Patents Issued in June 13, 2017
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Patent number: 9676739Abstract: The present invention relates to a novel acid dianhydride, a method for preparing the same, and a polyimide prepared therefrom. More specifically, the acid dianhydride according to the present invention is useful as a colorless transparent polyimide unit exhibiting excellent thermal stability and a low dielectric ratio, and the polyimide of the present invention has excellent solubility to an organic solvent compared with the conventional polyimide.Type: GrantFiled: May 16, 2014Date of Patent: June 13, 2017Assignee: KOLON INDUSTRIES, INC.Inventors: Hyo Jun Park, Hak Gee Jung, Chang Sik Ha, Prdip Kumar Tapaswi, Young Sik Jeong
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Patent number: 9676740Abstract: Disclosed is a process to produce a dry purified carboxylic acid product comprising furan-2,5-dicarboxylic acid (FDCA). The process comprises oxidizing at least one oxidizable compound selected from the following group: 5-(hydroxymethyl)furfural (5-HMF), 5-HMF esters (5-R(CO)OCH2-furfural where R is alkyl, cycloalkyl, or aryl), 5-HMF ethers (5-R?OCH2-furfural where R? is alkyl, cycloalkyl, or aryl), 5-alkyl furfurals (5-R?-furfural where R? is alkyl, cycloalkyl, or aryl), mixed feedstocks of 5-HMF and 5-HMF esters, mixed feedstocks of 5-HMF and 5-HMF ethers, and mixed feedstocks of 5-HMF and 5-alkyl furfurals to generate a crude carboxylic acid slurry comprising FDCA.Type: GrantFiled: January 14, 2016Date of Patent: June 13, 2017Assignee: Eastman Chemical CompanyInventors: Mesfin Ejerssa Janka, Kenny Randolph Parker, Paula Moody, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Bradford Russell Bowers, Michael Charles Morrow
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Patent number: 9676741Abstract: The present invention relates to a dapagliflozin-citric acid co-crystal, processes for its preparation, and its use for the treatment of type 2 diabetes mellitus. A dapagliflozin citric acid co-crystal. The dapagliflozin citric acid co-crystal of claim 1, characterized by X-ray powder diffraction peaks having d-spacing values at about 3.89, 3.90, 4.01, 4.35, 5.77, and 5.80.Type: GrantFiled: June 23, 2015Date of Patent: June 13, 2017Assignee: SUN PHARMACEUTICAL INDUSTRIES LIMITEDInventors: Ramkinkar Santra, Tarun Kumar Singh, Ram Thaimattam, Mohan Prasad
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Patent number: 9676742Abstract: The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a tautomer or salt thereof, where R1-R5, a, b, X and P2, are as defined in the specification.Type: GrantFiled: June 26, 2015Date of Patent: June 13, 2017Assignee: Theravance Biopharma R&D IP, LLCInventor: Miroslav Rapta
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Patent number: 9676743Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.Type: GrantFiled: September 4, 2013Date of Patent: June 13, 2017Assignee: Cornell UniversityInventors: Geoffrey W. Coates, John W. Kramer
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Patent number: 9676744Abstract: Long-chain carboxychromanol compounds useful for treating conditions associated with the need to inhibit cyclooxygenase-1, cyclooxygenase-2, and/or 5-lipoxygenase, and pharmaceutical formulations containing the compounds are provided herein.Type: GrantFiled: August 29, 2014Date of Patent: June 13, 2017Assignee: PURDUE RESEARCH FOUNDATIONInventor: Qing Jiang
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Patent number: 9676745Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined here, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.Type: GrantFiled: July 17, 2014Date of Patent: June 13, 2017Assignee: Heptares Therapeutics LimitedInventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Aves, Benjamin Gerald Tehan
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Patent number: 9676746Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.Type: GrantFiled: January 29, 2016Date of Patent: June 13, 2017Assignees: BioMed Valley Discoveries, Inc., Vertex Pharmaceuticals IncorporatedInventors: Gary DeCrescenzo, Dean Welsch, Petinka I. Vlahova, Stephan X. M. Boerrigter, Alexander Aronov, Ali Keshavarz-Shokri, Alexander N. Scangas, Kathy Stavropoulos, Benjamin Littler, Irina Nikolaevna Kadiyala, Rossitza Gueorguieva Alargova
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Patent number: 9676747Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.Type: GrantFiled: June 2, 2015Date of Patent: June 13, 2017Assignee: NOVIRA THERAPEUTICS, INC.Inventors: George D. Hartman, Osvaldo A. Flores
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Patent number: 9676748Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.Type: GrantFiled: December 20, 2013Date of Patent: June 13, 2017Assignee: Plexxikon Inc.Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
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Patent number: 9676749Abstract: Disclosed herein are compositions and methods for cancer detection and treatment. Compounds that inhibit PRMT5 are contemplated, as are pharmaceutical compositions comprising a therapeutically effective amount of at least one PRMT5 inhibitor. In some embodiments pharmaceutical compositions further comprising at least one HDAC inhibitor are contemplated. Methods of treating disorders in a mammal by inhibiting PRMT5 by administering to a mammal, a therapeutically effective amount of a PRMT5 inhibitor are also disclosed.Type: GrantFiled: May 4, 2015Date of Patent: June 13, 2017Assignee: Ohio State Innovation FoundationInventors: Robert Baiocchi, Chenglong Li, Pui Kai Li, Fengting Yan
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Patent number: 9676750Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: GrantFiled: January 20, 2016Date of Patent: June 13, 2017Assignees: Incyte Corporation, Incyte Holdings CorporationInventors: Yun-Long Li, David M. Burns, Hao Feng, Chu-Biao Xue, Anlai Wang, Jun Pan
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Patent number: 9676751Abstract: The present invention is directed to 2-amino-3-ester pyridyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-amino-3-ester pyridyl compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: GrantFiled: December 18, 2014Date of Patent: June 13, 2017Assignee: MERCK SHARP & DOHME CORP.Inventors: Scott D. Kuduk, Jason W. Skudlarek
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Patent number: 9676752Abstract: Imidazolidine-2,4-dione derivatives of formula (I): The compounds have anti-proliferative activity and are useful for treating pathological states and diseases linked to an abnormal cell proliferation such as cancer.Type: GrantFiled: December 31, 2013Date of Patent: June 13, 2017Assignee: IPSEN PHARMA S.A.S.Inventors: Serge Auvin, Christophe Lanco, Qi Chao, Kaichun Gu
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Patent number: 9676754Abstract: The invention disclosed herein is directed to compounds of Formula I and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of Formula I, or a pharmaceutically acceptable salt thereof. The invention disclosed herein is also directed to methods of treating prostate, breast, ovarian, liver, kidney, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention disclosed herein is further directed to methods of treating prostate, breast, colon, pancreatic, chronic lymphocytic leukemia, melanoma and other cancers comprising administration of a therapeutically effective amount of a selective PPAR? antagonist.Type: GrantFiled: December 10, 2013Date of Patent: June 13, 2017Assignee: Inception 2, Inc.Inventors: Nicholas Simon Stock, Austin Chih-Yu Chen, Yalda Mostofi Bravo, Jason Duarte Jacintho, Jill Melissa Baccei, Brian Andrew Stearns, Ryan Christopher Clark
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Patent number: 9676755Abstract: The present invention relates to a graphene nanoribbon, comprising a repeating unit which comprises at least one modification, wherein the modification is selected from a heteroatomic substitution, a vacancy, a sp3 hybridization, a Stone-Wales defect, an inverse Stone-Wales defect, a hexagonal sp2 hybridized carbon network ring size modification, and any combination thereof.Type: GrantFiled: May 13, 2013Date of Patent: June 13, 2017Assignees: BASF SE, EMPA-EIDGENOESSISCHE MATERIALPRUEFUNGS-UND FORSCHUNGSANSTALT, MAX-PLANCK-GESELLSCHAFT ZUR FOERDERUNG DER WISSENSCHAFEN E.V.Inventors: Roman Fasel, Pascal Ruffieux, Klaus Muellen, Jinming Cai, Xinliang Feng, Reinhard Berger
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Patent number: 9676756Abstract: Provided are substituted pyrimidinyl compounds for inhibition of JAK and/or Syk kinase, pharmaceutical compositions thereof, methods for inhibiting JAK and/or Syk kinase activity, and methods for treating conditions mediated at least in part by JAK and/or Syk kinase activity.Type: GrantFiled: October 8, 2013Date of Patent: June 13, 2017Assignee: PORTOLA PHARMACEUTICALS, INC.Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Anjali Pandey
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Patent number: 9676757Abstract: The present invention relates to heterocyclic compounds, and pharmaceutically acceptable compositions thereof, useful as Nav1.6 inhibitors.Type: GrantFiled: February 26, 2015Date of Patent: June 13, 2017Assignee: Merck Patent GmbHInventors: Brian A. Sherer, Nadia Brugger
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Patent number: 9676758Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g.Type: GrantFiled: April 29, 2016Date of Patent: June 13, 2017Assignee: Arena Pharmaceutical, Inc.Inventors: Yifeng Xiong, Andrew J. Grottick, Henry Korman, Juerg Lehmann, Albert S. Ren, Graeme Semple, Didier JC Bagnol
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Patent number: 9676759Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: May 7, 2013Date of Patent: June 13, 2017Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
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Patent number: 9676760Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: May 11, 2016Date of Patent: June 13, 2017Assignee: Gilead Sciences, Inc.Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
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Patent number: 9676761Abstract: The present invention relates to difluoroethyl-oxazole substituted bridged spiro[2.4] heptane derivatives of formula (I), wherein the substituents at the piperidine ring are in trans-arrangement, their preparation and their use as pharmaceutically active compounds.Type: GrantFiled: June 24, 2014Date of Patent: June 13, 2017Assignee: ACTELION PHARMACEUTICALS, LTD.Inventors: Olivier Corminboeuf, Sylvaine Cren, Davide Pozzi
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Patent number: 9676762Abstract: The present invention encompasses compounds of general formula (1) wherein A, B, X, R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.Type: GrantFiled: August 24, 2016Date of Patent: June 13, 2017Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Ioannis Sapountzis
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Patent number: 9676763Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.Type: GrantFiled: October 1, 2015Date of Patent: June 13, 2017Assignees: President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc.Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
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Patent number: 9676764Abstract: A compound having the structure according to formula III wherein: X is NH or S; R1 is H or (1C-4C)alkyl; R2 is (1C-4C)alkyl, phenyl or a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, which alkyl, phenyl or aromatic ring is optionally substituted with one or more groups selected from (1C-4C)alkyl, (1C-4C)alkyloxy, halo(1C-4C)alkyl, halo(1C-4C)alkyloxy, phenyloxy, phenylthio, halogen, or nitro; R3 and R4 are each independently H, (1C-6C)alkyl, (2C-6C) alkenyl, (2C-6C)alkynyl, cyano, (3C-6C)cycloalkyl, phenyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring, a monocyclic non-aromatic ring having one or more N-, O- or S-atoms in the ring, each optionally substituted with hydroxyl, (1C-4C)alkoxy, phenyl, cycloalkyl, piperidyl, piperazinyl, furyl, thienyl, pirazinyl, pyrrolyl, 2H-pyrrolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyrrolidonyl, pyrrolinyl, imidazolinyl, imidazolyl, a monocyclic aromatic ring having one or more N-, O- or S-atoms in the ring,Type: GrantFiled: July 22, 2016Date of Patent: June 13, 2017Assignees: Compound Handling B.V., Stichting Katholieke UniversiteitInventors: Onno Van Hooij, Jacobus Antonius Schalken, Hendrik Engelbertus Vietor, Dennis Patrick Piet, Petrus Emmanuel Marie Maas, Johann Heinrich Tijhuis, Sirik Deerenberg, Nanda Elisabeth Sprenkels, Siu Ha Tang
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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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Patent number: 9676766Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.Type: GrantFiled: November 17, 2010Date of Patent: June 13, 2017Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Ulf Bömer
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Patent number: 9676767Abstract: The disclosure provides an indoloacridine-containing derivative represented by formula (I), wherein A is a group represented by formula (II), and wherein X, Y, Z and W represent a carbon atom or a nitrogen atom, and at least one of W, X, Y and Z represent a nitrogen atom; R represents a phenyl group, a biphenylyl group, a naphthyl group or a phenanthryl group. The disclosure further provides a process for preparing the compound. The disclosure further provides an organic electroluminescent device comprising the compound. This compound can be used as a phosphorescence host material, a hole-injecting material or a hole-transporting material in an organic electroluminescent device.Type: GrantFiled: May 30, 2014Date of Patent: June 13, 2017Assignees: BOE TECHNOLOGY GROUP CO., LTD., JILIN OLED MATERIAL TECH CO., LTD.Inventors: Wenyu Ma, Xiaoyu Ma, Hui Wang, Na Li
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Patent number: 9676768Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: March 20, 2015Date of Patent: June 13, 2017Assignee: ASTEX THERAPEUTICS LIMITEDInventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
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Patent number: 9676769Abstract: The compounds of formula (I) are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumor growth.Type: GrantFiled: March 13, 2014Date of Patent: June 13, 2017Assignee: Proximagen LimitedInventors: Max Espensen, Lee Patient, David Evans, Iain Simpson, Edward Savory
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Patent number: 9676770Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as pancreatic cancer, prostate cancer, breast cancer, bladder cancer, lung cancer, gastric cancer, leukemia and/or melanoma and the like.Type: GrantFiled: September 15, 2015Date of Patent: June 13, 2017Assignee: Celgene Quanticel Research, Inc.Inventors: Young K. Chen, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
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Patent number: 9676771Abstract: A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is N, C(OH), or CH; Y is H or OH; each of Z1-Z5 is independently H or halogen; R4 is H, OH, NH2, NHR8, NR8R9 or R8; R5, R6, and R7 is each independently H, halogen, OR8, R8, NHR8, NR8R9, CO2R8, CONR8R9, SO2NR8R9, or R5 and R6 together with the carbon atoms to which R5 and R6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and R8 and R9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R8 and R9 together with the nitrogen tType: GrantFiled: May 13, 2014Date of Patent: June 13, 2017Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Xue Zhi Zhao, Steven Smith, Mathieu Metifiot, Barry Johnson, Christophe Marchand, Stephen H. Hughes, Yves Pommier, Terrence R. Burke, Jr.
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Patent number: 9676772Abstract: This invention concerns pyrroloquinoline derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, Parkinson's disease, Huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, Irritable Bowel Syndrome. The compounds have the general formula (XIV), wherein the symbols have the meanings given in the description.Type: GrantFiled: July 25, 2013Date of Patent: June 13, 2017Assignees: Uniwersyter Jagiellonski, Instytut Farmakologii Polskiej Akademii Nauk, Centre National De La Recherche Scientifique, Universite de MontpellierInventors: Pawel Zajdel, Katarzyna Grychowska, Maciej Pawlowski, Anna Partyka, Anna Wesolowska, Andrzej J. Bojarski, Piotr Popik, Tomasz Kos, Grzegorz Satala, Frederic Lamaty, Evelina Colacino, Jean Martinez, Gilles Subra, Xavier Bantreil
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Patent number: 9676773Abstract: Provided is a novel compound having a selective JAK3-inhibitory effect and also having excellent oral absorbability. Also provided is a pharmaceutical agent, which is based on a JAK3-inhibitory effect and is useful for preventing and/or treating a disease involving the JAK3, and in particular, rheumatoid arthritis or multiple sclerosis. An azaindole derivative having a cycloalkenyl group, which is represented by the following formula (I), or a salt thereof, and a pharmaceutical composition containing the same: where R1 to R4, m and n have the same meanings as those defined in the description.Type: GrantFiled: February 4, 2015Date of Patent: June 13, 2017Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Masayuki Nakamura, Hiroyoshi Yamanaka, Kazuaki Shibata, Morihiro Mitsuya, Takafumi Harada
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Patent number: 9676774Abstract: Compounds and compositions for treating, preventing or managing cancer are disclosed. The compositions provided herein comprise SNS-595 and N-desmethyl-SNS-595. Also provided are pharmaceutical compositions comprising the compounds and methods of treatment using the compounds and compositions.Type: GrantFiled: May 16, 2016Date of Patent: June 13, 2017Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Daniel C. Adelman, Marc J. Evanchik, Anantha Sudhakar, Jeffrey William Jacobs, Jeffrey A. Silverman
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Patent number: 9676775Abstract: Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).Type: GrantFiled: November 15, 2016Date of Patent: June 13, 2017Assignee: Bristol-Myers Squibb CompanyInventors: Ivar M. McDonald, Naidu S. Chowdari, Walter Lewis Johnson, Yong Zhang, Robert M. Borzilleri, Sanjeev Gangwar
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Patent number: 9676776Abstract: Provided herein are isoergoline compounds and pharmaceutical 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 pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1A, 5-HT1B and 5-HT1D receptors without agonizing the 5-HT2B receptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HT2B adrenergic alpha2A and/or the alpha2B receptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein.Type: GrantFiled: January 20, 2016Date of Patent: June 13, 2017Assignee: Xoc Pharmaceuticals, Inc.Inventors: Thomas Armer, Geoff McKinley, Scott Borland, Miguel Guzman
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Patent number: 9676777Abstract: An optically active (2S,5R)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid compound defined by the following formula (F): wherein R1 represents CO2R, CO2M, or CONH2, wherein R represents an allyl group or a benzyl group, and M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.Type: GrantFiled: January 27, 2016Date of Patent: June 13, 2017Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Takao Abe, Masayuki Okue, Yoshiaki Sakamaki
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Patent number: 9676778Abstract: The present disclosure provides compounds of formula (I) wherein the variables are as defined herein that are JAK3 inhibitors and therefore useful for the treatment of diseases treatable by inhibition of JAK3 such as cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: GrantFiled: November 19, 2013Date of Patent: June 13, 2017Assignee: PRINCIPIA BIOPHARMA INC.Inventors: David Michael Goldstein, Kenneth Albert Brameld, Tim Owens
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Patent number: 9676779Abstract: 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). 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: November 20, 2013Date of Patent: June 13, 2017Assignee: DiscoveryBiomed, Inc.Inventors: Erik Schwiebert, John Streiff, John Dixon, Hongwu Gao
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Patent number: 9676780Abstract: Disclosed are compounds of Formula A: (structurally represented) where “RG1”, “RG2a”, “RG4”, “RG5”, “MG1”, “n” and “m” are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.Type: GrantFiled: December 20, 2013Date of Patent: June 13, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Yeon-Hee Lim, Andrew Stamford, Rongze Kuang, Paul Tempest, Younong Yu, Michael Berlin, Pauline Ting, Gang Zhou, Tao Yu, Christopher Boyce, Joseph Michael Kelly, Jayaram R. Tagat, Junying Zheng, Xianhai Huang, Wei Zhou, Jae-Hun Kim, Nicolas Zorn, Dong Xiao, Gioconda V. Gallo, Walter Won, Heping Wu, Rajan Anand, Qiaolin Deng
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Patent number: 9676781Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: GrantFiled: May 19, 2015Date of Patent: June 13, 2017Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Sandra Handschuh, Herbert Nar
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Patent number: 9676782Abstract: Described are negative allosteric modulators of metabotropic glutamate receptor 3 (mGlu3), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, cognitive disorders, schizophrenia, Alzheimer's disease, or cancer in a subject.Type: GrantFiled: June 12, 2015Date of Patent: June 13, 2017Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Julie L. Engers, Leah C. Konkol
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Patent number: 9676783Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: GrantFiled: September 4, 2015Date of Patent: June 13, 2017Assignee: Array BioPharma, Inc.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 9676784Abstract: The present invention relates to new fused imidazolyl derivatives having a high affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.Type: GrantFiled: December 18, 2014Date of Patent: June 13, 2017Assignee: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: José-Luis Díaz-Fernández, Carmen Almansa-Rosales, Piotr Nieczypor
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Patent number: 9676785Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: July 14, 2014Date of Patent: June 13, 2017Assignee: Celgene CAR LLCInventors: Deqiang Niu, Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Lixin Qiao
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Patent number: 9676786Abstract: The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.Type: GrantFiled: December 23, 2014Date of Patent: June 13, 2017Assignee: THE UNIVERSITY OF LIVERPOOLInventors: Martin Leuwer, Paul O'Neill, Neil Berry, Chandrakala Pidathala
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Patent number: 9676787Abstract: Compounds used as labels with properties comparable to known fluorescent compounds. The compounds are conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.Type: GrantFiled: August 20, 2013Date of Patent: June 13, 2017Assignees: Pierce Biotechnology, Inc., Dyomics GmbHInventors: Greg Hermanson, Peter T. Czerney, Surbhi Desai, Matthias S. Wenzel, Frank G. Lehmann, Marie Christine Nlend
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Patent number: 9676788Abstract: Disclosed is a compound of formula (I) or formula (II): (Formulas should be inserted here) wherein R1-R6 are as defined herein. Also disclosed are a pharmaceutical composition comprising such a compound and a method of treating or preventing cancer in a mammal in need thereof, comprising administering to the mammal a compound of formula (I) or formula (II).Type: GrantFiled: February 5, 2015Date of Patent: June 13, 2017Assignees: The United States of America, as represented by the Secretary of Health and Human Services, University of HawaiiInventors: William J. Chain, John A. Beutler, David Fash, William D. Figg, Zhenwu Li, Cody John Peer, Joe William Ramos, Florian J. Sulzmaier
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Patent number: 9676789Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel aminated homoharringtonine derivatives of formula (I) and a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.Type: GrantFiled: August 20, 2012Date of Patent: June 13, 2017Assignee: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai