Deuterated 1,4-benzodiazepine-2,5-dione compound and use thereof
AssigneeNingbo Combireg Pharmaceutical Technology Co., Ltd.
InventorsGang Liu, Yao Ma, Wenjun Yu
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Abstract
Disclosed are a deuterated 1,4-benzodiazepine-2,5-dione compound and the use thereof. Provided is a compound as represented by formula I or a pharmaceutically acceptable salt thereof. The disclosed 1,4-benzodiazepine-2,5-dione active compound maintains the activity of inhibiting tumor cells and tumor stem cells, and prolongs the degradation function of in-vitro human liver microsomes on the compound, such that the half-life period is significantly prolonged, which provides a safer and more reliable candidate for developing new anti-tumor drugs.
Claims16
A compound represented by formula I or a pharmaceutically acceptable salt thereof,
- wherein, X is hydrogen, fluorine, chlorine, bromine or iodine;
- R1a and R1b are independently hydrogen, deuterium, C1-3 alkyl or deuterated C1-3 alkyl;
- R2a, R2b and R2c are independently hydrogen or deuterium;
- R3, R4 and R5 are independently C1-3 alkyl, C1-3 alkyl-O—, deuterated C1-3 alkyl or deuterated C1-3 alkyl-O—;
- R6 is H, C1-3 alkyl, C2-4 alkenyl, C2-4 alkynyl or deuterated C1-3 alkyl;
- R7 is —OR12, —NR13R14 or —C(R15R16)—P(═O)(OR17OR18), wherein R12, R17 and R18 are independently C1-3 alkyl, deuterated C1-3 alkyl or deuterated C1-3 alkyl-O—;
- R15 and R16 are independently H, C1-3 alkyl or deuterated C1-3 alkyl;
- R13 and R14 are independently OH, C1-3 alkyl, deuterated C1-3 alkyl, C1-3 alkyl-O— or deuterated C1-3 alkyl-O—;
- or, R13 and R14 together with the attached nitrogen atom form:
- a 4- to 6-membered aliphatic heterocycle or a 4- to 6-membered aliphatic heterocycle substituted by one or more R19;
- the 4- to 6-membered aliphatic heterocycle in the 4- to 6-membered aliphatic heterocycle and the 4- to 6-membered aliphatic heterocycle substituted by one or more R19 contains 0-2 heteroatoms selected from N, O or S, besides the 1 N attached to the shown carbonyl;
- R19 is halogen, O═, C1-3 alkyl or deuterated C1-3 alkyl;
- R8, R9, R10 and R11 are independently hydrogen or deuterium;
- wherein, at least one of R1a, R1b, R3, R4, R5, R6, R7, R8, R9, R10 and R11 is deuterium or a deuterated group.
Dependencies are inferred from the claim text.