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D1 dopamine receptor agonist compounds, pharmaceutical composition and their use
D1 dopamine receptor agonist compounds, pharmaceutical composition and their use
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机译:D1多巴胺受体激动剂化合物,药物组合物及其用途
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摘要
Invention Patent: "DOPAMINE D1 RECEPTOR AGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND ITS USE". The invention provides 2,3,4,5-tetrahydro-1H-3-benzazepines of general formula (I) in which: R ^ 1 ^ is hydrogen, halogen, C ~ 1 ~ -C ~ 4 ~ alkyl, or CF ~ 3 ~; R ^ 2 ^ is hydrogen, methyl, or lower alkenyl of 3 to 5 carbon atoms; R ^ 3 ^ and R ^ 4 ^ together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane or cyclohexane ring and R ^ 5 ~ is hydrogen or R ^ 4 ^ and R ^ 5 ~ together form a furan, dihydrofuran ring , thiophene, dihydrothiophene, cyclopentane or cyclohexane and R ^ 3 ^ is hydrogen; R ^ 6 ^ is hydrogen, halogen, CF ~ 3 ~, CN, N0 ~ 2 ~ or NH ~ 2 ~; R ^ 7 ^ is hydrogen, halogen, CF ~ 3 ~, CN, NO ~ 2 ~ or NH ~ 2 ~. The specific combination of substituents: R ~ 1 ~ = H, R ~ 2 ~ = H and R ~ 4 ~ and R ~ 5 ~ together forming a cyclohexane ring is excluded, namely 1- (5,6,7,8 -tetrahydronaphthalen-2-yl) - 2,3,4,5-tetrahydro-1 H -benzo [d] azepine-7,8-diol. The compounds of the invention provide therapeutic agents that selectively interact positively with postsynaptic dopamine D1 receptors in the striatum, directly or indirectly (called dopamine D1 agonists) and are particularly valuable as anti-Parkinsonian agents.
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机译:发明专利:“多巴胺D1受体激动剂化合物,药物组合物及其用途”。本发明提供了通式(I)的2,3,4,5-四氢-1H-3-苯并ze庚因,其中:R ^ 1 ^是氢,卤素,C〜1〜-C〜4〜烷基或CF〜 3〜; R ^ 2 ^为氢,甲基或3至5个碳原子的低级烯基; R ^ 3 ^和R ^ 4 ^一起形成呋喃,二氢呋喃,噻吩,二氢噻吩,环戊烷或环己烷环,R ^ 5〜为氢或R ^ 4 ^和R ^ 5〜一起形成呋喃,二氢呋喃环,噻吩,二氢噻吩,环戊烷或环己烷,R ^ 3 ^为氢; R ^ 6 ^是氢,卤素,CF〜3〜,CN,N0〜2〜或NH〜2〜; R ^ 7 ^是氢,卤素,CF〜3〜,CN,NO〜2〜或NH〜2〜。取代基的特定组合:R〜1〜= H,R〜2〜= H和R〜4〜和R〜5〜一起形成环己烷环,即1-(5,6,7,8-四氢萘-2-基)-2,3,4,5-四氢-1 H-苯并[d]氮杂7,8-二醇。本发明的化合物提供了治疗剂,其直接或间接地与纹状体中的突触后多巴胺D1受体选择性地正相互作用(称为多巴胺D1激动剂),并且作为抗帕金森氏剂特别有价值。
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