# US 12,600,731 B2 · Isoxazolo[5,4-H]quinazoline compounds as protein kinase inhibitors

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- Number: US 12,600,731 B2
- Document ID: US12600731B2
- Status: Granted
- Kind: B2
- Application number: 17/640,115
- Filed: 2020-09-03
- Published: 2022-11-17
- Granted: 2026-04-14
- Earliest claimed: 2019-09-05
- Assignees: Chengdu Cynogen Bio-Pharmaceutical Technology Co., Ltd.
- Applicants: Chengdu Cynogen Bio-Pharmaceutical Technology Co., Ltd.
- Inventors: Hang Cheng; Weiyan Xiong; Bin Yu; Wei Niu
- Web page: https://patentgrep.com/patent/US12600731B2

## CPC

- C07D 498/04: Ortho-condensed systems
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61P 35/00: Antineoplastic agents
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present disclosure provides a class of isoxazolo[5,4-H]quinazoline compounds represented by general formula (I), which can be used to treat cell proliferation disorders, and are effective cyclin-dependent kinase (CDK) inhibitors, which have a broad-spectrum and strong inhibitory activity against CDK. The present disclosure also provides a pharmaceutical composition comprising the compound, and a method of treating and/or preventing a CDK-mediated disease in a subject, including administering the compound or the composition of the present disclosure.

## Claims

### Claim 1

A compound of formula (I), or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof:
wherein:
indicates a single bond or a double bond;
A1 is selected from CR5 or N;
A2 is selected from CR6 or N;
A3 is selected from CR7 or N;
R1 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; wherein the said C3-7 cycloalkyl or 3- to 7-membered heterocyclyl is optionally substituted by oxo or thioxo;
R2 is selected from H, D, halogen, —CN, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; wherein the said C3-7 cycloalkyl or 3- to 7-membered heterocyclyl is optionally substituted by oxo or thioxo;
R3 is selected from H, D, halogen, —CN, —NO2, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, —O—C1-6 alkylene-R8, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 11-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl, each of which is optionally substituted by 1, 2, 3, 4, or 5 R8 groups;
R4 is selected from H, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl;
L is selected from a chemical bond, —O—, —NH—, —C(O)—, —C(O)NH—, —NHC(O)—, —C1-6 alkylene-, —C2-6 alkenylene- or —C2-6 alkynylene-;
and wherein,
R5 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R6 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R7 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-ORa, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; or two R8 on the same atom are taken together to form oxo or thioxo;
Ra is independently selected from H, —C0-6 alkylene-CN, —C0-6 alkylene-NO2, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl, —C0-6 alkylene-3- to 7-membered heterocyclyl, —C0-6 alkylene-C6-10 aryl or —C0-6 alkylene-5- to 10-membered heteroaryl;
Rb and Rc are independently selected from H, —C0-6 alkylene-CN, —C0-6 alkylene-NO2, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl, —C0-6 alkylene-3- to 7-membered heterocyclyl, —C0-6 alkylene-C6-10 aryl or —C0-6 alkylene-5- to 10-membered heteroaryl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl;
R″ and R′″ are independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; or, R″, R′″ and N atom are taken together to form 3- to 7-membered heterocyclyl;
m represents 0, 1, or 2;
and,
R1-R2 and R4-R8 are optionally substituted with 1, 2 or 3 R groups, wherein the R is independently selected from H, —OH, halogen, —NO2, carbonyl, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(S)Ra, —C(O)ORa, —C(S)ORa, —C(O)—NRbRc, —C(S)—NRbRc, —O—C(O)Ra, —O—C(S)Ra, —N(Rb)—C(O)—Ra, —N(Rb)—C(S)—Ra, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, —N(Rb)—S(O)m—Ra, —N(Rb)S(O)m—NRbRc, —N(R)C(O)ORa, —N(Rb)—C(S)ORa, —O—C1-6 alkylene-ORa, —C(O)—C1-6 alkylene-NRbRc, —N(Rb)—C(O)—NRbRc, —N(Rb)C(S)—NRbRc, —O—C(O)—NRbRc, —O—C(S)—NRbRc, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; wherein the said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl or 5- to 10-membered heteroaryl is each further optionally substituted by one or more groups consisting of the following:
—CN, —NO2, carbonyl, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(S)Ra, —C(O)ORa, —C(S)ORa, —C(O)—NRbRc, —C(S)—NRbRc, —O—C(O)Ra, —O—C(S)Ra, —N(Rb)—C(O)—Ra, —N(Rb)—C(S)—Ra, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, —N(Rb)—S(O)m—Ra, —N(R)S(O)m—RbRc, —N(Rb)—C(O)ORa, —N(Rb)—C(S)ORa, —O—C1-6 alkylene-ORa, —C(O)—C1-6 alkylene-NRbRc, —N(Rb)—C(O)—NRbRc, —N(R)—C(S)—NRbRc, —O—C(O)—NRbRc or —O—C(S)—NRbRc;
Ra, Rb and Rc are each further optionally substituted by one or more groups consisting of the following:
C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl or 5- to 10-membered heteroaryl.

### Claim 2 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-1):
wherein, each group is as defined in claim 1;
alternatively, which is a compound of general formula (I-1-1):
wherein,
indicates a single bond or a double bond;
A2 is selected from CR6 or N;
A3 is selected from CR7;
L is selected from a chemical bond, —O—, —NH—, —C(O)— or —C1-6 alkylene-;
R3 is selected from H, halogen, —CN, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 11-membered heterocyclyl, the said group is optionally substituted with 1, 2 or 3 R8 groups; alternatively, R3 is 5- to 6-membered heterocyclyl containing at least one N atom, which is optionally substituted with 1 or 2 R8 groups; alternatively, R3 is piperazinyl, morpholinyl, thiomorpholinyl or piperidinyl, which is optionally substituted with 1 or 2 R8 groups;
R4 is selected from H, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R6 is selected from H, halogen, —CN, C1-6 alkyl or C1-6 haloalkyl;
R7 is selected from H, halogen, —CN, C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-ORa, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl; or two R8 on the same atom are taken together to form oxo or thioxo;
alternatively, which is a compound of general formula (I-1-1):
wherein,
indicates a single bond or a double bond;
A2 is selected from CR6 or N;
A3 is CR7;
L is selected from a chemical bond or CH2;
R3 is selected from 5- to 6-membered heterocyclyl, which is optionally substituted with 1 or 2 R8 groups; alternatively, the 5- to 6-membered heterocyclyl is piperazinyl, morpholinyl, thiomorpholinyl or piperidinyl;
R4 is selected from iPr, iBu or cyclopentyl;
R6 is H or Me;
R7 is H or Me;
R8 is selected from H, Me, Et, iPr, iBu, NEt2, oxo or cyclopropyl.

### Claim 3 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-2):
wherein, each group is as defined in claim 1;
alternatively, which is a compound of general formula (I-2-1):
wherein, each group is as defined in claim 1;
alternatively, which is a compound of general formula (I-2-2):
wherein,
indicates a single bond or a double bond;
A2 is selected from CR6 or N;
L is selected from a chemical bond, —O—, —NH—, —C(O)— or —C1-6 alkylene-;
R3 is selected from H, halogen, —CN, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 11-membered heterocyclyl, the said group is optionally substituted with 1, 2 or 3 R8 groups; alternatively, R3 is 5- to 6-membered heterocyclyl containing at least one N atom, which is optionally substituted with 1 or 2 R8 groups; alternatively, R3 is piperazinyl, morpholinyl, thiomorpholinyl or piperidinyl, which is optionally substituted with 1 or 2 R8 groups;
R4 is selected from H, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R6 is selected from H, halogen, —CN, C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-ORa, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl; or two R8 on the same atom are taken together to form oxo or thioxo;
alternatively, which is a compound of general formula (I-2-2):
wherein,
indicates a single bond or a double bond;
A2 is selected from CR6 or N;
L is selected from a chemical bond or CH2;
R3 is selected from 5- to 6-membered heterocyclyl, which is optionally substituted with 1 or 2 R8 groups; alternatively, the 5- to 6-membered heterocyclyl is piperazinyl, morpholinyl, thiomorpholinyl or piperidinyl;
R4 is selected from iPr, iBu or cyclopentyl;
R6 is H or Me;
R8 is selected from H, Me, Et, iPr, iBu, NEt2, oxo or cyclopropyl.

### Claim 4 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-3):
wherein, each group is as defined in claim 1;
alternatively, which is a compound of general formula (I-3-1):
wherein, each group is as defined in claim 1;
alternatively, which is a compound of general formula (I-3-2):
wherein,
A2 is selected from CR6 or N;
L is selected from a chemical bond, —O—, —NH—, —C(O)— or —C1-6 alkylene-;
R3 is selected from H, halogen, —CN, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 11-membered heterocyclyl, the said group is optionally substituted with 1, 2 or 3 R8 groups; alternatively, R3 is 5- to 6-membered heterocyclyl containing at least one N atom, which is optionally substituted with 1 or 2 R8 groups; alternatively, R3 is piperazinyl or piperidinyl, which is optionally substituted with 1 or 2 R8 groups;
R4 is selected from H, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R6 is selected from H, halogen or —CN;
R8 is selected from H, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl or —C0-6 alkylene-ORa; or two R8 on the same atom are taken together to form oxo or thioxo;
alternatively, which is a compound of general formula (I-3-2):
wherein,
A2 is selected from CR6 or N;
L is selected from a chemical bond or CH2;
R3 is 5- to 6-membered heterocyclyl, the said group is optionally substituted with 1 or 2 R8 groups; alternatively, the 5- to 6-membered heterocyclyl is piperazinyl or piperidinyl;
R4 is selected from iPr, iBu or cyclopentyl;
R6 is H;
R8 is selected from H, Me, Et, iPr, iBu, NEt2 or oxo.

### Claim 5 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-4):
wherein, each group is as defined in claim 1;
alternatively, which is a compound of general formula (I-4-1):
wherein, each group is as defined in claim 1;
alternatively, which is a compound of general formula (I-4-2):
wherein,
A2 is selected from CR6 or N;
L is selected from a chemical bond, —O—, —NH—, —C(O)— or —C1-6 alkylene-;
R3 is selected from H, halogen, —CN, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 11-membered heterocyclyl, the said group is optionally substituted with 1, 2 or 3 R8 groups; alternatively, R3 is 5- to 6-membered heterocyclyl containing at least one N atom, which is optionally substituted with 1 or 2 R8 groups; alternatively, R3 is piperazinyl, morpholinyl, thiomorpholinyl or piperidinyl, which is optionally substituted with 1 or 2 R8 groups;
R4 is selected from H, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R6 is selected from H, halogen, —CN, C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-ORa, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl; or two R8 on the same atom are taken together to form oxo or thioxo;
alternatively, which is a compound of general formula (I-4-3):
wherein,
R3 is 5- to 6-membered heterocyclyl, the said group is optionally substituted with 1 or 2 R8 groups; alternatively, the 5- to 6-membered heterocyclyl is piperazinyl or morpholinyl;
R8 is selected from H or Et.

### Claim 6 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate thereof, and mixtures thereof, which is a compound of general formula (I-5) or (I-5-1):
wherein,
indicates a single bond or a double bond;
R1 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R2 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R3 is —NRbRc, —O—C1-6 alkylene-R8 or 4- to 7-membered heterocyclyl optionally substituted by 1, 2 or 3 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R5 is selected from H, D, halogen, ORa, —NRbRc, —S(O)mRa, —S(O)mORa or —S(O)mNRbRc;
R6 is selected from H, D, halogen, —S(O)mRa, —S(O)mORa or —S(O)mNRbRc;
R7 is selected from H, D, halogen, —S(O)mRa, —S(O)mORa or —S(O)mNRbRc;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
R8 is optionally substituted with 1, 2 or 3 R groups, wherein the R is independently selected from H, —OH, halogen, —NO2, carbonyl, —CN, —ORa, —SRa or —NRbRc;
Ra is independently selected from H, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
Rb and Rc are independently selected from H, —C0-6 alkylene-S(O)mR′, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 haloalkyl;
m represents 0, 1, or 2.

### Claim 7 (depends on 6)

The compound of formula (I-5) or (I-5-1) according to claim 6, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
indicates a single bond or a double bond;
R1 is selected from H, D, halogen, —CN or —ORa;
R2 is selected from H, D, halogen, —CN or —ORa;
R3 is —NRbRc, —O—C1-6 alkylene-R8 or 5- to 6-membered heterocyclyl optionally substituted by 1 or 2 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R5 is selected from H, D, halogen or ORa;
R6 is selected from H, D or halogen;
R7 is selected from H, D or halogen;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
R8 is optionally substituted with 1, 2 or 3 R groups, wherein the R is independently selected from H, —OH, halogen, —NO2, carbonyl, —CN, —ORa, —SRa or —NbRc;
Ra is independently selected from H, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
Rb and Rc are independently selected from H, —C0-6 alkylene-S(O)mR′, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 haloalkyl;
m represents 0, 1, or 2.

### Claim 8 (depends on 6)

The compound of formula (I-5) or (I-5-1) according to claim 6, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, wherein,
indicates a single bond or a double bond;
R1 is selected from H or D;
R2 is selected from H or D;
R3 is selected from —NRbRc, —O—C1-6 alkylene-R8, piperazinyl or morpholinyl, the said group is optionally substituted with 1 R8 group;
L is selected from a chemical bond or —C(O)—;
R4 is selected from C1-6 alkyl or C1-6 haloalkyl;
R5 is selected from H, D, F or OMe;
R6 is selected from H, D or F;
R7 is selected from H, D or F;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
R8 is optionally substituted with 1, 2 or 3 R groups, wherein the R is independently selected from H, —OH, halogen, —NO2, carbonyl, —CN, —ORa, —SRa or —NRbRc;
Ra is independently selected from H, C1-6 alkyl or C1-6 haloalkyl;
Rb and Rc are independently selected from H, —C0-6 alkylene-S(O)mR′, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 haloalkyl;
m represents 0, 1, or 2.

### Claim 9 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-6) or (I-6-1):
wherein,
indicates a single bond or a double bond;
R1 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R2 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R3 is —NRbRc, —O—C1-6 alkylene-R8 or 4- to 7-membered heterocyclyl optionally substituted by 1, 2 or 3 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R6 is selected from H, D, halogen, —S(O)mRa, —S(O)mORa or —S(O)mNRbRc;
R7 is selected from H, D, halogen, —S(O)mRa, —S(O)mORa or —S(O)mNRbRc;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
Rb and Rc are independently selected from H, —C0-6 alkylene-S(O)mR′, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 haloalkyl;
m represents 0, 1, or 2.

### Claim 10 (depends on 9)

The compound of formula (I-6) or (I-6-1) according to claim 9, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
indicates a single bond or a double bond;
R1 is selected from H, D, halogen, —CN or —ORa;
R2 is selected from H, D, halogen, —CN or —ORa;
R3 is —O—C1-6 alkylene-R8 or 5- to 6-membered heterocyclyl optionally substituted by 1 or 2 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R6 is selected from H, D or halogen;
R7 is selected from H, D or halogen;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, C1-6 alkyl or C1-6 haloalkyl.

### Claim 11 (depends on 9)

The compound of formula (I-6) or (I-6-1) according to claim 9, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
indicates a single bond or a double bond;
R1 is selected from H or D;
R2 is selected from H or D;
R3 is selected from —O—C1-6 alkylene-R8, piperazinyl or morpholinyl, the said group is optionally substituted with 1 R8 group;
L is selected from a chemical bond or —C(O)—;
R4 is selected from C1-6 alkyl or C1-6 haloalkyl;
R6 is selected from H, D or F;
R7 is selected from H, D or F;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl.

### Claim 12 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-7) or (I-7-1):
wherein,
R1 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R2 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R3 is 5- to 6-membered heterocyclyl optionally substituted with 1, 2 or 3 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, C1-6 alkyl or C1-6 haloalkyl.

### Claim 13 (depends on 12)

The compound of formula (I-7) or (I-7-1) according to claim 12, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
R1 is selected from H, D, halogen, —CN or —ORa;
R2 is selected from H, D, halogen, —CN or —ORa;
R3 is 5- to 6-membered heterocyclyl optionally substituted with 1 or 2 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R8 is independently selected from H, D, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, C1-6 alkyl or C1-6 haloalkyl.

### Claim 14 (depends on 12)

The compound of formula (I-7) or (I-7-1) according to claim 12, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
R1 is selected from H or D;
R2 is selected from H or D;
R3 is piperazinyl or morpholinyl optionally substituted with one R8 group;
L is selected from a chemical bond or —C(O)—;
R4 is selected from C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, D, C1-6 alkyl or C1-6 haloalkyl.

### Claim 15 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-8) or (I-8-1):
wherein,
R1 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R2 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R3 is 5- to 6-membered heterocyclyl optionally substituted with 1, 2 or 3 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R8 is independently selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, C1-6 alkyl or C1-6 haloalkyl.

### Claim 16 (depends on 15)

The compound of formula (I-8) or (I-8-1) according to claim 15, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
R1 is selected from H, D, halogen, —CN or —ORa;
R2 is selected from H, D, halogen, —CN or —ORa;
R3 is 5- to 6-membered heterocyclyl optionally substituted with 1 or 2 R8 groups;
L is selected from a chemical bond, —C(O)—, —C(O)NH— or —NHC(O)—;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R8 is independently selected from H, D, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, C1-6 alkyl or C1-6 haloalkyl.

### Claim 17 (depends on 15)

The compound of formula (I-8) or (I-8-1) according to claim 15, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
R1 is selected from H or D;
R2 is selected from H or D;
R3 is piperazinyl or morpholinyl optionally substituted with one R8 group;
L is selected from a chemical bond or —C(O)—;
R4 is selected from C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, D, C1-6 alkyl or C1-6 haloalkyl.

### Claim 18 (depends on 1)

The compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, which is a compound of general formula (I-9) or (I-9-1):
wherein,
indicates a single bond or a double bond;
R1 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; wherein the said C3-7 cycloalkyl or 3- to 7-membered heterocyclyl is optionally substituted by oxo or thioxo;
R2 is selected from H, D, halogen, —CN, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; wherein the said C3-7 cycloalkyl or 3- to 7-membered heterocyclyl is optionally substituted by oxo or thioxo;
R3 is selected from H, D, halogen, —CN, —NO2, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, —O—C1-6 alkylene-R8, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 11-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl, each of which is optionally substituted by 1, 2, 3, 4, or 5 R8 groups;
R4 is selected from H, D, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl;
R5 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R6 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R7 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-ORa, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; or two R8 on the same atom are taken together to form oxo or thioxo;
Ra is independently selected from H, —C0-6 alkylene-CN, —C0-6 alkylene-NO2, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl, —C0-6 alkylene-3- to 7-membered heterocyclyl, —C0-6 alkylene-C6-10 aryl or —C0-6 alkylene-5- to 10-membered heteroaryl;
Rb and Rc are independently selected from H, —C0-6 alkylene-CN, —C0-6 alkylene-NO2, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl, —C0-6 alkylene-3- to 7-membered heterocyclyl, —C0-6 alkylene-C6-10 aryl or —C0-6 alkylene-5- to 10-membered heteroaryl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl;
R″ and R′″ are independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; or, R″, R′″ and N atom are taken together to form 3- to 7-membered heterocyclyl;
m represents 0, 1, or 2.

### Claim 19 (depends on 18)

The compound of formula (I-9) or (I-9-1) according to claim 18, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
indicates a single bond or a double bond;
R1 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, C1-6 alkyl or C1-6 haloalkyl;
R2 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, C1-6 alkyl or C1-6 haloalkyl;
R3 is selected from H, D, halogen, —CN, —NO2, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 4- to 7-membered heterocyclyl, the said group is optionally substituted with 1, 2 or 3 R8 groups;
R4 is selected from H, D, C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R5 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, C1-6 alkyl or C1-6 haloalkyl;
R6 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R7 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, D, —NH2, —NHC1-6 alkyl, —N(C1-6 alkyl)2, C1-6 alkyl or C1-6 haloalkyl; or two R8 on the same atom are taken together to form oxo or thioxo;
Ra is independently selected from H, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl;
Rb and Rc are independently selected from H, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl;
R″ and R′″ are independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; or, R″, R′″ and N atom are taken together to form 3- to 7-membered heterocyclyl;
m represents 0, 1, or 2.

### Claim 20 (depends on 18)

The compound of formula (I-9) or (I-9-1) according to claim 18, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
indicates a single bond or a double bond;
R1 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R2 is selected from H, D, halogen, —CN, —ORa, C1-6 alkyl or C1-6 haloalkyl;
R3 is selected from H, D, halogen, —CN, —NO2, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C3-7 cycloalkyl or 4- to 7-membered heterocyclyl, the said group is optionally substituted with 1 or 2 R8 groups;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R5 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, C1-6 alkyl or C1-6 haloalkyl;
R6 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R7 is selected from H, D, halogen, —CN, —ORa, —SRa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C1-6 alkyl or C1-6 haloalkyl;
R8 is selected from H, D, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl;
Rb and Rc are independently selected from H, —C0-6 alkylene-OR′, —C0-6 alkylene-SR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-C(O)OR′, —C0-6 alkylene-C(O)NR″R′″, —C0-6 alkylene-S(O)mR′, —C0-6 alkylene-S(O)mOR′, —C0-6 alkylene-S(O)mNR″R′″, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl; or, Rb, Rc and N atom are taken together to form 3- to 7-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl;
R″ and R′″ are independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, 3- to 7-membered heterocyclyl, C6-10 aryl, or 5- to 10-membered heteroaryl; or, R″, R′″ and N atom are taken together to form 3- to 7-membered heterocyclyl;
m represents 0, 1, or 2.

### Claim 21 (depends on 18)

The compound of formula (I-9) or (I-9-1) according to claim 18, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate, thereof, wherein,
indicates a single bond or a double bond;
R1 is selected from H or D;
R2 is selected from H or D;
R3 is selected from H, D, —ORa, —NRbRc, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa, —S(O)mNRbRc, C4-6 cycloalkyl or 5- to 6-membered heterocyclyl, the said group is optionally substituted with 1 R8 group;
R4 is selected from C1-6 alkyl, C1-6 haloalkyl, C3-7 cycloalkyl or 3- to 7-membered heterocyclyl;
R5 is selected from H, D, halogen, —ORa, —SRa or —NRbRc;
R6 is selected from H, D, halogen, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa or —S(O)mNRbRc;
R7 is selected from H, D, halogen, —C(O)Ra, —C(O)ORa, —C(O)NRbRc, —S(O)mRa, —S(O)mORa or —S(O)mNRbRc;
R8 is selected from H, D, C1-6 alkyl or C1-6 haloalkyl;
Ra is independently selected from H, —C0-6 alkylene-OR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-S(O)mR′, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl;
Rb and Rc are independently selected from H, —C0-6 alkylene-OR′, —C0-6 alkylene-NR″R′″, —C0-6 alkylene-C(O)R′, —C0-6 alkylene-S(O)mR′, C1-6 alkyl, C1-6 haloalkyl, —C0-6 alkylene-C3-7 cycloalkyl or —C0-6 alkylene-3- to 7-membered heterocyclyl; or, Rb, Rc and N atom are taken together to form 5- to 6-membered heterocyclyl;
R′ is independently selected from H, C1-6 alkyl or C1-6 haloalkyl;
R″ and R′″ are independently selected from H, C1-6 alkyl or C1-6 haloalkyl; or, R″, R′″ and N atom are taken together to form 5- to 6-membered heterocyclyl;
m represents 0, 1, or 2.

### Claim 22

A compound, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, wherein the said compound is selected from the group consisting of:

### Claim 23 (depends on 1)

A pharmaceutical composition, comprising a compound according to claim 1, or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, and a racemate thereof, and pharmaceutically acceptable excipient(s).