Patent
FAK inhibitors
| العنوان: | FAK inhibitors |
|---|---|
| Patent Number: | 9,012,461 |
| تاريخ النشر: | April 21, 2015 |
| Appl. No: | 13/543276 |
| Application Filed: | July 06, 2012 |
| مستخلص: | A compound of the formula (I): [chemical expression included] where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor. |
| Inventors: | Holmes, Ian Peter (Bundoora, AU); Bergman, Ylva (Parkville, AU); Lunniss, Gillian Elizabeth (Parkville, AU); Nikac, Marica (Parkville, AU); Choi, Neil (Parkville, AU); Hemley, Catherine Fae (Parkville, AU); Walker, Scott Raymond (Parkville, AU); Foitzik, Richard Charles (Parkville, AU); Ganame, Danny (Bundoora, AU); Lessene, Romina (Bundoora, AU) |
| Assignees: | Cancer Therapeutics CRC Pty Ltd (Bundoora, AU) |
| Claim: | 1. A compound of formula (I): [chemical expression included] wherein: R 1 is selected from: H and [chemical expression included] wherein: R N1 is selected from H, C 1-3 alkyl and C(═O)Me; R N2 is selected from H, C 1-3 alkyl and C(═O)Me; R N3 is selected from H, C 1-3 alkyl and C(═O)Me; R N4 is selected from H and CH 3 ; R N7 and R N8 are independently selected from H and CH 3 ; R N9 is selected from H, C 1-3 alkyl and C(═O)Me; R N ′ is selected from H, C 1-3 alkyl and C(═O)Me; R N11 is selected from H, C 1-3 alkyl and C(═O)Me; R 2 is selected from H and [chemical expression included] wherein: R N5 is selected from H, C 1-3 alkyl and C(═O)Me; R N6 is selected from H, C 1-3 alkyl and C(═O)Me; and wherein only one of R 1 and R 2 is H; or R 1 and R 2 together form the group —CH 2 —N(R N12)—C 2 H 4 —, where R N12 is selected from H, C 1-3 alkyl and C(═O)Me; R 4 is selected from CF 3 , halo, CF 2 H and CN; and R 5 is selected from groups of the following formulae: [chemical expression included] wherein: R 6 is selected from H, (CHR C1) n1 C(O)N(R N13)Z 1 and (CH 2) n2 C(O)OZ 2 ; wherein: n1 is 1; R C1 is H or Me; R N13 is H or CH 3 ; Z 1 is H, CH 3 or OCH 3 ; n2 is 1; and Z 2 is CH 3 ; and where only one of R N12 and Z 1 can be CH 3 , R 7 , if present, is selected from H, and (CH 2) m1 C(O)N(R M1)Y 1 , wherein: m1 is 0 or 1; R M1 is H; and Y 1 is H, Me or OCH 3 ; and one of R 6 and R 7 is not H; and R 8 , if present, is H or, when R 7 is C(═O)NH 2 , R 8 is selected from H and C 1-2 alkyl. |
| Claim: | 2. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N1 is C(═O)Me. |
| Claim: | 3. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N1 is H, methyl or ethyl. |
| Claim: | 4. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N2 is selected from H, methyl and ethyl. |
| Claim: | 5. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N3 is selected from H and methyl. |
| Claim: | 6. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N4 is selected from H and methyl. |
| Claim: | 7. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N7 and R N8 are both H or both methyl. |
| Claim: | 8. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N9 is H. |
| Claim: | 9. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N10 is selected from H and methyl. |
| Claim: | 10. A compound according to claim 1 , wherein R 2 is H and R 1 is: [chemical expression included] wherein R N11 is H. |
| Claim: | 11. A compound according to claim 1 , wherein R 1 is H and R 2 is: [chemical expression included] where R N5 is selected from H and methyl. |
| Claim: | 12. A compound according to claim 1 , wherein R 1 is H and R 2 is: [chemical expression included] where R N6 is selected from H and methyl. |
| Claim: | 13. A compound according to claim 1 , wherein R 4 is selected from CF 3 , Cl and CF 2 H. |
| Claim: | 14. A compound according to claim 13 , wherein R 4 is CF 3 . |
| Claim: | 15. A compound according to claim 1 , wherein R 5 is a group of the following formula: [chemical expression included] |
| Claim: | 16. A compound according to claim 1 , wherein R 5 is a group selected from: [chemical expression included] |
| Claim: | 17. A compound according to claim 15 , wherein R 7 is H and R 6 is selected from CH 2 C(O)NH 2 , CH 2 C(O)NHCH 3 , CHCH 3 C(O)NH 2 and CHCH 3 C(O)NHCH 3 . |
| Claim: | 18. A compound according to claim 17 , wherein R 7 is H and R 6 is selected from CH 2 C(O)NH 2 , CHCH 3 C(O)NH 2 and CH 2 C(O)NHCH 3 . |
| Claim: | 19. A compound according to claim 18 , wherein R 7 is H and R 6 is selected from CH 2 C(O)NH 2 , and CHCH 3 C(O)NH 2 . |
| Claim: | 20. A compound according to claim 15 , wherein R 6 is H and R 7 is selected from C(O)NH 2 , C(O)NHCH 3 , CH 2 C(O)NH 2 and CH 2 C(O)NHCH 3 . |
| Claim: | 21. A compound according to claim 20 , wherein R 6 is H and R 7 is C(O)NH 2 . |
| Claim: | 22. A compound according to claim 21 , wherein R 8 is methyl. |
| Claim: | 23. A compound according to claim 1 , wherein R 5 is a group of the following formula: [chemical expression included] |
| Claim: | 24. A composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier or diluent. |
| Claim: | 25. A method of treating a disease ameliorated by the inhibition of FAK comprising administering a therapeutically-effective amount of a compound according to claim 1 . |
| Claim: | 26. The method of claim 25 , wherein the compound is administered as a pharmaceutical composition. |
| Claim: | 27. A compound have the following chemical structure: [chemical expression included] |
| Current U.S. Class: | 514/256 |
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| Primary Examiner: | Jean-Louis, Samira |
| Attorney, Agent or Firm: | Wallace, W. David Holland & Knight LLP |
| رقم الانضمام: | edspgr.09012461 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |