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US 2024/0391920 A1Published application
Ring-modified proline short peptide compound and use thereof
AssigneeFujian Akeylink Biotechnology Co., Ltd.
InventorsShuhui CHEN, Yaxun YANG, Jianchen ZHANG, Peng LI, Haiying HE, Zheng WANG, Jian LI
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Abstract
Disclosed are a ring-modified proline short peptide compound and the use thereof, and specifically disclosed is a compound represented by formula (X) or a pharmaceutically acceptable salt thereof.
Claims20
A compound represented by formula (X) or a pharmaceutically acceptable salt thereof,
- wherein,
- G is selected from
- ring A is selected from C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl;
- R1 is each independently selected from halogen, OR11, CN, CH3S(O)m—, —NH(R12), C1-3 alkyl and C1-3 haloalkyl;
- R11 is selected from H, C1-3 alkyl, C1-3 haloalkyl, CH3(OCH2CH2)p— and H(OCH2CH2)q—;
- R12 is selected from C1-3 alkyl, C1-3 haloalkyl, CH3CO— and CH3SO2—;
- m is selected from 0, 1 and 2;
- p and q are selected from 1, 2, 3, 4, 5 and 6;
- n is selected from 0, 1, 2, 3 and 4;
- X is selected from —CH(R3)—, —CH2CH2—, O, S, Se, SO2 and —N(R3)—, and the —CH2CH2— is optionally substituted by 1, 2, 3 or 4 R;
- R is each independently selected from halogen, OH, NH2, CN, C1-3 alkyl and C1-3 haloalkyl;
- R3 is each independently selected from H, C1-3 alkyl, C1-3 alkoxy, C1-3 haloalkyl, C1-3 haloalkoxy, C6-10 aryl and 5- to 10-membered heteroaryl, and the C6-10 aryl and 5- to 10-membered heteroaryl are optionally substituted by 1, 2 or 3 R31;
- R2 and R4 together with the atoms to which they are attached form C5-8 cycloalkyl, 5- to 6-membered heterocycloalkyl or 5- to 6-membered heterocycloalkenyl, and the C5-8 cycloalkyl, 5- to 6-membered heterocycloalkyl or 5- to 6-membered heterocycloalkenyl is optionally and independently substituted by 1 or 2 Ra;
- Ra is each independently selected from H, halogen, C1-3 alkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-6 cycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl, and the C3-6 cycloalkyl, C6-10 aryl and 5- to 10-membered heteroaryl are optionally substituted by 1, 2 or 3 R41;
- R21, R31 and R41 are each independently selected from halogen, OH, NH2, CN, C1-3 alkyl, C1-3 alkoxy, C1-3 haloalkyl and C1-3 haloalkoxy;
- R5 is selected from C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, —CH2—R6 and —CH2—O—R6;
- R6 is selected from phenyl, and the phenyl is optionally substituted by 1, 2 or 3 R61;
- R61 is selected from halogen, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy and C1-3 haloalkoxy.
15 more elements
A compound represented by the following formula or a pharmaceutically acceptable salt thereof, selected from
A compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and the compound is selected from:
- wherein,
- ring A is selected from C3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl and phenyl;
- R1 is each independently selected from halogen, OR11, CN, CH3S(O)m—, NHR12 and C1-3 alkyl, and the C1-3 alkyl is optionally substituted by 1, 2 or 3 F;
- R11 is selected from H, C1-3 alkyl, CH3(OCH2CH2)p— and H(OCH2CH2)q—, and the C1-3 alkyl is optionally substituted by 1, 2 or 3 halogens;
- R12 is selected from C1-3 alkyl, CH3CO— and CH3SO2—, and the C1-3 alkyl is optionally substituted by 1, 2 or 3 halogens;
- m is selected from 0, 1 and 2;
- p and q are selected from 1, 2, 3, 4, 5 and 6;
- n is selected from 0, 1, 2, 3 and 4;
- R2 is H, R3 and R4 together with the carbon atoms to which they are attached form C3-6 cycloalkyl, and the C3-6 cycloalkyl is optionally substituted by 1 or 2 Ra;
- or,
- R3 is H, R2 and R4 together with the carbon atoms to which they are attached form C5-8 cycloalkyl, and the C5-8 cycloalkyl is optionally substituted by 1 or 2 Ra;
- Ra is each independently selected from H and C1-3 alkyl;
- the “heterocycloalkyl” contains 1, 2 or 3 heteroatoms or heteroatom groups independently selected from O, S, SO2, N, P and Se;
- the carbon atom with “*” is a chiral carbon atom, which exists in a form of (R) or (S) single enantiomer or in a form rich in one enantiomer.
11 more elements
Dependencies are inferred from the claim text.