发明名称 TRICYCLIC HETEROCYCLE DERIVATIVES HAVING HIV REPLICATION INHIBITORY EFFECT
摘要 The present invention provides the following compound having anti-HIV activity of formula:;;wherein, A1 is C, CR1A or N; A2 is C, CR2A, or N;A3 is CR3A, CR3AR3B, N, NR3C, O, S, SO, or SO2;A4 is CR4A, CR4AR4B, N, NR4C, O, S, SO, or SO2;A5 is C, CR5A, or N;T1 ring is substituted or unsubstituted monocyclic carbocycle or substituted or unsubstituted monocyclic heterocycle;R1 is halogen, cyano, nitro or —X1—R11;R2 is substituted or unsubstituted alkyl and the like;n is 1 or 2;R3 is hydrogen, substituted or unsubstituted aromatic carbocyclyl;R4 is hydrogen or a carboxy protecting group;the other symbols are as specified in the description.
申请公布号 US2017107234(A1) 申请公布日期 2017.04.20
申请号 US201515311757 申请日期 2015.05.15
申请人 Shionogi & Co., Ltd. 发明人 KAWASUJI Takashi;TANIYAMA Daisuke;SUGIYAMA Shuichi;TAMURA Yoshinori
分类号 C07D513/06;C07D471/06;C07D471/16;C07D487/06 主分类号 C07D513/06
代理机构 代理人
主权项 1: A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1 is C, CR1A, or N; A2 is C, CR2A, or N; A3 is CR3A, CR3AR3B, N, NR3C, O, S, SO, or SO2; A4 is CR4A, CR4AR4B, N, NR4C, O, S, SO, or SO2; A5 is C, CR5A, or N; A6 is C, CR6A, or N; R1A, R2A, R3A, R3B, R4A, R4B, R5A, and R6A are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyl oxy, substituted or unsubstituted alkenyloxy, substituted or unsubstituted alkynyloxy, substituted or unsubstituted alkyl carbonyl, substituted or unsubstituted alkenyl carbonyl, substituted or unsubstituted alkynyl carbonyl, substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, substituted or unsubstituted non-aromatic heterocyclyl, substituted or unsubstituted aromatic carbocycle oxy, substituted or unsubstituted non-aromatic carbocycle oxy, substituted or unsubstituted aromatic heterocycle oxy, substituted or unsubstituted non-aromatic heterocycle oxy, substituted or unsubstituted aromatic carbocycle thio, substituted or unsubstituted non-aromatic carbocycle thio, substituted or unsubstituted aromatic heterocycle thio, substituted or unsubstituted non-aromatic heterocycle thio, substituted or unsubstituted aromatic carbocycle amino, substituted or unsubstituted non-aromatic carbocycle amino, substituted or unsubstituted aromatic heterocycle amino, substituted or unsubstituted non-aromatic heterocycle amino, substituted or unsubstituted aromatic carbocyclylcarbonyl, substituted or unsubstituted non-aromatic carbocyclylcarbonyl, substituted or unsubstituted aromatic heterocyclylcarbonyl, substituted or unsubstituted non-aromatic heterocyclylcarbonyl, substituted or unsubstituted aromatic carbocyclylalkylcarbonyl, substituted or unsubstituted non-aromatic carbocyclylalkylcarbonyl, substituted or unsubstituted aromatic heterocyclylalkyl carbonyl, substituted or unsubstituted non-aromatic heterocyclylalkylcarbonyl, substituted or unsubstituted amino, or substituted or unsubstituted carbamoyl; R3C and R4C are each independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyl oxy, substituted or unsubstituted alkenyloxy, substituted or unsubstituted alkynyloxy, substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl; or, R3A and R3B may be taken together to form oxo, R4A and R4B may be taken together to form oxo; R3A and R4A may be taken together with an adjacent atom to form substituted or unsubstituted monocyclic carbocycle, or substituted or unsubstituted monocyclic heterocycle, the carbocycle or heterocycle may be further fused to; R3A and R4C may be taken together with an adjacent atom to form substituted or unsubstituted monocyclic heterocycle, the heterocycle may be further fused to; R3C and R4A may be taken together with an adjacent atom to form substituted or unsubstituted monocyclic heterocycle, the heterocycle may be further fused to; R3C and R4C may be taken together with an adjacent atom to form substituted or unsubstituted monocyclic heterocycle, the heterocycle may be further fused to; R3A and R3B may be taken together with an adjacent atom to form substituted or unsubstituted spiro ring, the spiro ring may be further fused to; R4A and R4B may be taken together with an adjacent atom to form substituted or unsubstituted spiro ring, the spiro ring may be further fused to; R4B may be taken together with an atom on the circular arc of T1 ring to form substituted or unsubstituted monocyclic carbocycle, or substituted or unsubstituted monocyclic heterocycle, the carbocycle or heterocycle may be further fused to; R4C may be taken together with an atom on the circular arc of T1 ring to form substituted or unsubstituted monocyclic heterocycle, the heterocycle may be further fused to; the broken line means the presence or absence of bond, the adjacent broken lines do not exist at the same time, the carbon atoms on 1st, 2nd, and 3rd position are sp2 carbon; T1 ring is substituted or unsubstituted monocyclic carbocycle or substituted or unsubstituted monocyclic heterocycle, (1) the carbocycle or heterocycle may be fused with the other substituted or unsubstituted carbocycle or substituted or unsubstituted heterocycle, and/or (2) two atoms which are not adjacent to one another constituting the carbocycle or heterocycle may be bridged by substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene or substituted or unsubstituted alkynylene; R1 is halogen, cyano, nitro or —X1—R11, X1 is a bond, —O—, —S—, —NR12—, —CO—, —SO—, —SO2—, —O—CO—, —CO—O—, —NR12—CO—, —CO—NR12—, —NR12—CO—O—, —NR12—CO—NR13—, —NR12—SO2— or —SO2—NR12—, R11 is hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, or substituted or unsubstituted heterocyclyl, R12 and R13 are each independently hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or substituted or unsubstituted alkynyl, when X1 is —NR12—, —CO—NR12— or —SO2—NR12—, R11 and R12 may be taken together with an adjacent nitrogen atom to form substituted or unsubstituted heterocyclyl, X1 is —NR12—CO—NR13—, R11 and R13 may be taken together with an adjacent nitrogen atom to form substituted or unsubstituted heterocyclyl, R1 may be taken together with a carbon atom or a nitrogen atom on the circular arc of T1 ring to form substituted or unsubstituted monocyclic carbocycle, or substituted or unsubstituted monocyclic heterocycle, the carbocycle or heterocycle may be further fused to; R2 is each substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted alkenyloxy, substituted or unsubstituted alkynyloxy, substituted or unsubstituted cycloalkyloxy, or substituted or unsubstituted cycloalkenyloxy; n is 1 or 2; R3 is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, substituted or unsubstituted non-aromatic heterocyclyl, substituted or unsubstituted aromatic carbocycle alkenyl, substituted or unsubstituted non-aromatic carbocycle alkenyl, substituted or unsubstituted aromatic heterocycle alkenyl, substituted or unsubstituted non-aromatic heterocycle alkenyl, substituted or unsubstituted aromatic carbocycle alkynyl, substituted or unsubstituted non-aromatic carbocycle alkynyl, substituted or unsubstituted aromatic heterocycle alkynyl, or substituted or unsubstituted non-aromatic heterocycle alkynyl; and R4 is hydrogen or a carboxy protecting group.
地址 Osaka-shi, Osaka JP