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US 2026/0297069 A1Published application
Cyclopentylpyrazolamine derivative and use thereof
AssigneeChia Tai Tianqing Pharmaceutical Group Co., Ltd.
InventorsYong GAO, Yanpeng JI, Damin ZHAO, Lu FAN, Jinan WANG, Bin CAO, Yinsheng ZHANG
Life of this patent
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Abstract
The field of medicinal chemistry, relates to a cyclopentylpyrazolamine derivative and the use thereof, and specifically relates to a compound of formula (I), an isomer thereof, or a pharmaceutically acceptable salt thereof.
Claims20
A compound of formula (I), an isomer thereof, or a pharmaceutically acceptable salt thereof,
- wherein
- X1, X2, and X3 are each independently selected from the group consisting of N and C(Ra);
- Z1, Z2, and Z3 are each independently selected from the group consisting of O, S, N, N(Rb), S(O), S(O)2, C(O), C(Ra), and C(RaRa);
- L1 and L2 are each independently selected from the group consisting of a single bond, —N(Rb)—, —N═, —O—, —S—, —(CH2)m—, —(CD2)m-, —(CHD)m-, —C(═O)—, —S(═O)—, —S(═O)2—, —S(═O)(═N(Rb))—, —S(═O)(Rc)—, —P(═O)(Rc)—, and —P(═O)(NRbRb)—;
- R1 is selected from the group consisting of H, deuterium, C1-3 alkyl, C1-3 alkoxy, —NH2, —NH(C1-3 alkyl), —N(C1-3 alkyl)2, C3-6 cycloalkyl, C3-6 cycloalkenyl, 3- to 6-membered heterocyclyl, phenyl, and 5- to 6-membered heteroaryl, the C1-3 alkyl or C1-3 alkoxy being optionally independently substituted with 1, 2, or 3 Rd, and the C3-6 cycloalkyl, C3-6 cycloalkenyl, 3- to 6-membered heterocyclyl, phenyl, or 5- to 6-membered heteroaryl being optionally independently substituted with 1 or more Re;
- A is selected from the group consisting of
- and 3- to 6-membered heterocyclyl containing 1 or 2 N atoms, the 3- to 6-membered heterocyclyl being optionally independently substituted with 1 or more Rz;
- R2, R3, and R4 are each independently selected from the group consisting of H, deuterium, halogen, OH, CN, NH2, C1-3 alkyl, C1-3 alkoxy, C3-6 cycloalkyl, C3-6 cycloalkenyl, and 3- to 6-membered heterocyclyl, the C1-3 alkyl, C1-3 alkoxy, C3-6 cycloalkyl, C3-6 cycloalkenyl, or 3- to 6-membered heterocyclyl being optionally independently substituted with 1 or more Rz;
- or, R2 and R3, together with the carbon atom linked thereto, form C3-6 cycloalkyl, C3-6 cycloalkenyl, or 3- to 6-membered heterocyclyl, and R4 is selected from the group consisting of H, deuterium, halogen, OH, CN, NH2, C1-3 alkyl, and C1-3 alkoxy, the C1-3 alkyl, C1-3 alkoxy, C3-6 cycloalkyl, C3-6 cycloalkenyl, or 3- to 6-membered heterocyclyl being optionally independently substituted with 1 or more Rz;
- or, R2, R3, and R4, together with the carbon atom linked thereto, form C5-8 bicycloalkyl or 5- to 8-membered heterobicycloalkyl, the C5-8 bicycloalkyl or 5- to 8-membered heterobicycloalkyl being optionally independently substituted with 1 or more R2;
- Ra is each independently selected from the group consisting of hydrogen, deuterium, halogen, OH, CN, NH2, COOH, NO2, C1-3 alkyl, C1-3 alkoxy, C1-3 alkoxy C1-3 alkylene, C1-3 alkylamino, and (C1-3 alkyl)2 amino, the C1-3 alkyl or C1-3 alkoxy being optionally independently substituted with 1 or more Rx;
- or, the two Ra in C(RaRa), together with the carbon atom linked thereto, form C3-6 cycloalkyl, C3-6 cycloalkenyl, or 3- to 6-membered heterocyclyl, the C3-6 cycloalkyl, C3-6 cycloalkenyl, or 3- to 6-membered heterocyclyl being optionally independently substituted with 1 or more Ry;
- Rb is each independently selected from the group consisting of H, C1-3 alkyl, C1-3 alkoxy, —C(═O)H, —S(═O)2C1-3 alkyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, and 3- to 6-membered heterocyclyl, the C1-3 alkyl or C1-3 alkoxy being optionally independently substituted with 1, 2, or 3 Rx, and the C3-6 cycloalkyl, C3-6 cycloalkenyl, or 3- to 6-membered heterocyclyl being optionally independently substituted with 1 or more Ry;
- Rc is selected from the group consisting of halogen, OH, CN, and C1-3 alkyl, the C1-3 alkyl being optionally independently substituted with 1 or more Rx;
- Rd is each independently selected from the group consisting of deuterium, halogen, OH, CN, and NH2;
- Re is each independently selected from the group consisting of deuterium, halogen, OH, CN, NH2, ═O, C1-3 alkyl, and C1-3 alkoxy, the C1-3 alkyl or C1-3 alkoxy being optionally independently substituted with 1 or more Rx;
- Rx is each independently selected from the group consisting of deuterium, halogen, OH, CN, and NH2;
- Ry is each independently selected from the group consisting of deuterium, halogen, OH, CN, NH2, ═O, C1-3 alkyl, and C1-3 alkoxy, the C1-3 alkyl or C1-3 alkoxy being optionally independently substituted with 1 or more substituents selected from the group consisting of deuterium, halogen, OH, CN, and NH2;
- Rz is each independently selected from the group consisting of deuterium, halogen, OH, CN, NH2, C1-3 alkyl, and C1-3 alkoxy, the C1-3 alkyl or C1-3 alkoxy being optionally independently substituted with 1 or more substituents selected from the group consisting of deuterium, halogen, OH, CN, and NH2;
- m is selected from the group consisting of 1, 2, and 3;
- the carbon atom with “*” is a chiral carbon atom present in a form of a single (R) or (S) enantiomer or in a form enriched with one enantiomer;
- or, L1, L2, R1, R2, R3, R4, Ra, Rb, Rc, Rd, Re, Rx, Ry, or Rz is each independently optionally substituted with one or more substituents.
19 more elements
A compound of the formula below, an isomer thereof, or a pharmaceutically acceptable salt thereof,
A compound of the formula below, an isomer thereof, or a pharmaceutically acceptable salt thereof,
Dependencies are inferred from the claim text.