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-9962690-B2 优先权日:2014-04-27 标题:N-substituted pyridiniophosphines, processes for their preparation and their use 发明人:ALCARAZO MANUEL; WILLE CHRISTIAN; TINNERMANN HENDRIK 权利人:STUDIENGESELLSCHAFT KOHLE MBH 摘要:The present invention deals with the synthesis and applications of new cationic compounds being useful as metal ligands. Specifically, N-alkyl/aryl substituted pyridiniophosphines are prepared and used as ligands for transition metals. The so-obtained metal complexes and their use as catalysts in chemical synthesis is also described. It also worth mentioning that N-alkyl/aryl pyridiniophosphines can be synthesized through a short, scalable and highly modular route.
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.
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摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 202. 摘要:Primer, D. N.; Molander, G. A., Science of Synthesis, (2019) , 267. 摘要:Zeng, X., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 764.