IP Library Granted Patent US 10,035,810
Granted Patent B2
US 10,035,810 · App. 15/902,077 · Granted Jul 31, 2018

5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative

Inventors: Simon Fraser Hunt (Nottingham, GB); Stuart Thomas Onions (Nottingham, GB); Vladimir Sherbukhin (Nottingham, GB); Euan Alexander Fraser Fordyce (Nottingham, GB); Peter John Murray (London, GB); Daniel William Brookes (London, GB); Kazuhiro Ito (London, GB); Peter Strong (London, GB)
Assignee: PULMOCIDE LIMITED
C07D519/00A61K9/10A61K9/14A61K31/55A61K45/06
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Quick Facts
Patent No.
US 10,035,810
App. No.
15/902,077
Granted
Jul 31, 2018
Kind
B2
Abstract

There is provided a 5,6-dihydro-4H-benzo[b]thieno-[2,3-d]azepine derivative which is useful in the treatment of respiratory syncytial virus (RSV) infection and for the prevention of disease associated with RSV infection. (Formula (1)).

Claims (30)

1. A process for the preparation of a compound of formula (I):

or a pharmaceutically acceptable salt thereof which comprises:

reacting a compound of formula (II)

or a salt thereof;

with 2-fluoro-6-methylaniline; or

reacting a compound of formula (III)

wherein LG is a leaving group;

or a salt thereof;

with 7-oxa-2-azaspiro[3,5]nonane or a salt thereof; or

reacting a compound of formula (IV)

or a salt thereof;

with the compound of formula (VI)

or a salt thereof.

2. A process for the preparation of the compound of formula (II)

or a salt thereof which comprises:

reacting a compound of formula (X)

wherein LG is a leaving group and R a is lower alkyl;

or a salt thereof;

with 7-oxa-2-azaspiro[3,5]nonane or a salt thereof, followed by hydrolysis of the carboxylate ester to the free acid; or

reacting a compound of formula (IX)

wherein R a is lower alkyl;

or a salt thereof;

with a compound of formula (VI)

or a salt thereof;

followed by hydrolysis of the carboxylate ester to the free acid.

3. The process according to claim 1 wherein the leaving group is a halogen atom.

4. The process according to claim 3 wherein the halogen atom is chlorine.

5. The process according to claim 2 wherein the leaving group is a halogen atom.

6. The process according to claim 5 wherein the halogen atom is chlorine.

7. The process according to claim 2 wherein the lower alkyl group is ethyl.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 22, 2018
From: HUNT, SIMON FRASER; ONIONS, STUART THOMAS; SHERBUKHIN, VLADIMIR; FORDYCE, EUAN ALEXANDER FRASER; MURRAY, PETER JOHN; COATES, MATTHEW STEPHEN; BROOKES, DANIEL WILLIAM; ITO, KAZUHIRO; STRONG, PETER; SYGNATURE DISCOVERY LTD
To: PULMOCIDE LIMITED
Reel/Frame 045001/0277 →
Priority Claims (1)
EP 14188494 · Oct 10, 2014 · regional
Continuity (3)
Continuation 15642637 · Jul 6, 2017
Continuation 15305003
Related Publication 20180179228A1 · Jun 28, 2018