Heterocyclic compounds

• US 6,713,485 B2
• Filed: 02/08/2002
• Issued: 03/30/2004
• Est. Priority Date: 01/12/1998
• Status: Expired due to Term

• Current Assignee: Novartis Ag
• Original Assignee: Smithkline Beecham Corporation (GSK plc)
• Inventors: Lackey, Karen Elizabeth, Carter, Malcolm Clive, Cockerill, George Stuart, Smith, Kathryn Jane, Guntrip, Stephen Barry
• Primary Examiner(s): Rotman, Alan L.
• Assistant Examiner(s): TRUONG, TAMTHOM NGO
• Application Number:
  US10/071,358
• Publication Number:
  US 20020147205A1
• Time in Patent Office: 781 Days
• Field of Search: 514/266.24, 544/293
• US Class Current: 514/266.24
• CPC Class Codes: A61K 31/517 ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: C07D 239/94 Nitrogen atoms
• CPC Class Codes: C07D 405/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 405/14 containing three or more hetero rings
• CPC Class Codes: C07D 411/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 417/04 directly linked by a ring-member-to-ring-member bond
• CPC Class Codes: C07D 417/14 containing three or more hetero rings
• CPC Class Codes: C07D 471/04 Ortho-condensed systems

Abstract

The present invention relates to substituted heteroaromatic compounds, methods for their preparation, pharmaceutical compositions containing them and their use in medicine. Specifically, the invention relates to quinazoline derivatives useful in treating disorders mediated by protein tyrosine kinase activity, in particular erbB-2 and/or EGFR activity.

Claims

1. A compound of the formula:

and salts or solvates thereof.

2. A pharmaceutical formulation, comprising:

the compound of claim 1 or a pharmaceutically acceptable salt or solvate thereof together with one or more pharmaceutically acceptable carriers, diluents, or excipients.

3. A method of treating a susceptible cancer in a human or animal subject mammal, comprising administering to said subject an effective amount of a compound as claimed in claim 1, wherein said cancer is breast cancer, gastric cancer or head and neck cancer.

4. A method as claimed in claim 3, wherein the susceptible cancer is breast cancer.

5. A method as claimed in claim 3, wherein the susceptible cancer is gastric cancer.

6. A method as claimed in claim 3, wherein the susceptible cancer is head and neck cancer.

7. A compound of the formula:

and salts or solvates thereof.

8. A pharmaceutical formulation, comprising:

the compound of claim 7 or a pharmaceutically acceptable salt or solvate thereof together with one or more pharmaceutically acceptable carriers, diluents, or excipients.

9. A method of treating a susceptible cancer in a human or animal subject mammal, comprising administering to said subject an effective amount of a compound as claimed in claim 7, wherein said cancer is breast cancer, gastric cancer or head and neck cancer.

10. A method as claimed in claim 9, wherein the susceptible cancer is breast cancer.

11. A method as claimed in claim 9, wherein the susceptible cancer is gastric cancer.

12. A method as claimed in claim 9, wherein the susceptible cancer is head and neck cancer.

13. A compound of the formula:

and salts or solvates thereof.

14. A pharmaceutical formulation, comprising:

the compound of claim 13 or a pharmaceutically acceptable salt or solvate thereof together with one or more pharmaceutically acceptable carriers, diluents, or excipients.

15. A method of treating a susceptible cancer in a human or animal subject mammal, comprising administering to said subject an effective amount of a compound as claimed in claim 13, wherein said cancer is breast cancer, gastric cancer or head and neck cancer.

16. A method as claimed in claim 15, wherein the susceptible cancer is breast cancer.

17. A method as claimed in claim 15, wherein the susceptible cancer is gastric cancer.

18. A method as claimed in claim 15, wherein the susceptible cancer is head and neck cancer.