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    BENZODIAZEPINE DERIVATIVES, AS CCK AND GASTRIN ANTAGONISTS
    6.
    发明申请
    BENZODIAZEPINE DERIVATIVES, AS CCK AND GASTRIN ANTAGONISTS 审中-公开
    苯并噻唑衍生物，作为CCK和GASTRIN拮抗剂

    公开(公告)号：WO1993017011A1

    公开(公告)日：1993-09-02

    申请号：PCT/GB1993000299

    申请日：1993-02-12

    Applicant: MERCK SHARP & DOHME LIMITED ,  CHAMBERS, Mark, Stuart ,  FLETCHER, Stephen, Robert ,  MATASSA, Victor, Giulio

    Inventor： MERCK SHARP & DOHME LIMITED

    IPC: C07D403/12

    CPC classification number: C07D403/12 ,  C07D243/14

    Abstract: Compounds of formula (I), and salts and prodrugs thereof wherein: R is H, certain optionally substituted C1-6alkyl, or C3-7cycloalkyl; R is (CH2)q-tetrazolyl optionally substituted in the tetrazole ring by C1-4alkyl, (CH2)q-imidazolyl (where q is 0, 1, 2 or 3), CONHSO2R , SO2NHCOR (where R is C1-6alkyl, optionally substituted aryl or trifluoromethyl), SO2NHR (where R is a nitrogen containing heterocycle), cyclopropyl or (CH2)nCO2H, where n is 1 or 2; R is C1-6alkyl, halo or NR R ; R is C1-7 straight or branched chain alkyl; and x is 0, 1, 2 or 3; are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.

    Abstract translation: 式（I）化合物及其盐和前药其中：R 1是H，某些任选取代的C 1-6烷基或C 3-7环烷基; （CH 2）q-咪唑基（其中q为0,1,2或3），CONHSO 2 R 9，SO 2 NHCOR 9，（CH 2）q - 四唑基， （其中R 9为C 1-6烷基，任选取代的芳基或三氟甲基），SO 2 NHR 10（其中R 10为含氮杂环），环丙基或（CH 2）n CO 2 H，其中n为1或2; R 3是C 1-6烷基，卤素或NR 6 R 7; R 4是C 1-7直链或支链烷基; x为0,1,2或3; 是CCK和/或胃泌素受体拮抗剂。 它们及其组合物可用于治疗。

    SUBSTITUTED QUINOLINE-4-CARBOXYLIC HYDRAZIDES AS NK-2/NK-3 RECEPTOR LIGANDS
    10.
    发明申请
    SUBSTITUTED QUINOLINE-4-CARBOXYLIC HYDRAZIDES AS NK-2/NK-3 RECEPTOR LIGANDS 审中-公开
    作为NK-2 / NK-3受体配体的取代的喹啉-4-羧氧基水杨酸

    公开(公告)号：WO2004072045A1

    公开(公告)日：2004-08-26

    申请号：PCT/GB2004/000415

    申请日：2004-02-03

    Applicant: MERCK SHARP & DOHME LIMITED ,  CHAMBERS, Mark, Stuart ,  JONES, Philip ,  MACLEOD, Angus, Murray

    Inventor： CHAMBERS, Mark, Stuart ,  JONES, Philip ,  MACLEOD, Angus, Murray

    IPC: C07D215/52

    CPC classification number: C07D215/52

    Abstract: The present invention discloses a compound of formula (I): wherein: R 1 is an aryl or heteroaryl ring; R 2 is hydroxy, C 1-6 alkoxy, C 1-6 alkyl, amino, NR'R" or C 1-6 alkyl-NR'R" where R' and R" are independently chosen from hydrogen and C 1-4 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 R 2 is C 1-6 alkoxy substituted by NR'R" as defined above; R 3 is hydrogen or C 1-6 alkyl; R 4 is hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, aryl or aryl C 1-6 alkyl; R 5 is hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 3-8 cycloalkyl, aryl, aryl C 1-6 alkyl or C 1-6 alkoxycarbonyl; or R 4 and R 5 , together with the nitrogen atom to which they are attached, form a C 3 -C 10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF 3 , halogen and C 1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.

    Abstract translation: 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， 其中R'和R“与它们所连接的氮原子一起形成任选地含有另外的氮原子并且任选被如上定义的NR'R”所取代的饱和含氮3-7元杂环或R 2 >如上定义的被NR'R“取代的C 1-6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 3-8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。

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