Patents Issued in November 24, 2020
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Patent number: 10844026Abstract: Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.Type: GrantFiled: January 21, 2020Date of Patent: November 24, 2020Assignees: Biohaven Pharmaceutical Holding Company Ltd., Rutgers, The State University of New JerseyInventors: Garry Robert Smith, Allen B. Reitz, Mark McDonnell, Suzie Chen, Matthew D. Vera, Benjamin E. Blass, Jeffrey Claude Pelletier, Venkata N. Velvadapu, Jay Edward Wrobel
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Patent number: 10844027Abstract: The present invention provides a compound having the structure of the instant invention of a pharmaceutically acceptable salt or ester thereof, methods of preparing the same, and methods of treating a subject with compounds of the instant invention in combination therapies.Type: GrantFiled: September 16, 2016Date of Patent: November 24, 2020Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Andrew Kruegel, Dalibor Sames, Madalee G. Wulf, Jonathan A. Javitch
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Patent number: 10844028Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: GrantFiled: December 3, 2018Date of Patent: November 24, 2020Assignee: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
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Patent number: 10844029Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.Type: GrantFiled: June 15, 2017Date of Patent: November 24, 2020Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
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Patent number: 10844030Abstract: The present invention relates to a method for producing furfural, including: obtaining a sugar solution containing at least one of a monosaccharide having 5 carbon atoms and a polysaccharide containing the monosaccharide having 5 carbon atoms by carrying out a reaction with a specific resource as a raw material in the presence of a catalyst in a solvent; converting at least one of the monosaccharide and the polysaccharide containing the monosaccharide in the sugar solution into furfural by a dehydration reaction, so as to obtain a reaction solution; and separating the reaction solution into an organic layer and an aqueous layer, wherein an aromatic hydrocarbon solvent having a density of from 0.90 g/cm3 to 1.1 g/cm3 at 25° C. and under atmospheric pressure is used, and wherein the reaction solution is separated at a temperature higher than 90° C. and lower than 150° C.Type: GrantFiled: September 24, 2018Date of Patent: November 24, 2020Assignee: Mitsubishi Chemical CorporationInventors: Yusuke Izawa, Yosuke Suzuki, Masaru Utsunomiya
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Patent number: 10844031Abstract: The present application relates to a process for preparation of a compound of Formula (I) and Formula (IV): wherein is as described herein; and wherein and R are as described herein.Type: GrantFiled: November 15, 2019Date of Patent: November 24, 2020Assignee: IOWA STATE UNIVERSITY RESEARCH FOUNDATION, INC.Inventors: Aaron David Sadow, Zachary Benjamin Weinstein, George A. Kraus
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Patent number: 10844032Abstract: The present invention provides for compounds that inhibit the activity of an anti-apoptotic Bcl-2 family member Myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides for pharmaceutical compositions as well as methods for using compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein.Type: GrantFiled: July 2, 2018Date of Patent: November 24, 2020Assignee: Vanderbilt UniversityInventors: Taekyu Lee, Nicholas F. Pelz, Johannes Belmar, Zhiguo Bian, Edward T. Olejniczak, Stephen W. Fesik, Brian A. Chauder
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Patent number: 10844033Abstract: The present invention relates to methods of forming delta-lactone compounds by reaction of a diene with carbon dioxide in the presence of Pd and a phosphine ligand.Type: GrantFiled: May 16, 2017Date of Patent: November 24, 2020Assignees: Qatar Found. For Ed., Science and Community Development, Sultan Qaboos University, Leibniz-Institut Fur Katalyse e.V. an der Unversitat RostockInventors: Sarim Dastgir, Badria Al-Shihi, Mohammad Sharif, Matthias Beller, Ralf Jackstell
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Patent number: 10844034Abstract: A nonionic surfactant that is environmentally friendly, has excellent surface active power (emulsifying power and solubilizing power), and is capable of stably maintaining the excellent surface active power for a long time is provided. A nonionic surfactant of the present invention contains polyglycerol monoether represented by the formula (1), wherein a ring Z represents a condensed ring of an aromatic hydrocarbon ring having 6 to 14 carbon atoms and a 3 to 6-membered heterocycle containing an oxygen atom as a heteroatom; R1 is a substituent bonded to the ring Z and represents an aliphatic hydrocarbon group having 14 to 25 carbon atoms; the ring Z optionally has one or more substituents other than R1; and n is an average number of monomers of glycerol and represents 2 to 20.Type: GrantFiled: April 21, 2017Date of Patent: November 24, 2020Assignee: DAICEL CORPORATIONInventor: Yuichi Sakanishi
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Patent number: 10844035Abstract: The present disclosure relates to a cannabidiol compound and compositions thereof and processes for preparing the compound and compositions. The processes include an acid-catalyzed reaction of a suitably selected and substituted di-bromo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dibromo-cannabidiol compound or derivative thereof. The dibromo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.Type: GrantFiled: July 13, 2018Date of Patent: November 24, 2020Assignee: PURISYS LLCInventors: Lukas Dialer, Denis Petrovic, Ulrich Weigl
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Patent number: 10844036Abstract: A process of obtaining a purified geometric isomer of an unsaturated macrocyclic compound is disclosed herein. The process is effected by contacting an ion exchange medium comprising silver ions with a mixture comprising at least one geometric isomer of the unsaturated macrocyclic compound, to thereby obtain at least one fraction comprising the purified geometric isomer of the macrocyclic compound. A system configured for performing the process is also disclosed.Type: GrantFiled: December 5, 2017Date of Patent: November 24, 2020Assignee: Agan Aroma & fine chemicals Ltd.Inventors: Youlia Hagooly, Alexander Laskavy, Tehila Yosef Gerufi, Eyal Ben-Ari
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Patent number: 10844037Abstract: Acid generators comprising a carbocyclic aryl or heteroaromatic group substituted with at least one acetate moiety are provided. These acid generators are particularly useful as a photoresist composition component.Type: GrantFiled: February 24, 2016Date of Patent: November 24, 2020Assignee: Rohm and Haas Electronic Materials LLCInventor: Paul J. Labeaume
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Patent number: 10844038Abstract: This invention provides compounds of the formula (I): wherein Y1, Y2, Z, X1, X2, and W? are defined in the specification. These compounds are useful in the treatment of tyrosine kinases, MAPK signaling pathway kinases and PI3K/AKT/mTor signaling pathway kinases-mediated diseases or conditions, such as neurodegeneration, neuroprotection, cancer, autoimmune as well as other diseases and conditions associated with the modulation of tyrosine kinases selected from FYN, FYN Y531F, FLT3, FLT3-ITD, BRK, ITK, FRK, BTK, BMX, SRC, FGR, YES1, LCK, HCK, RET, CSK, LYN, and ROS1; MAPK pathway kinases selected from ARAF, BRAF, CRAF, ERK1/2, MEK1, MEK2, MEK3, MEK4, MEK5, MEK6, and MEK7; and PI3K/AKT/mTor pathway kinases: selected from mTor, PI3K ?, PI3K ?, PI3K ?, and PI3K ?.Type: GrantFiled: September 8, 2017Date of Patent: November 24, 2020Assignee: SABILA BIOSCIENCES LLCInventors: Tarek S. Mansour, Colleen E. Evans
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Patent number: 10844039Abstract: Substituted isoindolinones of Formula (I), methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat or ameliorate diseases, disorders, or conditions associated with protein malfunction, such as cancer, are provided.Type: GrantFiled: November 12, 2019Date of Patent: November 24, 2020Assignee: BioTheryX, Inc.Inventors: Kyle W. H. Chan, Aparajita Hoskote Chourasia, Paul E. Erdman, Leah Fung, Imelda Lam, Frank Mercurio, Robert Sullivan, Eduardo Torres
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Patent number: 10844040Abstract: Aspects of the present disclosure include compounds that activate Nrf2. Such compounds find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: December 20, 2019Date of Patent: November 24, 2020Assignee: Rigel Pharmaceuticals, Inc.Inventors: Matthew Duncton, Rajinder Singh
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Patent number: 10844041Abstract: The invention discloses compounds of Formula (I), wherein A1, R1, R2, R3, R4, and n are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.Type: GrantFiled: May 19, 2020Date of Patent: November 24, 2020Assignees: AbbVie Overseas S.à.r.l., Galapagos NVInventors: Robert J. Altenbach, Andrew Bogdan, Sylvain Couty, Nicolas Desroy, Gregory A. Gfesser, Christopher Gaëtan Housseman, Philip R. Kym, Bo Liu, Thi Thu Trang Mai, Karine Fabienne Malagu, Nuria Merayo Merayo, Olivier Laurent Picolet, Mathieu Rafaël Pizzonero, Xenia B. Searle, Steven Emiel Van der Plas, Xueqing Wang, Ming C. Yeung
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Patent number: 10844042Abstract: The invention discloses compounds of Formula (I), wherein A1, R1, R2, R3, R4, and n are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.Type: GrantFiled: May 19, 2020Date of Patent: November 24, 2020Assignees: AbbVie Overseas S.à.r.l., Galapagos NVInventors: Robert J. Altenbach, Andrew Bogdan, Sylvain Couty, Nicolas Desroy, Gregory A. Gfesser, Christopher Gaëtan Housseman, Philip R. Kym, Bo Liu, Thi Thu Trang Mai, Karine Fabienne Malagu, Nuria Merayo Merayo, Olivier Laurent Picolet, Mathieu Rafaël Pizzonero, Xenia B. Searle, Steven Emiel Van der Plas, Xueqing Wang, Ming C. Yeung
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Patent number: 10844043Abstract: A heteroaromatic compound which can be used as the fluorescent guest material in the light emitting layer of the organic electroluminescence device is disclosed. The organic electroluminescence device employing the heteroaromatic compound of the present invention can operate under reduced driving voltage, increase current efficiency, and prolong half-life time.Type: GrantFiled: April 24, 2018Date of Patent: November 24, 2020Inventors: Feng-Wen Yen, Li-Chieh Chuang
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Patent number: 10844044Abstract: Described are imino-azacycle-benzamide compounds that inhibit WDR5 and associated protein-protein interactions, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.Type: GrantFiled: June 14, 2019Date of Patent: November 24, 2020Assignee: Vanderbilt UniversityInventors: Joseph R. Alvarado, Shaun R. Stauffer, Rocco D. Gogliotti, Changho Han, Kenneth M. Meyers, Jianhua Tian, Jonathan D. Macdonald, Stephen W. Fesik, Taekyu Lee
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Patent number: 10844045Abstract: Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.Type: GrantFiled: June 16, 2017Date of Patent: November 24, 2020Assignee: BETA PHARMA, INC.Inventors: Michael N. Greco, Michael J. Costanzo, Michael A. Green, Jirong Peng, Victoria Lynn Wilde, Don Zhang
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Patent number: 10844046Abstract: The invention relates to a new class of substituted indole derivatives that are able to activate 5-HT7 serotonin receptor. These compounds bind 5-HT7 serotonin receptor with high affinity and selectivity, while possessing favourable physicochemical properties. The compounds of the invention are the first described low-basicity 5-HT7 receptor agonists. The invention also relates to use of such compounds in the treatment or prevention of 5-HT7 receptor-related disorders, especially of the central nervous system. The invention also relates to the isotopically labelled compounds for use in the in vivo diagnostics or imaging of a 5-HT7 serotonin receptor.Type: GrantFiled: July 21, 2017Date of Patent: November 24, 2020Assignee: INSTYTUT FARMAKOLOGII POLSKIEJ AKADEMII NAUKInventors: Adam Hogendorf, Agata Hogendorf, Grzegorz Satala, Rafal Kurczab, Ryszard Bugno, Jakub Staron, Tomasz Lenda, Andrzej J Bojarski
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Patent number: 10844047Abstract: The invention relates to a process for preparation of the compound 3-methyl-5-benzyloxy-2-(4-benzyloxyphenyl)-1H-indole 5, an intermediate for the synthesis of bazedoxifene and bazedoxifene acetate.Type: GrantFiled: June 19, 2019Date of Patent: November 24, 2020Assignee: ERREGIERRE S.p.A.Inventors: Massimo Ferrari, Daniele De Zani, Stefano Vezzosi, Paolo Belotti
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Patent number: 10844048Abstract: The present invention generally relates to crystalline forms of Lumacaftor, processes for its preparation and pharmaceutical compositions thereof. The present invention also relates to an improved process for preparation of Lumacaftor.Type: GrantFiled: January 6, 2018Date of Patent: November 24, 2020Assignee: Laurus Labs LimitedInventors: Ravindra Babu Bollu, Prasanta Kumar Dalasingh, Sushmita Dwarampudi, Chandrahasa Reddy Annem, Uma Maheswer Rao Vasireddi
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Patent number: 10844049Abstract: The invention described herein provides compounds of Formula (I) and pharmaceutical compositions thereof, for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and cardiovascular disease.Type: GrantFiled: May 15, 2020Date of Patent: November 24, 2020Assignee: QILU REGOR THERAPEUTICS INC.Inventor: Wenge Zhong
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Patent number: 10844050Abstract: The invention provides efficient cyclization processes of hydroxyalkenoic acids and products produced therefrom. The following reactions are claimed: Formula (I), (II), (V) and (VI).Type: GrantFiled: February 14, 2018Date of Patent: November 24, 2020Assignee: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.Inventor: Dmitry Tsvelikhovsky
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Patent number: 10844051Abstract: There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders.Type: GrantFiled: July 22, 2016Date of Patent: November 24, 2020Inventors: Jian Hui Wu, Xiaohong Tian, Qianhui Yi
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Patent number: 10844052Abstract: The present invention provides benzamidazole compounds and methods of using the compounds as galectin-1 inhibitors.Type: GrantFiled: April 4, 2017Date of Patent: November 24, 2020Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Kit S. Lam, Ruiwu Liu, Tsung-Chieh Shih
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Patent number: 10844053Abstract: This application features pyrazol-3-one compounds that activate pro-apoptotic BAX. Also featured are methods of using such compounds, e.g., for the treatment or prevention of diseases, disorders, and conditions associated with deregulated apoptosis of cells (e.g., insufficient apoptosis of diseased or damaged cells or essentially the absence of apoptosis of diseased or damaged cells).Type: GrantFiled: May 23, 2019Date of Patent: November 24, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Loren D. Walensky, Evripidis Gavathiotis
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Patent number: 10844054Abstract: The invention relates to compounds of formula (I), compositions containing the same, and methods for treating and/or diminishing pain in a subject. The compounds of formula (I) are effective for treating opioid-induced tachyphylaxis and opioid-induced hyperalgesia.Type: GrantFiled: December 27, 2019Date of Patent: November 24, 2020Assignee: CerSci Therapeutics, Inc.Inventors: Scott L. Dax, Pasquale N. Confalone
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Patent number: 10844055Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; Wherein R1, R3-R6, X2 and X3 are as defined herein, a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: March 1, 2019Date of Patent: November 24, 2020Assignee: NOVARTIS AGInventors: Guillaume Barbe, Gregory Raymond Bebernitz, Sicong Geng, Hatice Belgin Gulgeze Efthymiou, Lv Liao, Fupeng Ma, Ruowei Mo, David Thomas Parker, Yunshan Peng, Stefan Peukert, Ken Yamada, Kayo Yasoshima, Nichola Smith
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Patent number: 10844056Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.Type: GrantFiled: August 28, 2019Date of Patent: November 24, 2020Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Patent number: 10844057Abstract: The invention is directed to a process for preparing compounds which are useful as intermediates for the preparation of medicinal agents having inhibitory activity for JAK.Type: GrantFiled: September 3, 2019Date of Patent: November 24, 2020Assignee: Theravance Biopharma R&D IP, LLCInventors: Pierre-Jean Colson, Gene Timothy Fass
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Patent number: 10844058Abstract: Provided herein are salts of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,l-a]isoquinolin-2-yl ester in amorphous and crystalline forms, and processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating one or more symptoms of neurological disorders and diseases including hyperkinetic movement disorders or diseases.Type: GrantFiled: June 12, 2020Date of Patent: November 24, 2020Assignee: Neurocrine Biosciences, Inc.Inventors: Kevin McGee, Scott E. Zook, Andrew Carr, Thierry Bonnaud, Bin-Feng Li
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Patent number: 10844059Abstract: A heterocyclic compound may be represented by Formula 1. The heterocyclic compound may be included in an organic electroluminescence device. The organic electroluminescence device including the heterocyclic compound according to an embodiment of the present disclosure may attain high emission efficiency and a low driving voltage effect. where X is O, S, NR10, CR11R12 or SiR13R14.Type: GrantFiled: November 6, 2017Date of Patent: November 24, 2020Assignee: Samsung Display Co., Ltd.Inventor: Hiroaki Itoi
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Patent number: 10844061Abstract: The invention relates to pharmaceutical compositions comprising compounds of Formula Q: wherein W is N(H)—, or —N(CH3)—, and Y is —C(?O)— or —O—, in free base or pharmaceutically acceptable salt form, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.Type: GrantFiled: October 2, 2019Date of Patent: November 24, 2020Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
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Patent number: 10844062Abstract: The present invention provides a novel pyridine derivative, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The pyridine derivative according to the present invention inhibits Raf kinase (B-Raf, Raf-1, or B-RafV600E) and a vascular endothelial growth factor receptor (VEGFR2) involved in angiogenesis, and thus, can be favorably used for the prevention or treatment of melanoma, colorectal cancer, prostate cancer, thyroid cancer, lung cancer, pancreatic cancer, ovarian cancer, or the like, which is induced by RAS mutation.Type: GrantFiled: January 11, 2017Date of Patent: November 24, 2020Assignees: Incheon University Industry Academic Cooperation Foundation, Samjin Pharmaceutical Co., Ltd., Bamichem Co., Ltd.Inventors: Eui Hwan Cho, Hee Jong Shin, Min Hyo Ki, Ho Seok Kwon, Jae Woong Lee, Jeong Ho Joo, Keun Kuk Lee, Jong Min Kim, Yong Bin Park, Sung Hyun Kang, Hyoung Min Cho, Hyun Tae Kim, Soon Kil Ahn, Sung Pyo Hong, Sung Hye Kim
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Patent number: 10844063Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.Type: GrantFiled: December 16, 2019Date of Patent: November 24, 2020Assignee: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Soo Yei Ho, Stephanie Eliane Blanchard, Athisayamani Jeyaraj Duraiswamy, Jenefer Alam, Vikrant Arun Adsool
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Patent number: 10844064Abstract: The present patent application discloses at least the compounds according to Formula I? shown below, or pharmaceutically acceptable salts thereof, wherein ring D, ring A, ring E, JB, n, JD, J, X, Z, Z1, RC1, RC2, Y, R9, o and W are as defined herein.Type: GrantFiled: September 16, 2015Date of Patent: November 24, 2020Assignee: Cyclerion Therapeutics, Inc.Inventors: Glen Robert Rennie, Nicholas Perl, Ara Mermerian, Joon Jung, Lei Jia, Rajesh R. Iyengar, G-Yoon Jamie Im, Timothy Claude Barden, James Edward Sheppeck, Paul Allan Renhowe, Takashi Nakai, Thomas Wai-Ho Lee, Karthik Iyer
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Patent number: 10844065Abstract: Provided are a heterocyclic compound represented by Formula 1 and an organic electroluminescence device and an organic electroluminescence display device including the heterocyclic compound represented by Formula 1 in an emission layer. In Formula 1, A is represented by Formula 2, D1 is represented by Formula 3, and D2 is represented by Formula 4.Type: GrantFiled: April 25, 2018Date of Patent: November 24, 2020Assignee: Samsung Display Co., Ltd.Inventors: Jimyoung Ye, Myeongsuk Kim, Seulong Kim, Byeongwook Yoo, Jaehoon Hwang, Soo-byung Ko, Jihwan Yoon
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Patent number: 10844066Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: GrantFiled: March 1, 2017Date of Patent: November 24, 2020Assignee: Bayer Pharma AktiengesellschaftInventors: Thomas Schwarz, Ningshu Liu, Oliver Politz, Michael Gerisch, Dieter Lang
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Patent number: 10844067Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, X1, X2, X3, X4, integer a and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which RET kinase activity is implicated.Type: GrantFiled: April 18, 2017Date of Patent: November 24, 2020Assignee: Cancer Research Technology LimitedInventors: Allan Michael Jordan, Rebecca Newton, Bohdan Waszkowycz, Jonathan Mark Sutton, George Hynd, Silvia Paoletta, Euan Alexander Fraser Fordyce
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Patent number: 10844068Abstract: The invention provides compounds of Formula (I), immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat diseases or disorders associated with Toll-Like Receptor 7 activity.Type: GrantFiled: July 24, 2019Date of Patent: November 24, 2020Assignee: Novartis AGInventors: Alex Cortez, Timothy Hoffman, Yongkai Li, Tom Yao-Hsiang Wu, Xiaoyue Zhang
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Patent number: 10844069Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.Type: GrantFiled: September 4, 2019Date of Patent: November 24, 2020Assignee: Incyte CorporationInventors: Yun-Long Li, Xiaozhao Wang, Chunhong He
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Patent number: 10844070Abstract: The present invention provides compounds and compositions which are positive allosteric modulators of GABA-A receptors that selectively target the peripheral nervous system and organs of the body, and which do not pass through the blood-brain barrier. The compounds and compositions of the present invention are useful for treatment of diseases or disorders which are mediated by GABA-A neuronal activity, such as, for example, visceral pain, gut motility, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel diseases, drug induced pain, bile salt malabsorption, lactase or other carbohydrate intolerance.Type: GrantFiled: February 13, 2020Date of Patent: November 24, 2020Assignees: The Johns Hopkins University, Lieber Institute, Inc.Inventors: Pankaj Pasricha, Yifang Huang, James Barrow
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Patent number: 10844071Abstract: In certain embodiments compounds corresponding in structure to the formula: are provided that are effective to lower p-tau and/or to prevent or reduce elevation of p-tau, particularly in response to stress (e.g., elevated cortisol levels). The compounds are useful in the treatment or prophylaxis of pathologies characterized by abnormal amyloid plaque and or tangle formation and/or deposition.Type: GrantFiled: February 21, 2020Date of Patent: November 24, 2020Assignee: BUCK INSTITUTE FOR RESEARCH ON AGINGInventors: Varghese John, Dale E. Bredesen
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Patent number: 10844072Abstract: Processes for preparing oxycodone are provided. Said processes encompass a step which is a hydrogenation of an 14-hydroxycodeinone salt in the presence of trifluoroacetic acid and/or a glycol.Type: GrantFiled: July 31, 2019Date of Patent: November 24, 2020Assignee: RHODES TECHNOLOGIESInventors: Joshua Robert Giguere, Keith Edward McCarthy, Marcel Schleusner
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Patent number: 10844073Abstract: Provided herein are palladium-mediated coupling reactions useful in the preparation of ketone-containing organic molecules. The provided methods can be used for the preparation of natural products and pharmaceutical agents, including Eribulin, halichondrins, and analogs thereof. The present invention also provides novel halichondrin analogs which can be prepared via the palladium-mediated coupling reactions. The novel halichondrin analogs can be used in the prevention and/or treatment of diseases or conditions (e.g., proliferative diseases such as cancer).Type: GrantFiled: July 1, 2019Date of Patent: November 24, 2020Assignee: President and Fellows of Harvard CollegeInventors: Jung Hwa Lee, Yoshito Kishi, Ayumi Osawa, Zhanjie Li
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Patent number: 10844074Abstract: Compounds having the general formula (I) and pharmaceutical compositions that can be used as Bruton's Tyrosine Kinase (BTK), ITK, JAK3, and selective mutant epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor and their uses in the treatment of related diseases and disorders such as cancer.Type: GrantFiled: December 2, 2016Date of Patent: November 24, 2020Assignee: ZHEJIANG JIANFENG-YIEN BIOTECHNOLOGY CO., LTD.Inventors: Haixiao Zhai, Fan Wu, Zhanggui Wu
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Patent number: 10844075Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.Type: GrantFiled: July 2, 2019Date of Patent: November 24, 2020Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 10844076Abstract: The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.Type: GrantFiled: November 6, 2018Date of Patent: November 24, 2020Assignee: Nektar therapeuticsInventors: Pankaj Sharma, Vijay Kumar Khatri, Xuyuan Gu, Yuan Song, Michael Lixin Shen, Jennifer Riggs-Sauthier, Neel K. Anand, Antoni Kozlowski, Aleksandrs Odinecs, Timothy A. Riley, Zhongxu Ren, YongQi Mu, Xiaoming Shen, Xuejun Yuan, Natalia Aurrecoechea, Donogh John Roger O'Mahony, Bo-Liang Deng