Combinations comprising maba compounds and corticosteroids

Patent metadata

Field	Value
Publication number	US-2016015704-A1
Application number	US-201414770200-A
Country	US
Kind code	A1
Filing date	Feb 27, 2014
Priority date	Feb 27, 2013
Publication date	Jan 21, 2016
Grant date	—

Abstract

A combination which comprises (a) corticosteroid and (b) a dual muscarinic antagonist-β2 adrenergic agonist compound, or any pharmaceutically acceptable salt or solvate thereof.

First claim

1 . A combination comprising:
(a) a corticosteroid and (b) a dual muscarinic antagonist-β2 adrenergic agonist compound, wherein the dual muscarinic antagonist-β2 adrenergic agonist compound is trans-4-[{2-[({[2-chloro-4-({[(2R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}methyl)-5-methoxyphenyl]amino}carbonyl)oxy]ethyl}-(methyl)amino]cyclohexyl hydroxy(di-2-thienyl)acetate, or a pharmaceutically acceptable salt or solvate thereof.

2 . The combination according to claim 1 , wherein the dual muscarinic antagonist-β2 adrenergic agonist compound is trans-4-[{2-[({[2-chloro-4-({[(2R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}methyl)-5-methoxyphenyl]amino}carbonyl)oxy]ethyl}-(methyl)amino]cyclohexyl hydroxy(di-2-thienyl)acetate, disaccharinate.

3 . The combination according to claim 1 , wherein the dual muscarinic antagonist-β2 adrenergic agonist compound is L-tartrate salt of trans-4-[{2-[({[2-chloro-4-({[(2R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}methyl)-5-methoxyphenyl]amino}carbonyl)oxy]ethyl}-(methyl)amino]cyclohexyl hydroxy(di-2-thienyl)acetate.

4 . The combination according to claim 1 , wherein the corticosteroid is chosen from budesonide, beclomethasone dipropionate, triamcinolone, mometasone furoate, ciclesonide, fluticasone propionate, or fluticasone furoate.

5 . The combination according to claim 4 , wherein the corticosteroid is chosen from budesonide, mometasone furoate, fluticasone propionate, or fluticasone furoate.

6 . The combination according to claim 5 , wherein the corticosteroid is budesonide.

7 . The combination according to claim 5 , wherein the corticosteroid is mometasone furoate.

8 . The combination according to claim 5 , wherein the corticosteroid is fluticasone propionate.

9 . The combination according to claim 5 , wherein the corticosteroid is fluticasone furoate.

10 . The combination according to claim 1 , wherein the active ingredients (a) the corticosteroid and (b) the dual muscarinic antagonist-β2 adrenergic agonist compound form part of a single pharmaceutical composition.

11 . The combination according to claim 1 , further comprising at least one compound (c) chosen from: (i) PDE IV inhibitors, (ii) leukotriene D4 antagonists, (iii) inhibitors of egfr-kinase, (iv) p38 kinase inhibitors, (v) JAK inhibitors, or (vi) NK1 receptor agonists.

12 . A method of treating a respiratory disease susceptible to amelioration by both β2 adrenergic receptor agonist and muscarinic receptor antagonist activities comprising administering to a patient in need thereof a pharmaceutically effective amount of (a) the corticosteroid and (b) the dual muscarinic antagonist-β2 adrenergic agonist compound according to claim 1 .

13 . The method according to claim 12 , wherein the respiratory disease is asthma or chronic obstructive pulmonary disease.

14 . A product comprising (a) the corticosteroid and (b) the dual muscarinic antagonist-β2 adrenergic agonist compound according to claim 1 , as a combined preparation for simultaneous, concurrent, separate or sequential administration.

15 . The product according to claim 14 , further comprising at least one compound (c) chosen from: (i) PDE IV inhibitors, (ii) leukotriene D4 antagonists, (iii) inhibitors of egfr-kinase, (iv) p38 kinase inhibitors, (v) JAK inhibitors, or (vi) NK1 receptor agonists.

16 . A kit of parts comprising (a) the corticosteroid and (b) the dual muscarinic antagonist-β2 adrenergic agonist compound according to claim 1 , together with instructions for simultaneous, concurrent, separate or sequential administration of (a) the corticosteroid in combination with (b) the dual muscarinic antagonist-β2 adrenergic agonist compound.

17 . The kit according to claim 16 , further comprising at least one compound (c) chosen from: (i) PDE IV inhibitors, (ii) leukotriene D4 antagonists, (iii) inhibitors of egfr-kinase, (iv) p38 kinase inhibitors, (v) JAK inhibitors, or (vi) NK1 receptor agonists.

18 . A package comprising (a) the corticosteroid and (b) the dual muscarinic antagonist-β2 adrenergic agonist compound according to claim 1 , for the simultaneous, concurrent, separate or sequential administration.

19 . The package according to claim 18 , further comprising at least one compound (c) chosen from: (i) PDE IV inhibitors, (ii) leukotriene D4 antagonists, (iii) inhibitors of egfr-kinase, (iv) p38 kinase inhibitors, (v) JAK inhibitors, or (vi) NK1 receptor agonists.

20 . (canceled)

21 . (canceled)

22 . The dual muscarinic antagonist-β2 adrenergic agonist compound according to claim 1 , for simultaneous, concurrent, separate, or sequential use in combination with budesonide, beclomethasone dipropionate, triamcinolone, mometasone furoate, ciclesonide fluticasone propionate, or fluticasone furoate.

23 . The corticosteroid according to claim 1 , for simultaneous, concurrent, separate, or sequential use in combination with trans-4-[{2-[({[2-chloro-4-({[(2R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino}methyl)-5-methoxyphenyl]amino}carbonyl)oxy]ethyl}-(methyl)amino]cyclohexyl hydroxy(di-2-thienyl)acetate, or a pharmaceutically acceptable salt or solvate thereof.

24 . (canceled)

25 . The combination according to claim 2 , wherein the corticosteroid is chosen from budesonide, beclomethasone dipropionate, triamcinolone, mometasone furoate, ciclesonide, fluticasone propionate, or fluticasone furoate.

26 . The combination according to claim 3 , wherein the corticosteroid is chosen from budesonide, beclomethasone dipropionate, triamcinolone, mometasone furoate, ciclesonide, fluticasone propionate, or fluticasone furoate.

27 . The method according to claim 12 , wherein the pharmaceutically effective amount of (a) the corticosteroid and (b) the dual muscarinic antagonist-β2 adrenergic agonist compound are administered simultaneously, concurrently, separately, or sequentially.

Assignees

• Almirall Sa

Inventors

• Aparici Virgili Monica
• Calbet Murtro Marta
• Miralpeix Guell Montserrat
• Gavalda Monedero Amadeu
• Puig Duran Carlos

Classifications

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• A61P11/06

  Antiasthmatics · CPC title

• A61K9/008

  comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI] · CPC title

• A61K31/4709 Primary

  Non-condensed quinolines and containing further heterocyclic rings · CPC title

• C07D409/14

  containing three or more hetero rings · CPC title