IP Library › Granted Patent US 10,045,980
Granted Patent B2
US 10,045,980 · App. 15/457,810 · Granted Aug 14, 2018

Inhibitor of p38 map kinase

Inventors: Alistair Ian Longshaw (Nottingham, GB); Euan Alexander Fraser Fordyce (Nottingham, GB); Stuart Thomas Onions (Nottingham, GB); John King-Underwood (Pendock, GB); Jennifer Venable (Solana Beach, CA)
Assignee: Respivert Ltd
A61K31/497A61K9/0075A61K47/26
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Quick Facts
Patent No.
US 10,045,980
App. No.
15/457,810
Granted
Aug 14, 2018
Kind
B2
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.

Claims (15)

1. A dry powder pharmaceutical formulation for inhalation comprising: 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

optionally, 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.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2018
From: LONGSHAW, ALISTAIR IAN; FORDYCE, EUAN ALEXANDER FRASER; ONIONS, STUART THOMAS; KING-UNDERWOOD, JOHN; VENABLE, JENNIFER
To: RESPIVERT LTD.; TOPIVERT PHARMA LTD.
Reel/Frame 045365/0774 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2017
From: TOPIVERT PHARMA LIMITED
To: RESPIVERT LIMITED
Reel/Frame 042083/0755 →
Continuity (5)
Continuation 15253141 · Aug 31, 2016
Continuation 14622368 · Feb 13, 2015
Provisional Application 61940282 · Feb 14, 2014
Provisional Application 61941064 · Feb 18, 2014
Related Publication 20170182039A1 · Jun 29, 2017