# US 9,040,559 B2 · BETA2-adrenoceptor agonists

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- Number: US 9,040,559 B2
- Document ID: US9040559B2
- Status: Granted
- Kind: B2
- Application number: 14/450,692
- Filed: 2014-08-04
- Published: 2014-11-20
- Granted: 2015-05-26
- Earliest claimed: 1999-04-06
- Assignees: Novartis AG
- Applicants: Novartis AG
- Inventors: Bernard Cuenoud; Ian Bruce; Robin Alec Fairhurst; David Beattie
- Web page: https://patentgrep.com/patent/US9040559B2

## CPC

- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/06: Antiabortive agents; Labour repressants
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 215/80: containing at least two amino groups bound to the carbon skeleton
- C07C 233/43: having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
- C07C 311/08: having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
- C07D 215/227: only one oxygen atom which is attached in position 2
- C07D 215/26: Alcohols; Ethers thereof
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07C 2602/08: the other ring being five-membered, e.g. indane
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.

## Claims

### Claim 1

A capsule that contains a pharmaceutical composition comprising:
(A) (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one or a salt or solvate thereof;
(B) an anticholinergic or antimuscarinic agent; and
(C) a pharmaceutically acceptable carrier.

### Claim 2 (depends on 1)

A capsule according to claim 1, in which (A), (B) and (C) contained therein are in inhalable form.

### Claim 3 (depends on 2)

A capsule according to claim 2, in which the pharmaceutical composition contained therein is a dry powder formulation.

### Claim 4 (depends on 3)

A capsule according to claim 3 that contains a daily dose of (A) and a daily dose of (B).

### Claim 5 (depends on 4)

A capsule according to claim 4, in which the daily dose of (A) is from 1 μg to 5000 μg.

### Claim 6 (depends on 1)

A capsule according to claim 1, in which (A) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one maleate.

### Claim 7 (depends on 5)

A capsule according to claim 5, in which (A) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one maleate.

### Claim 8 (depends on 1)

A capsule according to claim 1, in which (B) is selected from the group consisting of ipratropium bromide, oxitropium bromide and tiotropium bromide.

### Claim 9 (depends on 8)

A capsule according to claim 8, in which (B) is tiotropium bromide.

### Claim 10 (depends on 4)

A capsule according to claim 4, in which (B) is selected from the group consisting of ipratropium bromide, oxitropium bromide and tiotropium bromide.

### Claim 11 (depends on 10)

A capsule according to claim 10, in which (B) is tiotropium bromide.

### Claim 12 (depends on 1)

A capsule according to claim 1, in which (A) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one maleate and (B) is selected from the group consisting of ipratropium bromide, oxitropium bromide and tiotropium bromide.

### Claim 13 (depends on 1)

A capsule according to claim 1, in which (A) is (R)-5-[2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one maleate and (B) is tiotropium bromide.