Substituted indazole derivatives active as kinase inhibitors

Patent metadata

Field	Value
Publication number	US-9102662-B2
Application number	US-201414534648-A
Country	US
Kind code	B2
Filing date	Nov 6, 2014
Priority date	Jul 20, 2007
Publication date	Aug 11, 2015
Grant date	Aug 11, 2015

Abstract

Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.

First claim

What is claimed is:

1. A compound which is N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(piperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)-benzamide, or a pharmaceutically acceptable salt thereof.

2. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient, carrier or diluent.

3. A pharmaceutical composition according to claim 2 , comprising from about 10 mg to about 500 mg of said N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(piperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)-benzamide, or a pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition according to claim 2 , wherein said pharmaceutical composition is in the form of a tablet, a capsule, a solution, or a suspension.

5. A pharmaceutical composition according to claim 4 , wherein said pharmaceutical composition is in the form of a capsule or tablet.

6. A pharmaceutical composition according to claim 5 , wherein said pharmaceutical composition is in the form of a capsule.

7. A pharmaceutical composition according to claim 5 , wherein said pharmaceutical composition is in the form of a tablet.

8. A pharmaceutical composition according to claim 2 , wherein said pharmaceutical composition comprises at least one pharmaceutically acceptable carrier or diluent.

9. A pharmaceutical composition according to claim 8 , wherein said at least one pharmaceutically acceptable carrier or diluent is selected from at least one of lactose, dextrose, saccharose, sucrose, cellulose, corn starch, potato starch, mannitol, sorbitol, natural gum, agar, sodium alginate, pectin, methylcellulose, caboxymethylcellulose, polyvinylalcohol, water, olive oil, ethyl oleate, propylene glycol, cocoa butter, polyethylene glycol, a polyoxyethylenesorbitan fatty acid ester surfactant and lecithin.

10. A pharmaceutical composition according to claim 2 , wherein said at least one pharmaceutically acceptable excipient is at least one lubricant.

11. A pharmaceutical composition according to claim 10 , wherein said at least one lubricant is selected from at least one of silica, talc, stearic acid, magnesium stearate, calcium stearate, and polyethylene glycols.

12. A pharmaceutical composition according to claim 2 , wherein said at least one pharmaceutically acceptable excipient is at least one binding agent.

13. A pharmaceutical composition according to claim 12 , wherein said at least one binding agent is selected from at least one of starches, arabic gum, gelatin methylcellulose, carboxymethylcellulose and polyvinylpyrrolidone.

14. A pharmaceutical composition according to claim 2 , wherein said at least one pharmaceutically acceptable excipient is at least one disintegrating agent.

15. A pharmaceutical composition according to claim 14 , wherein said at least one disintegrating agent is selected from at least one of starch, alginic acid, aligantes and sodium starch glycolate.

16. A pharmaceutical composition according to claim 2 , wherein said at least one pharmaceutically acceptable excipient, carrier or diluent comprises at least one diluent and at least one lubricant.

17. A pharmaceutical composition according to claim 16 , wherein said pharmaceutical composition is in the form of a capsule or tablet.

18. A pharmaceutical composition according to claim 17 , wherein said pharmaceutical composition is in the form of a capsule.

19. A pharmaceutical composition according to claim 17 , wherein said pharmaceutical composition is in the form of a tablet.

20. A pharmaceutical composition according to claim 2 , wherein said at least one pharmaceutically acceptable excipient, carrier or diluent comprises at least one diluent and at least one binding agent.

21. A pharmaceutical composition according to claim 2 , wherein said at least one pharmaceutically acceptable excipient, carrier or diluent comprises at least one diluent and at least one disintegrating agent.

22. A pharmaceutical composition according to claim 21 , further comprising at least one binding agent.

23. A pharmaceutical composition according to claim 20 , further comprising at least one disintegrating agent.

24. A pharmaceutical composition according to claim 2 , wherein said at least one pharmaceutically acceptable excipient, carrier or diluent comprises at least one diluent, at least one lubricant, at least one binding agent, and at least one disintegrating agent.

25. A pharmaceutical composition according to claim 10 , wherein said pharmaceutical composition is in the form of a capsule or tablet.

26. A pharmaceutical composition according to claim 25 , wherein said pharmaceutical composition is in the form of a capsule.

27. A pharmaceutical composition according to claim 25 , wherein said pharmaceutical composition is in the form of a tablet.

28. A pharmaceutical composition according to claim 24 , wherein said pharmaceutical composition is in the form of a capsule or tablet.

29. A pharmaceutical composition according to claim 28 , wherein said pharmaceutical composition is in the form of a capsule.

30. A pharmaceutical composition according to claim 28 , wherein said pharmaceutical composition is in the form of a tablet.

Assignees

• Nerviano Medical Sciences Srl

Inventors

• Lombardi Borgia Andrea
• Menichincheri Maria
• Orsini Paolo
• Panzeri Achille
• Perrone Ettore
• Vanotti Ermes
• Nesi Marcella
• Marchionni Chiara

Classifications

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P35/04

  specific for metastasis · CPC title

• A61P43/00

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

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61P41/00

  Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution · CPC title