunter Carlens, Kai Dallmeier, Suzanne Kaptein, Michael McNaughton, Arnaud Marchand, Johan Neyts, Wim Smets, Mohamed Koukni
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Patent number: 10464907Abstract: The present invention relates to a novel compound having HSP90 inhibitory activity or a pharmaceutically acceptable salt thereof, and a medicinal use thereof, and composition comprising a dihydroxyphenyl compound or a benzamide compound, which is a novel compound having the HSP90 inhibitory activity of the present invention can effectively inhibit HSP90, and thus can be usefully used as a pharmaceutical composition for preventing or treating HSP90-mediated diseases or a health functional food for preventing or improving HSP90-mediated diseases, which selected from the group consisting of cancer diseases, degenerative neurological diseases and viral infections.Type: GrantFiled: January 31, 2017Date of Patent: November 5, 2019Assignee: INDUSTRY ACADEMIC COOPERATION FOUNDATION KEIMYUNG UNIVERSITYInventor: Young Ho Seo
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Patent number: 10463654Abstract: Provided are methods for treating cancer in a patient by administering at least one antibiotic selected from the group consisting of clofazimine, rifabutin and clarithromycin, in combination with an aryladamantane compound. In an embodiment, the aryladamantane compound is [3-(4-chlorophenyl)-adamantane-1-carboxylic acid (pyridin-4-ylmethyl)amide], or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 7, 2017Date of Patent: November 5, 2019Assignee: RedHill Biopharma Ltd.Inventors: Reza Fathi, Dror Ben-Asher, Danielle Abramson
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Patent number: 10399924Abstract: Provided herein are deuterium substituted fumarate derivatives and pharmaceutical compositions comprising deuterium substituted fumarate derivatives. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a deuterium substituted fumarate derivative or a pharmaceutical composition comprising a deuterium substituted fumarate derivative. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.Type: GrantFiled: March 7, 2014Date of Patent: September 3, 2019Assignee: Biogen MA Inc.Inventor: Jianhua Chao
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Patent number: 10265322Abstract: The present invention relates to the use of PAR1 antagonists, in particular of vorapaxar, of atopaxar and of 3-(2-chlorophenyl)-1-[4-(4-fluorobenzyl)piperazin-1-yl]propenone, or a pharmaceutically acceptable salt thereof, for preventing and/or treating pelvi-perineal functional pathological conditions, and more particularly painful bladder syndrome.Type: GrantFiled: April 25, 2018Date of Patent: April 23, 2019Assignee: Pierre Fabre MedicamentInventors: Bruno Le Grand, Didier Junquero, Nicolas Monjotin
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Patent number: 9980970Abstract: The present invention relates to the use of PAR1 antagonists, in particular of vorapaxar, of atopaxar and of 3-(2-chlorophenyl)-1-[4-(4-fluorobenzyl)piperazin-1-yl]propenone, or a pharmaceutically acceptable salt thereof, for preventing and/or treating pelvi-perineal functional pathological conditions, and more particularly painful bladder syndrome.Type: GrantFiled: October 31, 2014Date of Patent: May 29, 2018Assignee: PIERRE FABRE MEDICAMENTInventors: Bruno Le Grand, Didier Junquero, Nicolas Monjotin
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Patent number: 9944650Abstract: The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.Type: GrantFiled: July 24, 2015Date of Patent: April 17, 2018Assignee: AstraZeneca ABInventors: Robert Hugh Bradbury, Alfred Arthur Rabow, Michael James Waring, James Francis McCabe, Steven Christopher Glossop, Arshed Mahmood, Zoe Ann Cotter
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Patent number: 9938262Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R6, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: GrantFiled: October 3, 2016Date of Patent: April 10, 2018Assignee: Merck Patent GmbHInventors: Henry Yu, Andreas Goutopoulos, Thomas E. Richardson, Jiezhen Li, Brian H. Heasley, Pandi Bharathi
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Patent number: 9907799Abstract: A tau aggregation inhibitor can sufficiently inhibit a tau protein from aggregating in cells. The inhibitor includes a 4-substituted catechol structure compound, having, at position 4 of its catechol ring, an electron-donating substituent R other than a hydrocarbon group, or a salt thereof. The 4-substituted catechol structure compound is preferably 4-aminocatechol or 1,2,4-benzenetriol. Examples of tauopathies to which this inhibitor is applicable include AD, Down's syndrome, frontotemporal dementia, cotricobasal degeneration (CBD) and progressive supranuclear palsy (PSP).Type: GrantFiled: April 2, 2014Date of Patent: March 6, 2018Assignees: THE DOSHISHA, National Center for Geriatrics and GerontologyInventors: Tomohiro Miyasaka, Hachiro Sugimoto, Rie Tokizane, Yuki Shinzaki, Yohei Oe, Tetsuo Ota, Akihiko Takashima, Yoshiyuki Soeda, Yasuo Ihara, Yoshikazu Inoue
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Patent number: 9908859Abstract: The invention relates to methods and compositions for the treatment or prevention of diseases and disorders associated with myeloproliferative disorders. In particular, the invention relates to an LSD 1 inhibitor for use in treating or preventing Philadelphia chromosome negative myeloproliferative disorders.Type: GrantFiled: February 20, 2014Date of Patent: March 6, 2018Assignee: Oryzon Genomics, S.A.Inventors: Jonathan Alleman Baker, Julio Castro Palomino, Matthew Colin Thor Fyfe, Tamara Maes, Marc Martinell Pedemonte
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Patent number: 9675600Abstract: Methods of treating cancer related conditions using anamorelin are described.Type: GrantFiled: August 28, 2015Date of Patent: June 13, 2017Assignee: HELSINN HEALTHCARE SAInventors: William Mann, John Friend, William Polvino, Suzan Allen, Ming Lu, Elizabeth Duus, Ruben Giorgino, Enrico Baroni
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Patent number: 9637473Abstract: The invention relates to novel acrylamide derivatives of the formula I wherein R1, R2, R3, X, and ring A are as defined in the description, and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.Type: GrantFiled: March 14, 2014Date of Patent: May 2, 2017Assignee: ACTELION PHARMACEUTICALS LTD.Inventors: Hamed Aissaoui, Christoph Boss, Claire-Lise Ciana, Thierry Kimmerlin, Romain Siegrist
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Patent number: 9289503Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: GrantFiled: March 2, 2015Date of Patent: March 22, 2016Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Patent number: 9089532Abstract: The invention relates to improved and stable pharmaceutical formulations of phenylalanine derivatives and the use thereof as urokinase inhibitors, particularly for the treatment of malignant tumors and tumoral metastases.Type: GrantFiled: September 20, 2005Date of Patent: July 28, 2015Assignee: Wilex AGInventors: Wolfgang Schmalix, Markus Bürgle, Klaus Koch
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Publication number: 20150148330Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 16, 2015Publication date: May 28, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Publication number: 20150140080Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Publication number: 20150140079Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Publication number: 20150140075Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Publication number: 20150140081Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Publication number: 20150140077Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Publication number: 20150140078Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: SARCODE BIOSCIENCE INC.Inventors: Thomas Gadek, John Burnier
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Publication number: 20150133430Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: January 16, 2015Publication date: May 14, 2015Inventors: Qing XU, Zhe LI
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Patent number: 9029381Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: GrantFiled: November 21, 2011Date of Patent: May 12, 2015Assignee: Astrazeneca ABInventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
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Publication number: 20150126494Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 30, 2013Publication date: May 7, 2015Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Konstantin Petrukhin, Janet R. Sparrow, Rando Allikmets
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Patent number: 8993577Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.Type: GrantFiled: February 19, 2010Date of Patent: March 31, 2015Assignee: Astrazeneca ABInventor: Andrew Griffin
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Publication number: 20150087645Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.Type: ApplicationFiled: October 7, 2014Publication date: March 26, 2015Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
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Publication number: 20150087629Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein saidType: ApplicationFiled: December 5, 2014Publication date: March 26, 2015Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
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Publication number: 20150079035Abstract: The present invention provides, inter alia, a compound having the structure: (Formula (I). Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for treating or ameliorating the effects of an excitotoxic disorder in a subject, methods of modulating ferroptosis in a subject, methods of reducing reactive oxygen species (ROS) in a cell, and methods for treating or ameliorating the effects of a neurodegenerative disease.Type: ApplicationFiled: April 2, 2013Publication date: March 19, 2015Inventors: Brent R. Stockwell, Scott J. Dixon, Rachid Skouta
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Publication number: 20150072984Abstract: Chemical entities that are curcumin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.Type: ApplicationFiled: August 29, 2012Publication date: March 12, 2015Inventor: Xiangping Qian
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Patent number: 8975399Abstract: A benzene sulphonamide compound of formula I or one of its addition salts with pharmaceutically acceptable acids, for its use in a method for treating a pathology linked to an excessive effect of TNF-alpha and for its use in a method for treating the human or animal body as a direct inhibitor of TNF-alpha.Type: GrantFiled: July 19, 2011Date of Patent: March 10, 2015Inventors: Jean-Francois Zagury, Matthieu Montes, Hadley Mouhsine, Helene Guillemain
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Patent number: 8975235Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: GrantFiled: August 14, 2012Date of Patent: March 10, 2015Assignee: InterMune, Inc.Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Patent number: 8969354Abstract: The invention relates to Fatty Acid Fumarate Derivatives; compositions comprising an effective amount of a Fatty Acid Fumarate Derivative; and methods for treating or preventing cancer, a metabolic disorder or neurodegenerative disorder comprising the administration of an effective amount of a Fatty Acid Fumarate Derivative.Type: GrantFiled: November 9, 2012Date of Patent: March 3, 2015Assignee: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Jean E. Bemis, Chi B. Vu
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Publication number: 20150051144Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.Type: ApplicationFiled: September 26, 2012Publication date: February 19, 2015Inventors: Harikishore Pingali, Vrajesh Pandya
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Publication number: 20150038493Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.Type: ApplicationFiled: October 5, 2012Publication date: February 5, 2015Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
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Publication number: 20150038498Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.Type: ApplicationFiled: March 22, 2013Publication date: February 5, 2015Inventors: Timothy Allen Blizzard, Tesfaye Biftu
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Patent number: 8946227Abstract: The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.Type: GrantFiled: January 30, 2013Date of Patent: February 3, 2015Assignee: Merck Serono SAInventors: Sharad Magar, Andreas Goutopoulos, Yihua Liao, Matthias Schwarz, Russell J. Thomas
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Publication number: 20150031663Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.Type: ApplicationFiled: October 13, 2014Publication date: January 29, 2015Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
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Publication number: 20150031635Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the phenolic opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.Type: ApplicationFiled: June 30, 2014Publication date: January 29, 2015Inventors: Thomas E. Jenkins, Julie D. Seroogy, Jonathan W. Wray
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Publication number: 20150018355Abstract: Compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating leukemia. In particular, compounds, and methods and uses of compounds, and pharmaceutical compositions thereof, are described herein for treating acute lymphoblastic leukemia (ALL) in its various forms.Type: ApplicationFiled: March 13, 2013Publication date: January 15, 2015Inventors: Mark R. Kelley, Melissa L. Fishel, Angelo A. Cardoso
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Publication number: 20150018335Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 7, 2013Publication date: January 15, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
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Patent number: 8933102Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).Type: GrantFiled: October 24, 2011Date of Patent: January 13, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson