频哪醇,1-(四氢-2H-吡喃-2-基)-1H-吡唑置于正丁基锂,硼酸三异丙酯,水,氯化铵体系中,用 四氢呋喃,Hexanes 作为反应溶剂,化学反应 17.58H,以78%的收率获得产物1-(2-四氢吡喃基)-1H-吡唑-5-硼酸频哪酯 参考文献: Phenylalanine Amide Derivatives Useful For Treating Insulin-Related Diseases And Conditions[fr] Dérivés De La Phénylalanine-Amide Utiles Pour Le Traitement De Maladies Et états Liés à L'Insuline 标题: Phenylalanine Amide Derivatives Useful For Treating Insulin-Related Diseases And Conditions[fr] Dérivés De La Phénylalanine-Amide Utiles Pour Le Traitement De Maladies Et états Liés à L'Insuline
专利号:US-12384788-B2 优先权日:2019-09-13 标 题 :1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds as LRRK2, NUAK1 and/or TYK2 kinase modulators for the treatment of e.g. autoimmune disease 发明人:KOESTLER ROLAND; TASSEL JEAN; THORMANN MICHAEL; YEHIA NASSER; TREML ANDREAS; ALMSTETTER MICHAEL 权利人:ORIGENIS GMBH 摘要:The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49). (Formula (II):
专利号:WO-2025125811-A1 优先权日:2023-12-12 标题:Heterocyclic compounds and their use for the treatment of neurological disorders 发明人:PLOWRIGHT ALLEYN THOMAS; PFEIFFER THOMAS; MÄRCHER-RØRSTED EMIL; DUCKWORTH EDWARD JOSEPH 权利人:ONTRACK THERAPEUTICS LTD 摘要:The present invention relates to novel synthetic compounds of Formula (I) and (II) related to naturally occurring flavonoids such as 7,8-dihydroxyflavone (7,8-DHF). The invention further relates to the method of synthesis, the use of these compounds as research tools and their use as pharmaceuticals.
专利号:US-11236070-B2 优先权日:2019-05-16 标 题 :Chemical process 发明人:BLANK JARRED; KOECHER CHRISTIAN; PACHINGER WERNER HEINZ; PAREDES GALATEA; SPAETI MARKUS 权利人:NOVARTIS AG 摘要:The present invention provides a novel chemical process for the synthesis of the compound N-[4-(Chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxpyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide.
专利号:US-2025026766-A1 优先权日:2022-01-12 标题 :Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors 发明人:LI JING; XU WENQING; WANG ZHIWEI 权利人:BEIGENE LTD 摘要:The present invention relates to compounds containing thiazolopyridyl amide structure, the process for their synthesis, as well as the use of such compounds for inhibiting DNA Polymerase Theta (Pol Theta), and in the treatment of various diseases including cancers.
专利号:CN-117304111-A 优先权日:2023-09-27 标 题:Synthesis method of darostaamine intermediate
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 201. 摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 209.