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    FUSED HETEROCYCLIC COMPOUNDS AND MEDICINAL USES THEREOF
    2.
    发明申请
    FUSED HETEROCYCLIC COMPOUNDS AND MEDICINAL USES THEREOF 审中-公开
    熔融杂环化合物及其药物用途

    公开(公告)号：WO1997047601A1

    公开(公告)日：1997-12-18

    申请号：PCT/JP1997001993

    申请日：1997-06-09

    Applicant: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. ,  KUROITA, Takanobu ,  TOGO, Yoshifumi ,  ISHIBUCHI, Seigo ,  FUJIO, Masakazu ,  FUTAMURA, Takashi

    Inventor： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

    IPC: C07D215/46

    CPC classification number: C07D401/06 ,  C07D215/12 ,  C07D215/44 ,  C07D217/14 ,  C07D217/22 ,  C07D237/30 ,  C07D239/70 ,  C07D239/74 ,  C07D239/88 ,  C07D239/93 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

    Abstract: Fused heterocyclic compounds represented by general formula (I), optical isomers or pharmaceutically acceptable salts thereof, medicinal compositions comprising these compounds and pharmaceutically acceptable additives, and drugs comprising these compounds. These compounds exert more potent blocking effects on D4 receptors than on D2 receptors. Moreover, they have high affinities for receptors other than dopamine receptors such as muscarine M1, serotonin-2 (5-HT2) and adrenalin alpha 1 and alpha 2 receptors. Thus, these compounds are efficacious against not only positive symptoms typified by hallucination and delusion characteristic of the acute stage of schizophrenia but also negative symptoms such as emotional torpidity, abulia and autism. In addition, they are useful as antipsychotic agents with relieved side effects such as extrapyramidal symptoms and abnormal internal secretion observed in association with the administration of the conventional antipsychotic agents having only D2 receptor antagonism. The above compounds are usable as remedies for diseases such as schizophrenia.

    Abstract translation: 由通式（I）表示的稠合杂环化合物，光学异构体或其药学上可接受的盐，包含这些化合物的药物组合物和药学上可接受的添加剂，以及包含这些化合物的药物。 这些化合物对D4受体的作用比对D2受体有更强的阻断作用。 此外，它们对多巴胺受体（例如毒蕈碱M1，5-羟色胺-2（5-HT2））和肾上腺素α1和α2受体以外的受体具有高亲和力。 因此，这些化合物不仅有效地抵抗了精神分裂症急性期特征的幻觉和妄想，而且还包括阴性症状，如情绪反应，厌食和自闭症。 此外，它们可用作具有减轻的副作用的抗精神病药物，例如与仅具有D2受体拮抗作用的常规抗精神病药物的给药相关联的观察到锥体外系症状和异常内分泌。 上述化合物可用作精神分裂症等疾病的补救措施。

    FUSED HETEROCYCLIC COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF
    6.
    发明申请
    FUSED HETEROCYCLIC COMPOUNDS AND PHARMACEUTICAL APPLICATIONS THEREOF 审中-公开
    熔融杂环化合物及其药物应用

    公开(公告)号：WO1997032848A1

    公开(公告)日：1997-09-12

    申请号：PCT/JP1997000641

    申请日：1997-03-03

    Applicant: YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. ,  TANAKA, Hiroshi ,  KUROITA, Takanobu ,  TOGO, Yoshifumi ,  ISHIBUCHI, Seigo ,  FUJIO, Masakazu ,  FUTAMURA, Takashi

    Inventor： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.

    IPC: C07D209/14

    CPC classification number: C07D413/06 ,  C07D209/14 ,  C07D231/54 ,  C07D231/56 ,  C07D261/20 ,  C07D401/04 ,  C07D401/06 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

    Abstract: Fused heterocyclic compounds represented by general formula (I), wherein each symbol is as defined in the description, optical isomers thereof, or pharmaceutically acceptable salts thereof; pharmaceutical compositions containing the compounds of formula (I), the optical isomers or pharmaceutically acceptable salts thereof, and pharmaceutically acceptable additives; and medicines containing the compounds of formula (I), the optical isomers thereof, or the pharmaceutically acceptable salts thereof. These compounds are useful antipsychotic agents efficacious against not only positive symptoms centering on the hallucination, delusion and the like peculiar to the acute stage of schizophrenia, but also negative symptoms such as emotional torpidity, abulia and autism. They are also expected as highly safe antipsychotic agents reduced in the side effects, such as extrapyramidal symptoms or abnormal internal secretion, observed in the case of administration of conventional antipsychotic agents having D2 receptor blocking effects. Thus these compounds can be used as remedies for diseases including schizophrenia.

    Abstract translation: 由通式（I）表示的稠合杂环化合物，其中每个符号如说明书中所定义，其光学异构体或其药学上可接受的盐; 含有式（I）化合物的药物组合物，其光学异构体或其药学上可接受的盐和药学上可接受的添加剂; 和含有式（I）化合物的药物，其光学异构体或其药学上可接受的盐。 这些化合物是有用的抗精神病药物，不仅有针对精神分裂症急性期特有的幻觉，妄想等症状的积极症状，而且还包括阴性症状，如情绪抑郁，腹部和自闭症。 也预期在施用具有D2受体阻断作用的常规抗精神病药的情况下观察到，高度安全的抗精神病药降低了副作用，如锥体外系症状或异常内分泌。 因此，这些化合物可用作包括精神分裂症在内的疾病的补救措施。

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