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4-Piperidinyl indole derivs. - with dopaminergic activity e.g. for treating Parkinsons disease and excessive prolactin secretion

机译:4-哌啶基吲哚衍生物。 -具有多巴胺能活性,例如治疗帕金森病和催乳素分泌过多

摘要

Indole derivs. of formula (I), within the general scope of the parent patent, and their acid addn. salts are new. (X is methyl and Y is 3-piperidinyl (cpd. Ia) or 1-propyl-3-piperidinyl (Ib); or X is H and Y is 1-ethyl-3-piperidinyl (Ic) or 1-ethyl-1,2,5,6-tetrahydro-3-pyridinyl (Id)). Specificed salts are the hydrochloride of (Ia); the oxalate of (Ib); the neutral fumarate of (Ic) and the phosphate of (Id). (I) are useful as dopaminergic stimulants; some also have adrenergic and serotoninergic activities. They are useful for treating extrapyramidal neurological disorders (e.g. Parkinson's disease); excessive secretion of prolactin (e.g. hypogonadism); cerebral senescence; vertebrobasal insufficiency; arterial hypertension; peripheral circulator disorders; and arteriopathy of the legs. All cpds. were tolerated at doses of 60 mg or more per kg, intraperitoneally in mice, without any deaths.
机译:吲哚衍生。在母专利的一般范围内的式(I)的化合物及其酸加成。盐是新的。 (X为甲基,Y为3-哌啶基(cpd.aa)或1-丙基-3-哌啶基(Ib);或X为H且Y为1-乙基-3-哌啶基(Ic)或1-乙基-1 ,2,5,6-四氢-3-吡啶基(Id))。具体的盐是(Ia)的盐酸盐。 (Ib)的草酸盐; (Ic)的中性富马酸酯和(Id)的磷酸盐。 (I)可用作多巴胺能兴奋剂;一些还具有肾上腺素能和5-羟色胺能活性。它们可用于治疗锥体束外神经系统疾病(例如帕金森氏病);催乳素分泌过多(例如性腺机能减退);脑衰老椎基底不全;动脉高血压;周围循环系统疾病;和腿的动脉病。所有cpds。小鼠腹膜内耐受的剂量为每公斤60 mg或更高,没有死亡。

著录项

  • 公开/公告号FR2492824B2

    专利类型

  • 公开/公告日1983-01-14

    原文格式PDF

  • 申请/专利权人 ROUSSEL UCLAF;

    申请/专利号FR19800022819

  • 发明设计人

    申请日1980-10-24

  • 分类号C07D401/10;A61K31/435;

  • 国家 FR

  • 入库时间 2022-08-22 10:01:12

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