专利号:US-11702430-B2 优先权日:2018-04-03 标 题:Aza-benzothiophene compounds as STING agonists 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T 权利人:MERCK SHARP & DOHME LLC; ALTMAN MICHAEL D; CASH BRANDON D; CUMMING JARED N; DEMONG DUANE E; HAIDLE ANDREW M; JEWELL JAMES P; LARSEN MATTHEW A; LU MIN; OTTE RYAN D; TAOKA BRANDON M; TROTTER BENJAMIN WESLEY; TRUONG QUANG T 摘要:Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 5 , R 6 , R 8 , R 9 , A, X 1 , X 2 , and X 3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
专利号:CN-109678752-A 优先权日:2018-12-27 标 题:A kind of method for asymmetric transformation and synthesis of L-2-aminobutanamide hydrochloride
专利号:US-8957226-B2 优先权日:2005-09-15 标题 :2-oxo-1-pyrrolidine derivatives, processes for preparing them and their uses 发明人:ATES CELAL; LURQUIN FRANCOISE; QUESNEL YANNICK; SCHULE ARNAUD 权利人:ATES CELAL; LURQUIN FRANCOISE; QUESNEL YANNICK; SCHULE ARNAUD; UCB PHARMA SA 摘要:The present invention relates to optically enriched or substantially optically pure 4-substituted-pyrrolidin-2-ones of formula (III), and their uses for the synthesis of 2-oxo-pyrrolidin-1-yl derivatives.
专利号:CN-101445476-A 优先权日:2008-12-25 标 题:Chemical Synthesis of α-Ethyl-2-oxo-1-pyrrolidine Acetate Methyl Ester
专利号:US-10730849-B2 优先权日:2016-10-04 标 题:Benzo[b]thiophene compounds as STING agonists 发明人:ALTMAN MICHAEL D; CASH BRANDON D; CHANG WONSUK; CUMMING JARED N; HAIDLE ANDREW M; HENDERSON TIMOTHY J; JEWELL JAMES P; LARSEN MATTHEW A; LIANG RUI; LIM JONGWON; LU MIN; OTTE RYAN D; SIU TONY; TROTTER BENJAMIN WESLEY; TYAGARAJAN SRIRAM 权利人:MERCK SHARP & DOHME 摘要:Compounds of general formula (Ia), compounds of general formula (Ia′), compounds of general formula (Ib), compounds of general formula (Ib′), compounds of general formula (I), compounds of general formula (I′), and their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , R 9 , X 1 , X 2 , and X 3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.
专利号:CN-103012190-B 优先权日:2012-12-05 标 题:Synthesis method of S-2-aminobutanamide hydrochloride
[参考文献]: Thomas Hjelmgaard, Et Al. Copper(I) Mediated Cross-Coupling Of Amino Acid Derived Organozinc Reagents With Acid Chlorides. Org Biomol Chem. 2006 May 7;4(9):1796-805.