# US 10,501,443 B2 · Pyridone compound as c-met inhibitor

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- Number: US 10,501,443 B2
- Document ID: US10501443B2
- Status: Granted
- Kind: B2
- Application number: 16/343,387
- Filed: 2017-10-27
- Published: 2019-08-15
- Granted: 2019-12-10
- Earliest claimed: 2016-10-27
- Assignees: Fujian Cosunter Pharmaceutical Co., Ltd.
- Applicants: Fujian Cosunter Pharmaceutical Co., Ltd.
- Inventors: Xiongbin Xu; Gang Li; Charles Z. Ding; Lihong Hu; Guoping Hu; Jian Li; Shuhui Chen; Zhigang Chi; Kun Wang
- Web page: https://patentgrep.com/patent/US10501443B2

## CPC

- C07D 401/14: containing three or more hetero rings
- A61K 31/435: having six-membered rings with one nitrogen as the only ring hetero atom
- A61K 31/4412: having oxo groups directly attached to the heterocyclic ring
- A61K 31/444: containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61P 35/00: Antineoplastic agents
- C07D 213/00: Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D 401/00: Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D 403/14: containing three or more hetero rings
- C07D 413/14: containing three or more hetero rings
- C07D 417/14: containing three or more hetero rings
- 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

Disclosed in the present invention is a type of pyridone compounds as c-met inhibitors, and specifically disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof.

## Claims

### Claim 1

A compound represented by formula (I) or a pharmaceutically acceptable salt,
R1 is selected from H or F;
R2 is selected from H or CH3;
while R2 is not H, the configuration of the carbon atom bonded to R2 is R or S;
A is selected from the group consisting of phenyl, pyridyl, pyrazolyl, isoxazolyl, isothiazolyl and thiazolyl, each of which is optionally substituted by 1, 2 or 3 R3;
R3 is selected from CN, halogen, C(═O)NH2, or is selected from the group consisting of C1-6 alkyl, C1-6 heteroalkyl, and C3-6 cycloalkyl, each of which is optionally substituted by 1, 2 or 3 R0;
R0 is selected from F, Cl, Br, I, OH, CN, NH2, C(═O)NH2, or is selected from the group consisting of C1-3 alkyl and C1-3 heteroalkyl, each of which is optionally substituted by 1, 2 or 3 R′;
R′ is selected from F, Cl, Br, I, CN, OH, NH2, CH3, CH3CH2, CF3, CHF2 or CH2F;
the “hetero” in the C1-3 heteroalkyl or C1-6 heteroalkyl is selected from the group consisting of —O—, —C(═O)NR′—, —C(═O)NH—, —NR′—, and —NH—;
in any of the above cases, the number of the heteroatom or the heteroatomic group is independently selected from 1, 2 or 3.

### Claim 2 (depends on 1)

The compound or the pharmaceutically acceptable salt as defined in claim 1, wherein, R0 is selected from F, Cl, Br, I, OH, CN, NH2, C(═O)NH2, CH3, CH3CH2, CF3, CHF2, CH2F, NH2CH2, (NH2)2CH, CH3O, CH3CH2O, CH3OCH2, CH3NH or (CH3)2N.

### Claim 3 (depends on 1)

The compound or the pharmaceutically acceptable salt as defined in claim 1, wherein, R1 is H.

### Claim 4 (depends on 1)

The compound or the pharmaceutically acceptable salt as defined in claim 1, wherein, R1 is F.

### Claim 5 (depends on 1)

The compound or the pharmaceutically acceptable salt as defined in claim 1, wherein, R2 is H.

### Claim 6 (depends on 1)

The compound or the pharmaceutically acceptable salt as defined in claim 1, wherein, R2 is CH3.

### Claim 7 (depends on 6)

The compound or the pharmaceutically acceptable salt as defined in claim 6, wherein, the configuration of the carbon atom bonded to R2 is R.

### Claim 8 (depends on 6)

The compound or the pharmaceutically acceptable salt as defined in claim 6, wherein, the configuration of the carbon atom bonded to R2 is S.

### Claim 9 (depends on 1)

The compound or the pharmaceutically acceptable salt as defined in claim 1, wherein, R3 is selected from CN, halogen, C(═O)NH2, or is selected from the group consisting of C1-3 alkyl and C1-3 heteroalkyl, each of which is optionally substituted by 1, 2 or 3 R0.

### Claim 10 (depends on 9)

The compound or the pharmaceutically acceptable salt as defined in claim 9, wherein, R3 is selected from CN, F, Cl, Br, CH3, CH3CH2, CF3, CHF2, CH2F, CH3O or C(═O)NH2.

### Claim 11 (depends on 1)

The compound or the pharmaceutically acceptable salt as defined in claim 1, wherein, A is selected from the group consisting of
each of which is optionally substituted by 1, 2 or 3 R3.

### Claim 12 (depends on 11)

The compound or the pharmaceutically acceptable salt as defined in claim 11, wherein, A is selected from the group consisting of

### Claim 13 (depends on 12)

The compound or the pharmaceutically acceptable salt as defined in claim 12, wherein, A is selected from the group consisting of

### Claim 14 (depends on 10)

The compound or the pharmaceutically acceptable salt as defined in claim 10, wherein, A is selected from the group consisting of

### Claim 15 (depends on 1)

The compound as defined in claim 1 is selected from the group consisting of

### Claim 16 (depends on 1)

A pharmaceutical composition comprising a therapeutically effective amount of the compound or the pharmaceutically acceptable salt thereof as defined in claim 1, as well as a pharmaceutically acceptable carrier.

### Claim 17 (depends on 16)

A method for treating tumor, comprising administering to a subject in need thereof the pharmaceutical composition as defined in claim 16, wherein the tumor is selected from liver cancer, non-small cell lung cancer, or gastric cancer.