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    • 1. 发明申请
    • Acrylamide derivative, process for producing the same, and use
    • 丙烯酰胺衍生物,其制造方法和用途
    • US20060160864A1
    • 2006-07-20
    • US10544275
    • 2004-02-02
    • Mitsuru ShiraishiMasaki SetoKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • Mitsuru ShiraishiMasaki SetoKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • A61K31/4439A61K31/4178A61K31/40C07D403/02
    • C07D213/73
    • A compound represented by the formula: wherein R1 is a 5- or 6-membered ring; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; R7 and R8 are each a hydrogen atom or a lower alkyl group; Z1 is another 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W1-Z2b- [wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group or a bond, and W1 is an alkylene chain]; X is CR (wherein R is a hydrogen atom, a lower alkyl group, a lower alkoxy group, an acyl group, or R and adjacent R4 may form a 5- or 6-membered alicyclic heterocyclic group) or N; R4 is NR5R6 (wherein R5 and R6 are each a hydrogen atom, a hydrocarbon group, a heterocyclic group or an acyl group), or R5 and R6 are bonded to each other to form a heterocyclic group of NR5R6; and R2 is (1) an amino group which may be a quaternary ammonium or oxide, (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 the like; or a salt thereof. The compound has excellent CCR5 antagonistic activity and thus is useful as a prophylactic and/or therapeutic medicine for HIV infection into human peripheral blood monocyte, especially for AIDS.
    • 由下式表示的化合物:其中R 1是5或6元环; R 3是氢原子,低级烷基或低级烷氧基; R 7和R 8各自为氢原子或低级烷基; Z 1是另一个5或6元芳环; Z 2是由-Z 2a表示的基团,其中Z 2a和Z 2b各自为O,S(O)m(其中m为0,1或2),亚氨基或键, 和W 1是亚烷基链]; X是CR(其中R是氢原子,低级烷基,低级烷氧基,酰基或R和相邻的R 4)可以形成5-或6-元脂环族杂环基 )或N; R 4是NR 5 R 6(其中R 5和R 6)是 各自为氢原子,烃基,杂环基或酰基)或R 5和R 6彼此键合以形成NR的杂环基 5< 5> 6< 6> 和R 2是(1)可以是季铵或氧化物的氨基,(2)可以含有硫原子或氧原子的含氮杂环基作为环的构成 原子,其中氮原子可以转化成季铵或氧化物等; 或其盐。 该化合物具有优异的CCR5拮抗活性,因此可用作HIV感染人外周血单核细胞,特别是用于艾滋病的预防和/或治疗药物。
    • 3. 发明申请
    • Fused-ring pyridine derivative, process for producing the same, and use
    • 稠环吡啶衍生物,其制备方法及用途
    • US20060100197A1
    • 2006-05-11
    • US10544435
    • 2004-02-05
    • Mitsuru ShiraishiKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • Mitsuru ShiraishiKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • A61K31/55A61K31/541A61K31/5377A61K31/496A61K31/4743A61K31/4741C07D498/02C07D491/02C07D471/02
    • A61K31/55C07D471/04
    • The present invention provides a compound represented by the formula: wherein R1 is a 5- or 6-membered ring which may be substituted; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W2-Z2b wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain which may be substituted; n is an integer of 0 to 4; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a hydrocarbon group, a heterocyclic group, or an acyl group); and R2 is (1) an amino group, in which the nitrogen atom is converted to quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as a ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, and the like, or a salt thereof. The compound has excellent CCR5 antagonist activity and is useful as a prophylactic and/or therapeutic medicine for HIV infection in human peripheral mononuclear blood cells, especially AIDS.
    • 本发明提供由下式表示的化合物:其中R 1是可被取代的5或6元环; R 3是氢原子,低级烷基或低级烷氧基; Z 1是5或6元芳环; Z 2是由-Z 2 O 2 -W 2 -Z 2b表示的基团,其中Z 2a (O)m(其中m为0,1或2),亚氨基或键; O,S(O) 且W 2是可以被取代的亚烷基链; n为0〜4的整数。 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,烃基,杂环基或酰基); 和R 2是(1)氮原子转化为季铵或氧化物的氨基,(2)可含有硫原子或氧原子的含氮杂环基 作为其中氮原子可以转化为季铵或氧化物的环构成原子等,或其盐。 该化合物具有优异的CCR5拮抗剂活性,可用作人外周血单核细胞尤其是艾滋病中HIV感染的预防和/或治疗药物。
    • 5. 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。
    • 10. 发明授权
    • Fused-ring pyridine derivative, process for producing the same, and use
    • 稠环吡啶衍生物,其制备方法及用途
    • US07288654B2
    • 2007-10-30
    • US10544435
    • 2004-02-05
    • Mitsuru ShiraishiKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • Mitsuru ShiraishiKatsuji AikawaNaoyuki KanzakiMasanori Baba
    • C07D471/02
    • A61K31/55C07D471/04
    • The present invention provides a compound represented by the formula: wherein R1 is a 5- or 6-membered ring which may be substituted; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W2-Z2b wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain which may be substituted; n is an integer of 0 to 4; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a hydrocarbon group, a heterocyclic group, or an acyl group); and R2 is (1) an amino group, in which the nitrogen atom is converted to quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as a ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, and the like, or a salt thereof. The compound has excellent CCR5 antagonist activity and is useful as a prophylactic and/or therapeutic medicine for HIV infection in human peripheral mononuclear blood cells, especially AIDS.
    • 本发明提供由下式表示的化合物:其中R 1是可被取代的5或6元环; R 3是氢原子,低级烷基或低级烷氧基; Z 1是5或6元芳环; Z 2是由-Z 2 O 2 -W 2 -Z 2b表示的基团,其中Z 2a (O)m(其中m为0,1或2),亚氨基或键; O,S(O) 且W 2是可以被取代的亚烷基链; n为0〜4的整数。 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,烃基,杂环基或酰基); 和R 2是(1)氮原子转化为季铵或氧化物的氨基,(2)可含有硫原子或氧原子的含氮杂环基 作为其中氮原子可以转化为季铵或氧化物的环构成原子等,或其盐。 该化合物具有优异的CCR5拮抗剂活性,可用作人外周血单核细胞尤其是艾滋病中HIV感染的预防和/或治疗药物。