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    • 1. 发明申请
    • ANTI-VIRAL AGENT CONTAINING HETEROCYCLIC AROMATIC COMPOUND AS ACTIVE INGREDIENT
    • 含有作为活性成分的杂环芳族化合物的抗病毒剂
    • US20100256379A1
    • 2010-10-07
    • US12739795
    • 2008-10-22
    • Masanori BabaYuichi HashimotoHiroshi AoyamaKumiko SakoShinichi SatoKatsuyuki Nagai
    • Masanori BabaYuichi HashimotoHiroshi AoyamaKumiko SakoShinichi SatoKatsuyuki Nagai
    • C07D471/04
    • C07D209/86C07D307/91C07D471/04
    • The present invention relates to an anti-viral agent comprising a compound represented by the following formula (I): (wherein X represents CH, a nitrogen atom, an oxygen atom, or a sulfur atom; Y and Z are the same or different and each represents a nitrogen atom or C—R8, and at least one of them represents a nitrogen atom; R1 to R8 are the same or different and each represents a hydrogen atom, a linear C1-10-hydrocarbon group, a hydroxy group, or a substituted or unsubstituted benzyl group; and, when X represents an oxygen atom or a sulfur atom, R5 is absent), or the following formula (II): (wherein X′ represents CH or a nitrogen atom; Y′ and Z′ are the same or different and each represents a nitrogen atom or N—R9, or C—R8 and at least one of them represents a nitrogen atom or N—R9; R1 to R4 and R6 to R8 are as defined above; R9 represents a hydrogen atom, a linear C1-10-hydrocarbon group, a hydroxy group, or a substituted or unsubstituted benzyl group; and, the C ring has the maximum number of double bonds at the dotted line portion) or a pharmaceutically acceptable salt thereof.
    • 本发明涉及包含由下式(I)表示的化合物的抗病毒剂:(其中X表示CH,氮原子,氧原子或硫原子; Y和Z相同或不同, 各自表示氮原子或C-R8,并且其中至少一个表示氮原子; R 1〜R 8相同或不同,表示氢原子,直链C 1-10烃基,羟基或 取代或未取代的苄基;当X表示氧原子或硫原子时,R 5不存在)或下式(II)表示:(其中X'表示CH或氮原子,Y'和Z'为 相同或不同,各自表示氮原子或N-R9或C-R8,并且其中至少一个表示氮原子或N-R 9; R 1至R 4和R 6至R 8如上所定义; R 9表示氢 原子,直链C 1-10烃基,羟基或取代或未取代的苄基;和C环h 作为虚线部分的双键的最大数目)或其药学上可接受的盐。
    • 7. 发明申请
    • Tricyclic compound, process for producing the same, and use
    • 三环化合物,其制备方法和用途
    • US20060178359A1
    • 2006-08-10
    • US10544470
    • 2004-02-05
    • Mitsuru ShiraishiMasaki SetoKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • Mitsuru ShiraishiMasaki SetoKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • A61K31/55A61K31/4745C07D487/14
    • C07D471/04A61K31/4353A61K31/55
    • A compound of the formula: wherein R1 is a 5- or 6-membered ring; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group -Z2a-W2-Z2b-, wherein Z2a and Z2b are each O, S(O)q (wherein q is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain; W is a group represented by wherein R3 and R3′ are each a hydrogen atom, a lower alkyl group, or a lower alkoxy group; X is CH or N; n and n′ are each an integer of 0 or 1 to 4; m and m′ are each 1 or 2; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a lower alkyl group, or a lower acyl group); and R2 is (1) an amino group, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide; or a salt thereof. The compound exhibits excellent CCR antagonist activity against CCR5, and is useful as a prophylactic and/or therapeutic agent for HIV infection in human peripheral blood mononuclear cells, especially for AIDS.
    • 下式的化合物:其中R 1是5或6元环; Z 1是5或6元芳环; Z 2是基团-Z 2 O 2 -W 2 -Z 2b 2,其中Z 2a 和/或O 2各自为O,S(O)q q(其中q为0,1或2),亚氨基或键; 和W 2是亚烷基链; W是由R 3和R 3'表示的基团各自为氢原子,低级烷基或低级烷氧基; X是CH或N; n和n'各自为0或1〜4的整数; m和m'分别为1或2; Y是O,S(O)p(其中p是0,1或2),CH 2或NR 4(其中R' SUP> 4 是氢原子,低级烷基或低级酰基); R 2是(1)可以将氮原子转化为季铵或氧化物的氨基,或者(2)可含有硫原子的含氮杂环基 或氧原子作为构成环的原子,其中氮原子可以转化为季铵或氧化物; 或其盐。 该化合物对CCR5表现出优异的CCR拮抗剂活性,并且可用作人外周血单核细胞(特别是AIDS)中HIV感染的预防和/或治疗剂。