Patents Issued in September 20, 2018
  • Born-Based Cycloaddition Catalysts and Methods for the Production of Bio-Based Terephthalic Acid, Isophthalic Acid and Poly (Ethylene Terephthalate)
    Publication number: 20180265468
    Abstract: Methods for producing cycloaddition products comprising: reacting a diene with a dienophile in the presence of one or more boron-based catalysts of Formula I or Formula II are provided. In particular, the methods can be used to prepare 4-methyl-3-cyclohexene-1-carboxylic acid and 3-methyl-3-cyclohexene-1-carboxylic acid, including bio-based versions thereof. The cycloaddition products can be advantageously used in the production of terephthalic acid and isophthalic acid, and ultimately, poly(ethylene terephthalate), and bio-based versions thereof.
    Type: Application
    Filed: September 23, 2016
    Publication date: September 20, 2018
    Inventors: John Wesley Frost, Peng Zhang
  • MALEIC ACID SALT OF A SILODOSIN INTERMEDIATE
    Publication number: 20180265469
    Abstract: The present invention relates to a salt of formula (I), the preparation method for preparing same, and the use thereof in the preparation of silodosin.
    Type: Application
    Filed: September 29, 2016
    Publication date: September 20, 2018
    Inventors: José Luis DEL RÍO PERICACHO, Xavier VILA TUSELL
  • Drier Composition and Use Thereof
    Publication number: 20180265470
    Abstract: The invention relates to a drier composition for an autoxidizable alkyd based coating composition, comprising: a) at least one Fe complex comprising Fe and at least one nitrogen donor ligand, wherein the nitrogen donor ligand is selected from tridentate, tetradentate, pentadentate and hexadentate nitrogen donor ligands; b) at least one metal salt of a carboxylic acid, wherein the metal is selected from Mn, Ce, V, and Cu; and c) at least one ligand comprising at least one moiety selected from 1,4,7-tri-azacyclononanyl, 2,2?-bipyridyl, 1,10-phenantrolinyl, imidazolyl, pyrazolyl, porphyrinyl, aliphatic, cycloaliphatic, and aromatic amines.
    Type: Application
    Filed: May 16, 2018
    Publication date: September 20, 2018
    Inventors: Tjian Hong Ang, John Weijnen
  • 4-(METHYLAMINOPHENOXY)PYRDIN-3-YL-BENZAMIDE DERIVATIVES FOR TREATING CANCER
    Publication number: 20180265471
    Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.
    Type: Application
    Filed: May 2, 2018
    Publication date: September 20, 2018
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Takashi NAKAGAWA, Makoto SAKAMOTO, Kazuya YAMAGUCHI, Yuki TERAUCHI, Masamichi SHIRAKURA, Yasuo HARADA, Yutaka KOJIMA, Takumi SUMIDA
  • PROCESS FOR PREPARING ARIPIPRAZOLE LAUROXIL AND INTERMEDIATES THEREOF
    Publication number: 20180265472
    Abstract: A process for preparing a compound of formula I?: or a pharmaceutically acceptable salt thereof, in which R represents optionally substituted or unsubstituted alkyl group, comprising reacting a compound of formula III: with a carboxylic acid in the presence of a coupling reagent and an organic solvent to obtain the compound of formula I?.
    Type: Application
    Filed: March 8, 2018
    Publication date: September 20, 2018
    Inventors: Tsung-Yu Hsiao, Yu-Hui Huang
  • CRYSTAL FORMS OF BEDAQUILINE FUMARATE AND PREPARATION METHODS THEREFOR
    Publication number: 20180265473
    Abstract: Provided are crystal forms I, II, and III of bedaquiline fumarate, and preparation methods thereof. The crystal forms have high purity, excellent physicochemical properties, and good stability. The preparation methods can effectively improve the quality of products, and are applicable to preparation and mass production of medicines.
    Type: Application
    Filed: October 20, 2015
    Publication date: September 20, 2018
    Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Jinyi Xu, Liang Zhang, Xiangyang Zhang, Xinzeng Wang, Jian Chai, Hongying Luo, Zhiqing Yang
  • POLYMORPHIC COMPOUNDS AND USES THEREOF
    Publication number: 20180265474
    Abstract: The present invention provides freebase and salt forms, and compositions and methods thereof, useful for treating various conditions, in which aldehyde toxicity is implicated in the pathogenesis, by the administration of small molecule therapeutics acting as a scavenger for toxic aldehydes.
    Type: Application
    Filed: March 16, 2018
    Publication date: September 20, 2018
    Inventors: Amanda BUIST, Eden FUCCI, Stephen G. MACHATHA, Osama SULEIMAN, Kate WITTERING
  • HALOGENATED QUINOLINE DERIVATIVES AS ANTIMICROBIAL AGENTS
    Publication number: 20180265475
    Abstract: The present invention provides halogenated quinoline derivatives, such as compounds of Formula (I) or (I?), and pharmaceutically acceptable salts thereof, and methods of preparing the halogenated quinoline derivatives. The halogenated quinoline derivatives are expected to be antimicrobial agents and may act through an iron(II)-dependent mode of action. The present invention also provides pharmaceutical compositions, kits, uses, and methods that involve the halogenated quinoline derivatives and may be useful in preventing or treating a microbial infection (e.g., a bacterial infection) in a subject, inhibiting the growth and/or reproduction of a microorganism (e.g., a bacterium), killing a microorganism (e.g., a bacterium), inhibiting the formation and/or growth of a biofilm, reducing or removing a biofilm, and/or disinfecting a surface.
    Type: Application
    Filed: September 23, 2016
    Publication date: September 20, 2018
    Applicant: University of Florida Research Foundation, Incorporated
    Inventors: Robert William Huigens, III, Akash Basak, Yasmeen Abouelhassan
  • CONDENSED RING DERIVATIVE, AND PREPARATION METHOD, INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
    Publication number: 20180265476
    Abstract: Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.
    Type: Application
    Filed: May 22, 2018
    Publication date: September 20, 2018
    Inventors: Zusheng XU, Nong ZHANG, Qingrui SUN, Tianzhi WU
  • SPIRO COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT COMPRISING SAME
    Publication number: 20180265477
    Abstract: The present specification provides a spiro structured compound and an organic light emitting device including the same.
    Type: Application
    Filed: September 30, 2016
    Publication date: September 20, 2018
    Applicant: LG Chem, Ltd.
    Inventors: Yongbum Cha, Jin Joo Kim, Sang Duk Suh
  • PRMT1 INHIBITORS AND USES THEREOF
    Publication number: 20180265478
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting PRMT1 activity. Methods of using the compounds for treating PRMT1-mediated disorders are also described.
    Type: Application
    Filed: December 21, 2017
    Publication date: September 20, 2018
    Inventors: Kevin Wayne Kuntz, Lorna Helen Mitchell, Gideon Shapiro, Richard Chesworth, Paula Ann Boriack-Sjodin
  • FATTY ACID SYNTHASE INHIBITORS AND METHODS OF USE
    Publication number: 20180265479
    Abstract: The present disclosure provides for methods of treating cancer in a subject. In certain embodiments, the method comprises administering a therapeutically effective amount of an inhibitor of fatty acid synthase, or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: March 19, 2018
    Publication date: September 20, 2018
    Inventors: Vivek KAUSHIK, Anandkrishnan IYER, Neelam AZAD
  • METHOD FOR PREPARING CONTRAST AGENT PRECURSOR
    Publication number: 20180265480
    Abstract: A method for preparing a contrast agent precursor is revealed. The method includes several steps. First dissolve di-tert-butyl 2,2?-(1,4,7-triazacyclononane-1,4-diyl)diacetate, benzyl-2-bromoacetate and an alkaline compound in a first solvent to perform a bimolecular nucleophilic substitution reaction and get a product. Then dissolve the product in a second solvent to get a solution and adjust the pH value of the solution. Next add an organic solvent when the solution becomes acid and then remove a first organic layer that contains the organic solvent. Adjust the solution to become an alkaline solution and add the organic solvent again to get a second organic layer containing the organic solvent. The second organic layer contains the final product, di-tert-butyl 2,2?-{7-[2-(benzyloxy)-2-oxyethyl-(1,4,7-triazacyclononane-1,4-diyl}-diacetate.
    Type: Application
    Filed: March 15, 2017
    Publication date: September 20, 2018
    Inventors: JHE-YU LIU, YU CHANG, CHENG-FANG HSU
  • METHOD FOR PREPARATION OF CERTAIN 1,5 DISUBSTITUTED TETRAZOLES
    Publication number: 20180265481
    Abstract: The invention discloses a method for the preparation of certain 1,5 disubstituted tetrazole and similar compounds starting from certain thioacetamides, which ultimately allows the preparation of these certain 1,5 disubstituted tetrazoles from readily available compounds such as acetophenone and similar compounds.
    Type: Application
    Filed: March 8, 2016
    Publication date: September 20, 2018
    Inventor: Florencio Zaragoza Doerwald
  • METHODS FOR PRODUCING VILOXAZINE SALTS AND NOVEL POLYMORPHS THEREOF
    Publication number: 20180265482
    Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
    Type: Application
    Filed: May 24, 2018
    Publication date: September 20, 2018
    Applicant: Supernus Pharmaceuticals, Inc.
    Inventors: Likan LIANG, Padmanabh P. BHATT, David DAIN, Jean-Philippe TAQUET, Aleksandr PECHENOV, Alexei TCHESNOKOV, Reynold MARIAUX
  • MICROBIOCIDAL OXADIAZOLE DERIVATIVES
    Publication number: 20180265483
    Abstract: Compounds of the formula (I) wherein, the substituents are as defined in claim 1, useful as a pesticides, especially as fungicides.
    Type: Application
    Filed: September 29, 2016
    Publication date: September 20, 2018
    Applicant: SYNGENTA PATRICIPATIONS AG
    Inventors: Daniel Stierli, Thomas Hoffman, Renaud Beaudegnies, Martin Pouliot
  • HEPATITIS B CORE PROTEIN MODULATORS
    Publication number: 20180265484
    Abstract: The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
    Type: Application
    Filed: September 15, 2016
    Publication date: September 20, 2018
    Inventors: William Turner, Hans Maag, Samson Francis
  • ORGANO-1-OXA-4-AZONIUM CYCLOHEXANE COMPOUNDS
    Publication number: 20180265485
    Abstract: Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.
    Type: Application
    Filed: May 16, 2018
    Publication date: September 20, 2018
    Inventors: Christopher P. Nicholas, Mark A. Miller, Melissa M. Galey, Benjamin D. Yuhas, Sesh Prabhakar
  • ORGANO-1-OXA-4-AZONIUM CYCLOHEXANE COMPOUNDS
    Publication number: 20180265486
    Abstract: Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. A substituted hydrocarbon is added to water to form a mixture, and a 1-oxa-4-azacyclohexane derivative is then added. The reaction mixture stirred until a solution containing the 1-oxa-4-azonium cyclohexane salt is obtained.
    Type: Application
    Filed: May 16, 2018
    Publication date: September 20, 2018
    Inventors: Christopher P. Nicholas, Mark A. Miller, Melissa M. Galey, Benjamin D. Yuhas, Sesh Prabhakar
  • SWEET TASTE MODULATORS
    Publication number: 20180265487
    Abstract: Sweet taste modulators for enhancing sweetness of an oral consumer product having a sweetener are described. The sweet taste modulators include 5-ethoxymethyl-2-furaldehyde, 2,3-dihydroxybenzoic acid, 2,4-dihydroxybenzoic acid, 2,5-dihydroxybenzoic acid, 2,6-dihydroxybenzoic acid, 3,4-dihydroxybenzoic acid, 3,5-dihydroxybenzoic acid, 2,3,4-trihydroxybenzoic acid, 2,4,6-trihydroxybenzoic acid and 3,4,5-trihydroxybenzoic acid, syringic aldehyde, sinapic aldehyde, ester of 5-hydroxymethylfurfural and vanillic acid, 4-hydrozybenzaldehyde, and 5-methoxymethylfurfural. A method of making 5-ethoxymethyl-2-furaldehyde and a method of making an oral consumer product are also described.
    Type: Application
    Filed: March 17, 2017
    Publication date: September 20, 2018
    Applicant: Altria Client Services LLC
    Inventors: Andrea Froschmeier, Thomas Hofmann, Christian Schuh
  • OXIDATION CHEMISTRY ON FURAN ALDEHYDES
    Publication number: 20180265488
    Abstract: Provided herein are methods of producing halomethylfuroic and acyloxymethylfuroic acid and ester compounds from furfural starting compounds. For example, 5-chloromethyl-2-furoic acid may be produced from 5-chloromethylfurfural, in the presence of various oxidants. Salts of the furoic acids may also be produced.
    Type: Application
    Filed: September 16, 2016
    Publication date: September 20, 2018
    Applicant: Micromidas, Inc.
    Inventors: Daniel R. HENTON, Makoto Nathanael MASUNO, Ryan L. SMITH, Alex B. WOOD, Dimitri A. HIRSCH-WEIL, Christian T. GORALSKI, Robert Joseph ARAIZA
  • NOVEL ANTICANCER AGENT
    Publication number: 20180265489
    Abstract: The problem of the present invention is to provide a useful prodrug compound of a naphthofuran compound. The present invention relates to a compound represented by the formula (IA): [wherein each symbol is as described in the DESCRIPTION] or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 23, 2018
    Publication date: September 20, 2018
    Applicants: Kyoto Pharmaceutical Industries, Ltd., Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshinobu YOSHIMURA, Masayasu KASAI, Yoshimichi SHOJI, Shigemitsu TAKEDA
  • METHODS FOR PRODUCING BERAPROST AND ITS DERIVATIVES
    Publication number: 20180265490
    Abstract: The present invention is directed to methods for preparing Beraprost and novel synthetic intermediates for Beraprost.
    Type: Application
    Filed: May 4, 2018
    Publication date: September 20, 2018
    Applicant: Lung Biotechnology PBC
    Inventors: Hitesh Batra, Sudersan M. Tuladhar, Sri Tummala, Raju Penmasta, David A. Walsh
  • INHIBITORS OF LYSINE SPECIFIC DEMETHYLASE-1
    Publication number: 20180265491
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: June 30, 2015
    Publication date: September 20, 2018
    Inventors: Young K. Chen, Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • ANTIFUNGAL COMPOUNDS AND PROCESSES FOR MAKING
    Publication number: 20180265492
    Abstract: Provided are polymorphic forms of compound 5 or 5*, or mixtures thereof, and polymorph forms of compound 14 or 14*, or mixtures thereof. Also provided are methods of preparing compound 5 or 5*, or mixtures thereof, and methods of preparing compound of 14 or 14*, or mixtures thereof, which are useful as antifungal agents. In particular, provided is new methodology for preparing polymorphs of the compounds described and substituted derivatives thereof.
    Type: Application
    Filed: September 16, 2016
    Publication date: September 20, 2018
    Inventors: David Dale Wirth, Christopher M. Yates
  • PROCESS FOR MAKING M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
    Publication number: 20180265493
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Application
    Filed: September 26, 2016
    Publication date: September 20, 2018
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited.
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS
    Publication number: 20180265494
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Application
    Filed: May 17, 2018
    Publication date: September 20, 2018
    Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
  • NEW CRYSTAL FORM OF NERATINIB MALEATE AND PREPARATION METHOD THEREFOR
    Publication number: 20180265495
    Abstract: The present invention relates to novel crystalline forms of Neratinib maleate and the preparation method thereof. The maleate novel crystalline forms of compound of Formula (I) in the present invention have high solubility, good stability, good processability, easy post-treatment process and other favorable properties. The preparation method is simple, low cost, and has an important value for future optimization and development of the drug.
    Type: Application
    Filed: January 8, 2016
    Publication date: September 20, 2018
    Applicant: CRYSTAL PHARMATECH CO., LTD
    Inventors: Minhua CHEN, Yanfeng ZHANG, Xiaojuan DIAO, Xiaoyu ZHANG
  • SUBSTITUTED QUINOLONE DERIVATIVES, OR PHARMACEUTICALLY ACCEPTABLE SALTS OR STEREOISOMERS THEREOF, AND PHARMACEUTICAL COMPOSITIONS AND USE THEREOF
    Publication number: 20180265496
    Abstract: Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.
    Type: Application
    Filed: August 18, 2016
    Publication date: September 20, 2018
    Applicants: JINAN UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES
    Inventors: Ke DING, Meiyu GENG, Li TAN, Jian DING, Zhang ZHANG, Jing AI, Xiaomei REN, Donglin GAO, Zhengchao TU, Xiaoyun LU, Dongmei ZHANG
  • PYRIMIDINYL-PYRIDYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF TREATING IRE1-RELATED DISEASES AND DISORDERS
    Publication number: 20180265497
    Abstract: Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I or I? structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I or I? compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: May 24, 2018
    Publication date: September 20, 2018
    Applicants: Genentech, Inc., The Regents of the University of California
    Inventors: Marie-Gabrielle Braun, Paul Gibbons, Wendy Lee, Cuong Ly, Joachim Rudolph, Jacob Schwarz, Avi Ashkenazi, Leo Fu, Tommy Lai, Fei Wang, Ramsay Beveridge, Liang Zhao
  • 1,4-DI-(4-METHYLTHIOPHENYL)-3-PHTALOYLAZETIDINE-2-ONE AND THE DERIVATIVES THEREOF
    Publication number: 20180265498
    Abstract: The present invention relates to a compound with formula (I) or a salt and/or a pharmaceutically acceptable solvate thereof, the method for preparing same as well as the uses thereof, in particular the therapeutic use thereof, mainly in the treatment of diseases associated with a hyperactivity of the endocannabinoid system.
    Type: Application
    Filed: September 23, 2016
    Publication date: September 20, 2018
    Applicants: Universite De Nantes, Universite de Bourgogne, Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Michel Robert, Stéphanie Troy-Fioramonti, Laurent Demizieux, Pascal DeGrace
  • BIARYL PIPERIDINE AMIDE COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20180265499
    Abstract: The present application is directed to biaryl piperidine amide compounds, or pharmaceutically acceptable salts, solvates, and prodrugs thereof, and methods of use thereof.
    Type: Application
    Filed: March 15, 2018
    Publication date: September 20, 2018
    Inventors: Michael P. SMOLINSKI, Sameer URGAONKAR, James Lindsay CLEMENTS, David G. HANGAUER, JR.
  • TETRAHYDROQUINOLINE SULFONAMIDE DERIVATIVES AS INVERSE AGONISTS OF RETINOID-RELATED ORPHAN RECEPTOR GAMMA (ROR GAMMA (T))
    Publication number: 20180265500
    Abstract: Tetrahydroquinoline sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma (ROR?t) are described. Pharmaceutical compositions including such compounds, as well as the use thereof for the topical and/or oral treatment of ROR?t receptor-mediated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described.
    Type: Application
    Filed: December 18, 2015
    Publication date: September 20, 2018
    Inventors: Branislav MUSICKI, Claire BOUIX-PETER, Gilles OUVRY, Etienne THOREAU
  • CYCLOPROPANECARBOXAMIDE MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    Publication number: 20180265501
    Abstract: The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 27, 2015
    Publication date: September 20, 2018
    Inventors: Chengzhi ZHANG, Justin CHAKMA
  • TETRAHYDROQUINOLINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORy AND THE TREATMENT OF DISEASE
    Publication number: 20180265502
    Abstract: The invention provides tetrahydroquinoline sulfonamide compounds, tetrahydronaphthalene sulfonyl compounds, and related compounds, pharmaceutical compositions, methods of promoting RORy activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.
    Type: Application
    Filed: February 7, 2018
    Publication date: September 20, 2018
    Inventors: Thomas D. Aicher, Clarke B. Taylor, Chad A. VanHuis
  • COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
    Publication number: 20180265503
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.
    Type: Application
    Filed: May 24, 2018
    Publication date: September 20, 2018
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
  • AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES
    Publication number: 20180265504
    Abstract: Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.
    Type: Application
    Filed: May 15, 2018
    Publication date: September 20, 2018
    Inventors: Ryan M. Moslin, David S. Weinstein, Stephen T. Wrobleski, John S. Tokarski, Amit Kumar, Douglas G. Batt, Shuqun Lin, Chunjian Liu, Steven H. Spergel, Yanlei Zhang, Qingjie Liu
  • PROCESS FOR THE PREPARATION OF N-[(3-AMINOOXETAN-3-YL) METHYL]-2-(1,1-DIOXO-3,5-DIHYDRO-1,4-BENZOTHIAZEPIN-4-YL)-6-METHYL-QUINAZOLIN-4-AMINE
    Publication number: 20180265505
    Abstract: The present invention relates to a novel process for the preparation of a compound of the formula (I): and pharmaceutically acceptable acid addition salts thereof, which is useful for prophylaxis and treatment of respiratory syncytial virus (RSV) infection in mammal or human being.
    Type: Application
    Filed: May 24, 2018
    Publication date: September 20, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: JUNLI CHEN, YI REN, JIN SHE, LIN WANG, JIANHUA YU, GUOCAI ZHANG
  • BENZYL AMINE-CONTAINING HETEROCYCLIC COMPOUNDS AND COMPOSITIONS USEFUL AGAINST MYCOBACTERIAL INFECTION
    Publication number: 20180265506
    Abstract: Described herein are compounds and compositions, and methods of making and their use as effective agents against mycobacterial infections.
    Type: Application
    Filed: September 19, 2016
    Publication date: September 20, 2018
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Marvin J. MILLER, Garrett C. MORASKI
  • HOST TARGETED INHIBITORS OF DENGUE VIRUS AND OTHER VIRUSES
    Publication number: 20180265507
    Abstract: Novel antiviral compounds of Formulae (I)-(III) are provided: The inventive compounds, pharmaceutical compositions thereof, and kits including the inventive compounds are useful for the prevention and treatment of infectious diseases caused by viruses, for example, by Flaviviridae virus (e.g., Dengue virus (DENV)), Kunjin virus, Japanese encephalitis virus, vesicular stomatitis virus (VSV), herpes simplex virus 1 (HSV-1), human cytomegalovirus (HCMV), poliovirus, Junin virus, Ebola virus, Marburg virus (MARV), Lassa fever virus (LASV), Venezuelan equine encephalitis virus (VEEV), or Rift Valley Fever virus (RVFV).
    Type: Application
    Filed: January 26, 2018
    Publication date: September 20, 2018
    Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College
    Inventors: Nathanael S. Gray, Priscilla L. Yang, Qingsong Liu, Mélissanne de Wispelaere
  • CRYSTALLINE FORMS OF A COMPOUND THAT INHIBITS BROMODOMAIN
    Publication number: 20180265508
    Abstract: Forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the forms of Compound I.
    Type: Application
    Filed: March 19, 2018
    Publication date: September 20, 2018
    Inventors: Jack Lin, Marika Nespi, Jason Walters
  • Tetrahydro-Pyrido-Pyrimidine Derivatives
    Publication number: 20180265509
    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: May 30, 2018
    Publication date: September 20, 2018
    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
  • 6,7-CYCLICMORPHINAN DERIVATIVES AND USE THEREOF
    Publication number: 20180265510
    Abstract: The application provides compounds of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, dash line a, dash line b, W, Z, X, and m are defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I and the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. In certain embodiments, the Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: December 5, 2014
    Publication date: September 20, 2018
    Inventors: Andrew Kassick, Dawit Tadesse, Laykea Tafesse
  • COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES
    Publication number: 20180265511
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: March 15, 2018
    Publication date: September 20, 2018
    Inventor: Jayhong Andrew Chong
  • FUSED PYRIMIDINE-BASED HYDROXAMATE DERIVATIVES
    Publication number: 20180265512
    Abstract: The present invention relates to fused pyrimidine-based hydroxamate compounds of formula (I), comprising a hydroxamate group, that are inhibitors of hiStone deacetylase (HDAC) and kinases. More particularly, the present invention relates to hydroxamate substituted purine or 5H-pyrrolo[3,2-d]pyrimidine derivatives, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of disorders/conditions/diseases involving, relating to or associated with enzymes having histone deacetylase, non-histone deacetylase and kinase activities/functions and/or via unspecified/multi-targeted mechanisms.
    Type: Application
    Filed: March 9, 2018
    Publication date: September 20, 2018
    Inventors: Haishan Wang, Dizhong Chen, Chang Kai Soh
  • NOVEL PROCESS FOR THE PREPARATION OF DIPEPTIDYL PEPTIDASE-4 (DPP-4) ENZYME INHIBITOR
    Publication number: 20180265513
    Abstract: The present invention relates to a novel and improved process for the preparation of Sitagliptin of Formula (I) and its pharmaceutically acceptable salts. The present invention also relates to novel intermediates and process for the preparation of intermediates used in the preparation of Sitagliptin.
    Type: Application
    Filed: February 20, 2015
    Publication date: September 20, 2018
    Inventors: Venkat Reddy Alla, Raghumitra Alla, Srinivas Reddy Mallepalli, Suresh Babu Nandam, Madhukar Reddy Guda, Raja Reddy Alluri
  • SALT OF CD80 ANTAGONIST
    Publication number: 20180265514
    Abstract: Choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide.
    Type: Application
    Filed: November 20, 2017
    Publication date: September 20, 2018
    Inventor: Ian Richard Matthews
  • THERAPEUTIC COMPOUNDS AND COMPOSITIONS, AND METHODS OF USE THEREOF
    Publication number: 20180265515
    Abstract: Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.
    Type: Application
    Filed: May 22, 2018
    Publication date: September 20, 2018
    Applicant: Genentech, Inc.
    Inventors: Yun-Xing Cheng, Paul Gibbons, Terry Kellar, Wei Li, Rohan Mendonca, Po-wai Yuen, Mark Edward Zak, Lei Zhang
  • Substituted triazolopiperazine PARP inhibitor, preparation method therefor and use thereof
    Publication number: 20180265516
    Abstract: The present invention relates to a class of substituted triazolopiperazine compounds, tautomers, enantiomers, diastereomers, racemates, metabolites, metabolic precursors, and pharmaceutically acceptable salts, esters, prodrugs or hydrate thereof, a preparation methods therefor, intermediates and a use thereof in the preparation of drugs for prevention and treatment of diseases associated with PARP including various ischemic diseases, neurodegenerative diseases and cancers.
    Type: Application
    Filed: May 23, 2018
    Publication date: September 20, 2018
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Ao Zhang, Zehong Miao, Pingyuan Wang, Shanshan Song, Zilan Song, Xiajuan Huan, Zhoulong Fan, Jian Ding
  • EZH2 Inhibitors
    Publication number: 20180265517
    Abstract: The present invention relates to compounds that inhibit EZH2 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
    Type: Application
    Filed: March 14, 2018
    Publication date: September 20, 2018
    Inventors: Matthew Arnold Marx, Matthew Randolph Lee, Robert Anthony Galemmo, Thomas P. Bobinski