Patents Issued in July 14, 2020
-
Patent number: 10710976Abstract: 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: GrantFiled: February 11, 2019Date of Patent: July 14, 2020Assignees: Cerecor Inc., Merck Sharp & Dohme Corp.Inventors: Reza Mazhari, Djelila Mezaache, Blake M. Paterson, James Vornov, Rachel M. Garner, Todd Nelson
-
Patent number: 10710977Abstract: 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: GrantFiled: February 8, 2018Date of Patent: July 14, 2020Assignee: Nissan Chemical CorporationInventors: Daisuke Tanima, Yoshiyuki Kusuoka, Keisuke Tsuji
-
Patent number: 10710978Abstract: 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: GrantFiled: March 31, 2016Date of Patent: July 14, 2020Assignees: DANA-FARBER CANCER INSTITUTE, INC., FONDAZIONE CENTRO SAN RAFFAELEInventors: Nathanael S. Gray, Sara Buhrlage, Kenneth Anderson, Francesca Cottini, Giovanni Tonon
-
Patent number: 10710979Abstract: 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: GrantFiled: July 11, 2016Date of Patent: July 14, 2020Assignee: ZHEJIANG BOSSAN PHARMACEUTICAL CO. LTD.Inventors: Dawei Ma, Qiang Yu, Junying Yuan, Hongguang Xia, Dongpo Cai, Kailiang Wang, Chen Zhang, Shanghua Xia
-
Patent number: 10710980Abstract: 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: GrantFiled: July 18, 2017Date of Patent: July 14, 2020Assignee: Novartis AGInventors: 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: 10710981Abstract: 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: GrantFiled: March 14, 2019Date of Patent: July 14, 2020Assignee: BEIJING INNOCARE PHARMA TECH CO., LTD.Inventors: Xiangyang Chen, Yingxiang Gao, Norman Xianglong Kong
-
Patent number: 10710982Abstract: 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: GrantFiled: February 12, 2020Date of Patent: July 14, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Pranav Gupta, Jiansheng Wan
-
Patent number: 10710983Abstract: 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: GrantFiled: June 26, 2017Date of Patent: July 14, 2020Assignee: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Rose Yen, Jiaxin Yu, Vanessa Taylor, Rajinder Singh
-
Patent number: 10710984Abstract: 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: GrantFiled: April 7, 2017Date of Patent: July 14, 2020Assignee: Boehringer Ingelheim International GmbHInventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec, Stefan Scheuerer
-
Patent number: 10710985Abstract: 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: GrantFiled: May 4, 2018Date of Patent: July 14, 2020Assignee: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll, Remy Halm
-
Patent number: 10710986Abstract: 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: GrantFiled: February 12, 2019Date of Patent: July 14, 2020Assignee: 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: 10710987Abstract: 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: GrantFiled: June 5, 2018Date of Patent: July 14, 2020Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.Inventors: Kevin Wayne Kuntz, Hyeong Wook Choi, Steven Mathieu, Kristen Sanders, Arani Chanda
-
Patent number: 10710988Abstract: [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: GrantFiled: July 18, 2017Date of Patent: July 14, 2020Assignee: Astellas Pharma Inc.Inventors: Takashi Sugane, Norio Asai, Hiroyuki Moritomo, Daisuke Yamashita, Naomi Hosogai
-
Patent number: 10710989Abstract: 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: GrantFiled: February 27, 2018Date of Patent: July 14, 2020Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Makoto Kanematsu, Kazuhisa Ishimoto, Tomoaki Katou
-
Patent number: 10710990Abstract: 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: GrantFiled: December 26, 2017Date of Patent: July 14, 2020Assignee: KAO CORPORATIONInventor: Takashi Aoki
-
Patent number: 10710991Abstract: 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: GrantFiled: April 19, 2019Date of Patent: July 14, 2020Assignee: Syngenta Participations AGInventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
-
Patent number: 10710992Abstract: 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: GrantFiled: December 1, 2015Date of Patent: July 14, 2020Assignee: 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: 10710993Abstract: 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: GrantFiled: June 27, 2017Date of Patent: July 14, 2020Assignee: HANGZHOU REX PHARMACEUTICAL CO., LTD.Inventors: Yonghui Wang, Juan Zhou, Yujun Gao, Dong Wang, Binbin Hong, Ximing Shen, Yaodong Wu, Chunqi Li
-
Patent number: 10710994Abstract: 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: GrantFiled: March 15, 2019Date of Patent: July 14, 2020Assignee: 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: 10710995Abstract: 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: GrantFiled: September 26, 2017Date of Patent: July 14, 2020Assignees: Rhode Island Hospital, Midwestern UniversityInventors: Jack R. Wands, Suzanne De La Monte, Arihiro Aihara, Mark Jon Olsen, John-Michael Thomas
-
Patent number: 10710996Abstract: 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: GrantFiled: May 23, 2016Date of Patent: July 14, 2020Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Yaqiu Long, Meiyu Geng, Zhongliang Xu, Jing Ai
-
Patent number: 10710997Abstract: 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: GrantFiled: September 1, 2017Date of Patent: July 14, 2020Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Andrew Felts, Aaron M. Bender
-
Patent number: 10710998Abstract: 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: GrantFiled: July 27, 2017Date of Patent: July 14, 2020Assignee: VERONA PHARMA PLCInventor: Peter Lionel Spargo
-
Patent number: 10710999Abstract: 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: GrantFiled: October 4, 2017Date of Patent: July 14, 2020Assignee: MYLAN LABORATORIES LIMITEDInventors: Mahdeshkumar Gadakar, Dnyandeo Punde, Rajendra Yadav, Yogesh Wakchaure
-
Patent number: 10711000Abstract: 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: GrantFiled: July 11, 2019Date of Patent: July 14, 2020Assignee: FRONTHERA U.S. PHARMACEUTICALS LLCInventors: Bohan Jin, Qing Dong, Gene Hung, Yao Li
-
Patent number: 10711001Abstract: 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: GrantFiled: December 23, 2016Date of Patent: July 14, 2020Assignees: GUERBET, UNIVERSITE DE BRETAGNE OCCIDENTALE, CENTRAL NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Mariane Le Fur, Raphaël Tripier, Olivier Rousseaux, Maryline Beyler
-
Patent number: 10711002Abstract: 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: GrantFiled: April 21, 2017Date of Patent: July 14, 2020Assignee: THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/MCGILL UNIVERSITYInventors: Moulay A. Alaoui-Jamali, Krikor Bijian, Dominik Wernic
-
Patent number: 10711003Abstract: 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: GrantFiled: October 22, 2019Date of Patent: July 14, 2020Assignee: Bristol-Myers Squibb CompanyInventors: Liqi He, Sanjeev Gangwar, Shoshana L. Posy, Yam B. Poudel, Prasanna Sivaprakasam
-
Patent number: 10711004Abstract: 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: GrantFiled: September 3, 2019Date of Patent: July 14, 2020Assignee: 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: 10711005Abstract: 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: GrantFiled: November 8, 2016Date of Patent: July 14, 2020Assignees: SHENZHEN UNIVERSITY, SHENZHEN KANGJUZHENG PHARMACEUTICAL TECHNOLOGY CO., LTD.Inventors: Guangyi Jin, Zhulin Wang
-
Patent number: 10711006Abstract: 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: GrantFiled: October 24, 2017Date of Patent: July 14, 2020Assignee: HANGZHOU HERTZ PHARMACEUTICAL CO., LTD.Inventors: Xinglu Zhou, Xingguo Liu, Miao Hu
-
Patent number: 10711007Abstract: 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: GrantFiled: April 5, 2019Date of Patent: July 14, 2020Assignee: Prelude Therapeutics IncorporatedInventors: Juan Luengo, Hong Lin, Michael Hawkins, Rupa Shetty, Philip Pitis, Gisela Saborit Villarroya
-
Patent number: 10711008Abstract: 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: GrantFiled: June 3, 2019Date of Patent: July 14, 2020Assignee: Oncternal Therapeutics, Inc.Inventor: Stephen E. Webber
-
Patent number: 10711009Abstract: 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: GrantFiled: December 7, 2018Date of Patent: July 14, 2020Assignees: Hyundai Motor Company, Kia Motors CorporationInventor: Chae Hwan Hong
-
Patent number: 10711010Abstract: 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: GrantFiled: January 15, 2019Date of Patent: July 14, 2020Assignees: LES LABORATORIES SERVIER, VERNALIS (R&d) LTDInventors: 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: 10711011Abstract: 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: GrantFiled: May 19, 2017Date of Patent: July 14, 2020Assignee: BUGWORKS RESEARCH, INC.Inventors: Shahul Hameed Peer Mohamed, Nagakumar Bharatham, Nainesh Katagihallimath, Sreevalli Sharma, Radha Nandishaiah
-
Patent number: 10711012Abstract: 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: GrantFiled: October 17, 2017Date of Patent: July 14, 2020Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Nitin Tukaram Patil, Aslam Chandbhai Shaikh, Prasad Padmakar Kulkarni, Dnyanesh Sadanand Ranade
-
Patent number: 10711013Abstract: 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: GrantFiled: September 25, 2018Date of Patent: July 14, 2020Assignee: ORION CORPORATIONInventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Koivikko, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
-
Patent number: 10711014Abstract: 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: GrantFiled: August 14, 2019Date of Patent: July 14, 2020Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Torrey Pines Institute for Molecular StudiesInventors: Said M. Sebti, Yangmei Li, Richard A. Houghten
-
Patent number: 10711015Abstract: 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: GrantFiled: November 14, 2017Date of Patent: July 14, 2020Assignee: LG CHEM, LTD.Inventors: Milim Lee, Seonkyoung Son, Cheol Jun Song, Hoyong Lee
-
Patent number: 10711016Abstract: 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: GrantFiled: May 1, 2019Date of Patent: July 14, 2020Assignee: The Goodyear Tire & Rubber CompanyInventors: Stefan Mecking, Margaret Flook Vielhaber, Inigo Göttker-Schnetmann, Philip Kenyon
-
Patent number: 10711017Abstract: 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: GrantFiled: February 7, 2019Date of Patent: July 14, 2020Assignee: United States of America as represented by the Secretary of the Air ForceInventors: Scott Iacono, Abby Rose Jennings
-
Patent number: 10711018Abstract: 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: GrantFiled: April 11, 2019Date of Patent: July 14, 2020Assignee: Evonik Operations GmbHInventors: Philipp Albert, Eckhard Just
-
Patent number: 10711019Abstract: 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: GrantFiled: August 17, 2016Date of Patent: July 14, 2020Assignee: Agency for Science, Technology and ResearchInventors: Fuke Wang, Fei Wang, Chaobin He
-
Patent number: 10711020Abstract: 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: GrantFiled: March 7, 2019Date of Patent: July 14, 2020Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, T. G. Murali Dhar, David Marcoux, Robert J. Cherney
-
Patent number: 10711021Abstract: 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: GrantFiled: November 24, 2015Date of Patent: July 14, 2020Assignee: YALE UNIVERSITYInventors: Aaron J. Bloomfield, Stafford W. Sheehan, Samuel L. Collom, Robert H. Crabtree, Paul T. Anastas
-
Patent number: 10711022Abstract: 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: GrantFiled: December 26, 2018Date of Patent: July 14, 2020Assignee: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Xuejun Pan, Ning Li
-
Patent number: 10711024Abstract: 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: GrantFiled: December 17, 2015Date of Patent: July 14, 2020Assignee: Cargill, IncorporatedInventors: Ting Liu Carlson, Dan Gaspard
-
Patent number: 10711025Abstract: 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: GrantFiled: April 2, 2019Date of Patent: July 14, 2020Assignee: INTERQUIM, S.A.Inventor: Francisco Javier López Cremades
-
Patent number: 10711026Abstract: 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: GrantFiled: September 2, 2016Date of Patent: July 14, 2020Assignee: AgriMetis, LLCInventors: Andrew Calabrese, Brian Michael Green, David R. Spring, Jerome Yves Cassayre, Pasquale N. Confalone