Patents Issued in March 21, 2019
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Publication number: 20190084981Abstract: The present invention provides for compounds of formula (I) wherein Rx, Ry, Rx1, L1, G1, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).Type: ApplicationFiled: November 16, 2018Publication date: March 21, 2019Inventors: Yujia Dai, Steven D. Fidanze, Lisa Hasvold, James Holms, Dachun Liu, William McClellan, Keith McDaniel, Jasmina Marjanovic, George Sheppard, Le Wang
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Publication number: 20190084982Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: ApplicationFiled: November 16, 2018Publication date: March 21, 2019Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Publication number: 20190084983Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.Type: ApplicationFiled: March 24, 2017Publication date: March 21, 2019Applicant: The Trustees of Columbia University in the City of New YorkInventors: Andrew Kruegel, Dalibor Sames, Madalee G. Wulf, Jonathan A. Javitch
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Publication number: 20190084984Abstract: Embodiments of calcium channel agonists, as well as methods of making and using the calcium channel agonists, are disclosed. The disclosed calcium channel agonists and corresponding salt forms have a structure according to general formula I: wherein each bond depicted as “” is a single bond or a double bond as needed to satisfy valence requirements; Z1, Z2, Z3, Z4, and Z5 independently are nitrogen or carbon; R1 and R3 are alkyl; R2 is alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; and R4 is alkyl or hydroxyalkyl.Type: ApplicationFiled: November 16, 2018Publication date: March 21, 2019Applicant: University of Pittsburgh - Of the Commonwealth System of Higher EducationInventors: Peter Wipf, Stephen D. Meriney, Mary Liang
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Publication number: 20190084985Abstract: A compound, or a pharmaceutically acceptable salt thereof, having a chemical structure of formula (I) or formula (II), and methods of using these compounds to treat cancer in an individual.Type: ApplicationFiled: November 1, 2016Publication date: March 21, 2019Inventors: Philip REIGAN, Christopher MATHESON
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Publication number: 20190084986Abstract: Provided are a heterocyclic compound represented by Formula 1 and an organic electroluminescence device and an organic electroluminescence display device including the heterocyclic compound represented by Formula 1 in an emission layer. In Formula 1, A is represented by Formula 2, D1 is represented by Formula 3, and D2 is represented by Formula 4.Type: ApplicationFiled: April 25, 2018Publication date: March 21, 2019Inventors: Jimyoung Ye, Myeongsuk Kim, Seulong Kim, Byeongwook Yoo, Jaehoon Hwang, Soo-byung Ko, Jihwan Yoon
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Publication number: 20190084987Abstract: Compositions for the inhibition of SUV39H1 methyltransferase activity and methods of use thereof are provided. The disclosed compositions may be used for treating certain types of cancer, inducing apoptosis in a cancer cell, increasing cell sensitivity to FasL-induced apoptosis, and overcoming cancer cell resistance to apoptosis and/or certain types of cancer immunotherapy.Type: ApplicationFiled: September 18, 2018Publication date: March 21, 2019Inventors: Chunwan Lu, Iryna Lebedyeva, Kebin Liu
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Publication number: 20190084988Abstract: Described are N-(6-(6,7-dihydro-5H-pyrrolo[1,2-a]imidazol-2-yl)-2,3-dihydro-1H-inden-1-yl)benzamide and acetamide-containing compounds that inhibit WDR5 and associated protein-protein interactions, pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating disorders and conditions in a subject.Type: ApplicationFiled: September 19, 2018Publication date: March 21, 2019Inventors: Stephen W. Fesik, Shaun R. Stauffer, James M. Salovich, William P. Tansey, Feng Wang, Jason Phan, Edward T. Olejniczak
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Publication number: 20190084989Abstract: Described herein, inter alia, are compositions and methods of using the same for modulating the activity of Ire1.Type: ApplicationFiled: October 2, 2018Publication date: March 21, 2019Inventors: Bradley J. Backes, Dustin J. Maly, Scott A. Oakes, Feroz R. Papa, Gayani Perera, Likun Wang
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Publication number: 20190084990Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: ApplicationFiled: October 25, 2018Publication date: March 21, 2019Applicants: Dana-Farber Cancer Institute, Inc., The Scripps Research InstituteInventors: Nathanael S. Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang, Amy Wojciechowski
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Publication number: 20190084991Abstract: The present application relates to novel compounds of formula (I) to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.Type: ApplicationFiled: November 20, 2018Publication date: March 21, 2019Applicant: ASTRAZENECA ABInventors: Johan Olof BRODDEFALK, Hans Fredrik EMTENÂS, Kenneth Lars GRANBERG, Malin Anita LEMURELL, Daniel Tor PETTERSEN, Alleyn Thomas PLOWRIGHT, Lars Johan Andreas ULANDER
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Publication number: 20190084992Abstract: Provided are a compound including nitrogen, represented by Formula 1, and an organic electroluminescence device including the same. In Formula 1, A1 to A10 are each independently CR3 or N. The organic electroluminescence device may include a first electrode, a second electrode which is opposite to the first electrode, and a plurality of organic layers disposed between the first electrode and the second electrode, wherein the plurality of organic layers include an emission layer, and at least one organic layer among the organic layers includes the compound including nitrogen.Type: ApplicationFiled: April 25, 2018Publication date: March 21, 2019Inventor: Naoya Sakamoto
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Publication number: 20190084993Abstract: The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.Type: ApplicationFiled: April 13, 2018Publication date: March 21, 2019Applicant: The University of LiverpoolInventors: Martin Leuwer, Paul M. O'Neill, Neil Berry, Chandrakala Pidathala
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Publication number: 20190084994Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: X-A-Y-L-R??(I) which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: November 19, 2018Publication date: March 21, 2019Inventors: Yao-Ling Qiu, Xuri Gao, Wei Li, Hui Cao, Meizhong Jin, Jorden Kass, Xiaowen Peng, Yat Sun Or
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Publication number: 20190084995Abstract: Provided herein is a compound of formula (I): wherein each R is independently selected from the group consisting of C1-8 alkyl, C1-8 heteroalkyl having 1-4 heteroatoms independently selected from N, O, and S, C3-6 cycloalkyl, 3-10 membered heterocycloalkyl having 1-4 heteroatoms independently selected from N, O, and S, C6-10 aryl, and 5-10 membered heteroaryl having 1-4 heteroatoms independently selected from N, O, and S; each X is independently selected from OH, PAr2, P(O)Ar2, OPAr2, C3-6 cycloalkyl, 3-10 membered heterocycloalkyl having 1-4 heteroatoms independently selected from N, O, and S or each X together form O2PNR?2; Ar is C6-10aryl; and each R? is independently selected from hydrogen and C1-8 alkyl. Also provided are methods of making and using the compound of formula (I).Type: ApplicationFiled: September 18, 2018Publication date: March 21, 2019Inventors: Pavel Nagorny, Siyuan Sun, Alonso Arguelles
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Publication number: 20190084996Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.Type: ApplicationFiled: September 19, 2018Publication date: March 21, 2019Inventors: Vasu Jammalamadaka, Kimberly Ann Tipton, Sanjeev Satyal, Hoyoung Huh
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Publication number: 20190084997Abstract: This application relates to derivatives of Formula I: and pharmaceutically acceptable salts thereof, which are inhibitors of PI3K, and compositions and methods of treatment related thereto.Type: ApplicationFiled: August 24, 2018Publication date: March 21, 2019Inventors: Yun-Long Li, Andrew P. Combs
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Publication number: 20190084998Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1,2,3, or 4, Ack1, Ack2, Abl, DCAMKL1, ABL1, Abl mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: November 20, 2018Publication date: March 21, 2019Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. Gray, David Waller, Hwan Guen Choi, Jinhua Wang, Xianming Deng
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Publication number: 20190084999Abstract: Disclosed herein are antimicrobial compounds, compositions, pharmaceutical compositions, and the use and preparation thereof. Some embodiments relate to cyclic boronic acid ester derivatives and their use as therapeutic agents.Type: ApplicationFiled: November 13, 2015Publication date: March 21, 2019Inventors: Scott Hecker, Raja K. Reddy, Tomasz Glink
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Publication number: 20190085000Abstract: The present invention relates to a siloxane monomer used in the production of a silicone hydrogel lens, a composition for the preparation of a lens containing the same, and a silicone hydrogel lens prepared from the same, wherein the silicone hydrogel lens according to the present invention has a feature of easy release from a component of a mold.Type: ApplicationFiled: February 17, 2017Publication date: March 21, 2019Inventors: Sang IL HYUN, Soo Chang LEE, Kyung Hee OH, Dong Hun SHIN
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Publication number: 20190085001Abstract: An aromatic compound which improves emission efficiency and an organic electroluminescence device including the same are provided. The organic electroluminescence device includes: a first electrode; a second electrode opposite to the first electrode; and a plurality of organic layers between the first electrode and the second electrode, where at least one organic layer among the plurality of organic layers includes the aromatic compound. The aromatic compound is represented by Formula 1 below.Type: ApplicationFiled: April 20, 2018Publication date: March 21, 2019Inventors: Heechoon Ahn, Soo-byung Ko, Mieun Jun, Sungbum Kim, Mina Jeon, Youngkook Kim, Seokhwan Hwang
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Publication number: 20190085002Abstract: Provided are an organosilicon compound capable of improving the storage stability of a composition (curability after long-term storage); and a method for producing the same. The organosilicon compound has, in one molecule, at least one carboxylic acid ester group represented by the following general formula (1) and at least one hydrolyzable silyl group represented by the following general formula (2): —OC(?O)CH2R1??(1) wherein R1 represents a hydrogen atom or a methyl group; —SiR23-nYn??(2) wherein R2 represents a substituted or unsubstituted monovalent hydrocarbon group having 1 to 12 carbon atoms, Y represents a hydrolyzable group, and n represents an integer satisfying 1?n?3.Type: ApplicationFiled: March 8, 2017Publication date: March 21, 2019Applicant: Shin-Etsu Chemical Co., Ltd.Inventors: Taiki KATAYAMA, Isao IWASAKI, Takafumi SAKAMOTO
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Publication number: 20190085003Abstract: Disclosed are a silane compound of the general formula (1) described below, as well as a rubber composition including the same, and a tire. A silane compound of the general formula (1) is useful because of its ability to provide a silane compound comprising: a reactive functional group having a high reactivity with an organic polymer material such as rubber, and having a low polarity; and a hydrolyzable group having a high reactivity with an inorganic material such as silica or glass. The symbols in the formula are defined in the specification.Type: ApplicationFiled: March 13, 2017Publication date: March 21, 2019Applicant: JXTG NIPPON OIL & ENERGY CORPORATIONInventors: Keisuke CHINO, Hiroaki SUZUKI
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Publication number: 20190085004Abstract: A method for producing a fluorine-containing compound represented by General formula (1), wherein X represents a halogen atom or an alkoxy group, R1 represents a hydrogen atom or a linear, branched, or cyclic alkyl group having 1 to 10 carbon atoms, Rf1 and Rf2 are each independently a fluorinated alkoxy group, and n represents an integer of 0 or more.Type: ApplicationFiled: November 16, 2018Publication date: March 21, 2019Applicants: Kanagawa University, Nikon CorporationInventors: Kazuo Yamaguchi, Yusuke Kawakami
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Publication number: 20190085005Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a phosphonate (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.Type: ApplicationFiled: October 16, 2018Publication date: March 21, 2019Applicant: Achillion Pharmaceuticals, Inc.Inventors: Jason Allan Wiles, Akihiro Hashimoto, Venkat Rao Gadhachanda, Godwin Pais, Qiuping wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash Phadke
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Publication number: 20190085006Abstract: The present invention relates to a method for producing one or more low molecular weight aromatic lignin-derived compounds. The method preferably comprises providing lignocellulosic material, subjecting the lignocellulosic material to a pulping process, separating pulp to provide a substantially pulp-free process stream comprising a modified lignin-derived component, isolating the modified lignin-derived component, subjecting the isolated modified lignin-derived component to a decomposition step comprising oxidative cracking (cracking and oxidizing) or reducing under the influence of a catalyst or electro-oxidation, and subjecting the resulting products to an isolation step, to provide a low molecular weight aromatic lignin-derived compound. Said compound may be further modified, e.g. by annulation. The inventive method preferably comprises further oxidizing said compound to a redox active compound.Type: ApplicationFiled: April 7, 2017Publication date: March 21, 2019Applicant: CMBLU PROJEKTAGInventors: Nastaran KRAWCZYK, Alexander MOELLER, Peter GEIGLE
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Publication number: 20190085007Abstract: The invention relates to phenoxy derivatives with glycosidically bound sugar moieties, pharmaceutical compositions containing such compounds, uses of such compounds and compositions, and methods of making such compounds and pharmaceutical compositions.Type: ApplicationFiled: April 12, 2018Publication date: March 21, 2019Inventors: Hans-Michael THIEDE, Wolfgang KEHR
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Publication number: 20190085008Abstract: Provided herein are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, and compositions comprising such compounds that are useful for increasing the amount of NAD+ in cells. Also disclosed are methods of using the disclosed compounds and compositions for treating mitochondrial-related diseases or disorders.Type: ApplicationFiled: November 2, 2016Publication date: March 21, 2019Applicant: Mitobridge, Inc.Inventors: Arthur Kluge, Nan Ji
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Publication number: 20190085009Abstract: The invention relates to crystalline forms of a ?-nicotinamide mononucleotide, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for nutraceutical, veterinary, and agriculturally-relevant uses.Type: ApplicationFiled: September 17, 2018Publication date: March 21, 2019Inventors: Andrew Carr, Philippe Fernandes, David J. Livingston
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Publication number: 20190085010Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.Type: ApplicationFiled: October 22, 2018Publication date: March 21, 2019Inventors: Genadiy KALAYANOV, Staffan TORSSELL, Horst WAHLING
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Publication number: 20190085011Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.Type: ApplicationFiled: November 28, 2018Publication date: March 21, 2019Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
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Publication number: 20190085012Abstract: Described are 5?-cyclo-phosphonate modified nucleotides, and oligonucleotides, such as interference (RNAi) agents, containing 5?-cyclo-phosphonate modified nucleotides. The RNAi agents having either double-stranded or single-stranded oligonucleotides described herein comprising 5?cyclo-phosphonate modified nucleotides are useful in modulating gene expression as well as therapeutic, diagnostic, target validation, and genomic discovery applications. The RNAi agents and single-stranded antisense oligonucleotides comprising 5?-cyclo-phosphonate modified nucleotides are useful in the treatment of diseases or conditions that respond to inhibition of gene expression or activity in a cell, tissue, or organism.Type: ApplicationFiled: December 3, 2018Publication date: March 21, 2019Inventors: Zhen Li, Tao Pei, Michael Lawler
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Publication number: 20190085013Abstract: This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.Type: ApplicationFiled: March 7, 2017Publication date: March 21, 2019Inventors: George PAINTER, Gregory R. BLUEMLING, Abel DE LA ROSA, Dennis C. LIOTTA, Damien KUIPER
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Publication number: 20190085014Abstract: This invention provides methods for attaching a nucleic acid to a solid surface and for sequencing nucleic acid by detecting the identity of each nucleotide analogue after the nucleotide analogue is incorporated into a growing strand of DNA in a polymerase reaction. The invention also provides nucleotide analogues which comprise unique labels attached to the nucleotide analogue through a cleavable linker, and a cleavable chemical group to cap the —OH group at the 3?-position of the deoxyribose.Type: ApplicationFiled: October 1, 2018Publication date: March 21, 2019Applicant: The Trustees of Columbia University in the City of New YorkInventors: Jingyue Ju, Zengmin Li, John Robert Edwards, Yasuhiro Itagaki
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Publication number: 20190085015Abstract: This invention provides methods for attaching a nucleic acid to a solid surface and for sequencing nucleic acid by detecting the identity of each nucleotide analogue after the nucleotide analogue is incorporated into a growing strand of DNA in a polymerase reaction. The invention also provides nucleotide analogues which comprise unique labels attached to the nucleotide analogue through a cleavable linker, and a cleavable chemical group to cap the —OH group at the 3?-position of the deoxyribose.Type: ApplicationFiled: October 2, 2018Publication date: March 21, 2019Applicant: The Trustees of Columbia University in the City of New YorkInventors: Jingyue Ju, Zengmin Li, John Robert Edwards, Yasuhiro Itagaki
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Publication number: 20190085016Abstract: This invention provides methods for attaching a nucleic acid to a solid surface and for sequencing nucleic acid by detecting the identity of each nucleotide analogue after the nucleotide analogue is incorporated into a growing strand of DNA in a polymerase reaction. The invention also provides nucleotide analogues which comprise unique labels attached to the nucleotide analogue through a cleavable linker, and a cleavable chemical group to cap the —OH group at the 3?-position of the deoxyribose.Type: ApplicationFiled: November 26, 2018Publication date: March 21, 2019Applicant: The Trustees of Columbia University in the City of New YorkInventors: Jingyue Ju, Zengmin Li, John Robert Edwards, Yasuhiro Itagaki
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Publication number: 20190085017Abstract: The present invention relates to certain purines of the following formulae, which act as topoisomerase II catalytic inhibitors: wherein: J is independently: —H or —NRN1RN2; X is independently: —O—, or —S—; Q is independently: a covalent bond, C1-7alkylene, C2-7alkenylene, C2-7alkynylene, C3-7cycloalkylene, C3-7cycloalkenylene, or C3-7cycloalkynylene; T is independently: a group A1 or a group A2; A1 is independently: C6-14carboaryl, C4-14heteroaryl, C3-12carbocyclic, or C3-12heterocyclic; and is independently unsubstituted or substituted; A2 is independently: —H, —CN, —OH, or —O(C?O)—C1-7alkyl; R is independently —H or a nitrogen ring substituent: R8 is independently —H or a ring substituent; either: each of RN1 and RN2 is independently —H or a nitrogen substituent; or: RN1 and RN2 taken together with the nitrogen atom to which they are attached form a ring having from 3 to 7 ring atoms; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugsType: ApplicationFiled: November 16, 2018Publication date: March 21, 2019Inventors: Lars Hollund Jensen, Maxwell Sehested
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Publication number: 20190085018Abstract: The invention provides a method of preparing a lyophilized pharmaceutical composition containing a compound described herein or a pharmaceutically-acceptable salt thereof. The process comprises dissolving the compound in a solvent comprising dimethylsulfoxide and optionally one or more co-solvents to form a solution, and then removing the solvent and any co-solvents by a freeze-drying process. Also provided by the invention are lyophilized pharmaceutical compositions and their use in medicine and in particular in the treatment of cancer.Type: ApplicationFiled: August 2, 2018Publication date: March 21, 2019Inventors: Rajashree JOSHI-HANGAL, Nipun DAVAR, Stephen R. PRIEBE
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Publication number: 20190085019Abstract: A method of forming a probe, wherein the method includes converting cholenic acid into a compound with a terminal alkyne group, wherein the converting the cholenic acid comprises using a sequence, wherein the sequence comprises synthesizing a THP-protection group, LiAlH4 reduction, Dess-Martin oxidation, and Seyferth-Gilbert-Bestmann homologation.Type: ApplicationFiled: November 20, 2018Publication date: March 21, 2019Applicant: Purdue Research FoundationInventor: Mingji Dai
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Publication number: 20190085020Abstract: A multifunctional chemical agents comprising functional agents Fn1, Fn2 and linkers, for the linchpin directed (LDM), protein directed (PDPM) modifications of proteins, and Fn1 accelerated kinetic labeling by Fn2.Type: ApplicationFiled: November 17, 2016Publication date: March 21, 2019Applicants: Department of Biotechnology, Indian Institute of Science Education and ResearchInventors: Vishal RAI, Srinivasa Rao ADUSUMALLI
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Publication number: 20190085021Abstract: The invention provides for the removal of a large fraction of contaminants from protein preparations while maintaining a high level of recovery using tentacle anion exchange matrix chromatography medium. Using the methods of the invention, leached affinity chromatography contaminants can be removed from recombinant protein preparations.Type: ApplicationFiled: July 23, 2018Publication date: March 21, 2019Applicant: AMGEN INC.Inventors: Samuel Ray TREJO, Robert Perry BRAKE
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Publication number: 20190085022Abstract: Disclosed herein are peptoids and related compounds, including peptoid affinity ligands, and hybrid peptoids, for binding and/or purifying immunoglobulins, immunoglobulin fragments or immunoglobulin fusion proteins thereof. Methods of making peptoid affinity ligands and using the same to bind, purify and/or isolate immunoglobulins and related compounds are also disclosed. Such peptoid affinity ligands comprise a peptoid compound consisting of sequentially coupled peptoid residues forming a peptoid backbone, with one or more functional groups appended to a Nitrogen of the peptoid residues of the peptoid backbone configured to provide the desired binding affinity. The peptoids can further comprise a peptoid backbone with at least one functional group coupled to an alpha carbon (C) of a peptide bond in the peptoid backbone thereby forming a hybrid peptoid.Type: ApplicationFiled: March 9, 2017Publication date: March 21, 2019Inventors: Andrew J. Murphy, Tee Bordelon, Michael Crapanzano
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Publication number: 20190085023Abstract: 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: ApplicationFiled: March 10, 2017Publication date: March 21, 2019Applicant: KYOWA HAKKO BIO CO., LTD.Inventors: Kazunari FUKUMOTO, Maya IGUCHI, Hiroshi NAGANO
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Publication number: 20190085024Abstract: The disclosure provides compounds comprising a ?-ketoamide linkage that is terminated on each end by an amino acid, such as compounds of Formula (I), wherein RA-RC are defined herein. Also provided are compositions containing these compounds and methods of inhibiting calpain activity, treating a calpain-mediated disorder, inhibiting cathepsin-B, cathepsin-L, cathepsin-S, or cathepsin-L activity, and methods of treating a cathepsin-B, cathepsin-L, cathepsin-S, or cathepsin-L mediated disorder using these compounds and compositions.Type: ApplicationFiled: September 17, 2018Publication date: March 21, 2019Inventors: Doron Greenbaum, Russ Addis, Janet Gaboury, Swapnil Kulkami, Nataline Meinhardt
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Publication number: 20190085025Abstract: This invention provides novel compounds and methods for promoting cell survival and/or plasticity, especially in neuronal cells, by targeting the microtubule End Binding (EB) proteins and other associated proteins (e.g., drebrin). Methods for identifying potential modulators of cell death/plasticity are also described.Type: ApplicationFiled: October 16, 2018Publication date: March 21, 2019Inventors: Illana Gozes, Saar Oz, Jacqueline Woang Cheing Tiong
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Publication number: 20190085026Abstract: The present invention relates to an improved process for the preparation of carfilzomib or a pharmaceutically acceptable salt thereof. The present invention also relates to a process for the preparation of amorphous form of carfilzomib.Type: ApplicationFiled: May 21, 2016Publication date: March 21, 2019Inventors: Sanjay Kumar Dehury, Nagaraju Mekala, Jahangeer Baba Shaik, Srinivasa Rao Buddepu, Lakshmi Kanth Kola, Venkata Sunil Kumar Indukuri, Seeta Rama Anjaneyulu Gorantla, Satyanarayana Chava
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Publication number: 20190085027Abstract: Provided is a cyclic peptide derivative which is derived from Paecilomyces tenuipes having an astrocyte proliferative activity, or a salt thereof.Type: ApplicationFiled: September 27, 2018Publication date: March 21, 2019Applicants: NATIONAL UNIVERSITY CORPORATION, IWATE UNIVERSITY, OSAKA CITY UNIVERSITY, IWATE MEDICAL UNIVERSITY EDUCATIONAL FOUNDATION, LOTTE CO., LTD.Inventors: Koichi SUZUKI, Shinichi ISHIGURO, Mayumi KARIMAZAWA, Makiko EBATA, Piyamas SILLAPAKONG, Takashi HIRAGA, Masaaki TSUSHIMA, Tetsuro SHINADA, Eiji NISHIMURA, Yasuo TERAYAMA, Hideyuki YASUDA
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Publication number: 20190085028Abstract: The invention provides a series of peptides with N-methyl-D-aspartate (NMDA) receptor modulating activity. Specifically it contains two synthetic peptides acting as ion inflow antagonists through the NMDA receptor with specificity GluN2B and GluN2A NMDA receptor subunits and a peptide having agonist activity regarding the NMDA receptor in rat hippocampal neuron cultures.Type: ApplicationFiled: December 22, 2016Publication date: March 21, 2019Inventors: Edgar Antonio Reyes Montaño, Edwin Alfredo Reyes Guzmán, Nohora Angélica Vega Castro
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Publication number: 20190085029Abstract: The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject a specific CDK5 peptide inhibitor and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 31, 2018Publication date: March 21, 2019Applicant: Massachusetts Institute of TechnologyInventors: Li-Huei Tsai, Jinsoo Seo
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Publication number: 20190085030Abstract: The present invention relates to novel D-enantiomeric A-beta-oligomer-binding peptides, homologs, fragments, parts and polymers thereof and use thereof.Type: ApplicationFiled: November 27, 2018Publication date: March 21, 2019Inventors: Dieter Willbold, Susanne Aileen Funke, Oleksander Brener, Luitgard Nagel-Steger, Dirk Bartnik, Antonia Nicole Klein