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30 条记录 (耗时 0.039 秒)

    Bicyclic Compound, Production and Use Thereof
    4.
    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。

    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。

    Acrylamide derivative, process for producing the same, and use
    7.
    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。

    Tricyclic compound, process for producing the same, and use
    9.
    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。

    Anilide derivative, production and use thereof
    10.
    发明授权
    Anilide derivative, production and use thereof 失效
    苯胺衍生物，生产和使用

    公开(公告)号：US06235771B1

    公开(公告)日：2001-05-22

    申请号：US09463924

    申请日：2000-03-27

    申请人： Mitsuru Shiraishi ,  Masanori Baba ,  Masaki Seto ,  Naoyuki Kanzaki ,  Osamu Nishimura

    发明人： Mitsuru Shiraishi ,  Masanori Baba ,  Masaki Seto ,  Naoyuki Kanzaki ,  Osamu Nishimura

    IPC分类号： A61K3138

    CPC分类号： C07D335/06 ,  A61K31/495 ,  A61K31/52 ,  A61K31/535 ,  A61K31/55 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K45/06 ,  C07D337/08 ,  C07D409/12 ,  C07D409/14 ,  C07F9/655372 ,  C07F9/65539 ,  A61K2300/00

    摘要： This invention is to provide a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula:  wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5 and R6 are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5 and R6 may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof , which is useful for antagonizing CCR5 and also for the prevention and treatment of infectious disease of HIV.

    摘要翻译： 本发明提供下式化合物：其中R 1为任选取代的5至6元环; 环A是任选取代的6至7元环; 环B是任选取代的苯环; n为1或2的整数; Z是化学键或二价基团; R2是（1）其中氮原子可以形成季铵的任选取代的氨基，（2）可以含有硫原子或氧原子作为构成原子的环的任选取代的含氮杂环基，其中 氮原子可以形成季铵，（3）通过硫原子结合的基团或（4）下式的基团：其中k为0或1，当k为0时，磷原子可以形成鏻; R 5和R 6各自独立地为任选取代的烃基，任选取代的羟基或任选取代的氨基，并且R 5和R 6可以彼此结合形成环状基团以及相邻的磷原子或其盐， 其可用于拮抗CCR5以及用于预防和治疗HIV感染性疾病。