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    Substituted quinoline-4-carboxylic hydrazides as nk-2/nk-3 receptor ligands
    9.
    发明申请
    Substituted quinoline-4-carboxylic hydrazides as nk-2/nk-3 receptor ligands 失效
    取代的喹啉-4-羧酸酰肼作为nk-2 / nk-3受体配体

    公开(公告)号：US20060089348A1

    公开(公告)日：2006-04-27

    申请号：US10544440

    申请日：2004-02-03

    申请人： Mark Chambers ,  Philip Jones ,  Angus MacLeod

    发明人： Mark Chambers ,  Philip Jones ,  Angus MacLeod

    IPC分类号： A61K31/55 ,  A61K31/47 ,  A61K31/496 ,  C07D215/38 ,  C07D403/02

    CPC分类号： C07D215/52

    摘要： The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR′R″ or C1-6 alkyl-NR′R″ where R′ and R″ are independently chosen from hydrogen and C1-4 alkyl and where R′ and R″, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR′R″ as defined above or R2 is C1-6 alkoxy substituted by NR′R″ as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.

    摘要翻译： 本发明公开了式（I）的化合物：其中：R 1是芳基或杂芳基环; R 2是羟基，C 1-6烷氧基，C 1-6烷基，氨基，NR'R“或C” 1-6烷基-NR'R“，其中R'和R”独立地选自氢和C 1-4烷基，并且其中R'和R“与 它们所连接的氮原子形成饱和的含氮3-7元杂环，其任选地含有另外的氮原子，并且任选地被如上所定义的NR'R“或R 2取代为C 被如上所定义的NR'R“取代的1-6位的烷氧基; R 3是氢或C 1-6烷基; R 4是氢，C 1-8 - 烷基，C 2-8 - 烯基，C 2-8 - 炔基 C 3-8环烷基，芳基或芳基C 1-6烷基; R 5是氢，C 1-8 - 烷基，C 2-8 - 烯基，C 2-8 - 炔基 C 3 -C 8环烷基，芳基，芳基C 1-6烷基或C 1-6烷氧基羰基; 或R 4和R 5与它们所连接的氮原子一起形成C 3 -C 10烷基， / SUB单环或双环饱和环; X和Y独立地选自氢，羟基，硝基，氨基，氰基，CF 3，卤素和C 1-4烷基; 或其药学上可接受的盐; 作为用于治疗精神分裂症，COPD，哮喘或肠易激综合征的NK-2 / NK-3配体。