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-2021085684-A1 优先权日:2016-07-06 标 题:Pde9 inhibitors for treatment of peripheral diseases 发明人:SVENSTRUP NIELS; PARACHIKOVA ANNA I; MCARTHUR JAMES 权利人:IMARA INC 摘要:The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyperplasia, beta thalassemia, and sickle cell disease.
专利号:CN-115785096-A 优先权日:2022-11-22 标 题:Method for highly selective synthesis of pyrazolone spirodihydroquinoline or pyrazolone spiroindoline compound
专利号:CN-115785096-B 优先权日:2022-11-22 标 题 :Method for highly selective synthesis of pyrazolone spirodihydroquinoline or pyrazolone spiroindoline compounds
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.