Quinazoline derivatives

• US 7,148,230 B2
• Filed: 06/01/2004
• Issued: 12/12/2006
• Est. Priority Date: 07/29/2003
• Status: Expired due to Fees

• Current Assignee: Astrazeneca AB (Astrazeneca PLC)
• Original Assignee: Astrazeneca AB (Astrazeneca PLC)
• Inventors: Kettle, Jason Grant, Bradbury, Robert Hugh, Hennequin, Laurent Francois Andre, Turner, Andrew, McCabe, James
• Primary Examiner(s): Wilson, James O.
• Assistant Examiner(s): TRUONG, TAMTHOM NGO
• Application Number:
  US10/857,342
• Publication Number:
  US 20050165035A1
• Time in Patent Office: 924 Days
• Field of Search: 514/266.22, 514/266.4, 544/284, 544/293
• US Class Current: 514/266.22
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: C07D 401/12 linked by a chain containing hetero atoms as chain links

Abstract

The invention concerns quinazoline derivatives of Formula I

wherein R¹ and R² have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB, particularly EGF, receptor tyrosine kinases.

Claims

1. A quinazoline derivative of the Formula I:

2. A quinazoline derivative according to claim 1 which is 4-(3-chloro-2-fluoroanilino)-6-[1-(hydroxyacetyl)piperidin-4-yloxy]-7-methoxyquinazoline;

or a pharmaceutically acceptable salt thereof.

3. A quinazoline derivative according to claim 1 or claim 2 or a pharmaceutically acceptable acid salt thereof.

4. A pharmaceutical composition which comprises a quinazoline derivative of the Formula I, or a pharmaceutically-acceptable salt, thereof, as defined in claim 1 or claim 2 in association with a pharmaceutically-acceptable diluent or carrier.

5. A process for the preparation of a quinazoline derivative of the Formula I, or a pharmaceutically acceptable salt, or a pharmaceutically acceptable salt thereof, which process comprises:

coupling a compound of the Formula II, or a salt thereof;