5-氨基-2-三氟甲基吡啶置于n-氯代丁二酰亚胺体系中,用 乙腈 用作溶剂,化学反应 2.0H,反应生成3-氨基-2-氯-6-三氟甲基吡啶 参考文献: Compounds And Compositions As Tlr-7 Activity Modulators[fr] Composés Et Compositions Permettant De Moduler L'Activité Des Tlr-7 标题: Compounds And Compositions As Tlr-7 Activity Modulators[fr] Composés Et Compositions Permettant De Moduler L'Activité Des Tlr-7 摘要:这项发明提供了包含这些化合物的免疫原组合物和药物组合物,以及使用这些化合物治疗或预防与toll样受体7相关的疾病或紊乱的方法.在一个方面,这些化合物可用作增强疫苗效果的佐剂.
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):