公开(公告)号：EP1636230A2

公开(公告)日：2006-03-22

申请号：EP04754702.1

申请日：2004-06-07

Applicant: Endacea, Inc.

Inventor： WILSON, Constance, N. ,  PARTRIDGE, John, J.

IPC: C07D473/06 ,  A61K31/522 ,  A61P9/04 ,  A61P11/06 ,  A61P37/08 ,  A61P13/12 ,  A61P25/28 ,  A61P25/24 ,  A61P3/10 ,  A61P29/00 ,  A61P25/16

CPC classification number: C07D473/06

Abstract: This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C8 alkyl; R2 is of the formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or (CH2)pCH3, and R6 is H or (CH2)mOH, wherein p is an integer ranging from 1 to 7 and m is an integer ranging from 1 to 8; R3 is of the formula (III), wherein q is an integer ranging from 1 to 8; and R7 is selected from the group consisting of H, OH, NH2, (CH2)tOH, and R9COOH; wherein R9 is a straight or branched chain alkylene or alkenylene group having 1 to 8 carbon atoms, and t is an integer ranging from 1 to 8; R4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 is selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COOH; wherein f is 0 or f and s are independently integers ranging from 1 to 8; and, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts, solvates, and hydrates thereof. The present invention further provides methods of preparing the compounds of formula (I) and their use as therapeutic agents and diagnostic agents.

Abstract translation: 本发明涉及式（I）的化合物：其中R 1为支链或直链C 1 -C 8烷基; R2具有式（II），其中n是1至8的整数; R5为H或（CH2）pCH3，R6为H或（CH2）mOH，其中p为1至7的整数，m为1至8的整数; R3具有式（III），其中q是1至8的整数; 且R 7选自H，OH，NH 2，（CH 2）t OH和R 9 COOH; 其中R9是具有1至8个碳原子的直链或支链亚烷基或亚烯基，并且t是1至8的整数; R4具有式（IV），其中r是1至8的整数，并且R8选自H，OH，（CH2）fNH2，（CH2）sOH和R10COOH; 其中f是0或f并且s独立地是1至8范围内的整数; 并且R 10是C 1 -C 8直链或支链亚烷基或亚烯基; 和; 盐，溶剂化物和水合物。 本发明进一步提供了制备式（I）化合物的方法及其作为治疗剂和诊断剂的用途。