Abstract: The present description discloses a preferred solution for controlling oxidation of QH without any need for formulation of reduced coenzyme Q10 (QH). One or more embodiments of the present invention relate to a method for storing reduced coenzyme Q10 (QH) or a method for controlling oxidation of QH, the method(s) including storing a composition containing a reduced coenzyme Q10 (QH) and having a water activity at 25° C. of 0.50 or more. One or more other embodiments of the present invention relate to a composition containing QH and having a water activity at 25° C. of 0.50 or more.
Abstract: The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
Type:
Application
Filed:
December 14, 2022
Publication date:
March 27, 2025
Inventors:
Donald J. P. Pinto, Michael J. Orwat, Leon M. Smith ll
Abstract: Novel deuterium- or fluorine-containing chemical compounds are provided. They are centrally acting skeletal muscle relaxants, effective for treating various types of muscle spasms, including acute musculoskeletal pain, low-back pain, inflammatory arthritis, fibromyalgia, and perioperative care for hip and knee replacements or related conditions. In addition, pharmaceutical compositions and methods for their preparation and use are described.
Abstract: A thiol-containing compound having at least two terminal groups of formula —NH—CO—CO—NH—R1—SH where R1 is an alkylene, reaction mixtures containing the thiol-containing compound and an epoxy resin, and compositions containing a polymerized product of the reaction mixture are provided. The compositions that contain the polymerized product of the reaction mixture can be used, for example, as an adhesive or sealant.
Abstract: The present invention relates to a process for separating at least one ?-caprolactam oligomeric compound CPO from a stream SR comprising said at least one CPO and ?-caprolactam monomeric compound CPM.
Type:
Application
Filed:
March 30, 2023
Publication date:
March 27, 2025
Inventors:
Stefan BLEI, Faissal-Ali EL-TOUFAILI, Alexander HETZ-HUNSINGER, Marc FELDEN, Jochen GAUER, Michel GASSMANN, Christian DIENES, Zeljko KOTANJAC, Vikram Raghavendhar RAVIKUMAR, Esther Matyka LARYEA
Abstract: Disclosed am compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and am useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Type:
Application
Filed:
May 23, 2024
Publication date:
March 27, 2025
Inventors:
Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
Abstract: Disclosed are novel hydroxylated psilocybin derivative compounds and pharmaceutical and recreational drug formulations containing the same. The compounds may be produced synthetically or biosynthetically.
Type:
Application
Filed:
December 6, 2024
Publication date:
March 27, 2025
Inventors:
Jillian M. Hagel, Peter J. Facchini, Chang-Chun Ling
Abstract: The present disclosure relates to compounds of Formula (I?): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating orexin receptor activity and may be used in the treatment of disorders in which orexin receptor activity is implicated, such as narcolepsy, a hypersomnia disorder, a neurodegenerative disorder, a symptom of a rare genetic disorder, a mental health disorder, a metabolic syndrome, osteoporosis, cardiac failure, coma, or a complication in emergence from anaesthesia.
Type:
Application
Filed:
August 28, 2024
Publication date:
March 27, 2025
Inventors:
Gregory R. OTT, Karl GIBSON, Bruce LEFKER, Paul HUMPHRIES
Abstract: A compound, to a rubber mixture containing the compound, to a vehicle tire comprising the rubber mixture in at least one component, to a process for producing the compound and to the use of the compound as an aging stabilizer and/or antioxidant.
Abstract: A method of treating an inflammatory disease selected from the group of atherosclerosis, ankylosing spondylitis, and Sjogren syndrome. The method includes administering a quinoline derivative to a patient in need thereof. The quinoline derivative is a compound of formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
December 9, 2024
Publication date:
March 27, 2025
Applicants:
ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
Abstract: A compound, a rubber mixture containing the compound, a vehicle tire comprising the rubber mixture in at least one component, a process for producing the compound and the use of the compound as an aging stabilizer and/or antiozonant and/or dye, in which the compound has the following formula I): wherein R1 is selected from the group consisting of xi) aromatic radicals, wherein the aromatic radicals optionally bear substituents selected from the group consisting of halogen radicals, cyano radicals, ester radicals, ketone radicals, ether radicals and thioether radicals, and xii) linear, branched and cyclic aliphatic C4- to C12-radicals and xiii) combinations of aromatic and aliphatic C1- to C12-radicals.
Type:
Application
Filed:
June 14, 2022
Publication date:
March 27, 2025
Applicant:
Continental Reifen Deutschland GmbH
Inventors:
Andreas Jacob, David-Raphael Dauer, Julian Strohmeier
Abstract: Provided are a diimide derivative represented by formula I, a preparation method therefor and the use thereof. The diimide derivative has a good anti-tumor activity, and the anti-proliferative activity against various cancer cells is significantly better than those of similar compounds.
Type:
Application
Filed:
January 31, 2023
Publication date:
March 27, 2025
Applicants:
XIANGBEI WELMAN PHARMACEUTICAL CO., LTD., GUANGZHOU CENTURY CLINICAL RESEARCH CO., LTD., GUANGZHOU XIN-CHUANGYI BIOPHARMACEUTICAL CO., LTD., GUANGZHOU XIN CHUANG YI NEW DRUG R&D CO.,LTD, NANJING KANGFUSHUN PHARMACEUTICAL CO., LTD.
Abstract: The present invention provides an improved process for the recovery of ?-caprolactam from Nylon 6 comprising multi-component material, in particular multi-layered film. Further, the invention provides a plant configured to carry out the process of the invention, and the recovered e-caprolactam obtainable by the process of the invention that has a product carbon footprint of less than 2.5 kg CO2 equivalent per kg purified e-caprolactam (based on data originating from ecoinvent version 3.7.1; location: Europe).
Type:
Application
Filed:
January 27, 2023
Publication date:
March 27, 2025
Applicant:
CAP III B.V.
Inventors:
Jasper Verduyckt, Marijke Hilde Leen Groothaert, Anna Dite Cuiper, Wenjing Fu, Johan Thomas Tinge
Abstract: This invention relates to pharmaceutically acceptable tryptamine analogues and salts thereof. In particular, though not exclusively, the a invention relates to formulations and uses of the same as a medicament.
Type:
Application
Filed:
January 17, 2022
Publication date:
March 27, 2025
Inventors:
Massimo MURATORE, Amir Lotfi MOGHADDAM, Vinod VISHWAPATHI, Christopher WONG, Oliver MCGAW
Abstract: The objective of the present invention is to develop a reaction control method for an inverse electron-demand Diels-Alder reaction and a method for producing a cycloaddition reaction product using a controlled inverse electron-demand Diels-Alder reaction. The invention provides a reaction control method for an inverse electron-demand Diels-Alder reaction, in which, in a cycloaddition reaction of a reaction substrate and a tetrazine using an inverse electron-demand Diels-Alder reaction, the reaction control for the inverse electron-demand Diels-Alder reaction is conducted using a stimulus-responsive cleavable macrocyclic tetrazine as the tetrazine, and a method for producing a cycloaddition reaction product using an inverse electron-demand Diels-Alder reaction controlled by the reaction control method of the invention.
Type:
Application
Filed:
October 29, 2021
Publication date:
March 27, 2025
Applicant:
TOHOKU UNIVERSITY
Inventors:
Shin MIZUKAMI, Ira NOVIANTI, Toshiyuki KOWADA
Abstract: The present disclosure provides a compound of Formula I, its stereoisomers, intermediates, and pharmaceutically acceptable salts thereof, capable of inhibiting DNA Ligase IV enzyme activity and nonhomologous end joining (NHEJ). The present disclosure also provides a process for preparing the compounds of Formula I and methods thereof.
Type:
Application
Filed:
December 30, 2022
Publication date:
March 27, 2025
Inventors:
Sathees C RAGHAVAN, Ujjayinee RAY, Vindya K GOPINATHA, Shivangi SHARMA, Kempegowda MANTELINGU, Kanchugarakoppal S RANGAPPA, Laijau GOYARY
Abstract: The present invention relates to a process for the production of melamine and the production plant including an off-gas condensation step carried out at a pressure of 70 to 220 bar by feeding gaseous and liquid streams at the same pressure, converting the liquid stream from the off-gas condensation step to a first stream, followed in succession by a high pressure decomposition step, a medium pressure decomposition step, a low pressure decomposition step, and urea concentration step.
Type:
Application
Filed:
September 23, 2024
Publication date:
March 27, 2025
Inventors:
Alberto DE AMICIS, Giuseppe DI RUOCCO, Roberto SANTUCCI, Matteo RABAIOLI, Mattia BOGOTTO, Francesca PETRILLO
Abstract: Embodiments of this disclosure describe a novel method for synthesizing a tetrazole derivative. The distinguishing feature lies in using aminoguanidine nitrate or aminoguanidine bicarbonate as the starting material, replacing the highly sensitive tetrazine. In a single operational step, the aqueous solution of the starting material is treated with sodium nitrite. The treatment resulted in the precipitation a solid product. Without isolating the intermediate, the solid is subjected undergoes Sandmeyer reaction conditions in-situ, involving nitric acid and sodium nitrite. The resulting solid is filtered, washed with cold water and isopropyl alcohol, and dried to obtain the tetrazole derivative. By eliminating the safety risks associated with the Hamiltonian precursor and streamlining the process, the invention offers a safer, more efficient, and commercially viable method for synthesizing the tetrazole derivative.
Abstract: The present invention relates to N-phenylbenzoxazolo-2-amine and N-phenyloxazolopyridin-2-amine derivatives as novel leukotriene B4 receptor inhibitors, and use thereof.
Type:
Application
Filed:
November 25, 2022
Publication date:
March 27, 2025
Applicants:
EWHA UNIVERSITY - INDUSTRY COLLABORATION FOUNDATION, DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
Inventors:
Hyun Ae WOO, Hea-Young PARK, Jihye YOO, Darong KIM, Joohye KIM, Chang-Hoon LEE, Hyun Ji KIM
Abstract: The present disclosure provides cis-5-(hydroxymethyl)morpholine-2-carboxamides that are agonists of somatostatin receptor 4 (SSTR4), and are therefore useful for the treatment of diseases or medical conditions associated with SSTR4. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
Type:
Application
Filed:
July 31, 2024
Publication date:
March 27, 2025
Inventors:
Joerg P. HEHN, Riccardo GIOVANNINI, Elaine PROULX, Heiko SOMMER, Christian SPECKER
Abstract: The present invention belongs to the field of medicinal chemistry, and particularly relates to a pleuromutilin derivative with a thiazole side chain and preparation and application. The pleuromutilin derivative with the thiazole side chain is a compound of formula 2 or a pharmaceutically acceptable salt thereof, and a solvent compound, enantiomer, diastereoisomer, tautomer, or mixture of any proportion of the compound of formula 2 or the pharmaceutically acceptable salt thereof, comprising racemic mixtures: The pleuromutilin derivative has good antibacterial activity, is particularly suitable for use as a novel antibacterial drug for animal or human systemic infection, and has good water solubility.
Abstract: The invention relates to certain 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives as defined herein. These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
Type:
Application
Filed:
September 25, 2024
Publication date:
March 27, 2025
Inventors:
Per-Göran Gillberg, Ingemar Starke, Santosh S. Kulkarni
Abstract: Methods described herein relate to a partial reduction of esters to aldehydes or nitrogen-containing products facilitated by Group IV transition metal catalysts, using hydrosilanes as the reductant. The method allows the product to be preserved at the aldehyde oxidation level rather than over-reduction to the corresponding alcohol and can result in the formation of value-added recycled monomers. Methods described herein can be used for the direct catalytic chemical upcycling of polyester plastic waste through depolymerization transformations.
Type:
Application
Filed:
September 24, 2024
Publication date:
March 27, 2025
Applicant:
BAYLOR UNIVERSITY
Inventors:
Liela A. Romero, Rebecca A. Kehner, Weiheng Huang, Jack Russo
Abstract: Compounds that inhibit p38? MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
Type:
Application
Filed:
December 5, 2024
Publication date:
March 27, 2025
Inventors:
Paul S. SHAPIRO, Alexander D. MACKERELL, Jr., Jeffrey D. HASDAY, Steven FLETCHER
Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, and X, are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.
Type:
Application
Filed:
October 17, 2024
Publication date:
March 27, 2025
Inventors:
Raymond John ANDERSEN, Marianne Dorothy SADAR, Kunzhong JIAN, Nasrin R. MAWJI, Jun WANG, Carmen Adriana BANUELOS, Yu-Chi YANG
Abstract: Compounds of Formulae (I), (II) and (III), including pharmaceutically acceptable salts are described herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions a disease or disorder that can be treated with a KOR agonist and/or MOR agonist. Compounds described herein, along with pharmaceutically acceptable salts and compositions thereof, can be used to alleviate at least one symptom of the disease or disorder described herein.
Abstract: Described herein is the preparation of a compound for treating gout or hyperuricemia and chemical intermediates used in the synthetic process.
Abstract: A photochromic compound represented by General Formula 1, wherein R represents an unsubstituted aliphatic monocyclic ring with 6 or less carbon atoms (including a carbon atom at the 13-position of an indeno-fused naphthopyran), and R1 to R8, B, and B? each independently represent a hydrogen atom or a substituent, provided that one or more of R1 to R8 represent electron-withdrawing groups.
Abstract: Disclosed herein are novel 1,3-benzodioxole esters and their homologues, having various advantages over current compounds used in certain methods of drug-assisted therapy, such as MDMA, together with pharmaceutical compositions containing such 1,3-benzodioxole esters, and methods of their use to treat CNS disorders, and in particular mental health disorders.
Type:
Application
Filed:
January 19, 2023
Publication date:
March 27, 2025
Inventors:
David Nutt, Alan Borthwick, Robin Tyacke
Abstract: The invention pertains to a process for processing a crude lactide comprising the steps of: separating a crude lactide stream comprising L-lactide, D-lactide, and meso-lactide in one or more steps to form a meso-lactide stream comprising at least 50 wt. % of meso-lactide (based on the total weight of lactide in the stream) and at least one purified lactide stream comprising L-lactide and/or D-lactide; oligomerizing the meso-lactide stream to form an oligomer-containing stream comprising lactic acid oligomers; and depolymerizing the oligomer-containing stream to form a product stream comprising meso-lactide, L-lactide and D-lactide. The invention also pertains to a process for producing a polylactide and to a process for producing a racemic mixture of (S)-lactic acid and (R)-lactic acid.
Type:
Application
Filed:
January 20, 2023
Publication date:
March 27, 2025
Inventors:
Hans DE VRIES, Gerrit GOBIUS DU SART, Jan VAN KRIEKEN
Abstract: Pharmaceutical compounds having anticancer activity are disclosed. A pharmaceutical composition may include a therapeutically effective amount of the compound(s) and a pharmaceutically acceptable vehicle. A method of treating a cancer or other disorders involves administering the pharmaceutical composition to an individual in need thereof.
Abstract: Described herein are selective HSD17B13 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of liver disease, metabolic disease, or cardiovascular disease, such as NAFLD or NASH, or drug induced liver injury (DILI).
Abstract: The present invention relates to a method for preparing a class of novel CDK12/13 covalent inhibitors or a pharmaceutical composition thereof, and use thereof. The class of novel CDK12/13 covalent inhibitors of the present invention have a structure shown in formula (I). Such compounds can serve as protein kinase inhibitors, can effectively and highly selectively inhibit the CDK12/13 protein kinase activity, and can inhibit the proliferation, migration, and invasion of various tumor cells.
Type:
Application
Filed:
September 27, 2024
Publication date:
March 27, 2025
Inventors:
Arul M. Chinnaiyan, George X. Wang, Yu Chang, Jean Tien, Ke Ding, Jianzhang Yang, Weixue Huang, Zhen Wang
Abstract: Provided herein are piperidine dione compounds having the following structure: (I) wherein R1, R2, R3, R4, RN, L, V, X, Y, A, A?, a, n and m are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
Type:
Application
Filed:
June 24, 2022
Publication date:
March 27, 2025
Inventors:
Matthew D. ALEXANDER, Matthew D. CORREA, Deepak DALVIE, Virginia Heather Sharron GRANT, Joshua HANSEN, Roy L. HARRIS, III, Evan J. HORN, Dehua HUANG, Christopher MAYNE, Stephen NORRIS, Veronique PLANTEVIN-KRENITSKY, John J. SAPIENZA, Lida TEHRANI, Brandon W. WHITEFIELD
Abstract: Disclosed are compounds I-A and I-B and salts thereof that bind to and modulate cereblon activity. In some embodiments, the binding and modulation of cereblon results in the degradation of IKAROS family zinc finger proteins (e.g., IKZF2).
Abstract: The present invention relates to a compound of general formula (I) inhibiting the transforming growth factor-? (TGF-?) type I receptor (ALK5), 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 diseases or conditions associated with a dysregulation of ALK5 signaling pathway in a mammal.
Type:
Application
Filed:
January 10, 2023
Publication date:
March 27, 2025
Applicant:
CHIESI FARMACEUTICI S.P.A.
Inventors:
Daniela PIZZIRANI, Paolo RONCHI, Donatella RESCIGNO
Abstract: Provided herein is a compound of Formula I: or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or deuterated analog thereof, a pharmaceutical composition comprising a compound of the present invention, together with a pharmaceutically acceptable excipient thereof, and a method of treating cancer with the same.
Type:
Application
Filed:
July 26, 2024
Publication date:
March 27, 2025
Inventors:
Jayaraman Chandrasekhar, Jonah J. Chang, Kevin S. Currie, Stephen D. Holmbo, Jesse M. Jacobsen, David L. Kukla, Seung H. Lee, Yasamin Moazami, Leena B. Patel, Thomas J. Paul, Stephane Perreault, Patrick J. Salvo, Jennifer A. Treiberg, Heath A. Weaver
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:
September 10, 2024
Publication date:
March 27, 2025
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
Abstract: The present disclosure provides compounds of the formula, wherein A, B, G, R2, R6, and X are defined herein, pharmaceutical compositions of the same, and methods for treating or inhibiting development of AGE- and/or ALE-associated complications in subjects in need thereof.
Abstract: Disclosed herein are compounds, compositions, and methods for promoting neuronal growth and/or improving neuronal structure with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the loss of synaptic connectivity and/or plasticity, such as neurological diseases and disorders, with constrained amine psychoplastogens.
Type:
Application
Filed:
December 14, 2022
Publication date:
March 27, 2025
Inventors:
Noel Aaron POWELL, Milan CHYTIL, Andrew Stephen FELTS
Abstract: Provided herein are compounds, or salts (e.g., pharmaceutically acceptable salts), esters, tautomers, prodrugs, zwitterionic forms, or stereoisomers thereof, which compounds comprise one or more deuterium atoms, as well as pharmaceutically compositions comprising the same. Also provided herein are methods of using the same in the treatment of various diseases, disorders, and conditions including cancers and skeletal dysplasias.
Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof wherein X1, R3, R4, a, b, p, q, r, L, and Ring A are as defined herein. The compounds are antagonists of the resistant (R-type) voltage-gated calcium ion channel Cav 2.3. Also disclosed are pharmaceutical compositions comprising the compounds; and the compounds for use in the treatment of diseases modulated Cav 2.3, including neurodegenerative conditions such as Parkinson's disease, focal, drug-resistant forms of epilepsy, and other neurological disorders such as developmental and epileptic encephalopathies and Fragile X syndrome.
Type:
Application
Filed:
November 25, 2022
Publication date:
March 27, 2025
Inventors:
Henning STEINHAGEN, Paolo PEVARELLO, Jean-Francois ROLLAND, Maria Pia CATALANI
Abstract: Disclosed are substituted indole compounds and other substituted nitrogen-containing heteroaryl compounds. The disclosed compounds and compositions thereof may be utilized in methods for inhibiting kalirin, including methods for treating and/or preventing diseases or disorders associated with kalirin activity or expression such as neuropathic pain, chronic pain, and epilepsy.
Abstract: An additive represented by the following formula (III): a resin composition comprising a resin and the additive; a transparent member comprising the resin composition; and a method for imparting ultraviolet absorbency and/or a high refractive index to a matrix comprising the matrix and the additive.
Abstract: The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
Type:
Application
Filed:
January 30, 2023
Publication date:
March 27, 2025
Inventors:
Markus BAENZIGER, Fabrice GALLOU, Fengfeng GUO, Rudolf HÄNGGI, Enjian HAN, Guido JORDINE, Jialiang LI, Weipeng LIU, Bukeyan MIAO, Shaofeng RONG, Ernesto SANTANDREA, Paul Bernd SCHIRNER, Xiaodong SHEN, Can WANG, Hao ZHANG
Abstract: The present disclosure provides a class of compounds including a ligand moiety that specifically binds to a cell surface asialoglycoprotein receptor (ASGPR). The cell surface ASGPR binding compounds can trigger the receptor to internalize into the cell a bound compound. The ligand moieties of this disclosure can be linked to a variety of moieties of interest without impacting the specific binding to, and function of, the cell surface receptor ASGPR. Also provided are compounds that are conjugates of the ligand moieties linked to a biomolecule, such as an antibody, which conjugates can harness cellular pathways to remove specific proteins of interest from the cell surface or from the extracellular milieu. Also provided herein methods of using the conjugates to target a polypeptide of interest for sequestration and/or lysosomal degradation.
Type:
Application
Filed:
December 9, 2024
Publication date:
March 27, 2025
Inventors:
Brett Bradley BUSCH, Justin Thomas ERNST, Garrick K. PACKARD, Jason G. LEWIS, Eric D. TURTLE
Abstract: The invention provides heterobifunctional cotinine-containing compounds, pharmaceutical compositions, and methods of using same to treat medical conditions, such as cancer.