公开(公告)号：KR100524701B1

公开(公告)日：2005-10-31

申请号：KR1020030057713

申请日：2003-08-20

Applicant: 한국화학연구원

Inventor： 공영대 ,  이일영 ,  김상요 ,  이진영 ,  김군도 ,  공재양

IPC: C07D239/54 ,  A61K31/505

Abstract: 본 발명은 5-이미노메틸기가 치환된 2,4-피리미딘다이온 유도체에 관한 것으로서, 더욱 상세하게는 2,4-피리미딘다이온 모핵의 C-5 위치에 다양한 이미노메틸기가 치환되어 있는 신규 화합물로서 수용체 티로신 키나제(RTK)로서의 상피세포 성장인자 수용체(EGFR)에 대한 우수한 억제활성을 나타내는 5-이미노메틸기가 치환된 2,4-피리미딘다이온 유도체에 관한 것이다.

상기 화학식 1에서, R
1 , R
2 , R
3 , R
4 및 R
5 는 각각 발명의 상세한 설명에서 정의한 바와 같다.

公开(公告)号：KR1020050020066A

公开(公告)日：2005-03-04

申请号：KR1020030057713

申请日：2003-08-20

Applicant: 한국화학연구원

Inventor： 공영대 ,  이일영 ,  김상요 ,  이진영 ,  김군도 ,  공재양

IPC: C07D239/54 ,  A61K31/505

Abstract: PURPOSE: Derivatives of 5-(iminomethyl)-2,4-pyrimidinedione are provided, which derivatives have activity inhibiting EGFR(epidermal growth factor receptor), so that they can be useful for treatment of cancer. CONSTITUTION: The derivatives of 5-(iminomethyl)-2,4-pyrimidinedione represented by formula (1) are provided, wherein R1 and R2 are independently hydrogen, optionally substituted C1-C10 alkyl or C3-C6 cycloalkyl, or optionally substituted C7-C15 benzyl; R3 and R4 are independently hydrogen, allyl, optionally substituted C1-C10 alkyl or C3-C6 cycloalkyl, optionally substituted C7-C15 benzyl, optionally substituted C6-C15 aryl, optionally substituted C6-C15 hetero atom containing ring, optionally substituted C3-C20 acyl, optionally substituted C3-C20 amide, or optionally substituted C3-C20 thioamide; and R5 is optionally substituted C1-C20 alkyl or C3-C6 cycloalkyl, optionally substituted C7-C15 benzyl, optionally substituted C6-C15 aryl, optionally substituted C6-C15 hetero atom containing ring, optionally substituted C1-C10 alkoxy, optionally substituted C7-C15 benzyloxy, optionally substituted C1-C10 amine, or cyano, provided that the substituent of R1, R2, R3, R4 and R5 is selected from halogen atom, cyano, amide, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, alkylsulfone and arylsulfone, and a case that R3 and R4 are hydrogen simultaneously, and R5 is methyl, hydroxy, phenyl or phenylamine is excluded.

Abstract translation: 目的：提供5-（亚氨基甲基）-2,4-嘧啶二酮的衍生物，该衍生物具有抑制EGFR（表皮生长因子受体）的活性，因此可用于治疗癌症。 构成：提供由式（1）表示的5-（亚氨基甲基）-2,4-嘧啶二酮的衍生物，其中R1和R2独立地为氢，任选取代的C 1 -C 10烷基或C 3 -C 6环烷基，或任选取代的C7- C15苄基; R 3和R 4独立地是氢，烯丙基，任选取代的C 1 -C 10烷基或C 3 -C 6环烷基，任选取代的C 7 -C 15苄基，任选取代的C 6 -C 15芳基，任选取代的C 6 -C 15杂原子的环，任选取代的C 3 -C 20 酰基，任选取代的C 3 -C 20酰胺或任选取代的C 3 -C 20硫代酰胺; 并且R 5是任选取代的C 1 -C 20烷基或C 3 -C 6环烷基，任选取代的C 7 -C 15苄基，任选取代的C 6 -C 15芳基，任选取代的C 6 -C 15杂原子的环，任选取代的C 1 -C 10烷氧基， C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷基， 烷氧基，C1-C6卤代烷氧基，C1-C6烷硫基，烷基砜和芳基砜，以及R3和R4同时为氢，R5为甲基，羟基，苯基或苯基胺的情况。