首页> 外国专利> Substituted 1,2,3,4-tetrahydro-1H-pyrido 4,3-b indoles and 1,2,3,4,5,6-hexahydro-azepino 4,3-b indol-drug substances, pharmaceutical compositions, methods for their preparation and use for treating neurodegenerative diseases and cognitive disorders

Substituted 1,2,3,4-tetrahydro-1H-pyrido 4,3-b indoles and 1,2,3,4,5,6-hexahydro-azepino 4,3-b indol-drug substances, pharmaceutical compositions, methods for their preparation and use for treating neurodegenerative diseases and cognitive disorders

机译:取代了1,2,3,4-四氢-1H-吡啶并[4,3-b]吲哚和1,2,3,4,5,6-六氢-氮杂环庚烷[4,3-b]吲哚药物,药物组合物,其制备方法以及用于治疗神经退行性疾病和认知障碍的方法

摘要

1. Medicinal substance possessing neurotrophic activity of the α-adrenoceptors, dopamine D serotonin receptors and CNS general formula 1 in the form of the free base (or acid) or in the form of pharmaceutically acceptable salts and / or hydrates, for pharmaceutical compositions and dosage forms intended for the treatment and / or prevention of neurodegenerative diseases and cognitive disorders. ! ! wherein R1 is an amino substituent, including a hydrogen atom, an optionally substituted C1-C4 alkyl, acyl, alkoxy, heterocyclyl, substituted sulfonyl; ! R2 represents a substituent of cyclic system, including a hydrogen atom, a halogen atom, an optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulfonyl; ! Ar represents optionally substituted aryl or optionally substituted heterocyclyl; ! Alk represents an optionally substituted C1-S3alkandiil, C2-S3alkendiil, C2-S4alkindiil or SO2 group; ! n = 1 or 2; ! solid line with its accompanying a broken line () represents a single or double bond. ! 2. Drug Substance according to claim 1, characterized in that the spectrum of receptor-specific agonsticheskoy and / or antagonistic activity includes activity to α1A, α1B, α1D, α2A adrenoceptors, dopamine D1, D2L, D2S, D3 and D4.2 receptors and serotonin 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 receptors. ! 3. Medicinal substance according to claim 1, characterized in that the spectrum of receptor-specific agonistic and / or antagonistic activity can also include some other receptors such as histamine H1,
机译:1.具有α-肾上腺素能受体,多巴胺D血清素受体和CNS通式1的神经营养活性的药物,其呈游离碱(或酸)形式或药学上可接受的盐和/或水合物形式,用于药物组合物和用于治疗和/或预防神经退行性疾病和认知障碍的剂型。 ! !其中R1为氨基取代基,包括氢原子,任选取代的C1-C4烷基,酰基,烷氧基,杂环基,取代的磺酰基; ! R2代表环状系统的取代基,包括氢原子,卤素原子,任选取代的C1-C4烷基,CF3,CN,烷氧基,烷氧基羰基,羧基,杂环基或取代的磺酰基; ! Ar表示任选取代的芳基或任选取代的杂环基; ! Alk表示任选取代的C 1 -S 3链烷二烷基,C 2 -S 3链烷二基,C 2 -S 4链烷二基或SO 2基团; ! n = 1或2; !实线及其随附的虚线()表示单键或双键。 ! 2.根据权利要求1的药物,其特征在于受体特异性激动和/或拮抗活性的谱包括对α1A,α1B,α1D,α2A肾上腺素能受体,多巴胺D1,D2L,D2S,D3和D4.2受体的活性。血清素5-HT2A,5-HT2B,5-HT2C,5-HT6和5-HT7受体。 ! 3.根据权利要求1的药用物质,其特征在于受体特异性激动和/或拮抗活性的光谱还可以包括一些其他受体,例如组胺H1,

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号