公开(公告)号：KR1020010006730A

公开(公告)日：2001-01-26

申请号：KR1020000010614

申请日：2000-03-03

Applicant: 한국화학연구원

Inventor： 손종찬 ,  신선실 ,  김신걸 ,  이종교 ,  김해수

IPC: C07D239/04

Abstract: PURPOSE: Provided are 2,4-pyrimidinedione derivatives which are excellent in selectivity and bioactivity for wild type and mutant HIV-1 and have low toxicity, therefore which can be used for treating AIDS. CONSTITUTION: The 2,4-pyrimidinedione derivatives represented by the formula I are prepared by coupling two compounds represented by the formulas II and III, wherein R1 is phenyl, pyridyl, methyl, amino, nitro, methoxy, trifluoromethyl, and etc., R2 is ethyl, isopropyl, etc., R3 and R4 is independently hydrogen, fluorine, chlorine, methyl, fluoromethyl, nitro, etc., A is oxygen or sulfur, Z is oxygen, sulfur, C=O, NH, or CH2, Z' is equal to the Z but Z' is acetamido if A is oxygen, Y is halogen, methane sulfonyl, toluene sulfonyl, or trifluoromethane sulfonyl.

Abstract translation: 目的：提供野生型和突变HIV-1的选择性和生物活性优异且毒性低的2,4-嘧啶二酮衍生物，因此可用于治疗AIDS。 构成：由式I表示的2,4-嘧啶二酮衍生物通过偶联由式II和III表示的两种化合物制备，其中R 1是苯基，吡啶基，甲基，氨基，硝基，甲氧基，三氟甲基等，R 2 是乙基，异丙基等，R3和R4独立地是氢，氟，氯，甲基，氟甲基，硝基等，A是氧或硫，Z是氧，硫，C = O，NH或CH2，Z 如果A是氧，Y是卤素，甲磺酰基，甲苯磺酰基或三氟甲磺酰基，则Z'是乙酰氨基。

公开(公告)号：KR100368891B1

公开(公告)日：2003-01-24

申请号：KR1020000010614

申请日：2000-03-03

Applicant: 한국화학연구원

Inventor： 손종찬 ,  신선실 ,  김신걸 ,  이종교 ,  김해수

IPC: C07D239/04

Abstract: PURPOSE: Provided are 2,4-pyrimidinedione derivatives which are excellent in selectivity and bioactivity for wild type and mutant HIV-1 and have low toxicity, therefore which can be used for treating AIDS. CONSTITUTION: The 2,4-pyrimidinedione derivatives represented by the formula I are prepared by coupling two compounds represented by the formulas II and III, wherein R1 is phenyl, pyridyl, methyl, amino, nitro, methoxy, trifluoromethyl, and etc., R2 is ethyl, isopropyl, etc., R3 and R4 is independently hydrogen, fluorine, chlorine, methyl, fluoromethyl, nitro, etc., A is oxygen or sulfur, Z is oxygen, sulfur, C=O, NH, or CH2, Z' is equal to the Z but Z' is acetamido if A is oxygen, Y is halogen, methane sulfonyl, toluene sulfonyl, or trifluoromethane sulfonyl.

Abstract translation: 用途：提供2,4-嘧啶二酮衍生物，对野生型和突变型HIV-1具有优异的选择性和生物活性，毒性低，因此可用于治疗艾滋病。 构成：由式I表示的2,4-嘧啶二酮衍生物是通过偶联由式II和III表示的两种化合物来制备的，其中R1是苯基，吡啶基，甲基，氨基，硝基，甲氧基，三氟甲基等，R2 为乙基，异丙基等，R 3和R 4独立地为氢，氟，氯，甲基，氟甲基，硝基等，A为氧或硫，Z为氧，硫，C = O，NH或CH 2，Z '等于Z但Z'是乙酰胺基，如果A是氧，Y是卤素，甲磺酰基，甲苯磺酰基或三氟甲磺酰基。