INHIBITOR OF p38 MAP KINASE

Patent metadata

Field	Value
Publication number	US-2019092752-A1
Application number	US-201816032858-A
Country	US
Kind code	A1
Filing date	Jul 11, 2018
Priority date	Feb 14, 2014
Publication date	Mar 28, 2019
Grant date	—

Abstract

A dry powder pharmaceutical formulation for inhalation including a compound of formula (I):

that is 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(4-((2-((6-ethylpyrazin-2-yl)amino)pyridin-4-yl)methoxy)naphthalen-1-yl)urea or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof; and lactose as a topically acceptable diluent. An inhaler device containing the dry powder pharmaceutical formulation is also described.

First claim

1 . A dry powder pharmaceutical formulation for inhalation consisting of particles, wherein the particles comprise a compound of formula (I)

that is 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(4-((2-((6-ethylpyrazin-2-yl)amino)pyridin-4-yl)methoxy)naphthalen-1-yl)urea or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof; and
lactose as a topically acceptable diluent.

2 . The dry powder pharmaceutical formulation according to claim 1 , wherein the compound of formula (I) has a mass median diameter (MMAD) of 1-10 μm.

3 . The dry powder pharmaceutical formulation according to claim 1 , wherein the compound of formula (I) is micronized.

4 . The dry powder pharmaceutical formulation according to claim 1 , wherein the formulation comprises magnesium stearate.

5 . The dry powder pharmaceutical formulation according to claim 1 , wherein the compound of formula (I) in the form of its maleate salt.

6 . The dry powder pharmaceutical formulation according to claim 2 , wherein the compound of formula (I) is in the form of its maleate salt.

7 . The dry powder pharmaceutical formulation according to claim 3 , wherein the compound of formula (I) is in the form of its maleate salt.

8 . The dry powder pharmaceutical formulation according to claim 4 , wherein the compound of formula (I) is in the form of its maleate salt.

9 . The dry powder pharmaceutical formulation according to claim 1 , wherein the compound of formula (I) is in the form of its free base.

10 . The dry powder pharmaceutical formulation according to claim 5 , wherein the compound of formula (I) is in the form of its Form 2 crystalline polymorph.

11 . The dry powder pharmaceutical formulation according to claim 6 , wherein the compound of formula (I) is in the form of its Form 2 crystalline polymorph.

12 . The dry powder pharmaceutical formulation according to claim 7 , wherein the compound of formula (I) is in the form of its Form 2 crystalline polymorph.

13 . The dry powder pharmaceutical formulation according to claim 8 , wherein the compound of formula (I) is in the form of its Form 2 crystalline polymorph.

14 . A dry powder inhaler device comprising a dry powder pharmaceutical formulation consisting of particles, wherein the particles comprise a compound of formula (I)

that is 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(4-((2-((6-ethylpyrazin-2-yl)amino)pyridin-4-yl)methoxy)naphthalen-1-yl)urea or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof; and
lactose as a topically acceptable diluent.

15 . The dry powder inhaler device according to claim 14 , wherein the compound of formula (I) has a mass median diameter (MMAD) of 1-10 μm.

16 . The dry powder inhaler device according to claim 14 , wherein the compound of formula (I) is micronized.

17 . The dry powder inhaler device according to claim 14 , wherein the compound of formula (I) is in the form of its maleate salt.

18 . The dry powder inhaler device according to claim 17 , wherein the compound of formula (I) is in the form of its Form 2 crystalline polymorph.

19 . The dry powder inhaler device according to claim 14 , wherein the compound of formula (I) is in the form of its free base.

20 . The dry powder inhaler device according to claim 14 which is a multidose device.

Assignees

• Respivert Ltd

Inventors

• Longshaw Alistair Ian
• Fordyce Euan Alexander Fraser
• Onions Stuart Thomas
• King-Underwood John
• Venable Jennifer

Classifications

• A61P27/12

  for cataracts · CPC title

• C07D403/14

  containing three or more hetero rings · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61K31/498

  Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine · CPC title