专利号:US-10759743-B2 优先权日:2016-10-24 标 题 :Pd-catalyzed γ-C(sp3)-H arylation / heteroarylation of free amines 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:US-9549917-B2 优先权日:2011-09-08 标 题 :Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases 发明人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS 权利人:MCCOMAS CASEY C; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO; PALANI ANANDAN; DAI XING; LIU HONG; HE SHUWEN; LAI ZHONG; DANG QUN; ZORN NICOLAS; MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:WO-2024185814-A1 优先权日:2023-03-06 标题:Method for producing aryl compound containing tritylsulfanyl group 发明人:OKAZOE TAKASHI; NOZAKI KYOKO; GATZENMEIER Tim; LIU YUE 权利人:AGC INC; UNIV TOKYO 摘要:The present invention provides: a substrate for achieving the highly efficient synthesis of an aryl compound containing a tritylsulfanyl group; a method for producing a compound containing an SF 5 group using the substrate; and others. The present invention is a method for producing an aryl compound containing a tritylsulfanyl group, the method comprising thiotritylating a halogenated aryl compound represented by general formula (1) [wherein A 1 represents an aryl group that may have a substituent or a heteroaryl group that may have a substituent; and X represents a halogen atom] using [(triphenylmethyl)sulfanyl]potassium or [(triphenylmethyl)sulfanyl]sodium to produce an aryl compound containing a tritylsulfanyl group, the aryl compound being represented by general formula (2) [wherein A 1 is the same as A 1 in general formula (1); and Ph represents a phenyl group].
专利号:CN-114014790-A 优先权日:2021-12-03 标 题 :Synthesis method of selenide/thioether compound and synthesized compound
专利号:US-10858359-B2 优先权日:2016-06-07 标题 :Heterocyclic ring derivatives useful as SHP2 inhibitors 发明人:MA CUNBO; GAO PANLIANG; CHU JIE; WU XINPING; WEN CHUNWEI; KANG DI; BAI JINLONG; PEI XIAOYAN 权利人:JACOBIO PHARMACEUTICALS CO LTD 摘要:Provided are certain novel pyrazine derivatives (I) as SHP2 inhibitors which is shown as formula (I), their synthesis and their use for treating a SHP2 mediated disorder. More particularly, provided are fused heterocyclic derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.