发明名称 Isoquinolidinobenzodiazepines
摘要 This disclosure provides novel isoquinolidinobenzodiazepines. These compounds can also be incorporated into antibody-drug conjugates.
申请公布号 US9504694(B2) 申请公布日期 2016.11.29
申请号 US201615048865 申请日期 2016.02.19
申请人 Cellerant Therapeutics, Inc. 发明人 Junutula Jagath R.;Jammalamadaka Vasu
分类号 C07D403/12;A61K31/551;C07D519/00;C07K5/062;A61K47/48;C07K16/30;A61K39/00 主分类号 C07D403/12
代理机构 Kilpatrick Townsend and Stockton LLP 代理人 Kilpatrick Townsend and Stockton LLP
主权项 1. A method of treating acute myeloid leukemia (AML) comprising administering to a subject having AML a therapeutically effective amount of a compound having a structure of Formula (I): wherein: the dotted bond shown between —C(Ra)— and —N(Rb)— or —C(Ra′)— and —N(Rb′)— is independently a single bond or a double bond;each of Ra and Ra′ is independently H or OH;each of Rb and Rb′ is not present or is H;R2, R2′, R3, R3′, R4, R4′, R6′ and R6 are each independently selected from H, OH, C1-C10 alkyl, C2-C10 alkenyl or C2-C10 alkynyl;each of R5 or R5′ is independently NH2, CO2H, H, OH, C1-C10 alkyl, C2-C10 alkenyl or C2-C10 alkynyl;each of R7 and R7′ is H;X is: C1-12 alkylene, optionally wherein the alkylene chain is interrupted by one or more hetero atoms selected from the group consisting of O, S, and NH; or—(CH2)m-Q-(CH2)p—, wherein m and p are each independently 0, 1 or 2;Q has a structure of formula: wherein each of R9, R10 and R11 is H, NH2 or CO2H; andJ is CH or N;each of Y and Y′ is independently O, S, or NH;each of Z and Z′ is independently H, R, OH, OR, SH, SR, NH2, or NHR, where each R is independently unsubstituted C1-C12 alkyl.
地址 San Carlos CA US