公开(公告)号：KR1020100041799A

公开(公告)日：2010-04-22

申请号：KR1020107002073

申请日：2008-06-26

Applicant: 한국화학연구원

Inventor： 구오혼지안 ,  김정은 ,  이일영 ,  미첼마이클엘 ,  로데스게리 ,  손종찬 ,  쉬리안홍

IPC: C07D239/54 ,  C07D401/04 ,  A61K31/506 ,  A61P31/18

CPC classification number: A61K31/513 ,  A61K31/496 ,  A61K31/536 ,  A61K31/551 ,  A61K31/66 ,  A61K31/7048 ,  A61K31/7072 ,  A61K31/708 ,  A61K39/39558 ,  A61K45/06 ,  C07D239/54 ,  C07D239/545 ,  C07D239/553 ,  C07D239/60 ,  C07D401/04 ,  C07D403/04

Abstract: PURPOSE: A compound of suppressing a novel HIV reverse transcriptase is provided to suppress both wild type HIV strain and mutant type HIV strain and to treat AIDS. CONSTITUTION: A compound suppressing a novel HIV reverse trascriptase is denoted by chemical formula I. HIV infection is treated by mixing a compound of chemical formula I, compound suppressing HIV protease, HIV non-nucleoside reverse transcriptase inhibitor, HIV nucleoside reverse transcriptase inhibitor, HIV nucleotide reverse transcriptase inhibitor, HIV integrase inhibitor, gp41 inhibitor, CXCR4 inhibitor, gp120 inhibitor, G6PD and NADH-oxidase inhibitor, CCR5 inhibitor, other HIV drug, or mixture thereof.

Abstract translation: 目的：提供抑制新型HIV逆转录酶的化合物以抑制野生型HIV菌株和突变型HIV病毒株，并治疗AIDS。 构成：抑制新型HIV逆转录酶的化合物由化学式I表示。HIV感染通过混合化学式I化合物，抑制HIV蛋白酶的化合物，HIV非核苷逆转录酶抑制剂，HIV核苷逆转录酶抑制剂，HIV 核苷酸逆转录酶抑制剂，HIV整合酶抑制剂，gp41抑制剂，CXCR4抑制剂，gp120抑制剂，G6PD和NADH-氧化酶抑制剂，CCR5抑制剂，其他HIV药物或其混合物。

公开(公告)号：KR101551238B1

公开(公告)日：2015-09-09

申请号：KR1020107002073

申请日：2008-06-26

Applicant: 한국화학연구원

Inventor： 구오혼지안 ,  김정은 ,  이일영 ,  미첼마이클엘 ,  로데스게리 ,  손종찬 ,  쉬리안홍

IPC: C07D239/54 ,  C07D401/04 ,  A61K31/506 ,  A61P31/18

CPC classification number: A61K31/513 ,  A61K31/496 ,  A61K31/536 ,  A61K31/551 ,  A61K31/66 ,  A61K31/7048 ,  A61K31/7072 ,  A61K31/708 ,  A61K39/39558 ,  A61K45/06 ,  C07D239/54 ,  C07D239/545 ,  C07D239/553 ,  C07D239/60 ,  C07D401/04 ,  C07D403/04

Abstract: 본발명은하기화학식 I의화합물, 또는그의약학적으로허용가능한염, 용매화물및/또는에스터, 이러한화합물을함유하는조성물, 이러한화합물의투여를포함하는치료방법에관한것이다: [화학식 I]

公开(公告)号：KR1020100092960A

公开(公告)日：2010-08-23

申请号：KR1020107013671

申请日：2008-12-17

Applicant: 한국화학연구원

Inventor： 구오혼지안 ,  휴맨스테이시 ,  이일영 ,  미첼마이클 ,  페이퍼스티븐 ,  손종찬

IPC: C07D239/10 ,  A61K31/513 ,  A61P31/18

CPC classification number: C07D239/54

Abstract: PURPOSE: A method for preparing HIV reverse transcriptase inhibitor is provided to improve the manufacture and to suppress replication of novel mutant strain. CONSTITUTION: A method for preparing a compound of chemical formula I with HIV reverse transcriptase suppression activity or pharmaceutically acceptable salt thereof comprises: a step of reacting a compound of chemical formula VIII with 3-chloro-5-methylbenzyl cyanide, 3-bromo-5-methylbenzyl cyanide or 3-iodo-5-methylbenzyl cyanide; a step of oxidizing a compound of chemical formula VII to obtain a compound of chemical formula VI; a step of hydrolyzing a compound of chemical formula VI to obtain a compound of chemical formula II; a step of reacting the compound of chemical formula II with cyanide reagent to form a compound of chemical formula III; a step of reacting the compound of chemical formula III with R^1Z^1(Z^1 is a leaving group) to obtain a compound of chemical formula IV; a step of reacting a compound of chemical formula IV with Y-X^2-O-X^1-Z62(Z^2 is a leaving group) to obtain the compound of chemical formula I.

Abstract translation: 目的：提供一种制备HIV逆转录酶抑制剂的方法，以改善制备和抑制新突变菌株的复制。 构成：用于制备具有HIV逆转录酶抑制活性的化学式I化合物或其药学上可接受的盐的方法包括：使化学式VIII的化合物与3-氯-5-甲基苄基氰，3-溴-5 氰甲基苄基氰或3-碘-5-甲基苄基氰; 氧化化学式VII的化合物以获得化学式VI的化合物的步骤; 水解化学式VI化合物以获得化学式II的化合物的步骤; 使化学式II的化合物与氰化物试剂反应形成化学式III的化合物的步骤; 使化学式III的化合物与R 1'Z ^ 1（Z 1是离去基团）反应以获得化学式IV的化合物的步骤; 使化学式IV化合物与Y-X 2 O-X 1 -Z 62（Z 2是离去基团）反应得到化学式I的化合物的步骤。