Patent
Quinazoline derivatives as kinase inhibitors
| العنوان: | Quinazoline derivatives as kinase inhibitors |
|---|---|
| Patent Number: | 8,324,205 |
| تاريخ النشر: | December 04, 2012 |
| Appl. No: | 12/471280 |
| Application Filed: | May 22, 2009 |
| مستخلص: | The present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. |
| Inventors: | Pandey, Anjali (Fremont, CA, US); Scarborough, Robert M. (Half Moon Bay, CA, US); Matsuno, Kenji (Tokyo, JP); Ichimura, Michio (Tokyo, JP); Nomoto, Yuji (Shizuoka, JP); Ide, Shinichi (Tokyo, JP); Tsukuda, Eiji (Tokyo, JP); Sasaki, Junko (Akita, JP); Oda, Shoji (Tokyo, JP) |
| Assignees: | Millennium Pharmaceuticals, Inc. (Cambridge, MA, US), Kyowa Hakko Kogyo Co., Ltd. (Tokyo, JP) |
| Claim: | 1. A method of treating glioma in a patient comprising the step of administering a compound of: [chemical expression included] wherein R 1 is a member selected from the group consisting of: —CN, —O-methyl, —O-ethyl, —O-propyl, —O-isopropyl, —O-butyl, —O-t-butyl, —O-isoamyl, 1-naphthyloxy, 2-naphthyloxy, 4-indolyloxy, 5-indolyloxy, 5-isoquinolyloxy, and position isomers thereof; n is 2 or 3; R 3 is a member selected from the group consisting of: —OH, —O—CH 3 , —O—CH 2 —CH 3 , —NH 2 , —N(—CH 3) 2 , —NH(—CH 2 -phenyl), —NH(-phenyl), —CN [chemical expression included] and all pharmaceutically acceptable isomers, salts, hydrates and solvates thereof to the patient. |
| Claim: | 2. A method according to claim 1 , wherein in the compound or pharmaceutically acceptable salt thereof, R 1 is a member selected from the group consisting of —CN and —O-isopropyl and n is 3. |
| Claim: | 3. A method according to claim 2 , wherein R 3 is selected from the group consisting of piperidine, pyrrolidine, morpholine, piperazine, 4-methyl-piperidine and 2-methyl-piperidine. |
| Claim: | 4. A method according to claim 3 , wherein the compound has the following formula: [chemical expression included] {4-[6-methoxy-7-(3-piperidylpropoxy)quinazolin-4-yl]piperazinyl}-N-[4-(methylethoxy)phenyl]carboxamide. |
| Current U.S. Class: | 5142/345 |
| Patent References Cited: | 6169088 January 2001 Matsuno et al. 6207667 March 2001 Matsuno et al. 6423716 July 2002 Matsuno et al. 6472391 October 2002 Matsuno et al. 6750218 June 2004 Matsuno et al. 6982266 January 2006 Pandey et al. 2002/0068734 June 2002 Matsuno et al. 2003/0100573 May 2003 Wang et al. 2005/0070560 March 2005 Himmelsbach et al. 0 882 717 December 1998 1 067 123 January 2001 WO 99-51582 October 1999 WO 02/16360 February 2002 WO 02/16361 February 2002 WO 02/16362 February 2002 WO 02/072578 September 2002 |
| Other References: | Agrawal, Vijai et al.: “Antiparasitic agents. Part VI: Synthesis of 7-chloro-4-(4-substituted-phenylanino)- and 7-chloro-4-(4-substituted-piperazin-1-yl)quinolines as potential antiparasitic agents” Indian J. Chem., Sect. B (1987), 26(B)6, pp. 550-555. cited by other |
| Assistant Examiner: | Sackey, Ebenezer O |
| Primary Examiner: | Wilson, James O |
| Attorney, Agent or Firm: | Kilpatrick Townsend and Stockton LLP |
| رقم الانضمام: | edspgr.08324205 |
| قاعدة البيانات: | USPTO Patent Grants |
| الوصف غير متاح. |