IP Library › Granted Patent US 9,067,936
Granted Patent B2
US 9,067,936 · App. 14/237,905 · Granted Jun 30, 2015

4-(8-methoxy-1-((1-methoxypropan-2-yl)-2-(tetrahydro-2H-pyran-4-yl)-1 H-imidazo[4,5-C]quinolin-7-yl)-3,5-dimethylisoxazole and its use as bromodomain inhibitor

Inventors: Emmanuel Hubert Demont (Stevenage, GB); Katherine Louise Jones (Stevenage, GB); Robert J. Watson (Stevenage, GB)
Assignee: GlaxoSmithKline LLC
C07D471/04A61K31/4745
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Quick Facts
Patent No.
US 9,067,936
App. No.
14/237,905
Granted
Jun 30, 2015
Kind
B2
Abstract

Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.

Claims (15)

1. A compound of formula (I) which is 4-(8-methoxy-1-(1-methoxypropan-2-yl)-2-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole

or a salt thereof.

2. A compound of formula (IA) which is 4-(8-methoxy-1-((R)-1-methoxypropan-2-yl)-2-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole

or a salt thereof.

3. A compound of formula (IB) which is 4-(8-methoxy-1-((S)-1-methoxypropan-2-yl)-2-(tetrahydro-2H-pyran-4-yl)-1H-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole

or a salt thereof.

4. A compound according to claim 2 or a pharmaceutically acceptable salt thereof.

5. A pharmaceutical composition which comprises a compound or a pharmaceutically acceptable salt thereof as defined in claim 4 and one or more pharmaceutically acceptable carriers, diluents or excipients.

6. A combination pharmaceutical product comprising a compound or a pharmaceutically acceptable salt thereof as defined in claim 4 together with one or more other therapeutically active agents.

7. A method of treating a chronic autoimmune and/or inflammatory condition which comprises administering, to a human subject in need thereof, a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof as defined in claim 4 .

8. A method of treating cancer which comprises administering, to a human subject in need thereof, a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof as defined in claim 4 .

9. A method according to claim 8 wherein said cancer is a leukaemia, a NUT-midline carcinoma, multiple myeloma, lung cancer, a neuroblastoma, Burkitt's lymphoma, cervical cancer, esophageal cancer, ovarian cancer, breast cancer, or colorectal cancer.

10. A salt of a compound of Formula (IA) according to claim 2 wherein said salt is selected from the group consisting of hydrochloride, sulfate, maleate, fumarate, citrate, p-toluenesulfonate, benzenesulfonate, and methanesulfonate salt.

11. A salt according to claim 10 wherein said salt is a methanesulfonate salt.

12. A compound of formula (IA) which is 4 -( 8 -methoxy- 1 -((R)- 1 -methoxypropan- 2 -yl)- 2 -(tetrahydro- 2 H-pyran- 4 -yl)- 1 H- imidazo[ 4 , 5 -c]quinolin- 7 -yl)- 3 , 5 -dimethylisoxazole.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 10, 2014
From: DEMONT, EMMANUEL HUBERT; JONES, KATHERINE LOUISE; WATSON, ROBERT J.
To: GLAXOSMITHKLINE LLC
Reel/Frame 032179/0939 →
Priority Claims (1)
GB 1114103.3 · Aug 17, 2011 · national
Continuity (1)
Related Publication 20140171462A1 · Jun 19, 2014