Patents Issued in August 2, 2018
  • METHODS FOR INHIBITING NATIVE AND PROMISCUOUS UPTAKE OF MONOAMINE NEUROTRANSMITTERS
    Publication number: 20180215710
    Abstract: The present invention relates to methods of inhibiting native and promiscuous uptake of biogenic amine neurotransmitters with triple reuptake inhibitors in the treatment of conditions affected by monoamine neurotransmitters.
    Type: Application
    Filed: September 8, 2017
    Publication date: August 2, 2018
    Inventors: Anthony McKinney, Frank Bymaster
  • DOPANT FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE
    Publication number: 20180215711
    Abstract: The present invention relates to a dopant for an organic optoelectronic device represented by Chemical Formula 1, and to an organic optoelectronic device and a display device comprising the dopant.
    Type: Application
    Filed: October 26, 2015
    Publication date: August 2, 2018
    Applicant: SAMSUNG SDI CO., LTD.
    Inventors: Sangshin LEE, Eun Sun YU, Jun Yeob LEE, Yong Joo CHO
  • SMALL MOLECULE ANDROGEN RECEPTOR INHIBITORS AND METHODS OF USE THEREOF
    Publication number: 20180215712
    Abstract: Small molecule carbazole compounds for use as androgen receptor inhibitors are provided herein. Also provided herein are methods for using the carbazole compounds in treating prostate cancer, including castration-resistant prostate cancer and enzalutamide-resistant prostate cancer. The methods include administering to a subject an effective amount of a compound or composition as described herein.
    Type: Application
    Filed: August 2, 2016
    Publication date: August 2, 2018
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton L. Brown, Shujie Hou, Partha Banerjee, Karishma Amin
  • AMINOBENZAMIDE DERIVATIVES AS USEFUL AGENTS FOR CONTROLLING ANIMAL PARASITES
    Publication number: 20180215713
    Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.
    Type: Application
    Filed: March 28, 2018
    Publication date: August 2, 2018
    Inventors: Ulrich GÖRGENS, Akihiko YANAGI, Katsuaki WADA, Tetsuya MURATA, Yukiyoshi WATANABE, Jun MIHARA, Koichi ARAKI
  • A Process for Preparing Indacaterol and Salts Thereof
    Publication number: 20180215714
    Abstract: The present invention relates to a process for preparing indacaterol or salts thereof. The process comprises of forming compound of Formula 1 by reacting compound of Formula 2 and compound of Formula 3 in the presence of a solvent to Form compound of Formula 4, which on removal of the protecting groups forms compound of Formula 1.
    Type: Application
    Filed: August 20, 2015
    Publication date: August 2, 2018
    Inventor: G. Pratap REDDY
  • SOLID STATE FORMS OF NETARSUDIL MESYLATE
    Publication number: 20180215715
    Abstract: Disclosed are solid state forms of Netarsudil mesylate, processes for preparation thereof, uses thereof, and pharmaceutical compositions thereof.
    Type: Application
    Filed: February 1, 2018
    Publication date: August 2, 2018
    Inventors: Alexander Mainfeld, Sharona Shachan-tov, Ariel Mittelman, Rotem Sella-Erez, Yifat Ronen, Tamar Nidam
  • AROMATIC COMPOUND PRODUCTION METHOD
    Publication number: 20180215716
    Abstract: Provided is a method for producing an aromatic compound, which can produce a particular aromatic compound at high yield and can be industrially utilized. According to the invention, there is provided a method for producing an aromatic compound, including an aromatization reaction which includes reacting an oxime compound represented by Formula (1) with an acylating agent in the presence of a hydroquinone compound and a palladium compound, and thus obtaining an aromatic compound.
    Type: Application
    Filed: March 29, 2018
    Publication date: August 2, 2018
    Applicant: FUJIFILM Corporation
    Inventor: Motomasa TAKAHASHI
  • FUSED IMIDAZOLES AS MIDH1 INHIBITORS
    Publication number: 20180215717
    Abstract: The present invention relates to compounds of general formula (I): in which R1, R2, R3, R4, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: July 14, 2016
    Publication date: August 2, 2018
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Olaf PANKNIN, Ingo HARTUNG, Hartmut REHWINKEL, Duy NGUYEN, Ludwig ZORN, Petra HELFRICH, Katja ZIMMERMANN, Roland NEUHAUS
  • PYRIDAZIN-3(2H)-ONE DERIVATIVES AS MONOAMINE OXIDASE SELECTIVE ISOFORM B INHIBITORS (As Amended)
    Publication number: 20180215718
    Abstract: The present invention refers to pyridazin-3(2H)-one derivatives of general structure I, II and III, which are selective MAO-B inhibitors, and to the use thereof for preparing medicaments intended to treat disorders derived from MAO-B hyperactivity, particularly degenerative disorders of the central nervous system (CNS), such as Parkinson's disease (PD), Alzheimer's disease (AD) and other dementias. These are pyridazin-3(2H)-one derivatives having dithiocarbamate moieties bonded to position 4, 5 or 6 through an alkyl chain of variable length (n=1, 2, 3). This invention is also directed to the preparation of said compounds.
    Type: Application
    Filed: March 3, 2015
    Publication date: August 2, 2018
    Applicants: UNIVERSIDADE DE VIGO, UNIVERSIDADE DE SANTIAGO DE COMPOSTELA
    Inventors: Mª del Carmen TERÁN MOLDES, Pedro BESADA PEREIRA, Tamara COSTAS CAAMAÑO, Mª del Carmen COSTAS LAGO, Noemí VILA MOLARES, Dolores VIÑA CASTELAO
  • SIK INHIBITOR FOR USE IN A METHOD OF TREATING AN INFLAMMATORY AND/OR IMMUNE DISORDER
    Publication number: 20180215719
    Abstract: The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.
    Type: Application
    Filed: May 26, 2017
    Publication date: August 2, 2018
    Applicants: Dana-Farber Cancer Institute, Inc., University Court of the University of Dundee
    Inventors: Philip Cohen, Kristopher Clark, Hwan Geun Choi, Nathanael S. Gray
  • PYRIMIDINES AND USES THEREOF
    Publication number: 20180215720
    Abstract: The various examples presented herein are directed to compounds of the Formula: wherein R1-R5 are defined herein, and uses of such compounds to, among other things, inhibit an immune response in a subject.
    Type: Application
    Filed: January 25, 2018
    Publication date: August 2, 2018
    Inventors: Sunil Abraham David, Mallesh Beesu
  • TEAD TRANSCRIPTION FACTOR AUTOPALMITOYLATION INHIBITORS
    Publication number: 20180215721
    Abstract: The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.
    Type: Application
    Filed: September 23, 2016
    Publication date: August 2, 2018
    Inventor: Xu Wu
  • PROCESS FOR THE PREPARATION OF ISOCARBOXAZID
    Publication number: 20180215722
    Abstract: This invention relates to a novel chemical process for the synthesis of N?-benzyl-5-methylisoxazole-3-carbohydrazide (Isocarboxazid) which comprises reacting 5-methyl-3-isoxazole carboxylic acid ester with benzylhydrazine or a salt thereof in an aprotic organic solvent and in the presence of an organic base.
    Type: Application
    Filed: July 27, 2016
    Publication date: August 2, 2018
    Inventors: Carla De Faveri, Florian Anton Martin Huber, Nicola Antolini
  • Substituted Hydrophobic Benzene Sulfonamide Thiazole Compounds for Use in Treating Cancer
    Publication number: 20180215723
    Abstract: The present invention relates to compound of general formula (I) R1 is selected from H, aryl and alkyl, R2 is selected from H, alkyl, aryl and CO—R6; R3 is selected from H, halogen, alkyl, alkenyl, alkynyl, aryl, NHR7, NR7R8, OR7 and SR7; R4 is selected from (C6-C12) alkyl, (C2-C12) alkenyl, (C2-C12) alkynyl and (C6-C10) aryl, R5 represents H, R6, aryl, OH, OR6, O-aryl, SH, SR6, S-aryl, CN, NO2, CF3, COOR6, SO2NR6R7, CONR6R7, NH2, NHR6, NH-aryl, NR6R7, NHCOR6 or aminoacyl; R6 is alkyl optionally substituted with halogen, OH, SH, NH2, O-alkyl, S-alkyl, NH-alkyl or NH-di(alkyl); R7 and R8 identical or different are H or alkyl optionally substituted with halogen, OH, SH, NH2, O-alkyl, S-alkyl, NH-alkyl or NH-di (alkyl), their pharmaceutically acceptable salts and/or isomers, tautomers, solvates or isotopic variations thereof. The compounds are useful for the treatment of cancers.
    Type: Application
    Filed: July 22, 2016
    Publication date: August 2, 2018
    Inventors: Stephane Rocchi, Rachid Benhida, Robert Ballotti, Magali Plaisant, Cyril Ronco, Antoine Millet
  • PROCESS FOR PREPARING FURAN-2,5-DICARBOXYLIC ACID
    Publication number: 20180215724
    Abstract: A process for preparing furan-2,5-dicarboxylic acid is disclosed. The process includes the following steps: preparing or providing a starting mixture including 5-(hydroxy-methyl)furfural (HMF), 5,5?-[oxy-bis(methylene)]bis-2-furfural (di-HMF), and water; subjecting said starting mixture to oxidation conditions in the presence of an oxygen-containing gas and a catalytically effective amount of a heterogeneous catalyst including one or more noble metals on a support so that both HMF and di-HMF react to give furane-2,5-dicarboxylic acid in a product mixture also including water and oxidation by-products. The use of a catalyst is also disclosed, the catalyst including one or more noble metals on a support as an heterogeneous oxidation catalyst for catalyzing in an aqueous starting mixture the reaction of both HMF and di-HMF to furane-2,5-dicarboxylic acid.
    Type: Application
    Filed: July 1, 2016
    Publication date: August 2, 2018
    Inventors: Alvaro Gordillo, Holger Werhan, Richard Dehn, Benoit Blank, Joaquim Henrique Teles, Stephan A Schunk, Markus Piepenbrink, Rene Backes, Lei Zhang
  • PURIFYING CRUDE FURAN 2,5-DICARBOXYLIC ACID BY HYDROGENATION AND A PURGE ZONE
    Publication number: 20180215725
    Abstract: A process for purifying a crude furan 2,5-dicarboxylic acid composition (cFDCA) by hydrogenation of a FDCA composition dissolved in a hydrogenation solvent such as water, and hydrogenating under mild conditions, such as at a temperature within a range of 130° C. to 225° C. by contacting the solvated FDCA composition with hydrogen in the presence of a hydrogenation catalyst under a hydrogen partial pressure within a range of 10 psi to 900 psi.
    Type: Application
    Filed: March 29, 2018
    Publication date: August 2, 2018
    Applicant: EASTMAN CHEMICAL COMPANY
    Inventors: MESFIN EJERSSA JANKA, Kenny Randolph Parker, Ashfaq Shahanawaz Shaikh, Lee Reynolds Partin, Charles Edwan Sumner, Shane Kipley Kirk
  • CYCLOALKENYL HYDROXAMIC ACID DERIVATIVES AND THEIR USE AS HISTONE DEACETYLASE INHIBITORS
    Publication number: 20180215726
    Abstract: The present invention provides compounds of formula (I): or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them.
    Type: Application
    Filed: January 24, 2018
    Publication date: August 2, 2018
    Applicant: The Broad Institute, Inc.
    Inventors: Edward Holson, Fanny Lazzaro, David Olson, Florence Fevrier Wagner, Michel Weiwer
  • LYSYL OXIDASE-LIKE 2 INHIBITORS AND USES THEREOF
    Publication number: 20180215727
    Abstract: Described herein are compounds that are LOXL2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with LOXL2 activity.
    Type: Application
    Filed: July 18, 2016
    Publication date: August 2, 2018
    Inventors: Martin W. ROWBOTTOM, John Howard HUTCHINSON
  • Benzodiazepine Derivatives As CCK2/Gastrin Receptor Antagonists
    Publication number: 20180215728
    Abstract: The invention relates to benzodiazepine derivatives of formula (A) useful as CCK2/gastrin receptor antagonists, their preparation and their use in the treatment or prevention of disorders associated with CCK2/gastrin receptors, disorders caused by or associated with hypergastrinaemia, and gastric acid-related disorders.
    Type: Application
    Filed: August 7, 2015
    Publication date: August 2, 2018
    Inventors: Malcolm James Boyce, Liv Thomsen, Donald Alan Gilbert, David Wood
  • NK 1 ANTAGONISTS
    Publication number: 20180215729
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: March 28, 2018
    Publication date: August 2, 2018
    Inventors: Anandan PALANI, Xianhai HUANG, Dong XIAO, Sunil PALIWAL, Hon-Chung TSUI, Michelle Laci WROBLESKI, Ashwin U. RAO, Cheng WANG, Sapna S. SHAH, Neng-Yang SHIH
  • AZOLOPYRIMIDINE FOR THE TREATMENT OF CANCER-RELATED DISORDERS
    Publication number: 20180215730
    Abstract: Compound that is an inhibitor of at least one of the A2A and A2B adenosine receptors, and compositions containing the compound and methods for synthesizing the compound, are described herein. The use of such compound and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.
    Type: Application
    Filed: January 19, 2018
    Publication date: August 2, 2018
    Inventors: Joel BEATTY, Laurent DEBIEN, Jenna JEFFREY, Manmohan Reddy LELETI, Debashis MANDAL, Dillon MILES, Jay POWERS, Brandon ROSEN, Ehesan SHARIF, Rhiannon THOMAS-TRAN
  • CEREBLON LIGANDS AND BIFUNCTIONAL COMPOUNDS COMPRISING THE SAME
    Publication number: 20180215731
    Abstract: The description relates to cereblon E3 ligase binding compounds, including bifunctional compounds comprising the same, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present disclosure. In particular, the description provides compounds, which contain on one end a ligand which binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. Compounds can be synthesized that exhibit a broad range of pharmacological activities consistent with the degradation/inhibition of targeted polypeptides of nearly any type.
    Type: Application
    Filed: January 31, 2018
    Publication date: August 2, 2018
    Inventors: Andrew P. Crew, Michael Berlin, Hanqing Dong, Keith R. Homberger, Yimin Qian, Lawrence B. Snyder, Jing Wang, Kurt Zimmermann
  • BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS
    Publication number: 20180215732
    Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Application
    Filed: September 5, 2017
    Publication date: August 2, 2018
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • POLYMORPHS OF SELINEXOR
    Publication number: 20180215733
    Abstract: The present invention relates to crystalline forms of the compound represented by Structural Formula I, and compositions comprising crystalline forms of the compound represented by Structural Formula I described herein. The crystalline forms of the compound of Structural Formula I and compositions comprising the crystalline forms of the compound of Structural Formula I provided herein, in particular, single crystalline Form A, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders associated with CRM1 activity, including cancer. Also described herein are methods for preparing the compound of Structural Formula I and its single crystalline forms.
    Type: Application
    Filed: August 14, 2015
    Publication date: August 2, 2018
    Inventors: Brian C. Austad, David G. Roe
  • PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS AND THEIR THERAPEUTICAL APPLICATIONS
    Publication number: 20180215734
    Abstract: The present invention provides kinase inhibitors with anti-proliferative activity comprising substituted pyrimidine derivatives and pharmaceutically-acceptable formulations thereof. In addition, the invention provides methods for making novel compounds and methods for using the compounds.
    Type: Application
    Filed: February 29, 2016
    Publication date: August 2, 2018
    Inventors: Chunlin Tao, Qinwei Wang, Laxman Nallan, David Ho, Tulay Polat, Forrest Arp, Paul Weingarten
  • METHOD FOR PREPARING METHYL (Z)-3-[[4-[METHYL[2-(4-METHYL-1-PIPERAZINYL)ACETYL]AMINO]PHEHYL]AMINO]PHENYLMETHYLENE)-OXINDOLE-6-CARBOXYLATE (INTEDANIB, NINTEDANIB)
    Publication number: 20180215735
    Abstract: The invention relates to a method of synthesizing methyl (Z)-3-[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl] amino]phenylmethylene)-oxindole-6-carboxylate of formula (1), known under the generic name of intedanib or nintedanib. The present method comprises a) a reaction of methyl oxindole-6-carboxylate with acetic anhydride at a temperature of 130-140° C.
    Type: Application
    Filed: July 28, 2016
    Publication date: August 2, 2018
    Applicant: Zentiva k.s.
    Inventor: Ludek MECA
  • BISAMIDINIUM-BASED INHIBITORS FOR THE TREATMENT OF MYOTONIC DYSTROPHY
    Publication number: 20180215736
    Abstract: The invention provides compounds, compositions and therapeutic methods. The compounds and compositions can be used for the treatment of myotonic dystrophy. The compounds can selectively bind to CUG repeats in RNA, or to CTG repeats in DNA, and inhibit replication of the nucleic acids. RNA-targeted therapeutic agents for the treatment of myotonic dystrophy type 1 (DM1) are described. In one embodiment, two bisamidinium ligands are linked using “click” chemistry to form a heterodimer that is a potent inhibitor of the MBNL1-rCUGexp complex (KI=25±8 nM), is relatively non-toxic to HeLa cells, dissolves nuclear foci, corrects >80% of the IR misregulated alternative splicing in DM1 model cells (1 ?M), and shows improvement of disease phenotypes in a DM1 Drosophila model.
    Type: Application
    Filed: August 10, 2015
    Publication date: August 2, 2018
    Applicant: The Board of Trustees of the University of lllinois
    Inventors: Steven C. Zimmerman, Long M. Luu, Lien T.T. Nguyen
  • SUBSTITUTED QUINAZOLINE COMPOUNDS AND PREPARATION AND USES THEREOF
    Publication number: 20180215737
    Abstract: The present invention relates quinazolinone compounds of Formula (I), as well as their preparation and uses, and further relates pharmaceutical compositions comprising these compounds and their uses; wherein the compounds or pharmaceutical compositions disclosed herein can be used for antagonizing the orexin receptor. The present invention also relates to uses of the compounds or pharmaceutical compositions in treating or preventing neurological and psychiatric disorders and diseases of the central nervous system in mammals, especially in humans.
    Type: Application
    Filed: July 14, 2016
    Publication date: August 2, 2018
    Applicant: Sunshine Lake Pharma Co., Ltd.
    Inventors: Yingjun ZHANG, Chuanfei JIN, Jinheng GAO, Ji ZHANG
  • INHIBITORS OF ACK1/TNK2 TYROSINE KINASE
    Publication number: 20180215738
    Abstract: Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of ACK1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new ACK1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I are disclosed.
    Type: Application
    Filed: August 2, 2016
    Publication date: August 2, 2018
    Inventors: Nupam P. Mahajan, Kiran N. Mahajan, Nicholas J. Lawrence, Harshani R. Lawrence
  • 2-(1-HETEROARYLPIPERAZIN-4-YL)METHYL-1,4-BENZODIOXANE DERIVATIVES AS ALPHA2C ANTAGONISTS
    Publication number: 20180215739
    Abstract: Compounds of formula I, wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2, or 3 N, O, or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.
    Type: Application
    Filed: June 3, 2016
    Publication date: August 2, 2018
    Applicant: ORION CORPORATION
    Inventors: Shouming WANG, Esa KUMPULAINEN, Jarmo PYSTYNEN, Antti POHJAKALLIO, Anssi HAIKARAINEN
  • PARA-SUBSTITUTED INDANYL AND TETRALINYL DERIVATIVES
    Publication number: 20180215740
    Abstract: Compounds of formula I and formula II their intermediates, as well as processes for the preparation of compounds of formula I and formula II, are disclosed. Use of compounds of formula I for the production of compounds of formula VI is also disclosed. Additionally, the use of compounds of formula I or formula II for the production of active compounds is disclosed.
    Type: Application
    Filed: July 13, 2016
    Publication date: August 2, 2018
    Inventors: Gopal Krishna Datta, Pascal Bindschaedler, Wolfgang von Deyn, Michael Rack, Karsten Koerber
  • 1-(Arylmethyl)quinazoline-2,4(1H,3H)-Diones as PARP Inhibitors and the Use Thereof
    Publication number: 20180215741
    Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones represented by the Formula (I): wherein Ar, R1-R6, are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
    Type: Application
    Filed: March 26, 2018
    Publication date: August 2, 2018
    Inventors: Sui Xiong CAI, Ye Edward TIAN, Haijun DONG, Qingbing XU, Lizhen WU, Lijun LIU, Yangzhen JIANG, Qingli BAO, Guoxiang WANG, Feng YIN, Chengyun GU, Xiuhua HU, Xiaozhu WANG, Sishun KANG, Shengzhi CHEN
  • PROTEASOME CHYMOTRYPSIN-LIKE INHIBITION USING PI-1833 ANALOGS
    Publication number: 20180215742
    Abstract: Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e.
    Type: Application
    Filed: January 29, 2018
    Publication date: August 2, 2018
    Inventors: Harshani R. Lawrence, Said M. Sebti, Sevil Ozcan
  • 1,3,4-OXADIAZOLE AMIDE DERIVATIVE COMPOUND AS HISTONE DEACETYLASE 6 INHIBITOR, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
    Publication number: 20180215743
    Abstract: The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds.
    Type: Application
    Filed: July 27, 2016
    Publication date: August 2, 2018
    Inventors: Jaekwang Lee, Moo Sung Ko, Younghue Han, Yuntae Kim
  • SALTS OF QUINAZOLINE DERIVATIVE OR CRYSTALS THEREOF, AND THE PROCESS FOR PRODUCING THEREOF
    Publication number: 20180215744
    Abstract: Crystals of a quinazoline derivative are provided. The present invention relates to an acid addition salt of a compound represented by Formula (I): a pharmaceutical composition containing it, and the like.
    Type: Application
    Filed: July 28, 2016
    Publication date: August 2, 2018
    Applicant: Shionogi & Co., Ltd.
    Inventors: Yukio TADA, Yuusuke TAMURA, Shuji YONEZAWA, Kenichi ISHIBASHI, Yuki MURAKAMI
  • KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
    Publication number: 20180215745
    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease.
    Type: Application
    Filed: December 21, 2017
    Publication date: August 2, 2018
    Inventors: Leticia M. Toledo-Sherman, Celia Dominguez, Michael Prime, William Mitchell, Naomi Went
  • POTASSIUM CHANNEL MODULATORS
    Publication number: 20180215746
    Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels.
    Type: Application
    Filed: March 28, 2018
    Publication date: August 2, 2018
    Inventors: Dipak Vasantrao Amrutkar, Kelly Foster, Thomas Amos Jacobsen, Martin R. Jefson, Gregg F. Keaney, Janus Schreiber Larsen, Karin Sandager Nielsen
  • COMPOUND HAVING EP2 AGONIST ACTIVITY
    Publication number: 20180215747
    Abstract: Provided is an EP2 agonist having excellent safety. A compound represented by general formula (I) (wherein all symbols are as defined in the description), a salt or N-oxide of the compound, or a solvate or prodrug of the compound or the salt or N-oxide has an EP2 agonist activity and is highly safe, and is therefore useful as a medicine, particularly a therapeutic agent for diseases associated with EP2 receptors, such as immune diseases, allergic diseases, neuronal death, dysmenorrhea, premature birth, miscarriage, baldness, ocular diseases, erectile dysfunction, arthritis, lung injury, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, bone diseases and cartilage injury.
    Type: Application
    Filed: July 22, 2016
    Publication date: August 2, 2018
    Applicant: ONO Pharmaceutical Co., Ltd.
    Inventors: Seiji OGAWA, Toshihide WATANABE, Isamu SUGIMOTO, Kousuke TANI, Kazumi MORIYUKI, Yoshikazu GOTO, Shinsaku YAMANE
  • EPOTHILONE B AND DICTYOSTATIN ANALOGS, THEIR PREPARATION AND USE
    Publication number: 20180215748
    Abstract: A compound having the structure:
    Type: Application
    Filed: July 22, 2016
    Publication date: August 2, 2018
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: James Leighton, Stephen Ho, Corinne Foley
  • DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE
    Publication number: 20180215749
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Application
    Filed: March 16, 2018
    Publication date: August 2, 2018
    Inventors: Mitchell A. deLong, Jill M. Sturdivant, Susan M. Royalty
  • Novel Aminothiazole Compounds and Methods Using Same
    Publication number: 20180215750
    Abstract: The present invention includes novel aminothiazole compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
    Type: Application
    Filed: July 21, 2016
    Publication date: August 2, 2018
    Inventors: Jean-Pierre J. Issa, Hanghang Zhang, Magid Abu-Gharbia, Wayne E. Childers, George C. Morton
  • 5-METHYL-1,2,4-OXADIAZOL-3-YL COMPOUNDS
    Publication number: 20180215751
    Abstract: The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treatment of neurodegenerative diseases and disorders, such as Alzheimer's disease.
    Type: Application
    Filed: January 19, 2018
    Publication date: August 2, 2018
    Applicant: Eli Lilly and Company
    Inventors: Nicolas Jacques Francois Dreyfus, Peter James Lindsay-Scott
  • TETRAHYDRO-AZEPINOQUINOLINES AS AGONISTS OF THE 5-HT2C RECEPTOR
    Publication number: 20180215752
    Abstract: Certain tetrahydro-azepinoquinolines of structural formula I are agonists of the mammalian 5-HT2c receptor, and, in particular, are selective agonists of the mammalian 5-HT2c receptor. The compounds of the present invention are therefore useful for the treatment, control, or prevention of diseases, conditions, or disorders responsive to stimulation of the 5-HT2c receptor, such as obesity, obesity-related conditions, and certain CNS-related disorders, including schizophrenia and depression. They are also useful as aids for tobacco smoking cessation.
    Type: Application
    Filed: August 26, 2015
    Publication date: August 2, 2018
    Applicant: Sunnylife Pharma, Inc.
    Inventors: Jonathan A. Groeper, Xibin Liao, Zhijian Lu
  • 2-(1H-INDAZOL-3-YL)-1H-IMIDAZO[4,5-C]PYRIDINE AND THERAPEUTIC USES THEREOF
    Publication number: 20180215753
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: September 27, 2017
    Publication date: August 2, 2018
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • 1-SUBSTITUTED 1,2,3,4-TETRAHYDRO-1,7-NAPHTHYRIDIN-8-AMINE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR ANTAGONISTS
    Publication number: 20180215754
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof has an EP4 receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of EP4 receptor associated diseases (e.g., rheumatoid arthritis, aortic aneurysm (e.g. abdominal aortic aneurysm, thoracic aortic aneurysm, thoracoabdominal aortic aneurysm etc.), endometriosis, ankylosing spondylitis, inflammatory breast cancer etc.) and the like.
    Type: Application
    Filed: July 26, 2016
    Publication date: August 2, 2018
    Inventors: Dinesh BARAWKAR, Anil M DESHPANDE, Santosh PATIL, Yogesh WAMAN, Anil PANMAND, Dilip JADHAV, Bheemashankar KULKARNI
  • FACTOR XIA MACROCYCLIC INHIBITORS BEARING ALKYL OR CYCLOALKYL P2' MOIETIES
    Publication number: 20180215755
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: July 28, 2016
    Publication date: August 2, 2018
    Inventors: Kumar Balashanmuga Pabbisetty, James R. Corte, Andrew K. Dilger, William R. Ewing, Yeheng Zhu
  • PROCESSES FOR PREPARING AN FGFR INHIBITOR
    Publication number: 20180215756
    Abstract: Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.
    Type: Application
    Filed: August 10, 2016
    Publication date: August 2, 2018
    Applicant: Principia Biopharma, Inc.
    Inventors: Jiang ZHU, Mohammad MASJEDIZADEH
  • COMPOUNDS AND METHODS FOR INHIBITING FASCIN
    Publication number: 20180215757
    Abstract: Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof.
    Type: Application
    Filed: December 21, 2017
    Publication date: August 2, 2018
    Inventors: Xin-Yun Huang, Christy Young Shue
  • TYROSINE AMIDE DERIVATIVES AS RHO- KINASE INHIBITORS
    Publication number: 20180215758
    Abstract: Bicyclic dihydropyrimidine-carboxamide compounds of formula I described herein inhibit Rho Kinase and may be used for the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Type: Application
    Filed: January 30, 2018
    Publication date: August 2, 2018
    Applicant: CHIESI FARMACEUTICI S.P.A.
    Inventors: Alessandro Accetta, Fabio Rancati, Anna Maria Capelli, David Edward Clark, Patrizia Tisselli, Christine Edwards, Gurdip Bhalay, Arnaud Jean Francois Auguste Cheguillaume
  • BICYCLIC INHIBITORS OF HISTONE DEACETYLASE
    Publication number: 20180215759
    Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g., HDAC2).
    Type: Application
    Filed: March 23, 2018
    Publication date: August 2, 2018
    Inventors: Nathan Oliver Fuller, John A. Lowe, III