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:US-9067934-B2 优先权日:2011-03-31 标题 :Bicyclic pyridinones 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; FISH BENJAMIN ADAM; GREEN MICHAEL ERIC; MULLINS PATRICK BRADLEY; STIFF CORY MICHAEL; TRAN TUAN PHONG; NAVARATNAM THAYALAN 权利人:PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
参考标题:Synthesis Of Phenanthridines Through Palladium-Catalyzed Cascade Reaction Of 2-Halo-N-Ms-Arylamines With Benzyl Halides/sulfonates 作者:Si-Yi Yang,Wen-Yong Han,Ding-Lei Zhang,Xiao-Jian Zhou,Mei Bai,Bao-Dong Cui,Nan-Wei Wan,Wei-Cheng Yuan,Yong-Zheng Chen |发布日期:2017.2.3 摘要:An Efficient Palladium-Catalyzed Nucleophilic Substitution/c-H Activation/aromatization Cascade Reaction Between Readily Available 2-Halo-N-Ms-Arylamines (Ms = Methanesulfonyl) And Benzyl Halides/sulfonates Has Been Described. A Wide Variety Of Phenanthridines Were Synthesized In A One-Pot Fashion In Moderate To High Yields (37-86 %). Notably, This Method Provides A Straightforward, Facile Approach
合成参考文献
参考文献:10.1007/978-981-16-4655-3_3 摘要:Kaur N. Thiazole Synthesis by Thionation of C=O to C=S. 2021 Sep 11. In: Lawesson’s Reagent in Heterocycle Synthesis.