Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
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Patent number: 9957234Abstract: The present invention relates to novel polymorphic forms of ivacaftor, process for its preparation and pharmaceutical compositions comprising the same.Type: GrantFiled: December 9, 2015Date of Patent: May 1, 2018Assignee: Laurus Labs LimitedInventors: Ram Thaimattam, Venkata Srinivasa Rao Dama, Venkata Sunil Kumar Indukuri, Seeta Rama Anjaneyulu Gorantla, Satyanarayana Chava
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Patent number: 9956215Abstract: The present invention relates to the field of cancer therapy. Specifically, provided are methods of treating cancer, for example, peripheral T-cell lymphoma (“PTCL”), with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on gene expression characteristics.Type: GrantFiled: November 21, 2017Date of Patent: May 1, 2018Assignee: Kura Oncology, Inc.Inventors: Antonio Gualberto, Catherine Rose Scholz
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Patent number: 9956212Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of multiple myeloma.Type: GrantFiled: September 18, 2015Date of Patent: May 1, 2018Assignee: Active Biotech ABInventors: David Liberg, Anders Olsson, Dmitry Gabrilovich, Yuliya Nefedova
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Patent number: 9949485Abstract: Compounds (A) can be used for increasing the yield of useful plants or crop plants with respect to their harvested plant organs, wherein the Compound (A) is selected from compounds of the formula (I) or salts thereof, wherein the symbols are defined as in claim 1, preferably N-(2-methoxybenzoyl)-4-[(methylaminocarbonyl)-amino]benzenesulfonamide [Compound (A1)].Type: GrantFiled: February 28, 2014Date of Patent: April 24, 2018Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Udo Bickers, Stefan Lehr, Klaus Trabold, Mathias Schmidt, Martin Jeffrey Hills, Juan Pedro Ruiz-Santaella Moreno, Erwin Hacker
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Patent number: 9890406Abstract: A method for producing cathine ((1S,2S)-norpseudoephedrine), in which, in a first reaction step, benzaldehyde is reacted with an acetyl donor according to formula (1), where R?H or COOH, by way of an (S)-selective lease to yield an enantiomer mixture according to formulas (2) and (3) and, in a second step, the compound according to formula (3) is reacted with an amine donor by way of an (S)-selective transaminase to yield (1S,2S)-norpseudoephedrine.Type: GrantFiled: May 17, 2014Date of Patent: February 13, 2018Assignee: Forschungszentrum Juelich GmbHInventors: Doerte Rother, Martina Pohl, Torsten Sehl, Alvaro Gomez Baraibar
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Patent number: 9883673Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5- to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].Type: GrantFiled: April 29, 2016Date of Patent: February 6, 2018Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Nozomu Nakanishi, Yoshimasa Fukuda, Shigeki Kitsuda, Ikuya Ohno
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Patent number: 9880154Abstract: Acetylcholine and its receptors appeared in evolution before development of a nervous system. Cholinergic agonists functions include proliferation, differentiation, and cell-to-cell contact in protozoa] as well as vertebrate cells. Animal models for infection by Apicomplexan parasites require cell-to-cell contact followed by differentiation of parasite and host cells to produce clinical disease. Experimental infections are produced by introducing parasite infected leukocytes into a host. Binding cholinergic receptors on the parasites and leukocytes with levamisole HCl induces non-progressive infections and absence of signs of disease.Type: GrantFiled: May 20, 2014Date of Patent: January 30, 2018Inventors: William T Killeen, Siobhan Ellison
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Patent number: 9867816Abstract: Methods of treatment of multiple sclerosis (MS) with PPAR? agonists, and in particular with the compound of formula (I) known as INT131:Type: GrantFiled: January 10, 2017Date of Patent: January 16, 2018Assignee: InteKrin Therapeutics, Inc.Inventor: David Weinstein
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Patent number: 9861624Abstract: This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF.Type: GrantFiled: May 2, 2013Date of Patent: January 9, 2018Assignee: Exelixis, Inc.Inventor: Dana T. Aftab
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Patent number: 9856220Abstract: The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: GrantFiled: July 11, 2016Date of Patent: January 2, 2018Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Jürgen Dinges, Clarissa Jakob
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Patent number: 9840499Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: April 12, 2016Date of Patent: December 12, 2017Assignee: Vertex Pharmaceuticals IncorporatedInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Patent number: 9833444Abstract: The present invention relates preferably to the use of 4-bromo-N-[(E)-(2-methyl-1H-indol-3-yl)methyleneamino]benzenesulphonamide and 4-methyl-3-oxo-2-(3-pyridylmethylene) benzo[3,4-b]furan-6-yl-4-chlorobenzenesulphonate (compounds 5 and 6, respectively), which are compounds that can inhibit the toxic activity of sphingomyelinase D from Loxosceles venom, controlling the development of cutaneous and systemic loxoscelism; reducing haemolysis; inhibiting the formation of skin lesions; inhibiting skin necrosis; inhibiting intracellular signaling pathways and the production of reactive oxygen species. In addition to the therapeutic potential thereof, said inhibitors can be used to study the activity of sphingomyelinases and phospholipases D.Type: GrantFiled: December 2, 2014Date of Patent: December 5, 2017Assignee: FUNDAÇÃO BUTANTANInventors: Denise Vilarinho Tambourgi, Priscila Hess Lopes, Mario Tyago Murakami, Fernanda Calheta Vieira Portaro
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Patent number: 9820997Abstract: A method of accelerating remyelination or suppressing demyelination of neurons in a mammal, and a method of treating a disease associated with demyelination of neurons in a mammal.Type: GrantFiled: November 5, 2015Date of Patent: November 21, 2017Assignee: SAMSUNG ELECTRONICS CO., LTD.Inventors: Yunil Lee, Kiyoung Chang, Sangchul Park, Sungchun Cho
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Patent number: 9822078Abstract: The present invention relates to quinoline compounds as defined by Formula I below. Such quinoline compounds have been shown to inhibit the formation of amyloid deposits (e.g., amyloid oligomers, fibrils or plaques). Consequently, these compounds are suitable for treating a range of diseases and disorders in which amyloid deposits are implicated, such as type-2 diabetes and Alzheimer's disease.Type: GrantFiled: February 27, 2015Date of Patent: November 21, 2017Assignee: Oxford University Innovation LimitedInventors: David Vaux, Letitia Jean, Stephen Davies, Angela Russell, Graham Wynne, Carole Bataille, Méabh Brennan
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Patent number: 9815825Abstract: Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis and chronic obstructive pulmonary diseases). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.Type: GrantFiled: March 14, 2014Date of Patent: November 14, 2017Assignee: DiscoveryBiomed, Inc.Inventors: Erik Schwiebert, John Streiff, John Dixon, Hongwu Gao
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Patent number: 9783501Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.Type: GrantFiled: July 30, 2015Date of Patent: October 10, 2017Assignee: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
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Patent number: 9750717Abstract: The present invention relates to compounds acting as selective inhibitors of CD40-TRAF6 interaction, their use as medicaments and their use in the treatment of (chronic) inflammatory diseases. The present invention also relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: February 9, 2016Date of Patent: September 5, 2017Assignees: LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN, MAASTRICHT UNIVERSITYInventors: Esther Lutgens, Christian Weber, Gerry Nicolaes
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Patent number: 9732076Abstract: Described herein are solid oral dosage forms containing Compound (1) or a pharmaceutically acceptable salt thereof (Formula 1), wherein Compound (1) is in the amorphous state. Also described are solid oral dosage forms comprising a composition of Compound (1) in the amorphous state and one or more pharmaceutically acceptable excipients. Compound (1) is a specific inhibitor of the hepatitis C virus (HCV) NS3/4A serine protease. Thus, also described herein are methods for using the described solid oral dosage forms in the treatment of HCV infection. Also described are processes for the manufacture of the solid oral dosage forms.Type: GrantFiled: March 13, 2014Date of Patent: August 15, 2017Assignee: Boehringer Ingelheim International GmbHInventors: Chitra Telang, Zeren Wang, Li Zhong
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Patent number: 9732048Abstract: The invention relates to N-(isoxazol-3-yl)-aryl-carboxylic acid amides and use thereof as herbicides. In formula (I), A stands for N or C—Y. R, V, X, Y, and Z stand for groups such as hydrogen, halogen, and organic groups such as substituted alkyl.Type: GrantFiled: December 3, 2013Date of Patent: August 15, 2017Assignee: BAYER CROPSCIENCE AGInventors: Arnim Koehn, Hartmut Ahrens, Ralf Braun, Ines Heinemann, Joerg Tiebes, Christian Waldraff, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
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Patent number: 9717738Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.Type: GrantFiled: April 18, 2016Date of Patent: August 1, 2017Assignee: Horizon Orphan LLCInventors: David C. Griffith, Michael N. Dudley, Mark W. Surber, Keith A. Bostian, Olga Rodny
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Patent number: 9708331Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: GrantFiled: February 2, 2016Date of Patent: July 18, 2017Assignee: Sunovion Pharmaceuticals Inc.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Patent number: 9701639Abstract: The present disclosure relates to co-crystals comprising N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and a co-former and methods for their preparation. The present disclosure further relates to pharmaceutical compositions comprising the co-crystal forms, as well as methods of treatment therewith and kits.Type: GrantFiled: October 7, 2015Date of Patent: July 11, 2017Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark Strohmeier, John Caesar, Jr., Patrick Raymond Connelly, Majed Fawaz, Eduard Luss-Lusis, Brian McClain, Ales Medek, Hai Miao, Kwame Wiredu Nti-Addae, Ping Yin, Yuegang Zhang
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Patent number: 9694004Abstract: A novel crystalline form of a compound is disclosed.Type: GrantFiled: September 1, 2016Date of Patent: July 4, 2017Assignee: Glaxo Group LimitedInventor: Mei-yin Lee
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Patent number: 9687490Abstract: A compound of formula (I) for use in the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidase.Type: GrantFiled: October 22, 2013Date of Patent: June 27, 2017Assignee: GLUCOX BIOTECH ABInventors: Mona Wilcke, Erik Walum, Per Wikstrom
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Patent number: 9682967Abstract: The present invention is directed to N-substituted-5-substituted phthalamic acids which of formula (A). The compounds are considered useful for the treatment of diseases treatment of a neurodegenerative disease, psychiatric disease, motorneuron disease, peripheral neuropathies, pain, neuroinflammation or atherosclerosis such as Alzheimer's disease and Parkinson's disease.Type: GrantFiled: January 27, 2014Date of Patent: June 20, 2017Assignee: H. Lundbeck A/SInventors: Philip James Maltas, Stephen Watson, Morten Langg{hacek over (a)}rd, Laurent David
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Patent number: 9676724Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.Type: GrantFiled: October 12, 2015Date of Patent: June 13, 2017Assignee: Tianjin Hemay Oncology Pharmaceutical Co., Ltd.Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
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Patent number: 9676765Abstract: A compound of the formula: (I) or a pharmaceutically acceptable salt thereof, wherein: L is a 5-membered nitrogen-containing heteroaryl which is optionally fused to a benzene; Y is a 5, 6 or 7-membered nitrogen-containing heteroaryl, which is optionally fused to a benzene; and W is a zinc-binding group. The compounds are HDAC inhibitors and therefore have potential utility in therapy.Type: GrantFiled: November 6, 2013Date of Patent: June 13, 2017Assignee: Karus Therapeutics LimitedInventors: Stephen J. Shuttleworth, Cyrille D. Tomassi, Alexander R. Cecil, Somhairle Maccormick, William J. Nodes, Franck A. Silva
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2-amino-3-(imidazol-2-yl)-pyridin-4-one derivatives and their use as VEGF receptor kinase inhibitors
Patent number: 9675606Abstract: The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.Type: GrantFiled: July 24, 2015Date of Patent: June 13, 2017Assignee: SANOFIInventors: Alain Braun, Olivier Duclos, Gilbert Lassalle, Franz Lorge, Valerie Martin, Olaf Ritzeler, Aurelie Strub -
Patent number: 9662327Abstract: Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.Type: GrantFiled: June 18, 2012Date of Patent: May 30, 2017Assignee: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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Patent number: 9662322Abstract: This invention provides a method for treating or for reducing ambulatory deterioration in a human patient diagnosed to be afflicted with relapsing-remitting multiple sclerosis (RRMS) and having a high baseline disability score according to the Kurtzke Expanded Disability Status Scale (EDSS), comprising periodically administering to only the patient diagnosed with RRMS and having a high baseline disability score an amount of laquinimod effective to treat the patient or to reduce ambulatory deterioration. This invention further provides pharmaceutical compositions and packages comprising an effective amount of laquinimod for treating a human patient diagnosed to be afflicted with RRMS and having a high baseline disability score according to the EDSS.Type: GrantFiled: November 19, 2015Date of Patent: May 30, 2017Assignee: TEVA PHARMACEUTICAL INDUSTRIES, LTD.Inventor: Volker Knappertz
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Patent number: 9636375Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: GrantFiled: November 9, 2015Date of Patent: May 2, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Alan Xiangdong Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
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Patent number: 9624235Abstract: A method for treating a neoplasm in a subject, comprising co-administering to the subject a therapeutically effective amount of an anticancer agent and a substituted 6,7-methylenedioxy-4-amino-quinoline, or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: January 29, 2013Date of Patent: April 18, 2017Assignee: University of Pittsburgh—Of the Commonwealth System of Higher EducationInventors: Barry I. Gold, Xiangqun Xie, Ajay Srinivasan, LiRong Wang
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Patent number: 9617217Abstract: The present application provides novel compounds having anti-cancer or anti-Helicobacter pylori activity, pharmaceutical compositions and method for producing and using the novel compound.Type: GrantFiled: February 24, 2014Date of Patent: April 11, 2017Assignee: MICROBIAL CHEMISTRY RESEARCH FOUNDATIONInventors: Manabu Kawada, Hikaru Abe, Takumi Watanabe, Hiroyuki Inoue, Shun-ichi Ohba, Chigusa Hayashi, Masayuki Igarashi
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Patent number: 9603804Abstract: [Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less.Type: GrantFiled: April 24, 2014Date of Patent: March 28, 2017Assignee: KYORIN PHARMACEUTICAL CO., LTD.Inventors: Hiroshi Uchida, Masataka Hanada
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Patent number: 9592186Abstract: Embodiments of the invention are generally directed to compositions useful for reducing pigmentation in the skin. The composition may further include other depigmenting agents such as nicotinamide and its melanasome transfer-inhibiting derivatives, 3,3?-thiodipropanoic acid and its tyrosinase-inhibiting derivatives, or resorcinol and its tyrosinase-inhibiting derivatives, in a topically acceptable vehicle.Type: GrantFiled: September 30, 2014Date of Patent: March 14, 2017Assignee: Avon Products, Inc.Inventors: Hong Hu, Sunghan Yim, Uma Santhanam, John W. Lyga
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Patent number: 9585878Abstract: This application provides for a method of increasing brain-derived neurotrophic factor (BDNF) serum level in a human subject comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to increase BDNF serum level in the human subject. The method can further comprise periodically administering to the subject an amount of a second BDNF-increasing agent. This application also provides for a method for treating a human subject suffering from a BDNF-related disease comprising periodically administering laquinimod or a pharmaceutically acceptable salt thereof in an amount effective to treat the human subject. This application additionally provides for use of laquinimod in the manufacture of a medicament for increasing BDNF serum level in a human subject. This application further provides for a pharmaceutical composition comprising an amount of laquinimod effective for use in increasing BDNF serum level in a human subject.Type: GrantFiled: August 9, 2010Date of Patent: March 7, 2017Assignee: TEVA PHARMACEUTICAL INDUSTRIES, LTD.Inventor: Liat Hayardeny
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Patent number: 9580409Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: GrantFiled: November 7, 2012Date of Patent: February 28, 2017Assignee: SUNOVION PHARMACEUTICALS, INC.Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
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Patent number: 9540389Abstract: Novel compounds are disclosed having the structure of Formula I: wherein, n is an integer from 1 to 5; X is —CN, —F, —Cl, —Br, —I, —NO2; W is S, SO, SO2, O, NH, or NR5; R5 is alkyl, aralkyl, alkenyl, or alkynyl; Y is O, S; Z is NR1R2 or heterocycloalkyl; R1, R2 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups; R3 and R4 are, independently, hydrogen, alkyl, aralkyl, alkenyl, alkynyl, or cycloalkyl and may be optionally substituted with halo, hydroxy, alkoxy, amino, alkylamino, carboxy, alkoxycarbonyl, or nitrile groups, and may together form a cyclic structure; and Ar is mono-, di-, or tri-substituted phenyl or heteroaryl, a pharmaceutically acceptable salts thereof. The compounds are potent bacterial efflux pump inhibitors (EPIs).Type: GrantFiled: May 3, 2014Date of Patent: January 10, 2017Assignee: Microbiotix, Inc.Inventors: Timothy J. Opperman, Son T. Nguyen, Steven M. Kwasny, Xiaoyuan Ding
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Patent number: 9499552Abstract: The present invention relates to a pyrazolo[1,5-a]pyrimidine derivative of general formula 1 and a pharmaceutically acceptable salt thereof. The present invention also relates to use of compounds of formula 1 in the preparation of an anti-tumor medicament.Type: GrantFiled: May 22, 2015Date of Patent: November 22, 2016Assignees: Yanti University, Wuhan UniversityInventors: Hongbo Wang, Xuechuan Hong, Xi Zhu, Mingmin Ding, Guangyao Lv, Jianqiao Zhang, Meng Wen, Chunrong Qu, Jinmei Zhu, Xianming Hu
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Patent number: 9475772Abstract: The invention relates to new and improved processes for the preparation of Indacaterol and pharmaceutically acceptable salts thereof as well as intermediates for the preparation of Indacaterol. The new process avoids the use of the epoxide compound known in the art and the impurities associated therewith and results in a higher yield.Type: GrantFiled: September 9, 2013Date of Patent: October 25, 2016Assignee: Crystal Pharma S.A.U.Inventors: Antonio Lorente Bonde-Larsen, Yolanda Fernández Sainz, Jesús Iglesias Retuerto, Javier Gallo Nieto
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Patent number: 9468693Abstract: Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into cells via the cystine/glutamate antiporter and subsequent detection.Type: GrantFiled: January 23, 2014Date of Patent: October 18, 2016Assignee: General Electric CompanyInventors: Bruce Allan Hay, Jack Mathew Webster
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Patent number: 9464058Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3 and R4 n are as described herein, compositions including the compounds and methods of using the compounds.Type: GrantFiled: February 13, 2013Date of Patent: October 11, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan
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Patent number: 9463194Abstract: The disclosure describes methods for treatment of patients co-infected with HIV and tuberculosis, wherein the patient receives effective amounts of elvitegravir, an antimycobacterial agent and a CYP inhibitor.Type: GrantFiled: February 4, 2015Date of Patent: October 11, 2016Assignee: Gilead Sciences, Inc.Inventors: Rebecca Restituto Begley, Joseph Marcello Custodio, Brian P. Kearney
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Patent number: 9408829Abstract: The present invention relates to compounds acting as selective inhibitors of CD40-TRAF6 interaction, their use as medicaments and their use in the treatment of (chronic) inflammatory diseases. The present invention also relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: August 27, 2013Date of Patent: August 9, 2016Assignees: LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN, MAASTRICHT UNIVERSITY, ACADEMISCH ZIEKENHUIS MAASTRICHTInventors: Esther Lutgens, Christian Weber, Gerry Nicolaes
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Patent number: 9403816Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: GrantFiled: October 15, 2013Date of Patent: August 2, 2016Assignee: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Maxwell D. Cummings
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Patent number: 9394303Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having pyrazolopyridine structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.Type: GrantFiled: April 3, 2015Date of Patent: July 19, 2016Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Zaneta Nikolovska-Coleska, Fardokht Abulwerdi, Hollis Showalter, Lei Miao, Jeanne Stuckey, Ahmed Mady
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Patent number: 9382232Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.Type: GrantFiled: December 7, 2012Date of Patent: July 5, 2016Assignees: Shenyang Pharmaceutical University, Shenyang Pharmaceutical University (Benxi) Pharmaceutical Science and Technology Co., Ltd.Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
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Patent number: 9371295Abstract: The present invention relates to compounds of formula (I) and (IV), and pharmaceutically acceptable salts, tautomers, stereoisomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are for use in the treatment of disorders that are ameliorated by inhibition of HDAC such as cancer and hemoglobinopathies like ?-thalassemia or sickle cell anemia.Type: GrantFiled: August 7, 2013Date of Patent: June 21, 2016Assignees: IRBM-SCIENCE PARK S.P.A., C.N.C.C.S. SCARL COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENINGInventors: Sergio Altamura, Alberto Bresciani, Giulia Breveglieri, Danilo Fabbrini, Roberto Gambari, Steven Harper, Ralph Laufer, Edith Monteagudo, Emanuela Nizi, Paola Pace, Vincenzo Summa
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Patent number: 9359363Abstract: Herein, methods of modulating inclusion formation and stress granules in cells are described. The methods comprise contacting a cell with an inclusion inhibitor. Methods for screening for modulators of TDP-43 aggregation are also described.Type: GrantFiled: May 21, 2012Date of Patent: June 7, 2016Assignees: AQUINNAH PHARMACEUTICALS, INC., THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Benjamin Wolozin, Marcie Glicksman, Gregory D. Cuny, Justin Boyd
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Patent number: 9340503Abstract: Compounds of the invention are of the formula wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.Type: GrantFiled: April 30, 2014Date of Patent: May 17, 2016Assignee: Karus Therapeutics, LimitedInventors: Stephen Joseph Shuttleworth, Cyrille Davy Tomassi