Patents Issued in September 11, 2018
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Patent number: 10071999Abstract: The present invention relates to novel crystalline forms of compound (I), (3-Amino-oxetan-3-ylmethyl)-[2-(5,5-dioxo-5,6,7,9-tetrahydro-5lambda*6*-thia-8-aza-benzocyclohepten-8-yl)-6-methyl-quinazolin-4-yl]-amine and pharmaceutical compositions comprising the crystalline forms thereof disclosed herein, which may be used for the treatment or prophylaxis of a viral disease in a patient relating to respiratory syncytial virus (RSV) infection or a disease caused by RSV infection.Type: GrantFiled: January 12, 2018Date of Patent: September 11, 2018Assignee: HOFFMANN-LA ROCHE INC.Inventors: Wei Zhang, Lin Wang, Wei Li
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Patent number: 10072000Abstract: The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.Type: GrantFiled: August 13, 2013Date of Patent: September 11, 2018Assignee: FERRER INTERNACIONAL, S.A.Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
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Patent number: 10072001Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed:Type: GrantFiled: June 2, 2015Date of Patent: September 11, 2018Assignee: Gilead Sciences, Inc.Inventors: Zhimin Du, Juan Arnaldo Guerrero, Joshua Aaron Kaplan, John Edward Knox, Jr., Devan Naduthambi, Barton W. Phillips, Chandrasekar Venkataramani, Peiyuan Wang, William J. Watkins, Jeff Zablocki
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Patent number: 10072002Abstract: The present invention relates to pyridinylaminopyrimidine derivatives represented by the following formula (I), and pharmaceutically acceptable salts, preparation process and use thereof, wherein R1, R2, R3, R4, R5, m and A are defined as in the description. Pyridinylaminopyrimidine derivatives of the present invention can selectively inhibit the activity of mutant-type epidermal growth factor receptor (EGFR), have a good inhibition for the cancer cell proliferation, and therefore can be used as a therapeutic agent for treating tumors and relevant diseases.Type: GrantFiled: July 29, 2015Date of Patent: September 11, 2018Assignee: Shanghai Allist Pharmaceuticals, Inc.Inventors: Huibing Luo, Huayong Zhou, Shuhui Wang, Yong Wu
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Patent number: 10072003Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.Type: GrantFiled: August 24, 2015Date of Patent: September 11, 2018Inventors: Ashok Arasappan, Christopher James Bungard, Jessica L. Frie, Yongxin Han, Scott B. Hoyt, Peter J. Manley, Robert S. Meissner, James J. Perkins, Iyassu K. Sebhat, Robert R. Wilkening, Kenneth J. Leavitt
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Patent number: 10072004Abstract: Provided herein is a synthetic process for preparing a compound of Formula (1). The disclosure also provides useful intermediates and salts, amorphous and polymorph forms of the compound of Formula (1). These compounds are useful for various disease including cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, and osteoarthritis as well as Wnt-related diseases.Type: GrantFiled: June 1, 2017Date of Patent: September 11, 2018Assignee: Samumed, LLCInventor: Sunil Kumar KC
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Patent number: 10072005Abstract: 4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.Type: GrantFiled: January 19, 2018Date of Patent: September 11, 2018Assignee: Eisai R&D Management Co., Ltd.Inventors: Andrew Payne, Jose Luis Castro Pineiro, Louise Michelle Birch, Afzal Khan, Alan James Braunton, James Edward Kitulagoda, Motohiro Soejima
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Patent number: 10072006Abstract: The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as ?-lactamase inhibitors and/or as antibacterial agents.Type: GrantFiled: March 30, 2016Date of Patent: September 11, 2018Assignee: MUTABILISInventors: Audrey Caravano, Sophie Chasset, Francis Chevreuil, Fabien Faivre, Nicolas Lecointe, Benoît Ledoussal, Frédéric Le Strat, Sébastien Richard, Christophe Simon, Sophie Vomscheid, Julie Brias, Julien Barbion
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Patent number: 10072007Abstract: The present invention is directed to a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.Type: GrantFiled: March 24, 2016Date of Patent: September 11, 2018Assignee: Tetraphase Pharmaceuticals, Inc.Inventors: Chi-Li Chen, Roger B. Clark, Yonghong Deng, Minsheng He, Louis Plamondon, Cuixiang Sun, Xiao-Yi Xiao, Magnus P. Ronn
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Patent number: 10072008Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to spiro-isoquinoline-3,4?-piperidine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.Type: GrantFiled: April 27, 2016Date of Patent: September 11, 2018Assignee: ESTEVE PHARMACEUTICALS S.A.Inventor: Carmen Almansa-Rosales
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Patent number: 10072009Abstract: The present invention relates to the N-substituted beta-carbolinium compounds of general formula A and formulae I and II wherein, R1 and R2 groups are selected from halogens or trifluoromethyl; R3 group is selected from hydrogen or methyl; Ar is selected from aryl and heteroaryl, X is selected from halogens; and R1 and R2 groups may be attached to any position on ring E. The present invention particularly relates to synthesis and p-glycoprotein induction activity of the N-substituted beta-carbolinium compounds. In addition, the invention relates to methods of using compounds for treating or preventing Alzheimer's disease.Type: GrantFiled: October 21, 2015Date of Patent: September 11, 2018Assignee: Council of Scientific and Industrial ResearchInventors: Sandip Bharate, Ajay Kumar, Sudhakar Manda, Prashant Joshi, Sonali Bharate, Ram Vishwakarma
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Patent number: 10072010Abstract: The invention relates to substituted pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]-quinoxaline compounds, represented by Formula 1, defined herein, free base or pharmaceutically acceptable salt forms of the compounds, pharmaceutical compositions thereof, and methods of treating conditions of the central nervous system therewith:Type: GrantFiled: June 21, 2017Date of Patent: September 11, 2018Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
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Patent number: 10072011Abstract: The present invention relates to novel substituted bridged urea analog compounds of Formula (I) or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, processes for making and use of such compounds, alone or in combination with other therapeutic agents, as Sirtuin Modulators useful for increasing lifespan of a cell, and in treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.Type: GrantFiled: November 19, 2015Date of Patent: September 11, 2018Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: James Lamond Ellis, Karen Anderson Evans, Ryan Michael Fox, William Henry Miller, Mark Andrew Seefeld
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Patent number: 10072012Abstract: The present invention provides process for preparing crystalline Pemetrexed dipotassium (I) Form-SP9 characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2?° peaks selected from the XRPD peak set of 5.0, 12.5, 17.2, 20.8, 22.4, 25.7, 26.9 and 27.9±0.2 2?°. The invention also provides process for preparing its pharmaceutical composition thereof, which may be useful for anti-cancer treatment.Type: GrantFiled: November 11, 2014Date of Patent: September 11, 2018Assignee: Shilpa Mecicare LimitedInventors: Bhagat Raj Pipal, Venkata Reddy Gayam, Akshay Kant Chaturvedi
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Patent number: 10072013Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.Type: GrantFiled: April 5, 2017Date of Patent: September 11, 2018Assignee: RHIZEN PHARMACEUTICALS SAInventors: Swaroop Kumar V. S. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
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Patent number: 10072014Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.Type: GrantFiled: December 2, 2015Date of Patent: September 11, 2018Assignee: JANSSEN PHARMACEUTICA NVInventors: Michiel Luc Maria Van Gool, Manuel Jesús Alcázar-Vaca, Sergio-Alvar Alonso-de Diego, Ana Isabel De Lucas Olivares
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Patent number: 10072015Abstract: HIV replication inhibitors of formula wherein a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substitutedType: GrantFiled: September 22, 2017Date of Patent: September 11, 2018Assignee: Janssen Sciences Ireland UCInventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Paul Adriaan Jan Janssen
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Patent number: 10072016Abstract: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 2, 2017Date of Patent: September 11, 2018Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Konstantin Petrukhin, Christopher Cioffi, Graham Johnson, Rando Allikmets, Emily Freeman, Ping Chen, Michael Conlon, Lei Zhu
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Patent number: 10072017Abstract: The invention relates to a compound of Formula I or IA compositions comprising compounds of Formula I or IA, and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: GrantFiled: December 28, 2016Date of Patent: September 11, 2018Assignee: Flatley Discovery Lab, LLCInventors: Michael P. Zawistoski, Asmita Deshpande, Bridget M. Cole
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Patent number: 10072018Abstract: The aspects of the disclosed embodiments are directed to novel compounds, specifically, quaternary ammonium derivatives of tertiary amine containing opioid drug compounds such as hydrocodone, hydromorphone and oxycodone, formulations containing said. compounds or pharmaceutically acceptable salts thereof, which are capable of providing controlled release of the opioid drug upon administration to a patient in order to treat pain.Type: GrantFiled: April 16, 2014Date of Patent: September 11, 2018Assignee: BIOPHARMA WORKSInventors: Robert Volkmann, Anthony Marfat, Peter Cornelius, Panayiotis Zagouras, Fredrick Raymond Nelson, Anton Franz Joseph Fliri
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Patent number: 10072019Abstract: The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, and Formula IV, and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: December 17, 2014Date of Patent: September 11, 2018Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Patent number: 10072020Abstract: An isatin spiro compound having the following formula (I): R1 is halogen or C1-3 alkyl; R2 is C1-3 alkyl or benzyl; and R3 and R3? are independently H, C1-3 alkyl or phenyl.Type: GrantFiled: April 19, 2018Date of Patent: September 11, 2018Assignee: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Chengyuan Liang, Danni Tian, Shunjun Ding
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Patent number: 10072021Abstract: Disclosed is a new compound that inhibits binding between a DX2 protein and a p14/ARF protein, a pharmaceutical composition including the new compound as an effective component for treating or preventing a cancer disease, an anticancer adjuvant for improving an anticancer effect of a drug-resistant anticancer drug, and a composition including an AIMP2-DX2 protein or a fragment thereof for diagnosing lung cancer.Type: GrantFiled: June 30, 2015Date of Patent: September 11, 2018Assignees: PUSAN NATIONAL UNIVERSITY INDUSTRY-UNIVERSITY COOPERATION FOUNDATION, THE INDUSTRY & ACADEMIC COOPERATION IN CHUNGNAM NATIONAL UNIVERSITY (IAC)Inventors: Bum Joon Park, Gyu Yong Song, Ah-Young Oh, Jee-Hyun Lee, Jin-Hyuk Her
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Patent number: 10072022Abstract: Certain embodiments are directed to oridonin analogs or derivatives. In certain aspects, the derivatives are used as anticancer or anti-inflammatory agents.Type: GrantFiled: June 28, 2017Date of Patent: September 11, 2018Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventors: Jia Zhou, Chunyong Ding, Qiang Shen
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Patent number: 10072023Abstract: A compound according to Formula IA and IB, reversibly convertible under photochromic and electrochromic conditions between a ring-open isomer A and a ring-closed isomer B is provided. For substitutent groups, Z is N, O or S; each R1 is independently selected from the group consisting of H, or halo; each R2 is independently selected from the group consisting of H, halo, a polymer backbone, alkyl or aryl; or, when both R2 together form —CH?CH— and form part of a polymer backbone; each R3 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl; each R4 is aryl; and each R5 is independently selected from the group consisting of H, halo, alkyl, alkoxy, thioalkyl or aryl.Type: GrantFiled: November 20, 2015Date of Patent: September 11, 2018Assignee: Switch Materials, Inc.Inventors: Neil Robin Branda, Jeremy Graham Finden, Simon James Gauthier, Ali Hayek, Kyle Andrew Hope-Ross, James Daniel Senior, Andreea Spantulescu, Serguei Sviridov
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Patent number: 10072024Abstract: The present invention relates to methods and compositions for inhibiting the activity of skin proteases, especially human kallikrein 7 (KLK7), human kallikrein 5 (KLK5), and human kallikrein 14 (KLK14). More specifically, the invention relates to the use of substituted 3,1-benzoxazin-4-ones being selective inhibitors of human skin kallikreins for the treatment of skin diseases, more specifically for the treatment of inflammatory skins diseases, especially Netherton syndrome.Type: GrantFiled: June 5, 2017Date of Patent: September 11, 2018Assignee: SIXERA PHARMA ABInventors: Fredrik Wagberg, Goran Leonardsson
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Patent number: 10072025Abstract: The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the treatment and prevention of JAK-mediated diseases and disorders using the novel compounds, as well as pharmaceutical compositions containing the compounds.Type: GrantFiled: October 21, 2015Date of Patent: September 11, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Mark E. Scott, David Guerin, Danielle Molinari, Sam Kattar, Peter Fuller, Christopher Dinsmore, Norman Kong, Yunfeng Bai, Jianmin Fu, Yumei Liu, Zhixiang Zheng
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Patent number: 10072026Abstract: The invention provides a crystalline form of the compound of formula: that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such crystalline form and methods of using such crystalline form in mammals suffering from inflammatory bowel diseases.Type: GrantFiled: June 23, 2017Date of Patent: September 11, 2018Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Xiaojun Huang, Venkat R. Thalladi
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Patent number: 10072027Abstract: What is described is a process for producing high-purity gadobutrol in a purity (according to HPLC) of more than 99.7 or 99.8 or 99.9% and the use for preparing a pharmaceutical formulation for parenteral administration. The process is carried out using specifically controlled crystallization conditions. The more recent developments in the field of the gadolinium-containing MR contrast agents (EP 0448191 B1, CA Patent 1341176, EP 0643705 B1, EP 0986548 B1, EP 0596586 B1) include the MRT contrast agent gadobutrol (Gadovist® 1.0) which has been approved for a relatively long time in Europe and more recently also in the USA under the name Gadavist®.Type: GrantFiled: April 17, 2012Date of Patent: September 11, 2018Assignee: BAYER INTELLECTUAL PROPERTY GMBHInventors: Johannes Platzek, Wilhelm Trentmann
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Patent number: 10072028Abstract: Provided are methods for site- and stereo-retentive cross-couplings with unactivated secondary boronic acids, which methods are particularly useful in building block-based approach for small molecule synthesis. Also provided is a method of forming an air-stable chiral secondary boronic acid.Type: GrantFiled: November 3, 2014Date of Patent: September 11, 2018Assignee: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, Pulin Wang, Ian Crouch
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Patent number: 10072029Abstract: The present disclosure relates to a novel crystalline form of a proteasome inhibitor, and to the processes for the preparation thereof. The novel crystalline form according to the disclosure may be used in the preparation of pharmaceutical compositions for the treatment of cancer.Type: GrantFiled: February 10, 2016Date of Patent: September 11, 2018Assignee: Millennium Pharmaceuticals, Inc.Inventors: Marianne Langston, Debra Mazaik, Eric Elliott, Anton Peterson, Patricia Andres, Jing Teng
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Patent number: 10072030Abstract: The present invention is directed to a mild, efficient, and general direct C(sp)-H bond silylation. Various embodiments includes methods, each method comprising or consisting essentially of contacting at least one organic substrate comprising a terminal alkynyl C—H bond, with a mixture of at least one organosilane and an alkali metal hydroxide, alkali metal alkoxide, or alkali metal hydride under conditions sufficient to form a silylated terminal alkynyl moiety. The methods are operable in the presence or substantially absence of transition-metal compounds. The systems associated with these methods are also disclosed.Type: GrantFiled: December 12, 2016Date of Patent: September 11, 2018Assignee: California Institute of TechnologyInventors: Anton Toutov, Kerry Betz, Brian M. Stoltz, Wenbo Liu, Robert H. Grubbs
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Patent number: 10072031Abstract: Systems and methods for mechanosynthesis including those that avoid the need for a bootstrap process, avoid the need to build tips via mechanosynthesis, avoid the need for charging tips with feedstock during a build sequence, avoid the need to dispose of reaction byproducts, reduce the design complexity of new tips, and reduce or avoid the need for multiple positional means or tip switching.Type: GrantFiled: May 12, 2016Date of Patent: September 11, 2018Assignee: CBN Nano Technologies, Inc.Inventors: Ralph C. Merkle, Robert A. Freitas, Jr., Jeremy Barton, Aru Hill, Michael Drew, Damian Allis, Tait Takatani
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Patent number: 10072032Abstract: The present invention relates to novel aminobisphosphonate compounds useful as antiwear and/or friction modifier additive components, lubricant additive compositions and lubricant compositions each comprising such compounds, and methods for making and using the same.Type: GrantFiled: September 15, 2017Date of Patent: September 11, 2018Assignee: Afton Chemical CorporationInventors: John Marshall Baker, Guillaume Carpentier
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Patent number: 10072033Abstract: The purpose of the present invention is to provide: a ligand that is useful in a catalytic organic synthetic reaction; a method for producing said ligand; and a metal complex that is useful as a catalyst in an organic synthetic reaction. The present invention provides a compound represented by general formula (1A), a method for producing said compound, and a metal complex including said compound as a ligand. (In the formula, H, N, P, S, L, R1, R2, R3, Q1, and Q2 have the meaning as defined in the Description.Type: GrantFiled: August 26, 2015Date of Patent: September 11, 2018Assignee: TAKASAGO INTERNATIONAL CORPORATIONInventors: Yuji Nakayama, Osamu Ogata
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Patent number: 10072034Abstract: There are provided compounds of formula I, wherein T, A, Q, Z, G, R4, R5a, R5b and n have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: GrantFiled: April 6, 2017Date of Patent: September 11, 2018Assignees: Respivert Limited, Topivert Pharma LimitedInventors: Matthew Colin Thor Fyfe, Stephen Malcolm Thom
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Patent number: 10072035Abstract: The present invention relates to a novel phenanthroline phosphonic acid compound and a pharmaceutical salt thereof, as well as an application of the compound and the pharmaceutical salt thereof as collagen prolyl hydroxylase inhibitors in the preparation of drugs for preventing or treating collagen prolyl-4-hydroxylase related disease.Type: GrantFiled: April 10, 2015Date of Patent: September 11, 2018Assignee: GUANGZHOU BERYL THERAPEUTICS, INCInventors: Yue Zhu, Yuzhen Liao, Li Zhang, Xu Bai
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Patent number: 10072036Abstract: The invention relates to an N-heterocyclic carbene complex of general formulas I to IV (I) (II) (III) (IV), according to which A1 stands for NR2 or PR2, A2 stands for CR2 R2?, NR2, PR2, 0 or S, A3 stands for N or P, and C stands for a carbene carbon atom, ring B is an unsubstituted or a mono or poly-substituted 5 to 7-membered ring, substituents R2 and R2? stand, inter alia, for a linear or branched C1-Cw-alkyl group and, if N and N each stand for NR2 or PR2, are the same or different, M in formulas I, II, III or IV stands for Cr, Mo or W, X 1 or X2 in formulas I to IV are the same or different and represent, inter alia, C1-C1s carboxylates and C1-C1s-alkoxides, Y is inter alia oxygen or sulphur, Z is inter alia a linear or branched C1-Cw-alkylenoxy group, and R 1 and R1? in formulas I to IV are, inter alia, an aliphatic or aromatic group.Type: GrantFiled: April 24, 2015Date of Patent: September 11, 2018Assignee: UNIVERSITÄT STUTTGARTInventors: Michael R. Buchmeiser, Suman Sen, Roman Schowner
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Patent number: 10072037Abstract: The method is for separation of lignin from original black liquor (BLIN) that has a first precipitation stage (PR) for precipitation of lignin by a first acidification using acidifier AC1, preferably using CO2, at alkaline conditions, then separating a lignin cake with subsequent suspension of the lignin cake in a strong acid in order to leach our metals from the lignin followed by dewatering and obtaining a clean lignin product LP. The process further is improved by intensified hydrolysis of lignin cake such that most of the carbohydrates are broken down to dissolvable monomers that could be separated from the lignin in the filtrate from a filtering stage subsequent to the hydrolysis. The improved hydrolysis could reduce as much as 90% of the carbohydrate content using a moderately increased temperature and increased charge of acidifier while avoiding any larger lignin yield losses.Type: GrantFiled: July 13, 2017Date of Patent: September 11, 2018Assignee: VALMET ABInventor: Panu Tikka
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Patent number: 10072038Abstract: According to the present invention, a crystal of ammonium N-acetylneuraminate anhydrate, and a process for producing a crystal of ammonium N-acetylneuraminate anhydrate, comprising adding or adding dropwise a solvent selected from the group consisting of alcohols and ketones to an aqueous N-acetylneuraminic acid solution containing an ammonium-containing compound and having a pH of 3.0 to 9.0 to precipitate a crystal of ammonium N-acetylneuraminate anhydrate, and collecting the crystal of ammonium N-acetylneuraminate anhydrate from the aqueous solution, can be provided.Type: GrantFiled: January 27, 2016Date of Patent: September 11, 2018Assignee: KYOWA HAKKO BIO CO., LTD.Inventor: Kazunari Fukumoto
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Patent number: 10072039Abstract: The present invention provides improved processes of preparing Fondaparinux sodium comprising converting a compound of formula ABCDE4 to Fondaparinux sodium at a reaction pH of no more than about 9.0. In some embodiments, the intermediates for the synthesis of Fondaparinux sodium, are also provided.Type: GrantFiled: July 25, 2013Date of Patent: September 11, 2018Assignee: ScinoPharm Taiwan, Ltd.Inventors: Lung-Huang Kuo, Shang-Hong Chen, Li-Ting Wang, Wen-Li Shih, Yuan-Xiu Liao
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Patent number: 10072040Abstract: The present invention pertains to derivatives of tylosin A. In particular, the present invention pertains to compounds having a structure of Formula (I). The present invention also pertains to compositions comprising derivatives of tylosin A and methods of treating or preventing conditions or disorders using such compounds and compositions.Type: GrantFiled: March 10, 2015Date of Patent: September 11, 2018Assignee: ABBVIE INC.Inventors: Thomas W. von Geldern, Dale J. Kempf, Kennan C. Marsh
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Patent number: 10072041Abstract: Method for preparing a peptide assembly of n fragments and n?1 amino acids bearing a thiol function, represented by the formula: A1-C1-A2-C2-A3- . . . -Ci?1-Ai- . . . -Cn?1-An??(I) in which A1, A2, A3, . . . Ai . . . , An are peptide fragments, C1, C2, C3 . . . Ci?1 . . . Cn?1 are amino acid residues bearing a thiol function, n is comprised between 3 and 50, and i is 2 to n, in which a peptide-thioester is prepared of formula: A1-SR (II) in which A1 is a peptide fragment and SR is an alkyl thioester residue, R being alkyl optionally substituted, starting from a bis(2-sulphanylethyl)amino peptide.Type: GrantFiled: February 15, 2012Date of Patent: September 11, 2018Assignees: Centre National de la Recherche Scientifique, Universite de Lille 1 Sciences et TechnologiesInventors: Oleg Melnyk, Nathalie Ollivier, Reda Mhidia, Julien Dheur
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Patent number: 10072042Abstract: Methods for conducting controlled grafting-from radical polymerizations from biomolecules under conditions that are biologically compatible are described. The methods provide biomolecule-polymer conjugates with highly controlled structures and narrow polydispersities under aqueous reaction conditions and biological temperatures. Biomolecules, such as proteins and nucleotides can be conjugated to polymers with high levels of control.Type: GrantFiled: December 14, 2016Date of Patent: September 11, 2018Assignee: CARNEGIE MELLON UNIVERSITYInventors: Krzysztof Matyjaszewski, Saadyah E. Averick, Antonina Simakova
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Patent number: 10072043Abstract: Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.Type: GrantFiled: December 18, 2015Date of Patent: September 11, 2018Assignee: Indiana University Research and Technology CorporationInventors: Zhong-Yin Zhang, Sheng Zhang
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Patent number: 10072044Abstract: The present application provides synthetic modified peptides of five to seven natural or non-natural amino acids as well as pharmaceutical compositions comprising them, for use in the treatment a disease or disorder presenting behavioral abnormalities associated with impairment of sensory gating function, depression or cognitive impairment, particularly schizophrenia and Alzheimer's disease.Type: GrantFiled: June 12, 2016Date of Patent: September 11, 2018Assignee: Yeda Research and Development Co. Ltd.Inventors: Michal Schwartz-Eisenbach, Matityahu Fridkin, Michal Cardon-Yaakov
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Patent number: 10072045Abstract: Novel antibacterial lipopeptides, pharmaceutical compositions, and methods for their preparation and use are described.Type: GrantFiled: February 6, 2018Date of Patent: September 11, 2018Assignee: RAMAPO PHARMACEUTICALS, INC.Inventor: Haiyin He
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Patent number: 10072046Abstract: A non-naturally occurring porcine reproductive and respiratory syndrome virus (PRRSV) is provided herein, and methods of making and using the non-naturally occurring PRRSV also are provided.Type: GrantFiled: March 25, 2015Date of Patent: September 11, 2018Assignees: NUtech Ventures, The Board of Trustees of the University of IllinoisInventors: Hiep Lai Xuan Vu, Fernando Osorio, William W. Laegreid, Asit K. Pattnaik, Fangrui Ma
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Patent number: 10072047Abstract: The present invention relates to methods and uses for screening anti-hepadnaviral substances, wherein the substances are screened for the capacity to inhibit covalently closed circular (ccc) DNA of a hepadnavirus, like hepatitis B virus. The methods and uses take advantage of cells comprising a nucleic sequence encoding a tagged hepadnavirus e antigen, like Hepatitis B virus e antigen (HBeAg). Furthermore, the present invention provides nucleic acid sequences encoding a tagged hepadnavirus e antigen and proteins encoded thereby. Also kits for use in the screening methods are provided.Type: GrantFiled: June 19, 2015Date of Patent: September 11, 2018Assignees: Drexel University, Baruch S. Blumberg Institute, Hoffmann-La Roche Inc.Inventors: Haitao Guo, Dawei Cai, Andrea Cuconati, Changhua Ji
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Patent number: 10072048Abstract: Provided are astexin-1, astexin-2 and astexin-3 lasso peptides, which are based on sequences identified in Asticaccaulis excentricus, and methods of making and using same. Astexin-1 is highly polar, in contrast to many lasso peptides that are primarily hydrophobic, and has modest antimicrobial activity against Caulobacter crescentus, a bacterium related to Asticaccaulis excentricus. The solution structure of astexin-1 was determined, revealing a unique topology that is stabilized by hydrogen bonding between segments of the peptide. Astexins-2 and -3 are intracellular lasso peptides.Type: GrantFiled: August 29, 2013Date of Patent: September 11, 2018Assignee: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: A. James Link, Mikhail O. Maksimov