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49 条记录 (耗时 0.066 秒)

    Biaryl compound and use thereof
    1.
    发明授权
    Biaryl compound and use thereof 失效
    双芳基化合物及其用途

    公开(公告)号：US07507753B2

    公开(公告)日：2009-03-24

    申请号：US10499903

    申请日：2002-12-26

    申请人： Nobuo Cho ,  Kazuyoshi Aso ,  Satoshi Endo ,  Naoyuki Kanzaki ,  Satoshi Sasaki

    发明人： Nobuo Cho ,  Kazuyoshi Aso ,  Satoshi Endo ,  Naoyuki Kanzaki ,  Satoshi Sasaki

    IPC分类号： A61K31/445 ,  C07D211/58

    CPC分类号： C07D401/06 ,  C07D211/58 ,  C07D401/12 ,  C07D405/06

    摘要： The present invention provides a compound having melanocortin receptor agonist activity or antagonist activity, which is a novel biaryl compound represented by the formula (I): wherein ring A and ring B are optionally further substituted 6-membered aromatic rings; X is —CONR4—, —SO2NR4—, —CH2NR4— (R4 is a hydrogen atom, an optionally substituted hydrocarbon group, etc.), etc.; Y is a spacer having 1 to 12 atoms, etc.; Z is —CONR6—, —CO— (R6 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group), etc.; R1 is an optionally substituted amino group, etc.; R2 is an optionally substituted hydrocarbon group, etc.; R3 is an optionally substituted hydrocarbon group, etc.; and R5 is an optionally substituted hydrocarbon group, etc.; or a salt thereof.

    摘要翻译： 本发明提供具有黑皮质素受体激动剂活性或拮抗剂活性的化合物，其为由式（I）表示的新型联芳基化合物：其中环A和环B任选进一步被取代的6元芳环; X是-CONR 4 - ，-SO 2 NR 4 - ， - CH 2 NR 4 - （R 4是氢原子，任选取代的烃基等）等; Y为1〜12个原子的间隔基等。 Z是-CONR 6 - ，-CO-（R 6是氢原子，任选取代的烃基或任选取代的杂环基）等; R1是任选取代的氨基等; R2是任选取代的烃基等; R3是任选取代的烃基等; R5是任意取代的烃基等; 或其盐。

    Receptor antagonist
    3.
    发明申请
    Receptor antagonist 审中-公开
    受体拮抗剂

    公开(公告)号：US20070117840A1

    公开(公告)日：2007-05-24

    申请号：US10549889

    申请日：2004-03-16

    申请人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Yoshihiro Banno ,  Hiromi Yoshida ,  Hirokazu Matsumoto

    发明人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Yoshihiro Banno ,  Hiromi Yoshida ,  Hirokazu Matsumoto

    IPC分类号： A61K31/4704

    CPC分类号： A61K31/4704

    摘要： A compound represented by the formula (I): wherein ring A represents an aromatic ring; X represents a bond, oxygen, NR4 (R4 represents hydrogen, a hydrocarbon group, or a heterocyclic group), or alkylene; R1 represents a hydrocarbon group, or a heterocyclic group; R2 represents —COYR5 (Y represents a bond, alkylene, oxygen, sulfur, or NR6 (R6 represents hydrogen, a hydrocarbon group, or a heterocyclic group), and R5 represents a hydrocarbon group, or a heterocyclic group), a hydrocarbon group, or a heterocyclic group; and R3 represents a hydrocarbon group, a heterocyclic group, optionally substituted hydroxy, optionally substituted amino, or —S(O)nR7 (R7 represents a hydrocarbon group, or a heterocyclic group, and n is 0 to 2), a salt of the compound, or a prodrug or either is useful as an agent for modulating the function of an RFRP receptor.

    摘要翻译： 由式（I）表示的化合物：其中环A表示芳环; X表示键，氧，NR 4（R 4表示氢，烃基或杂环基）或亚烷基; R 1表示烃基或杂环基; R 2表示-COYR 5（Y表示键，亚烷基，氧，硫或NR 6（R 6） SUP>表示氢，烃基或杂环基），R 5表示烃基或杂环基），烃基或杂环基; 和R 3表示烃基，杂环基，任选取代的羟基，任选取代的氨基或-S（O）n R 7 （R 7表示烃基或杂环基，n为0〜2），化合物或前药的盐或其可用作调节其功能的试剂 RFRP受体。

    Fused-ring pyridine derivative, process for producing the same, and use
    8.
    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。

    Benzazepine derivatives, process for the preparation of the same and uses thereof
    9.
    发明授权
    Benzazepine derivatives, process for the preparation of the same and uses thereof 失效
    苯并氮杂衍生物，其制备方法及其用途

    公开(公告)号：US06936602B1

    公开(公告)日：2005-08-30

    申请号：US10018321

    申请日：2000-06-15

    申请人： Mitsuru Shiraishi ,  Masanori Baba ,  Yoshio Aramaki ,  Naoyuki Kanzaki ,  Osamu Nishimura

    发明人： Mitsuru Shiraishi ,  Masanori Baba ,  Yoshio Aramaki ,  Naoyuki Kanzaki ,  Osamu Nishimura

    IPC分类号： A61P31/18 ,  A61P43/00 ,  C07D223/16 ,  C07D405/12 ,  A61K31/55 ,  A61P31/00

    CPC分类号： C07D223/16 ,  C07D405/12

    摘要： Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R1 is a 5- to 6-membered aromatic ring which bears a substituent represented by the general formula: R-Z1-X-Z2- (wherein R1 is hydrogen or optionally substituted hydrocarbyl; X is optionally substituted alkylene; and Z1 and Z2 are each a heteroatom) and may be further substituted, with R being optionally bonded to the aromatic ring to form another ring; Y is optionally substituted imino; and R2 and R3 are each optionally substituted aliphatic hydrocarbyl or an optionally Substituted hetero-alicyclic group.

    摘要翻译： 具有CCR5拮抗作用并对HIV感染发挥预防和治疗作用的通式（I）的化合物或其盐：其中R 1是5至6元芳环，其带有 由以下通式表示的取代基：RZ 1 - ZZ 2 - （其中R 1是氢或任选取代的烃基; X是任选取代的亚烷基 ; Z 1和Z 2各自为杂原子），并且可以进一步被取代，其中R任选地与芳环键合形成另一个环; Y是任选取代的亚氨基; R 2和R 3各自为任选取代的脂族烃基或任选取代的杂脂环基团。