US 7,501,424 B2
N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
Dong-Yeon Kim, Seoul (Korea, Republic of); Dae-Jin Cho, Seoull (Korea, Republic of); Gong-Yeal Lee, Gyeonggi-Do (Korea, Republic of); Hong-Youb Kim, Seoul (Korea, Republic of); Seok-Hun Woo, Gyeonggi-do (Korea, Republic of); Yong-Seok Kim, Gyeonggi-Do (Korea, Republic of); Sun-Ahe Lee, Gyeonggi-Do (Korea, Republic of); and Byoung-Cheol Han, Incheon (Korea, Republic of)
Assigned to Il-Yang Pharm. Co., Ltd., Gyeonggi-do (Korea, Republic of)
Appl. No. 11/813,175
PCT Filed Sep. 07, 2005, PCT No. PCT/KR2005/002962
§ 371(c)(1), (2), (4) Date Sep. 18, 2007,
PCT Pub. No. WO2007/018325, PCT Pub. Date Feb. 15, 2007.
Claims priority of application No. 10-2005-0071656 (KR), filed on Aug. 05, 2005.
Prior Publication US 2008/0096899 A1, Apr. 24, 2008
Int. Cl. C07D 239/28 (2006.01); A61K 31/505 (2006.01)
U.S. Cl. 514—255.05  [514/275; 544/295; 544/331] 7 Claims
 
1. N-phenyl-2-pyrimidine-amine compound represented by the following formula (1):

OG Complex Work Unit Drawing
or its salt, in which
R1 represents optionally substituted thiazole, imidazole or pyrazine
(wherein the substituent is amino group or lower alkyl);
R2, R3 and R6 each independently represent hydrogen, halogen, lower alkyl or lower alkoxy;
R4 and R5 each independently represent hydrogen and R4 and R5 are not simultaneously hydrogen; or
R4 or R5 each represents a radical having the following formula (2):

OG Complex Work Unit Drawing
wherein R7 represents lower alkyl or lower alkyl substituted with 1 to 3 halogen, R8 represents aliphatic having 5 to 10 carbon atoms, or represents optionally substituted 5 to 7 membered saturated or unsaturated monocyclic radical (wherein the substituent is lower alkyl), or bi- or tri-cyclic radical optionally combined with
a benzene ring(s), each of which has 1 to 3 hetero atoms selected from a group
consisting of nitrogen, oxygen and sulfur, or represents piperazinyl or
homopiperazinyl each of which is substituted by lower alkyl.