IP Library Granted Patent US 9,717,732
Granted Patent B2
US 9,717,732 · App. 14/771,097 · Granted Aug 1, 2017

Drug combination

Inventors: Michael J. A. Walker (Vancouver, CA); Mario Cazzola (Naples, IT); Luigino Calzetta (Rome, IT)
Assignee: VERONA PHARMA PLC
A61K31/519A61K9/008A61K9/0075A61K9/0078A61K9/0095A61K9/4858A61K31/137A61K31/167A61K31/40A61K31/44A61K31/46A61K45/06A61M15/009A61M2202/064
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Quick Facts
Patent No.
US 9,717,732
App. No.
14/771,097
Granted
Aug 1, 2017
Kind
B2
Abstract

The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a β 2 -adrenergic receptor agonist.

Claims (16)

1. A nebulizer inhaler, a dry powder inhaler or a metered dose inhaler comprising:

a composition comprising (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a β 2 -adrenergic receptor agonist;

and one or more pharmaceutically acceptable carriers, diluents, or excipients.

2. A nebulizer inhaler, a dry powder inhaler or a metered dose inhaler according to claim 1 , in which the PDE3/PDE4 inhibitor (a) is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one.

3. A nebulizer inhaler, a dry powder inhaler or a metered dose inhaler according to claim 1 , in which the β 2 -adrenergic receptor agonist (b) is salbutamol, bitolterol, fenoterol, formoterol, indacaterol, isoetharine, levalbuterol, metaproterenol, pirbuterol, salmefamol, salmeterol or terbutaline.

4. A nebulizer inhaler, a dry powder inhaler or a metered dose inhaler according to claim 1 , in which β 2 -adrenergic receptor agonist (b) is salbutamol, salmeterol, formoterol, or pirbuterol.

5. A nebulizer inhaler, a dry powder inhaler or a metered dose inhaler according to claim 1 , wherein the composition is a fixed combination.

6. A method of treating a disease or condition, in a subject in need thereof, which method comprises administering to said subject

(a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof, and

(b) a β 2 -adrenergic receptor agonist,

wherein the disease or condition is selected from the group consisting of asthma, allergic asthma, hay fever, allergic rhinitis, bronchitis, emphysema, bronchiectasis, chronic obstructive pulmonary disease (COPD), adult respiratory distress syndrome (ARDS), steroid resistant asthma, severe asthma and paediatric asthma.

7. A method according to claim 6 , which method comprises administering to said subject a therapeutically effective, non-toxic amount of a composition comprising (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a β 2 -adrenergic receptor agonist.

8. A method according to claim 6 , wherein the disease or condition is asthma or chronic obstructive pulmonary disease (COPD).

9. A method according claim 6 , wherein said subject is a human.

10. A method of treating a disease or condition in a subject in need thereof, which method comprises administering to said subject (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof simultaneously, separately or sequentially in combination with (b) a β 2 -adrenergic receptor agonist, wherein the disease or condition is selected from the group consisting of asthma, allergic asthma, hay fever, allergic rhinitis, bronchitis, emphysema, bronchiectasis, chronic obstructive pulmonary disease (COPD), adult respiratory distress syndrome (ARDS), steroid resistant asthma, severe asthma and paediatric asthma.

11. A method of treating a disease or condition in a subject in need thereof, which method comprises administering to said subject (b) a β 2 -adrenergic receptor agonist simultaneously, separately or sequentially in combination with (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof, wherein the disease or condition is selected from the group consisting of asthma, allergic asthma, hay fever, allergic rhinitis, bronchitis, emphysema, bronchiectasis, chronic obstructive pulmonary disease (COPD), adult respiratory distress syndrome (ARDS), steroid resistant asthma, severe asthma and paediatric asthma.

Assignments (7)
RELEASE OF SECURITY INTEREST Recorded Oct 7, 2025
From: OAKTREE FUND ADMINISTRATION, LLC
To: VERONA PHARMA PLC
Reel/Frame 072495/0271 →
RELEASE OF SECURITY INTEREST IN PATENTS AT R/F 067387/0799 Recorded Mar 25, 2025
From: OAKTREE FUND ADMINISTRATION, LLC, AS AGENT
To: VERONA PHARMA PLC
Reel/Frame 070618/0561 →
SECURITY INTEREST Recorded May 13, 2024
From: VERONA PHARMA PLC
To: OAKTREE FUND ADMINISTRATION, LLC
Reel/Frame 067387/0708 →
SECURITY INTEREST Recorded May 13, 2024
From: VERONA PHARMA PLC
To: OAKTREE FUND ADMINISTRATION, LLC
Reel/Frame 067387/0799 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2016
From: CAZZOLA, MARIO
To: VERONA PHARMA PLC
Reel/Frame 037688/0030 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2016
From: CALZETTA, LUIGINO
To: VERONA PHARMA PLC
Reel/Frame 037688/0051 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2016
From: WALKER, MICHAEL J.A.
To: VERONA PHARMA PLC
Reel/Frame 037687/0990 →
Continuity (2)
Provisional Application 61799177 · Mar 15, 2013
Related Publication 20160008363A1 · Jan 14, 2016