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CAS号21717-96-4 2-氨基-5-氟吡啶 | CAS号1114523-56-6 1-(2-溴-5-氟吡啶-4-基)乙酮 | CAS号1104606-44-1 1-(5-氟-2-吡啶基)-2-氯乙酮 | CAS号1052714-48-3 6-溴-3-氟甲酸吡啶 | CAS号327056-62-2 2-氰基-5-氟吡啶 | CAS号148541-70-2 5-氟-2-吡啶羧酸乙酯 | CAS号791819-04-0 5-氟-2-吡啶硼酸频哪醇酯 | CAS号31181-88-1 5-氟吡啶-2-醛 | CAS号802325-29-7 (5-氟吡啶-2-基)甲醇 | CAS号1005291-43-9 2-溴-5-氟-4-吡啶甲醛 | CAS号827579-38-4 (2-aminophenyl)...2-氨基-5-氟吡啶 反应生成 2-溴-5-氟吡啶
参考文献:羧酰胺基-二芳基醚作为类阿片受体拮抗剂(opras)的构效关系研究.第1部分.
标题:羧酰胺基-二芳基醚作为类阿片受体拮抗剂(opras)的构效关系研究.第1部分.
摘要:已经发现一种结构独特的新型类阿片受体拮抗剂(opra),其与吗啡或内源性阿片肽不具有结构相似性.一系列的羧酰胺基-二芳基醚被确定为针对mu,Kappa和delta阿片样物质受体的有效受体拮抗剂.结构-活性关系表明,在远端苯环上带有胺系的对位取代的芳氧基芳基伯羧酰胺是对三种阿片受体亚型有效的体外功能拮抗作用的最佳选择.
DOI:10.1016/j.Bmcl.2007.08.008
专利信息
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:WO-2023122754-A1
优先权日:2021-12-23
标 题 :Processes and intermediates for preparing gb13, gb22 and himgaline
发明人:LANDWEHR ELEANOR; SHENVI RYAN; BAKER MEGHAN; OGUMA TAKUYA
权利人:SCRIPPS RESEARCH INST
摘要:Provided herein are processes for the streamlined synthesis of Galbulimima alkaloids, such as himbadine, isolated from Galbulimima belgraveana and G. baccatta, trees endemic to the rainforests of Northern Australia and Papua New Guinea, as well as analogs thereof, such as GB13, GB16, GB22, and himgaline, and further including intermediates useful in the synthesis of these and related compounds.
专利号:US-8138188-B2
优先权日:2006-02-23
标题 :Melanocortin type 4 receptor agonist piperidinoylpyrrolidines
发明人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; LANSDELL MARK IAN; SUMMERHILL NICHOLAS WILLIAM
权利人:ANDREWS MARK DAVID; BROWN ALAN DANIEL; LANSDELL MARK IAN; SUMMERHILL NICHOLAS WILLIAM; PFIZER
摘要:The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) n nwherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in medicine, particularly in the treatment of sexual dysfunction and obesity, to intermediates useful in their synthesis and to compositions containing them.
专利号:US-9192612-B2
优先权日:2013-02-13
标题:Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; BECK ELIZABETH MARY; DAVOREN JENNIFER ELIZABETH; LACHAPELLE ERIK ALPHIE; O'NEILL BRIAN THOMAS
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nand the variables R 1 and R 2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-12152038-B2
优先权日:2017-09-05
标 题:Vasopressin receptor antagonists and products and methods related thereto
发明人:JONES ROBERT M; URBANO MARIANGELA; BRANDT GARY; CHAMBERS MARK; HARDICK DAVID; KNIGHT CHRIS; TIERNEY JASON; LOCK CHRIS
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 Q1, Q2, Q3, R2a, R2b, R3 and X are as defined herein.
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.