Patents Issued in January 25, 2024
  • PKC-ACTIVATING COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
    Publication number: 20240025870
    Abstract: The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimers disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids.
    Type: Application
    Filed: October 2, 2023
    Publication date: January 25, 2024
    Applicant: Synaptogenix, Inc.
    Inventors: Thomas J. NELSON, Daniel L. ALKON
  • METHODS AND SYSTEMS FOR PRODUCTION OF FURFURAL
    Publication number: 20240025871
    Abstract: Systems and method for production of furfural comprising combining a xylose-containing solution with an extraction solution comprising water-insoluble boronic acid to provide a first combined solution comprising an aqueous phase and a non-aqueous phase, said non-aqueous phase comprising xylose-diboronate ester (BA2X); combining at least a portion of the non-aqueous phase with a conversion solution to form a second combined solution, heating the second combined solution to convert at least a portion of the xylose-diboronate ester into furfural to a temperature at or above which the second combined solution consists essentially of a homogeneous liquid phase, cooling down the heated second combined solution to a temperature wherein the cooled second combined solution comprises an aqueous phase comprising water and furfural and (ii) a non-aqueous phase comprising water-insoluble boronic acid and furfural.
    Type: Application
    Filed: December 17, 2021
    Publication date: January 25, 2024
    Inventors: Jean Paul Andre Marie Joseph Ghislain LANGE, Luca RICCIARDI, Willem VERBOOM, Jurriaan HÜSKENS
  • COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME
    Publication number: 20240025872
    Abstract: The present specification relates to a compound of Chemical Formula 1, and an organic light emitting device including the same.
    Type: Application
    Filed: October 22, 2021
    Publication date: January 25, 2024
    Applicant: LT MATERIALS CO., LTD.
    Inventors: Ji-Un KIM, Gi-Back LEE, Won-Jang JEONG, Dong-Jun KIM
  • METHOD FOR PRODUCING KETONE DERIVATIVE
    Publication number: 20240025873
    Abstract: An object of the present invention is to provide a novel method for producing a ketone derivative, and more specifically, a method for producing a ketone derivative (I) represented by formula (I), including mixing a thioester derivative (II) represented by formula (II), a Grignard reagent (III) represented by formula (III) and a copper salt to form a ketone derivative (I).
    Type: Application
    Filed: October 1, 2021
    Publication date: January 25, 2024
    Applicants: TOKUYAMA CORPORATION, OSAKA UNIVERSITY
    Inventors: Masahiko SEKI, Kazushi MASHIMA, Hayato TSURUGI, Daiki KATO, Tomoya MURASE, Jalindar Bhausaheb TALODE
  • Quinazoline Derivative Salt Crystal Form, Preparation Method and Application
    Publication number: 20240025874
    Abstract: A quinazoline derivative (represented by the formula (I)) salt's crystal form, a preparation method and application are provided; specifically, the hydrochloride crystal form A, B, C, D, F, H, I, Sulphate crystal form A, Maleate crystal form A, Succinate crystal form A, Adipate crystal form A, Glycolate crystal form A, Malate crystal form A, Fumarate Salt crystal form A, besylate crystal form A, B, C, benzoate crystal form A, hippurate crystal form A and oxalate crystal form A of the quinazoline derivative represented by formula (I). The salt crystal form provided by the present invention has good stability, which can be used in the treatment of non-small cell lung cancer brain metastasis, meningeal metastasis, primary brain cancer or glioma, etc., and has good bioavailability, which is of great significance for further research on the efficacy of such solid drugs.
    Type: Application
    Filed: March 21, 2019
    Publication date: January 25, 2024
    Applicant: Wayshire Biopharm Holding Limited
    Inventors: Wei ZHONG, Jinqiang ZHANG
  • A COMPOUND AS A THYROID HORMONE BETA RECEPTOR AGONIST AND USE THEREOF
    Publication number: 20240025875
    Abstract: A compound serving as a thyroid hormone ? receptor agonist and uses of the compound, also provided is a pharmaceutical composition comprising the compound. The compound or the pharmaceutical composition is applicable in preparing a medicament for preventing, treating, or alleviating thyroid hormone ? receptor agonist-modulated diseases, and specifically applicable in preparing a medicament for treating nonalcoholic fatty liver disease.
    Type: Application
    Filed: September 16, 2021
    Publication date: January 25, 2024
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Zheng GU, Jianhao LI, Jianchao DENG, Yongxiang LI, Haoxiong QIN, Daoqian CHEN, Xiaomin ZHENG, Jianghong YU, Huantian ZHAO
  • HETEROARYL COMPOUNDS, SOLID FORMS, PREPARATION METHODS AND USES THEREOF
    Publication number: 20240025876
    Abstract: Provided herein are compounds, crystalline free forms, crystalline salt forms, and pharmaceutical compositions of Compound 1. Also provided are methods of preparing and methods of using the same, e.g., for inhibiting a kinase and/or for treating various diseases or disorders, such as autoimmune diseases.
    Type: Application
    Filed: June 20, 2023
    Publication date: January 25, 2024
    Applicants: InventisBio Co., Ltd., InventisBio LLC
    Inventors: Wei LI, Yanqin LIU, Dongmei QIANG, Xiaojun WANG, Xing DAI
  • PROCESSES FOR MAKING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
    Publication number: 20240025877
    Abstract: The disclosure provides processes for preparing a compound of Formula (I):
    Type: Application
    Filed: August 31, 2022
    Publication date: January 25, 2024
    Inventors: Paul T. Angell, Cristian Harrison, Robert M. Hughes, Berenice Lewandowski, Benjamin J. Littler, Vito Melillo, William A. Nugent, David Andrew Siesel, David Smith, John Studley
  • MDM2 DEGRADERS AND USES THEREOF
    Publication number: 20240025878
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: October 10, 2022
    Publication date: January 25, 2024
    Inventors: Nan JI, Matthew M. WEISS, Xiaozhang ZHENG, Xiao ZHU
  • PYRIDAZINONE COMPOUNDS AND USES THEREOF
    Publication number: 20240025879
    Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.
    Type: Application
    Filed: September 1, 2023
    Publication date: January 25, 2024
    Inventors: Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
  • AMINO QUINAZOLINE DERIVATIVES AS P2X3 INHIBITORS
    Publication number: 20240025880
    Abstract: The present invention relates to compounds of formula I inhibiting P2X purinoceptor 3; particularly the invention relates to compounds that are amino quinazoline derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of many disorders associated with P2X3 receptors mechanisms, such as respiratory diseases including cough, asthma, idiopathic pulmonary fibrosis (IPF) and chronic obstructive pulmonary disease (COPD).
    Type: Application
    Filed: November 26, 2021
    Publication date: January 25, 2024
    Applicant: CHIESI FARMACEUTICI S.P.A.
    Inventors: Claudio FIORELLI, Paolo BRUNO, Matteo BIAGETTI, Daniela PIZZIRANI, Daniele PALA, Paolo RONCHI, Sara GUARIENTO, Charles BAKER-GLENN, Hervé VAN DE POËL, Kim Louise HIRST
  • Belumosudil Metabolites and Uses Thereof In The Treatment of Chronic Graft-Versus-Host Disease
    Publication number: 20240025881
    Abstract: The present disclosure provides metabolites of belumosudil and uses of the metabolites in of treating patients with ROCK2-mediated diseases including cGVHD.
    Type: Application
    Filed: February 3, 2023
    Publication date: January 25, 2024
    Applicant: Kadmon Corporation, LLC
    Inventors: Olivier Schueller, Jeegar P. Patel
  • BENZAMIDES OF PYRAZOLYLAMINO- PYRIMIDINYL DERIVATIVES, AND COMPOSITIONS AND METHODS THEREOF
    Publication number: 20240025882
    Abstract: The invention provides novel benzamides of pyrazolyl-amino-pyrimidinyl derivatives of Formula (I) as selective and potent JAK inhibitors for treating various diseases and disorders. The invention also provides pharmaceutical composition of these compounds and methods of their preparation and use thereof.
    Type: Application
    Filed: September 10, 2023
    Publication date: January 25, 2024
    Inventors: Zhaokui Wan, Michael Lawrence Vazquez, Xiaodong Li
  • PYRIMIDIN-2-YL SULFONAMIDE DERIVATIVES
    Publication number: 20240025883
    Abstract: Compounds having the general formula I wherein R1, R2, R3, R4, X1 and X2 are as described herein, composition including the compounds and methods of using the compounds for treatment of GPR17-mediated diseases.
    Type: Application
    Filed: August 24, 2023
    Publication date: January 25, 2024
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Guido GALLEY, Luca GOBBI, Wolfgang GUBA, Dmitry MAZUNIN, Emmanuel PINARD, Antonio RICCI
  • COMPOUNDS AS GCN2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
    Publication number: 20240025884
    Abstract: Provided herein are novel compounds, e.g., those of Formula (I), as GCN2 inhibitors. Also provided are pharmaceutical compositions including one or more of the novel compounds, and pharmaceutical uses thereof. Compounds provided herein can typically inhibit an activity of a GCN2 and thus can be used for treating or preventing diseases related thereto.
    Type: Application
    Filed: July 5, 2022
    Publication date: January 25, 2024
    Inventors: Cheonhyoung Park, Kimoon Ryu, Tae-Hun Kim, Ha Yoon Kim, Eunhye Ju, Hyung Ki Lee, Youngjee Jeong, Doyoung Choi, Jun Hwan Moon, Nayeon Park, Iksoo Jang, Kyu Hwan Kim, Hyangsoo Lee, Min Jung Lee
  • TRIAZINE DERIVATIVES AND METHODS OF USE THEREOF
    Publication number: 20240025885
    Abstract: Certain anti-viral compounds, pharmaceutical compositions, and methods related thereto are disclosed.
    Type: Application
    Filed: December 16, 2022
    Publication date: January 25, 2024
    Inventor: Jinzi Jason WU
  • INHIBITORS OF IGF2BP1-RNA BINDING
    Publication number: 20240025886
    Abstract: The present invention is directed to compounds and compositions comprising thereof. Further, methods of use such as for the treatment and prevention of a disorder associated with binding of IGF2BP1 to an RNA in a subject in need thereof are also provided.
    Type: Application
    Filed: November 18, 2021
    Publication date: January 25, 2024
    Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., THE PENN STATE RESEARCH FOUNDATION
    Inventors: Vladimir SPIEGELMAN, Vikash SINGH, Arun SHARMA, Amandeep SINGH, Joel YISRAELI, Nadav WALLIS, Froma OBERMAN
  • THIENYL AND CYCLOALKYL AMINOPYRIMIDINE COMPOUNDS AS INHIBITORS OF NUAK KINASES, COMPOSITIONS AND USES THEREOF
    Publication number: 20240025887
    Abstract: The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.
    Type: Application
    Filed: January 7, 2022
    Publication date: January 25, 2024
    Inventors: Rima Al-Awar, Liliana Attisano, Methvin Isaac, Yong Liu, David Smil, David Uehling, Jeff Wrana
  • HETEROARYL DERIVATIVE COMPOUNDS, AND USES THEREOF
    Publication number: 20240025888
    Abstract: The present disclosure relates to a heteroaryl derivative and uses thereof. The heteroaryl derivative of the present disclosure exhibits excellent inhibitory activity against EGFR and/or HER2, and thus may be usefully employed as a therapeutic agent for EGFR- and/or HER2-related diseases.
    Type: Application
    Filed: May 16, 2022
    Publication date: January 25, 2024
    Applicant: Voronoi Inc.
    Inventors: Youn Ho LEE, Seon Ah HWANG, In Seob SHIM, Hyeon Ho JEON, Woo Mi DO, Hee Sun RYU, Jung Beom SON, Nam Doo KIM, Sung Hwan KIM, Hong Ryul JUNG, Young Yi LEE
  • PROCESS FOR THE PRODUCTION OF 5-(4-((2S,5S)-5-(4-CHLOROBENZYL)-2-METHYL-MORPHOLINO)PIPERIDIN-1-YL)-1H-1,2,4-TRIAZOL-3-AMINE
    Publication number: 20240025889
    Abstract: The present invention relates to a process for the synthesis of 5-(4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)piperidin-1-yl)-1H-1,2,4-triazol-3-amine in two hydrated crystalline forms and in one anhydrous crystalline form. The present invention further relates to methyl (Z)-4-((2S,5S)-5-(4-chlorobenzyl)-2-methylmorpholino)-N-cyanopiperidine-1-carbimidothioate which is an intermediate in this process.
    Type: Application
    Filed: July 17, 2023
    Publication date: January 25, 2024
    Inventors: Grzegorz Witkowski, Marta Magdycz, Magdalena Tyszkiewicz, Marcin Zakrzewski, Stanislaw Pikul
  • HEPATITIS B CORE PROTEIN MODULATORS
    Publication number: 20240025890
    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 1, 2023
    Publication date: January 25, 2024
    Inventors: William W. TURNER, Lee D. ARNOLD, Hans MAAG, Leping LI, Mark G. BURES, Simon Nicolas HAYDAR, Samson FRANCIS
  • HETEROCYCLIC COMPOUNDS AND THEIR USE FOR TREATMENT OF HELMINTHIC INFECTIONS AND DISEASES
    Publication number: 20240025891
    Abstract: Provided herein are Heterocyclic Compounds of formula (I), formula (II), formula (III), formula (IlIa), formula (Mb), formula (IIIc), formula (Hid), formula (IV), formula (IVa), formula (IVb), and formula (IVc), and pharmaceutically acceptable salts, tautomers, isotopologues, and stereoisomers thereof, compositions comprising an effective amount of a Heterocyclic Compound of formula (I), formula (II), formula (III), formula (IlIa), formula (Mb), formula (IIIc), formula (Hid), formula (IV), formula (IVa), formula (IVb), and formula (IVc), and methods for treating or preventing animal and human filarial worm infections and diseases.
    Type: Application
    Filed: October 22, 2021
    Publication date: January 25, 2024
    Inventors: Natalie Hawryluk, Stacie Canan, Kevin R. Condroski, Matthew Bedore, Graham Kyne, Sanjay Menon
  • SALT INDUCIBLE KINASE INHIBITORS
    Publication number: 20240025892
    Abstract: The present application provides compounds that modulate the activity of one or more salt inducible kinases (SIKs). Pharmaceutical composition and methods of treating diseases associated with abnormal expression and/or activity of one or more SIKs are also provided.
    Type: Application
    Filed: August 5, 2021
    Publication date: January 25, 2024
    Inventors: Marc Nathan Wein, William J. Greenlee
  • PYRIMIDINE-AND NITROGEN-CONTAINING BICYCLIC COMPOUND
    Publication number: 20240025893
    Abstract: A compound represented by the general formula (1) or a salt thereof, which has a superior IRAK-4 inhibitory activity, and is useful as active ingredients of medicaments for prophylactic treatment and/or therapeutic treatment of diseases relating to IRAK-4 inhibition.
    Type: Application
    Filed: September 30, 2020
    Publication date: January 25, 2024
    Applicants: Asahi Kasei Pharma Corporation, Vernalis (R&D) Limited
    Inventors: Koichiro ARAI, Kenichiro TAKABA, Masakazu ATOBE, Misato TAKASHIMA, Naomi AONO, Andrew John POTTER, Daniel Paul MADDOX
  • SUBSTITUTED 5,6,7,8-TETRAHYDROPYRIDO[2,3-D]PYRIMIDINE-2,4-DIONES FOR TREATING CARDIAC DISEASES
    Publication number: 20240025894
    Abstract: The present disclosure provides novel tetrahydropyran (THP)-substituted bicyclic pyrimidinedione compounds that are useful for the treatment of hypertrophic cardiomyopathy (HCM), conditions associated with left ventricular hypertrophy, conditions associated with diastolic dysfunction, and/or symptoms associated thereof. The synthesis and characterization of the compounds is described, as well as methods for treating HCM and other forms of heart disease.
    Type: Application
    Filed: August 1, 2023
    Publication date: January 25, 2024
    Inventors: Mark Grillo, Brian Kane, Johan Oslob, Fabienne Thompson
  • COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH
    Publication number: 20240025895
    Abstract: The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.
    Type: Application
    Filed: September 1, 2023
    Publication date: January 25, 2024
    Inventors: William E. Lowry, Michael E. Jung, Heather R. Christofk, Xiaoguang Liu, Aimee Flores
  • PROCESS FOR PREPARING 7-CHLORO-6-FLUORO-1-(2-ISOPROPYL-4-METHYLPYRIDIN-3-YL)PYRIDO[2,3-D]PYRIMIDINE-2,4(1H,3H)-DIONE
    Publication number: 20240025896
    Abstract: Provided herein is a process for preparing compound A comprising (a) admixing 2-isopropyl-4-methylpyridin-3-amine (Compound B), or a salt thereof, a first base, and a reactive compound comprising phosgene or a phosgene equivalent in an organic solvent to form 3-isocyanato-2-isopropyl-4-methylpyridine (Compound C); (b) admixing Compound C and 2,6-dichloro-5-fluoronicotinamide (Compound D) to form 2,6-dichloro-5-fluoro-N-((2-isopropyl-4-methylpyridin-3-yl)carbamoyl)nicotinamide (Compound E); and (c) admixing Compound E and a second base to form a product mixture comprising Compound A and the second base. Also provided herein is a process for synthesizing AMG 510 comprising using Compound A prepared according to the disclosed processes [Insert Structure] (Compound A).
    Type: Application
    Filed: November 19, 2021
    Publication date: January 25, 2024
    Applicant: AMGEN INC.
    Inventors: Michal ACHMATOWICZ, John T. COYLER, Michael T. CORBETT, Daniel J. GRIFFIN, Andrew T. PARSONS, Joanna ROBINSON, Kyle QUASDORF
  • CRYSTALLINE HYDRATE OF A JAK INHIBITOR COMPOUND
    Publication number: 20240025897
    Abstract: Provided herein is a crystalline hydrate of the compound of formula 1: Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.
    Type: Application
    Filed: May 31, 2023
    Publication date: January 25, 2024
    Inventor: Gene Timothy Fass
  • HPK1 ANTAGONISTS AND USES THEREOF
    Publication number: 20240025898
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
    Type: Application
    Filed: July 11, 2023
    Publication date: January 25, 2024
    Inventors: Neelu KAILA, Ian LINNEY, Stuart WARD, Grant WISHART, Ben WHITTAKER, Alexandre COTE, Jeremy Robert GREENWOOD, Abba LEFFLER, Steven K. ALBANESE, Daniel L. SEVERANCE
  • TRIHETEROCYCLIC DERIVATIVE, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
    Publication number: 20240025899
    Abstract: A triheterocyclic derivative, and a pharmaceutical composition and an application thereof. The triheterocyclic derivative (I), and a stereoisomer or a pharmacologically acceptable salt thereof have the following structure. The triheterocyclic derivative has good effects of inhibiting ATR levels in vivo and in vitro, and furthermore, the triheterocyclic derivative can also effectively treat diseases caused by abnormal ATR levels, such as cancers.
    Type: Application
    Filed: October 15, 2021
    Publication date: January 25, 2024
    Inventors: Xiaohui LIU, Fengtao LIU, Daxin GAO
  • TETRACYCLIC COMPOUNDS AS DGK INHIBITORS
    Publication number: 20240025900
    Abstract: The present application provides tetracyclic compounds that modulate the activity of diacylglycerol kinase (DGK), which are useful in the treatment of various diseases, including cancer.
    Type: Application
    Filed: July 17, 2023
    Publication date: January 25, 2024
    Inventors: Joshua Hummel, Shicheng Shi, Xiaozhao Wang
  • METHOD FOR PRODUCING CYCLIC IMIDE COMPOUND, COMPOSITION, AND COMPOUND
    Publication number: 20240025901
    Abstract: A first object of the present invention is to provide a method for producing a cyclic imide compound with high yield and high purity. A second object of the present invention is to provide a composition that can be used in the method for producing a cyclic imide compound with high yield and high purity. A third object of the present invention is to provide an intermediate compound that can be used in the method for producing a cyclic imide compound with high yield and high purity. The method for producing a cyclic imide compound according to the present invention includes reacting a compound represented by formula (1) below with at least one amine compound to obtain a compound represented by formula (2) below.
    Type: Application
    Filed: July 13, 2023
    Publication date: January 25, 2024
    Applicants: FUJIFILM Corporation, The University of Tokyo
    Inventors: Hiroki SUGIURA, Yukio TANI, Tetsuya MATSUSHITA, Tetsuya WATANABE, Toshihiro OKAMOTO
  • BIFUNCTIONAL COMPOUNDS FOR DEGRADATION OF EGFR AND RELATED METHODS OF USE
    Publication number: 20240025902
    Abstract: Disclosed herein are bifunctional compounds formed by conjugating EGFR inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation of mutant EGFR kinase, and methods of preparation and uses thereof.
    Type: Application
    Filed: September 29, 2021
    Publication date: January 25, 2024
    Inventors: Bailin LEI, Huaqing LIU, Songzhe HAN, Zhiwei WANG
  • Bicyclic Compounds and Uses Thereof for the Treatment of Diseases
    Publication number: 20240025903
    Abstract: Provided herein are compounds and compositions thereof for modulating hepatocyte growth factors. In some embodiments, the compounds and compositions are provided for treatment of diseases, including neurological disorders.
    Type: Application
    Filed: November 1, 2021
    Publication date: January 25, 2024
    Applicant: Athira Pharma, Inc.
    Inventors: Leen Kawas, Kevin Church, Robert Taylor, Jewel Johnston, Douglas Boatman
  • PDE9 INHIBITORS FOR TREATING CARDIAC FAILURE
    Publication number: 20240025904
    Abstract: The present disclosure relates to PDE9 inhibitors, compositions comprising the PDE9 inhibitors, and methods of using the PDE9 inhibitors and compositions for treatment of cardiac failure.
    Type: Application
    Filed: October 26, 2021
    Publication date: January 25, 2024
    Inventors: Rahul Dilip BALLAL, Thiago Trovati MACIEL, Deepak GUPTA, Thomas WANG
  • SALTS OF DIHYDROPYRIMIDINE DERIVATIVES, COMPLEXES AND USES THEREOF IN MEDICINE
    Publication number: 20240025905
    Abstract: Salts of dihydropyrimidine derivatives, complexes and uses thereof in medicine, and complexes and pharmaceutical compositions thereof. The uses of the addition salts, the complexes or the pharmaceutical compositions in the manufacture of a medicament, especially in the manufacture of a medicament for preventing, managing, treating or lessening hepatitis B virus (HBV) infection.
    Type: Application
    Filed: November 30, 2021
    Publication date: January 25, 2024
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Qingyun REN, Xinchang LIU, Yingjun ZHANG, Guanghua YAN
  • KINASE MODULATORS AND METHODS OF USE THEREOF
    Publication number: 20240025906
    Abstract: The invention provides compounds that modulate the activity of protein kinases that are associated with human diseases, disorders, and conditions. In particular, compounds of the invention inhibit TYK2, a member of the Janus Kinase (JAK) family of non-receptor protein kinases.
    Type: Application
    Filed: June 16, 2023
    Publication date: January 25, 2024
    Inventors: Zhonghua Pei, Gyanendra Kumar, Anh Truong, Claudio Aquino, Derek Kejia Wu, Andrew Tasker
  • QUINAZOLINE PAN-KRas INHIBITORS
    Publication number: 20240025907
    Abstract: The present invention relates to compounds that inhibit at least one of KRas G12A, KRas G12C, KRas G12D, KRas G12R, KRas G12S, KRas G12V, KRas G13D and KRas Q61H, pharmaceutical compositions comprising the compounds and methods of use therefor.
    Type: Application
    Filed: August 2, 2023
    Publication date: January 25, 2024
    Inventors: Xiaolun Wang, Anthony Ivetac, Svitlana Kulyk, John David Lawson, Matthew Arnold Marx, Christopher Ronald Smith
  • COMPOUND USED AS KINASE INHIBITOR AND USE THEREOF
    Publication number: 20240025908
    Abstract: A compound represented by formula (I) or a stereoisomer, a tautomer, a crystal form, a pharmaceutically acceptable salt, a hydrate, a solvate or a prodrug thereof are provided. The compound represented by formula (I) can be used as a kinase inhibitor for preparing a medicament for treating diseases mediated by kinase such as ROS1, NTRK and ALK.
    Type: Application
    Filed: November 3, 2021
    Publication date: January 25, 2024
    Inventors: Jun LI, Apeng LIANG, Chengshan NIU, Yusheng WU
  • COMPOUND AND COMPOSITION
    Publication number: 20240025909
    Abstract: An object of the present invention is to provide a composition that gives a cured product excellent in heat resistance and solvent resistance. The present invention provides a compound represented by the general formula (I) below and having at least one reactive group in a molecule. In the formula, A represents a hydrocarbon ring having 6 carbon atoms; X1 and X2 each represent, for example, an aryl group having 6 to 30 carbon atoms and optionally substituted with a reactive group or a group having a reactive group; R1, R2, R3, R4, R6, R7, R8, and R9 each represent, for example, a hydrogen atom, a reactive group, or a hydrocarbon group having 1 to 20 carbon atoms and optionally substituted with a reactive group; and R5 and R10 each represent, for example, a hydrogen atom, or a hydrocarbon group having 1 to 20 carbon atoms and optionally substituted with a reactive group.
    Type: Application
    Filed: December 16, 2021
    Publication date: January 25, 2024
    Inventors: Hiromasa SAITO, Yousuke MURAMATSU, Mizuki SUZUKI, Masatomi IRISAWA
  • BRAIN-MIGRATING TUMOR THERAPEUTIC AGENT CONTAINING FUSED PYRIMIDINE COMPOUND AS ACTIVE INGREDIENT
    Publication number: 20240025910
    Abstract: An object to be solved of the present invention is to provide a brain-penetrable antitumor agent showing an excellent brain penetration property and RET inhibitory activity. The present invention provides brain-penetrable antitumor agent including a compound represented by Formula (I) below or a salt thereof as an active ingredient: wherein R1, R2, and R3 are as described in Specification.
    Type: Application
    Filed: November 18, 2021
    Publication date: January 25, 2024
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Isao MIYAZAKI, Satoru IGUCHI, Kentaro WAKAYAMA
  • Process for the preparation of 4-(3,5-difluorophenyl)-N-[3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl]-6,7-dihydro-5H-[1,2,4]triazolo[1,5-a]pyrimidin-2-amine
    Publication number: 20240025911
    Abstract: The present invention relates to a process for the preparation of a compound (I), (I); or pharmaceutically acceptable salt thereof, which is useful as the key intermediate for the synthesis of compounds for prophylaxis and treatment of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Application
    Filed: December 8, 2021
    Publication date: January 25, 2024
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Guocai ZHANG, Weichun CHEN
  • RIPK1 INHIBITORS AND METHODS OF USE
    Publication number: 20240025912
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
    Type: Application
    Filed: May 17, 2023
    Publication date: January 25, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Joanna L. Chen, Yi-Heng Chen, Erin F. DiMauro, Min Liu, Joey L. Methot, Andrew J. Musacchio, Anandan Palani, Barbara Pio, Lorena Rico Duque, Phieng Siliphaivanh, Brandon A. Vara
  • TERTIARY CARBOXAMIDE COMPOUNDS
    Publication number: 20240025913
    Abstract: Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating diseases. Specific diseases include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
    Type: Application
    Filed: October 19, 2021
    Publication date: January 25, 2024
    Inventors: Andrei W. KONRADI, Tracy Tzu-Ling Tang LIN
  • FUSED BICYCLIC COMPOUNDS FOR THE TREATMENT OF DISEASE
    Publication number: 20240025914
    Abstract: Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.
    Type: Application
    Filed: May 2, 2023
    Publication date: January 25, 2024
    Inventors: Raju Mohan, Benjamin Anthony Pratt
  • SOLID FORMS OF 4-(3,3-DIFLUORO-2,2-DIMETHYL-PROPANOYL)-3,5-DIHYDRO-2H-PYRIDO[3,4-F][1,4]OXAZEPINE-9-CARBONITRILE
    Publication number: 20240025915
    Abstract: Described herein are solid forms of 4-(3,3-difluoro-2,2-dimethyl-propanoyl)-3,5-dihydro-2H-pyrido[3,4-f][1,4]oxazepine-9-carbonitrile, the process of preparing the forms, pharmaceutical compositions comprising same, and methods of use thereof.
    Type: Application
    Filed: July 24, 2023
    Publication date: January 25, 2024
    Applicant: Denali Therapeutics Inc.
    Inventors: Javier de Vicente Fidalgo, Brian M. Fox, Christopher R.H. Hale
  • KRAS G12C INHIBITORS
    Publication number: 20240025916
    Abstract: The present disclosure provides compounds of the formula: where R1, R2, R3, R4, R5, A, and B are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and salts for treating patients for cancer.
    Type: Application
    Filed: November 24, 2021
    Publication date: January 25, 2024
    Inventors: David Michael HYMAN, Gregory Lawrence LACKNER, Sheng-Bin PENG, Bree Leigh RICHEY, Chong SI
  • PLASMA KALLIKREIN INHIBITORS
    Publication number: 20240025917
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age related macular edema, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.
    Type: Application
    Filed: November 18, 2021
    Publication date: January 25, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Jianming Bao, Natalija Cernaka, Alan C. Cheng, Ying-Duo Gao, Salman Jabri, Jovan Alexander Lopez, Rohan Merchant, Anthony Ken Ogawa, Skylar K. Osler, Christopher J. Sinz, Phillip Patrick Sharp, Haiqun Tang, Maoqun Tian, Dong Xiao, Song Yang
  • KRAS G12D Inhibitors
    Publication number: 20240025918
    Abstract: Provided are KRAS G12D inhibitors of formula (I), a composition containing the inhibitors, a prodrug thereof, a PROTAC compound thereof and the use thereof.
    Type: Application
    Filed: November 19, 2021
    Publication date: January 25, 2024
    Inventors: Huifeng HAN, Panliang GAO, Wenlong ZHANG, Cunbo MA, Peng WANG, Dan LIU, Hao ZHANG, Wei LONG
  • AZA-TETRACYCLIC OXAZEPINE COMPOUNDS AND USES THEREOF
    Publication number: 20240025919
    Abstract: Provided herein are aza-tetracyclic oxazepinyl compounds useful in the treatment of cancers.
    Type: Application
    Filed: May 19, 2023
    Publication date: January 25, 2024
    Inventors: Matthew Leo Landry, Christian Nilewski, Michael Siu, Elisia Villemure, Yong Wang, BinQing Wei, Melissa Ann Ashley, Steven Do, Lewis John Gazzard, Samantha Alyson Green