CZ20024235A3 - Substituované nitrované katecholy, jejich použití v léčbě některých chorobných stavů centrálního a periferního nervového systému a farmaceutické přípravky, které je obsahují - Google Patents

Substituované nitrované katecholy, jejich použití v léčbě některých chorobných stavů centrálního a periferního nervového systému a farmaceutické přípravky, které je obsahují Download PDF

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CZ20024235A3
CZ20024235A3 CZ20024235A CZ20024235A CZ20024235A3 CZ 20024235 A3 CZ20024235 A3 CZ 20024235A3 CZ 20024235 A CZ20024235 A CZ 20024235A CZ 20024235 A CZ20024235 A CZ 20024235A CZ 20024235 A3 CZ20024235 A3 CZ 20024235A3
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dihydroxy
nitrophenyl
nitro
group
compound
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David Alexander Learmonth
Da Silva Patricio Manuel Vieira Soares
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Portela & Ca Sa
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Claims (9)

  1. (sloučenina 17, tabulka 1).
    31 9 9 9· • · • · • 9 • · • · · · NÁROKY 9 ·· ···9 9 · · · 0 0 9 9 0 0 9 • · · · 9· · · ·· ··♦· 0 0 · • 0 9 9 9 9 9 9 9 · 0 09 99 P A Τ Ε N T 0 V É 1. Sloučenina vzorce I: T3 f4 rS Riv. XT JI J .0 i- kde Ri a I R2 j sou stejné nebo různé a znamenají atom vodíku, volitelně substituovanou nižší alkanoylovou skupinu nebo
    aroylovou skupinu, volitelně substituovanou nižší alkoxykarbonylovou skupinu nebo volitelně substituovanou nižší alkylkarbamoylovou skupinu, R3 znamená atom vodíku nebo volitelně substituovanou alkanoylovou skupinu nebo aroylovou skupinu, R4 znamená volitelně substituovanou saturovanou nebo částečně nesaturovanou nižší alkylovou skupinu nebo arylovou skupinu nebo společně s R3 znamená volitelně substituovaný saturovaný nebo částečně nesaturovaný karbocyklický kruh a znamená atom kyslíku nebo skupinu NR5, kde R5 znamená skupinu NHR6, kde R6 znamená volitelně substituovanou nižší alkylovou skupinu nebo arylovou skupinu nebo skupinu OR7, kde R7 znamená atom vodíku, nižší alkylovou skupinu nebo nižší alkanoylovou skupinu nebo A znamená volitelně substituovanou alkylidenovou skupinu, když R4 znamená skupinu ORs, kde Rg znamená volitelně substituovanou alkanoylovou skupinu nebo aroylovou skupinu, a její farmaceuticky přijatelné soli.
    • ···· ·· ···· ·· ···· • 9 9 · 9 · 9 · · • · · · · · · · · 9 • · ···· · · · · ···« ·· ·· ·· ··
  2. 2. Sloučenina podle nároku 1, kde R4 je substituovaný alespoň jednou arylovu skupinou nebo heterocykloalkylovou skupinou.
  3. 3. Sloučenina podle nároku 1, zahrnující:
    6,7-dihydroxy-8-nitro-3,4-dihydro-2H-naftalen-l-on,
    5.6- dihydroxy-7-nitroindan-l-on,
    2-(3,4-dimethoxybenzyliden)-6,7-dihydroxy-8-nitro-3,4-dihydro2H-naftalen~l-on, (3,4-dihydroxy-2-nitrofenyl)fenylmethanon,
    5.6- dihydroxy-7-nitroindan-l-on-oxim,
    2-(3,4-dimethoxybenzyliden)-5,6-dihydroxy-7-nitroindanon,
    2-(4-dimethylaminobenzyliden)-5,6-dihydroxy-7-nitroindan-l-on,
    2-(4-dimethylaminobenzyliden)-6,7-dihydroxy-8-nitro-3,4dihydro-2H-naftalen-l-on,
    5.6- dihydroxy-2-(4-hydroxy-3-methoxy-5-nitrobenzyliden)-7nitroindan-l-on,
    6.7- dihydroxy-2-(4-hydroxy-3-methoxy-5-nitrobenzyliden)-8nitro-3,4-dihydro-2H-naftalen-l-on,
    2- (3,4-dihydroxybenzyliden)-5,6-dihydroxy-7-nitroindan-l-on,
    2-(3,4-dihydroxybenzyliden)-6, 7-dihydroxy-8-nitro-3,4-dihydro2H-naftalen-l-on,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-fenylpropan-l-on,
    1- (3,4-dihydroxy-2-nitrofenyl)-4-fenylbutan-l-on,
    99 9 99 9
    2- (3,4-dihydroxy-5-nitrobenzyliden)-5,6-dihydroxy-7nitroindan-l-on,
    1- (3,4-dihydroxy-2-nitrofenyl)pentan-l-on,
    2,3-dihydroxy-l-nitroantrachinon,
    6-butyryloxy-2-nitro-3-(3-fenylpropionyl)fenylester máselné kyseliny,
    3- benzoyl-6-butyryloxy-2-nitrofenylester máselné kyseliny, 4benzoyl-2-ethoxycarbony)oxy-3-nitrofenylester ethylester uhličité kyseliny,
    2- ethoxykarbonyloxy-3-nitro-4-(3-fenylpropionyl)fenylester ethylester uhličité kyseliny,
  4. 4.5- dibenzoyl-2-ethoxykarbonyloxy-3-nitrofenylester ethylester uhličité kyseliny,
    1-(3, 4-dihydroxy-2-nitrofenyl)-2-fenylethanon,
    3- acetoxy-7,7-dimethyl-l-nitro-8-oxo-5,6,7,8-tetrahydronaftalen-2-ylester octové kyseliny,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-morfolin-4-ylpropan-l-on,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-piperidin-l-ylpropan-l-on,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-pyrolidin-l-ylpropan-l-on,
  5. 5.6- dihydroxy-2-morfolin-4-ylmethyl-7-nitroindan-l-on,
    Diethylamid 1-[3-(3,4-dihydroxy-2-nitrofenyl)-3-oxo-propyl]piperidin-3-karboxylové kyseliny,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-(3-methylpiperidin-lyl)propan-1-on,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-(4-methylpiperidin-lyl)propan-l-on, • ·· · ·· ·· ··· · • · · · · · · · · • · · 9 · · · · • · 9 9 9 9 9 9 9 9
    9 9 9 9 9 9 9 9 9 9
    999 9 90 99 90 99
    1-(3, 4-dihydroxy-2-nitrofenyl)-3-(oktahydrochinolin-1yl)propan-l-on,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-(3,5-dimethylpiperidin-lyl)propan-l-on,
    3-(4-benzylpiperidin-l-yl)-1-(3,4-dihydroxy-2-nitrofenyl)propan-l-on,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-[4-(4-methoxy-fenyl)piperazin-l-yl] propan-l-on,
    1- (3, 4-dihydroxy-2-nitrofenyl) -3- [4- (3-t.rifluormethylfenyl)piperazin-l-yl]propan-l-on,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-(4-propylpiperazin-lyl)propan-l-on,
  6. 6-acetoxy-2-nitro-3-(3-fenylakryloyl)fenylester octové kyseliny,
    1-(3,4-dihydroxy-2-nitrofenyl)-3-fenylpropenon,
    1- (3,4-dihydroxy-2-nitrofenyl)-2-morfolin-4-ylethanon,
    5.6- dihydroxy-7-nitro-2-[4-(3-trifluormethylfenyl)piperazin-1ylmethyl]indan-l-on,
    5.6- dihydroxy-7-nitro-2-(4-fenylpiperazin-l-ylmethyl)indan-lon,
    6-acetoxy-2-nitro-3-fenylacetylfenylester octové kyseliny,
    2- acetoxy-4-(l-acetoxy-2-fenylvinyl)-3-nitrofenylester octové kyseliny,
    6-butyryloxy-2-nitro-3-fenylacetylfenylester máselné kyseliny, 2-ethoxykarbonyloxy-3-nitro-4-fenylacetylfenylester ethylester uhličité kyseliny,
    6-acetoxy-2-nitro-3-(4-fenylbutyryl)fenylester octové ·· ··· · ·· · · · · · · · • · · · · · · · • · ··· ···· · • · · ♦ · · ···· ·· · · ·» ·· »♦ ♦♦ kyseliny,
    6-butyryloxy-2-nitro-3~(4-fenylbutynyl)fenylester máselné kyseliny nebo
    2-ethoxykarbonyloxy-3-nitro-4-(4-fenylbutynyl)fenylester ethylester uhličité kyseliny.
    4. Způsob léčení pacienta trpícího některým chorobným stavem centrálního a periferního nervového systému, kde může být terapeuticky výhodná redukce O-methylace katecholaminů, jako jsou například poruchy nálady, Parkinsonova nemoc a parkinsonský syndrom, gastrointestinální choroby, stavy vedoucí ke tvorbě edému a hypertenze, vyznačuj ící se t í m, že obsahuje podávání pacientovi množství sloučeniny podle nároku 1, 2 nebo 3 účinné pro léčbu nemocí pacienta.
    5. Farmaceutický přípravek vyznačující se tím, že obsahuje terapeuticky účinné množství sloučeniny podle nároku 1, 2 nebo 3, v kombinaci s farmaceuticky přijatelným nosičem.
    6. Použití sloučeniny podle nároku 1, 2 nebo 3 pro výrobu léku pro léčení pacienta trpícího chorobným stavem centrálního nebo periferního nervového systému.
    • ··*· ·♦ ···* »· ···· *· · · · · · · · • · · · * ···· · • · · · ♦ · · · · · ·· · < · · · · · · ·w
  7. 7. Použití sloučeniny podle nároku 1, 2 nebo 3 pro výrobu léku pro léčení poruch nálady, Parkinsonovy nemoci a parkinsonského syndromu, gastrointestinálních chorob, stavů vedoucích ke tvorbě edému a hypertenze.
  8. 8. Použití sloučeniny podle nároku 1, 2 nebo 3 při léčení.
  9. 9. Použití sloučeniny podle nároku 1, 2 nebo 3 pro výrobu léku pro použití jako inhibitor COMT.
CZ20024235A 2000-06-21 2001-06-21 Substituované nitrované katecholy, jejich použití v léčbě některých chorobných stavů centrálního a periferního nervového systému a farmaceutické přípravky, které je obsahují CZ20024235A3 (cs)

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MY148644A (en) * 2005-07-18 2013-05-15 Orion Corp New pharmaceutical compounds
GB0515327D0 (en) * 2005-07-26 2005-08-31 Portela & Ca Sa Comt inhibitors
RU2441001C2 (ru) * 2005-07-26 2012-01-27 Биал-Портела Энд Ка. С.А. Производные нитрокатехола в качестве ингибиторов сомт
JP5517453B2 (ja) * 2005-07-26 2014-06-11 ノヴィファーマ，エス．アー． Ｃｏｍｔ阻害剤
CA2729405C (en) * 2008-07-04 2016-08-02 Kissei Pharmaceutical Co., Ltd. Novel catechol derivative, pharmaceutical composition containing the same, use of the catechol derivative, and use of the pharmaceutical composition
JP5641494B2 (ja) * 2009-09-18 2014-12-17 株式会社Ｒｉｖｅｒｓｏｎ ポリフェノール誘導体及びそれの産生方法
CN102260239B (zh) * 2010-05-28 2014-10-08 暨南大学新药研究所 胡黄连素衍生物及其制备与应用
JP5883591B2 (ja) * 2010-08-06 2016-03-15 キッセイ薬品工業株式会社 新規なカテコール誘導体、それを含有する医薬組成物およびそれらの用途
TWI638802B (zh) 2012-05-24 2018-10-21 芬蘭商奧利安公司 兒茶酚ｏ－甲基轉移酶活性抑制化合物
CN110325508B (zh) 2017-01-20 2023-06-30 加利福尼亚大学董事会 雄激素受体的n-末端结构域的抑制剂
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