IP Library › Granted Patent US 8,927,563
Granted Patent B2
US 8,927,563 · App. 14/242,531 · Granted Jan 6, 2015

Kinase inhibitor

Inventor: Matthew Colin Thor Fyfe (London, GB)
Assignees: Respivert Limited; Topivert Pharma Limited
A61K31/5377C07D239/47C07D211/86A61K31/44A61K31/506C07D405/12C07D405/14A61K31/444A61K31/4427A61K31/505A61K31/541A61K31/551A61K31/553C07C311/08C07D403/12C07D213/74C07D401/12C07D413/12
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Quick Facts
Patent No.
US 8,927,563
App. No.
14/242,531
Granted
Jan 6, 2015
Kind
B2
Abstract

There is provided a compound of formula I, which compound has antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases, e.g., Src and Lck) and has use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Claims (27)

1. A compound of formula I,

or a pharmaceutically acceptable salt thereof.

2. A compound according to claim 1 that is:

3-((4-((4-(3-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)phenyl)ureido)naphthalen-1-yl)oxy)pyrimidin-2-yl)amino)-5-ethynyl-N-(2-(2-(2-methoxyethoxy)ethoxy)ethyl)-benzamide.

3. A pharmaceutical formulation comprising a compound as defined in claim 1 , or pharmaceutically acceptable salt thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.

4. A combination product comprising

(A) a compound as defined in claim 1 , or pharmaceutically acceptable salt thereof, and

(B) another therapeutic agent,

wherein each of components (A) and (B) is formulated in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier.

5. A process for the preparation of a compound of formula I which process comprises:

(a) reaction of a compound of formula II,

with a compound of formula III,

wherein one of Z 1 and Z 2 is a structural fragment of formula IV

and the other of Z 1 and Z 2 is a structural fragment of formula V

(b) reaction of a compound of formula Ha,

wherein Z 1 is as defined above, with a suitable azide-forming agent,

which reaction is followed, without isolation, by thermal rearrangement of the intermediate acyl azide (of formula Z 1 —C(O)—N 3 ) to provide, in situ, a compound of formula II, which compound is then reacted with a compound of formula III as defined above;

(c) reaction of a compound of formula IIb,

wherein LG 1 represents a leaving group and Z 1 is as defined above, with a compound of formula III, as defined above;

(d) reaction of a compound of formula VI,

wherein LG 2 represents a leaving group, with a compound of formula VII,

 or

(e) reaction of a compound of formula VIIa,

wherein R 4′ represents H or a C 1-3 alkyl group, with a compound of formula VIIb, H 2 N—[CH 2 CH 2 —O] 2 —CH 2 CH 2 —OCH 3 VIIb.

6. A process as claimed in claim 4 , which process comprises reaction of a compound of formula XV

with a compound of formula XVI,

wherein LG 1 is as defined in claim 4 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 10, 2020
From: TOPIVERT PHARMA LIMITED
To: OXULAR ACQUISITIONS LIMITED
Reel/Frame 054610/0455 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 10, 2018
From: RESPIVERT LIMITED
To: TOPIVERT PHARMA LIMITED
Reel/Frame 047725/0470 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 10, 2014
From: FYFE, MATTHEW COLIN THOR
To: RESPIVERT LIMITED; TOPIVERT PHARMA LIMITED
Reel/Frame 032654/0672 →
Priority Claims (3)
GB 1305945.6 · Apr 2, 2013 · national
GB 1322678.2 · Dec 20, 2013 · national
GB 1402647.0 · Feb 14, 2014 · national
Continuity (1)
Related Publication 20140296271A1 · Oct 2, 2014