Compound used as autophagy regulator, and preparation method therefor and uses thereof
AssigneeWigen Biomedicine Technology (Shanghai) Co., Ltd.
InventorsCheng Luo, Yuli Xie, Bing Zhou, Zhiyi Yao, Liyan Yue, Wei Wan, Bidong Zhang, Yuanyuan Zhang, Hualiang Jiang, Kaixian Chen
Life of this patent
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Abstract
It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators.
Claims6
A compound of general formula (IVd), or pharmaceutically acceptable salts thereof:
- wherein:
- R1 is selected from the group consisting of H deuterium, and C1-6 hydroxyalkyl;
- R3 is selected from the group consisting of
- wherein, Rc, Rc1, Rc2, Rc′ and Rc″ are each independently selected from the group consisting of H, hydroxyl, amino group, NRaRa′, halogen, cyano, nitro, carboxyl, formyl, amide group, ester group, C1-6 haloalkyl, C1-6 hydroxyalkyl, C1-6 alkoxy, C1-6 alkoxyalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, 5-10 membered heteroaryl, C3-10 cycloalkyl, 3-10 membered heterocycloalkyl, 3-7 membered heterocycloalkenyl, C1-6 alkyl C6-10 aryl, 5-10 membered heteroaryl C1-6 alkyl or C1-6 alkyl 5-10 membered heteroaryl;
- and
- Ra and Ra′ are each independently H or C1-6 alkyl;
- or
- R3 is
- Rc is -hydroxyl, amino group, NRaRa′, halogen, cyano, nitro, carboxyl, formyl, amide group, ester group, C1-6 haloalkyl, C1-6 hydroxyalkyl, C1-6 alkoxy, C1-6 alkoxyalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, 5-10 membered heteroaryl, C3-10 cycloalkyl, 3-10 membered heterocycloalkyl, 3-7 membered heterocycloalkenyl, C1-6 alkyl C6-10 aryl, 5-10 membered heteroaryl C1-6 alkyl, or C1-6 alkyl 5-10 membered heteroaryl, and Ra and Ra′ are each independently H or C1-6 alkyl;
- or
- R3 is selected from the following groups:
- wherein, X1 is F, Cl, Br, I or trifluoromethyl;
- X2 is H, F, Cl, Br, or I;
- Rc1, Rc2, Rc3, or Rc4 is each independently selected from the group consisting of H, hydroxyl, amino group, NRaRa′, halogen, cyano, nitro, carboxyl, formyl, amide group, ester group, C1-6 haloalkyl, C1-6 hydroxyalkyl, C1-6 alkoxy, C1-6 alkoxyalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, 5-10 membered heteroaryl, C3-10 cycloalkyl, 3-10 membered heterocycloalkyl, 3-7 membered heterocycloalkenyl, C1-6 alkyl C6-10 aryl, 5-10 membered heteroaryl C1-6 alkyl or C1-6 alkyl 5-10 membered heteroaryl;
- and
- Ra and Ra′ are each independently H or C1-6 alkyl;
- and
- R4 is H;
- unsubstituted or substituted means that the group is unsubstituted or substituted by one or more substituents selected from the group consisting of hydroxyl, amino group, cyano, nitro, carboxyl, halogen, C1-6 alkyl, C1-6 haloalkyl or C1-6 hydroxyalkyl, or two adjacent substituents may be bonded to form a C6-10 aryl group, a C5-10 heteroaryl group, a C3-10 cycloalkyl group or a C3-10 heterocycloalkyl group.
A compound selected from the group consisting of following compounds or pharmaceutically acceptable salts thereof:
- No.
- Structures
- 415
- 416
- 417
- 418
- 419
- 420
- 421
- 422
- 423
- 424
- 425
- 426
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- 428
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- 453
- 454
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- 461
A compound selected from the group consisting of following compounds or pharmaceutically acceptable salts thereof:
- No.
- Structures
- 8
- 17
- 18
- 19
- 20
- 21
- 22
- 23
- 24
- 25
- 26
- 27
- 28
- 29
- 33
- 34
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- 72
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- 90
- 91
- 92
- 93
- 108
- 109
- 110
- 139
- 161
- 171
- 184
- 185
- 186
- 187
- 188
- 189
- 211
- 212
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- 258
- 260
- 263
- 315
- 320
- 322
- 329
- 332
- 353
- 372
- 373
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- 375
- 387
- 392
- 393
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- 400
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- 406
Dependencies are inferred from the claim text.