Patents Issued in June 1, 2017
  • Publication number: 20170152237
    Abstract: The present invention provides a process for the treatment of a liquid first furan stream comprising furan and carbon monoxide, said process comprising the steps of: i) contacting said first furan stream with a CO-lean first gaseous stream; and ii) stripping at least a portion of the carbon monoxide in the first furan stream into the first gaseous stream to produce a second furan stream comprising less carbon monoxide than the first furan stream and a CO-enriched second gaseous stream.
    Type: Application
    Filed: March 26, 2015
    Publication date: June 1, 2017
    Inventors: Sipke Hidde WADMAN, Jean Paul Andre Marie Joseph Ghislain LANGE
  • Publication number: 20170152238
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Application
    Filed: August 4, 2016
    Publication date: June 1, 2017
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20170152239
    Abstract: This invention relates to compounds of general formula in which R1, R2, R6, U, V, W, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, pharmaceutical compositions containing such compounds and salts, and to methods of using such compounds, salts and compositions.
    Type: Application
    Filed: February 6, 2017
    Publication date: June 1, 2017
    Applicant: Pfizer Inc.
    Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCALPINE, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES
  • Publication number: 20170152240
    Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
    Type: Application
    Filed: February 9, 2017
    Publication date: June 1, 2017
    Inventors: Elizabeth M. Bacon, Gayatri Balan, Chien-Hung Chou, Christopher T. Clark, Jeromy J. Cottell, Musong Kim, Thorsten A. Kirschberg, John O. Link, Gary Phillips, Scott D. Schroeder, Neil H. Squires, Kirk L. Stevens, James G. Taylor, William J. Watkins, Nathan E. Wright, Sheila M. Zipfel
  • Publication number: 20170152241
    Abstract: The present invention provides: a bicyclic derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof; a preparation method therefor, a pharmaceutical composition comprising the same; and a use therefor. According to the present invention, the bicyclic compound derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof acts as a 5-HT4 receptor agonist, and thus can be usefully applied to the prevention or treatment of dysfunction in gastrointestinal motility, for example, gastrointestinal diseases such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, diabetic gastric atony and the like.
    Type: Application
    Filed: May 23, 2014
    Publication date: June 1, 2017
    Inventors: Jae Young SIM, Myung Hun CHA, Tae Kyun KIM, Young Ae YOON, Dong Hoon KIM
  • Publication number: 20170152242
    Abstract: Provided is a novel pyrazine derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof which is useful for treating or preventing diseases in which URAT1 is involved, including gout, hyperuricemia, hypertension, renal diseases such as interstitial nephritis and the like, diabetes, arteriosclerosis, Lesch-Nyhan syndrome, and the like.
    Type: Application
    Filed: May 12, 2015
    Publication date: June 1, 2017
    Applicant: TEIJIN PHARMA LIMITED
    Inventors: Akinobu MARUYAMA, Susumu TAKEUCHI, Yoshimasa TAKAHASHI
  • Publication number: 20170152243
    Abstract: Disclosed are polymorph of allisartan isoproxil and a pharmaceutical composition thereof. The polymorph is non-electrostatic, highly flowable and highly stable, and can be used for treating hypertension and complications thereof.
    Type: Application
    Filed: June 5, 2015
    Publication date: June 1, 2017
    Inventors: Duanming Tan, Jun Ou
  • Publication number: 20170152244
    Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where R1 can be hydro, methoxy, difluoromethoxy or trifluoromethoxy; R2 can be hydro, methoxy, trifluoromethoxy or trifluoromethyl; and R3 can be hydro or methoxy. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
    Type: Application
    Filed: November 23, 2016
    Publication date: June 1, 2017
    Applicants: AstraZeneca AB, Cancer Research Technology Limited
    Inventor: Maurice Raymond Verschoyle Finlay
  • Publication number: 20170152245
    Abstract: The present invention provides substituted benzimidazoles, pharmaceutical composition comprising the substituted benzimidazoles, and their use for preventing or treating a subject suffering from diseases or conditions associated with platelet activation aggregation and/or platelet activation.
    Type: Application
    Filed: November 25, 2016
    Publication date: June 1, 2017
    Applicant: National Taiwan University
    Inventors: Tur-Fu Huang, Shiu-Wen Huang, Jin-Cherng Lien, Sheng-Chu Kuo
  • Publication number: 20170152246
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: September 9, 2016
    Publication date: June 1, 2017
    Inventors: Rajinder Singh, Kin Tso, Jing Zhang, Matthew Duncton, Salvador Alvarez, Rao Kolluri, John Ramphal, Sacha Holland
  • Publication number: 20170152247
    Abstract: Compositions and methods for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Application
    Filed: January 25, 2017
    Publication date: June 1, 2017
    Applicant: Monsanto Technology LLC
    Inventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford
  • Publication number: 20170152248
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: February 13, 2017
    Publication date: June 1, 2017
    Inventors: Michael A. Poss, David R. Tortolani, Ashok Vinayak Purandare, John S. Tokarski, Christopher P. Mussari, Muthoni G. Kamau, Dharmpal S. Dodd, Ashvinikumar V. Gavai, Daniel O'Malley, Tram N. Huynh, Wayne Vaccaro, Lalgudi S. Harikrishnan
  • Publication number: 20170152249
    Abstract: The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.
    Type: Application
    Filed: June 10, 2016
    Publication date: June 1, 2017
    Inventors: Wojciech CZARDYBON, Krzysztof Brzózka, Michal Galezowski, Renata Windak, Mariusz Milik, Magdalena Zawadzka, Pawel Guzik, Ewelina Wincza, Marta Prokop, Katarzyna Wiklik, Aleksandra Sabiniarz, Wieslaw Marek Cholody, Raymond Horvath, Tomasz Rzymski
  • Publication number: 20170152250
    Abstract: The present invention relates to compounds of formula (I): wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 10, 2017
    Publication date: June 1, 2017
    Applicant: Syngenta Crop Protection LLC
    Inventors: Jerome Yves CASSAYRE, Peter RENOLD, Myriem EL QACEMI, Thomas PITTERNA, Julie Clementine TOUEG
  • Publication number: 20170152251
    Abstract: The present invention relates to a novel crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulfonate and a pharmaceutical composition containing the same. The novel crystalline form of a compound according to the present invention exhibits excellent stability even in high-temperature and humidity environments, and thus can be favorably used to prevent or treat diseases, such as thrombosis, myocardial infarction, atherosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty, and thromboembolism.
    Type: Application
    Filed: July 18, 2014
    Publication date: June 1, 2017
    Applicants: GREEN CROSS CORPORATION, LEGOCHEM BIOSCIENCES,INC.
    Inventors: Soongyu CHOI, Jungsub CHOI, So-Hyun YOON, Yoo Hoon KIM, Jae Yeon KIM, Suk Ho LEE, Young Lag CHO, Ho Young SONG, Dae Yon LEE, Sung Yoon BAEK, Sang Eun CHAE, Tae Kyo PARK, Sung Ho WOO, Yong Zu KIM
  • Publication number: 20170152252
    Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.
    Type: Application
    Filed: February 13, 2017
    Publication date: June 1, 2017
    Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
  • Publication number: 20170152253
    Abstract: A process for preparing [(1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, by the resolution of racemic 4-oxo-1,2-cyclopentanedicarboxylic acid (V), said process comprising: (a) reacting 4-oxo-1,2-cyclopentanedicarboxylic acid (V) with brucine or (1R,2S)-(?)-ephedrine, thus preparing the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of (V), and (b) precipitating selectively the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of (1R,2R)-4-oxo-1,2-cyclopentanedicarboxylic acid II, while the bis-brucine or bis-(1R,2S)-(?)-ephedrine salt of [(1S,2S)-4-oxo-1,2-cyclopentanedicarboxylic acid stays in solution; (c) liberating the acid II by removal of brucine or (1R,2S)-(?)-ephedrine from the precipitated salt obtained in step (b).
    Type: Application
    Filed: February 10, 2017
    Publication date: June 1, 2017
    Applicant: Janssen Pharmaceuticals, Inc.
    Inventors: Dominic John Ormerod, Dominique Paul Michel Depre, Andras Horvath
  • Publication number: 20170152254
    Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl, 5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R1 can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R2 can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
    Type: Application
    Filed: November 29, 2016
    Publication date: June 1, 2017
    Applicants: AstraZeneca AB, Cancer Research Technology Limited
    Inventors: Johannes Wilhelmus Maria Nissink, Maurice Raymond Verschoyle Finlay, Mark David Charles, Matt Wood
  • Publication number: 20170152255
    Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
    Type: Application
    Filed: November 29, 2016
    Publication date: June 1, 2017
    Applicants: AstraZeneca AB, Cancer Research Technology Limited
    Inventors: Johannes Wilhelmus Maria Nissink, Maurice Raymond Verschoyle Finlay, Mark David Charles
  • Publication number: 20170152256
    Abstract: The invention relates to novel 3,5-dichloro,4-(3,4-(cyclo-) alkoxyphenyl)-2-carbonyloxy)ethyl)pyridine compounds which are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
    Type: Application
    Filed: June 4, 2014
    Publication date: June 1, 2017
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele AMARI, Elisabetta ARMANI, Mauro RICCABONI, Andrea RIZZI, Charles BAKER-GLENN, Wesley BLACKABY, Herve VAN DE POEL, Ben WHITTAKER
  • Publication number: 20170152257
    Abstract: A phenanthroindolizidine and phenanthroquinolizidine alkaloid having a hydroxyl group on the phenanthrene ring thereof was synthesized, which exhibits potent activity as an anticancer agent against, such as breast cancer, lung cancer, and prostate cancer.
    Type: Application
    Filed: February 4, 2016
    Publication date: June 1, 2017
    Applicant: CHINA MEDICAL UNIVERSITY
    Inventors: TA-HSIEN CHUANG, CHIEN-FU LI, CHIA-CHEN TSAI, CHI-FEN CHANG, CHIEH-YU PENG
  • Publication number: 20170152258
    Abstract: The present invention relates to pyridopyrazine compounds of formula (I), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, L, m, p and W are as defined in the specification.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 1, 2017
    Inventors: Wei-Guo SU, Wei DENG
  • Publication number: 20170152259
    Abstract: Provided is a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein X is selected from a 3-9 membered carbon ring or a ring which is formed by 3-9 membered carbocyclic ring fused with benzo ring, and a 4-10 membered heterocyclic ring or a ring which is formed by 4-10 membered heterocyclic ring fused with benzo ring; Y and Z are independently selected from 4-9 membered saturated heterocyclic rings respectively; R1-3 are independently selected from H, F, Cl, Br, I, CN, OH, SH, NH2, CHO, COOH respectively, or selected from the group, optionally substituted by R01, consisting of C1-10 alkyl, C1-10 heteroalkyl, C3-10 cyclohydrocarbyl, C3-10 heterocyclohydrocarbyl, C1-10 alkyl substituted by C3-10 cyclohydrocarbyl or C3-10 heterocyclohydrocarbyl, and C1-10 heteroalkyl substituted by C3-10 cyclohydrocarbyl or C3-10 heterocyclohydrocarbyl.
    Type: Application
    Filed: May 18, 2015
    Publication date: June 1, 2017
    Inventors: Zhaozhong DING, Guanghua LAI, Shuhui CHEN, Xiaobing YAN
  • Publication number: 20170152260
    Abstract: Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.
    Type: Application
    Filed: December 15, 2016
    Publication date: June 1, 2017
    Applicant: Board of Regents, The University of Texas System
    Inventors: Jia ZHOU, Haijun CHEN, Qiang SHEN
  • Publication number: 20170152261
    Abstract: The invention provides a series of bioactive small molecules that target expanded r(CGG) repeats, termed r(CGG)exp, that causes Fragile X-associated Tremor Ataxia Syndrome (FXTAS). The compound was identified by using information on the chemotypes and RNA motifs that interact. Specifically. 9-hydroxy-5,11-dimethyl-2-(2-(piperidin-1-yl)ethyl)-6H-pyrido[4,3-b]carbazol-2-ium, binds the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Specifically, dimeric compounds incorporating two 9-hydroxyellipticine analog structures can even more potently bind the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Structure-activity relationships (SAR) studies determined that the alkylated pyridyl and phenolic side chains are important chemotypes that drive molecular recognition of r(CGG) repeats, such as r(CGG)exp.
    Type: Application
    Filed: January 23, 2017
    Publication date: June 1, 2017
    Inventors: Matthew D. Disney, Biao Liu, Jessica L. Childs-Disney, Wang-Yong Yang
  • Publication number: 20170152262
    Abstract: Provided herein are vinylogous thioester compounds and methods for using the compounds.
    Type: Application
    Filed: September 30, 2016
    Publication date: June 1, 2017
    Inventors: Yolanda Sanchez, Robert Allaway, Stephanie Bouley, Matthew Wood
  • Publication number: 20170152263
    Abstract: The present invention provides substituted indazole compound of formula (I) and pharmaceutically acceptable salts thereof, and their use to inhibit IRAK4 and/or for the treatment of diseases or disorders induced by IRAK4.
    Type: Application
    Filed: June 19, 2015
    Publication date: June 1, 2017
    Inventors: Venkateshwar Rao Gummadi, Susanta Samajdar
  • Publication number: 20170152264
    Abstract: The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
    Type: Application
    Filed: October 20, 2014
    Publication date: June 1, 2017
    Applicant: ETERNITY BIOSCIENCE INC.
    Inventors: Dong LIU, Minsheng ZHANG, Qiyue HU
  • Publication number: 20170152265
    Abstract: The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.
    Type: Application
    Filed: December 7, 2016
    Publication date: June 1, 2017
    Inventors: Richard Chesworth, Gerhard Koenig, Amy Ripka, Gideon Shapiro
  • Publication number: 20170152266
    Abstract: The invention describes pharmaceutical compounds and compositions comprised of a ligand attached to the opioid oxycodone, in a manner that substantially decreases or deters the potential for opioid abuse, addiction, illicit and illegal use, and overdose. When delivered at the proper dosage, the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent.
    Type: Application
    Filed: November 29, 2015
    Publication date: June 1, 2017
    Inventor: John K. Thottathil
  • Publication number: 20170152267
    Abstract: Compounds used as labels with properties comparable to known fluorescent compounds. The compounds are conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.
    Type: Application
    Filed: August 20, 2013
    Publication date: June 1, 2017
    Applicants: DYOMICS GMBH, PIERCE BIOTECHNOLOGY, INC.
    Inventors: Greg Hermanson, Peter T. Czerney, Surbhi Desai, Matthias S. Wenzel, Frank G. Lehmann, Marie Christine Nlend
  • Publication number: 20170152268
    Abstract: The present invention relates to a novel indene derivative, a preparation method for the same, and a pharmaceutical composition for preventing or treating retinal disease comprising the same as an active ingredient. The novel indene derivative of the present invention, the optical isomer of the same, or the pharmaceutically acceptable salts of the same have excellent inhibitory efficiency of receptor-interacting serine/threonine-protein kinase 1 (RIPK1).
    Type: Application
    Filed: January 27, 2017
    Publication date: June 1, 2017
    Inventors: Eunhee KIM, Sung-Eun YOO, Nam Sook KANG, Tae-Sung KOO, Min-Young PARK, Young-Hoon KIM, Hyun-Ju BAE, Jin-Woo KIM, Tae-Kyu IN, Choun-Ki JOO
  • Publication number: 20170152269
    Abstract: The present invention provides a fused bicyclic compound according to formula (H) or a pharmaceutically acceptable salt thereof, wherein L is —S— or —O—; M is —CH?, —N? or —CJ=, wherein J is a non-hydrogen monovalent group; and W, G0 and G1 are independently of each other a non-hydrogen monovalent group. The invention further provides a pharmaceutical composition comprising the compound, a method of synthesizing the compound, a method for inhibiting CDK(s), a method for treating a disease or disorder in a mammal mediated by or associated with cyclin-dependent kinase (CDK), and a use of the compound in the manufacturing of a medicament for treating a CDK-mediated disease or disorder.
    Type: Application
    Filed: February 13, 2017
    Publication date: June 1, 2017
    Applicant: ANONCO SCIENCES, INC.
    Inventors: Jin Li, Liu Liu, Minmin Yang
  • Publication number: 20170152270
    Abstract: A pyridine compound represented by formula (1) that is useful as an insecticide is produced by reacting a compound represented by formula (2) and a compound represented by formula (3). In formula (2) L1 represents a halogen atom; R2, R3, R4, R5, and R6 represent chain hydrocarbon groups, etc., having 1-6 carbon atoms optionally substituted by fluorine atoms; A1 represents —NR7—, an oxygen atom, or a sulfur atom; A2 represents a nitrogen atom or ?CR8—; and R7 and R8 represent C1-6 chain hydrocarbon groups or hydrogen atoms. In formula (3) M+ represents a sodium ion, a potassium ion, or a lithium ion.
    Type: Application
    Filed: May 29, 2015
    Publication date: June 1, 2017
    Inventors: Takayuki WAKAMATSU, Rika KASAI
  • Publication number: 20170152271
    Abstract: The present invention relates to the use of a class of novel isothiazolo[4,3-b]pyridine derivatives as well as to pharmaceutical compositions comprising one or more of said isothiazolo[4,3-b]pyridine derivatives and one or more pharmaceutically acceptable excipients as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as viral diseases.
    Type: Application
    Filed: July 23, 2015
    Publication date: June 1, 2017
    Applicant: Katholieke Universiteit Leuven
    Inventors: Steven De Jonghe, Piet Herdewyn, Elena Bekerman, Shirit Einav, Gregory Neveu
  • Publication number: 20170152272
    Abstract: The disclosure provides an improved synthesis for a zinc-lysine complex having the formula [Zn(C6H14N2O2)2Cl]+Cl ?, in which a zinc compound selected from ZnO and ZnCl2, is reacted with a lysine compound selected from lysine and lysineHCl, in aqueous acid. The disclosure also provides oral care and personal care compositions comprising the complex prepared by the synthesis, and methods of using these complexes and compositions.
    Type: Application
    Filed: June 18, 2014
    Publication date: June 1, 2017
    Applicant: Colgate-Palmolive Company
    Inventors: Michael FITZGERALD, Joseph CONVERY, Harsh TRIVEDI, Lisa MANUS
  • Publication number: 20170152273
    Abstract: Topical pharmaceutical formulations, and methods of treating inflammatory conditions with these formulations, are disclosed.
    Type: Application
    Filed: November 30, 2016
    Publication date: June 1, 2017
    Applicant: Anacor Pharmaceuticals Inc.
    Inventors: Tejal Merchant, Dina Jean Coronado, Charles Edward Lee, Delphine Caroline Imbert, Sylvia Zarela Yep
  • Publication number: 20170152274
    Abstract: Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 1, 2017
    Applicant: Hangzhou DAC Biotech Co., Ltd.
    Inventors: Robert Yongxin ZHAO, Xing LI, Yuangyuang HUANG, Qingliang YANG
  • Publication number: 20170152275
    Abstract: The present invention relates to a novel compound represented by formula (1), or salt thereof, wherein R is hydroxy group or hydrogen atom; R1 and R2 are the same or different, and are each independently benzyl group which may have a substituent. The present invention provides therapeutically agents, which have remarkable stability against cytidine deaminase, a metabolic enzyme, can be absorbed in vivo by oral administration and inhibit protein synthesis by being incorporated easily into nucleic acid bio-synthesis in vivo for replacing injection agent (5-azacytidine or 2?-deoxy-5-azacytidine) used in clinic for treating myeloma.
    Type: Application
    Filed: November 18, 2016
    Publication date: June 1, 2017
    Applicant: OHARA PHARMACEUTICAL CO., LTD.
    Inventors: MAGOICHI SAKO, XIONG LUO
  • Publication number: 20170152276
    Abstract: Disclosed is a novel tenofovir disoproxil edisylate salt having the structure of Chemical Formula 1.
    Type: Application
    Filed: July 9, 2015
    Publication date: June 1, 2017
    Applicant: JW Pharmaceutical Corporation
    Inventors: Do-Kyu PYUN, Won-Kyoung LEE, Su-Ha PARK
  • Publication number: 20170152277
    Abstract: Disclosed herein is a method of forming a thin film. The method includes forming a niobium-containing film by using a niobium precursor composition and a reactant, the niobium precursor composition including a niobium compound represented by Formula (1): Nb(R5Cp)2(L)??Formula (1) (where each R is independently H, a C1 to C6 alkyl group, or R13Si, with each R1 being independently H or a C1 to C6 alkyl group, Cp is a cyclopentadienyl group, and L is selected from among formamidinates (NR, R?-fmd), amidinates (NR, R?, R?-amd), and guanidinates (NR, R?, NR?, R??-gnd)).
    Type: Application
    Filed: November 29, 2016
    Publication date: June 1, 2017
    Inventors: Jae-soon LIM, Gyu-hee PARK, Youn-joung CHO, Clement LANSALOT, Won-tae NOH, Julien LIEFFRIG, Joo-ho LEE
  • Publication number: 20170152278
    Abstract: A method of obtaining depolymerized lignin from biomass using a transition metal catalyst and a solvent mixture of organic solvent and water. The invention further relates to a composition obtainable by the method and the production of fuel.
    Type: Application
    Filed: November 27, 2014
    Publication date: June 1, 2017
    Inventors: Joseph SAMEC, Maxim GALKIN
  • Publication number: 20170152279
    Abstract: The invention relates to dendritic compounds, the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, processes for preparing the compounds, and methods of treating diseases or conditions in which it is desirable to inhibit ?-secretase.
    Type: Application
    Filed: November 28, 2013
    Publication date: June 1, 2017
    Inventors: Peter Charles Tyler, Olga Vladimirovna Zubkova, Jeremy E. Turnbull
  • Publication number: 20170152280
    Abstract: The present disclosure relates to scaphopetalone analogs, methods of making the analogs, and their uses.
    Type: Application
    Filed: September 30, 2016
    Publication date: June 1, 2017
    Inventors: Merritt B. Andrus, F. Brent Johnson, Mary Ruth Jaeger Greer, Rex G. Cates
  • Publication number: 20170152281
    Abstract: The invention provides and describes solid state 17?-ethynyl-androst-5-ene-3?,7?,17?-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-androst-5-ene-3?,7?,17?-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17?-ethynyl-androst-5-ene-3?,7?,17?-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-androst-5-ene-3?,7?,17?-triol and uses of such formulations in treating the described conditions.
    Type: Application
    Filed: November 10, 2016
    Publication date: June 1, 2017
    Applicant: NeurMedix, Inc.
    Inventors: Steven K. White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
  • Publication number: 20170152282
    Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 1, 2017
    Applicant: Washington University
    Inventors: Douglas Covey, Albert Jean Robichaud
  • Publication number: 20170152283
    Abstract: Disclosed are inhibitors of the farnesoid X receptor, for example of formula (I), wherein R1, R2, R4, X, Y, Z, m, and n are as defined herein, which are useful in treating or preventing obesity, type 2 diabetes/insulin resistance and non-alcoholic fatty liver disease in a mammal in need thereof. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, a method of method of inhibiting a farnesoid X receptor in a mammal, and a method of treating or preventing obesity in a mammal.
    Type: Application
    Filed: December 6, 2016
    Publication date: June 1, 2017
    Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Services, The Penn State Research Foundation
    Inventors: Frank J. Gonzalez, Changtao Jiang, Cen Xie, Andrew D. Patterson, Fei Li, James B. Mitchell, Shantu Amin, Dhimant Desai
  • Publication number: 20170152284
    Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17(20)-Z-vinylcyano-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: October 4, 2013
    Publication date: June 1, 2017
    Inventor: Douglas F. Covey
  • Publication number: 20170152285
    Abstract: The present invention is related to an extracting method of kuguacin, pharmaceutical composition comprising the kuguacin and use thereof, specifically related to a use of the kuguacin for treating periodontal diseases.
    Type: Application
    Filed: October 4, 2016
    Publication date: June 1, 2017
    Applicants: National Taiwan Normal University, Chang Gung Memorial Hospital, Keelung
    Inventors: Po-Jung Tsai, Wen-Cheng Huang, Tzung-Hsun Tsai, How-Ting Ying, Ya-Ling Hung
  • Publication number: 20170152286
    Abstract: The present disclosure relates to the design and generation of stapled helical peptides that perturb protein-protein interactions (PPIs). The methods disclosed herein for preparing stapled peptides involve providing a peptide having a first amino acid that is functionalized with a salicylaldehyde ester side group and a second amino acid functionalized with a 1,2-hydroxyl amine side group; reacting the first and second amino acids to generate an N,O-benzylidene acetal moiety; and performing acidolysis of the resultant N,O-benzylidene acetal moiety to generate the stapled peptide. In many forms, the stapled helical peptides described herein are not hydrophobic.
    Type: Application
    Filed: November 29, 2016
    Publication date: June 1, 2017
    Inventors: Xuechen Li, Chi-Lung Lee, Jiaochao Xu