Composition and synthesis of new reagents for inhibition of HIV replicationThe present invention provides compounds and compositions for inhibiting Vif and methods for treating viral infection, e.g., HIV infection.Formula i chemical compound or its enantiomer, diastereomer or officinal salt:whereinr is h, c 1-6alkyl, c 2-6thiazolinyl, c 2-6alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclylalkyl, wherein said c 1-6alkyl, c 2-6thiazolinyl, c 2-6alkynyl, aryl, heteroaryl, cycloalkyl or heterocyclylalkyl are optional independently to be selected from following substituent group replacement by 1,2,3,4 or 5: halogen, c 1-6alkyl, c 2-6thiazolinyl, c 2-6alkynyl, c 1-6haloalkyl, c 1-6hydroxy alkyl, c 1-6cyano group alkyl, aryl, heteroaryl, cycloalkyl, heterocyclylalkyl, heteroaryl alkyl, cycloalkyl, heterocyclylalkyl, cn, no 2, or a,-(c 1-4alkyl)-or a, sr a,-(c 1-4alkyl)-sr a, c (o) r b,-(c 1-4alkyl)-c (o) r b, c (o) nr cr d,-(c 1-4alkyl)-c (o) nr cr d, c (o) or a,-(c 1-4alkyl)-c (o) or a, oc (o) r b,-(c 1-4alkyl)-oc (o) r b, oc (o) nr cr d,-(c 1-4alkyl)-oc (o) nr cr d, nr cr d, nr cc (o) r b,-(c 1-4alkyl)-nr ccor b, nr cc (o) nr cr d,-(c 1-4alkyl)-nr cc (o) nr cr d, nr cc (o) or a,-(c 1-4alkyl)-nr cc (o) or a, c (=nr i) nr cr d, nr cc (=nr i) nr cr d, p (r f) 2, p (or e) 2, p (o) r er f, p (o) or eor f, s (o) r b,-(c 1-4alkyl)-s (o) r b, s (o) nr cr d,-(c 1-4alkyl)-s (o) nr cr d, s (o) 2r b,-(c 1-4alkyl)-s (o) 2r b, nr cs (o) 2r b,-(c 1-4alkyl)-nr cs (o) 2r b, s (o) 2nr cr dwith-(c 1-4alkyl)-s (o) 2nr cr dr a, r b, r c, r d, r d, r eand r findependently be selected from h, c separately 1-10alkyl, c 1-10haloalkyl, c 2-10thiazolinyl, c 2-10alkynyl, aryl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl alkyl, heteroaryl alkyl, cycloalkyl-alkyl and heterocyclylalkyl alkyl, wherein said c 1-10alkyl, c 1-10haloalkyl, c 2-10thiazolinyl, c 2-10alkynyl, aryl, cycloalkyl, heteroaryl, heterocyclylalkyl, aryl alkyl, heteroaryl alkyl, cycloalkyl-alkyl or heterocyclylalkyl alkyl be optional to be substituted with 1,2,3,4 or 5 and independently to be selected from following substituent group: oh, amino, halogen, c 1-6alkyl, aryl, aryl alkyl, heteroaryl, heteroaryl alkyl, cycloalkyl and heterocyclylalkyl; r gbe h, c 1-10alkyl, c 1-10haloalkyl, c 2-10thiazolinyl or c 2-10alkynyl; r 1, r 2and r 3independently be selected from h, no 2, nh 2, cf 3, br, cl, f and i; y is c (o), nr gco, so 2nr g, nr gso 2, nhc (o) nh, nhc (o) o, oc (o) nh or conr gand z does not exist, or is o, s, nr g, ch 2, so 2, c 1-6alkyl-or g, co or c 1-6alkyl-nr geliminating shown chemical compound 1,2,3,4,5,6,7,8 and 9 in figure 10 a-b.
ＨＩＶ 복제를 억제하기 위한 시약의 조성물 및 합성법 본 발명은 Vif를 억제하는 화합물 및 조성물 및 바이러스 감염증, 예를 들어, HIV 감염증을 치료하는 방법을 제공한다.  화학식 (I)의 화합물, 또는 이의 거울상이성체, 부분입체이성체 또는 약제학적으로 허용되는 염: [이미지] 상기 식에서, R은 H, C1-6 알킬, C2-6 알케닐, C2-6 알키닐, 아릴, 헤테로아릴, 시클로알킬, 또는 헤테로시클로알킬이고, 여기서, 상기 C1-6 알킬, C2-6 알케닐, C2-6 알키닐, 아릴, 헤테로아릴, 시클로알킬, 또는 헤테로시클로알킬은 할로, C1-6 알킬, C2-6 알케닐, C2-6 알키닐, C1-6 할로알킬, C1-6 히드록시알킬, C1-6 시아노알킬, 아릴, 헤테로아릴, 시클로알킬, 헤테로시클로알킬, 헤테로아릴알킬, 시클로알킬, 헤테로시클로알킬, CN, NO2, ORa, -(C1-4 알킬)-ORa, SRa, -(C1-4 알킬)-SRa, C(O)Rb, -(C1-4 알킬)-C(O)Rb, C(O)NRcRd, -(C1-4 알킬)-C(O)NRcRd, C(O)ORa, -(C1-4 알킬)-C(O)ORa, OC(O)Rb, -(C1-4 알킬)-OC(O)Rb, OC(O)NRcRd, -(C1-4 알킬)-OC(O)NRcRd, NRcRd, NRcC(0)Rb, -(C1-4 알킬)-NRcCORb, NRcC(O)NRcRd, -(C1-4 알킬)-NRcC(O)NRcRd, NRcC(O)ORa, -(C1-4 알킬)-NRcC(O)ORa, C(=NRi)NRcRd, NRcC(=NRi)NRcRd, P(Rf)2, P(ORe)2, P(O)ReRf, P(O)OReORf, S(O)Rb, -(C1-4 알킬)-S(O)Rb, S(O)NRcRd, -(C1-4 알킬)-S(O)NRcRd, S(O)2Rb, -(C1-4 알킬)-S(O)2Rb, NRcS(O)2Rb, -(C1-4 알킬)-NRcS(O)2Rb, S(O)2NRcRd, 및 -(C1-4 알킬)-S(O)2NRcRd로부터 독립적으로 선택된 1, 2, 3, 4, 또는 5개의 치환체에 의해서 치환되거나 치환되지 않으며; Ra, Rb, Rc, Rd, Rd, Re, 및 Rf은 각각 독립적으로 H, C1-10 알킬, C1-10 할로알킬, C2-10 알케닐, C2-10 알키닐, 아릴, 시클로알킬, 헤테로아릴, 헤테로시클로알킬, 아릴알킬, 헤테로아릴알킬, 시클로알킬알킬, 및 헤테로시클로알킬알킬로부터 선택되고, 여기서, 상기 C1-10 알킬, C1-10 할로알킬, C2-10 알케닐, C2-10 알키닐, 아릴, 시클로알킬, 헤테로아릴, 헤테로시클로알킬, 아릴알킬, 헤테로아릴알킬, 시클로알킬알킬 또는 헤테로시클로알킬알킬은 OH, 아미노, 할로, C1-6 알킬, 아릴, 아릴알킬, 헤테로아릴, 헤테로아릴알킬, 시클로알킬, 및 헤테로시클로알킬로부터 독립적으로 선택된 1, 2, 3, 4, 또는 5개의 치환체로 치환되거나 치환되지 않으며; Rg는 H, C1-10 알킬, C1-10 할로알킬, C2-10 알케닐, 또는 C2-10 알키닐이고; R1, R2, 및 R3는 독립적으로 H, NO2, NH2, CF3, Br, Cl, F, 및 I로부터 선택되고; Y는 C(O), NRgCO, SO2NRg, NRgSO2, NHC(O)NH, NHC(O)O, OC(O)NH, 또는 CONRg이고; Z는 부재하거나, O, S, NRg, CH2, SO2, C1-6 알킬-ORg, CO, C1-6 알킬-NRg이고; 단, 도 10A 내지도 10B에 도시된 화합물 1, 2, 3, 4, 5, 6, 7, 8 및 9는 배제된다. 