IP Library › Granted Patent US 10,392,346
Granted Patent B2
US 10,392,346 · App. 16/035,502 · Granted Aug 27, 2019

Kinase inhibitors

Inventors: Thomas Matthew Baker (Nottingham, GB); Matthew Colin Thor Fyfe (London, GB); Geraint Jones (Nottingham, GB); Stephen Malcolm Thom (Nottingham, GB)
Assignee: Topivert Pharma Limited
C07D213/74A61K31/4375A61K31/44A61K31/444A61K31/4412A61K31/4439A61K31/4545A61K31/496A61K31/505A61K31/506A61K31/5377A61K31/541A61K31/551A61K31/553A61K31/635A61K31/675A61K31/706A61K31/7052A61K45/06C07D213/80C07D239/47C07D401/12C07D405/12C07D413/12C07D453/02C07F9/58C07F9/59C07F9/6512C07F9/65031C07F9/65583C07H13/08C07H15/26C07H19/048
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Quick Facts
Patent No.
US 10,392,346
App. No.
16/035,502
Granted
Aug 27, 2019
Kind
B2
Abstract

There are provided compounds of formula IIb, wherein: LG 1 represents imidazolyl, chloro, or aryloxy; and Z 1 represents a structural fragment of formula V: wherein R 2 to R 4 , R 5a , L and X 1 to X 3 have meanings given in the description, or a salt or protected derivative thereof, wherein said protected derivative is a compound in which the carboxyl moiety of R 4 is protected as a C 1-8 alkyl ester. The compounds have antiinflammatory activity, for example 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) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Claims (19)

1. A compound of formula IIb,

wherein:

LG 1 represents imidazolyl, chloro, or aryloxy; and

Z 1 represents a structural fragment of formula V:

wherein:

R 2 and R 3 , together with the C-atoms to which they are attached, form a fused phenyl ring;

X 1 , X 2 and X 3 all represent CH;

L represents a direct bond;

R 5a represents methoxy; and

R 4 represents —CO 2 H,

or a salt or protected derivative thereof, wherein said protected derivative is a compound in which the carboxyl moiety of R 4 is protected as a C 1-8 alkyl ester.

2. A compound as claimed in claim 1 , wherein LG 1 represents phenoxy.

3. A compound as claimed in claim 1 , wherein Z 1 represents a structural fragment of formula Vp

wherein:

R 4′ represents a C 1-4 alkyl group; and

R 2 , R 3 , X 1 , X 2 , X 3 , L and R 5a are as defined in claim 1 .

4. A compound as claimed in claim 3 , wherein R 4′ represents a C 1-3 alkyl group.

5. A compound as claimed in claim 1 , wherein the carboxyl moiety of R 4 is protected as an ethyl or methyl ester.

6. A compound as claimed in claim 1 , wherein the carboxyl moiety of R 4 is protected as a methyl ester.

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 Jun 29, 2020
From: BAKER, THOMAS MATTHEW; FYFE, MATTHEW COLIN THOR; JONES, GERAINT; THOM, STEPHEN MALCOLM
To: TOPIVERT PHARMA LIMITED; RESPIVERT LIMITED
Reel/Frame 053072/0626 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 10, 2018
From: RESPIVERT LIMITED
To: TOPIVERT PHARMA LIMITED
Reel/Frame 047725/0470 →
Priority Claims (2)
GB 1417344.7 · Oct 1, 2014 · national
GB 1510694.1 · Jun 18, 2015 · national
Continuity (3)
Continuation 15604258 · May 24, 2017
Division 14872527 · Oct 1, 2015
Related Publication 20180319748A1 · Nov 8, 2018