Patents Issued in July 14, 2020
  • Patent number: 10710976
    Abstract: The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: July 14, 2020
    Assignees: Cerecor Inc., Merck Sharp & Dohme Corp.
    Inventors: Reza Mazhari, Djelila Mezaache, Blake M. Paterson, James Vornov, Rachel M. Garner, Todd Nelson
  • Patent number: 10710977
    Abstract: Provided is a novel process for selectively producing the E-geometrical isomer or Z-geometrical isomer of an oximino compound useful as a medicine or agrochemical. In the process, a mixture of geometrical isomers of an oximino compound represented by formula (EZ)-1 is mixed with an acidic compound to produce the E-isomer of the oximo compound represented by the formula (E)-1 or the Z-isomer of the oximino compound represented by the formula (Z)-1 in high yields with high stereoselectivity.
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: July 14, 2020
    Assignee: Nissan Chemical Corporation
    Inventors: Daisuke Tanima, Yoshiyuki Kusuoka, Keisuke Tsuji
  • Patent number: 10710978
    Abstract: The application relates to compounds of Formula (I?): which modulate the activity of a kinase (e.g., STK4), a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease or disorder associated with the modulation of a kinase, such as STK4.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: July 14, 2020
    Assignees: DANA-FARBER CANCER INSTITUTE, INC., FONDAZIONE CENTRO SAN RAFFAELE
    Inventors: Nathanael S. Gray, Sara Buhrlage, Kenneth Anderson, Francesca Cottini, Giovanni Tonon
  • Patent number: 10710979
    Abstract: The present invention provides an EGFR kinase inhibitor and a preparation method and use thereof. Specifically, the present invention provides a compound as shown in formula (I), the definition of each group therein being as described in the description. Said compound is an efficient EGFR inhibitor.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: July 14, 2020
    Assignee: ZHEJIANG BOSSAN PHARMACEUTICAL CO. LTD.
    Inventors: Dawei Ma, Qiang Yu, Junying Yuan, Hongguang Xia, Dongpo Cai, Kailiang Wang, Chen Zhang, Shanghua Xia
  • Patent number: 10710980
    Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I) to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.
    Type: Grant
    Filed: July 18, 2017
    Date of Patent: July 14, 2020
    Assignee: Novartis AG
    Inventors: Luca Arista, Sreehari Babu, Jianwei Bian, Kai Cui, Michael Patrick Dillon, Rene Lattmann, Jialiang Li, Lv Liao, Dimitrios Lizos, Rita Ramos, Nikolaus Johannes Stiefl, Thomas Ullrich, Peggy Usselmann, Xiaoyang Wang, Liladhar Murlidhar Waykole, Sven Weiler, Yubo Zhang, Yizong Zhou, Tingying Zhu
  • Patent number: 10710981
    Abstract: The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: July 14, 2020
    Assignee: BEIJING INNOCARE PHARMA TECH CO., LTD.
    Inventors: Xiangyang Chen, Yingxiang Gao, Norman Xianglong Kong
  • Patent number: 10710982
    Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
    Type: Grant
    Filed: February 12, 2020
    Date of Patent: July 14, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, Jiansheng Wan
  • Patent number: 10710983
    Abstract: Compounds within the scope of the present invention have a Formula 1 or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R2 and R3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC50 of from 0.003 ?M to 3.7 ?M; a TAK1 IC50 of from 0.008 ?M to 132 ?M; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
    Type: Grant
    Filed: June 26, 2017
    Date of Patent: July 14, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
  • Patent number: 10710984
    Abstract: The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyridinylamino)propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: July 14, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec, Stefan Scheuerer
  • Patent number: 10710985
    Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein the substituents are defined in claim 1. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: July 14, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll, Remy Halm
  • Patent number: 10710986
    Abstract: Compounds of Formula (I), methods of using said compounds singly or in combination with additional agents and compositions of said compounds for the treatment of cancer are disclosed.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: July 14, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Aesop Cho, Zhimin Du, Michael Graupe, Lateshkumar Thakorlal Lad, Paulo A. Machicao Tello, Jonathan William Medley, Samuel E. Metobo, Prasenjit Kumar Mukherjee, Devan Naduthambi, Eric Q. Parkhill, Barton W. Phillips, Scott Preston Simonovich, Neil H. Squires, Peiyuan Wang, William J. Watkins, Jie Xu, Kin Shing Yang, Christopher Allen Ziebenhaus
  • Patent number: 10710987
    Abstract: Provided herein are novel solid forms of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4?-(morpholinomethyl)-[1,1?-biphenyl]-3-carboxamide hydrochloride, and related compositions and methods.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: July 14, 2020
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin Wayne Kuntz, Hyeong Wook Choi, Steven Mathieu, Kristen Sanders, Arani Chanda
  • Patent number: 10710988
    Abstract: [Problem] To provide a compound useful as an MC4 receptor agonist. [Means for Solution] The present inventors studied MC4 receptor agonists, and have found that a piperazine derivative has an MC4 receptor agonistic action, thereby completing the present invention. The piperazine derivative of the present invention has an MC4 receptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.
    Type: Grant
    Filed: July 18, 2017
    Date of Patent: July 14, 2020
    Assignee: Astellas Pharma Inc.
    Inventors: Takashi Sugane, Norio Asai, Hiroyuki Moritomo, Daisuke Yamashita, Naomi Hosogai
  • Patent number: 10710989
    Abstract: The present invention provides a method of producing a heterocyclic compound useful as an agent for the prophylaxis and/or treatment of Alzheimer's disease and the like. The present invention relates to a method of producing 1,5-anhydro-2,4-dideoxy-2-(4-fluoro-5-methyl-1-oxo-6-(4-(1H-pyrazol-1-yl)benzyl)-1,3-dihydro-2H-isoindol-2-yl)-L-threo-pentitol or a salt thereof, which comprises reacting 4-fluoro-3-hydroxy-5-methyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2-benzofuran-1(3H)-one or a salt thereof, 3-fluoro-2-formyl-4-methyl-5-[4-(1H-pyrazol-1-yl)benzyl]benzoic acid or a salt thereof, or a mixture thereof, with 2-amino-1,5-anhydro-2,4-dideoxy-L-threo-pentitol.
    Type: Grant
    Filed: February 27, 2018
    Date of Patent: July 14, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Makoto Kanematsu, Kazuhisa Ishimoto, Tomoaki Katou
  • Patent number: 10710990
    Abstract: The present invention is to provide a method of producing a glyceric acid ester which is easy for production and high in yield, and in which a pyridine to be used for the reaction is easily reused. Provided is a method of producing a compound represented by the following formula (II), including a step of oxidatively esterifying Compound A represented by the following formula (I) with Compound B selected from an organic nitroxyl radical, an N-hydroxy form thereof, and a salt containing an oxo ammonium cation of them, and an oxidizing agent in the presence of a pyridine having an alkyl substituent, wherein the use amount of Compound B is 0.0001 or more and 0.1 or less in terms of a molar ratio relative to Compound A: wherein, in the formulae (I) and (II), R1 and R2 each independently represent a hydrogen atom or a monovalent hydrocarbon group, or R1 and R2 are bonded to each other to form a divalent hydrocarbon group for constituting a ring structure.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: July 14, 2020
    Assignee: KAO CORPORATION
    Inventor: Takashi Aoki
  • Patent number: 10710991
    Abstract: The present invention relates to processes for the preparation of thietane derivatives of the formula IA and thietane derivatives of the formula IB wherein R1, R2, A1, A2, A3, A4, B, and n are as defined in the claims. The invention also relates to intermediates useful in the processes, as well as the compounds of formula IA and IB and their use as pesticides.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: July 14, 2020
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Patent number: 10710992
    Abstract: The present disclosure relates to substituted pyridinones, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: July 14, 2020
    Assignee: Zenith Epigenetics Ltd.
    Inventors: May Xiaowu Jiang, Bruce Francis Molino, Shuang Liu, Ruifang Wang, Bryan Cordell Duffy, John Frederick Quinn, Gregory Steven Wagner
  • Patent number: 10710993
    Abstract: The present invention discloses a compound for regulating protein kinase activity and used for treating or preventing diseases associated with protein kinases. Specifically, the present invention relates to a benzofuran pyrazole amine protein kinase inhibitor which belongs to compounds that regulate anaplastic lymphoma kinase (ALK), and provides a method of preparing such a compound and a pharmaceutical use of such a compound in the treatment or prevention of diseases associated with ALK. The inhibitor can solve the problem of the drug resistance of the first generation and the second generation of ALK inhibitors.
    Type: Grant
    Filed: June 27, 2017
    Date of Patent: July 14, 2020
    Assignee: HANGZHOU REX PHARMACEUTICAL CO., LTD.
    Inventors: Yonghui Wang, Juan Zhou, Yujun Gao, Dong Wang, Binbin Hong, Ximing Shen, Yaodong Wu, Chunqi Li
  • Patent number: 10710994
    Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof wherein A, X, R1, R4 and n are as defined herein. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: July 14, 2020
    Assignee: Genentech, Inc.
    Inventors: Jack Alexander Terrett, Huifen Chen, Lea Constantineau-Forget, Robin Larouche-Gauthier, Luce Lépissier, Francis Beaumier, Martin Déry, Chantal Grand-Maître, Claudio Sturino, Matthew Volgraf, Elisia Villemure
  • Patent number: 10710995
    Abstract: The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.
    Type: Grant
    Filed: September 26, 2017
    Date of Patent: July 14, 2020
    Assignees: Rhode Island Hospital, Midwestern University
    Inventors: Jack R. Wands, Suzanne De La Monte, Arihiro Aihara, Mark Jon Olsen, John-Michael Thomas
  • Patent number: 10710996
    Abstract: The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: July 14, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Yaqiu Long, Meiyu Geng, Zhongliang Xu, Jing Ai
  • Patent number: 10710997
    Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) of the following formula: synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: July 14, 2020
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Andrew Felts, Aaron M. Bender
  • Patent number: 10710998
    Abstract: The present invention relates to a novel nitrile derivative of a pyrimido[6,1-a]isoquinolin-4-one compound of formula (A). The invention further relates to a process for producing a compound of formula (A). The invention also relates to a process which comprises reducing a compound of formula (A). Compounds of the invention are useful in the production of compounds such as RPL554.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: July 14, 2020
    Assignee: VERONA PHARMA PLC
    Inventor: Peter Lionel Spargo
  • Patent number: 10710999
    Abstract: The present disclosure provides a novel polymorph of an intermediate useful in the preparation of palbociclib. The polymorph has enhanced properties that influence process ability of the intermediate and synthesis of palbociclib.
    Type: Grant
    Filed: October 4, 2017
    Date of Patent: July 14, 2020
    Assignee: MYLAN LABORATORIES LIMITED
    Inventors: Mahdeshkumar Gadakar, Dnyandeo Punde, Rajendra Yadav, Yogesh Wakchaure
  • Patent number: 10711000
    Abstract: Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with autotaxin activity. The methods and compositions disclosed herein include the use of at least one autotaxin inhibitor compound.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: July 14, 2020
    Assignee: FRONTHERA U.S. PHARMACEUTICALS LLC
    Inventors: Bohan Jin, Qing Dong, Gene Hung, Yao Li
  • Patent number: 10711001
    Abstract: The present invention relates to compounds, ligands, and/or complexes that are useful in medical imaging and/or in therapy, especially in cancer treatment. The present invention also relates to a pharmaceutical composition comprising said compounds, ligands, and/or complexes that are useful for medical imaging, targeting, and/or treatment of cancers. The present invention also relates to a process for preparing these compounds, ligands, and/or complexes.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: July 14, 2020
    Assignees: GUERBET, UNIVERSITE DE BRETAGNE OCCIDENTALE, CENTRAL NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Mariane Le Fur, Raphaël Tripier, Olivier Rousseaux, Maryline Beyler
  • Patent number: 10711002
    Abstract: The present disclosure relates to novel compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof; wherein R1, R2, Ra, Rb and Rc are as defined herein, pharmaceutical compositions containing same and methods for the treatment of cancer using same.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: July 14, 2020
    Assignee: THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITY
    Inventors: Moulay A. Alaoui-Jamali, Krikor Bijian, Dominik Wernic
  • Patent number: 10711003
    Abstract: Compounds having a structure according to formula (I) or (II) where R1, R2, and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
    Type: Grant
    Filed: October 22, 2019
    Date of Patent: July 14, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Liqi He, Sanjeev Gangwar, Shoshana L. Posy, Yam B. Poudel, Prasanna Sivaprakasam
  • Patent number: 10711004
    Abstract: The invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.
    Type: Grant
    Filed: September 3, 2019
    Date of Patent: July 14, 2020
    Assignee: Genentech, Inc.
    Inventors: Huifen Chen, Brian Safina, Daniel Shore, Jack Terrett, Elisia Villemure, Matthew Volgraf, Stuart Ward, Aijun Lu, Robin Larouche-Gauthier, Francis Beaumier, Martin Dery, Lea Constantineau-Forget, Chantal Grand-Maitre, Luce Lepissier
  • Patent number: 10711005
    Abstract: Compound I and a compound II as well as preparation methods therefor and use thereof are disclosed. A newly synthesized compound of formula I is capable of stimulating congenital immunity and cellular immunity for tumor resistance while greatly improving the antitumor effect of ethacrynic acid (EA), and thus an integrated synergistic anti-tumor dual-immunity drug design is explored. The immune response mechanism for resisting melanoma of the compound as shown in the formula I is demonstrated. A compound that is as shown in a formula II and is prepared from the compound of formula I and ROR1 by means of covalency markedly slows down the growth of subcutaneously transplanted mammary cancer tumor, such that the immune response mechanism, for treating the mammary cancer, of the compound as shown in the formula II is demonstrated.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: July 14, 2020
    Assignees: SHENZHEN UNIVERSITY, SHENZHEN KANGJUZHENG PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Guangyi Jin, Zhulin Wang
  • Patent number: 10711006
    Abstract: The present invention relates to a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and use thereof in preparation of a drug. The compound of the present invention has a structure of Formula II or Formula II?: or their optical isomers, or pharmaceutically acceptable salts or solvates; where each Rg is independently H, halogen, —CF2H, —CF3, —CN, C1-C3 alkyl, or C1-C3 alkoxy; n is selected from 0, 1 and 2; Rd is selected from Re is selected from H, CH3, C2-C6 alkyl, C1-C6 azaalkyl, and C1-C6 oxaalkyl, wherein CH3, C2-C6 alkyl, C1-C6 azaalkyl and C1-C6 oxaalkyl are further substituted with amino, hydroxyl, and C1-C3 alkyl; Y1, Y2, Y3 and Y4 are independently selected from C(Rf) and N, and at least one of Y1, Y2, Y3 and Y4 is N, wherein Rf is selected from H, halogen, C1-C3 alkyl, —CF3, and —CF2H.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: July 14, 2020
    Assignee: HANGZHOU HERTZ PHARMACEUTICAL CO., LTD.
    Inventors: Xinglu Zhou, Xingguo Liu, Miao Hu
  • Patent number: 10711007
    Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
    Type: Grant
    Filed: April 5, 2019
    Date of Patent: July 14, 2020
    Assignee: Prelude Therapeutics Incorporated
    Inventors: Juan Luengo, Hong Lin, Michael Hawkins, Rupa Shetty, Philip Pitis, Gisela Saborit Villarroya
  • Patent number: 10711008
    Abstract: Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: July 14, 2020
    Assignee: Oncternal Therapeutics, Inc.
    Inventor: Stephen E. Webber
  • Patent number: 10711009
    Abstract: Disclosed is a method of preparing d-glucaro-1,4:6,3-dilactone using an organic acid or a salt thereof, such that d-glucaro-1,4:6,3-dilactone having high purity can be obtained using potassium glucarate as the organic acid, and simultaneously, the economic efficiency of the preparation process can be remarkably improved.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: July 14, 2020
    Assignees: Hyundai Motor Company, Kia Motors Corporation
    Inventor: Chae Hwan Hong
  • Patent number: 10711010
    Abstract: Compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R13, Ra, Rb, A and n are as defined in the description. Medicinal products containing the same which are useful in treating conditions requiring a pro-apoptotic agent.
    Type: Grant
    Filed: January 15, 2019
    Date of Patent: July 14, 2020
    Assignees: LES LABORATORIES SERVIER, VERNALIS (R&d) LTD
    Inventors: Zoltán Szlávik, András Kotschy, Maïa Chanrion, Didier Demarles, Olivier Geneste, James Edward Paul Davidson, James Brooke Murray, Szabolcs Sipos, Attila Paczal, Balázs Bálint
  • Patent number: 10711011
    Abstract: The present disclosure relates to compounds of Formula I, its stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms thereof and pharmaceutical compositions containing them as the active ingredient which can be used as medicaments. The aforementioned substances can also be used in the manufacture of medicaments for treatment, prevention or suppression of diseases, and conditions mediated by microbes. The present disclosure also relates to the synthesis and characterization of aforementioned substances.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: July 14, 2020
    Assignee: BUGWORKS RESEARCH, INC.
    Inventors: Shahul Hameed Peer Mohamed, Nagakumar Bharatham, Nainesh Katagihallimath, Sreevalli Sharma, Radha Nandishaiah
  • Patent number: 10711012
    Abstract: The present invention relates to a pyridinium oxazole dyad scaffold of formula (I) and a process for the preparation thereof. The present invention further discloses a pyridine compound of formula (II) which is used for the preparation of formula (I) and a process for preparation thereof.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: July 14, 2020
    Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Nitin Tukaram Patil, Aslam Chandbhai Shaikh, Prasad Padmakar Kulkarni, Dnyanesh Sadanand Ranade
  • Patent number: 10711013
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 25, 2018
    Date of Patent: July 14, 2020
    Assignee: ORION CORPORATION
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Koivikko, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Patent number: 10711014
    Abstract: Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.
    Type: Grant
    Filed: August 14, 2019
    Date of Patent: July 14, 2020
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Torrey Pines Institute for Molecular Studies
    Inventors: Said M. Sebti, Yangmei Li, Richard A. Houghten
  • Patent number: 10711015
    Abstract: The present specification relates to a compound containing nitrogen, and a color conversion film, a backlight unit, and a display device, including the same.
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: July 14, 2020
    Assignee: LG CHEM, LTD.
    Inventors: Milim Lee, Seonkyoung Son, Cheol Jun Song, Hoyong Lee
  • Patent number: 10711016
    Abstract: The invention is directed to functionalized aluminum reagents of formula 1 where R is a linear or branched alkane group containing 1 to 8 carbon atoms, and R1 is phenylene, or a linear or branched alkane diyl group containing 2 to 10 carbon atoms, or a combination of one or more phenylene groups and one or more linear or branched alkane diyl groups containing 1 to 10 carbon atoms; Q is of formula 2 where R3 and R4 are independently phenyl or a linear or branched alkyl group containing 1 to 10 carbon atoms, or R3 and R4 taken together with the nitrogen atom represent a nitrogen containing heterocyclic group containing from 4 to 12 carbon atoms.
    Type: Grant
    Filed: May 1, 2019
    Date of Patent: July 14, 2020
    Assignee: The Goodyear Tire & Rubber Company
    Inventors: Stefan Mecking, Margaret Flook Vielhaber, Inigo Göttker-Schnetmann, Philip Kenyon
  • Patent number: 10711017
    Abstract: Fluorinated cyclopentene moieties and fluorinated cyclopentene functionalized silica materials are provided. The fluorinated cyclopentene functionalized silica materials include a silica material having the fluorinated cyclopentene moiety covalently bonded thereto. Exemplary silica materials include a polysilsesquioxane, a nanosilica, a microsilica, a silica gel, a silica aerogel, or combinations thereof. The fluorinated cyclopentene moieties are based on a modification of perfluorocyclopentene (i.e., 1,2,3,3,4,4,5,5-octafluoro-1-cyclopentene) by nucleophilic substitution with an appropriate nucleophile having a reactive functional group. Methods for preparing fluorinated cyclopentene moieties and the corresponding fluorinated cyclopentene functionalized silica materials are also provided.
    Type: Grant
    Filed: February 7, 2019
    Date of Patent: July 14, 2020
    Assignee: United States of America as represented by the Secretary of the Air Force
    Inventors: Scott Iacono, Abby Rose Jennings
  • Patent number: 10711018
    Abstract: A process can prepare an isocyanurate compound by hydrosilylation. The compound is a tris[3-(trialkoxysilyl)propyl] isocyanurate, a tris[3-(alkyldialkoxysilyl)propyl] isocyanurate, and/or a tris[3-(dialkylalkoxysilyl)propyl] isocyanurate, The process includes (A) preparing a mixture of at least one carboxylic acid, a platinum catalyst, and 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione; (B) heating the mixture to a temperature in the range of 40 to 140° C.; (C) adding at least one H-silane among a hydrotrialkoxysilane, a hydroalkyldialkoxysilane, and a hydrodialkylalkoxysilane to the mixture; (D) adding at least one alcohol to the mixture prepared in step (C); and (E) isolating the isocyanurate compound.
    Type: Grant
    Filed: April 11, 2019
    Date of Patent: July 14, 2020
    Assignee: Evonik Operations GmbH
    Inventors: Philipp Albert, Eckhard Just
  • Patent number: 10711019
    Abstract: This invention relates to a photoinitiator compound comprising: a polyhedral oligomeric silsesquioxane (POSS) moiety and a photoinitiator moiety, wherein the photoinitiator compound having the structure according to formula (I): [R—SiO1.5]n (I), wherein n is 6, 8, 10 or 12 and R is independently selected from the group consisting of H, linear or branched (hetero)alkyl, linear or branched (hetero)alkenyl, (hetero)aryl, (hetero)alkyl aryl, (hetero)aryl alkyl and a photoinitiator moiety, wherein at least one R is a photoinitiator moiety and the photoinitiator compound is a nanoparticle. The present invention also relates to a method for the production of the photoinitiator compound of the invention, a photopolymerizable composition comprising the photoinitiator compound of the invention, the use of the photoinitiator compound of the invention for photopolymerization. The present invention is further related to a coated substrate comprising the photopolymerizable composition of the invention.
    Type: Grant
    Filed: August 17, 2016
    Date of Patent: July 14, 2020
    Assignee: Agency for Science, Technology and Research
    Inventors: Fuke Wang, Fei Wang, Chaobin He
  • Patent number: 10711020
    Abstract: There are described ROR? modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating ROR? activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of ROR? activity, for example, autoimmune and/or inflammatory disorders.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: July 14, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, T. G. Murali Dhar, David Marcoux, Robert J. Cherney
  • Patent number: 10711021
    Abstract: Catalysts prepared from abundant, cost effective metals, such as cobalt, nickel, chromium, manganese, iron, and copper, and containing one or more neutrally charged ligands (e.g., monodentate, bidentate, and/or polydentate ligands) and methods of making and using thereof are described herein. Exemplary ligands include, but are not limited to, phosphine ligands, nitrogen-based ligands, sulfur-based ligands, and/or arsenic-based ligands. In some embodiments, the catalyst is a cobalt-based catalyst or a nickel-based catalyst. The catalysts described herein are stable and active at neutral pH and in a wide range of buffers that are both weak and strong proton acceptors. While its activity is slightly lower than state of the art cobalt-based water oxidation catalysts under some conditions, it is capable of sustaining electrolysis at high applied potentials without a significant degradation in catalytic current. This enhanced robustness gives it an advantage in industrial and large-scale water electrolysis schemes.
    Type: Grant
    Filed: November 24, 2015
    Date of Patent: July 14, 2020
    Assignee: YALE UNIVERSITY
    Inventors: Aaron J. Bloomfield, Stafford W. Sheehan, Samuel L. Collom, Robert H. Crabtree, Paul T. Anastas
  • Patent number: 10711022
    Abstract: Provided herein are methods for preparing prebiotic oligosaccharides by non-enzymatic methods of glycosylation of monosaccharides and/or disaccharides or by hydrolysis of polymeric sugars to monosaccharides and simultaneous glycosylation of hydrolytic products. The methods may include mixing one or more types of monosaccharides and/or disaccharides with a water-deficient system at a temperature sufficient to form one or more types of prebiotic oligosaccharides. Also provided are methods of preparing prebiotic oligosaccharides comprising mixing starch, cellulose and/or lignocellulosic biomass with a water-deficient system at a temperature sufficient to form one or more types of prebiotic oligosaccharides that collectively make up at least 25% of the products of the synthesis.
    Type: Grant
    Filed: December 26, 2018
    Date of Patent: July 14, 2020
    Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Xuejun Pan, Ning Li
  • Patent number: 10711024
    Abstract: Novel steviol glycoside compounds characterized by a first group of four glucopyranose residues attached via the number 13 carbon (C13) of the steviol moiety and a second group of two or three glucopyranose residues attached via the number 19 carbon (C19) of the steviol moiety are described, and exemplified by compounds 1-4. These compounds can be present in a composition with other steviol glycosides (e.g., Reb D and Reb M) to enhance their solubilities. Accordingly, the novel compounds can facilitate the preparation of aqueous compositions having a higher concentration of steviol glycosides. A steviol glycoside composition including one or more of compounds 1-4 can be used as a sweetener composition to sweeten other compositions (sweetenable compositions) such as foods, beverages, medicines, oral hygiene compositions, nutraceuticals, and the like.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: July 14, 2020
    Assignee: Cargill, Incorporated
    Inventors: Ting Liu Carlson, Dan Gaspard
  • Patent number: 10711025
    Abstract: Provided is a process for the preparation of diosmin from hesperidin. The process involves the oxidation of acylated hesperidin with iodine or bromine in a C2-C4 carboxylic acid medium and subsequent treatment with an inorganic base to partially neutralize the acidic media. The process allows obtaining diosmin with low iodine or bromine content, avoiding the use of organic solvents.
    Type: Grant
    Filed: April 2, 2019
    Date of Patent: July 14, 2020
    Assignee: INTERQUIM, S.A.
    Inventor: Francisco Javier López Cremades
  • Patent number: 10711026
    Abstract: Compositions including derivatives of spinosyns and methods for the production of derivatives of spinosyns are provided. The spinosyn derivatives described herein include spinosyn derivatives functionalized on the C5-C6 double bond of spinosyn A to provide an additional ring system. The method produces spinosyn derivatives that exhibit activity towards insects, arachnids, and/or nematodes and are useful in the agricultural and animal health markets.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: July 14, 2020
    Assignee: AgriMetis, LLC
    Inventors: Andrew Calabrese, Brian Michael Green, David R. Spring, Jerome Yves Cassayre, Pasquale N. Confalone