Patents Issued in November 24, 2020
  • Patent number: 10844026
    Abstract: 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: Grant
    Filed: January 21, 2020
    Date of Patent: November 24, 2020
    Assignees: Biohaven Pharmaceutical Holding Company Ltd., Rutgers, The State University of New Jersey
    Inventors: 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
  • Patent number: 10844027
    Abstract: 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: Grant
    Filed: September 16, 2016
    Date of Patent: November 24, 2020
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Andrew Kruegel, Dalibor Sames, Madalee G. Wulf, Jonathan A. Javitch
  • Patent number: 10844028
    Abstract: 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: Grant
    Filed: December 3, 2018
    Date of Patent: November 24, 2020
    Assignee: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher G. Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel Griffith Anderson
  • Patent number: 10844029
    Abstract: 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: Grant
    Filed: June 15, 2017
    Date of Patent: November 24, 2020
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
  • Patent number: 10844030
    Abstract: 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: Grant
    Filed: September 24, 2018
    Date of Patent: November 24, 2020
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Yusuke Izawa, Yosuke Suzuki, Masaru Utsunomiya
  • Patent number: 10844031
    Abstract: 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: Grant
    Filed: November 15, 2019
    Date of Patent: November 24, 2020
    Assignee: IOWA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
    Inventors: Aaron David Sadow, Zachary Benjamin Weinstein, George A. Kraus
  • Patent number: 10844032
    Abstract: 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: Grant
    Filed: July 2, 2018
    Date of Patent: November 24, 2020
    Assignee: Vanderbilt University
    Inventors: Taekyu Lee, Nicholas F. Pelz, Johannes Belmar, Zhiguo Bian, Edward T. Olejniczak, Stephen W. Fesik, Brian A. Chauder
  • Patent number: 10844033
    Abstract: 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: Grant
    Filed: May 16, 2017
    Date of Patent: November 24, 2020
    Assignees: Qatar Found. For Ed., Science and Community Development, Sultan Qaboos University, Leibniz-Institut Fur Katalyse e.V. an der Unversitat Rostock
    Inventors: Sarim Dastgir, Badria Al-Shihi, Mohammad Sharif, Matthias Beller, Ralf Jackstell
  • Patent number: 10844034
    Abstract: 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: Grant
    Filed: April 21, 2017
    Date of Patent: November 24, 2020
    Assignee: DAICEL CORPORATION
    Inventor: Yuichi Sakanishi
  • Patent number: 10844035
    Abstract: 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: Grant
    Filed: July 13, 2018
    Date of Patent: November 24, 2020
    Assignee: PURISYS LLC
    Inventors: Lukas Dialer, Denis Petrovic, Ulrich Weigl
  • Patent number: 10844036
    Abstract: 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: Grant
    Filed: December 5, 2017
    Date of Patent: November 24, 2020
    Assignee: Agan Aroma & fine chemicals Ltd.
    Inventors: Youlia Hagooly, Alexander Laskavy, Tehila Yosef Gerufi, Eyal Ben-Ari
  • Patent number: 10844037
    Abstract: 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: Grant
    Filed: February 24, 2016
    Date of Patent: November 24, 2020
    Assignee: Rohm and Haas Electronic Materials LLC
    Inventor: Paul J. Labeaume
  • Patent number: 10844038
    Abstract: 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: Grant
    Filed: September 8, 2017
    Date of Patent: November 24, 2020
    Assignee: SABILA BIOSCIENCES LLC
    Inventors: Tarek S. Mansour, Colleen E. Evans
  • Patent number: 10844039
    Abstract: 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: Grant
    Filed: November 12, 2019
    Date of Patent: November 24, 2020
    Assignee: BioTheryX, Inc.
    Inventors: Kyle W. H. Chan, Aparajita Hoskote Chourasia, Paul E. Erdman, Leah Fung, Imelda Lam, Frank Mercurio, Robert Sullivan, Eduardo Torres
  • Patent number: 10844040
    Abstract: 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: Grant
    Filed: December 20, 2019
    Date of Patent: November 24, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Matthew Duncton, Rajinder Singh
  • Patent number: 10844041
    Abstract: 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: Grant
    Filed: May 19, 2020
    Date of Patent: November 24, 2020
    Assignees: AbbVie Overseas S.à.r.l., Galapagos NV
    Inventors: 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
  • Patent number: 10844042
    Abstract: 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: Grant
    Filed: May 19, 2020
    Date of Patent: November 24, 2020
    Assignees: AbbVie Overseas S.à.r.l., Galapagos NV
    Inventors: 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
  • Patent number: 10844043
    Abstract: 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: Grant
    Filed: April 24, 2018
    Date of Patent: November 24, 2020
    Inventors: Feng-Wen Yen, Li-Chieh Chuang
  • Patent number: 10844044
    Abstract: 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: Grant
    Filed: June 14, 2019
    Date of Patent: November 24, 2020
    Assignee: Vanderbilt University
    Inventors: Joseph R. Alvarado, Shaun R. Stauffer, Rocco D. Gogliotti, Changho Han, Kenneth M. Meyers, Jianhua Tian, Jonathan D. Macdonald, Stephen W. Fesik, Taekyu Lee
  • Patent number: 10844045
    Abstract: 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: Grant
    Filed: June 16, 2017
    Date of Patent: November 24, 2020
    Assignee: BETA PHARMA, INC.
    Inventors: Michael N. Greco, Michael J. Costanzo, Michael A. Green, Jirong Peng, Victoria Lynn Wilde, Don Zhang
  • Patent number: 10844046
    Abstract: 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: Grant
    Filed: July 21, 2017
    Date of Patent: November 24, 2020
    Assignee: INSTYTUT FARMAKOLOGII POLSKIEJ AKADEMII NAUK
    Inventors: Adam Hogendorf, Agata Hogendorf, Grzegorz Satala, Rafal Kurczab, Ryszard Bugno, Jakub Staron, Tomasz Lenda, Andrzej J Bojarski
  • Patent number: 10844047
    Abstract: 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: Grant
    Filed: June 19, 2019
    Date of Patent: November 24, 2020
    Assignee: ERREGIERRE S.p.A.
    Inventors: Massimo Ferrari, Daniele De Zani, Stefano Vezzosi, Paolo Belotti
  • Patent number: 10844048
    Abstract: 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: Grant
    Filed: January 6, 2018
    Date of Patent: November 24, 2020
    Assignee: Laurus Labs Limited
    Inventors: Ravindra Babu Bollu, Prasanta Kumar Dalasingh, Sushmita Dwarampudi, Chandrahasa Reddy Annem, Uma Maheswer Rao Vasireddi
  • Patent number: 10844049
    Abstract: 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: Grant
    Filed: May 15, 2020
    Date of Patent: November 24, 2020
    Assignee: QILU REGOR THERAPEUTICS INC.
    Inventor: Wenge Zhong
  • Patent number: 10844050
    Abstract: 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: Grant
    Filed: February 14, 2018
    Date of Patent: November 24, 2020
    Assignee: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD.
    Inventor: Dmitry Tsvelikhovsky
  • Patent number: 10844051
    Abstract: There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: November 24, 2020
    Inventors: Jian Hui Wu, Xiaohong Tian, Qianhui Yi
  • Patent number: 10844052
    Abstract: The present invention provides benzamidazole compounds and methods of using the compounds as galectin-1 inhibitors.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: November 24, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Kit S. Lam, Ruiwu Liu, Tsung-Chieh Shih
  • Patent number: 10844053
    Abstract: 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: Grant
    Filed: May 23, 2019
    Date of Patent: November 24, 2020
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Loren D. Walensky, Evripidis Gavathiotis
  • Patent number: 10844054
    Abstract: 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: Grant
    Filed: December 27, 2019
    Date of Patent: November 24, 2020
    Assignee: CerSci Therapeutics, Inc.
    Inventors: Scott L. Dax, Pasquale N. Confalone
  • Patent number: 10844055
    Abstract: 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: Grant
    Filed: March 1, 2019
    Date of Patent: November 24, 2020
    Assignee: NOVARTIS AG
    Inventors: 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
  • Patent number: 10844056
    Abstract: 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: Grant
    Filed: August 28, 2019
    Date of Patent: November 24, 2020
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 10844057
    Abstract: 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: Grant
    Filed: September 3, 2019
    Date of Patent: November 24, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Pierre-Jean Colson, Gene Timothy Fass
  • Patent number: 10844058
    Abstract: 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: Grant
    Filed: June 12, 2020
    Date of Patent: November 24, 2020
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Kevin McGee, Scott E. Zook, Andrew Carr, Thierry Bonnaud, Bin-Feng Li
  • Patent number: 10844059
    Abstract: 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: Grant
    Filed: November 6, 2017
    Date of Patent: November 24, 2020
    Assignee: Samsung Display Co., Ltd.
    Inventor: Hiroaki Itoi
  • Patent number: 10844061
    Abstract: 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: Grant
    Filed: October 2, 2019
    Date of Patent: November 24, 2020
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
  • Patent number: 10844062
    Abstract: 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: Grant
    Filed: January 11, 2017
    Date of Patent: November 24, 2020
    Assignees: 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
  • Patent number: 10844063
    Abstract: 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: Grant
    Filed: December 16, 2019
    Date of Patent: November 24, 2020
    Assignee: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
    Inventors: Soo Yei Ho, Stephanie Eliane Blanchard, Athisayamani Jeyaraj Duraiswamy, Jenefer Alam, Vikrant Arun Adsool
  • Patent number: 10844064
    Abstract: 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: Grant
    Filed: September 16, 2015
    Date of Patent: November 24, 2020
    Assignee: 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
  • Patent number: 10844065
    Abstract: 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: Grant
    Filed: April 25, 2018
    Date of Patent: November 24, 2020
    Assignee: Samsung Display Co., Ltd.
    Inventors: Jimyoung Ye, Myeongsuk Kim, Seulong Kim, Byeongwook Yoo, Jaehoon Hwang, Soo-byung Ko, Jihwan Yoon
  • Patent number: 10844066
    Abstract: 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: Grant
    Filed: March 1, 2017
    Date of Patent: November 24, 2020
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Thomas Schwarz, Ningshu Liu, Oliver Politz, Michael Gerisch, Dieter Lang
  • Patent number: 10844067
    Abstract: 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: Grant
    Filed: April 18, 2017
    Date of Patent: November 24, 2020
    Assignee: Cancer Research Technology Limited
    Inventors: Allan Michael Jordan, Rebecca Newton, Bohdan Waszkowycz, Jonathan Mark Sutton, George Hynd, Silvia Paoletta, Euan Alexander Fraser Fordyce
  • Patent number: 10844068
    Abstract: 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: Grant
    Filed: July 24, 2019
    Date of Patent: November 24, 2020
    Assignee: Novartis AG
    Inventors: Alex Cortez, Timothy Hoffman, Yongkai Li, Tom Yao-Hsiang Wu, Xiaoyue Zhang
  • Patent number: 10844069
    Abstract: 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: Grant
    Filed: September 4, 2019
    Date of Patent: November 24, 2020
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Xiaozhao Wang, Chunhong He
  • Patent number: 10844070
    Abstract: 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: Grant
    Filed: February 13, 2020
    Date of Patent: November 24, 2020
    Assignees: The Johns Hopkins University, Lieber Institute, Inc.
    Inventors: Pankaj Pasricha, Yifang Huang, James Barrow
  • Patent number: 10844071
    Abstract: 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: Grant
    Filed: February 21, 2020
    Date of Patent: November 24, 2020
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Patent number: 10844072
    Abstract: 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: Grant
    Filed: July 31, 2019
    Date of Patent: November 24, 2020
    Assignee: RHODES TECHNOLOGIES
    Inventors: Joshua Robert Giguere, Keith Edward McCarthy, Marcel Schleusner
  • Patent number: 10844073
    Abstract: 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: Grant
    Filed: July 1, 2019
    Date of Patent: November 24, 2020
    Assignee: President and Fellows of Harvard College
    Inventors: Jung Hwa Lee, Yoshito Kishi, Ayumi Osawa, Zhanjie Li
  • Patent number: 10844074
    Abstract: 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: Grant
    Filed: December 2, 2016
    Date of Patent: November 24, 2020
    Assignee: ZHEJIANG JIANFENG-YIEN BIOTECHNOLOGY CO., LTD.
    Inventors: Haixiao Zhai, Fan Wu, Zhanggui Wu
  • Patent number: 10844075
    Abstract: 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: Grant
    Filed: July 2, 2019
    Date of Patent: November 24, 2020
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 10844076
    Abstract: 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: Grant
    Filed: November 6, 2018
    Date of Patent: November 24, 2020
    Assignee: Nektar therapeutics
    Inventors: 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