Substituted indazole derivatives active as kinase inhibitors

Patent metadata

Field	Value
Publication number	US-9616059-B2
Application number	US-201514971372-A
Country	US
Kind code	B2
Filing date	Dec 16, 2015
Priority date	Jul 20, 2007
Publication date	Apr 11, 2017
Grant date	Apr 11, 2017

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 method for treating a patient having a cancer selected from the group consisting of ovarian cancer, lung cancer, colon cancer and lymphoma, comprising administering to said patient an effective amount of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide, or a pharmaceutically acceptable salt thereof, and an effective amount of at least one second therapeutic agent, wherein said at least one second therapeutic agent is selected from antihormonal agents, antiestrogens, antiandrogens, aromatase inhibitors, topoisomerase I inhibitors, topoisomerase II inhibitors, agents that target microtubules, platin-based agents, alkylating agents, DNA damaging agents, DNA intercalating agents, antineoplastic antimetabolites, kinase inhibitors, anti-angiogenic agents, inhibitors of kinesins, therapeutic monoclonal antibodies, mTOR inhibitors, histone deacetylase inhibitors, farnesyl transferase inhibitors, and hypoxic response inhibitors.

2. The method of claim 1 , wherein said cancer is lung cancer.

3. The method of claim 1 , wherein said cancer is colon cancer.

4. The method of claim 1 , wherein said cancer is lymphoma.

5. The method of claim 1 , wherein said cancer is ovarian cancer.

6. The method of claim 1 , wherein said N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide, or a pharmaceutically acceptable salt thereof, and said at least one second therapeutic agent are simultaneously administered to said patient.

7. The method of claim 1 , wherein said N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide, or a pharmaceutically acceptable salt thereof, and said at least one second therapeutic agent are sequentially administered to said patient.

8. The method according to claim 1 , wherein said at least one second therapeutic agent is selected from kinase inhibitors.

9. The method according to claim 8 , wherein said cancer is selected from lung cancer, colon cancer, ovarian cancer, and lymphoma.

10. The method of claim 9 , wherein said cancer is lung cancer.

11. The method of claim 9 , wherein said cancer is colon cancer.

12. The method of claim 9 , wherein said cancer is ovarian cancer.

13. The method of claim 9 , wherein said cancer is lymphoma.

Assignees

• Nerviano Medical Sciences Srl

Inventors

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

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• 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

• A61P41/00

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

• A61P35/04

  specific for metastasis · CPC title

• A61P39/06

  Free radical scavengers or antioxidants · CPC title