专利号:US-12247037-B2 优先权日:2018-12-12 标题:1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4h-benzo[f][1,2,4]triazolo[4,3-A][1,4]diazepine derivatives and related compounds as vasopressin antagonists for the treatment of neuro-psychological disorders 发明人:BRANDT GARY 权利人:NEUMORA THERAPEUTICS INC 摘要:The present invention relates to 1-(2,6-diazaspiro[3.3]heptan-6-yl)-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine derivatives and related compounds of Formula (I): wherein A, B, G, R1, R1b, RiC, R2 and X are as defined herein. The present compounds are vasopressin receptor antagonists (in particular of the Via receptor) for the treatment of neuro-psychological disorders, such as e.g. autism, anxiety, stress-related disorders, depression, schizophrenia or bipolar disorder. The present description discloses the synthesis of exemplary compounds, as well as pharmacological data thereof (e.g. pages 71 to 246; examples 1 to 49; tables 1 to 5). An exemplary compound is e.g. 8-chloro-1-(2-(5-fluoropyridin-2-yl)-2,6-diazaspiro[3.3]heptan-6-yl)-5-methyl-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine (example 1, compound no. 1).
专利号:US-9744252-B2 优先权日:2011-08-17 标 题:Compounds for binding to the platelet specific glycoprotein IIb/IIIa and their use for imaging of thrombi 发明人:BERGER MARKUS; KRUGER MARTIN; LOHRKE JESSICA; REINHARDT MICHAEL; SIEBENEICHER HOLGER 权利人:PIRAMAL IMAGING SA 摘要:The present invention relates to novel fluorine containing compounds, methods for their preparation, the intermediates of the synthesis, their use as diagnostic agents, especially for imaging of thrombi. The invention relates to positron emission tomography (PET) agents and associated precursor reagents, and methods for producing such radiolaveled agents for imaging of thrombi in a mammalian body. More particularly, the invention relates to small nonpeptide, high-affinity, specific-binding glycoprotein IIb/IIIa antagonists for imaging of thrombi.
专利号:WO-2024041503-A1 优先权日:2022-08-22 标 题:Compounds targeting y220c mutant of p53 发明人:LI SUJING; LI AMIN; ZHENG QIAN; Dang Chaojie; FAN XINRUI; LONG WEI; WANG YANPING 权利人:JACOBIO PHARMACEUTICALS CO LTD 摘要:The present invention discloses compounds of formula (I) which can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Also provided are processes for the synthesis and use of the compounds of formula (I).
专利号:CN-109384651-A 优先权日:2018-12-07 标 题:A novel method for coupling synthesis of 4,4,4-trifluorobutanol
专利号:WO-2023057548-A1 优先权日:2021-10-07 标题:Ccr6 receptor modulators 发明人:AISSAOUI HAMED; ALLEMANN OLIVER; CAROFF EVA; MEYER EMMANUEL; RICHARD-BILDSTEIN SYLVIA 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the prevention or treatment of e.g. inflammatory/autoimmune diseases/disorders and cancer.
专利号:US-11858943-B2 优先权日:2017-06-05 标题:Vasopressin receptor antagonists and products and methods related thereto 发明人:JONES ROBERT M; URBANO MARIANGELA; BRANDT GARY; HARDICK DAVID; KNIGHT CHRIS; TIERNEY JASON 权利人:NEUMORA THERAPEUTICS INC 摘要:Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof:wherein A, B, G, R1, R1b, R1c, R2 and X are as defined herein.