公开(公告)号：KR1019990074328A

公开(公告)日：1999-10-05

申请号：KR1019980007843

申请日：1998-03-10

Applicant: 한국화학연구원

Inventor： 손종찬 ,  김진철 ,  김신걸 ,  강석구

IPC: C07D239/54 ,  A61K31/505 ,  C07D239/60

Abstract: 본 발명은 하기 일반식(I)의 2,4-피리미딘디온 유도체 및 그의 약제학적으로 허용되는 염, 이의 제조방법 및 이를 유효성분으로 함유하는 항바이러스제 조성물에 관한 것으로, 일반식(I)의 화합물은 바이러스, 특히 HIV-1에 대한 선택도 및 생리활성도가 우수하고 독성이 낮아서 후천성 면역결핍증(AIDS) 치료제로 유용하다.
(I)
상기식에서,
R
1 은 C
1 -C
10 의 알콕시메틸, C
1 -C
10 의 알케닐메틸, C
1 -C
10 의 알킬, C
1 -C
10 의 알키닐메틸 또는 C
1 -C
10 의 알콕시카르보닐메틸이고;
R
2 는 수소, 할로겐, C
1 -C
6 의 알킬, C
3 -C
6 의 시클로알킬, C
2 -C
8 의 알케닐, C
2 -C
8 의 알키닐 또는 벤질이고;
R
3 및 R
4 는 각각 독립적으로 수소, 할로겐, 히드록시, 아지도, 아미노, C
1 -C
3 의 알킬, 불소화알킬, C
1 -C
8 의 알콕시, C
2 -C
8 의 알케닐, C
2 -C
8 의 알키닐 또는 벤질이고;
X는 할로겐, 아지도, 시아노, 아미노, C
1 -C
4 의 알킬에스테르, C
1 -C
10 의 알킬아미드 또는 C
1 -C
20 의 알콕시이다.

公开(公告)号：KR100390096B1

公开(公告)日：2003-08-19

申请号：KR1019980007843

申请日：1998-03-10

Applicant: 한국화학연구원

Inventor： 손종찬 ,  김진철 ,  김신걸 ,  강석구

IPC: C07D239/54 ,  A61K31/505 ,  C07D239/60

Abstract: PURPOSE: Provided are a novel antiviral 2,4-pyrimidinone derivative, its pharmaceutically acceptable salt, a method for manufacturing the same and an antiviral composition containing it as an active ingredient. The 2,4-pyrimidinone derivative is excellent in HIV-1 selectivity and physiological activity, and has low toxicity. Therefore, it is useful as the therapeutics for AIDS. CONSTITUTION: A novel 2,4-pyrimidinone derivative is represented by the formula(I), wherein R1 is C1-10 alkoxymethyl; R2 is hydrogen or C1-6 alkyl; R3 and R4 are independently hydrogen, halogen, C1-3 alkyl or fluorinated alkyl; and X is halogen, azido, cyano or C1-10 alkoxy. It is manufactured by the steps of; reacting a compound of the formula(II) with hexamethyldisilaxane to give a compound of the formula(III), and coupling the compound of the formula(III) with a compound of the formula(IV).

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。