RU2010138410A - Производные ретиналя и способы их применения для лечения нарушений зрения - Google Patents
Производные ретиналя и способы их применения для лечения нарушений зрения Download PDFInfo
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Abstract
1. Фармацевтическая композиция, восстанавливающая зрительный пигмент при недостаточности эндогенного 11-цис-ретиналя, содержащая эффективное количество производного ретиналя и фармацевтически приемлемый носитель, ! где производное ретиналя преобразовывается в ретиналь, способный формировать функциональный комплекс опсин/ретиналь, ! где производное ретиналя представляет собой сложный эфир 9-цис-ретинила формулы I ! ! сложный эфир 11-цис-ретинила формулы II ! ! или их комбинацию, ! где А означает CH2OR и R представляет собой карбоксилатный радикал монокарбоновой кислоты C1-C10 или поликарбоновой кислоты C3-C22. ! 2. Фармацевтическая композиция по п.1, составленная в виде офтальмологической композиции в офтальмологически приемлемом носителе. ! 3. Фармацевтическая композиция по п.1, составленная в виде композиции для перорального приема. ! 4. Фармацевтическая композиция по п.1, где композиция составлена для введения в виде глазных капель, раствора для внутриглазной инъекции или раствора для окологлазной инъекции. ! 5. Фармацевтическая композиция по любому из пп.1-4, где недостаточность эндогенного 11-цис-ретиналя имеет место у человека. ! 6. Способ восстановления фоторецепторной функции или ослабления потери фоторецепторной функции при недостаточности эндогенного 11-цис-ретиналя, предусматривающий введение эффективного количества производного ретиналя в качестве активного ингредиента, ! где производное ретиналя преобразовывается в ретиналь, способный формировать функциональный комплекс опсин/ретиналь, ! где производное ретиналя представляет собой сложный эфир 9-цис-ретинила формулы I ! ! сложный эфир 11-цис-ретинила
Claims (18)
1. Фармацевтическая композиция, восстанавливающая зрительный пигмент при недостаточности эндогенного 11-цис-ретиналя, содержащая эффективное количество производного ретиналя и фармацевтически приемлемый носитель,
где производное ретиналя преобразовывается в ретиналь, способный формировать функциональный комплекс опсин/ретиналь,
где производное ретиналя представляет собой сложный эфир 9-цис-ретинила формулы I
сложный эфир 11-цис-ретинила формулы II
или их комбинацию,
где А означает CH2OR и R представляет собой карбоксилатный радикал монокарбоновой кислоты C1-C10 или поликарбоновой кислоты C3-C22.
2. Фармацевтическая композиция по п.1, составленная в виде офтальмологической композиции в офтальмологически приемлемом носителе.
3. Фармацевтическая композиция по п.1, составленная в виде композиции для перорального приема.
4. Фармацевтическая композиция по п.1, где композиция составлена для введения в виде глазных капель, раствора для внутриглазной инъекции или раствора для окологлазной инъекции.
5. Фармацевтическая композиция по любому из пп.1-4, где недостаточность эндогенного 11-цис-ретиналя имеет место у человека.
6. Способ восстановления фоторецепторной функции или ослабления потери фоторецепторной функции при недостаточности эндогенного 11-цис-ретиналя, предусматривающий введение эффективного количества производного ретиналя в качестве активного ингредиента,
где производное ретиналя преобразовывается в ретиналь, способный формировать функциональный комплекс опсин/ретиналь,
где производное ретиналя представляет собой сложный эфир 9-цис-ретинила формулы I
сложный эфир 11-цис-ретинила формулы II
или их комбинацию,
где А означает CH2OR и R представляет собой карбоксилатный радикал монокарбоновой кислоты C1-C10 или поликарбоновой кислоты C3-C22.
7. Способ по п.6, где недостаточность эндогенного 11-цис-ретиналя связана с дегенерацией желтого пятна, связанной с возрастом, врожденным амаврозом Лебера (LCA), белоточечным ретинитом, врожденной стационарной ночной слепотой или белоточечным глазным дном.
8. Способ по п.6 или 7, где функциональный комплекс опсин/ретиналь устраняет необходимость в эндогенном 11-цис-ретинале.
9. Способ по п.6 или 7, где недостаточность эндогенного 11-цис-ретиналя имеет место в случае потери способности ночного зрения или потери контрастной чувствительности, или в случае пожилого возраста пациента.
10. Способ по п.9, где сложный эфир ретиналя формулируют для профилактического введения.
11. Применение производного ретиналя для приготовления лекарственного средства для применения в случае недостаточности эндогенного 11-цис-ретиналя в глазу, где производное ретиналя представляет собой сложный эфир 9-цис-ретинила формулы I
сложный эфир 11-цис-ретинила формулы II
или их комбинацию,
где А означает CH2OR и R представляет собой карбоксилатный радикал монокарбоновой кислоты C1-C10 или поликарбоновой кислоты C3-C22.
12. Применение по п.11, где производное ретиналя обеспечивает восстановление фоторецепторной функции.
13. Применение по п.11 или 12, где производное ретиналя обеспечивает ослабление потери фоторецепторной функции.
14. Применение по п.11 или 12, где недостаточность эндогенного 11-цис-ретиналя имеет место в случае дегенерации желтого пятна, связанной с возрастом, врожденного амавроза Лебера (LCA), белоточечного ретинита, врожденного стационарной ночной слепоты или белоточечного глазного дна.
15. Применение по п.11 или 12, где производное ретиналя устраняет необходимость в эндогенном 11-цис-ретинале.
16. Применение по п.11 или 12, где производное ретиналя преобразуется в ретиналь, связывающий свободный опсин в глазу пациента.
17. Применение по п.11 или 12, где недостаточность эндогенного 11-цис-ретиналя имеет место в случае потери способности ночного зрения или потери контрастной чувствительности или в случае пожилого возраста пациента.
18. Применение по п.17, где лекарственное средство формулируют для профилактического введения.
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| RU2010138410/04A RU2554003C2 (ru) | 2004-06-18 | 2005-06-20 | Производные ретиналя и способы их применения для лечения нарушений зрения |
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| US20060281821A1 (en) * | 2003-03-14 | 2006-12-14 | Krzysztof Palczewski | Retinoid replacements and opsin agonists and methods for the use thereof |
| EP2397132B1 (en) | 2004-06-18 | 2017-07-26 | University of Washington | Retinal derivatives and methods for the use thereof for the treatment of visual disorders |
| CA2569691C (en) | 2004-06-23 | 2010-08-17 | Sirion Therapeutics, Inc. | Methods and compositions for treating ophthalmic conditions with retinyl derivatives |
| CN101129344A (zh) * | 2004-12-08 | 2008-02-27 | 西来昂诊疗公司 | 治疗与视黄醇有关的疾病的方法、分析和组合物 |
| EP2069390A4 (en) * | 2006-07-27 | 2009-12-30 | Univ Florida | OPSIN STABILIZING COMPOUNDS AND METHODS OF USE |
| EP2069391A4 (en) * | 2006-07-27 | 2009-12-30 | Univ Florida | COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING EYE DRYING |
| WO2008063768A2 (en) * | 2006-10-12 | 2008-05-29 | Case Western Reserve University | Compositions and methods for treating metabolic diseases |
| US20090170841A1 (en) * | 2007-04-20 | 2009-07-02 | Acucela Inc. | Styrenyl Derivative Compounds for Treating Ophthalmic Diseases and Disorders |
| CN101969938A (zh) * | 2008-02-11 | 2011-02-09 | 华盛顿大学 | 治疗和预防年龄相关视网膜功能障碍的方法 |
| AU2015200520B2 (en) * | 2008-02-11 | 2017-02-09 | University Of Washington | Methods for the treatment and prevention of age-related retinal dysfunction |
| JP5443470B2 (ja) * | 2008-04-29 | 2014-03-19 | 株式会社日健総本社 | 眼障害の治療方法 |
| IN2012DN00352A (ru) | 2009-06-16 | 2015-08-21 | Bikam Pharmaceuticals Inc | |
| AU2009352678B2 (en) | 2009-09-15 | 2015-05-21 | Eluminex Biosciences (Suzhou) Limited | Pharmaceutical formulations comprising 9-cis-retinyl esters in a lipid vehicle |
| AU2010328186B2 (en) | 2009-12-08 | 2014-12-18 | Case Western Reserve University | Compounds and methods of treating ocular disorders |
| US8889660B2 (en) | 2010-01-20 | 2014-11-18 | Case Western Reserve University | Methods for treating obesity or an obesity related condition |
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