[EN] COMPOSITIONS AND METHODS FOR CORRECTION OF ABERRANT SPLICING<br/>[FR] COMPOSITIONS ET PROCÉDÉS DE CORRECTION D'ÉPISSAGE ABERRANT
申请人:SKYHAWK THERAPEUTICS INC
公开号:WO2020190793A1
公开(公告)日:2020-09-24
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
Dihydro-10<i>H</i>-indeno[1,2-<i>b</i>]benzofurans and Tetrahydroindeno[1,2-<i>c</i>]isochromenes via Stereoselective Intramolecular Carbocation Cascade Cyclization
Nazarov cyclization of the (E)-(2-stilbenyl)methanols under the catalysis of p-TsOH immobilized on silica (PTS-Si) proceeded to give the corresponding indanyl cation with the exclusive trans relationship at the two newly formed adjacent stereogenic centers. The ensuing intramolecular nucleophilic addition by the MOM-protected phenol (m = 0) or benzyl alcohol (m = 1) furnished the Indane-fused benzofuran
( E )-(2-二苯乙烯基)甲醇在固定于二氧化硅(PTS-Si)上的p -TsOH的催化下进行纳扎罗夫环化,得到相应的茚满基阳离子,在两个新形成的相邻立体中心处具有排他性的反式关系。随后由 MOM 保护的苯酚 ( m = 0) 或苯甲醇 ( m = 1) 进行的分子内亲核加成分别为茚满稠合的苯并呋喃 [5/5] 或异色满 [5/6] 系统提供了专有的顺式两个碳环连接处的立体控制。因此,在一个步骤中,从非手性起始材料,分子内级联碳阳离子环化(CCC)以中等至良好的产率提供了[5/5]或[5/6]含氧茚满稠环系统,并且具有优异的立体选择性。所有三个连续的立体中心。
Methods and compositions for modulating splicing
申请人:SKYHAWK THERAPEUTICS, INC.
公开号:US11008572B2
公开(公告)日:2021-05-18
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.