Patents Issued in February 7, 2019
  • SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
    Publication number: 20190040059
    Abstract: Provided is a compound having ?4 integrin inhibitory action. The compound is a sulfonamide derivative represented by the following formula (I), or pharmaceutically acceptable salt thereof: where R1 to R5, e to h, D, and B represent those as described in the specification.
    Type: Application
    Filed: February 6, 2017
    Publication date: February 7, 2019
    Applicant: EA PHARMA CO., LTD.
    Inventors: Munetaka TOKUMASU, Masatsugu NOGUCHI, Mizuki KAWAHIRA, Kana IWASAKI, Nobuhiko HAYAKAWA, Wataru MIYANAGA, Yuki SAITOU, Yui YAMAURA, Ayatoshi ANDO, Atsushi TSURUTA, Misto NOGUCHI
  • PESTICIDALLY ACTIVE TETRACYCLIC DERIVATIVES WITH SULFUR CONTAINING SUBSTITUENTS
    Publication number: 20190040060
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
    Type: Application
    Filed: October 9, 2018
    Publication date: February 7, 2019
    Applicant: Syngenta Participations AG
    Inventors: Pierre Joseph Marcel JUNG, Andrew EDMUNDS, Michel MUEHLEBACH, Roger Graham HALL, Jerome Yves CASSAYRE
  • Tetrahydro-Pyrido-Pyrimidine Derivatives
    Publication number: 20190040061
    Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
    Type: Application
    Filed: October 17, 2018
    Publication date: February 7, 2019
    Inventors: Nigel Graham Cooke, Paulo Fernandes Gomes Dos Santos, Nadege Graveleau, Christina Hebach, Klemens Hoegenauer, Gregory John Hollingworth, Alexander Baxter Smith, Nicolas Soldermann, Frank Stowasser, Ross Sinclair Strang, Nicola Tufilli, Anette von Matt, Romain Wolf, Frederic Zecri
  • BCL-2 INHIBITORS
    Publication number: 20190040062
    Abstract: The disclosure includes compounds of Formula (I) wherein W, R1, R2, R3, R4, R5, R6, m, n, L, and Z1, are defined herein. Also disclosed is a method for treating a neoplastic disease and autoimmune disease with these compounds.
    Type: Application
    Filed: July 26, 2018
    Publication date: February 7, 2019
    Inventors: Yi Chen, Yan Lou
  • TRICYCLIC COMPOUND FOR BROMODOMAIN-CONTAINING PROTEIN INHIBITOR AND PREPARATION PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
    Publication number: 20190040063
    Abstract: The present application present application relates to a compound represented by Formula (III) or a pharmaceutically acceptable salt, solvent compound, active metabolite, crystal polymorph, ester, isomer, or prodrug thereof. The application further provides a pharmaceutical composition comprising the compound represented by Formula (III) and a use thereof for preparing a bromodomain inhibitor for preventing or treating various diseases, such as inflammation and cancer, related to the bromodomain.
    Type: Application
    Filed: February 4, 2017
    Publication date: February 7, 2019
    Inventors: Jijun LI, Wei WU, Yan ZHU, Huting WANG, Lijia ZHAO, Welnan HE, Yinghui SUN, Yong PENG, Yongxin Han
  • MULTI-KINASE INHIBITOR COMPOUND, AND CRYSTAL FORM AND USE THEREOF
    Publication number: 20190040064
    Abstract: The present invention relates to a compound as represented by formula (I) or a pharmaceutically acceptable salt and stereoisomer thereof, wherein R1, R2, X, Y, P, W, and Ar are as defined in the description. The compound of formula (I) of the present invention can be used in the preparation of a drug for treating cancers mediated by abnormality of multi-kinases. Also provided is a crystal form I of a compound 4-(5-(2-chlorophenyl)-3-methyl-2,10-dihydropyrazolo[4,3-b]pyrido[4,3-e][1,4]diazepin-8-yl)morpholine, wherein in an X-ray powder diffraction pattern of crystal form I, there are characteristic peaks at 7.4±0.20, 17.9±0.2°, 18.9±0.2°, 19.4±0.2°, 21.5±0.2°, and 23.7±0.2°.
    Type: Application
    Filed: October 10, 2018
    Publication date: February 7, 2019
    Inventor: Frank Wu
  • EGFR Inhibitors and Methods of Treating Disorders
    Publication number: 20190040065
    Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: March 2, 2018
    Publication date: February 7, 2019
    Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
  • PROCESS FOR THE PREPARATION OF PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR
    Publication number: 20190040066
    Abstract: The present invention relates to processes for the preparation of Phosphatidylinositol 3-Kinase Inhibitor (PI3K) compound of formula-1 via novel intermediates (I).
    Type: Application
    Filed: February 3, 2017
    Publication date: February 7, 2019
    Inventors: Sanket Pandurang Jadhav, Dipak Vasant Patil, Deepak Puna Mahajan, Sagar Purushottam Nehate, Himanshu Madhav Godbole, Girij Pal Singh
  • USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS
    Publication number: 20190040067
    Abstract: The present application provides methods of treating PI3K? related disorders using compounds of Formula I: or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: March 2, 2018
    Publication date: February 7, 2019
    Inventors: Yun-Long Li, Wenqing Yao, Andrew P. Combs, Eddy W. Yue, Song Mei, Wenyu Zhu, Joseph Glenn, Thomas P. Maduskuie, JR., Richard B. Sparks, Brent Douty, Chunhong He
  • PYRROLOPYRIMIDINE FIVE-MEMBERED AZACYCLIC DERIVATIVE AND APPLICATION THEREOF
    Publication number: 20190040068
    Abstract: A pyrrolopyrimidine five-membered azacyclic derivative as a novel JAK kinase (Janus kinase) inhibitor, and use thereof in a preparation of a pharmaceutical product for preventing and/or treating an indication related to a JAK kinase function. The pyrrolopyrimidine five-membered azacyclic derivative is an ideal JAK kinase inhibitor with a high potency, and can be used to treat or prevent diseases such as rheumatoid arthritis, polycythemia vera, psoriasis, primary thrombocytosis, myelofibrosis, and the like.
    Type: Application
    Filed: January 25, 2017
    Publication date: February 7, 2019
    Inventors: Jianming YIN, Yubin LV, Bangliang LI
  • PROCESS FOR THE PREPARATION OF IBRUTINIB
    Publication number: 20190040069
    Abstract: The present invention relates to a process for the preparation of 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one or Ibrutinib of Formula (I).
    Type: Application
    Filed: February 2, 2017
    Publication date: February 7, 2019
    Applicant: SHILPA MEDICARE LIMITED
    Inventors: SRIRAM RAMPALLI, LAV KUMAR UPALLA, CHANTI BABU PATNEEDI, GOPALA KRISHNA DASARI, AKSHAY KANT CHATURVEDI
  • PROCESS FOR THE SYNTHESIS OF STABLE AMORPHOUS IBRUTINIB
    Publication number: 20190040070
    Abstract: Disclosed herein is a new route of synthesis and a new stable amorphous form of ibrutinib. Also disclosed are pharmaceutical compositions, oral dosage forms and the use of the amorphous ibrutinib in the treatment of mantle cell lymphoma or chronic lymphocytic leukemia.
    Type: Application
    Filed: February 8, 2017
    Publication date: February 7, 2019
    Inventors: Thomas MAIER, Inna KARAPETYAN, Alvard ARAKELYAN, Tamara MARGARYAN, Vardan SARGSYAN, Heghine STEPANYAN, Hermine ABOVYAN, Roman GERBER AESCHBACHER, Sven HAFERKAMP
  • TLR7 AGONIST CRYSTALLINE FORM A, PREPARATION METHOD AND USE THEREOF
    Publication number: 20190040071
    Abstract: The present invention relates to crystalline form A of a TLR7 agonist 2-butoxy-7-(4-(pyrrolidin-1-ylmethyl)-benzyl)-5H-pyrrolo[3,2-d]pyrimidin-4-amine (formula I), a method for preparing the crystalline form A, and the use thereof.
    Type: Application
    Filed: February 4, 2017
    Publication date: February 7, 2019
    Inventors: Zhaozhong DING, Fei SUN, Yinghu HU, Yilong ZHOU, Zheng WANG, Rui ZHAO, Ling YANG
  • METHOD FOR PREPARING PYRROLO[3,2-D]PYRIMIDINE COMPOUND, AND INTERMEDIATES THEREOF
    Publication number: 20190040072
    Abstract: The present invention relates to a method for preparing a pyrrolo[3,2-d]pyrimidine compound (the compound represented by formula I), and corresponding intermediates.
    Type: Application
    Filed: February 4, 2017
    Publication date: February 7, 2019
    Inventors: Zhaozhong DING, Fei SUN, Yinghu HU, Yilong ZHOU, Rui ZHAO, Ling YANG
  • NONANOIC AND DECANOIC ACID DERIVATIVES AND USES THEREOF
    Publication number: 20190040073
    Abstract: The present disclosure relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present disclosure also relates to pharmaceutical compositions containing the fluorinated compounds of the disclosure, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: October 5, 2018
    Publication date: February 7, 2019
    Inventors: Takeru FURUYA, Ben C. ASKEW
  • PYRAZOLOPYRIMIDINE COMPOUNDS
    Publication number: 20190040074
    Abstract: The present teachings provide a compound represented by structural formula (I-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: October 9, 2018
    Publication date: February 7, 2019
    Inventors: Yong Liu, Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Peter Brent Sampson, Miklos Feher, Grace Ng, Narendra Kumar B. Patel, Yunhui Lang
  • Substituted Pyrrolo, -Furano, and Cyclopentylpyrimidines Having Antimitotic and/or Antitumor Activity and Methods of Use Thereof
    Publication number: 20190040075
    Abstract: 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: Application
    Filed: August 7, 2018
    Publication date: February 7, 2019
    Inventor: Aleem Gangjee
  • Spirocyclic Quinolizine Derivatives Useful as HIV Integrase Inhibitors
    Publication number: 20190040076
    Abstract: The present invention relates to spirocyclic quinolizine derivatives and pharmaceutically acceptable salts or prodrug thereof, compositions comprising at least one spirocyclic quinolizine derivative, and methods of using the spirocyclic quinolizine derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: December 12, 2016
    Publication date: February 7, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Yonglian Zhang, Sherman T. Waddell, Tao Yu, John A. McCauley, Andrew Stamford
  • TRIAZOLE DERIVATIVES OF MELAMPOMAGNOLIDE B AND METHODS OF USE THEREOF
    Publication number: 20190040077
    Abstract: The present disclosure relates to triazole derivatives of melampomagnolide B, their synthesis, and their use as anti-cancer compounds.
    Type: Application
    Filed: January 27, 2017
    Publication date: February 7, 2019
    Inventors: Venumadhav Janganati, Peter Crooks, Jessica Ponder, Craig Jordan
  • PESTICIDAL COMPOSITIONS AND USES THEREOF
    Publication number: 20190040078
    Abstract: Provided herein are compounds that exhibit activity as fungicides and are useful, for example, in methods for the control of fungal pathogens in plants and can be applied to said plants in a variety of ways.
    Type: Application
    Filed: July 9, 2018
    Publication date: February 7, 2019
    Inventors: Jennifer Lynn Bennett, Karen C. Fitzsimmons, Shomir Ghosh, Jeremy Robert Greenwood, William P. Haakenson, JR., Geraldine C. Harriman, Silvana Marcel Leit De Moradei, Barry J. Shortt, Urszula J. Slomczynska, Jeffrey Michael Stein
  • TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS
    Publication number: 20190040079
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110?, and therefore have utility in therapy.
    Type: Application
    Filed: March 1, 2018
    Publication date: February 7, 2019
    Inventors: Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Thomas James Hill, Franck Alexandre Silva
  • BIARYL KINASE INHIBITORS
    Publication number: 20190040080
    Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.
    Type: Application
    Filed: September 29, 2016
    Publication date: February 7, 2019
    Inventors: Joanne J. BRONSON, Ling CHEN, Jonathan L. DITTA, Carolyn Diane DZIERBA, Prasada Rao JALAGAM, Guanglin LUO, John E. MACOR, Tarun Kumar MAISHAL, Susheel Jethanand Nara, Ramkumar RAJAMANI, Ramesh Kumar SISTLA, Soodamani THANGAVEL
  • C5-C6-Oxacyclic Fused Iminothiadiazine Dioxide Compounds Bearing an Ether Linker as BACE Inhibitors, Compositions, and Their Use
    Publication number: 20190040081
    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, R2, RA, ring A, ring C, and m are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: February 6, 2017
    Publication date: February 7, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Jared N. Cumming, Xing Dai
  • HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
    Publication number: 20190040082
    Abstract: Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
    Type: Application
    Filed: February 27, 2018
    Publication date: February 7, 2019
    Inventors: Kaijiong Xiao, Fenglei Zhang, Liangxing Wu, Wenqing Yao
  • ANTIBACTERIAL COMPOUNDS
    Publication number: 20190040083
    Abstract: This invention relates to antibacterial drug compounds containing a bicyclic core, typically a bicycle in which one of the rings is an oxazolidinone. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections and in methods of treating bacterial infections.
    Type: Application
    Filed: February 8, 2017
    Publication date: February 7, 2019
    Inventors: Ian Cooper, Amanda Lyons
  • HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
    Publication number: 20190040084
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: August 10, 2018
    Publication date: February 7, 2019
    Inventors: Jianming Yu, Brian C. Shook, Thomas P. Blaisdell, In Jong Kim, Joseph Panarese, Kevin McGrath, Solymar Negretti-Emmanuelli, Yat Sun Or
  • PHOTOCHEMICAL METHODS OF MAKING CYCLOBUTANE BORONATES AND RELATED COMPOUNDS
    Publication number: 20190040085
    Abstract: The present technology relates generally cyclobutane boronates, including methods of preparation by exposing a mixture of a compound of Formula I in a solvent and a catalytic amount of a visible light sensitizer to provide a compound of Formula II, stereoisomers thereof, and/or salts of any of the foregoing. The cyclobutane boronate compounds are useful intermediates in the preparation of pharmaceutically active compounds as well as other other useful compounds.
    Type: Application
    Filed: August 2, 2018
    Publication date: February 7, 2019
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Tehshik Peter Yoon, Spencer Owen Scholz, Rowan Mark Littlefield, Niecia Elizabeth Flikweert
  • Preparation Of Ammonium or Phosphonium Borate Salts
    Publication number: 20190040086
    Abstract: A process for preparing an ammonium or phosphonium borate salt KA containing a cation K and an anion A. The process includes providing a melt of a borate salt K1A, and adding a solution of an ammonium or phosphonium salt KA1 in a solvent or solvent mixture (i), wherein K is an organic ammonium or phosphonium cation, and A is a borate anion of formula (Ia) or (Ib).
    Type: Application
    Filed: January 27, 2017
    Publication date: February 7, 2019
    Inventors: Nicole Holub, Juergen Herbel
  • MICROBIOCIDALLY ACTIVE BENZOXABOROLES
    Publication number: 20190040087
    Abstract: Compounds of formula (I) are as defined in the claims, and their use in compositions and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
    Type: Application
    Filed: August 7, 2018
    Publication date: February 7, 2019
    Applicant: Syngenta Participations AG
    Inventors: Ramya Rajan, Daniel STIERLI, Renaud BEAUDEGNIES
  • PROCESS FOR THE PREPARATION OF A TRIARYL PHOSPHATE ESTER COMPOSITION
    Publication number: 20190040088
    Abstract: The invention relates to a process for the preparation of a triaryl phosphate ester composition comprising a. reacting a phosphorous oxyhalide with a (C1-C15-alkyl)phenol to obtain a first product; b. reacting the first product with phenol to obtain a triaryl phosphate ester composition; wherein in step a., for every mol of phosphorous oxyhalide 1.3 to 1.6 mols of (C1-C15-alkyl)phenol are used. The invention also relates to a triaryl phosphate ester composition obtainable according to the process of the invention.
    Type: Application
    Filed: February 13, 2017
    Publication date: February 7, 2019
    Inventors: Lukasz Gorecki, Grzegorz Janus, Uwe Storzer
  • GOLD COMPLEX-CONTAINING CANCER ACTIVITY COMPOSITION
    Publication number: 20190040089
    Abstract: Gold(I) complex with mixed ligands as an anticancer agent. The gold(I) ion is coordinated to a dithiocarbamate ligand and a phosphorus-containing ligand (e.g. phosphines). Also described are a pharmaceutical composition incorporating the gold(I) complex, a methods of synthesizing the gold(I) complex, and a method for treating cancer.
    Type: Application
    Filed: August 24, 2018
    Publication date: February 7, 2019
    Applicants: KING FAHD UNIVERSITY OF PETROLEUM AND MINERALS, KING SAUD UNIVERSITY
    Inventors: Said S. AL-JAROUDI, Ali ALHOSHANI, Muhammad ALTAF, Anvarhusein Abdulkadir ISAB
  • N,N-BIS(2-DIALKYLPHOSPHINOETHYL)AMINE-BORANE COMPLEX AND PRODUCTION METHOD THEREFOR, AND METHOD FOR PRODUCING RUTHENIUM COMPLEX CONTAINING N,N-BIS(2-DIALKYLPHOSPHINOETHYL)AMINE AS LIGAND
    Publication number: 20190040090
    Abstract: The purpose of the present invention is to provide an N,N-bis(2-dialkylphosphinoethyl)amine-borane complex which is a ruthenium complex that exhibits excellent catalytic activity in a hydrogenation reaction, etc., and a production method therefor, and a method for efficiently producing a ruthenium complex containing N,N-bis(2-dialkylphosphinoethyl)amine as a ligand. The present invention is capable of efficiently producing an amine-borane complex (3) by reacting an oxazolidinone compound (1) with a dialkylphosphine-borane compound (2) in the presence of a base. The present invention is also capable of efficiently producing a ruthenium complex (5) by reacting the amine-borane complex (3) with a ruthenium compound (4) in the presence of an amine. (In the formula, a solid line, a dashed line, B, C, H, L1-L3, LG, n, N, O, P, Ru, X, and R1-R10 are as defined in the description.
    Type: Application
    Filed: January 30, 2017
    Publication date: February 7, 2019
    Inventors: Yuji Nakayama, Hikaru Nakajima
  • COMPOSITIONS USEFUL IN THERAPY OF AUTOPHAGY-RELATED PATHOLOGIES, AND METHODS OF MAKING AND USING THE SAME
    Publication number: 20190040091
    Abstract: Lanthionine ketimine derivatives, and methods of making and using the same, are described. Included are lanthionine ketimine phosphonate (LK-P), lanthionine ketimine ester phosphonate (LKE-P) derivatives, as well as lanthionine ketimine derivatives having a tert-enamide moiety at the 2-position (NVP-LKE).
    Type: Application
    Filed: February 24, 2017
    Publication date: February 7, 2019
    Applicants: The University of Toledo, Washington State University
    Inventors: Kenneth Hensley, Travis Denton
  • CRYSTALLINE FORMS OF ETHYL ((S)-((((2R,5R)-5-(6-AMINO-9H-PURIN-9-YL)-4-FLUORO-2,5-DIHYDROFURAN-2-YL)OXY)METHYL)(PHENOXY)PHOSPHORYL)-L-ALANINATE
    Publication number: 20190040092
    Abstract: The present invention relates to novel forms of ethyl ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydrofuran-2-yl)oxy)methyl)(phenoxy)phosphoryl)-L-alaninate, pharmaceutical formulations, and therapeutic uses thereof in treating viral infections (e.g., an HIV infection).
    Type: Application
    Filed: July 30, 2018
    Publication date: February 7, 2019
    Inventors: Olga Viktorovna Lapina, Bing Shi, Silas Wang
  • BIOPARTICLE ISOLATION AND THERAPEUTIC APPLICATION THEREOF
    Publication number: 20190040093
    Abstract: Compositions and methods for the isolation of protein-nucleic acid complexes, extracellular vesicle (EV) (e.g., microvesicles) and free nucleic acids (collectively referred to as “bioparticles”) released by mammalian cells into body fluids or cell culture media are provided. Isolated bioparticles of the current disclosure contain biomolecules that are useful as diagnostic/prognostic biomarkers or for identification of therapeutic targets (e.g., disease or disorder-associated miRNAs, circulating tumor DNA). Isolation of biomolecules results in purification and concentration. Methods for producing biofluids without detectable bioparticles, largely depleted of bioparticles, and/or possessing a reduced concentration of bioparticles compared to a biofluid starting material (collectively termed “bioparticle-depleted”) are provided. Bioparticle-depleted biofluid is useful, e.g.
    Type: Application
    Filed: February 10, 2017
    Publication date: February 7, 2019
    Applicant: YMIR GENOMICS LLC
    Inventors: Patrick Shannon Pendergrast, Robert Scott Pendergrast, John Stephen Pendergrast, Anna Irmina Markowska
  • PROCESS FOR THE PREPARATION OF D-GLUCITOL, 1,5-ANHYDRO-1-C-[4-CHLORO-3-[[4-[[(3S)-TETRAHYDRO-3-FURANYL] OXY]PHENYL] METHYL] PHENYL]-, (1S) AND ITS CRYSTALLINE FORMS THEREOF
    Publication number: 20190040094
    Abstract: The present invention relates to process for the preparation of D-glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl] methyl]phenyl]-, (1S) formula-1 and its crystalline forms thereof.
    Type: Application
    Filed: January 27, 2017
    Publication date: February 7, 2019
    Inventors: Thirumalai Rajan SRINIVASAN, Eswaralah SAJJA, Venkata Panakala Rao GOGULAPATI, Rajeshwar Reddy SAGYAM, Rajesham BODGE, Mohammad Rafee SHAIK
  • Rhamnolipid Amides For Hair Scent Retention
    Publication number: 20190040095
    Abstract: The invention provides derivatives of rhamnolipids, formulations comprising these, and the use thereof.
    Type: Application
    Filed: February 15, 2017
    Publication date: February 7, 2019
    Applicant: Evonik Degussa GmbH
    Inventors: Xin Lu, Sandra Nattland, Monica Desiree van Logchem, Hans Henning Wenk, Fabien Cabirol, Verena Dahl, Ralph Scheuermann, Kathrin Daniels Brandt, Jochen Kleinen
  • CRYSTALLINE FORMS OF A MACROLIDE, AND USES THEREFOR
    Publication number: 20190040096
    Abstract: New crystalline forms of macrolide compounds, and pharmaceutical compositions thereof, are described herein. In addition, processes for preparing the crystalline forms are described herein.
    Type: Application
    Filed: February 26, 2018
    Publication date: February 7, 2019
    Inventor: David Eugene PEREIRA
  • METHOD FOR SEPARATING AND PURIFYING MOGROSIDE V BY SUBCRITICAL WATER DESORPTION TECHNOLOGY
    Publication number: 20190040097
    Abstract: The invention relates to a method for separating and purifying mogroside V by subcritical water desorption technology. The macroporous adsorption resin enriched with mogroside V is subjected to desorption under a subcritical condition of water using water as a solvent, to give an aqueous solution rich in mogroside V. The method not only improves the content of mogroside V in product, but also effectively removes bitter impurities and residual pesticides, greatly improves the taste adaptability of the product, and improves the safety and quality of the product. The method reduces the processing steps and reduces the use of organic solvents in the prior art, and reduces total production costs.
    Type: Application
    Filed: October 10, 2018
    Publication date: February 7, 2019
    Inventors: Minglian JIANG, Wenguo YANG, Yunfei SONG, Yuanyuan LI
  • STEROIDAL COMPOUND, COMPOSITION CONTAINING THE SAME AND USE THEREOF
    Publication number: 20190040098
    Abstract: Disclosed are a steroidal compound as shown in formula (I) and a drug composition containing the same, or a crystal form, a pharmaceutically acceptable salt, a hydrate or solvate, a stereoisomer, a prodrug, a metabolite or an isotopic variant thereof. The compound can be used as a CYP17 enzyme inhibitor, and has better pharmacokinetic parameters, which can improve drug concentration of the compound in an animal, thereby improving the efficacy and safety of the drug, and in turn the compound may be applied in the preparation of the drug for treating CYP17 enzyme-related diseases (such as prostate cancer).
    Type: Application
    Filed: December 29, 2016
    Publication date: February 7, 2019
    Applicant: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Xingye Ren
  • CHROMATOGRAPHY MEMBRANES, DEVICES CONTAINING THEM, AND METHODS OF USE THEREOF
    Publication number: 20190040099
    Abstract: Described herein are fluid treatment devices for use in tangential flow filtration, comprising a housing unit and a composite material, wherein the composite material comprises: a support member comprising a plurality of pores extending through the support member; and a non-self-supporting macroporous cross-linked gel comprising macropores having an average size of 10 nm to 3000 nm, said macroporous gel being located in the pores of the support member. The invention also relates to a method of separating a substance from a fluid, comprising the step of placing the fluid in contact with an inventive device, thereby adsorbing or absorbing the substance to the composite material contained therein.
    Type: Application
    Filed: August 10, 2018
    Publication date: February 7, 2019
    Inventors: Damian Brellisford, Donna Lisa Crossley, Greg McIntosh, Robert Ruman, John Rydall, Christopher S. Shields
  • PEPTIDE HAVING ACTIVITY TO IMPROVE SKIN CONDITION AND USE THEREOF
    Publication number: 20190040100
    Abstract: The present invention provides a peptide having activity to improve skin condition. The peptide of the present invention exhibits a very excellent effect in improving skin condition by inhibiting MMP2 activity. A composition containing the peptide of the present invention exhibits excellent biological activities, such as inhibiting collagen decomposition and melanosome migration, and thus can be used in wrinkle reduction, skin regeneration, skin elasticity improvement, anti-skin aging, wound regeneration, acne reduction, skin regeneration or skin whitening. The composition containing the peptide of the present invention can be used as a pharmaceutical composition for preventing or treating MMP activity-related diseases and inflammation diseases.
    Type: Application
    Filed: July 26, 2018
    Publication date: February 7, 2019
    Inventors: Yong Ji CHUNG, Eun Mi KIM
  • COMPOUND FOR TREATING SEQUELAE OF ISCHEMIC CEREBRAL STROKE
    Publication number: 20190040101
    Abstract: The present invention provides a compound (I) for treating sequelae of ischemic cerebral stroke: H—(NH—CHR1—CO)—(NH—CHR2—CO)—(NH—CHR3—CO)—(NH—CHR4—CO)—(NH—CHR5—CO)—(NH—CHR6—CO)—(NH—CHR7—CO)—OH??(I) or a pharmaceutically acceptable salt thereof, wherein R1-R7 are defined herein. The present invention also provides a pharmaceutical composition comprising said compound and use of the same in the manufacture of a medicament for treating sequelae of ischemic cerebral stroke. The compound and pharmaceutical composition according to the present invention have good pharmacological activities so that they are able to improve significantly the symptom of sequelae of ischemic cerebral stroke.
    Type: Application
    Filed: August 9, 2018
    Publication date: February 7, 2019
    Inventor: Jingyi WANG
  • SOMATOSTATIN RECEPTOR ANTAGONIST COMPOUNDS AND METHODS OF USING THE SAME
    Publication number: 20190040102
    Abstract: The present invention is directed to somatostatin receptor antagonist compounds having the structure of Formula I, compositions comprising the same, and methods of using such compounds and compositions. The compounds may be useful in the prevention or treatment of hypoglycemia.
    Type: Application
    Filed: February 9, 2017
    Publication date: February 7, 2019
    Inventors: Stephen Paul ARNS, James Brian JAQUITH, Davy Jérémy BAUDELET, Eric Roy SIMONSON, Richard Tom LIGGINS, Nag Sharwan KUMAR, Tom Han Hsiao HSIEH
  • PROTEINACEOUS COMPOUNDS AND USES THEREFOR
    Publication number: 20190040103
    Abstract: Disclosed are proteinaceous molecules and their use in conditions associated with PKC-? overexpression, such as cancer. More particularly, the present invention discloses proteinaceous molecules and their use in altering at least one of (i) formation; (ii) proliferation; (iii) maintenance; (iv) epithelial to mesenchymal cell transition; or (v) mesenchymal to epithelial cell transition of a PKC-? overexpressing cell.
    Type: Application
    Filed: February 1, 2017
    Publication date: February 7, 2019
    Inventors: Sudha RAO, Peter MILBURN
  • STABILIZED PEPTOID-PEPTIDE HYBRIDS AND USES THEREOF
    Publication number: 20190040104
    Abstract: The current invention pertains to stabilized peptoids or peptoid-peptide hybrids. The peptoids or peptoid-peptide hybrids are stabilized by side chain-side to side chain linkages and/or backbone cyclization. The current invention also provides a positional library scanning method for identification of peptoids or peptoid-peptide hybrids having a desired biological activity.
    Type: Application
    Filed: October 11, 2018
    Publication date: February 7, 2019
    Inventors: Mark McLaughlin, Amod A. Sarnaik
  • Method for Preventing and Treating Hyperpermeability
    Publication number: 20190040105
    Abstract: A peptide is described, which consists of 7-17 adjacent amino acids and comprises the hexamer TXEXXE, wherein X, X and X can be any natural or non-natural amino acid, wherein the peptide has no TNF receptor binding activity and is cyclized, for the prevention and treatment of hyperpermeability of epithelial cells and endothelial cells.
    Type: Application
    Filed: October 19, 2018
    Publication date: February 7, 2019
    Inventors: Bernhard Fischer, Rudolf Lucas
  • USE OF HUMAN DERIVED IMMUNOSUPPRESSIVE PROTEINS AND PEPTIDES AS MEDICAMENTS
    Publication number: 20190040106
    Abstract: The present invention concerns uses of immune modulating and immune suppressing peptides from human endogenous retroviruses. In particular, the present invention concerns a use of an immune suppressive peptide for immune suppression and for reduction of inflammation.
    Type: Application
    Filed: September 30, 2016
    Publication date: February 7, 2019
    Applicant: AIMVION A/S
    Inventors: Magdalena Janina Laska, Anne Margrethe Troldborg, Kristian Stengaard-Pedersen, Shervin Bahrami
  • ASTEXIN PEPTIDES
    Publication number: 20190040107
    Abstract: Provided are astexin-1, astexin-2 and astexin-3 lasso peptides, which are based on sequences identified in Asticcacaulis 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 Asticcacaulis 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: Application
    Filed: August 7, 2018
    Publication date: February 7, 2019
    Applicant: The Trustees of Princeton University
    Inventors: A. James Link, Mikhail O. Maksimov
  • VACCINE AND METHODS FOR DETECTING AND PREVENTING FILARIASIS
    Publication number: 20190040108
    Abstract: The present invention is a multivalent vaccine for immunizing an animal against filariasis. In some embodiments, the antigens of the multivalent vaccine are protein-based, DNA-based, or a combination thereof. This invention also provides a method and kit for detecting a filarial nematode and determining vaccine efficacy.
    Type: Application
    Filed: August 29, 2018
    Publication date: February 7, 2019
    Inventor: Ramaswamy Kalyanasundaram