Heterocyclic tachykinin receptor antagonists
    1.
    发明公开
    Heterocyclic tachykinin receptor antagonists 失效
    Heterozyklische Tachykinin-Rezeptorantagonisten

    公开(公告)号:EP0714891A1

    公开(公告)日:1996-06-05

    申请号:EP95308164.3

    申请日:1995-11-14

    摘要: This invention provides a novel series substituted piperidines, pyrrolidines, and hexamethyleneimines which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds. The compounds have the formula

    wherein:
       p is 1, 2, or 3;
       m and n are independently 0-6;
       X is




            N-R a , or CH-NR b R c ,


       where R a , R b , and R c are independently selected from the group consisting of hydrogen and C 1 -C 6 alkyl;
       R 1 and R 2 are independently hydrogen, halo, trifluoromethyl, trichloromethyl, C 1 -C 6 alkyl, or C 1 -C 6 alkoxy; and
       R 3 , R 4 , and R 5 are independently selected from the group consisting of hydrogen, halo, trifluoromethyl, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, cyano, hydroxy, amino, -NHCONH 2 , nitro, -CONH 2 , C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkenyl, C 3 -C 8 cycloalkoxy, C 1 -C 10 alkylthio, C 1 -C 10 alkylamino, C 2 -C 6 alkanoyl, and C 2 -C 6 alkanoyloxy;
    or a pharmaceutically acceptable salt or solvate thereof.

    摘要翻译: 本发明提供了一种新颖的系列取代的哌啶,吡咯烷和六亚甲基亚胺,其可用于治疗或预防与超速激肽相关的生理障碍。 本发明还提供了治疗这种生理疾病的方法以及采用这些新化合物的药物制剂。 化合物具有式CHEM,其中:p为1,2或3; m和n独立地为0-6; X是 NR a或CH-NR b R c,其中R a,R b和R c独立地选自 由氢和C 1 -C 6烷基组成; R 1和R 2独立地是氢,卤素,三氟甲基,三氯甲基,C 1 -C 6烷基或C 1 -C 6烷氧基; R 3,R 4和R 5独立地选自氢,卤素,三氟甲基,C 1 -C 6烷基,C 1 -C 6烷氧基,氰基,羟基,氨基,-NHCONH 2,硝基 ,-CONH 2,C 2 -C 10烯基,C 2 -C 10炔基,C 3 -C 8环烷基,C 3 -C 8环烯基,C 3 -C 8环烷氧基,C 1 -C 10烷硫基,C 1 -C 10烷基氨基,C 2 -C 6烷酰基和C 2 -C 6烷酰氧基; 或其药学上可接受的盐或溶剂合物。

    2-Acylaminopropanamides as growth hormone secretagogues
    3.
    发明公开
    2-Acylaminopropanamides as growth hormone secretagogues 失效
    2-酰基氨基丙酰胺zurFörderungder Wachstumshormon-Sekretion

    公开(公告)号:EP0761220A1

    公开(公告)日:1997-03-12

    申请号:EP96305929.0

    申请日:1996-08-14

    IPC分类号: A61K31/445 A61K31/495

    摘要: This invention provides a series of substituted propanamides which are useful in the treatment of a physiological condition which may be modulated by an increase in growth hormone. This invention also provides methods for the treatment of such physiological conditions which comprise administering a growth hormone secretagogue as described in the present invention in combination with growth hormone releasing hormone.

    摘要翻译: 本发明提供一系列取代的丙酰胺,其可用于治疗可通过生长激素增加而调节的生理状态。 本发明还提供了治疗这种生理条件的方法,其包括与生长激素释放激素组合施用本发明所述的生长激素促分泌素。

    1-Aryl-2-acetylamidopentanone derivatives for use as tachykinin receptor antagonists
    10.
    发明公开
    1-Aryl-2-acetylamidopentanone derivatives for use as tachykinin receptor antagonists 失效
    1-芳基-2-乙酰氨基戊酸 - 衍生物zur Verwendung als速激肽受体激动剂

    公开(公告)号:EP0699674A1

    公开(公告)日:1996-03-06

    申请号:EP95305084.6

    申请日:1995-07-20

    CPC分类号: C07D209/16

    摘要: This invention provides a novel series of the formula I substituted 1-aryl-2-acetamidopentanone derivatives which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.

    摘要翻译: 本发明提供了一种新型的式I取代的1-芳基-2-乙酰氨基戊酮衍生物,其可用于治疗或预防与超速激肽相关的生理障碍。 本发明还提供了治疗这种生理疾病的方法以及采用这些新化合物的药物制剂。