Kinase inhibitor

Patent metadata

Field	Value
Publication number	US-9822076-B2
Application number	US-201615291359-A
Country	US
Kind code	B2
Filing date	Oct 12, 2016
Priority date	Oct 1, 2014
Publication date	Nov 21, 2017
Grant date	Nov 21, 2017

Abstract

There is provided a compound of formula VIIa,

wherein Q x represents —C(O)O—C 1-4 alkyl, or a salt or protected derivative thereof, and other compounds that are useful in the preparation of compounds that have 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) 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.

First claim

What is claimed is:

1. A compound of formula VIIa,

wherein Q x represents —C(O)O—C 1-4 alkyl,
or a salt thereof.

2. A compound of formula VIIa, or a salt thereof, as claimed in claim 1 , wherein said compound is methyl 4-((4-((4-(3-(5-(tert-butyl)-2-methoxy-3-(methylsulfonamido)phenyl)ureido)naphthalen-1-yl)oxy)pyridin-2-yl)amino)-2-methoxybenzoate.

3. A process for the preparation of a compound of formula VIIa, as defined in claim 1 , which process comprises:
(a) reaction of a compound of formula IIp,

with a compound of formula IIIp,

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

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

wherein Q x represents —C(O)O—C 1-4 alkyl;
(b) reaction of a compound of formula IIap

 wherein Z 1p 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 1p —C(O)—N 3 ) to provide, in situ, a compound of formula II, which compound is then reacted with a compound of formula IIIp as defined above;
(c) reaction of a compound of formula IIbp,

 wherein LG 1 represents a leaving group and Z 1p is as defined above, with a compound of formula IIIp, as defined above; or
(d) reaction of a compound of formula VI,

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

wherein Q x is as defined above.

Assignees

• Respivert Ltd
• Topivert Pharma Ltd

Inventors

• Fyfe Matthew Colin Thor

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P9/12

  Antihypertensives · CPC title