IP Library Granted Patent US 9,670,191
Granted Patent B2
US 9,670,191 · App. 14/688,207 · Granted Jun 6, 2017

Pyridyl-and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors

Inventors: Ermes Vanotti (Milan, IT); Marina Caldarelli (Milan, IT); Alessandra Cirla (Varese, IT); Barbara Forte (Milan, IT); Antonella Ermoli (Buccinasco, IT); Maria Menichincheri (Milan, IT); Antonio Pillan (Milan, IT); Alessandra Scolaro (Bresso, IT)
Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
C07D409/14A61K31/4439A61K31/4545A61K31/4725A61K31/496A61K31/506A61K31/5377A61K45/06A61N5/10C07D401/04C07D401/14C07D403/04C07D403/14C07D405/04C07D405/14C07D409/04
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Quick Facts
Patent No.
US 9,670,191
App. No.
14/688,207
Granted
Jun 6, 2017
Kind
B2
Abstract

The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Claims (20)

1. A method for treating cell proliferative disorders caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a compound which is 5-(2-amino-pyrimidin-4-yl)-2-(2,3-dimethyl-phenyl)-1H-pyrrole-3-carboxylic acid amide, or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 , wherein the cell proliferative disorder is selected from the group consisting of cervical cancer, colon cancer, ovarian cancer, pancreatic cancer, breast cancer, ductal breast cancer, epidermal cancer, lung cancer, large cell lung cancer, squamous cell lung cancer, small cell lung cancer, non-small cell lung cancer, medullary thyroid cancer, papillary thyroid cancer, astrocitoma, neuroblastoma, glioblastoma, gliosarcoma, melanoma and osteosarcoma.

3. The method according to claim 1 , wherein the cell proliferative disorder is selected from the group consisting of colon cancer, pancreatic cancer, breast cancer, ductal breast cancer, large cell lung cancer, squamous cell lung cancer, small cell lung cancer, non-small cell lung cancer, medullary thyroid cancer, papillary thyroid cancer, neuroblastoma, glioblastoma, gliosarcoma, melanoma and osteosarcoma.

4. The method according to claim 3 , wherein the cell proliferative disorder is selected from the group consisting of colon cancer, pancreatic cancer, breast cancer, large cell lung cancer, squamous cell lung cancer, small cell lung cancer, non-small cell lung cancer, medullary thyroid cancer, papillary thyroid cancer, neuroblastoma, glioblastoma, and melanoma.

5. The method according to claim 4 , wherein the cell proliferative disorder is selected from the group consisting of colon cancer, non-small cell lung cancer, medullary thyroid cancer, papillary thyroid cancer, neuroblastoma, glioblastoma, and melanoma.

6. The method according to claim 5 , wherein the cell proliferative disorder is selected from the group consisting of colon cancer, non-small cell lung cancer, neuroblastoma, glioblastoma, and melanoma.

7. The method according to claim 6 , wherein the cell proliferative disorder is selected from the group consisting of colon cancer and non-small cell lung cancer.

8. The method according to claim 1 further comprising subjecting the mammal in need thereof to radiation therapy or chemotherapy regimen in combination with at least one cytostatic or cytotoxic agent.

9. The method according to claim 1 wherein the mammal in need thereof is a human.

10. A method for treating cell proliferative disorders caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of pharmaceutical composition comprising a compound which is 5-(2-amino-pyrimidin-4-yl)-2-(2,3-dimethyl-phenyl)-1H-pyrrole-3-carboxylic acid amide, or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient, carrier or diluent.

11. The method according to claim 10 , wherein said pharmaceutical composition comprises from about 10 mg to about 1000 mg of said 5-(2-amino-pyrimidin-4-yl)-2-(2,3-dimethyl-phenyl)-1H-pyrrole-3-carboxylic acid amide, or a pharmaceutically acceptable salt thereof.

12. The method according to claim 11 , wherein said pharmaceutical composition is in the form of a tablet, a capsule, a solution, or a suspension.

13. The method according to claim 12 , wherein said pharmaceutical composition is in the form of a tablet or capsule.

14. The method according to claim 13 , wherein said pharmaceutical composition is in the form of a tablet.

15. The method according to claim 14 , wherein said pharmaceutical composition is in the form of a capsule.

16. The method according to claim 10 , wherein the cell proliferative disorder is selected from the group consisting of cervical cancer, colon cancer, ovarian cancer, pancreatic cancer, breast cancer, ductal breast cancer, epidermal cancer, lung cancer, large cell lung cancer, squamous cell lung cancer, small cell lung cancer, non-small cell lung cancer, medullary thyroid cancer, papillary thyroid cancer, astrocitoma, neuroblastoma, glioblastoma, gliosarcoma, melanoma and osteosarcoma.

17. The method according to claim 16 , wherein the cell proliferative disorder is selected from the group consisting of colon cancer, non-small cell lung cancer, medullary thyroid cancer, papillary thyroid cancer, neuroblastoma, glioblastoma, and melanoma.

18. The method according to claim 17 , wherein the cell proliferative disorder is selected from the group consisting of colon cancer and non-small cell lung cancer.

19. The method according to claim 10 further comprising subjecting the mammal in need thereof to radiation therapy or chemotherapy regimen in combination with at least one cytostatic or cytotoxic agent.

20. The method according to claim 10 wherein the mammal in need thereof is a human.

Priority Claims (1)
EP 06111766 · Mar 27, 2006 · regional
Continuity (4)
Continuation 14531261 · Nov 3, 2014
Continuation 13559762 · Jul 27, 2012
Division 12293951
Related Publication 20150218138A1 · Aug 6, 2015