RU2013115635A - Способы получения и использования ингибитора sglt2 - Google Patents
Способы получения и использования ингибитора sglt2 Download PDFInfo
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- SCXDLEDWPGORNG-SONWIMMPSA-N CCOc1ccc(Cc(cc([C@@H](C2)O[C@H](COC(C)=O)C[C@@H]2OC(C)=O)cc2)c2Cl)cc1 Chemical compound CCOc1ccc(Cc(cc([C@@H](C2)O[C@H](COC(C)=O)C[C@@H]2OC(C)=O)cc2)c2Cl)cc1 SCXDLEDWPGORNG-SONWIMMPSA-N 0.000 description 1
- FKECIHAYTCUJBW-HFSMHLIXSA-N CCOc1ccc(Cc2cc([C@@H](C3)O[C@H](CO)C[C@@H]3O)ccc2Cl)cc1 Chemical compound CCOc1ccc(Cc2cc([C@@H](C3)O[C@H](CO)C[C@@H]3O)ccc2Cl)cc1 FKECIHAYTCUJBW-HFSMHLIXSA-N 0.000 description 1
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Abstract
1. Способ лечения или замедления прогрессирования или начала диабета, диабетической ретинопатии, диабетической нейропатии, диабетической нефропатии, медленного заживления ран, инсулиновой резистентности, гипергликемии, гиперинсулинемии, повышенных уровней жирных кислот или глицерина в крови, гиперлипидемии, ожирения, гипертриглицеридемии, Синдрома X, осложнений диабета, атеросклероза или гипертензии, или повышения в крови уровней липопротеинов высокой плотности, включающий введение млекопитающим, нуждающимся в лечении, терапевтически эффективного количества соединения, имеющего структуру,или его фармацевтически приемлемой соли, стереоизомера или сложного эфира, представляющего собой пролекарство.2. Способ по п.1, в котором соединение имеет структуру.3. Способ лечения диабета 2-го типа, включающий введение млекопитающим, нуждающимся в лечении, терапевтически эффективного количества соединения, имеющего структуру,или его фармацевтически приемлемой соли, стереоизомера или сложного эфира, представляющего собой пролекарство, отдельно или в комбинации с другим антидиабетическим средством, средством для лечения осложнений диабета, средством против ожирения, антигипертензивным средством, антитромбоцитарным средством, антиатеросклеротическим средством и/или гиполипидемическим средством.4. Способ по п.3, в котором соединение вводят отдельно.5. Способ по п.3, в котором соединение вводят в комбинации с другим антидиабетическим средством.6. Способ по п.5, в котором антидиабетическое средство представляет собой 1, 2, 3 или более из бигуанида, сульфонилмочевины, ингибитора глюкозидазы, PRAR γ агониста, PRAR α/γ двойног�
Claims (27)
1. Способ лечения или замедления прогрессирования или начала диабета, диабетической ретинопатии, диабетической нейропатии, диабетической нефропатии, медленного заживления ран, инсулиновой резистентности, гипергликемии, гиперинсулинемии, повышенных уровней жирных кислот или глицерина в крови, гиперлипидемии, ожирения, гипертриглицеридемии, Синдрома X, осложнений диабета, атеросклероза или гипертензии, или повышения в крови уровней липопротеинов высокой плотности, включающий введение млекопитающим, нуждающимся в лечении, терапевтически эффективного количества соединения, имеющего структуру
или его фармацевтически приемлемой соли, стереоизомера или сложного эфира, представляющего собой пролекарство.
3. Способ лечения диабета 2-го типа, включающий введение млекопитающим, нуждающимся в лечении, терапевтически эффективного количества соединения, имеющего структуру
или его фармацевтически приемлемой соли, стереоизомера или сложного эфира, представляющего собой пролекарство, отдельно или в комбинации с другим антидиабетическим средством, средством для лечения осложнений диабета, средством против ожирения, антигипертензивным средством, антитромбоцитарным средством, антиатеросклеротическим средством и/или гиполипидемическим средством.
4. Способ по п.3, в котором соединение вводят отдельно.
5. Способ по п.3, в котором соединение вводят в комбинации с другим антидиабетическим средством.
6. Способ по п.5, в котором антидиабетическое средство представляет собой 1, 2, 3 или более из бигуанида, сульфонилмочевины, ингибитора глюкозидазы, PRAR γ агониста, PRAR α/γ двойного агониста, ингибитора аР2, ингибитора DP4, сенсибилизатора инсулина, глюкагоноподобного пептида-1 (GLP-1), инсулина, меглитинида, ингибитора РТР1В, ингибитора гликоген-фосфорилазы и/или ингибитора глюкозо-6-фосфатазы.
7. Способ по п.5, в котором антидиабетическое средство представляет собой 1, 2, 3 или более из метформина, глибурида, глимепирида, глипирида, глипизида, хлорпропамида, гликлазида, акарбозы, миглитола, пиоглитазона, троглитазона, розиглитазона, инсулина, G1-262570, изаглитазона, JTT-501, NN-2344, L895645, YM-440, R-119702, AJ9677, репаглинида, натеглинида, KAD1129, AR-HO39242, GW-409544, KRP297, АС2993, LY315902 и/или NVP-DPP-728A.
8. Способ по п.5, в котором соединение и антидиабетическое средство вводят в весовом соотношении, находящемся в пределах от приблизительно 0.01:1 до приблизительно 300:1.
9. Способ по п.3, в котором соединение вводят в комбинации со средством для лечения ожирения.
10. Способ по п.9, в котором средство для лечения ожирения представляет собой агонист бета-3-адренергических рецепторов, ингибитор липазы, ингибитор обратного захвата серотонина (и допамина), средство для воздействия на бета-рецепторы щитовидной железы, и/или аноректическое средство.
11. Способ по п.9, в котором средство для лечения ожирения представляет собой орлистат, ATL-962, AJ9677, L750355, СР331648, сибутрамин, топирамат, аксокин, дексамфетамин, фентермин, фенилпропаноламин, и/или мазиндол.
12. Способ по п.3, в котором соединение вводят в комбинации с гиполипидемическим средством.
13. Способ по п.12, в котором гиполипидемическое средство представляет собой ингибитор МРТ, ингибитор ГМГ-КоА редуктазы, ингибитор сквален-синтетазы, производное фиброевой кислоты, регулятор активности рецепторов ЛПНП, ингибитор липоксигеназы или ингибитор АЛАТ.
14. Способ по п.12, в котором гиполипидемическое средство представляет собой правастатин, ловастатин, симвастатин, аторвастатин, церивастатин, флувастатин, нисвастатин, визастатин, атавастатин, розувастатин, фенофибрат, гемфиброзил, клофибрат, авазимиб, TS-962, MD-700 и/или LY295427.
17. Способ по п.16, в котором основание представляет собой LiOH или NaOH.
18. Способ по п.16 или 17, в котором обработку проводят в растворителе, выбранном из группы, состоящей из смеси Н2О/THF/МеОН в соотношении 1:2:3, водного метанола и водного этанола.
21. Способ по п.20, в котором обработку уксусным ангидридом осуществляют в CH2Cl2 в присутствии пиридина и диметиламинопиридина.
23. Способ по п.22, в котором восстанавливающий агент представляет собой Et3SiH, и реакцию проводят в присутствии кислого катализатора Льюиса.
24. Способ по п.23, в котором кислый катализатор Льюиса представляет собой BF3·Et2O.
26. Способ по п.25, в котором ацетилирование осуществляют в толуоле или CH2Cl2, содержащем основание Хьюнига или Et3N и диметиламинопиридин.
27. Способ по п.24 или 25, в котором восстанавливающий агент представляет собой Et3SiH, и восстановление осуществляют в MeCN, содержащем 1 эквивалент Н2О и BF3·Et2O.
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Application Number | Priority Date | Filing Date | Title |
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US10/151,436 US6515117B2 (en) | 1999-10-12 | 2002-05-20 | C-aryl glucoside SGLT2 inhibitors and method |
US10/151,436 | 2002-05-20 |
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RU2008122558A Division RU2489151C3 (ru) | 2002-05-20 | 2008-06-06 | Фармацевтическая комбинация, содержащая ингибитор sglt2 |
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RU2017131447A Division RU2017131447A (ru) | 2002-05-20 | 2017-09-07 | Способы получения и использования ингибитора sglt2 |
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RU2013115635A true RU2013115635A (ru) | 2014-10-20 |
RU2643764C2 RU2643764C2 (ru) | 2018-02-05 |
RU2643764C9 RU2643764C9 (ru) | 2021-12-15 |
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RU2004137489/04A RU2337916C2 (ru) | 2002-05-20 | 2003-05-15 | C-арил глюкозидные sglt2 ингибиторы и способ их применения |
RU2008122558A RU2489151C3 (ru) | 2002-05-20 | 2008-06-06 | Фармацевтическая комбинация, содержащая ингибитор sglt2 |
RU2013115635A RU2643764C9 (ru) | 2002-05-20 | 2013-04-08 | Способы получения и использования ингибитора sglt2 |
RU2017131447A RU2017131447A (ru) | 2002-05-20 | 2017-09-07 | Способы получения и использования ингибитора sglt2 |
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RU2004137489/04A RU2337916C2 (ru) | 2002-05-20 | 2003-05-15 | C-арил глюкозидные sglt2 ингибиторы и способ их применения |
RU2008122558A RU2489151C3 (ru) | 2002-05-20 | 2008-06-06 | Фармацевтическая комбинация, содержащая ингибитор sglt2 |
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