Patents Issued in March 28, 2024
  • DIAMINOTRIAZINE COMPOUNDS
    Publication number: 20240101521
    Abstract: The present invention relates to diaminotriazine compounds and to their use as herbicides. It also relates to agrochemical compositions for crop protection and to a method for controlling unwanted vegetation.
    Type: Application
    Filed: January 17, 2022
    Publication date: March 28, 2024
    Inventors: Danny Geerdink, Matthias Witschel, Veronica Lopez Carrillo, Martin Hartmueller, Michael Rack, Desislava Slavcheva Petkova, Trevor William Newton, Sandra Lange, Thomas Seitz
  • NOVEL METHOD FOR PRODUCING BENZOXAZINE COMPOUND
    Publication number: 20240101522
    Abstract: A method for producing a benzoxazine compound represented by general formula (3), includes performing a reaction by mixing a mixture containing a bisphenol compound represented by general formula (1) and a formaldehyde with an amine compound represented by general formula (2):
    Type: Application
    Filed: January 24, 2022
    Publication date: March 28, 2024
    Inventor: Yoshimi UTAKA
  • NOVEL BENZOXAZINE COMPOUND, RESIN RAW MATERIAL COMPOSITION CONTAINING THE SAME, CURABLE RESIN COMPOSITION, AND CURED PRODUCT THEREOF
    Publication number: 20240101523
    Abstract: An object is to provide a novel benzoxazine compound that has high heat resistance and can cure under low temperature conditions, a resin raw material composition containing the benzoxazine compound, a curable resin composition, and a cured product thereof. As a solution, a benzoxazine compound represented by general formula (1) is provided: wherein R1 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and R2 represents an alkylene group having 1 to 6 carbon atoms.
    Type: Application
    Filed: January 24, 2022
    Publication date: March 28, 2024
    Inventor: Yoshimi UTAKA
  • A METHOD FOR PREPARATION OF 1-(2-((2,4-DIMETHYLPHENYL)THIO)PHENYL) PIPERAZINE AND ITS SALTS
    Publication number: 20240101524
    Abstract: A method for preparation of 1-(2-((2,4-Dimethylphenyl)thio)phenyl)piperazine and its salts through a novel intermediate, 2-((2,4-dimethylphenyl)thio)-N-hydroxybenzamide involves mild conditions, eco-friendly and cost effective reagents to provide the target compound with purity level greater than 99.5% in high yield.
    Type: Application
    Filed: July 16, 2021
    Publication date: March 28, 2024
    Applicant: R L FINE CHEM PRIVATE LIMITED
    Inventors: Vinay KUMAR, V, Dantham SOWMYA, Rajat Rudragoud BIRADAR PATIL, Puttaraju BOREGOWDA, Sivakumar RALLAPALLI
  • Crosslinkable Mesogenic Dianhydride Monomers
    Publication number: 20240101525
    Abstract: Applicants disclose a family of rod-like dianhydrides that contain two phthalic anhydride moieties linked by a bridge that is comprised of at least one ethynyl and one paraphenylene group and processes of making and using such rod-like dianhydrides. Such rod-like dianhydrides can endow net-work structures with improved mechanical and thermal properties in the crosslinked-polymer products.
    Type: Application
    Filed: April 12, 2023
    Publication date: March 28, 2024
    Inventors: Loon-Seng Tan, Zhenning Yu
  • PARA ACYL SUBSTITUTED DIAZACYCLOHEXENE DERIVATIVES
    Publication number: 20240101526
    Abstract: Para-acyl substituted diazacyclohexenes, medical formulations thereof and methods for making and using the same.
    Type: Application
    Filed: November 7, 2023
    Publication date: March 28, 2024
    Inventors: Bishwajit Nag, Ananda Sen, Nitish Nag, Arjun Sanyal, Srinivasan Narasimhan
  • QUINOLONE CARBOXYLIC DERIVATIVES
    Publication number: 20240101527
    Abstract: A compound of Formula (I) below, or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof: in which R1, R2, R3, R5, R6, and R7 are defined as in the SUMMARY section. Further disclosed are a method of using the above-described compound, salt, stereoisomer, solvate, or prodrug for treating microbial infections and a pharmaceutical composition containing the same.
    Type: Application
    Filed: October 23, 2020
    Publication date: March 28, 2024
    Applicant: TAIGEN BIOTECHNOLOGY CO., LTD.
    Inventors: Chu-Chung Lin, Hung-Chuan Chen, Chiayn Chiang, Chih-Ming Chen
  • SUBSTITUTED PYRAZOLO PIPERIDINE CARBOXYLIC ACIDS
    Publication number: 20240101528
    Abstract: The invention relates to substituted pyrazolo piperidine carboxylic acids, their salts and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and cardiac diseases, preferably heart failure with reduced and preserved ejection fraction (HFrEF, HFmrEF and HFpEF), hypertension (HTN), peripheral arterial diseases (PAD, PAOD), cardio-renal and kidney diseases, preferably chronic and diabetic kidney disease (CKD and DKD), cardiopulmonary and lung diseases, preferable pulmonary hypertension (PH), and other diseases, preferably neurodegenerative diseases and different forms of dementias, fibrotic diseases, systemic sclerosis (SSc), sickle cell disease (SCD), wound healing disorders such as diabetic foot ulcer (DFU).
    Type: Application
    Filed: December 9, 2021
    Publication date: March 28, 2024
    Inventors: Alexandros VAKALOPOULOS, Marie-Pierre COLLIN-KRÖPELIN, Nuria ORTEGA HERNANDEZ, Andre DIESKAU, Melissa BOULTADAKIS-ARAPINIS, Lisa CANDISH, Timo STELLFELD, Ilka MATHAR, Lucas Hudson HOFMEISTER, Peter SANDNER, Frank WUNDER, Lisa DIETZ, Robert Alan WEBSTER, Carsten SCHMECK
  • ANTIVIRAL INDOLINYL COMPOUNDS AND USES THEREOF
    Publication number: 20240101529
    Abstract: The present disclosure relates to indolinyl compounds. The present disclosure further relates to compounds that inhibit viral helicase-primase. The present disclosure further relates to the use of the compounds for the preparation a medicament for the treatment of diseases and/or condition through inhibiting viral helicase-primase. The present disclosure also relates to use of those compounds in the treatment of viral infections. The present disclosure further relates to intermediates for its preparation and to pharmaceutical compositions containing those compounds.
    Type: Application
    Filed: May 18, 2023
    Publication date: March 28, 2024
    Inventors: Aesop Cho, Katherine De La Fuente, Thomas P. Stratton, Peiyuan Wang, William J. Watkins, Jie Xu, Kin S. Yang
  • HDAC INHIBITOR SOLID STATE FORMS
    Publication number: 20240101530
    Abstract: The present disclosure relates to various solid-state forms of N-hydroxy 2-{6-[(6-fluoro-quinolin-2-ylmethyl)-amino]-3-aza-bicyclo[3.1.0]hex-3-yl}pyrimidine-5-carboxamide and methods of making the same. Such forms of N-hydroxy 2-{6-[(6-fluoro-quinolin-2-ylmethyl)-amino]-3-aza-bicyclo[3.1.
    Type: Application
    Filed: August 31, 2023
    Publication date: March 28, 2024
    Inventors: Xiaohu DENG, Stewart JONES, David SLACK
  • PYRIDINAMINE DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS
    Publication number: 20240101531
    Abstract: The present disclosure is directed to compounds of Formula (1): wherein m, n, Y, R1, R2, R3, R4 and R5 are each as described herein, as stereoisomers, enantiomers or tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, and pharmaceutical compositions comprising the compounds of Formula (I), as described herein, which are useful as voltage-gated potassium channel modulators and are therefore are useful in treating seizure disorders such as epilepsy.
    Type: Application
    Filed: June 6, 2023
    Publication date: March 28, 2024
    Inventors: Paul Scott Charifson, Christoph Martin Dehnhardt, Julien A. Delbrouck, Thilo Focken, Wei Gong, Shawn Johnstone, Xiangyu Li, Jia Yi Mo, Juliette Sabbatani, Hong Wang, Steven Sigmund Wesolowski, Alla Yurevna Zenova, Wei Zhang
  • HETEROARYL CARBOXAMIDE COMPOUND
    Publication number: 20240101532
    Abstract: A compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy is provided. The present inventors have conducted studies on a compound useful as an active ingredient of a pharmaceutical composition for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy, and confirmed that a heteroaryl carboxamide compound has DGK ? (DGKzeta) inhibitory effect, leading to completion of the present invention. The heteroaryl carboxamide compound of the present invention has DGK ? inhibitory effect, and can be used as a therapeutic agent for treatment of cancer related to activation of immune cells or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody therapy.
    Type: Application
    Filed: November 28, 2023
    Publication date: March 28, 2024
    Inventors: Hideyuki Watanabe, Takashi Kamikubo, Akio Kamikawa, Takuya Washio, Yohei Seki, Keiichiro Okuyama, Osamu Ikeda, Hiroshi Tomiyama, Yoshinori Iwai, Akihiko Nakamura, Kozo Miyasaka
  • METHODS AND INTERMEDIATES FOR PREPARING THERAPEUTIC COMPOUNDS
    Publication number: 20240101533
    Abstract: The present disclosure relates to methods and intermediates useful for preparing a compound of formula I: or a co-crystal, solvate, salt or combination thereof.
    Type: Application
    Filed: June 5, 2023
    Publication date: March 28, 2024
    Inventors: Kevin McCormack Allan, Amanda Lynn Vandehey, Gediminas Brizgys, Sachin Dhar, Ian James Doxsee, Alex Goldberg, Lars V. Heumann, Zilin Huang, Nathaniel Thomas Kadunce, Shahrokh Kazerani, Willard Lew, Vinh Xuan Ngo, Brian Michael O`Keefe, Trevor James Rainey, Benjamin James Roberts, Bing Shi, Dietrich P. Steinhuebel, Winston C. Tse, Anna Michelle Wagner, Xianghong Wang, Scott Alan Wolckenhauer, Chloe Yuyi Wong, Jennifer R. Zhang
  • COMPOUNDS AND USES THEREOF
    Publication number: 20240101534
    Abstract: The present disclosure features compounds and methods useful for the treatment of BAF complex-related disorders.
    Type: Application
    Filed: November 22, 2021
    Publication date: March 28, 2024
    Inventors: Matthew NETHERTON, Francois BRUCELLE, Jing DENG, Johannes H. VOIGT
  • DIHYDROISOQUINOLINONE DERIVATIVE AND APPLICATION THEREOF
    Publication number: 20240101535
    Abstract: Provided are a dihydroisoquinolinone derivative and an application thereof. The dihydroisoquinolinone derivative is represented by formula I, and comprises a pharmaceutically acceptable salt thereof, or an enantiomer, a diastereomer, a tautomer, a solvate, an isotope substitute, a polymorph, a prodrug or a metabolite thereof. The compound of formula I has higher protein-protein interaction inhibition activity on WDR5, and therefore can be used to prevent or treat diseases associated with WDR5.
    Type: Application
    Filed: December 10, 2021
    Publication date: March 28, 2024
    Inventor: Qiangang ZHENG
  • COMPOUNDS FOR TREATING CERTAIN LEUKEMIAS
    Publication number: 20240101536
    Abstract: Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease.
    Type: Application
    Filed: June 22, 2023
    Publication date: March 28, 2024
    Inventors: F. Anthony ROMERO, Thorsten A. KIRSCHBERG, Randall HALCOMB, Yingzi XU
  • ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
    Publication number: 20240101537
    Abstract: Provided are organometallic compounds comprising a carbazole group as the central moiety to which at least two further groups selected from carbazole and benzo[d]benzo[4,5]imidazo[1,2-a]imidazole are attached. Also provided are formulations comprising these organometallic compounds. Further provided are organic light emitting devices (OLEDs) and related consumer products that utilize these organometallic compounds.
    Type: Application
    Filed: July 26, 2023
    Publication date: March 28, 2024
    Applicant: UNIVERSAL DISPLAY CORPORATION
    Inventors: Hsiao-Fan CHEN, Tyler FLEETHAM, Sean Michael RYNO, Peter WOLOHAN
  • PROTEIN-PROTEIN INTERACTION MODULATORS OF AURORA KINASE A AND THEIR USE IN THE PREVENTION AND/OR TREATMENT OF CANCER
    Publication number: 20240101538
    Abstract: The present invention relates to compounds that modulate the conformation of Aurora Kinase A (AURKA). The compounds of the present invention are also modulators of the interactome of AURKA, and preferably alter the protein-protein interaction of AURKA with binding proteins, such as MYC and/or TPX2. The present invention also pertains to the use of such compounds in the prevention and/or treatment of proliferative diseases, such as cancer, and kits comprising the same.
    Type: Application
    Filed: November 5, 2021
    Publication date: March 28, 2024
    Inventors: Juliander J. REINER, Tatu PANTSAR, Dirk FLÖTGEN, Stefan LAUFER, Lars ZENDER, Melanie HENNING
  • POTENT ASGPR-BINDING COMPOUNDS FOR THE DEGRADATION OF IMMUNOGLOBULINS AND OTHER PROTEINS
    Publication number: 20240101539
    Abstract: Extracellular protein degraders and compositions are provided that have a potent asialoglycoprotein receptor (ASGPR) Binding Ligand bound to an Extracellular Protein Targeting Ligand for the selective degradation of the Target Extracellular Protein, for example immunoglobulin in vivo to treat disorders mediated by the extracellular protein.
    Type: Application
    Filed: July 11, 2023
    Publication date: March 28, 2024
    Applicant: Avilar Therapeutics, Inc.
    Inventors: Jason Allan Wiles, Srinivasa Karra, Mark George Saulnier, Jesse Jingyang Chen, Kevin Tyler Sprott, Soumya Ray
  • TARGETED PROTEIN DEGRADATION OF PARP14 FOR USE IN THERAPY
    Publication number: 20240101540
    Abstract: The present invention relates to quinazolinones and related compounds which degrade PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: July 28, 2023
    Publication date: March 28, 2024
    Inventors: Nicholas Robert Perl, Kevin Wayne Kuntz, Jennifer Downing
  • COMPOUNDS FOR THE TREATMENT OF SARS
    Publication number: 20240101541
    Abstract: Bis-amide inhibitors of SARS-CoV-2 (COVID) and methods of using them to treat a severe acute respiratory syndrome.
    Type: Application
    Filed: November 30, 2021
    Publication date: March 28, 2024
    Applicant: Purdue Research Foundation
    Inventors: Arun K. Ghosh, Andrew Mesecar, Hiroaki Mitsuya
  • ERAP INHIBITORS
    Publication number: 20240101542
    Abstract: The present disclosure relates to novel compounds of formula (I) which are useful as inhibitors of endoplasmic reticulum aminopeptidases (ERAP), in particular as inhibitors of ERAP2. The disclosure also relates to the therapeutic use of these compounds, in particular the use of these compounds in the treatment or prophylaxis of proliferative disorders, autoinflammatory disorders and autoimmune disorders.
    Type: Application
    Filed: December 17, 2021
    Publication date: March 28, 2024
    Inventors: Rebecca DEPREZ POULAIN, Ronan GEALAGEAS, Virgyl CAMBERLEIN, Charlotte TABEY FLEAU, Valentin GUILLAUME, Damien BOSC, Benoit DEPREZ, Pierre SIEROCKI
  • NOVEL BENZOXAZINE COMPOUND, RESIN RAW MATERIAL COMPOSITION CONTAINING THE SAME, CURABLE RESIN COMPOSITION, AND CURED PRODUCT THEREOF
    Publication number: 20240101543
    Abstract: A benzoxazine compound is represented by general formula (1): wherein R1 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R2 represents a divalent group having 1 to 10 carbon atoms, and X represents a single bond, an oxygen atom, a sulfur atom, a sulfonyl group, a carbonyl group, or a divalent group represented by general formula (1a) or general formula (1b), and wherein R3 and R4 each independently represent hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkyl halide group having 1 to 10 carbon atoms, or an aryl group having 6 to 12 carbon atoms, R3 and R4 are optionally bonded to each other to together form a cycloalkylidene group having 5 to 20 carbon atoms, An and Are each independently represent an aryl group having 6 to 12 carbon atoms, and * represents a bonding position.
    Type: Application
    Filed: January 24, 2022
    Publication date: March 28, 2024
    Inventor: Yoshimi UTAKA
  • INHIBITORS OF QPCTL AND QPCT
    Publication number: 20240101544
    Abstract: Provided herein are compounds of formula (I) and formula (II) that are inhibitors of QPCTL and QPCT: Also provided are pharmaceutical compositions comprising the compounds, and methods for using the compounds for the treatment of disease.
    Type: Application
    Filed: July 20, 2023
    Publication date: March 28, 2024
    Inventors: James M. Veal, Jeffrey A. Stafford, Donald S. Karanewsky, Shyama Herath
  • SUBSTITUTED NICOTINIMIDE INHIBITORS OF BTK FOR TREATING CANCER
    Publication number: 20240101545
    Abstract: Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).
    Type: Application
    Filed: October 27, 2023
    Publication date: March 28, 2024
    Inventors: Xiangyang CHEN, Yingxiang GAO, Chong LIU, Haihong NI
  • HETEROARYL-ACETYLENES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND THEIR THERAPEUTIC APPLICATIONS
    Publication number: 20240101546
    Abstract: Provided herein are heteroaryl-acetylene compounds, e.g., a compound of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of GPX4-mediated disorders, diseases, or conditions.
    Type: Application
    Filed: December 3, 2022
    Publication date: March 28, 2024
    Inventors: Sheldon Cao, Chaoran Huang, Xiaolie Wang
  • METHOD FOR PREPARING 2-[2-(2-CHLOROTHIAZOL-5-YL)-2-OXO-ETHYL]SULFANYL-6-HYDROXY-3-METHYL-5-PHENYL-PYRIMIDIN-4-ONE
    Publication number: 20240101547
    Abstract: The present invention relates to a method for preparing 2-[2-(2-chlorothiazol-5-yl)-2-oxo-ethyl]sulfanyl-6-hydroxy-3-methyl-5-phenyl-pyrimidin-4-one or a tautomer thereof, to 2-[2-(2-chlorothiazol-5-yl)-2-oxo-ethyl]sulfanyl-6-hydroxy-3-methyl-5-phenyl-pyrimidin-4-one or a tautomer thereof and to its use as intermediate in the preparation of 2,3-dihydrotheiazolo [3,2-a]pyrimidinium compounds, and specifically of 3-(2-chlorothiazol-5-yl)-8-methyl-7-oxo-6-phenyl-2,3-dihydrothiazolo [3,2-a]pyrimidin-4-ium-5-olate and enantiomerically enriched forms thereof.
    Type: Application
    Filed: January 21, 2022
    Publication date: March 28, 2024
    Inventors: Christopher Koradin, Martin John McLaughlin, Roland Goetz, Rahul Kaduskar, Harish Shinde, Guillaume Michel Jacques Garivet
  • HYDROXAMATE COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
    Publication number: 20240101548
    Abstract: The present invention relates to a hydroxamate compound represented by formula (I), a preparation method therefor, and an application thereof. The present invention also relates to a pharmaceutical composition comprising the compound as an active ingredient and a use of the compound or pharmaceutical composition for treating and/or preventing related diseases mediated by TYK2.
    Type: Application
    Filed: December 2, 2021
    Publication date: March 28, 2024
    Inventors: Wei Wang, You Zhou, Song Shan, Desi Pan, Zhibin Li, Xianping Lu
  • N-(2-(4-CYANOTHIAZOLIDIN-3-YL)-2-OXOETHYL)-QUINOLINE-4-CARBOXAMIDES
    Publication number: 20240101549
    Abstract: Compounds having the structure of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, R1, R2, R3, R4, R5 and R6 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.
    Type: Application
    Filed: December 16, 2021
    Publication date: March 28, 2024
    Inventors: Jonas BRÅNALT, Björn HOLM, Maria JOHANSSON, Olle KARLSSON, Daniel Laurent KNERR, Anneli NORDQVIST, Robert John SHEPPARD, Marianne SWANSON, Anna TOMBERG
  • COMPOUNDS AND USES THEREOF
    Publication number: 20240101550
    Abstract: The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
    Type: Application
    Filed: September 27, 2023
    Publication date: March 28, 2024
    Inventors: Rishi G. VASWANI, David S. HUANG
  • CRYSTAL FORM AND SALT FORM OF BROMINE DOMAIN PROTEIN INHIBITOR AND PREPARATION METHOD THEREFOR
    Publication number: 20240101551
    Abstract: A crystal form and salt form of a bromine domain protein inhibitor represented by formula (I), a preparation method therefor, and a use of the crystal form and salt form in the preparation of a drug for treating diseases mediated by BET protein.
    Type: Application
    Filed: January 19, 2021
    Publication date: March 28, 2024
    Applicants: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., SHOUYAO HOLDINGS (BEIJING) CO., LTD.
    Inventors: Wenwei XU, Zhenliang SHAN, Yingya ZHANG, Guoliang ZHANG, Yun GE, Aiming ZHANG, Xiquan ZHANG
  • CARBONYL HETEROCYCLIC COMPOUND AND APPLICATION THEREOF
    Publication number: 20240101552
    Abstract: Provided is the carbonyl heterocyclic compound shown in formula (I) or a pharmaceutically acceptable salt thereof, capable of being used as a compound having a targeted lanthionine synthetase C-like protein 2 pathway and being used for the treatment of various conditions, including infectious diseases, autoimmune diseases, diabetes, and chronic inflammatory diseases.
    Type: Application
    Filed: September 18, 2021
    Publication date: March 28, 2024
    Inventors: Chaoxin ZHANG, Guangxin XIA, Zhijun XIANG, Ying KE, Jiangsong LOU, Menghao ZHAO, Lijun HAO
  • KRAS G12C INHIBITORS
    Publication number: 20240101553
    Abstract: The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
    Type: Application
    Filed: August 4, 2023
    Publication date: March 28, 2024
    Inventors: Matthew Arnold MARX, James Gail CHRISTENSEN, Christopher Ronald SMITH, James F. BLAKE, Laurence E. BURGESS, Mark Joseph CHICARELLI, Adam COOK, Jay Bradford FELL, John P. FISCHER, Macedonio J. MEJIA, Martha E. RODRIGUEZ, Pavel SAVECHENKOV, Tony P. TANG, Guy P.A. VIGERS
  • CYCLIN-DEPENDENT KINASE 7 (CDK7) NON-COVALENT INHIBITORS
    Publication number: 20240101554
    Abstract: The invention relates to pharmaceutical compounds of formula (I) and pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds as inhibitors of cyclin-dependent kinase 7 (CDK7) and to their use in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: September 24, 2021
    Publication date: March 28, 2024
    Inventors: Laurence Anne MEVELLEC, Sophie COUPA ép. DESCAMPS, Christophe Denis Pascal ADELINET, Yannick Aimé Eddy LIGNY, Christophe MEYER
  • UREA OREXIN RECEPTOR AGONISTS
    Publication number: 20240101555
    Abstract: The present invention is directed to urea compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: December 14, 2021
    Publication date: March 28, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Kira A. Armacost, Maria Irina Chiriac, Danielle M. Hurzy, Jeffrey C. Kern, Jian Liu, Peter J. Manley, Philippe Nantermet, Vanessa L. Rada, Michael T. Rudd, Craig A. Stump
  • COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY
    Publication number: 20240101556
    Abstract: This disclosure features compounds of Formula I (and their pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said compounds are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.
    Type: Application
    Filed: January 7, 2022
    Publication date: March 28, 2024
    Inventors: Shankar Venkatraman, Jason Katz, William R. Roush, Hans Martin Seidel
  • FUSED TRICYCLIC COMPOUNDS AS INHIBITORS OF KRAS G12V MUTANTS
    Publication number: 20240101557
    Abstract: Disclosed are compounds of Formula I, methods of using the compounds for inhibiting KRAS activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with KRAS activity such as cancer.
    Type: Application
    Filed: July 10, 2023
    Publication date: March 28, 2024
    Inventors: GENCHENG LI, LEI LIU, PEI GAN, CHANG MIN, ALEXANDER SOKOLSKY, XIAOZHAO WANG, QINDA YE, LE ZHAO
  • AMPK ACTIVATORS
    Publication number: 20240101558
    Abstract: This disclosure is directed, at least in part, to AMPK activators useful for the treatment of conditions or disorders associated with AMPK. In some embodiments, the condition or disorder is associated with the gut-brain axis. In some embodiments, condition or disorder is associated with systemic infection and inflammation from having a leaky gut barrier. In some embodiments, the AMPK activators are gut-restricted compounds. In some embodiments, the AMPK activators are agonists or partial agonists.
    Type: Application
    Filed: November 1, 2023
    Publication date: March 28, 2024
    Inventors: Iyassu SEBHAT, Shuwen HE, Ann WEBER, Nancy THORNBERRY, Lisa KRUG, Paul RICHARDS, Brett LAURING
  • TRICYCLIC KINASE INHIBITORS AND USES THEREOF
    Publication number: 20240101559
    Abstract: The present disclosure provides compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be kinase (e.g., Janus kinase (JAK) (e.g., Janus kinase 2 (JAK2)) and/or cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 11 (CDK11)) inhibitors. Also provided are pharmaceutical compositions and kits including the provided compounds. Further provided are methods of using the provided compounds, pharmaceutical compositions, and kits (e.g., for treating a disease (e.g., proliferative disease) in a subject in need thereof).
    Type: Application
    Filed: October 2, 2020
    Publication date: March 28, 2024
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Tinghu Zhang, Yao Liu, David Weinstock, Loretta Sze-Mun Li
  • NITROGENOUS HETEROAROMATIC COMPOUNDS FOR ORGANIC ELECTROLUMINESCENT DEVICES
    Publication number: 20240101560
    Abstract: The present invention relates to nitrogen-containing heteroaromatics suitable for use in electronic devices, and to electronic devices, especially organic electroluminescent devices, comprising these compounds.
    Type: Application
    Filed: December 15, 2021
    Publication date: March 28, 2024
    Inventor: Philipp STOESSEL
  • NOVEL TETRAZOLES
    Publication number: 20240101561
    Abstract: This invention relates to tetrazoles and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune diseases and CNS-related diseases.
    Type: Application
    Filed: October 14, 2020
    Publication date: March 28, 2024
    Inventors: Martin Thomas FLECK, Florian Paul Christian BINDER, Georg DAHMANN, Joerg P. HEHN, Uta Friederike LESSEL, Jens WILLWACHER
  • NOVEL COMPOUND, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING RESISTANT CANCER, COMPRISING SAME
    Publication number: 20240101562
    Abstract: The present application relates to a novel compound, and a pharmaceutical composition for preventing or treating resistant cancer, the composition comprising the novel compound or a pharmaceutically acceptable salt thereof. When a composition according to the present application and an anticancer agent are administered together, an excellent anticancer effect may be exhibited.
    Type: Application
    Filed: June 26, 2021
    Publication date: March 28, 2024
    Inventors: Yeo Jin YUN, Hyeong Nam KIM, In Hye LEE
  • NOVEL COMPOUNDS
    Publication number: 20240101563
    Abstract: The present invention relates to novel compounds for the treatment, alleviation or prevention of a group of diseases, disorders and abnormalities which are responsive to the modulation or inhibition of the activation of a component of the NLRP3 inflammasome pathway. In particular, the component of the inflammasome pathway is a NOD-like receptor (NLR) family, pyrin domain-containing protein 3 (NLRP3) inflammasome. More particularly, the compounds of the present invention have the capability to modulate the NLRP3 inflammasome pathway. Further, the compounds of the present invention are suitable for the treatment, alleviation or prevention of a group of diseases, disorders and abnormalities which are responsive to the modulation, in particular decrease of IL-1 beta and/or IL-18 levels.
    Type: Application
    Filed: July 27, 2023
    Publication date: March 28, 2024
    Applicant: AC Immune SA
    Inventor: Jérôme MOLETTE
  • SALTS OF A PI3Kdelta INHIBITOR, CRYSTALLINE FORMS, METHODS OF PREPARATION, AND USES THEREFORE
    Publication number: 20240101564
    Abstract: The present invention relates to salts of a PI3Kdelta inhibitor (referred to as “Compound A” hereinafter), preferably fumarate, and the crystalline forms thereof. The present invention also relates to the process of preparation and uses of the salts and crystalline forms of Compound A.
    Type: Application
    Filed: November 22, 2023
    Publication date: March 28, 2024
    Applicant: BeiGene Switzerland GmbH
    Inventors: Jing LI, Xiaosong YU, Xiaopeng CAI, Zhiwei WANG
  • ORGANIC COMPOUND, LIGHT ABSORPTION SENSOR, SENSOR-EMBEDDED DISPLAY PANEL, AND ELECTRONIC DEVICE
    Publication number: 20240101565
    Abstract: An organic compound is represented by Chemical Formula 1A or Chemical Formula 1B. In Chemical Formulas 1A and 1B, Ar1, Ar2, R1, R2, n, and m are each the same as in the detailed description.
    Type: Application
    Filed: August 18, 2023
    Publication date: March 28, 2024
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Jeong Il PARK, Feifei FANG, Sungyoung YUN, Chul Joon HEO, Kyung Bae PARK, Hwijoung SEO
  • TRICYCLIC UBIQUITIN SPECIFIC PROTEASE 1 INHIBITOR AND USE THEREOF
    Publication number: 20240101566
    Abstract: Disclosed is a tricyclic ubiquitin specific protease 1 inhibitor compound, a pharmaceutically acceptable salt thereof, an ester thereof, a deuterated compound or a stereoisomer thereof; a pharmaceutical composition and a formulation containing the compound, the pharmaceutically acceptable salt thereof, the ester thereof, the deuterated compound or the stereoisomer thereof; a method for preparing the compound, the pharmaceutically acceptable salt thereof, the ester thereof, the deuterated compound or the stereoisomer thereof; and use of the compound, the pharmaceutically acceptable salt thereof, the ester thereof, the deuterated compound or the stereoisomer thereof in the manufacture of a medicament for treating and/or preventing a disease mediated by USP1 and a disease related thereto.
    Type: Application
    Filed: November 1, 2023
    Publication date: March 28, 2024
    Inventors: Bin LIU, Bo CHEN
  • FACTOR XIA INHIBITORS
    Publication number: 20240101567
    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 thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: January 24, 2022
    Publication date: March 28, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: John S. Debenham, Cheng Zhu, Amjad Ali, Sung-Sau So, Ying-Duo Gao
  • NOVEL BENZAZEPINE SPIRO DERIVATIVE
    Publication number: 20240101568
    Abstract: A benzazepine spiro derivative as represented by formula (I) and a pharmaceutically acceptable salt thereof, and the use of a compound in the diagnosis, prevention and/or treatment of diseases related to vasopressin receptors.
    Type: Application
    Filed: November 25, 2021
    Publication date: March 28, 2024
    Inventors: Hongfu LU, Yongcong LV, Yan YE, Jianbiao PENG, Haibing GUO
  • SALT CRYSTALS
    Publication number: 20240101569
    Abstract: The present disclosure relates to free base and salt crystals of 2-(4-acetylbenzyl)-3-((4-fluorophenyl)amino)-5,7,7-trimethyl-7,8-dihydro-2H-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one, composition comprising the same and the method of making and using such free base and salt crystals.
    Type: Application
    Filed: January 27, 2022
    Publication date: March 28, 2024
    Inventor: Peng LI
  • TRICYCLIC CARBOXAMIDE DERIVATIVES AS PRMT5 INHIBITORS
    Publication number: 20240101570
    Abstract: Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formula (I).
    Type: Application
    Filed: November 22, 2021
    Publication date: March 28, 2024
    Inventors: Albert AMEGADZIE, Diane Jennifer BEYLKIN, Shon BOOKER, Matthew Paul BOURBEAU, John R. BUTLER, Sanne Ormholt Schroder GLAD, Todd J. KOHN, Brian Alan LANMAN, Kexue LI, Qingyian LIU, Patricia LOPEZ, Francesco MANONI, Primali Vasundera NAVARATNE, Liping H. PETTUS, Rene RAHIMOFF, Nuria A. TAMAYO, Mikkel VESTERGAARD, Hui-Ling WANG, Nicholas Anthony WEIRES