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

    Abstract: 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.

    Abstract translation: 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。

    Furan or thiopene derivative and medicinal use thereof
    2.
    发明申请
    Furan or thiopene derivative and medicinal use thereof 失效
    呋喃或噻吩衍生物及其医药用途

    公开(公告)号:US20060100261A1

    公开(公告)日:2006-05-11

    申请号:US10526507

    申请日:2003-09-04

    Abstract: The present invention provides a compound represented by the formula (I): [wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, p is 0, 1 or 2, and when p is 2, each R may be the same or different, R1 is a hydrogen atom or an optionally substituted hydrocarbon group, R2 is an optionally substituted aromatic group, Ring A is an optionally substituted monocyclic aromatic ring or optionally substituted bicyclic aromatic fused ring, X1 is an oxygen atom or a sulfur atom, X2 is a bond, an oxygen atom or —S(O)n— (wherein n is 0, 1 or 2), Y is a bond, an oxygen atom, —S(O)m—, —C(═O)—N(R3)— or —N(R3)—C(═O)— (R3 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, and m is 0, 1 or 2), M1, M2 and M3 may be the same or different and are each independently a bond or an optionally substituted divalent aliphatic hydrocarbon group, and M4 is an optionally substituted divalent aliphatic hydrocarbon group] or a salt thereof, which is useful as a prophylactic and/or therapeutic agent for lipid metabolism abnormality, arteriosclerotic disease and sequelae thereof, diabetes mellitus and the like.

    Abstract translation: 本发明提供由式(I)表示的化合物:[其中R是任选取代的烃基或任选取代的杂环基,p是0,1或2,当p是2时,每个R可以相同 或不同的R 1是氢原子或任选取代的烃基,R 2是任选取代的芳族基团,环A是任选取代的单环芳环或任选取代的芳环 取代的双环芳族稠合环,X 1是氧原子或硫原子,X 2是一个键,氧原子或-S(O)n (其中n为0,1或2),Y为键,氧原子,-S(O)m - , - C(-O)-N(R (O) - (R 3)是氢原子,任选取代的烃 基团或任选取代的杂环基,m为0,1或2),M 1,M 2和M 3可以是 相同或不同,各自独立 键或任选取代的二价脂族烃基,M 4是任选取代的二价脂族烃基]或其盐,其可用作脂质代谢异常的预防和/或治疗剂 ,动脉硬化疾病及其后遗症,糖尿病等。

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