# US 9,040,548 B2 · Quinazoline derivatives as VEGF inhibitors

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- Number: US 9,040,548 B2
- Document ID: US9040548B2
- Status: Granted
- Kind: B2
- Application number: 14/146,954
- Filed: 2014-01-03
- Published: 2014-05-01
- Granted: 2015-05-26
- Earliest claimed: 2006-12-21
- Assignees: AstraZeneca AB
- Applicants: AstraZeneca AB
- Inventors: Andrew Peter Thomas; Elaine Sophie Elizabeth Stokes; Laurent Francois Andre Hennequin
- Web page: https://patentgrep.com/patent/US9040548B2

## CPC

- C07D 401/12: linked by a chain containing hetero atoms as chain links
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/14: Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/06: Antipsoriatics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3, wherein R3 is piperidinyl-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3, wherein R3 is as defined herein; 3) C2-5alkynylR3, wherein R3 is as defined herein; and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

## Claims

### Claim 1

A method of treating breast cancer in a warm-blooded animal in need of such treatment which comprises administering to the animal an effective amount of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The method as claimed in claim 1, wherein the warm-blooded animal is a human.

### Claim 3

A method of treating lung cancer in a warm-blooded animal in need of such treatment which comprises administering to the animal an effective amount of 1 to 50 mg/kg of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline or a pharmaceutically acceptable salt thereof.

### Claim 4 (depends on 3)

The method as claimed in claim 3, wherein the warm-blooded animal is a human.

### Claim 5

A method of treating prostate cancer in a warm-blooded animal in need of such treatment which comprises administering to the animal an effective amount of 1 to 50 mg/kg of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline or a pharmaceutically acceptable salt thereof.

### Claim 6 (depends on 5)

The method as claimed in claim 5, wherein the warm-blooded animal is a human.