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    Bicyclic Compound, Production and Use Thereof
    2.
    发明申请
    Bicyclic Compound, Production and Use Thereof 有权
    双环化合物，其生产和使用

    公开(公告)号：US20090030032A1

    公开(公告)日：2009-01-29

    申请号：US12119355

    申请日：2008-05-12

    申请人： Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Iizawa

    发明人： Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Iizawa

    IPC分类号： A61K31/44 ,  C07D401/02

    CPC分类号： A61K31/4196 ,  A61K31/395 ,  A61K31/4178 ,  C07D225/06 ,  C07D313/20 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12

    摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

    摘要翻译： 本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。 本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

    Acrylamide derivative, process for producing the same, and use
    4.
    发明申请
    Acrylamide derivative, process for producing the same, and use 审中-公开
    丙烯酰胺衍生物，其制造方法和用途

    公开(公告)号：US20060160864A1

    公开(公告)日：2006-07-20

    申请号：US10544275

    申请日：2004-02-02

    申请人： Mitsuru Shiraishi ,  Masaki Seto ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    发明人： Mitsuru Shiraishi ,  Masaki Seto ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    IPC分类号： A61K31/4439 ,  A61K31/4178 ,  A61K31/40 ,  C07D403/02

    CPC分类号： C07D213/73

    摘要： 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.

    摘要翻译： 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＆lt; 5＆gt; 6＆lt; 6＆gt; 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。

    Bicyclic compound, production and use thereof
    5.
    发明授权
    Bicyclic compound, production and use thereof 有权
    双环化合物，其生产和使用

    公开(公告)号：US08741943B2

    公开(公告)日：2014-06-03

    申请号：US13476454

    申请日：2012-05-21

    申请人： Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Iizawa

    发明人： Mitsuru Shiraishi ,  Masanori Baba ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masaki Seto ,  Yuji Iizawa

    IPC分类号： C07D403/02 ,  A61K31/4178

    CPC分类号： A61K31/4196 ,  A61K31/395 ,  A61K31/4178 ,  C07D225/06 ,  C07D313/20 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12

    摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

    摘要翻译： 本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。 本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

    Tricyclic compound, process for producing the same, and use
    6.
    发明申请
    Tricyclic compound, process for producing the same, and use 审中-公开
    三环化合物，其制备方法和用途

    公开(公告)号：US20060178359A1

    公开(公告)日：2006-08-10

    申请号：US10544470

    申请日：2004-02-05

    申请人： Mitsuru Shiraishi ,  Masaki Seto ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    发明人： Mitsuru Shiraishi ,  Masaki Seto ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    IPC分类号： A61K31/55 ,  A61K31/4745 ,  C07D487/14

    CPC分类号： C07D471/04 ,  A61K31/4353 ,  A61K31/55

    摘要： 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.

    摘要翻译： 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。

    Fused-ring pyridine derivative, process for producing the same, and use
    9.
    发明申请
    Fused-ring pyridine derivative, process for producing the same, and use 失效
    稠环吡啶衍生物，其制备方法及用途

    公开(公告)号：US20060100197A1

    公开(公告)日：2006-05-11

    申请号：US10544435

    申请日：2004-02-05

    申请人： Mitsuru Shiraishi ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    发明人： Mitsuru Shiraishi ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    IPC分类号： A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4743 ,  A61K31/4741 ,  C07D498/02 ,  C07D491/02 ,  C07D471/02

    CPC分类号： A61K31/55 ,  C07D471/04

    摘要： 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.

    摘要翻译： 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。

    Fused-ring pyridine derivative, process for producing the same, and use
    10.
    发明授权
    Fused-ring pyridine derivative, process for producing the same, and use 失效
    稠环吡啶衍生物，其制备方法及用途

    公开(公告)号：US07288654B2

    公开(公告)日：2007-10-30

    申请号：US10544435

    申请日：2004-02-05

    申请人： Mitsuru Shiraishi ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    发明人： Mitsuru Shiraishi ,  Katsuji Aikawa ,  Naoyuki Kanzaki ,  Masanori Baba

    IPC分类号： C07D471/02

    CPC分类号： A61K31/55 ,  C07D471/04

    摘要： 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.

    摘要翻译： 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。