专利号:WO-2018108954-A1 优先权日:2016-12-12 标题 :Process for the preparation of 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol 发明人:GOSSELIN FRANCIS; LINGHU XIN 权利人:HOFFMANN LA ROCHE; GENENTECH INC 摘要:Methods of making 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol 9, an intermediate useful for the synthesis of estrogen receptor modulating compounds are described.
专利号:US-2009170828-A1 优先权日:2006-06-12 标题:Azetidine Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase 发明人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL 权利人:ISABEL ELISE; OBALLA RENATA; POWELL DAVID; ROBICHAUD JOEL 摘要:Azetidine derivatives of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; liver steatosis; and non-alcoholic steatohepatitis. (I)
专利号:US-8633182-B2 优先权日:2012-05-30 标题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN 权利人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-8785632-B2 优先权日:2004-08-26 标 题:Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors 发明人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE 权利人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE; AGOURON PHARMA; PFIZER 摘要:Enantiomerically pure compound of formula 1 n nare provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
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合成参考文献
参考文献:10.1080/14756366.2022.2070909 摘要:Kaur S, Nieto NS, McDonald P, Beck JR, Honzatko RB, Roy A, Nelson SW. Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase. Journal of Enzyme Inhibition and Medicinal Chemistry. 2022 May 05;37(1):1320–6. doi: 10.1080/14756366.2022.2070909.