Amine compounds, their production and use
    1.
    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

    IPC分类号: A01N4342

    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。

    Quinoline compound
    5.
    发明授权
    Quinoline compound 失效
    喹啉化合物

    公开(公告)号:US07183415B2

    公开(公告)日:2007-02-27

    申请号:US10493427

    申请日:2002-10-24

    IPC分类号: C07D215/38 C07D215/14

    摘要: A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Ar is a cyclic group optionally having substituent(s); X is a bond or a spacer having a main chain of 1 to 6 atoms; R1 and R2 are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s); Y is a divalent hydrocarbon group optionally having substituent(s) (except CO); R3 is a hydrogen atom or a hydrocarbon group optionally having substituent(s); and ring A and ring B may further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.

    摘要翻译: 一种化合物,其具有黑色素浓集激素拮抗作用并且可用作预防或治疗肥胖症的药剂,并且其由下式表示:其中Ar是任选具有取代基的环状基团; X是具有1至6个原子的主链的键或间隔基; R 1和R 2相同或不同,各自为氢原子或任选具有取代基的烃基,或R 1〜 >和R 2可以与相邻的氮原子一起形成任选具有取代基的含氮杂环; Y是任选具有取代基(CO除外)的二价烃基; R 3是氢原子或任选具有取代基的烃基; 并且环A和环B可以进一步具有取代基,并且当环B还具有取代基时,取代基可以与R 1连接形成环,或其盐或其前药, 被提供。

    Indole derivatives as somatostatin agonists or antagonists
    7.
    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

    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
    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

    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。

    Amine derivative
    9.
    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

    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。