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48 条记录 (耗时 0.04 秒)

    Adenosine A3 receptor antagonists
    5.
    发明授权
    Adenosine A3 receptor antagonists 失效
    腺苷A3受体拮抗剂

    公开(公告)号：US06436966B1

    公开(公告)日：2002-08-20

    申请号：US09463639

    申请日：2000-01-27

    申请人： Shigenori Ohkawa ,  Hiroyuki Kimura ,  Naoyuki Kanzaki

    发明人： Shigenori Ohkawa ,  Hiroyuki Kimura ,  Naoyuki Kanzaki

    IPC分类号： A01N4340

    CPC分类号： A61K31/4439 ,  A61K31/4436

    摘要： A pharmaceutical composition for antagonizing adenosine at adenosine A3 receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.

    摘要翻译： 提供了一种用于拮抗腺苷A3受体上的腺苷的药物组合物，其包含通过可被取代的吡啶基在4-或5-位或两者取代的1,3-唑化合物，并且可用作预防和治疗 哮喘，过敏原，炎症等的代理。

    Bicyclic compound, production and use thereof
    6.
    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
    8.
    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。

    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof
    9.
    发明申请
    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效
    5-吡啶基-1,3-唑化合物，其制备方法及其用途

    公开(公告)号：US20060135566A1

    公开(公告)日：2006-06-22

    申请号：US11354897

    申请日：2006-02-16

    申请人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    发明人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    IPC分类号： A61K31/4439 ,  C07D417/04 ,  C07D413/04

    CPC分类号： C07D417/14 ,  C07D417/04

    摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

    摘要翻译： 由下式表示的任选的N-氧化化合物：其中R 1表示氢，烃，杂环，氨基，酰基，R 2表示芳族基团， 3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR 4表示的基团（R 4代表氢，烃或酰基），Z表示键或二价无环烃，或其盐具有优异的腺苷A 3受体拮抗活性，并用作 用于预防或治疗与腺苷A 3受体相关的疾病的药剂。 此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。