PARP inhibitor containing piperazine structure. preparation method therefor and pharmaceutical use thereof
AssigneeWigen Biomedicine Technology (Shanghai) Co., Ltd.
InventorsYuli Xie, Yongcong Lv, Lihui Qian, Houxing Fan
Life of this patent
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Abstract
Disclosed in the present invention are a PARP inhibitor containing a piperazine structure, a preparation method therefor and pharmaceutical use thereof. Particularly, the present invention relates to novel compounds of general formulas (1), (2), (3), (4) and (5) and/or a pharmaceutically acceptable salt thereof, a composition comprising the compounds of general formulas (1), (2), (3), (4) and (5) and/or the pharmaceutically acceptable salt thereof, a preparation method therefor and use thereof as a PARP inhibitor in the preparation of anti-tumor drugs.
Claims6
A compound of general formula (1), or an optical isomer, a crystalline form, a pharmaceutically acceptable salt, a hydrate, or a solvate thereof:
- wherein in general formula (1):
- R1 is (C1-C4) alkyl, (C1-C4) fluoroalkyl, or (C3-C5) cycloalkyl;
- R2 is H or (C1-C3) alkyl;
- R3 is H, F, Cl, (C1-C4) alkyl, or (C1-C4) fluoroalkyl;
- n is 1 or 2;
- R4 and R5 represent two substituents on a cycloalkyl ring, and are each independently H or F;
- and
- X1 and X2 are each independently CH or N.
A compound of general formula (5), or an optical isomer, a crystalline form, a pharmaceutically acceptable salt, a hydrate, or a solvate thereof:
- wherein in general formula (5):
- R1 is (C1-C4) alkyl, (C1-C4) fluoroalkyl, or (C3-C5) cycloalkyl;
- R3 is H, F, Cl, (C1-C4) alkyl, or (C1-C4) fluoroalkyl;
- R7 is H, (C1-C4) alkyl or (C3-C4) cycloalkyl substituted with 0-2 F;
- and
- X6 is NR8, O or CR9R10, R8 is H or (C1-C3) alkyl, and R9 and R10 are each independently H, (C1-C3) alkyl, (C1-C3) fluoroalkyl, or (C3-C4) cycloalkyl.
Dependencies are inferred from the claim text.