Ring Nitrogen In The Additional Hetero Ring Patents (Class 514/235.5)
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Patent number: 12097200Abstract: The present invention relates to a use of BI853520 or a pharmaceutically acceptable salt thereof in preparing drugs for treating tumors in combination with chemotherapeutic drugs.Type: GrantFiled: July 5, 2023Date of Patent: September 24, 2024Assignee: INXMED (NANJING) CO., LTD.Inventors: Zaiqi Wang, Jiangwei Zhang
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Patent number: 11572368Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.Type: GrantFiled: August 11, 2016Date of Patent: February 7, 2023Assignees: The General Hospital Corporation, The Broad Institute, Inc., Massachusetts Institute of TechnologyInventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen J. Haggarty, Yan-Ling Zhang
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Patent number: 11541050Abstract: This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.Type: GrantFiled: September 4, 2020Date of Patent: January 3, 2023Assignee: JANSSEN SCIENCES IRELAND UCInventors: David Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach
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Patent number: 11542242Abstract: Provided herein are compounds of Formula IV, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.Type: GrantFiled: August 19, 2020Date of Patent: January 3, 2023Assignee: REGENACY PHARMACEUTICALS, LLCInventors: John H. van Duzer, Ralph Mazitschek
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Patent number: 11459308Abstract: The present invention is related to the development of therapeutics and prophylactics for the treatment and/or prevention of filovirus infection in humans and other mammals. A new class of small molecules is disclosed that inhibits the interaction of naturally processed (i.e., proteolytically cleaved) filovirus glycoprotein (GPCL) with its host receptor Niemann-Pick C1 (NPC1) protein and thus block infection of host cells by filoviruses. Also disclosed are methods of using the small molecule inhibitors in the treatment/prevention of filovirus infection.Type: GrantFiled: December 5, 2017Date of Patent: October 4, 2022Assignees: Microbiotix, Inc., Albert Einstein College of Medicine, The Government of the United States as Represented by the Secretary of the ArmyInventors: Terry L. Bowlin, Donald T. Moir, Kartik Chandran, John M. Dye, Jr., John D. Williams, Zachary D. Aron, Jay P. Barbor, Kelly N. Lively, Peter J. Nash, Debra M. Mills, Arnab Basu
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Patent number: 11433068Abstract: This disclosure provides compositions and methods of treating cancer by inhibiting histone methyltransferases alone or in combination by synergistically inhibiting a histone demethylase, or a histone deacetylase (HDAC), or a bromodomain (BRD)-containing protein, or a B-Raf kinase. In particular, the cancers have deficient of SWI/SNF chromatin remodeling complexes because of mutations in one or more of the complex's subunit members.Type: GrantFiled: September 7, 2017Date of Patent: September 6, 2022Assignee: THE GENERAL HOSPITAL CORPORATIONInventors: David E. Fisher, Qing Yu Weng, Shinichiro Kato
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Patent number: 11434240Abstract: The present invention provides compounds of formula I, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.Type: GrantFiled: July 24, 2020Date of Patent: September 6, 2022Assignee: Nimbus Lakshmi, Inc.Inventors: Craig E. Masse, Jeremy Robert Greenwood, Donna L. Romero, Geraldine C. Harriman, Ronald T. Wester, Mee Shelley, Joshua Jahmil Kennedy-Smith, Markus Dahlgren, Sayan Mondal, Shaughnessy Robinson
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Patent number: 11420969Abstract: Anti-angiogenic treatments, for example treatment of ocular neovascularization or cancer, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of treating or preventing fibrosis and compounds for use in such methods are described.Type: GrantFiled: September 26, 2018Date of Patent: August 23, 2022Assignee: Exonate LimitedInventors: Andrew Douglas Baxter, Jonathan Morris, Andrew David Morley
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Patent number: 11407744Abstract: The present disclosure relates to a novel compound and a pharmaceutical composition comprising the same. The compound according to the present disclosure has effects for activating autophagy, and thus can be valuably used for preventing or treating diseases associated with autophagy regulation.Type: GrantFiled: May 31, 2019Date of Patent: August 9, 2022Assignee: AUTOPHAGYSCIENCES INC.Inventors: Jung Ju Kim, Seong-Won Song, Hye Jeong Shin, Hyeongwan Choi
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Patent number: 11149035Abstract: A compound of formula (I) wherein R1, R2, R3, R4, X, Y, and A are as defined herein. The compounds of the present invention are inhibitors of hematopoletic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: June 11, 2018Date of Patent: October 19, 2021Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DFVELOPMENT LIMITEDInventors: David Norman Deaton, Barry George Shearer, Mark Andrew Youngman
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Patent number: 11130779Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).Type: GrantFiled: December 17, 2019Date of Patent: September 28, 2021Assignee: The Salk Institute for Biological StudiesInventors: Ronald M. Evans, Michael Downes
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Patent number: 10959984Abstract: The present invention provides compositions, methods, and kits comprising one or more ROR? inhibitors, alone or in combination with one or more anticancer drugs, such as an anti-androgen drug, that are useful for treating cancer, e.g., prostate cancer, such as castration-resistant prostate cancer (CRPC), and numerous other types of cancer including lung cancer, breast cancer, liver cancer, ovarian cancer, endometrial cancer, bladder cancer, colon cancer, lymphoma, and glioma.Type: GrantFiled: September 11, 2017Date of Patent: March 30, 2021Assignee: The Regents of the University of CaliforniaInventors: Hongwu Chen, June X. Zou, Junjian Wang
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Patent number: 10946024Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.Type: GrantFiled: June 18, 2019Date of Patent: March 16, 2021Assignee: Epizyme, Inc.Inventor: Heike Keilhack
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Patent number: 10864159Abstract: The present invention relates to an ophthalmic aqueous composition containing PGF2? analogues for treating ocular hypertension and glaucoma, to a method for treating ocular hypertension and glaucoma by administering said composition to a subject in need of such treatment, and to a method for increasing aqueous solubility and stability of PGF2? analogues in an aqueous composition.Type: GrantFiled: June 18, 2018Date of Patent: December 15, 2020Assignees: SANTEN PHARMACEUTICAL CO., LTD., AGC INC.Inventors: Timo Reunamaki, Pertti Pellinen, Olli Oksala, Kari Lehmussaari
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Patent number: 10813920Abstract: Provided is an agent for treating or preventing a corneal endothelial disorder wherein cell proliferation is required. More specifically, provided is an agent for treating or preventing a corneal endothelial disorder, wherein cell proliferation is required, said agent comprising a p38MAP kinase inhibitor. In a preferred embodiment, the corneal endothelial disorder is a wound. In a preferred embodiment, the p38MAP kinase inhibitor is soluble in water. The p38MAP kinase inhibitor may comprise 4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole (SB203580) or a salt thereof.Type: GrantFiled: November 13, 2014Date of Patent: October 27, 2020Assignee: THE DOSHISHAInventors: Noriko Koizumi, Naoki Okumura, Shigeru Kinoshita
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Patent number: 10807952Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I? and I?? or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.Type: GrantFiled: February 26, 2018Date of Patent: October 20, 2020Assignee: Achillion Pharmaceuticals, Inc.Inventors: Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
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Patent number: 10772858Abstract: This disclosure relates to benzhydrol derivatives for managing conditions related to the Hypoxia Inducible Factor (HIF) pathway such as uses in treating cancer. In certain embodiment, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiment, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof.Type: GrantFiled: May 2, 2016Date of Patent: September 15, 2020Assignees: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC., EMORY UNIVERSITYInventors: Binghe Wang, Erwin Van Meir, Jalisa Holmes Ferguson, Stefan Kaluz, Xingyue Ji
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Patent number: 10745350Abstract: The invention relates to new compounds with low cytotoxicity for blocking ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of treating disorders including, but not limited to, cancers, neurodegenerative diseases, inflammatory disorders and autoimmune disorders and metabolic disorders.Type: GrantFiled: July 30, 2016Date of Patent: August 18, 2020Assignee: Calgent Biotechnology Co., Ltd.Inventors: Yun Yen, Jing-ping Liou, Shiow-lin Pan
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Patent number: 10738010Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.Type: GrantFiled: March 13, 2019Date of Patent: August 11, 2020Assignee: Akebia Therapeutics, Inc.Inventors: Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
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Patent number: 10577356Abstract: The present invention provides compounds having a CB1 receptor-binding moiety and a directing moiety. In related aspects, the invention provides pharmaceutical compositions containing compounds of the invention, methods for inhibiting a pathway modulated in part by the CB1 receptor activity, and methods for treating a condition or disorder mediated in part by CB1 receptor activity. In certain embodiments, the compounds are compounds of Formula I. Methods of preparing compounds of Formula I are also described. In another aspect, the invention provides methods of identifying a selective agonist of the beta-arrestin pathway over the G-protein pathway.Type: GrantFiled: October 5, 2018Date of Patent: March 3, 2020Assignee: The University of North Carolina at GreensboroInventors: Patricia H. Reggio, Derek M. Shore, Dow P. Hurst
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Patent number: 10550149Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).Type: GrantFiled: June 28, 2018Date of Patent: February 4, 2020Assignee: Salk Institute for Biological StudiesInventors: Ronald M. Evans, Michael Downes
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Patent number: 10481169Abstract: Provided is a novel method and the like for diagnosing a lifestyle disease. The method for diagnosing a lifestyle disease provided by the present invention includes: collecting a biological sample from a subject; measuring the concentration of a fatty acid amide contained in the biological sample; determining whether the subject suffers from a lifestyle disease or a lifestyle disease has progressed when the measured value of the concentration of the fatty acid amide in the sample obtained from the subject is lower than a measurement result obtained from a healthy subject.Type: GrantFiled: February 27, 2018Date of Patent: November 19, 2019Assignees: TOYOTA JIDOSHA KABUSHIKI KAISHA, NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITYInventors: Koji Uchida, Takahiro Shibata, Kenji Ishikawa, Oi Lun Helena Li, Tadashi Matsushita, Ryosuke Kikuchi, Junzo Ukai
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Patent number: 10472314Abstract: Using a combination of Kumada, Suzuki and Biellmann chemistry, various menaquinones can synthesized rapidly and with stereochemical integrity offering a new way of preparing these vitamin K2 components for the pharmaceutical market. In one embodiment a process for the preparation of a compound of formula (I) is defined including a step in which (i) a compound of formula (II) is reacted with a compound of formula (III) wherein R is an alkyl group; LG is a leaving group; m is an integer from 0 to 8; n is an integer of from 0 to 9; and X is hydrogen, halide, hydroxyl or protected hydroxyl; in the presence of a copper, nickel or palladium catalyst.Type: GrantFiled: June 20, 2017Date of Patent: November 12, 2019Assignee: KAPPA BIOSCIENCE ASInventors: Lars Skattebol, Inger Reidun Aukrust, Marcel Sandberg
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Patent number: 10399950Abstract: The present invention relates to novel non-steroidal brassinosteroid mimetic derivatives of formula (I) as defined herein, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.Type: GrantFiled: January 31, 2014Date of Patent: September 3, 2019Assignee: Syngenta Partcipations AGInventors: Mathilde Denise Lachia, Pierre Joseph Marcel Jung, Joerg Leipner, David Brocklehurst, Alain De Mesmaeker, Sebastian Volker Wendeborn
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Patent number: 10357477Abstract: The invention provides compounds having the general formula I: and salts thereof, wherein the variables RA, RB, RC, L1, L2, L3, A, B, C, X, Y, Z, E, m, n, and p have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.Type: GrantFiled: September 13, 2017Date of Patent: July 23, 2019Assignee: Regents of the University of MinnesotaInventors: Liqiang Chen, Teng Ai
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Patent number: 10329314Abstract: Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: February 28, 2018Date of Patent: June 25, 2019Assignee: ChemoCentryx, Inc.Inventors: Pingchen Fan, Antoni Krasinski, Venkat Reddy Mali, Shichang Miao, Sreenivas Punna, Yang Song, Valentino J. Stella, Yibin Zeng, Penglie Zhang
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Patent number: 10266492Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.Type: GrantFiled: July 25, 2017Date of Patent: April 23, 2019Assignee: ChemoCentryx, Inc.Inventors: Pingchen Fan, Jaroslaw Kalisiak, Antoni Krasinski, Rebecca M. Lui, Jay Powers, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Patent number: 10266505Abstract: The invention describes compounds that inhibit both HDAC and GSK3? (i.e., HDAC/GSK3? dual inhibitors). The invention further describes compositions containing these HDAC/GSK3? dual inhibitors, as well as methods and kits using these HDAC/GSK3? dual inhibitors to treat various medical conditions. The invention also provides methods and kits using a HDAC inhibitor and a GSK3? to treat various medical conditions, and compositions containing a HDAC inhibitor and a GSK3?. Medical conditions treatable with various embodiments of the invention include but are not limited to cancers and tumors.Type: GrantFiled: June 19, 2018Date of Patent: April 23, 2019Assignee: CEDARS-SINAI MEDICAL CENTERInventors: Mouad Edderkaoui, Ramachandran Murali, Stephen Pandol
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Patent number: 10238661Abstract: Disclosed are methods for treating various bacterial infections with (2R,4S,4aS)-11-fluoro-2,4-dimethyl-8-[(4S)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,2,4,4a-tetrahydro-2?H,6H-spiro[1,4-oxazino[4,3-a][1,2]oxazolo[4,5-g]quinoline-5,5?-pyrimidine]-2?,4?,6?(1?H,3?H)-trione, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 27, 2015Date of Patent: March 26, 2019Assignee: Entasis Therapeutics LimitedInventor: Michael Huband
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Patent number: 10189830Abstract: Disclosed herein are alkyl-heteroaryl substituted quinone derivative compounds and methods of using such compounds for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging.Type: GrantFiled: March 14, 2014Date of Patent: January 29, 2019Assignee: BIOELECTRON TECHNOLOGY CORPORATIONInventors: Andrew W. Hinman, Kieron E. Wesson, Christopher R. Cornell
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Patent number: 10155725Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.Type: GrantFiled: December 28, 2015Date of Patent: December 18, 2018Assignee: MERIAL, INC.Inventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
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Patent number: 10118914Abstract: The present invention provides compounds having a CB1 receptor-binding moiety and a directing moiety. In related aspects, the invention provides pharmaceutical compositions containing compounds of the invention, methods for inhibiting a pathway modulated in part by the CB1 receptor activity, and methods for treating a condition or disorder mediated in part by CB1 receptor activity. In certain embodiments, the compounds are compounds of Formula I. Methods of preparing compounds of Formula I are also described. In another aspect, the invention provides methods of identifying a selective agonist of the beta-arrestin pathway over the G-protein pathway.Type: GrantFiled: December 19, 2016Date of Patent: November 6, 2018Assignee: The University of North Carolina at GreensboroInventors: Patricia H. Reggio, Derek M. Shore, Dow P. Hurst
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Patent number: 10112926Abstract: The present invention provides compounds of formula (I) which inhibit the activity of PI 3-kinase gamma isoform, which are useful for the treatment of diseases mediated by the activation of PI 3-kinase gamma isoform.Type: GrantFiled: April 24, 2014Date of Patent: October 30, 2018Assignee: Novartis AGInventors: Benjamin Richard Bellenie, Graham Charles Bloomfield, Ian Bruce, Andrew James Culshaw, Edward Charles Hall, Gregory John Hollingworth, James Neef, Matthew Spendiff, Simon James Watson
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Patent number: 10100019Abstract: The present invention relates to a N2-(2-methoxyphenyl)pyrimidine derivative, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of cancer comprising the same as an active ingredient. The N2-(2-methoxyphenyl)pyrimidine derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention is very effective in suppressing anaplastic lymphoma kinase (ALK) activity and as a result it can improve the effectiveness of treatment on cancer cells having anaplastic lymphoma kinase (ALK) fusion proteins such as EML4-ALK and NPM-ALK, so that it can be effectively used as a pharmaceutical composition for preventing or treating cancer.Type: GrantFiled: April 6, 2016Date of Patent: October 16, 2018Assignee: Korea Research Institute of Chemical TechnologyInventors: Pilho Kim, Hyoung Rae Kim, Sung Yun Cho, Jae Du Ha, Hee Jung Jung, Chang Soo Yun, Jong Yeon Hwang, Chi Hoon Park, Chong Ock Lee, Sunjoo Ahn, Chong Hak Chae
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Patent number: 10080750Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: GrantFiled: April 18, 2017Date of Patent: September 25, 2018Assignee: Merck Patent GmbHInventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth C. Deselm, Hui Qiu, Yufang Xiao, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
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Patent number: 10076529Abstract: Compositions, compounds, and methods with significant antiviral effect against RNA viruses and especially orthomyxoviruses are contemplated, and target the viral promoter that is formed by the 5? and 3?-UTR sequences of the viral genome.Type: GrantFiled: March 11, 2016Date of Patent: September 18, 2018Assignee: NANT HOLDINGS IP, LLCInventors: Kayvan Niazi, Shahrooz Rabizadeh, Anne-Laure Le Ny, Oleksandr Buzko, Justin Golovato, Patrick Soon-Shiong
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Amide derivatives of 1-oxa-4,9-diazaspiro undecane compounds having multimodal activity against pain
Patent number: 10065971Abstract: The present invention relates to compounds having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opiod receptor and more particularly to diazaspiro undecane compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain. wherein Y is n is 1 or 2; q is 1, 2, 3, 4, 5 or 6; X is a bond, —C(O)O—, —C(O)NR8—, —C(O)—, —O— or —C(R4R4?)—; R1 is C(O)R5 or S(O)2R5.Type: GrantFiled: June 2, 2015Date of Patent: September 4, 2018Assignee: ESTEVE PHARMACEUTICALS S.A.Inventors: Marina Virgili-Bernado, Monica Alonso-Xalma, Carlos Alegret-Molina, Carmen Almansa-Rosales, Ramón Merce-Vidal -
Patent number: 10035819Abstract: Provided herein are deuterated compounds and compositions useful in increasing PPAR? activity. The compounds have a formula where L5 comprises at least one deuterium. Exemplary species include The compounds and compositions provided herein are useful for the treatment of PPAR? related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).Type: GrantFiled: April 7, 2017Date of Patent: July 31, 2018Assignee: The Salk Institute for Biological StudiesInventors: Ronald M. Evans, Michael Downes
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Patent number: 10010547Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.Type: GrantFiled: February 9, 2015Date of Patent: July 3, 2018Assignee: Cascadian Therapeutics, Inc.Inventors: Robert George Boyle, David Winter Walker, Richard Justin Boyce, Scott Peterson, Francine Farouz, Cong Hung Vo
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Patent number: 9944597Abstract: The present invention provides polysubstituted pyrrole compounds, pharmaceutically effective salts, prodrugs, solvates and hydrates thereof, having antimitotic, antiproliferative and cytotoxic activity, activity against cells expressing the drug efflux protein, P-glycoprotein, or cells expressing the ?-III isotype of tubulin and antitumor activity. Also provided are methods of utilizing these compounds for inhibiting the proliferation of cancer cells as well as their medical use, in particular for treating cancer, including drug resistant cancer.Type: GrantFiled: September 16, 2014Date of Patent: April 17, 2018Assignees: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, VIRGINIA COMMONWEALTH UNIVERSITY, UNIVERSITY OF RICHMONDInventors: Glen E. Kellogg, Chenxiao Da, Ashutosh Tripathi, John T. Gupton, Nakul Telang, James A. Sikorski, Susan L. Mooberry, Cristina Rohena
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Patent number: 9938273Abstract: Disclosed are compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Z2, Z3, and Z5 are as described herein, compositions thereof, and uses thereof.Type: GrantFiled: December 6, 2016Date of Patent: April 10, 2018Assignee: Plexxikon Inc.Inventors: Guoxian Wu, Jeffrey Wu, Katrina Chan, Ken Dong, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Wayne Spevak, Ying Zhang
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Patent number: 9932330Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.Type: GrantFiled: September 19, 2017Date of Patent: April 3, 2018Assignees: The University of Nottingham, NewSouth Innovations PTY LimitedInventors: David Bates, Jonathan Morris
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Patent number: 9926319Abstract: The invention provides novel substituted pyridyl piperidine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.Type: GrantFiled: March 10, 2015Date of Patent: March 27, 2018Assignees: MERCK PATENT GMBH, Cancer Research Technology LimitedInventors: Kai Schiemann, Frank Stieber, Michel Calderini, Julian Blagg, Aurelie Mallinger, Dennis Waalboer, Christian Rink, Simon Ross Crumpler
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Patent number: 9889138Abstract: The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.Type: GrantFiled: July 15, 2016Date of Patent: February 13, 2018Assignee: Epizyme, Inc.Inventor: Heike Keilhack
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Patent number: 9850207Abstract: Provided are methods for treating, reducing, alleviating, and/or inhibiting neuropathic pain by orally, intravenously or intrathecally administering an effective amount of an inhibitor of soluble epoxide hydrolase (“sEH”), to a patient in need thereof. The neuropathic pain treated is selected from the group consisting of post-herpetic neuralgia, trigeminal neuralgia, focal peripheral nerve injury, and anesthesia dolorosa, central pain due to stroke or mass lesion, spinal cord injury, or multiple sclerosis, and peripheral neuropathy due to diabetes, HIV, or chemotherapy.Type: GrantFiled: February 1, 2013Date of Patent: December 26, 2017Assignee: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Kin Sing Lee, Bora Inceoglu, Karen Wagner
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Patent number: 9796707Abstract: Anti-angiogenic treatments, treatments of hyperpermeability disorders, treatments of neuropathic and neurodegenerative disorders, pain treatments, methods of reducing the risk of pre-eclampsia and compounds for use in such methods are described.Type: GrantFiled: May 31, 2017Date of Patent: October 24, 2017Assignees: The University of Nottingham, NewSouth Innovations PTY LimitedInventors: David Bates, Jonathan Morris
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Patent number: 9745268Abstract: Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.Type: GrantFiled: September 28, 2015Date of Patent: August 29, 2017Assignee: CHEMOCENTRYX, INC.Inventors: Pingchen Fan, Jaroslaw Kalisiak, Antoni Krasinski, Rebecca Lui, Jay Powers, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Patent number: 9717737Abstract: Methods of treating autophagy related diseases, e.g. cancer and malaria, using novel autophagy inhibiting agents are described.Type: GrantFiled: February 25, 2015Date of Patent: August 1, 2017Assignee: THE UNIVERSITY OF HONG KONGInventors: Jianbo Yue, Yingying Lu
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Patent number: 9675584Abstract: Disclosed herein are substituted pyrazinyl acrylic acids of Formula (II): and compositions thereof, which may be useful as inhibitors of PAS Kinase (PASK) activity in a human or animal for the treatment of diseases such as diabetes mellitus.Type: GrantFiled: March 19, 2015Date of Patent: June 13, 2017Assignee: BioEnergenix, LLCInventors: John M. McCall, Donna L. Romero, Michael Clare
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Patent number: 9610249Abstract: Methods for determining dosage of HER2-targeted anthracycline-containing immunoliposomes are disclosed, as are methods of treating cancer patients with HER2-positive tumors using dosages so determined. Upon administration, the dosages share the low cardiotoxicity profile of standard dosages of non-immunoliposomal (untargeted), anthracycline-containing liposomes.Type: GrantFiled: August 21, 2015Date of Patent: April 4, 2017Assignee: Merrimack Pharmaceuticals. Inc.Inventors: Joseph G. Reynolds, Kenneth J. Olivier, Jr., Bart S. Hendriks, Thomas Wickham, Stephan Klinz, Elena Geretti