CHOI JANG-SIK,SONG HO-JUHN,KIM HONG WOO,LIM SUN-HEE,KIM YOUNGSAM,LEE JAEKYOO,KOH JONG SUNG,CHANG SUNHWA,LEE HEE KYU
申请号：
NZ59904010
公开号：
NZ599040A
申请日:
2010.10.29
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
Disclosed are 2-(piperidin-1-yl)-4-amino-pyrido[4,3-d]pyrimidine-5(6H)-one and 2-(benzylamino)-4-amino-pyrido[4,3-d]pyrimidine-5(6H)-one derivatives as represented by the general formula (I), wherein: R1 is H X is NR2R3 or NR4R5 Y is NHR6 Z is selected from H, halogen, alkyl, alkynyl, aryl, heteroaryl, or cycloalkyl, wherein the alkyl, cycloalkyl, aryl, alkynyl or heteroaryl is optionally substituted R2 and R3, taken together with the nitrogen atom to which they are bonded form: i) a 3-8 membered saturated or partially unsaturated monocyclic group having no heteroatom other than the nitrogen atom to which R2 and R3 are bonded, wherein said 3-8 membered saturated or partially unsaturated monocyclic group is substituted at one or more carbon atoms with 1-2 R7 or ii) an 8-10 membered bicyclic aryl group having 0-5 heteroatoms independently selected from nitrogen, oxygen, sulfur, sulfoxide, or sulfone R4 is selected from H, alkyl, or hydroxyalkyl R5 is arylalkyl, wherein the aryl group is independently substituted at one or more carbon atoms with 1-3 R11 R11 is independently selected from OR9, NR9R9, NR9COR9, or NR9S(O)nR9 R6 is selected from alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, arylalkyl, or heteroaryl, wherein the heterocycloalkyl, aryl, or heteroaryl is optionally substituted and wherein the remaining substituents are as defined herein. Representative compounds include 2-(4-hydroxypiperidin-1-yl)-4-(3-(trifluoromethyl)phenylamino)pyrido[4,3-d] pyrimidine-5(6H)-one and 2-(4-hydroxy-4-(hydroxymethyl)piperidin-1-yl)-4-(4-methoxy-3-(trifluromethyl) phenylamino)pyrido[4,3-d]pyrimidin-5(6H)-one.
