欧盟法规
ECHA物质C&L通报专利信息
专利号:US-2025129021-A1
优先权日:2023-09-19
标 题:Small molecule protein synthesis modulators
发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:WO-2023086801-A1
优先权日:2021-11-09
标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-2024325572-A1
优先权日:2021-07-15
标 题 :N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives as fluorophors for detection of amyloid and amyloid-like proteins for diagnosis of neurodegenerative disorders
发明人:SARRAF STELLA T
权利人:AMYDIS INC
摘要:Provided herein is the design and synthesis of novel molecular rotor fluorophores of formula I useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are the compounds for use in methods for diagnosis and treatment of diseases associated with an amyloid or amyloid like proteins, such as e.g. Alzheimer's disease or traumatic brain injury (TBI), Parkinson's disease, vascular dementia, amyotrophic lateral sclerosis, Down syndrome, traumatic brain injury, chronic traumatic encephalopathy, schizophrenia or depression. Exemplary compounds are e.g. N-heterocyclyl substituted 2-cyano-3-(naphthalen-2-yl)acrylamide derivatives, such as e.g. (E)-2-cyano-N-(2-(2-hydroxy)ethoxy)ethyl)-3-(6-(pyrrolidin-1-yl)naphthalen-2-yl) acrylamide (example 1): Experimental data on in-vitro binding studies with amyloid beta is provided.
专利号:US-4870189-A
优先权日:1987-01-28
标 题:Process for synthesis of azetidine and novel intermediates therefor
发明人:LO YOUNG S; SHAMBLEE DWIGHT A; CAUSEY DAVID H; MAYS RICHARD P
权利人:ROBINS CO INC A H
摘要:A novel process is described for preparing azetidine and 2 or 3 methyl and ethyl azetidine free bases by reacting primary arylmethylamine having suitable bulk providing substituents attached to the methyl carbon and an appropriate propane derivative having leaving groups in the one and three position in hot organic solvent containing a non-nucleophilic base and an amount of water sufficient to promote azetidine ring formation to give N-protected-azetidines and deprotecting by hydrogenolysis under acidic conditions to give an acid salt of the azetidines and thereafter flashing off vaporized azetidine from a hot, agitated strong base solution or slurry and condensing to give the liquid azetidine free bases.
专利号:US-4966979-A
优先权日:1987-01-28
标题 :Process for synthesis of azetidine and novel intermediates therefor
发明人:LO YOUNG S; SHAMBLEE DWIGHT A; CAUSEY DAVID H; MAYS RICHARD P
权利人:ROBINS CO INC A H
摘要:A novel process is described for preparing azetidine and 2 or 3 methyl and ethyl azetidine free bases by reacting primary arylmethylamine having suitable bulk providing substituents attached to the methyl carbon and an appropriate propane derivative having leaving groups in the one and three position in hot organic solvent containing a non-nucleophilic base and an amount of water sufficient to promote azetidine ring formation to give N-protected-azetidines and deprotecting by hydrogenolysis under acidic conditions to give an acid salt of the azetidines and thereafter flashing off vaporized azetidine from a hot, agitated strong base solution or slurry and condensing to give the liquid azetidine free bases.
专利号:US-9045520-B2
优先权日:2008-12-23
标题:Synthesis of purine nucleosides
发明人:CHUN BYOUNG-KWON; DU JINFA; RACHAKONDA SUGUNA; ROSS BRUCE; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; CHANG WONSUK; ZHANG HAI-REN; NAGARATHNAM DHANPALAN
权利人:CHUN BYOUNG-KWON; DU JINFA; RACHAKONDA SUGUNA; ROSS BRUCE; SOFIA MICHAEL JOSEPH; PAMULAPATI GANAPATI REDDY; CHANG WONSUK; ZHANG HAI-REN; NAGARATHNAM DHANPALAN; GILEAD PHARMASSET LLC
摘要:A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.