Patents Issued in June 20, 2019
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Publication number: 20190185479Abstract: The present invention provides: a novel use of a specific bicyclic nitrogen-containing heterocyclic compound as a PDE7 inhibitor; a novel bicyclic nitrogen-containing heterocyclic compound having a PDE7 inhibitory effect, a method for producing the compound, a use of the compound, and a pharmaceutical composition containing the PDE7 inhibitor or the compound; and others. More specifically, the present invention provides a PDE7 inhibitor containing the compound represented by the formula (I): [wherein the symbols have the same meanings as those described in the description] or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: August 25, 2017Publication date: June 20, 2019Applicants: MITSUBISHI TANABE PHARMA CORPORATION, UBE INDUSTRIES, LTD.Inventors: Tatsuo NAKAJIMA, Norimitsu HAYASHI, Kouhei ISHIZAWA, Yasunori TSUZAKI, Ryo IWAMURA, Kazunari TSUBOIKE
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Publication number: 20190185480Abstract: The present invention relates to organic semiconducting compounds of formula (I) wherein X1 is C, Si or Ge; X2 is 0, S or Se; and X3 is N or P as well as to organic electronic devices comprising such organic semiconducting compounds.Type: ApplicationFiled: August 8, 2017Publication date: June 20, 2019Applicant: Merck Patent GmbHInventors: Daniel BECKER, Andreas TAUGERBECK, Martin SCHRAUB
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Publication number: 20190185481Abstract: Embodiments of the present disclosure provide compounds derived by Troger's amine as shown below, microporous structures, membranes, methods of making said compounds, structures, and membranes, methods of use for gas separation, and the like (Formula A1).Type: ApplicationFiled: June 19, 2017Publication date: June 20, 2019Inventors: Xiaohua MA, Ingo PINNAU
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Publication number: 20190185482Abstract: The present invention relates to polymorphic forms of marizomib (e.g., Morphic Form I). The morphic forms can be used alone and in pharmaceutical compositions for the treatment of disease.Type: ApplicationFiled: August 18, 2017Publication date: June 20, 2019Inventor: Robert MANSFIELD
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Publication number: 20190185483Abstract: Compounds of formula (II) or a pharmaceutically acceptable salt or solvate thereof, the medical uses thereof for diseases or medical conditions where the inhibition of the voltage-gated potassium channel Kv1.3 is beneficial, and methods for their preparation.Type: ApplicationFiled: February 13, 2019Publication date: June 20, 2019Applicant: 4SC AGInventors: Stefan TASLER, Ilga KRIMMELBEIN, Juergen KRAUS, Mirko ZAJA
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Publication number: 20190185484Abstract: Provided herein are compounds of Formula (A), (B), (C), (D) and (E), pharmaceutically acceptable salts, quaternary amine salts, and N-oxides thereof, and pharmaceutical compositions thereof. Compounds of Formula (A), (B), (C), (D), and (E) are contemplated useful as therapeutics for treating a wide variety of conditions, e.g., including but not limited to, conditions associated with angiogenesis and with CDK8 and/or CDK19 kinase activity. Further provided are methods of inhibiting CDK8 and/or CDK19 kinase activity, methods of modulating the ?-catenin pathway, methods of modulating STAT 1 activity, methods of modulating the TGF?/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using a compound of Formula (A), (B), (C), (D), or (E). Further provided are CDK8 and CDK19 point mutants and methods of use thereof.Type: ApplicationFiled: March 5, 2019Publication date: June 20, 2019Applicant: President and Fellows of Harvard CollegeInventors: Matthew D. Shair, Juergen Ramharter, Henry Efrem Pelish, Brian Bor-Jen Liau, Jae Young Ahn
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Publication number: 20190185485Abstract: Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.14,7.011,15,016,21.020,24.030,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid (Formula I) and enantiomers and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions of 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.14,7.011,15.016,21.020,24.030,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid, and enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer with such compounds and compositions.Type: ApplicationFiled: December 18, 2018Publication date: June 20, 2019Inventors: Alexander HIRD, Matthew BELMONTE, Wenzhan YANG, Paul SECRIST, Daniel ROBBINS, Steven KAZMIRSKI, Dedong WU, Bo PENG, Jeffrey JOHANNES, Michelle LAMB, Qing YE, Xiaolan ZHENG
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Publication number: 20190185486Abstract: The present invention relates to novel Chromane-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A?, R2 R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising a Chromane-Substituted Tetracyclic Compound, and methods of using the Chromane-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: August 14, 2017Publication date: June 20, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: Wensheng Yu, Joseph A. Kozlowski, Ling Tong, Craig A. Cobum, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang
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Publication number: 20190185487Abstract: A compound of chemical formula I: or chemical formula II: or a pharmaceutical acceptable salt thereof is disclosed. R1, R2, R3, and R4 are independently H, halogen, nitro, hydroxyl, cyano, benzyloxy, C1-C8 straight or branched alkyl, C1-C8 straight or branched haloalkyl, C1-C8 straight or branched alkoxy.Type: ApplicationFiled: October 23, 2018Publication date: June 20, 2019Applicant: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Chengyuan LIANG, Lei TIAN, Nan QIN, Juan XIA, Shaomeng PEI
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Publication number: 20190185488Abstract: A compound of chemical formula I or a pharmaceutical acceptable salt thereof is disclosed. R1 is OH or OAc; X is C or N; and R2 is H, alkyl, alkoxy, benzyloxy, haloalkyl, OH, CN, NO2, or halogen, provided that when X is N, R2 is nil.Type: ApplicationFiled: October 23, 2018Publication date: June 20, 2019Applicant: SHAANXI UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Chengyuan LIANG, Lei TIAN, Nan QIN, Juan XIA, Shaomeng PEI
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Publication number: 20190185489Abstract: The present invention provides macrocycles of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.Type: ApplicationFiled: December 12, 2018Publication date: June 20, 2019Inventors: Karsten Juhl, Mikkel Jessing, Morten Langgård, Paulo Jorge Vieira Vital, Jan Kehler, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson, Mauro Marigo
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Publication number: 20190185490Abstract: Described herein are complexes comprising a cationic antibacterial agent and a metal salt; oral care compositions comprising same; along with methods of making and using these complexes and compositions.Type: ApplicationFiled: December 11, 2018Publication date: June 20, 2019Applicant: Colgate-Palmolive CompanyInventors: Viktor DUBOVOY, Long PAN, Ravi SUBRAMANYAM
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Publication number: 20190185491Abstract: Embodiments of the present disclosure describe compositions comprising a molecular building block (MBB) having the formula [RE6(?3-OH)8(O2C—)6N4C—)6] or [RE6(?3-OH)8(O2C—)12], wherein RE is a rare earth metal ion. Embodiments of the present disclosure further describe methods of making a metal-organic framework (MOF) composition comprising contacting one or more molecular building blocks (MBBs) with one or more bidentate ligands, wherein the MBBs have the formula [RE6(?3-OH)8(O2C—)6N4C—)6] or [RE6(?3-OH)8(O2C—)12], wherein RE is a rare earth metal ion.Type: ApplicationFiled: February 20, 2019Publication date: June 20, 2019Inventors: Mohamed EDDAOUDI, Dong-Xu Dong-Xu, Amy J. CAIRNS, Youssef BELMABKHOUT
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Publication number: 20190185492Abstract: The invention provides novel ionic covalent organic frameworks comprising stable tetra-coordinated borate linkages. The invention further provides methods of making novel ionic covalent organic frameworks comprising tetra-coordinated borate linkages. The invention also provides compositions comprising novel ionic covalent organic frameworks.Type: ApplicationFiled: December 20, 2017Publication date: June 20, 2019Inventors: Shun Wan, Wei Zhang
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Publication number: 20190185493Abstract: Compounds, pharmaceutical formulations, and methods of treating bacterial infections are disclosed.Type: ApplicationFiled: February 27, 2017Publication date: June 20, 2019Inventors: Xianfeng Li, Christopher S. Lunde, Robert T. Jacobs, Yasheen Zhou
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Publication number: 20190185494Abstract: The present invention relates to a method for releasing an unsaturated aldehyde or ketone represented by the general formula (2) by irradiating the compound represented by the general formula (1) with light, in which the compound represented by the general formula (1) is used as a flavor or fragrance precursor:Type: ApplicationFiled: August 1, 2017Publication date: June 20, 2019Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventors: Shinya YAMADA, Tadahide HATAKEYAMA, Hideki NARA, Takahiro ISHIKAWA
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Publication number: 20190185495Abstract: This invention is related to a method for the preparation of halide perovskite or perovskite-related materials on a substrate and to optoelectronic devices and photovoltaic cells comprising the perovskites prepared by the methods of this invention The method for the preparation of the perovskite includes a direct conversion of elemental metal or metal alloy to halide perovskite or perovskite-related materials.Type: ApplicationFiled: May 8, 2017Publication date: June 20, 2019Applicant: YE DA RESEARCH AND DEVELOPMENT CO. LTD.Inventors: David CAHEN, Gary MODES, Yevgeny RAKITA, Nir KEDEM
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Publication number: 20190185496Abstract: Provided are crystals of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate, compositions comprising the same, and methods of making and using such crystals.Type: ApplicationFiled: May 12, 2017Publication date: June 20, 2019Applicant: AEROMICS, INC.Inventors: Paul Robert MCGUIRK, Robert ZAMBONI, Melanie BEVILL, Stephan PARENT
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Publication number: 20190185497Abstract: A pinene-based flame retardant compound, a process for forming a flame retardant polymer, and an article of manufacture comprising a material that contains a pinene-based flame retardant polymer are disclosed. The pinene-based flame retardant compound includes a pinene derivative core and at least one flame retardant substituent having a phosphorus-based moiety. The process for forming the flame retardant polymer includes obtaining pinene, forming a derivative of pinene, obtaining a phosphorus-based compound, reacting the phosphorus-based compound and the pinene derivative to form a pinene-based flame retardant compound, and incorporating the pinene-based flame retardant compound into a polymer to form the pinene-based flame retardant polymer.Type: ApplicationFiled: December 14, 2017Publication date: June 20, 2019Inventors: Brandon M. Kobilka, Joseph Kuczynski, Jacob T. Porter, Jason T. Wertz
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Publication number: 20190185498Abstract: 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 an aryl, heteroaryl or heterocycle (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: February 14, 2019Publication date: June 20, 2019Applicant: Achillion Pharmaceuticals, Inc.Inventors: Jason Allan Wiles, Venkat Rao Gadhachanda, Qiuping Wang, Godwin Pais, Akihiro Hashimoto, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash S. Phadke
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Publication number: 20190185499Abstract: Disclosed herein are stannous-ascorbyl phosphate and stannic-asorbyl phosphate complexes, oral care compositions stannous-ascorbyl phosphate and stannic-asorbyl phosphate complexes, and methods of making and using the same.Type: ApplicationFiled: December 11, 2018Publication date: June 20, 2019Applicant: Colgate-Palmolive CompanyInventors: Zhigang HAO, Chi-Yuan CHENG, Long PAN, Ravi SUBRAMANYAM
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Publication number: 20190185500Abstract: A metal complex represented by formula (1) is provided. In formula (1), X represents a nitrogen atom or a group represented by ?C(RX)—; R1 represents an alkyl group having 4 or more carbon atoms; R2 represents an alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, aryloxy, monovalent heterocyclic, or substituted amino group or a halogen atom; rings A and B each independently represent an aromatic hydrocarbon ring or an aromatic heterocyclic ring; M represents a rhodium, palladium, iridium, or platinum atom; n1 represents an integer of 1 or more, n2 represents an integer of 0 or more, and n1+n2 is 2 or 3; A1-G1-A2 represents an anionic bidentate ligand; A1 and A2 each independently represent a carbon atom, an oxygen atom, or a nitrogen atom; and G1 represents a single bond or an atomic group constituting a bidentate ligand together with A1 and A2.Type: ApplicationFiled: March 30, 2017Publication date: June 20, 2019Inventors: Mayu YOSHIOKA, Taichi ABE, Toshiaki SASADA, Kohei ASADA, Nobuhiko AKINO
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Publication number: 20190185501Abstract: The present invention provides purified compounds extracted from seaweeds having the formula (I): wherein R1 and R2 is each independently H or a fatty acid and their use for inhibiting the growth of cancer cells.Type: ApplicationFiled: November 16, 2016Publication date: June 20, 2019Inventors: Judith BOBBITT, Ahmed ZEIN
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Publication number: 20190185502Abstract: There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis.Type: ApplicationFiled: December 17, 2018Publication date: June 20, 2019Inventors: Jiasheng LU, Jiamin GU, Xiang JI, Daiqiang HU, Xiuchun ZHANG, Xinyong LV, Jinchao AI, Dongdong WU, Xianqi KONG, Lin WANG, Dongqing ZHU, Xiaolin HE
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Publication number: 20190185503Abstract: Hypersulfated disaccharides with utility in asthma or asthma related disorders are disclosed. The heptasulfated disaccharides administered orally have comparable bioavailability to the intravenous administered dosage form.Type: ApplicationFiled: August 14, 2017Publication date: June 20, 2019Inventors: Tahir AHMED, ARIE GUTMAN, IRINA FEDOTEV, IGOR RUKHMAN, OLGA GROSSMAN
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Publication number: 20190185504Abstract: An object of the present invention is to solve the various problems with the conventional process for producing a sugar fatty acid ester, such as a sucrose fatty acid ester (FASuc), and to provide a process which has advantages such as no production of a soap by-product and ease of separation between the catalyst and the product and also enables efficient synthesis by a simple operation under mild conditions in a flow system, and to provide a composition including the sugar fatty acid ester. The present invention is directed to a process for producing a sugar fatty acid ester by a transesterification reaction of a fatty acid ester and a saccharide using an anion exchanger as a catalyst, and to a composition including such a sugar fatty acid ester.Type: ApplicationFiled: January 16, 2017Publication date: June 20, 2019Applicant: TOHOKU UNIVERSITYInventors: Naomi KITAKAWA, Tomone SASAYAMA, Yuto KAMIKANDA
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Publication number: 20190185505Abstract: The invention provides a process of controlling the impurities of clindamycin hydrochloride, comprising a step of purifying said clindamycin hydrochloride by two-phase high performance liquid chromatography, wherein the chromatographic conditions are as follows: the detection wavelength is 200-220 nm; the column temperature is 20-40° C.; the flow rate is 0.8-1 ml/min; Mobile phase A: 0.025 mol/L potassium dihydrogen phosphate solution; Mobile phase B: Acetonitrile; and gradient elution is performed. The method of controlling impurities of the invention can solve the problem of the interference by excipients and the problem of the separation of many impurities at the same time. It also provides an effective method for setting quality standard of impurities in such a formulation.Type: ApplicationFiled: December 14, 2018Publication date: June 20, 2019Inventors: Dongsheng Ni, Jing Liu, Gang Li, Xiangrong Dai, Xiaoyi Li
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Publication number: 20190185506Abstract: The present invention provides a myricetin derivative, a preparation method thereof, a pharmaceutical composition containing the same, an application thereof for treating colitis, preventing and treating colitis-associated tumorigenesis and treating colorectal cancer, and an application thereof in preparing a composition for modulating activities of endoplasmic reticulum stress signaling molecules. The myricetin derivative disclosed herein has excellent water solubility, and has biological activities including inhibition of colitis, prevention and treatment of colitis-associated tumorigenesis, and treatment of colorectal cancer. The preparation method disclosed herein uses myricetrin as starting material which is economical and easily available. With the merits of low cost, high yield, high product purity and suitability for large-scale industrial production, the preparation method disclosed herein represents significant market value and economic prospects.Type: ApplicationFiled: August 4, 2017Publication date: June 20, 2019Applicant: MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD.Inventors: Wenbao LI, Xianjun QU, Feng LI, Liang ZHANG, Shixiao WANG, Zhiyu SONG, Feng WANG, Chong YANG, Huashi GUAN
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Publication number: 20190185507Abstract: The present invention relates to novel compounds for the treatment of Hepatitis C.Type: ApplicationFiled: August 17, 2017Publication date: June 20, 2019Applicant: Sandoz AGInventors: George Moore, Desiree Strych, Michael Papp, Olga Schoene, Thorsten Wilhelm, Hannes Lengauer
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Publication number: 20190185508Abstract: The present invention is directed to deuterated 4?-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.Type: ApplicationFiled: December 6, 2018Publication date: June 20, 2019Applicants: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLCInventors: Francois-Rene Alexandre, Izzat Raheem
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Publication number: 20190185509Abstract: Provided herein are 2?2? cyclic phosphonate dinucleotides of formula (J), their pharmaceutically acceptable salts, hydrates or solvates, a pharmaceutical composition containing them and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, the dinucleotides can be used as adjuvants in vaccines.Type: ApplicationFiled: December 19, 2018Publication date: June 20, 2019Inventors: Gabriel Birkus, Ondrej Pav, Tomas Jandusik, Ivan Rosenberg, Radim Nencka
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Publication number: 20190185510Abstract: The present disclosure relates to 2?3? cyclic phosphonate dinucleotides of general formula (J), their pharmaceutically acceptable salts, their pharmaceutical composition and combinations of said substances and other medicaments or pharmaceuticals. The disclosure also relates to the use of said compounds for the treatment or prevention of diseases or conditions modifiable by STING protein modulation, such as cancer or viral, allergic and inflammatory diseases. In addition, these substances can be used as adjuvants in vaccines.Type: ApplicationFiled: December 19, 2018Publication date: June 20, 2019Inventors: Gabriel Birkus, Ondrej Pav, Tomas Jandusik, Ivan Rosenberg, Radim Nencka
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Publication number: 20190185511Abstract: The present invention provides highly active locked nucleic acid cyclic-dinucleotide (LNA-CDN) immune stimulators that activate DCs via the cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the LNA-CDNs of the present invention are provided in the form of a composition comprising one or more cyclic dinucleotides that induce human STING-dependent type I interferon production, wherein the cyclic dinucleotides present in the composition have at least one 2?, 4? locked nucleic acids within the cyclic dinucleotide.Type: ApplicationFiled: July 1, 2017Publication date: June 20, 2019Applicants: ADURO BIOTECH, INC., NOVARTIS AGInventors: David Braun KANNE, Chudi Obioma NDUBAKU, Jacob Robert BRUML, Thanh Ngoc Lan LE, Jeffrey MCKENNA, George Scott TRIA, Stephen CANHAM
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Publication number: 20190185512Abstract: Compounds and methods of synthesizing oxysterols are provided. The compounds and methods provided allow the oxysterol to be safely produced at a high yield. The compounds and methods provided can produce the oxysterol in a stereoselective manner.Type: ApplicationFiled: February 25, 2019Publication date: June 20, 2019Inventors: Roger E. Harrington, Jerbrena C. Jacobs, Damodaragounder Gopal, Ke-Qing Ling, Marco Burello
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Publication number: 20190185513Abstract: This invention relates to methods of stimulating the activity of the human and animal enteric nervous system. The method comprises orally administering an aminoserol, such as squalamine, a naturally occurring aminosterol isolated from Squalus acanthias, or derivatives thereof, to a subject in need.Type: ApplicationFiled: December 13, 2018Publication date: June 20, 2019Applicant: Enterin Laboratories, Inc.Inventor: Michael Zasloff
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Publication number: 20190185514Abstract: The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections: R1—Ar1-L1-Ar2-L2-Ar3-L3-Ar4-L4-Ar5—R2??(I):Type: ApplicationFiled: July 23, 2018Publication date: June 20, 2019Inventors: Sascha Baumann, Jennifer Herrmann, Kathrin Mohr, Heinrich Steinmetz, Klaus Gerth, Ritesh Raju, Rolf Müller, Rolf W. Hartmann, Mostafa Hamed, Walid A. M. Elgaher, Maria Moreno, Franziska Gille, Liang Liang Wang, Andreas Kirschning, Stephan Hüttel
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Publication number: 20190185515Abstract: In some aspects, the present invention provides methods of treating a subject in need of treatment for neuropathic pain, the method comprising administering a compstatin analog to the subject. In some embodiments, the compstatin analog is administered parenterally, e.g., intravenously.Type: ApplicationFiled: July 9, 2018Publication date: June 20, 2019Inventors: Cedric Francois, Pascal Deschatelets
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Publication number: 20190185516Abstract: Provided are backbone cyclized peptides that interfere with signaling of the intracellular adaptor protein MyD88. Pharmaceutical compositions including these backbone cyclized peptides as well as their use in treatment of multiple sclerosis (MS) and other diseases associated with MyD88 signaling are also disclosed.Type: ApplicationFiled: June 4, 2017Publication date: June 20, 2019Applicant: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Gabriel NUSSBAUM, Amnon HOFFMAN, Chaim GILON
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Publication number: 20190185517Abstract: In one aspect, the invention relates to substituted urea depsipeptide analogs, derivatives thereof, and related compounds, which are useful as activators the ClpP endopeptidease; synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating infectious disease using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: September 1, 2017Publication date: June 20, 2019Inventors: Richard E. LEE, Ying Zhao
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Publication number: 20190185518Abstract: The disclosed peptidomimetic macrocycles modulate the activity of BFL-1 or a BCL-2 family protein. BFL-1, an anti-apoptotic BCL-2 family member, blocks p53-mediated apoptosis and has oncogenic transforming activity. Peptidomimetic macrocycles, pharmaceutical compositions, and methods disclosed herein can be used for the treatment of disease in which BFL-1 or a BCL-2 family protein is over-expressed, such as cancer. In particular, BFL-1-modulating or a BCL-2 family protein-modulating peptidomimetic macrocycles disclosed herein can be applied in the setting of resistance to BCL-2 family inhibitors, which is often engendered by BFL-1 or BCL-2 family protein over-expression or hyper-activation.Type: ApplicationFiled: March 9, 2018Publication date: June 20, 2019Inventor: Vincent Guerlavais
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Publication number: 20190185519Abstract: The present invention relates to a nucleic acid complex having a novel structure, which can introduce a bioactive nucleic acid into cells, a composition for treating and diagnosing disease, which comprises the same, and a method of regulating expression of a target gene using the same, and more particularly to a nucleic acid complex comprising a bioactive nucleic acid complementarily bound to a carrier peptide nucleic acid modified to be generally positively charged, a composition for treating and diagnosing disease, which comprises the same, and a method of regulating expression of a target gene using the same.Type: ApplicationFiled: August 9, 2017Publication date: June 20, 2019Inventors: Goonho JEO, Hye Joo KIM, Ji-Yeon YU, Chinbayar BATOCHIR, Deokhwe HUR, Hee Kyung PARK
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Publication number: 20190185520Abstract: The subject application provides a genetically modified recombinant facultative intracellular invasive bacterial pathogen (RFIIBP) or a recombinant attenuated Salmonella vaccine (RASV) strains encoding Zika virus (ZIKV) antigens. These strains exhibit high immunogenicity, complete safety, and attenuation, and are unable to persist or be shed in an infective or viable form. These RFIIBPs and RASVs also exhibit regulated delayed attenuation in vivo, regulated delayed in vivo synthesis of protective ZIKV antigens. Methods of inducing mucosal, systemic and cellular immunities in hosts are also provided and antibodies produced using the disclosed RFIIBPs and RASVs can comprise neutralizing antibodies against ZIKV that do not crossreact with Dengue virus (DENV).Type: ApplicationFiled: July 24, 2017Publication date: June 20, 2019Inventor: ROY CURTISS, III
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Publication number: 20190185521Abstract: The disclosure provides nucleic acids encoding variant polypeptides having pesticidal activity against insect pests, including Lepidoptera and Diptera. Particular embodiments provide isolated nucleic acids encoding Cyt1A variant polypeptides, pesticidal compositions, DNA constructs, and transformed microorganisms and plants comprising a nucleic acid of the embodiments. These compositions find use in methods for controlling pests, particularly Diptera pests.Type: ApplicationFiled: April 18, 2017Publication date: June 20, 2019Applicant: Universidad Nacional Autónoma de MéxicoInventors: Maria Alejandra BRAVO DE LA PARRA, Mario Soberón CHAVEZ
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Publication number: 20190185522Abstract: It provides novel fusion proteins that are capable of self-crystallization and exhibit improved physical properties such as enhanced tolerance to organic solvents and increased thermostability. Polynucleotides encoding the fusion proteins as well as methods of making and using such fusion proteins are also described.Type: ApplicationFiled: July 10, 2017Publication date: June 20, 2019Inventors: Michael CHAN, Marianne LEE, Bradley HEATER
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Publication number: 20190185523Abstract: A polypeptide having an amino acid sequence corresponding to a binding domain of a botulinum toxin is described. The polypeptide modulates expression of genes involved in, for example, collagen production and extra cellular matrix organization, and finds use, therefore in modulating skin quality attributes such as elasticity, firmness etc. Moreover, the polypeptide inhibits lipogenesis in specialized cells and finds use, therefore, in reducing skin oiliness, which is frequently observed in skin tissue afflicted with large pores and acne. Nucleic acids encoding the polypeptide, as well as vectors, host cells, and systems comprising the nucleic acids, are further described.Type: ApplicationFiled: December 20, 2018Publication date: June 20, 2019Inventors: Birgitte PS Jacky, Amy Brideau-Andersen, Hui You, Shiazah Z. Malik, Donald E. Frail, Mitchell F. Brin
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Publication number: 20190185524Abstract: Disclosed herein are botulinum neurotoxin (BoNT) polypeptides with a modified BoNT/B4 receptor binding domain (B4-HC) having amino acid mutations that modify the binding of the BoNT to the human SytII receptor. Specific mutations and combinations of mutations are disclosed. Isolated modified HCs, polypeptides comprising such modified HCs, chimeric molecules, pharmaceutical compositions, and methods of making and using the same are also disclosed. Methods of identifying additional such modified receptor binding domains, are further disclosed.Type: ApplicationFiled: August 24, 2017Publication date: June 20, 2019Inventors: Min Dong, Liang Tao
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Publication number: 20190185525Abstract: The present invention relates to a polypeptide comprising an epitope of an antigen; a kit and a composition for diagnosing allergy, wherein the kit and the composition comprise the aforementioned polypeptide, and a method for diagnosing allergy and a method for treating allergy, wherein the methods use the aforementioned polypeptide; a pharmaceutical composition comprising the aforementioned polypeptide; and a raw material or a processed product in which the antigen comprising the aforementioned polypeptide is removed or reduced. Furthermore, the present invention relates to a tester for determining the presence or absence of the antigen in an object.Type: ApplicationFiled: December 18, 2018Publication date: June 20, 2019Inventors: Yuji Aoki, Fumiaki Ono
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Publication number: 20190185526Abstract: Disclosed are double stranded RNA molecules that are toxic to coleopteran insects. In particular, interfering RNA molecules capable of interfering with pest target genes and that are toxic to the target pest are provided. Further, methods of making and using the interfering RNA, for example in transgenic plants or as the active ingredient in a composition, to confer protection from insect damage are disclosed.Type: ApplicationFiled: August 1, 2017Publication date: June 20, 2019Applicant: Syngenta Participations AGInventors: Kevin L. DONOHUE, Yann NAUDET, Pascale FELDMANN, Lies DEGRAVE, Isabelle MAILLET
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Publication number: 20190185527Abstract: A fusion protein having the amino acid sequence of SEQ ID NO: 3 or SEQ ID NO: 3 has enhanced skin cell proliferation effect. A composition includes, as an effective ingredient, the fusion protein for improving skin wrinkle, skin elasticity, and anti-aging. Because the composition has an excellent cell proliferation effect and an effect of improving skin wrinkle and enhancing skin elasticity, it is expected to be used advantageously in the field of functional cosmetics.Type: ApplicationFiled: August 25, 2017Publication date: June 20, 2019Inventor: Sun Kyo LEE
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Publication number: 20190185528Abstract: Transgenic silkworms comprising at least one nucleic acid encoding a chimeric silk polypeptide comprising one or more spider silk elasticity and strength motifs are disclosed. Expression cassettes comprising nucleic acids encoding a variety of chimeric spider silk polypeptides (Spider 2, Spider 4, Spider 6, Spider 8) are also disclosed. A piggyBac vector system is used to incorporate nucleic acids encoding chimeric spider silk polypeptides into the mutant silkworms to generate stable transgenic silkworms. Chimeric silk fibers having improved tensile strength and elasticity characteristics compared to native silkworm silk fibers are also provided. The transgenic silkworms greatly facilitate the commercial production of chimeric silk fibers suitable for use in a wide variety of medical and industrial applications.Type: ApplicationFiled: February 13, 2019Publication date: June 20, 2019Inventors: Malcolm James Fraser, Randolph V. Lewis, Donald L. Jarvis, Kimberly Thompson, Joseph Hull, Yun-Gen Miao, Florence Teule, Bong-Hee Sohn, Young-Soo Kim