# US 8,772,315 B2 · Pharmaceutical composition for treating overactive bladder

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- Number: US 8,772,315 B2
- Document ID: US8772315B2
- Status: Granted
- Kind: B2
- Application number: 13/748,956
- Filed: 2013-01-24
- Published: 2013-06-13
- Granted: 2014-07-08
- Earliest claimed: 2007-11-02
- Assignees: Astellas Pharma Inc.
- Applicants: Astellas Pharma Inc.
- Inventors: Masanori Suzuki; Masashi Ukai; Akiyoshi Ohtake
- Web page: https://patentgrep.com/patent/US8772315B2

## CPC

- A61K 31/4725: containing further heterocyclic rings
- A61K 31/426: 1,3-Thiazoles
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/10: of the bladder
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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

A pharmaceutical composition comprising (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof and (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof, as active ingredients, in particular for improving various symptoms accompanying overactive bladder, such as urinary urgency, pollakiuria and/or urinary incontinence.

## Claims

### Claim 1

A pharmaceutical composition, comprising: (i) (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof present from 25 to 50 mg in terms of (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide and (ii) (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof present at 5 mg in terms of (3R)-quinuclidin-3-yl (1S)-I-phenyl-I,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof is (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide.

### Claim 3 (depends on 2)

The pharmaceutical composition of claim 2, wherein the (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof is (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1, wherein the (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof is (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate.

### Claim 5

A method for treating urinary urgency, pollakiuria and/or urinary incontinence accompanying overactive bladder, comprising administering effective amounts of (i) (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or a pharmaceutically acceptable salt thereof at a dosage of 25 to 50 mg in terms of (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide, and (ii) (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a pharmaceutically acceptable salt thereof at a dosage of 5 mg in terms of (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate.

### Claim 6 (depends on 5)

The method claim 5, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or pharmaceutically acceptable salt thereof, and said (3R)-quinuclidin-3-yl (1S)-1-phenyl-I,2,3,4-tetrahydroisoquinoline-2-carboxylate or pharmaceutically acceptable salt thereof are both administered orally.

### Claim 7 (depends on 5)

The method for treating of claim 5, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or pharmaceutically acceptable salt thereof and said (3R)-quinuclidin-3-yl (1S)-I-phenyl-I,2,3,4-tetrahydroisoquinoline-2-carboxylate or pharmaceutically acceptable salt thereof are administered simultaneously.

### Claim 8 (depends on 7)

The method of claim 7, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or pharmaceutically acceptable salt thereof, and said (3R)-quinuclidin-3-yl (1S)-I-phenyl-I,2,3,4-tetrahydroisoquinoline-2-carboxylate or pharmaceutically acceptable salt thereof are both administered orally.

### Claim 9 (depends on 5)

The method of claim 5, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or pharmaceutically acceptable salt thereof and said (3R)-quinuclidin-3-yl (1S)-I-phenyl-I,2,3,4-tetrahydroisoquinoline-2-carboxylate or pharmaceutically acceptable salt thereof are administered at a time interval.

### Claim 10 (depends on 9)

The method of claim 9, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or pharmaceutically acceptable salt thereof, and said (3R)-quinuclidin-3-yl (1S)-I-phenyl-I,2,3,4-tetrahydroisoquinoline-2-carboxylate or pharmaceutically acceptable salt thereof are both administered orally.

### Claim 11 (depends on 5)

The method of claim 5, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide or pharmaceutically acceptable salt thereof is (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide, and said (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or pharmaceutically acceptable salt thereof is (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate.

### Claim 12 (depends on 11)

The method of claim 11, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide, and said (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate are both administered orally.

### Claim 13 (depends on 11)

The method of claim 11, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide and said (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate are administered simultaneously.

### Claim 14 (depends on 13)

The method of claim 13, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide, and said (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate are both administered orally.

### Claim 15 (depends on 11)

The method of claim 11, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide and said (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate are administered at a time interval.

### Claim 16 (depends on 15)

The method of claim 15, wherein said (R)-2-(2-aminothiazol-4-yl)-4′-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl}acetanilide, and said (3R)-quinuclidin-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate succinate are both administered orally.