Patents Issued in October 3, 2024
  • BTK INHIBITORS
    Publication number: 20240327380
    Abstract: Provided are compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R7, R8, R9, A1, A2, Q1, Q2, Q3, A, Z, m and n are as defined herein; pharmaceutical compositions comprising said compounds or pharmaceutically acceptable salts thereof, and pharmaceutically acceptable excipients; and methods of treating a disorder responsive to inhibition of Bruton's tyrosine kinase using said compounds, or pharmaceutically acceptable salts thereof, or said pharmaceutical compositions.
    Type: Application
    Filed: August 5, 2021
    Publication date: October 3, 2024
    Applicant: BIOGEN MA INC.
    Inventors: Brian T. Hopkins, Isaac Marx, Jürgen Schulz, Harold George Vandeveer, Robin Prince, Marta Nevalainen, TeYu Chen, Zain Yousaf, Martin Himmelbauer, Vatee Pattaropong, John Howard Jones, Rab Gilfillan, Edward Yin Shiang Lin, Felix Gonzalez Lopez de Turiso, Bin Ma
  • Compounds and Compositions for Selective Degradation of Engineered Proteins
    Publication number: 20240327381
    Abstract: Provided herein are compounds and compositions thereof for degrading an engineered polypeptide in a cell. In some embodiments, the compounds and compositions are provided for treatment of cancer.
    Type: Application
    Filed: February 7, 2024
    Publication date: October 3, 2024
    Applicants: Celgene Corporation, Bristol-Myers Squibb Company
    Inventors: Laura Akullian D'Agostino, Godwin Kumi, Haibo Liu
  • PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF UBIQUITIN SPECIFIC PROTEASE 19
    Publication number: 20240327382
    Abstract: The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of the ubiquitin specific protease USP19. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in therapy.
    Type: Application
    Filed: March 24, 2022
    Publication date: October 3, 2024
    Inventors: James Samuel Shane ROUNTREE, Steven Kristopher WHITEHEAD, Steven David SHEPHERD, Matthew Duncan HELM, Frank BURKAMP, Colin O'DOWD, Timothy HARRISON
  • PIPERIDINE DERIVATIVE, AND PHARMACEUTIAL COMPOSITION THEREOF, PREPARATION METHOD THEREFOR, AND USE THEREOF
    Publication number: 20240327383
    Abstract: A piperidine derivative, and a pharmaceutical composition thereof, a preparation method therefor, and a use thereof. A compound of the piperidine derivative is as shown in formula (I), and definitions of substituents are detailed in the description. The piperidine derivative can be used as a bifunctional selective ligand for a ?(mu)-opioid peptide receptor (MOPR) and a ?(kappa)-opioid peptide receptor (KOPR), or a bifunctional selective ligand for a MOPR and a nociceptin opioid peptide receptor (NOPR)/opioid receptor like-1 (ORL-1) receptor. Such a compound or a pharmaceutical composition thereof can be used for treating pain, anxiety, depression, alcohol addiction, and substance abuse/dependence.
    Type: Application
    Filed: July 14, 2022
    Publication date: October 3, 2024
    Applicants: YICHANG HUMANWELL PHARMACEUTICAL CO., LTD., TSINGHUA UNIVERSITY
    Inventors: Jian WANG, Xijun SHENG, Lie LI, Luanyuan TIAN, Jinliang LV, Miao WANG, Hao ZHOU, Xiaoqing YANG
  • SALTS AND SOLID STATE FORMS OF A KIF18A INHIBITOR COMPOUND
    Publication number: 20240327384
    Abstract: Disclosed herein is a salt, a crystalline anhydrous form, a hydrate, a solvate, or a co-crystal of a free base compound 2-(6-azaspiro[2.5]octan-6-yl)-N-[2-(4,4-difluoropiperidin-1-yl)-6-methylpyrimidin-4-yl]-4-[(2-hydroxyethanesulfonyl)amino]benzamide (Compound A); method of preparation, pharmaceutical compositions, and method of treating a disease mediated by a motor protein kinesin family member 18A (KIF18A) inhibition, wherein said disease is a neoplastic disease, including a cancer or a tumor.
    Type: Application
    Filed: July 21, 2022
    Publication date: October 3, 2024
    Applicant: Amgen Inc.
    Inventors: Tian WU, Prashant AGARWAL, Andreas R. ROTHELI, Hyunsoo PARK, Michael J. FROHN
  • SUBSTITUTED PIPERIDINE COMPOUNDS AS RENIN INHIBITORS
    Publication number: 20240327385
    Abstract: Compounds having the formula I or II, pharmaceutical compositions containing the same, and their uses as renin inhibitors.
    Type: Application
    Filed: March 7, 2024
    Publication date: October 3, 2024
    Inventor: Guibai LIANG
  • AHR INHIBITOR, USE THEREOF, AND PREPARATION METHOD THEREFOR
    Publication number: 20240327386
    Abstract: The present disclosure relates to a compound having an AhR inhibitory effect as shown in FIG. (I) or a pharmaceutically acceptable salt thereof, and a use thereof and a preparation method therefor. The compound has obvious AhR inhibitory activity.
    Type: Application
    Filed: September 13, 2022
    Publication date: October 3, 2024
    Inventors: Yuxun WANG, Xiaohui LIU, Zhicheng JIANG, Jichao WU, Xiaoquan WU, Qi HUANG, Shengyong YANG
  • TRIAZINE DERIVATIVES FOR THE TREATMENT OF TUMOURS AND NEURODEGENERATIVE DISORDERS
    Publication number: 20240327387
    Abstract: The present invention relates to compounds of Formula (I) to their pharmaceutical composition and their use as a medicament, in particular for the treatment and/or prevention of a tumour, viral infection, bacterial infection or neurodegenerative disease.
    Type: Application
    Filed: June 23, 2022
    Publication date: October 3, 2024
    Inventors: Luciana Marinelli, Daniela Arosio, Pierfausto Seneci
  • QUINOLINAMINE COMPOUND, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF IN PHARMACEUTICALS
    Publication number: 20240327388
    Abstract: The present invention relates to a quinolinamine compound, a preparation method therefor and an application thereof in pharmaceuticals. Specifically, the present invention relates to a quinolinamine compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof as a therapeutic agent, especially use thereof as a miRNA regulator and use thereof in preparation of a drug for treating diseases or conditions that can be improved by regulating miRNA levels.
    Type: Application
    Filed: May 27, 2022
    Publication date: October 3, 2024
    Inventors: Fanglong YANG, Minqiang JIA, Huanyu TANG, Yonglei QUE, Feng HE, Weikang TAO
  • LACTONE AND LACTAM CONTAINING COMPOUNDS USEFUL AS IMMUNOMODULATORS
    Publication number: 20240327389
    Abstract: The present disclosure generally relates to lactone and lactam containing compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds. and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
    Type: Application
    Filed: May 4, 2022
    Publication date: October 3, 2024
    Inventors: TAO WANG, Zhongxing Zhang, Zhiwei Yin
  • SUBSTITUTED NITROGEN CONTAINING COMPOUNDS
    Publication number: 20240327390
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is: each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
    Type: Application
    Filed: May 9, 2024
    Publication date: October 3, 2024
    Inventors: Navnath Dnyanoba Yadav, Rajeev S. Bhide, Rajesh Onkardas Bora, Prashantha Gunaga, Manoranjan Panda, Eldon Scott Priestley, Jeremy Richter
  • PREPARATION OF OXINDOLE DERIVATIVES AS NOVEL DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 INHIBITORS
    Publication number: 20240327391
    Abstract: Invented are compounds of formula I and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I to a patient in need thereof.
    Type: Application
    Filed: May 23, 2024
    Publication date: October 3, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Yeon-Hee Lim, Jianming Bao, James P. Roane
  • HETEROCYCLOALKYL-SUBSTITUTED POLYHETEROAZOLE DERIVATIVES AS MEDICAMENTS FOR TREATING AND/OR PREVENTING RS VIRUS INFECTIONS
    Publication number: 20240327392
    Abstract: The present invention provide compounds useful for treating and/or preventing RS virus infections. The present invention relates to compounds represented by formula (I), its enantiomer, or a pharmaceutically acceptable salt thereof: wherein Y1, Y2, Y3 and X4 and so on are as defined in the specification; as well as a use of the compounds for treating and/or preventing RS virus infections, and pharmaceutical compositions comprising those compounds.
    Type: Application
    Filed: June 24, 2022
    Publication date: October 3, 2024
    Inventors: Shigeru MATSUOKA, Hiroshi TSUCHIKAWA, Kentaro YAMADA, Akira KATO
  • FERROPTOSIS MODULATORS, PREPARATIONS, AND USES THEREOF
    Publication number: 20240327393
    Abstract: Provided are compounds of Formula I, compositions comprising the same, and methods of using the same, including use in treating various diseases and conditions, e.g., those involving ferroptosis.
    Type: Application
    Filed: July 8, 2022
    Publication date: October 3, 2024
    Inventors: Jianguang HAN, Zhiyuan ZHANG, Weijie HOU, Yimin JIANG, Yanping XU
  • HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN THE TREATMENT OR AMELIORATION OF CANCER
    Publication number: 20240327394
    Abstract: The present invention relates to compounds of formula (I) or salts, solvates, cocrystals, tautomers, or mixtures thereof. Furthermore, the present invention relates to pharmaceutical compositions comprising said compounds. Moreover, the present invention relates to the compounds of formula (I) or the salts, solvates, cocrystals, tautomers, or mixtures thereof or the pharmaceutical compositions for use as a medicament and to the compounds of formula (I) or the salts, solvates, cocrystals, tautomers, or mixtures thereof or the pharmaceutical compositions for use in the treatment or amelioration of cancer. Optionally, the compounds of formula (I) or the salts, solvates, cocrystals, tautomers, or mixtures thereof or the pharmaceutical compositions are administered in combination with a second therapeutic agent, in particular an anti-cancer agent.
    Type: Application
    Filed: April 7, 2022
    Publication date: October 3, 2024
    Inventors: Charles-Henry Fabritius, Koen Hekking, Dorothea Gruber, Rutger Folmer, Stefanie Flückiger-Mangual, Thomas Bohnacker, Martin Schwill, Debora Schmitz-Rohmer
  • A PROCESS FOR PREPARING BENZOXAZINONE COMPOUNDS
    Publication number: 20240327395
    Abstract: The present disclosure provides a process for preparing a compound of Formula I, the process comprising: a. mixing a compound of Formula II with a compound of Formula III in a mole ratio range of 1:1 to 1.3:1 to obtain a first mixture; b. adding a solvent to the first mixture to obtain a second mixture followed by cooling the second mixture; c. contacting a scavenger with the second mixture to obtain a reaction mass; and d. heating the reaction mass followed by addition of a reagent to obtain the compound of Formula I, wherein X is selected from Cl, Br, I, or CN; and the scavenger in step c and the reagent in step d are added in single lot.
    Type: Application
    Filed: August 11, 2022
    Publication date: October 3, 2024
    Inventors: Srikrishnan RAJAIAH, Dinesh MURUGAN, R. KUPPUSWAMY
  • TRI-SUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF PI3-KINASE AND AUTOPHAGY PATHWAYS
    Publication number: 20240327396
    Abstract: The present disclosure relates to tri-substituted aryl and heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for modulating autophagy or preventing, reversing, slowing or inhibiting the PI3K-AKT-MTOR pathway, and methods of treating diseases that are associated with autophagy or the PI3K-AKT-MTOR pathway.
    Type: Application
    Filed: June 12, 2024
    Publication date: October 3, 2024
    Applicant: Neuropore Therapies, Inc.
    Inventors: Emily M. STOCKING, Wolfgang J. WRASIDLO
  • Pesticidally Active Fused Bicyclic Heteroaromatic Compounds
    Publication number: 20240327397
    Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides.
    Type: Application
    Filed: July 27, 2022
    Publication date: October 3, 2024
    Applicant: SYNGENTA CROP PROTECTION AG
    Inventors: Thomas PITTERNA, Jagadeesh Prathap KILARU, Mangala PHADTE, Simone BERARDOZZI, Matthias WEISS, Andre JEANGUENAT, Michel MUEHLEBACH, Roger Graham HALL
  • COMPOSITIONS AND METHODS FOR MAKING AND USING SMALL MOLECULES FOR THE TREATMENT OF HEALTH CONDITIONS
    Publication number: 20240327398
    Abstract: The novel compounds, compositions and methods disclosed herein are effective for treating a subject having or suspected of developing a health condition, for example, cancer (i.e. brain cancer or a cancer metastasizing to the brain). The method of treating cancer can include administering a pharmaceutical composition to a subject, the composition including at least one of the novel compounds disclosed herein, and optionally, one or more additional anti-cancer therapies. The compounds, compositions and methods can be further used for drug screening and other methods of detection and isolation.
    Type: Application
    Filed: February 28, 2024
    Publication date: October 3, 2024
    Inventors: Vijay Gokhale, Teri C. Suzuki
  • THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS AND USES THEREOF
    Publication number: 20240327399
    Abstract: Disclosed herein are compounds of Formula (I): that inhibit DNA Polymerase Theta (Pol?) activity, in particular inhibit Pol? activity by inhibiting ATP dependent helicase domain activity of Pol?. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Pol? such as cancer, including homologous recombination (HR) deficient cancers.
    Type: Application
    Filed: May 10, 2024
    Publication date: October 3, 2024
    Inventors: Janos BOTYANSZKI, Kevin Duffy, Young Eun Choi, Claire L. Neilan, Marcus M. Fischer
  • COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH
    Publication number: 20240327400
    Abstract: The present disclosure relates to novel 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: June 29, 2021
    Publication date: October 3, 2024
    Inventors: Daniel L. Sun, Michael E. Jung, Daniel Gil, William E. Lowry, Heather R. Christofk, Aimee Flores, Xiaoguang Liu
  • FUSED RING COMPOUND, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
    Publication number: 20240327401
    Abstract: A fused ring compound shown in formula I or a pharmaceutically acceptable salt has a novel structure and good SOS1 inhibitory activity.
    Type: Application
    Filed: August 3, 2022
    Publication date: October 3, 2024
    Applicant: EVOPOINT BIOSCIENCES CO., LTD.
    Inventors: Dongdong WU, Xin LI, Jiajing XU, Linfeng XU, Yuchuan WU, Yonghan HU
  • PYRIMIDINE OR PYRIDINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND APPLICATION THEREOF IN PHARMACY
    Publication number: 20240327402
    Abstract: A pyrimidine or pyridine derivative having a structure represented by formula (I), a preparation method therefor, a pharmaceutical composition containing same, a use thereof as an EGFR inhibitor, and a use thereof in the preparation of a drug for treating and/or preventing cancer, tumors, or metastatic diseases associated at least in part with EGFR exon 20 insertions, deletions, or other mutations, especially a use thereof in the preparation of a drug for treating and/or preventing hyperproliferative diseases and the induction of cell death disorders.
    Type: Application
    Filed: August 3, 2022
    Publication date: October 3, 2024
    Inventors: Tao FENG, Baowei ZHAO, Mingming ZHANG, Shuqun YANG, Hongping YU, Zhui CHEN, Yaochang XU
  • PYRIDO[2,3-d]PYRIMIDIN-7-ONES AND RELATED COMPOUNDS AS INHIBITORS OF PROTEIN KINASES
    Publication number: 20240327403
    Abstract: Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.
    Type: Application
    Filed: February 20, 2024
    Publication date: October 3, 2024
    Applicants: UNIVERSITY OF HOUSTON SYSTEM, TRUSTEES OF TUFTS COLLEGE
    Inventors: Gregory Cuny, Sameer Nikhar, Alexei Degterev
  • HETEROCYCLIC GLP-1 AGONISTS
    Publication number: 20240327404
    Abstract: The present disclosure relates generally to GLP-1 agonists and pharmaceutical compositions comprising the same, as well as methods for treating a GLP-1 associated disease, disorder, or condition.
    Type: Application
    Filed: April 5, 2024
    Publication date: October 3, 2024
    Inventors: Wei HUANG, Hui LEI, Chunliang LU, Haizhen ZHANG
  • THIOAMIDE DERIVATIVE AND PREPARATION METHOD AND APPLICATION THEREOF
    Publication number: 20240327405
    Abstract: A thioamide derivative of formula (I) and a preparation method thereof: An application of the thioamide derivative, or an isomer, a pharmaceutically-acceptable salt, or a prodrug molecule thereof in the preparation of a drug for the treatment of cancer is also provided. The thioamide derivative is a new compound with high antitumor activity, and can be used for antitumor therapy alone or in combination with other drugs.
    Type: Application
    Filed: April 25, 2024
    Publication date: October 3, 2024
    Inventors: Zhengwu SHEN, Bin DENG, Mengqi ZHANG, Hongzhu BIAN
  • POTASSIUM CHANNEL MODULATORS
    Publication number: 20240327406
    Abstract: Ion channel modulator compounds of the formula: (Formula (I)), and related aspects.
    Type: Application
    Filed: August 10, 2022
    Publication date: October 3, 2024
    Inventors: Giuseppe ALVARO, Agostino MARASCO, Dean RIVERS
  • NOVEL INHIBITORS OF AUTOTAXIN
    Publication number: 20240327407
    Abstract: The present invention relates to compounds of the general formula (I) their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds and their use as Autotaxin (ATX) inhibitors.
    Type: Application
    Filed: November 19, 2021
    Publication date: October 3, 2024
    Inventors: Rajiv SHARMA, Rajesh BAHEKAR, Vijay PRAJAPATI, Darshan JOSHI, Kamal DAVE
  • COMPOUNDS CONTAINING TETRAHYDRONAPHTHYRIDINONE OR TETRAHYDROPYRIDOPYRIMIDINONE SKELETON, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
    Publication number: 20240327408
    Abstract: The present invention is related to compounds of formula I containing a tetrahydronaphthyridinone or tetrahydropyridopyrimidinone skeleton and preparation methods therefor. It has been experimentally verified that the compounds containing a tetrahydronaphthyridinone or tetrahydropyridopyrimidinone skeleton have significant agonistic effects on caseinolytic protease P (ClpP), and can be applied in the treatment of various cancers.
    Type: Application
    Filed: July 14, 2022
    Publication date: October 3, 2024
    Applicant: CHINA PHARMACEUTICAL UNIVERSITY
    Inventors: Haiying SUN, Yibei XIAO, Yuantao FU, Rongliang TAN, Guangjun XIE, Jinxin JIANG, Yinan YUAN
  • SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SYNTHESIS
    Publication number: 20240327409
    Abstract: The present invention provides improved methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.
    Type: Application
    Filed: June 12, 2024
    Publication date: October 3, 2024
    Inventors: Peng LI, Qiang ZHANG
  • Monoacylglycerol Lipase Modulators
    Publication number: 20240327410
    Abstract: Bridged compounds of Formula (I) and Formula (II), pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, bipolar disorder), cancers and eye conditions. wherein R2, R3 R4, R5 and R6 are defined herein.
    Type: Application
    Filed: May 24, 2024
    Publication date: October 3, 2024
    Inventors: Michael K. Ameriks, Gang Chen, Chaofeng Huang, Brian Ngo Laforteza, Suchitra Ravula, Wei Zhang
  • SIRT6 ACTIVATORS
    Publication number: 20240327411
    Abstract: The present invention relates to novel small molecule activators of Sirt6, for example, compounds of the general Formula (I), their methods and use for the treatment of various human diseases such as cancer, inflammatory diseases, neurodegenerative diseases, and infectious diseases:
    Type: Application
    Filed: September 21, 2023
    Publication date: October 3, 2024
    Inventors: Jia Zhou, Wenbo Zhang, Hua Liu
  • FACTOR XIIA INHIBITORS
    Publication number: 20240327412
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds: the use of such compounds in medicine; and methods of treating patients with such compounds: wherein A, W, V, Z, U, X, Y and B are as defined herein.
    Type: Application
    Filed: February 18, 2022
    Publication date: October 3, 2024
    Inventors: Rebecca Louise DAVIE, Hannah Joy EDWARDS, Christophe FROMONT, William Jack GREVES, Sally Louise MARSH, Carl Leslie NORTH, Alicja Stela OBARA, Jake Simon PEAT, Stephen John PETHEN, David Philip ROOKER, David Edward CLARK
  • NLRP3 MODULATORS
    Publication number: 20240327413
    Abstract: Described herein are NLRP3 modulators and methods of utilizing NLRP3 modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 28, 2022
    Publication date: October 3, 2024
    Inventors: James COLLINS, Venkat BOLLU, Shendong YUAN, John NUSS
  • CYCLOPROPYL-(HETERO)ARYL-SUBSTITUTED ETHYL- SULFONE / SULFOXIMINE-PYRIDINE N-OXIDE DERIVATIVES
    Publication number: 20240327414
    Abstract: The present invention relates to N-oxide compounds of formula (I) or formula (Ia) or formula (Ib) wherein the variables are as defined in the description and/or in the claims, which can be used as antiparasitic agents for the treatment, prevention and/or control of parasitic infections and/or infestations in/on animals as well as crop protection agents.
    Type: Application
    Filed: February 20, 2024
    Publication date: October 3, 2024
    Inventors: Bart Herlé, Hannes Fiepko KOOLMAN, Alan Long, Robin Meier, Ikki Yonemura
  • Multicomponent Complexes, Including Salts, Crystalline Forms, and Hydrates and Solvates of ENT1 Inhibitors
    Publication number: 20240327415
    Abstract: In some embodiments, the present disclosure relates to multicomponent complexes, such as salts, of Compound 1, and hydrates and solvates thereof. In some embodiments, the present disclosure relates to pharmaceutically acceptable salts of Compound 1, and hydrates and solvates thereof. In some embodiments, the present disclosure relates to crystalline complexes comprising Compound 1 (free base) and a coformer, and hydrates and solvates thereof. In some embodiments, the present disclosure relates to a crystalline salt of Compound 1 comprising Compound 1 (free base) and a salt coformer, and hydrates and solvates thereof. In some embodiments, the present disclosure relates to crystalline forms of Compound 1 (free base), and hydrates and solvates thereof. In some embodiments, the present disclosure relates to compositions, dosage forms, and kits comprising a multicomponent complex as disclosed herein.
    Type: Application
    Filed: March 21, 2024
    Publication date: October 3, 2024
    Applicant: iTeos Belgium SA
    Inventors: Ron Lawrence, Hayley Ann Reece, Juliet Adeoye, Laura Allan, Erica Joke Katelijne Heleen Houthuys
  • Further Substituted Triazolo Quinoxaline Derivatives
    Publication number: 20240327416
    Abstract: The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
    Type: Application
    Filed: May 14, 2024
    Publication date: October 3, 2024
    Inventors: Florian JAKOB, Jo ALEN, Simon LUCAS, Tobias CRAAN, Ingo KONETZKI, Achim KLESS, Stefan SCHUNK, Paul RATCLIFFE, Sebastian WACHTEN, Simon CRUWYS
  • HETEROCYCLIC COMPOUNDS
    Publication number: 20240327417
    Abstract: Disclosed herein is a compound of Formula (I) having the following structure for activating T cells, promoting T cell proliferation, and/or exhibiting antitumor activity, a method of using the compounds disclosed herein for treating cancer, and a pharmaceutical composition comprising the same.
    Type: Application
    Filed: June 4, 2024
    Publication date: October 3, 2024
    Applicant: Beigene Switzerland GMBH
    Inventors: Guoliang Zhang, Zhikun Ni, Jianzhuang Miao, Ce Wang
  • MULTI-TARGET INHIBITOR TARGETING HDAC AND NAD SYNTHESIS AND USE OF MULTI-TARGET INHIBITOR
    Publication number: 20240327418
    Abstract: A compound targeting HDAC and NAD synthesis and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof, as well as preparation and application thereof. Specifically, a compound shown in structural general formula (I) and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof are provided. The compound of the structural general formula (I) is a multi-target inhibitor, targeting HDAC and NAD targets, and exhibiting significant HDAC inhibitory activity, while representative compounds exhibit certain NAD inhibitory activity.
    Type: Application
    Filed: August 1, 2022
    Publication date: October 3, 2024
    Inventors: Xiaoyang LI, Zhongren ZHOU, Yuqi JIANG, Kairui YUE, Wenfang XU
  • SYNTHESIS OF SUBSTITUTED TRICYCLIC AMIDES AND ANALOGUES THEREOF
    Publication number: 20240327419
    Abstract: The present disclosure includes synthetic methods for preparing certain substituted tricyclic amides, which can be used to treat, ameliorate, and/or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a subject.
    Type: Application
    Filed: July 15, 2022
    Publication date: October 3, 2024
    Inventors: Jeremy Mason, Mahesh Pallerla, Ganapati Reddy Pamulapati
  • FERROPTOSIS INHIBITOR AND USE THEREFOR
    Publication number: 20240327420
    Abstract: The present invention provides a means whereby it is possible to clarify the mechanism of manifestation of symptoms, an illness, or dysfunction caused by mitochondrial dysfunction and prevent or treat symptoms, an illness, or dysfunction relating to the same mechanism of manifestation. One embodiment of the present invention relates to a ferroptosis inhibitor containing a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof as an active ingredient. Another embodiment of the present invention relates to a medicine that contains the ferroptosis inhibitor as an active ingredient and is for use in the prevention or treatment of symptoms, an illness, or dysfunction relating to ferroptosis. Yet another embodiment of the present invention relates to a compound represented by formula (I-1), a salt thereof, or a solvate thereof.
    Type: Application
    Filed: November 14, 2022
    Publication date: October 3, 2024
    Applicant: JICHI MEDICAL UNIVERSITY
    Inventors: Hitoshi OSAKA, Akihiko MIYAUCHI, Eriko JIMBO, Mizuki KOBAYASHI
  • Substituted (4-Hydroxyphenyl)Cycloalkane and (4-Hydroxyphenyl)Cycloalkene Compounds and Uses Thereof as Selective Agonists of the Estrogen Receptor Beta Isoform for Enhanced Memory Consolidation
    Publication number: 20240327421
    Abstract: Disclosed are substituted (4?-hydroxylphenyl) cycloalkane compounds and substituted (4?-hydroxylphenyl) cycloalkene compounds and there use as selective agonists of the estrogen receptor beta isoform (ER?). The disclosed compounds may be formulated as pharmaceutical compositions and administered for treating diseases associated with ER activity, such as neurological, psychiatric, and/or cell proliferative diseases and disorders as well as for enhancing memory consolidation in subjects in need thereof.
    Type: Application
    Filed: February 16, 2024
    Publication date: October 3, 2024
    Inventors: William A. Donaldson, Daniel S. Sem, Karyn M. Frick
  • HETEROCYCLE-CONTAINING ORGANIC COMPOUNDS, MIXTURES AND ORGANIC ELECTRONIC DEVICES
    Publication number: 20240327422
    Abstract: The present application discloses heterocyclic-containing organic compounds, mixtures and organic electronic devices. The heterocyclic group-containing organic compounds in the present application have good performance of transferring and adjusting charge balance, and can be used as host materials in an organic electronic device, thereby improving the luminous efficiency and the lifetime of the device.
    Type: Application
    Filed: April 22, 2022
    Publication date: October 3, 2024
    Applicant: Guangzhou Chinaray Optoelectronic Materials Ltd.
    Inventors: Ruifeng HE, Canjie WU, Xuexiong WU, Jingyao SONG
  • A SERIES OF PYRROLE DERIVATIVES AND THEIR PREPARATION METHOD AND THERAPEUTIC USE
    Publication number: 20240327423
    Abstract: The invention discloses a series of pyrrole derivatives and their preparation method and therapeutic use. This type of compounds can be used as DHODH-specific inhibitors that have significant inhibitory and blocking effects on fungal DHODH. The compounds can be used for treatment of diseases caused by fungal infections. They can also be used to prepare agricultural fungicides. The anti-fungal activity of the compounds thus hold great promise in the future.
    Type: Application
    Filed: October 27, 2021
    Publication date: October 3, 2024
    Inventors: Shenghong HUANG, Renchong YAO, Zhiquan SONG, Shoubing YI, Chenguang YUAN, Yingfu LI
  • SUBSTITUTED POLYCYCLIC PYRIDONE DERIVATIVES AND PRODRUGS THEREOF
    Publication number: 20240327424
    Abstract: The present inventon provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.
    Type: Application
    Filed: January 26, 2024
    Publication date: October 3, 2024
    Inventors: Makoto KAWAI, Kenji TOMITA, Toshiyuki AKIYAMA, Azusa OKANO, Masayoshi MIYAGAWA
  • KRAS G12D INHIBITOR AND USE THEREOF
    Publication number: 20240327425
    Abstract: A KRAS inhibitor compound represented by formula (I), and an isomer or a pharmaceutically acceptable salt thereof. The compound represented by formula (I) and the composition thereof can effectively treat diseases related to KRAS mutation.
    Type: Application
    Filed: June 30, 2022
    Publication date: October 3, 2024
    Inventors: Feng WANG, Jinglu WANG, Chuanxiu ZHANG, Feng Zhou, Man ZHANG, Daxin GAO
  • CRYSTALLINE FORMS OF CEFTIBUTEN
    Publication number: 20240327426
    Abstract: Disclosed herein are crystalline forms of ceftibuten, methods of making such crystalline forms, and methods of using such crystalline forms. The crystalline forms of ceftibuten may be used in combination with ?-lactamase inhibitors for the treatment of bacterial infections.
    Type: Application
    Filed: June 17, 2022
    Publication date: October 3, 2024
    Inventors: Scott J. Hecker, David Jonaitis
  • NEW COMPOUNDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
    Publication number: 20240327427
    Abstract: Disclosed herein are novel drugs useful in treating Alzheimer's Disease and methods of use.
    Type: Application
    Filed: October 22, 2021
    Publication date: October 3, 2024
    Applicant: Icahn School of Medicine at Mount Sinai
    Inventors: Bin Zhang, Jian Jin, Husnu Umit Kaniskan, Lihuai Qin, Minghui Wang, Aiqun Li, Kristen J. Brennand, Eric E. Schadt, Vahram Haroutunian, Lap Ho, Xianxiao Zhou, Zhenyu Yue
  • Inhibitors of human immunodeficiency virus replication, method of making and method of using thereof
    Publication number: 20240327428
    Abstract: The present application describes compounds of capsid inhibitors that are useful for treating HIV infection in a human. One aspect of the present application relates to a compound of Formula I, stereoisomers thereof, pharmaceutically acceptable salts thereof, or deuterium substitutes thereof as described in the present disclosure.
    Type: Application
    Filed: February 22, 2024
    Publication date: October 3, 2024
    Inventors: Jinzi Jason WU, Bin LIANG, Bailing YANG
  • [1,3]Thiazolo[4,5-d]-pyrimidon-7-ones as inhibitors of NOX4
    Publication number: 20240327429
    Abstract: The present disclosure provides [1,3]thiazolo[4,5-d]-pyrimidon-7-ones that are inhibitors of NOX4, and are therefore useful for the treatment of diseases treatable by inhibition of NOX4. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
    Type: Application
    Filed: February 27, 2024
    Publication date: October 3, 2024
    Inventors: Christian GNAMM, Elmar BAUSCHATZ, Frank BUETTNER, Cédrickx GODBOUT, Annekatrin Charlotte HEIMANN, Christoph HOENKE, Ferenc KONTES, Christian Andreas KUTTRUFF, Dieter WIEDENMAYER, Raphael WILDERMUTH