# US 11,306,095 B2 · Use of pteridinone derivative serving as EGFR inhibitor

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- Number: US 11,306,095 B2
- Document ID: US11306095B2
- Status: Granted
- Kind: B2
- Application number: 15/577,518
- Filed: 2016-05-30
- Published: 2018-05-31
- Granted: 2022-04-19
- Earliest claimed: 2015-05-29
- Assignees: East China University of Science and Technology
- Applicants: East China University of Science and Technology
- Inventors: Honglin Li; Yufang Xu; Zhenjiang Zhao; Wei Zhou; Yuqiong Xu; Deheng Sun; Xia Wang; Zhuo Chen
- Web page: https://patentgrep.com/patent/US11306095B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- C07D 475/00: Heterocyclic compounds containing pteridine ring systems
- 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 invention relates to a pteridinone derivative serving as an EGFR inhibitor and use thereof. Specifically, the present invention relates to a compound represented by the following formula I, pharmaceutical composition comprising the compound of the following formula I, and use of the compound in preparation of drugs for treating EGFR-mediated diseases or inhibiting EGFR.

## Claims

### Claim 1

A compound of formula I or a pharmaceutical acceptable salt thereof:
wherein,
R1 is independently selected from the group consisting of substituted or unsubstituted phenyl, and optionally substituted C3-C8 cycloalkyl;
A is a divalent radical -A′-;
A′ is a benzene ring, or a five- or six-membered nitrogen-containing heterocycle;
R2 is independently selected from the group consisting of C2-C4 alkenyl substituted acylamino and substituted or unsubstituted C2-C4 alkenyl substituted acyl;
m is 0;
R7 is independently selected from the group consisting of:
and
R3, R4, R5 and R6 are independently selected from the group consisting of H, substituted or unsubstituted C1-C6 alkoxy, and substituted or unsubstituted C1-C6 alkyl;
provided that when R1 is H and m is 0, R3, R4, R5 and R6 are not each H; and
when R1 is H, m is 0, A′ is a benzene ring and R7 is
if one of R3 and R6 is a methoxy, the other is not H.

### Claim 2

A compound or a pharmaceutical acceptable salt thereof selected from the group consisting of:

### Claim 3 (depends on 1)

The compound of claim 1, wherein
R1 is substituted or unsubstituted phenyl;
R2 is independently C2-C4 alkenyl substituted acylamino, or C2-C4 alkenyl substituted acyl;
R7 is:
and
R3, R4, R5 and R6 are independently selected from the group consisting of H, substituted or unsubstituted C1-C3 alkoxy, and substituted or unsubstituted C1-C3 alkyl.

### Claim 4

A compound or a pharmaceutical acceptable salt thereof selected from the group consisting of:

### Claim 5 (depends on 1)

The compound of claim 1, wherein R3, R4, R5 and R6 are independently selected from the group consisting of substituted or unsubstituted C1-C3 alkoxy and substituted or unsubstituted C1-C3 alkyl.

### Claim 6 (depends on 1)

The compound of claim 1, wherein the substituted phenyl is halogen or C1-4 alkoxy substituted phenyl.

### Claim 7 (depends on 2)

A pharmaceutical composition, comprising the compound or a pharmaceutical acceptable salt thereof of claim 2 and a pharmaceutically acceptable carrier or excipient.

### Claim 8 (depends on 2)

A method for inhibiting EGFR comprising administering to a patient in need thereof an effective amount of the compound of claim 2.

### Claim 9 (depends on 2)

A method for treating EGFR-mediated diseases comprising administering to a patient in need thereof an effective amount of the compound of claim 2.

### Claim 10 (depends on 9)

The method of claim 9, wherein the EGFR-mediated disease is cancer.

### Claim 11 (depends on 10)

The method of claim 10, wherein the cancer is selected from the group consisting of non-small cell lung cancer, small cell lung cancer, lung adenocarcinoma, lung squamous cell carcinoma, breast cancer, prostate cancer, glioblastoma, ovarian cancer, squamous cell carcinoma of head and neck, cervical cancer, esophageal cancer, liver cancer, kidney cancer, pancreas cancer, colon cancer, skin cancer, leukemia, lymphoma, stomach cancer, multiple myeloma, and solid tumors.