Patents Issued in September 15, 2020
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Patent number: 10774073Abstract: The invention relates to inhibitors of dihydrofolate reductase and pharmaceutical preparations thereof. The invention further relates to methods of treatment of parasitic infections, such as T. gondii, T. cruzi, P. falciparum, T. brucei, or L. major infections, using the novel inhibitors of the invention.Type: GrantFiled: February 2, 2017Date of Patent: September 15, 2020Assignee: Vyera Pharmaceuticals, LLCInventors: Stephen B. Thomas, Allen T. Hopper, Matthew Welsch
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Patent number: 10774074Abstract: Compounds of formula I, wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2, or 3 N, O, or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.Type: GrantFiled: June 3, 2016Date of Patent: September 15, 2020Assignee: ORION CORPORATIONInventors: Shouming Wang, Esa Kumpulainen, Jarmo Pystynen, Antti Pohjakallio, Anssi Haikarainen
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Patent number: 10774075Abstract: This disclosure relates to compositions including certain compounds identified by a quantitative, high throughput assay to be effective in the treatment of a Rac-GTPase mediated disorder (e.g., acute lymphoblastic or chronic myelogenous leukemia), as well as methods for the manufacture of and the use of these compounds for treating a Rac-GTPase mediated disorder.Type: GrantFiled: April 15, 2016Date of Patent: September 15, 2020Assignee: Children's Medical Center CorporationInventors: David A Williams, Serena De Vita
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Patent number: 10774076Abstract: Disclosed are novel benzazole compounds and compositions comprising the compounds. The compounds are useful as kinase inhibitors including interleukin receptor associated kinases (IRAK) inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent an IRAK-associated disease or condition.Type: GrantFiled: August 7, 2018Date of Patent: September 15, 2020Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rose Yen, Yan Chen, Rajinder Singh, Vanessa Taylor
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Patent number: 10774077Abstract: The invention relates to a compound comprising the following general formula (1): and said compound for use as a medicament, in particular for use in the treatment psychiatric or neurological disorders and inflammation, in particular neuroinflammation: (formula 1) wherein each of R1, R2 and R3 are selected independently from each other from alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, or heteroaryl.Type: GrantFiled: August 21, 2019Date of Patent: September 15, 2020Assignee: UNIVERSITAT BERNInventors: Jean-Louis Reymond, Simon Nicolussi, Jurg Gertsch
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Patent number: 10774078Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.Type: GrantFiled: June 21, 2019Date of Patent: September 15, 2020Assignee: MISSION THERAPEUTICS LTDInventors: Alison Jones, Mark Ian Kemp, Martin Lee Stockley, Karl Richard Gibson, Gavin Alistair Whitlock, Andrew Madin
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Patent number: 10774079Abstract: Provided are a quinazoline derivative, a pharmaceutical composition containing the same, a method for preparation of said derivative, and an application of same as an anti-cancer drug.Type: GrantFiled: August 8, 2019Date of Patent: September 15, 2020Assignee: CSPC ZHONGQI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO., LTD.Inventors: Ying Shi, Qingzhi Gao, Xiaozhuo Chen, Yi Mi, Yaran Zhang, Hanyu Yang, Yujie Chen, Chunlei Liu, Guorui Mi, Yuxiu Ma, Dongmin Shen, Yang Guo, Linjing Fan
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Patent number: 10774080Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.Type: GrantFiled: January 8, 2020Date of Patent: September 15, 2020Assignee: Theravance Biopharma R&D IP, LLCInventors: Jennifer Kozak, Ryan Hudson
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Patent number: 10774081Abstract: Disclosed in the present invention is a type of indole substituted piperidine compounds as an estrogen receptor down-regulator. Specifically disclosed are a compound as shown in formula (I), a pharmaceutically acceptable salt, hydrate or prodrug thereof, a preparation method therefor, a pharmaceutical composition thereof, and a use thereof as an estrogen receptor down-regulator in the treatment of estrogen receptor positive breast cancers.Type: GrantFiled: October 30, 2017Date of Patent: September 15, 2020Assignees: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD., SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.Inventors: Jianyu Lu, Charles Z. Ding, Xu Zeng, Huijun He, Shuhui Chen, Lihong Hu, Jiaqiang Dong, Tie-Lin Wang
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Patent number: 10774082Abstract: [Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.Type: GrantFiled: December 12, 2019Date of Patent: September 15, 2020Assignee: Astellas Pharma Inc.Inventors: Kazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike
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Patent number: 10774083Abstract: Provided is a heterocyclic amide compound that may have a PRS inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for PRS associated diseases and the like including cancer. A compound represented by the following formula (I): wherein a group represented by is a group represented by the following formula (II) or the following formula (III): and other symbols are as described in the DESCRIPTION, or a salt thereof.Type: GrantFiled: September 14, 2017Date of Patent: September 15, 2020Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takaharu Hirayama, Yasuhiro Hirata, Yusuke Tominari, Naoki Iwamura, Yusuke Sasaki, Moriteru Asano, Terufumi Takagi, Masanori Okaniwa, Shinichi Imamura
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Patent number: 10774084Abstract: Adenine derivatives substituted at the C2, N6, and N9 purine positions having antisenescent and combined photoprotective UVA/UVB effects. These substances are particularly suitable as anti-senescent and UV-photoprotective component in cosmetic preparations, plant protection preparations and in preparations for the treatment/application of tissue cultures.Type: GrantFiled: August 24, 2016Date of Patent: September 15, 2020Assignee: UNIVERZITA PALACKEHO V OLOMOUCIInventors: Martin Hönig, Lucie Plihalova, Karel Dolezal, Jiri Voller, Miroslav Strnad, Lukas Spichal, Jitka Vostalova, Alena Rajnochova Svobodova, Jitka Ulrichova, Alena Kadlecova, Ondrej Plihal
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Patent number: 10774085Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.Type: GrantFiled: July 25, 2018Date of Patent: September 15, 2020Assignee: ARRAY BIOPHARMA INC.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Patent number: 10774086Abstract: The disclosure generally relates to compounds of formula (I), including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.Type: GrantFiled: November 27, 2017Date of Patent: September 15, 2020Assignee: Bristol-Myers Squibb CompanyInventors: Richard A. Hartz, Vijay T. Ahuja, Prasanna Sivaprakasam, Gene M. Dubowchik, John E. Macor
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Patent number: 10774087Abstract: Provided is a novel compound or a salt thereof inhibiting MTHFD2 and useful for treating a disease caused by overexpression of MTHFD2, a disease involved in overexpression of MTHFD2 and/or a disease associated with overexpression of MTHFD2. Solution Provided is a sulfonamide derivative having a coumarin skeleton represented by the following formula (I) and having various substituents: wherein R1, R2, R3, R4, R5, R6 and R7 are the same as defined in the specification, and a salt thereof.Type: GrantFiled: November 22, 2017Date of Patent: September 15, 2020Assignee: Daiichi Sankyo Company, LimitedInventors: Masahiro Ota, Hidekazu Inoue, Junya Kawai, Hitoshi Ohki, Tadashi Toki
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Patent number: 10774088Abstract: The present invention relates to an improved process for preparing [(1S,2R)-3-[[(4-aminophenyl)-sulfonyl](2-methyl-propyl)amino]-2-hydroxy-1-(phenylmethyl)-propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester—which compound is also known under its INN as darunavir—by reacting carbonic acid 2,5-dioxo-1-pyrrolidinyl[(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl]ester with 4-amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(2-methylpropyl)-benzenesulfonamide in ethanol as solvent. Furthermore said process allows for darunavir to be isolated immediately in its ethanolate form, i.e. darunavir monoethanolate, which is the marketed form of darunavir under the tradename Prezista™.Type: GrantFiled: November 16, 2017Date of Patent: September 15, 2020Assignee: Janssen Sciences Ireland Unlimited CompanyInventors: Alfred Elisabeth Stappers, Yolande Lydia Lang, Shane Barry Robinson
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Patent number: 10774089Abstract: There is described a method of producing (?)-levoglucosenone, said method comprising, heating lignin to a temperature in excess of 150° C. for a time sufficient to convert a proportion of the lignin to (?)-evoglucosenone.Type: GrantFiled: April 20, 2016Date of Patent: September 15, 2020Assignee: UNIVERSITY OF YORKInventors: James Hanley Clark, Mario De Bruyn, Vitaliy Lvovich Budarin
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Patent number: 10774090Abstract: The present invention discloses a compound comprising the formula: wherein R is hydrogen or an alkyl group having from one to ten carbon atoms, or a compound of the formula wherein the S is replaced by CH2 or O, and optionally comprising a pharmaceutically acceptable salt or hydrate thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: January 22, 2019Date of Patent: September 15, 2020Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 10774091Abstract: The present invention generally relates to novel pharmaceutical formulations containing 2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide, methods of preparation thereof and their use in medical therapy.Type: GrantFiled: March 13, 2019Date of Patent: September 15, 2020Assignee: KaNDy Therapeutics LimitedInventors: Mike Trower, Monica Lazaro, Derek Bush, David Elder, Mary Kerr
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Patent number: 10774092Abstract: In certain aspects, the invention provides a method for treating a disease or condition in a subject, the method comprising co-administering to a subject in need thereof a therapeutically effective amount of at least one ULK1-inhibiting pyrimidine, and a therapeutically effective amount of an mTOR inhibitor.Type: GrantFiled: April 19, 2019Date of Patent: September 15, 2020Assignees: SALK INSTITUTE FOR BIOLOGICAL STUDIES, SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE, YALE UNIVERSITYInventors: Reuben J. Shaw, Daniel F. Egan, Nicholas Cosford, Benjamin Turk, Mitchell Vamos, Dhanya Raveendra Panickar, Matthew Chun, Douglas Sheffler
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Patent number: 10774093Abstract: The invention provides synthetic intermediates and synthetic processes that are useful for preparing the antibacterial agent TXA709:Type: GrantFiled: March 30, 2018Date of Patent: September 15, 2020Assignee: Taxis Pharmaceuticals, Inc.Inventors: Sanjeevani Ghone, Fu-An Kang, Nareshkumar Jain, Ajit S. Parhi, Ravi Ponnaiah, Anil Kumar Soni, Siva Rami Reddy Athunuri, Thrisulapani Korrakuti, Pullarao Seelam
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Crystal forms and salt forms of 7h-pyrrolo[2,3-d]pyrimidine compounds and preparation method thereof
Patent number: 10774094Abstract: The present invention discloses crystal forms and salt forms of a 7H-pyrrolo[2,3-d]pyrimidine compounds and preparation methods thereof, and further discloses use of the crystal forms and the salt forms in the manufacture of a medicament for treating arthritis.Type: GrantFiled: November 23, 2017Date of Patent: September 15, 2020Assignee: Wuxi Fortune Pharmaceutical Co., LtdInventors: Weiwei Mao, Hao Wu, Qiang Guo, Xuejian Zheng, Yonggang Liao -
Patent number: 10774095Abstract: The invention provides metal-ascorbic acid crystals and a method for synthesizing the metal-ascorbic acid crystals. The metal in the metal-ascorbic acid crystals is one of copper (Cu), gold (Au) and silver (Ag). The method for synthesizing the metal-ascorbic acid crystals includes sonicating a solution of ascorbic acid and a solvent in dark to obtain a clear solution, wherein the solvent is one of dimethylformamide (DMF) and dimethyl sulfoxide (DMSO). A metal salt is added to the clear solution, wherein the metal salt is one of copper (II) sulfate pentahydrate (CuSO4.5H2O), gold (III)-chloride (AuCl3), and silver sulfate (Ag2SO4). The clear solution is sonicated after adding the metal salt to obtain a reaction mixture. Thereafter, the reaction mixture is heated in dark. The reaction mixture is treated to facilitate solvent extraction of the metal-ascorbic acid. Finally, the metal-ascorbic acid is crystallized.Type: GrantFiled: December 9, 2015Date of Patent: September 15, 2020Assignee: THE KING ABDULAZIZ CITY FOR SCIENCE AND TECHNOLOGYInventors: Nezar Hassan Khdary, Abdulaziz Almalik
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Patent number: 10774096Abstract: Substituted benzoxaboroles whose structure comprises Formula (III), wherein R3 is selected from —CH3, —CH2CH3, —CH2?CH2, —CH2CH2CH3, —CH(CH3)2, —CH2CH2?CH2, and cyclopropyl, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, and —CH(CH3)2; compositions containing such compounds, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.Type: GrantFiled: February 12, 2016Date of Patent: September 15, 2020Assignees: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED, ANACOR PHARMACEUTICALS, INC.Inventors: Carlos Alemparte-Gallardo, Michael Richard Kevin (Dickon) Alley, David Barros-Aguirre, Ilaria Giordano, Vincent Hernandez, Xianfeng Li, Jacob J. Plattner
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Patent number: 10774097Abstract: The invention relates to chemical compound of the general structure [A-R3—X—R4] where A=[R1-R2] or [R1] R1=aryl, heteroaryl R2=alkyl, aryl, heteroaryl, carbonyl, thiocarbonyl, alkyl ester, alkyl thioester R3=O, S, NH X=closo- or nido-boron cluster R4= where Z=OH, SH, NH2 where R5 is selected from H, alkyl, aryl, heteroaryl, alkyl ether, alkyl thioether, alkylamine and R6 is selected from alkyl, aryl, heteroaryl, alkyl ether, alkyl thioether, alkylamine and where R3 and R4 are in meta or para positions to one another, to a process for preparation thereof and to the use thereof, especially in medicine, for example in the inhibition of lipoxygenase.Type: GrantFiled: October 21, 2016Date of Patent: September 15, 2020Assignee: UNIVERSITÄT LEIPZIGInventors: Evamarie Hey-Hawkins, Robert Kuhnert
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Patent number: 10774098Abstract: Provided is a method for separating the four optical isomers of Nahlsgen.Type: GrantFiled: September 12, 2017Date of Patent: September 15, 2020Assignees: KYOTO UNIVERSITY, NAHLS CORPORATION CO., LTD.Inventors: Jun Hiratake, Bunta Watanabe, Ryuzo Yoshioka, Hideaki Ishida
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Patent number: 10774099Abstract: The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)—active and toll-like receptor (TLR8)—active imidazoquinolines and oxoadenines.Type: GrantFiled: December 12, 2016Date of Patent: September 15, 2020Assignee: GLAXOSMITHKLINE BIOLOGICALS SAInventors: Helene G. Bazin-Lee, Laura S. Bess, David A. Johnson
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Patent number: 10774100Abstract: An object t of the present invention is to proroaide crystal of a cyclic phosphonic acid sodium salt (2ccPA) with high purity and excellent storage stability and a method for producing the crystal.Type: GrantFiled: July 2, 2019Date of Patent: September 15, 2020Assignees: OTSUKA CHECMIAL CO., LTD., SANSHO CO., LTD.Inventors: Hiroaki Yuasa, Hiroki Okazaki
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Patent number: 10774101Abstract: Optionally substituted BODIPY-Iridium complexes, such as those depicted Formula 4, may be useful in filters for display devices.Type: GrantFiled: June 5, 2018Date of Patent: September 15, 2020Assignee: NITTO DENKO CORPORATIONInventor: Tissa Sajoto
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Patent number: 10774102Abstract: An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.Type: GrantFiled: January 28, 2016Date of Patent: September 15, 2020Assignee: Galecto Biotech ABInventors: Thomas Brimert, Richard Johnsson, Hakon Leffler, Ulf Nilsson, Fredrik Zetterberg
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Patent number: 10774103Abstract: Disclosed are steviol glycosides referred to as rebaudioside V and rebaudioside W. Also disclosed are methods for producing rebaudioside M (Reb M), rebausoside G (Reb G), rebaudioside KA (Reb KA), rebaudioside V (Reb V) and rebaudioside (Reb W).Type: GrantFiled: November 2, 2017Date of Patent: September 15, 2020Assignee: Conagen Inc.Inventors: Guohong Mao, Xiaodan Yu
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Patent number: 10774104Abstract: Disclosed is a method for the preparation of intermediates useful in the synthesis of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. Also disclosed is a method of preparing gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate.Type: GrantFiled: December 9, 2016Date of Patent: September 15, 2020Assignee: Laurus Labs Private LtdInventors: Mani Bushan Kotala, Venkata Lakshmi Narasimha Rao Dammalapati
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Patent number: 10774105Abstract: Phosphoramidate esters and related nucleotide analogs useful in polynucleotide sequencing techniques, and synthetic methods for preparing those compounds, are disclosed, including compounds having the following structure: wherein R1, R2, R3 and R4 are as defined herein. These compounds include nucleotide phosphoramidates analogs that are modified on the alpha-phosphate to enable attachment of a variety of application-specific substituents such as tether molecules.Type: GrantFiled: April 10, 2019Date of Patent: September 15, 2020Assignee: STRATOS GENOMICS, INC.Inventors: Mark Stamatios Kokoris, John Tabone, Melud Nabavi, Aaron Jacobs
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Patent number: 10774106Abstract: The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: GrantFiled: December 19, 2019Date of Patent: September 15, 2020Assignee: Janssen Sciences Ireland Unlimited CompanyInventors: Ioannis Nicolaos Houpis, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
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Patent number: 10774107Abstract: Novel compositions and methods for engineering wireframe architectures and scaffolds of increasing complexity by creating gridiron-like DNA structures (FIG. 1). A series of four-arm junctions are used as vertices within a network of double-helical DNA fragments. Deliberate distortion of the junctions from their most relaxed conformations ensures that a scaffold strand can traverse through individual vertices in multiple directions. DNA gridirons, ranging from two-dimensional arrays with reconfigurability to multilayer and three-dimensional structures and curved objects, can be assembled according the methods presented herein.Type: GrantFiled: November 28, 2018Date of Patent: September 15, 2020Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITYInventors: Dongran Han, Hao Yan
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Patent number: 10774108Abstract: Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6 and are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.Type: GrantFiled: November 27, 2015Date of Patent: September 15, 2020Assignee: Sage Therapeutics, Inc.Inventors: Gabriel Martinez Botella, Boyd L. Harrison, Albert Jean Robichaud, Francesco G. Salituro, Richard Thomas Beresis
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Patent number: 10774109Abstract: The present invention provides a crystal of reduced glutathione having excellent powder properties and a method for producing the same. The present invention relates to a crystal of reduced glutathione, wherein the average crystal thickness is 10 ?m or more.Type: GrantFiled: March 10, 2017Date of Patent: September 15, 2020Assignee: KYOWA HAKKO BIO CO., LTD.Inventors: Kazunari Fukumoto, Maya Iguchi, Hiroshi Nagano
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Patent number: 10774110Abstract: A compound of Formula (I), and its analogs are provided. Compositions that include Formula I can be used to inhibit human equilibrative nucleoside transporter 1, increase adenosine signaling and produce effects that include increasing antiviral activity, increasing antiparasitic activity, increasing alcohol tolerance, decreasing pain protecting from ischemia as well as many other conditions.Type: GrantFiled: February 3, 2017Date of Patent: September 15, 2020Assignee: The Johns Hopkins UniversityInventors: Jun Liu, Jingxin Wang, Zhaoli Sun, Sam Hong
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Patent number: 10774111Abstract: The present invention relates to an opioid peptide represented by general formula TyrGlyGly-X1-X2-X3-X4, wherein: X1 is represented by Thr or Glu; X1 is represented by Gly or Thr or Ala; X3 is represented by Ala or Val or Gly or Glu; and X4 is represented by His or Gln or Thr or SEQ ID NO:1, or HisTyr or GlnTyr or ThrTyr. The invention also relates to pharmaceutical and food compositions comprising the peptide and to the use of the same for analgesic purposes, and/or for providing a feeling of satiety to a subject.Type: GrantFiled: August 17, 2015Date of Patent: September 15, 2020Assignees: EMBRAPA-EMPRESA BRASILEIRA DE PESQUISA AGROPECUARIA, FUNDAÇÃO UNIVERSIDADE DE BRASÍLIA—FUB—UNBInventors: Carlos Bloch, Jr., Felipe Vinecky, Karla Graziella Moreira, Márcia Renata Mortari
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Patent number: 10774112Abstract: Mimetic peptides having anti-angiogenic and anti-tumorigenic properties and methods of their use for treating cancer, ocular diseases, such as age-related macular degeneration, and other-angiogenesis-dependent diseases are disclosed. More particularly, an isolated peptide comprising the amino acid sequence LRRFSTAPFAFIDINDVINF, which exhibits anti-angiogenic activity in endothelial cell proliferation, migration, adhesion, and tube formation assays, anti-migratory activity in human breast cancer cells in vitro, anti-angiogenic and anti-tumorigenic activity in vivo in breast cancer xenograft models, and age-related macular degeneration models is disclosed. The isolate peptide also exhibits anti-lymphangiogenic and directly anti-tumorigenic properties.Type: GrantFiled: September 22, 2017Date of Patent: September 15, 2020Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Aleksander S. Popel, Niranjan B. Pandey, Esak Lee, Jordan J. Green, Ron B. Shmueli
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Patent number: 10774113Abstract: The invention relates to novel infective agents, the use thereof for the production of a pharmaceutical composition for the treatment and prophylaxes of a disease, preferably an infectious disease, a pharmaceutical composition comprising said compound, and to methods of producing said compounds. The invention further relates to a new probiotic configured for preventing or reducing the colonization by a pathogenic microorganism of an organ of a living being.Type: GrantFiled: September 22, 2017Date of Patent: September 15, 2020Assignee: Eberhard Karls Universitaet TuebingenInventors: Bernhard Krismer, Andreas Peschel, Stephanie Grond, Alexander Zipperer, Martin Christoph Konnerth, Daniela Janek, Hubert Kalbacher, Nadine Anna Schilling
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Patent number: 10774114Abstract: The invention provides polypeptides interacting with the binding of the RSV phosphoprotein P with the RSV nucleoprotein N and methods of using such polypeptides in the treatment and/or prevention of RSV infection.Type: GrantFiled: March 10, 2015Date of Patent: September 15, 2020Assignee: FONDATION THE ARKInventors: Origéne Nyanguile, Jean-François Eleouet, Marie Galloux
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Patent number: 10774115Abstract: A first Fab region-binding peptide includes an amino acid sequence selected from the group consisting of SEQ ID NOs: 1 to 5 with substitution of one or more amino acid residues at the 17th position and the 36th position, wherein an acid dissociation pH thereof is shifted to a neutral side. A second Fab region-binding peptide further includes deletion, substitution and/or addition of one or more amino acid residues at positions other than the 17th position and the 36th position. A third Fab region-binding peptide includes an amino acid sequence with a sequence identity of 80% or more to the amino acid sequence of the first Fab region-binding peptide.Type: GrantFiled: August 25, 2017Date of Patent: September 15, 2020Assignee: KANEKA CORPORATIONInventor: Shinichi Yoshida
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Patent number: 10774116Abstract: The present invention provides a recombinant protein capable of binding to complement factor H (CFH), and thereby inducing increased binding of C3d and C3b by bound CFH compared to unbound CFH. Methods and medical devices for using utilising the same are also described.Type: GrantFiled: July 6, 2018Date of Patent: September 15, 2020Assignee: The University Court of the University of EdinburghInventors: Paul Barlow, Andrew Herbert, Elisavet Makou
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Patent number: 10774117Abstract: In one aspect, the invention relates to an immunogenic composition that includes a mutant Clostridium difficile toxin A and/or a mutant Clostridium difficile toxin B. Each mutant toxin includes a glucosyltransferase domain having at least one mutation and a cysteine protease domain having at least one mutation, relative to the corresponding wild-type C. difficile toxin. The mutant toxins may further include at least one amino acid that is chemically crosslinked. In another aspect, the invention relates to antibodies or binding fragments thereof that binds to said immunogenic compositions. In further aspects, the invention relates to isolated nucleotide sequences that encode any of the foregoing, and methods of use of any of the foregoing compositions.Type: GrantFiled: July 12, 2017Date of Patent: September 15, 2020Assignee: Wyeth LLCInventors: Kathrin Ute Jansen, Annaliesa Sybil Anderson, Robert G. K. Donald, Maninder K. Sidhu, Narender K. Kalyan, Justin Keith Moran, Mark E. Ruppen, Michael James Flint
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Patent number: 10774118Abstract: The present invention provides a family of non-naturally occurring polypeptides having cholesterol efflux activity that parallels that of full-length apolipoproteins (e.g., Apo AI and Apo E), and having high selectivity for ABCA1 that parallels that of full-length apolipoproteins. Further, the peptides of the invention have little or no toxicity when administered at therapeutic and higher doses. The invention also provides compositions comprising such polypeptides, methods of identifying, screening and synthesizing such polypeptides, and methods of treating, preventing or diagnosing diseases and disorders associated with dyslipidemia, hypercholesterolemia, or inflammation; or diseases involving abnormal glucose metabolism, e.g., diabetes, metabolic syndrome; or Alzheimer's Disease or frontotemporal dementia.Type: GrantFiled: June 27, 2018Date of Patent: September 15, 2020Assignee: The Regents of the University of CaliforniaInventors: John K. Bielicki, Jan Johansson, Waleed Danho
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Patent number: 10774119Abstract: The present invention relates to novel, specific-binding therapeutic and/or diagnostic polypeptides directed against the target of Swiss Prot Q16552 and novel, specific-binding therapeutic and/or diagnostic polypeptides directed against the target of Swiss Prot Q9NPF7. In addition, the present invention relates to novel, specific-binding therapeutic and/or diagnostic polypeptides directed against one or both of Swiss Prot Q16552 and Swiss Prot Q9NPF7. The invention also relates to nucleic acid molecules encoding such polypeptides and to methods for generation of such polypeptides and nucleic acid molecules. In addition, the invention is directed to compositions comprising the polypeptides, and therapeutic and/or diagnostic uses of these polypeptides.Type: GrantFiled: May 20, 2015Date of Patent: September 15, 2020Assignee: Pieris Pharmaceuticals GmbHInventors: Marlon Hinner, Alexander Wiedenmann, Andrea Allersdorfer
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Patent number: 10774120Abstract: The disclosure pertains to conformational epitopes in A-beta, antibodies thereto and methods of making and using immunogens and antibodies specific thereto.Type: GrantFiled: November 9, 2016Date of Patent: September 15, 2020Assignee: The University of British ColumbiaInventors: Neil R. Cashman, Steven S. Plotkin
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Patent number: 10774121Abstract: The disclosure relates generally to neurodegenerative disorders and more specifically to a group of presenilin/G-protein/c-src binding polypeptides and methods of use for modulating signaling and progression of Alzheimer's disease.Type: GrantFiled: February 21, 2019Date of Patent: September 15, 2020Assignee: The Regents of the University of CaliforniaInventors: Nazneen Dewji, S. Jonathan Singer
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Patent number: 10774122Abstract: The present disclosure relates to compositions and methods for cancer therapy, including but not limited to, targeted inhibition of cancer markers. In particular, the present disclosure relates to recurrent gene fusions as clinical targets for cancer.Type: GrantFiled: March 19, 2018Date of Patent: September 15, 2020Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Arul Chinnaiyan, Xiaoju Wang