Quinazolin-4 (3H)-one derivatives used as P13 kinase inhibitors

Patent metadata

Field	Value
Publication number	US-9637494-B2
Application number	US-201615092707-A
Country	US
Kind code	B2
Filing date	Apr 7, 2016
Priority date	Oct 18, 2010
Publication date	May 2, 2017
Grant date	May 2, 2017

Abstract

The present invention relates to the compound of formula (I)

and to compositions comprising the same and to the use of the compound and to compositions of the compound in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compound.

First claim

The invention claimed is:

1. A method of treatment of a condition selected from: COPD (including chronic bronchitis and emphysema), asthma, paediatric asthma, cystic fibrosis, sarcoidosis, idiopathic pulmonary fibrosis, allergic rhinitis, rhinitis, sinusitis, allergic conjunctivitis, conjunctivitis, allergic dermatitis, contact dermatitis, psoriasis, ulcerative colitis, inflamed joints secondary to rheumatoid arthritis or osteoarthritis, rheumatoid arthritis, pancreatitis, cachexia, inhibition of the growth and metastasis of tumours including non-small cell lung carcinoma, breast carcinoma, gastric carcinoma, colorectal carcinomas and malignant melanoma which comprises administering to a subject in need thereof an effective amount of a compound of formula (I):

that is 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl) methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof.

2. A method according to claim 1 , wherein the compound of formula (I) is in free base form.

3. A method for sensitizing a subject suffering from COPD or asthma to treatment with a corticosteroid, where the subject has previously become refractory to treatment with a corticosteroid, comprising administering to a subject in need thereof a an effective amount of a compound of formula (I):

that is 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl) methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof.

4. A method according to claim 3 , wherein the compound of formula (I) is in free base form.

Assignees

• Respivert Ltd
• Respivert Ltd

Inventors

• King-Underwood John
• Ito Kazuhiro
• Murray Peter John
• Hardy George
• Brookfield Frederick Arthur
• Brown Christopher John

Classifications

• A61P35/04

  specific for metastasis · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P37/08

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

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title