首页> 外国专利> New 9-alkyl-beta-carboline compounds are dopamine receptor stimulators useful to treat and/or prevent movement disorder, Alzheimer's disease, Parkinson's disease and Wilson's diseases, and as additives for accelerating cell growth

New 9-alkyl-beta-carboline compounds are dopamine receptor stimulators useful to treat and/or prevent movement disorder, Alzheimer's disease, Parkinson's disease and Wilson's diseases, and as additives for accelerating cell growth

机译:新的9-烷基-β-咔啉化合物是多巴胺受体刺激剂,可用于治疗和/或预防运动障碍,阿尔茨海默氏病,帕金森氏病和威尔逊氏病,并作为促进细胞生长的添加剂

摘要

9-Alkyl-beta -carboline compounds (I) and their salts, solvates, hydrates, complex compounds, enantiomers, diastereomers and racemates, are new. 9-Alkyl-beta -carboline compounds of formula (I) and their salts, solvates, hydrates, complex compounds, enantiomers, diastereomers and racemates, are new. R 1-R 16, -CR 4R 5R 6, -X-CR 4R 5R 6, -X-R 4, -CO-NH-R 16, -CO-O-R 16; R 2, R 3-H, -R 7, -R 8, -CR 9R 10R 11, -CR 12R 13R 14, -Y 1-CR 9R 10R 11, -Z-CR 12R 13R 14, -Y 1-R 15, -Z-R 15, -O-R 17, -S-R 18, -NH-R 19, -CO-NH-R 20 or -CO-O-R 21; X : -(CH 2) n-, -CH=CH-, -C?=C-, -CH 2-CO-, -CO- or -CO-CH 2-; Y 1, Z : -(CH 2) m-, -CH=CH-, -C?=C-, -O-(CH 2) p-, -NH-(CH 2) q-, -NH-CO-, -CO- or -O-CO-; R 4-R 15e.g. -H, -OH, -OCH 3, -OC 2H 5, -OC 3H 7, -O-cyclo-C 3H 5, -OCH(CH 3)2, -OC(CH 3) 3, -OC 4H 9, -OPh, -OCH 2-Ph, -OCPh 3, -SH, -SCH 3, -SC 2H 5, -SC 3H 7, -S-cyclo-C 3H 5, -SCH(CH 3) 2, -SC(CH 3) 3, -NO 2, -F, -Cl, -Br, -I, -N 3, -CN, -OCN, -NCO, -SCN, -NCS, -CHO, -COCH 3, -COC 2H 5 or -COC 3H 7; R 4-R 21-CH 2F, -CHF 2, -CF 3, -CH 2Cl, -CH 2Br, -CH 2I, -CH 2-CH 2F, -CH 2-CHF 2, -CH 2-CF 3, -CH 2-CH 2Cl, -CH 2-CH 2Br, -CH 2-CH 2I, cyclo-C 3H 5, cyclo-C 4H 7, cyclo-C 5H 9, cyclo-C 6H 11, cyclo-C 7H 13 or cyclo-C 8H 15; m, p, q : 1-4; and n : 1-6. Full Definitions are given in the Definitions (Full Definitions) section. An independent claim is included for a pharmaceutical composition comprising (I) and/or its salt, a carrier, an auxiliary material and/or a solvent. [Image] ACTIVITY : Antiparkinsonian; Neuroprotective; Nootropic; Antimicrobial; Antithyroid; Endocrine-Gen; Cytostatic; Cerebroprotective; Cardiant; Anticonvulsant; Muscular-Gen; Gastrointestinal-gen.; CNS-gen. The neuroprotective effect of (I) was tested in central brain cells. The results showed that after 48 hours, in a control culture about 20% of the cells were killed and in a culture with 9-alkyl-beta -carboline only about 10% of the cells were killed. MECHANISM OF ACTION : Dopamine receptor stimulator.
机译:9-烷基-β-咔啉化合物(I)及其盐,溶剂化物,水合物,复杂化合物,对映异构体,非对映异构体和外消旋体是新的。式(I)的9-烷基-β-咔啉化合物及其盐,溶剂化物,水合物,络合物,对映异构体,非对映异构体和外消旋体是新的。 R 1> -R 16>,-CR 4> R 5> R 6>,-X-CR 4> R 5> R 6>,-XR 4>,-CO-NH-R 16>,-CO-OR 16>; R 2>,R 3> -H,-R 7>,-R 8>,-CR 9> R 10> R 11>,-CR 12> R 13> R 14>,-Y 1> -CR 9> R 10> R 11>,-Z-CR 12> R 13> R 14>,-Y 1> -R 15>,-ZR 15>,-OR 17>,-SR 18>,-NH-R 19> ,-CO-NH-R 20>或-CO-OR 21>; X :-( CH 2)n-,-CH = CH-,-C 2 = C-,-CH 2 -CO-,-CO-或-CO-CH 2-; Y 1>,Z :-( CH 2)m-,-CH = CH-,-C′= C-,-O-(CH 2)p-,-NH-(CH 2)q-,-NH- CO-,-CO-或-O-CO-; R 4> -R 15>例如-H,-OH,-OCH 3,-OC 2H 5,-OC 3H 7,-O-cyclo-C 3H 5,-OCH(CH 3)2,-OC(CH 3)3,-OC 4H 9, -OPh,-OCH 2-Ph,-OCPh 3,-SH,-SCH 3,-SC 2H 5,-SC 3H 7,-S-cyclo-C 3H 5,-SCH(CH 3)2,-SC( CH 3)3,-NO 2--F,-Cl,-Br,-I,-N 3,-CN,-OCN,-NCO,-SCN,-NCS,-CHO,-COCH 3,-COC 2H 5或-COC 3H 7; R 4> -R 21> -CH 2F,-CHF 2,-CF 3,-CH 2Cl,-CH 2Br,-CH 2I,-CH 2-CH 2F,-CH 2-CHF 2,-CH 2-CF 3,-CH 2 -CH 2Cl,-CH 2 -CH 2Br,-CH 2 -CH 2I,环C 3H 5,环C 4H 7,环C 5H 9,环C 6H 11,环C 7H 13或cyclo-C 8H 15; m,p,q:1-4; n:1-6。完整定义在“定义(完整定义)”部分给出。对包含(I)和/或其盐,载体,辅助材料和/或溶剂的药物组合物包括独立权利要求。活动:Antiparkinsonian;具有神经保护作用;促智;抗菌;抗甲状腺;内分泌基因细胞抑制脑保护卡迪恩抗惊厥药;肌肉型胃肠道CNS-gen。 (I)的神经保护作用在中枢脑细胞中进行了测试。结果表明,在48小时后,在对照培养物中约20%的细胞被杀死,而在具有9-烷基-β-咔啉的培养物中仅约10%的细胞被杀死。作用机理:多巴胺受体刺激剂。

著录项

  • 公开/公告号DE102007009264A1

    专利类型

  • 公开/公告日2008-08-28

    原文格式PDF

  • 申请/专利权人 ELLNEUROXX LTD.;

    申请/专利号DE20071009264

  • 发明设计人 ROMMELSPACHER HANS;

    申请日2007-02-26

  • 分类号C07D471/04;A61K31/437;A61P25/14;C12N5/06;C12N5/08;

  • 国家 DE

  • 入库时间 2022-08-21 19:49:22

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