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13 条记录 (耗时 0.038 秒)

    Indole derivatives as somatostatin agonists or antagonists
    1.
    发明申请
    Indole derivatives as somatostatin agonists or antagonists 审中-公开
    吲哚衍生物作为生长抑素激动剂或拮抗剂

    公开(公告)号：US20060223826A1

    公开(公告)日：2006-10-05

    申请号：US10534725

    申请日：2003-11-18

    申请人： Hidenori Abe ,  Shinichiro Matsunaga ,  Shiro Takekawa ,  Masanori Watanabe

    发明人： Hidenori Abe ,  Shinichiro Matsunaga ,  Shiro Takekawa ,  Masanori Watanabe

    IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D403/02

    CPC分类号： C07D401/12 ,  C07D209/20 ,  C07D209/42 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04

    摘要： The present invention provide a compound of the formula (I) wherein ring A represents an aromatic ring optionally having substituents; B, Y and Ya are the same or different and each represents a bond, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrogen atom, etc.; R4 and R5 are the same or different and each represents a hydrogen, etc.; R6 represents an indolyl group optionally having substituents; and Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibition activity and is useful for preventing and/or treating diseases associated with somatostatin.

    摘要翻译： 本发明提供式（I）的化合物，其中环A表示任选具有取代基的芳环; B，Y和Ya是相同或不同的，每个代表一个债券等; R 1和R 2相同或不同，各自表示氢原子等; R 3表示氢原子等; R 4和R 5相同或不同，各自表示氢等; R 6表示任选具有取代基的吲哚基; Z和Za相同或不同，各自表示氢原子等; 或其盐或其前药，具有生长抑素受体结合抑制活性，并且可用于预防和/或治疗与生长抑素相关的疾病。

    Amine derivative
    2.
    发明申请
    Amine derivative 审中-公开
    胺衍生物

    公开(公告)号：US20050245571A1

    公开(公告)日：2005-11-03

    申请号：US10492420

    申请日：2002-10-17

    申请人： Hidenori Abe ,  Shizuo Kasai ,  Shiro Takekawa ,  Masanori Watanabe

    发明人： Hidenori Abe ,  Shizuo Kasai ,  Shiro Takekawa ,  Masanori Watanabe

    IPC分类号： A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61P3/10 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  C07D43/14

    CPC分类号： A61K31/496 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D401/06 ,  C07D401/14

    摘要： The present invention provide a compound of the formula: wherein X and X′ are the same or different and each represents a hydrogen atom, etc.; R1 and R2 are the same or different and each represents a hydrogen atom, etc.; R3 represents a hydrocarbon group optionally having substituents, etc.; R4 represents a hydrogen atom, etc.; Y and Ya are the same or different and each represents a bond or a spacer having a main chain of 1 to 8 atoms; Z and Za are the same or different and each represents a hydrogen atom, etc.; or a salt thereof or a prodrug thereof, having a somatostatin receptor binding inhibitory activity and is useful for preventing and/or treating diseases associated with somatostatin.

    摘要翻译： 本发明提供下式的化合物：其中X和X'相同或不同，各自表示氢原子等; R 1和R 2相同或不同，各自表示氢原子等; R 3表示任选具有取代基的烃基等; R 4表示氢原子等; Y和Ya相同或不同，各自表示键或具有1至8个原子的主链的间隔基; Z和Za相同或不同，各自表示氢原子等; 或其盐或其前药，具有生长抑素受体结合抑制活性，并且可用于预防和/或治疗与生长抑素相关的疾病。

    Amine compounds, their production and use
    4.
    发明授权
    Amine compounds, their production and use 失效
    胺化合物，其生产和使用

    公开(公告)号：US06329389B1

    公开(公告)日：2001-12-11

    申请号：US09424285

    申请日：1999-11-19

    申请人： Nobuhiro Suzuki ,  Kaneyoshi Kato ,  Shiro Takekawa ,  Jun Terauchi ,  Satoshi Endo

    发明人： Nobuhiro Suzuki ,  Kaneyoshi Kato ,  Shiro Takekawa ,  Jun Terauchi ,  Satoshi Endo

    IPC分类号： A01N4342

    CPC分类号： C07D401/06 ,  C07D215/12 ,  C07D215/18 ,  C07D215/20 ,  C07D215/38 ,  C07D215/58 ,  C07D241/42 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D409/10 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/10

    摘要： The present invention provides a compound of the formula: wherein Ar represents an aromatic group which may be substituted; X represents methylene, S, SO, SO2 or CO; Y represents a spacer having a main chain of 2 to 5 atoms; n represents an integer of 1 to 5; i) R1 and R2 each represents a hydrogen atom or a lower alkyl which may be substituted, ii) R1 and R2 form, taken together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring which may be substituted, or iii) R1 or R2 together with —(CH2)n—N═ form, bonded to a component atom of Ring B, a spiro-ring which may be substituted; Ring A represents an aromatic ring which may be substituted; Ring B represents a 4- to 7-membered nitrogen-containing non-aromatic ring which may be further substituted by alkyl or acyl, with a proviso that X represents S, SO, SO2 or CO when Ring A has as a substituent a group represented by the formula: —NHCOR11 where R11 represents alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or a group represented by the formula: —NHR12 where R12 represents alkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, or a salt thereof; which has an excellent somatostatin receptor binding inhibition action.

    摘要翻译： 本发明提供下式的化合物：其中Ar表示可被取代的芳族基团; X表示亚甲基，S，SO，SO 2或CO; Y表示主链为2至5个原子的间隔基; n表示 1至5的整数; i）R 1和R 2各自表示氢原子或可被取代的低级烷基，ii）R 1和R 2与相邻的氮原子一起形成可被取代的含氮杂环 ，oriii）R1或R2与 - （CH2）nN =形成键合，键合到环B的组分原子，可被取代的螺环;环A表示可被取代的芳环;环B表示4 - 可以进一步被烷基或酰基取代的7-元含氮非芳香环，条件是当环A具有由下式表示的基团作为取代基时，X表示S，SO，SO 2或CO：其中 R11表示烷基，烷氧基烷基，烷硫基烷基，环烷基，环烷基烷基，芳基，芳基 烷基或由下式表示的基团：其中R 12表示烷基，环烷基，环烷基烷基，芳基或芳基烷基或其盐; 其具有优异的生长抑素受体结合抑制作用。

    Antiobestic agents methods for screening antiobestic agents and kits comprising same
    6.
    发明授权
    Antiobestic agents methods for screening antiobestic agents and kits comprising same 失效
    用于筛选抗生物剂的抗生物剂方法和包含其的试剂盒

    公开(公告)号：US06991908B1

    公开(公告)日：2006-01-31

    申请号：US09869540

    申请日：1999-12-27

    申请人： Masaaki Mori ,  Yukio Shimomura ,  Shiro Takekawa ,  Tsukasa Sugo ,  Yoshihiro Ishibashi ,  Chieko Kitada ,  Nobuhiro Suzuki

    发明人： Masaaki Mori ,  Yukio Shimomura ,  Shiro Takekawa ,  Tsukasa Sugo ,  Yoshihiro Ishibashi ,  Chieko Kitada ,  Nobuhiro Suzuki

    IPC分类号： G01N33/53

    CPC分类号： C07K7/08 ,  A61K38/10 ,  G01N33/74 ,  G01N2333/575 ,  G01N2333/726 ,  G01N2500/00 ,  G01N2500/02 ,  Y10S436/808

    摘要： The present invention provides a method for screening a compound or its salt that alters the binding property between MCH or its salt and SLC-1 or its salt, characterized by using MCH or its derivative or a salt thereof and SLC-1 or its salt is useful for screening an SLC-1 agonist which can be used not only as an appetite (eating) promoting agent but also as a prophylactic/therapeutic agent for weak pains, atonic bleeding, before and after expulsion, subinvolution of uterus, cesarean section, induced abortion, galactostasis, and the like, and an SLC-1 antagonist which can be used not only as an antiobestic agents (drug), an appetite (eating) modulator, and the like, but also as a prophylactic/therapeutic agent for hyperstimulation, ankylosing uterine contractions, fetal distress, uterine rupture, cervical laceration, preterm delivery, Prader-Wili syndrome and the like.

    摘要翻译： 本发明提供一种筛选化合物或其盐的方法，其改变MCH或其盐与SLC-1或其盐之间的结合性质，其特征在于使用MCH或其衍生物或其盐，SLC-1或其盐是 可用于筛选SLC-1激动剂，其不仅可以用作食欲（进食）促进剂，而且可用作弱疼痛，无症状出血，驱除前后，子宫切除，剖宫产，诱导 流产，半乳糖淀粉酶等，以及不仅可以用作抗生素（药物），食欲调节剂等的SLC-1拮抗剂，而且可以用作过度刺激的预防/治疗剂， 强直性子宫收缩，胎儿窘迫，子宫破裂，子宫颈撕裂，早产，Prader-Wili综合征等。

    Amine derivative
    8.
    发明申请
    Amine derivative 失效
    胺衍生物

    公开(公告)号：US20060128690A1

    公开(公告)日：2006-06-15

    申请号：US10545120

    申请日：2004-02-12

    申请人： Yuji Ishihara ,  Makoto Kamata ,  Shiro Takekawa

    发明人： Yuji Ishihara ,  Makoto Kamata ,  Shiro Takekawa

    IPC分类号： A61K31/55 ,  A61K31/401 ,  A61K31/445

    CPC分类号： C07D211/16 ,  A61K31/55 ,  C07C233/73 ,  C07C235/42 ,  C07D207/09 ,  C07D207/12 ,  C07D211/14 ,  C07D213/82 ,  C07D233/24 ,  C07D295/135

    摘要： The present invention provides a compound represented by the formula wherein Ar1 is a cyclic group optionally having substituent(s); R is a hydrogen atom, an optionally halogenated C1-6 alkyl, a phenyl optionally having substituent(s) or a pyridyl optionally having substituent(s); Ra1, Ra2, Ra3 and Ra4 are the same or different and each is a hydrogen atom, an optionally halogenated C1-6 alkyl or the like; Ar is a monocyclic aromatic ring optionally having substituent(s); Y is an optionally halogenated alkylene group; and R1 and R2 are (1) the same or different and each is a hydrogen atom or a C1-6 alkyl, (2) R1 and R2 form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, or (3) R1 and Y form a nitrogen-containing heterocycle optionally having substituent(s) together with the adjacent nitrogen atom, and R2 is a hydrogen atom or a C1-6 alkyl; provided that when the nitrogen-containing heterocycle formed by R1 and R2 together with the adjacent nitrogen atom is a piperazine, or when R is a C1-4 alkyl, Ar1 is a cyclic group having substituent(s), or a salt thereof, having a melanin-concentrating hormone antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like.

    摘要翻译： 本发明提供由下式表示的化合物：其中Ar 1是任选具有取代基的环状基团; R是氢原子，任选卤代的C 1-6烷基，任选具有取代基的苯基或任选具有取代基的吡啶基; Ra 1，R 2，R 3，R 3和R 4相同或不同，各自为氢原子 ，任选卤代的C 1-6烷基等; Ar是任选具有取代基的单环芳环; Y是任选卤代的亚烷基; 且R 1和R 2均为（1）相同或不同，并且各自为氢原子或C 1-6烷基，（ 2）R 1和R 2 2形成任选具有取代基的氮杂环与相邻的氮原子，或（3）R 1， Y和Y形成任选具有取代基的氮杂环与相邻的氮原子一起形成，R 2是氢原子或C 1-6 烷基; 条件是当由R 1和R 2与相邻氮原子一起形成的含氮杂环是哌嗪时，或当R是C 1〜 4个烷基，Ar 1是具有取代基的环状基团或其盐，其具有黑色素浓缩激素拮抗作用并且可用作预防或治疗的药剂 肥胖等。