RU2004126861A - Производные пиридинамидов в качестве ингибиторов моноаминоксидазы (мао-в) - Google Patents

Производные пиридинамидов в качестве ингибиторов моноаминоксидазы (мао-в) Download PDF

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RU2004126861A
RU2004126861A RU2004126861/04A RU2004126861A RU2004126861A RU 2004126861 A RU2004126861 A RU 2004126861A RU 2004126861/04 A RU2004126861/04 A RU 2004126861/04A RU 2004126861 A RU2004126861 A RU 2004126861A RU 2004126861 A RU2004126861 A RU 2004126861A
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fluorobenzyloxy
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Андреа СЕСУРА (CH)
Андреа СЕСУРА
Роса-Мари РОДРИГЕС-САРМИЕНТО (CH)
Роса-Мария РОДРИГЕС-САРМИЕНТО
Эндрью Уилль м ТОМАС (CH)
Эндрью Уилльям Томас
Рене ВИЛЕР (CH)
Рене ВИЛЕР
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Ф.Хоффманн-Ля Рош Аг (Ch)
Ф.Хоффманн-Ля Рош Аг
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3

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Claims (18)

1. Соединения общей формулы
Figure 00000001
где один из Х или Уозначает -N=, а другой означает -CR7=;
R1 означает водород или (С16)алкил;
R2 означает водород или (С16)алкил;
R3 означает водород или (С16)алкил;
R4 означает галоген(С16)алкил или незамещенный арил, или арил, замещенный одним или несколькими заместителями, выбранными из группы, состоящей из (С16)алкила, галогена, галоген(С16)-алкила, (С16)алкоксигруппы и циангруппы;
R5 означает водород или (С16)алкил;
R6 означает водород или (С16)алкил;
R7 означает водород или (С16)алкил;
а также их фармацевтически приемлемые соли.
2. Соединения формулы I по п.1, где Х означает -N=.
3. Соединения формулы I по п.2, где R4 означает незамещенный арил или арил, замещенный одним или несколькими заместителями, выбранными из группы, состоящей из (С16)алкила, галогена, галоген(С16)алкила, (С16)алкоксигруппы и циангруппы.
4. Соединения формулы I по п.3, где R4 означает фенил или фенил, замещенный одним или несколькими заместителями, выбранными из группы, состоящей из (С16)-алкила, галогена, галоген(С16)алкила, (С16)алкоксигруппы и циангруппы.
5. Соединения формулы I по п.4, где R4 означает фенил, замещенный одним или несколькими атомами галогена.
6. Соединения формулы I по п.5, которые выбираются из группы, включающей
карбамоилметиламид 5-(3-фторбензилокси)пиридин-2-карбоновой кислоты,
карбамоилметиламид 5-(4-фторбензилокси)пиридин-2-карбоновой кислоты,
карбамоилметиламид 5-(3,4-дифторбензилокси)пиридин-2-карбоновой кислоты,
(1-карбамоилэтил)амид(S)-5-(3-фторбензилокси)пиридин-2-карбоновой кислоты,
(1-карбамоилэтил)амид(S)-5-(4-фторбензилокси)пиридин-2-карбоновой кислоты и
(1-карбамоилэтил)амид(S)-5-(3,4-дифторбензилокси)пиридин-2-карбоновой кислоты.
7. Соединения формулы I по п.1, где Y означает -N=.
8. Соединения формулы I по п.7, где R4 означает незамещенный арил или арил, замещенный одним или несколькими заместителями, выбранными из группы, состоящей из (С16)алкила, галогена, галоген(С16)алкила, (C16)алкоксигруппы и циангруппы.
9. Соединения формулы I по п.8, где R4 означает фенил или фенил, замещенный одним или несколькими заместителями, выбранными из группы, состоящей из (С16)-алкила, галогена, галоген(С16)алкила, (С16)алкоксигруппы и циангруппы.
10. Соединения формулы I по п.9, где R4 означает фенил или фенил, замещенный одним или несколькими атомами галогена.
11. Соединения формулы I по п.10, которые выбираются из группы, включающей:
6-бензилокси-N-карбамоилметилникотинамид,
N-карбамоилметил-6-(3-фторбензилокси)никотинамид,
N-карбамоилметил-6-(4-фторбензилокси)никотинамид,
(S)-6-бензилокси-N-(1-карбамоилэтил)никотинамид,
(S)-N-(1-карбамоилэтил)-6-(3-фторбензилокси)никотинамид и
(S)-N-(1-карбамоилэтил)-6-(4-фторбензилокси)никотинамид.
12. Способ получения соединения формулы I по п.1, а также его фармацевтически приемлемой соли, который включает взаимодействие соединения формулы
Figure 00000002
где X, Y, R4, R5 и R6 являются такими, как указано в п.1,
с соединением формулы
Figure 00000003
где R1, R2 и R3 являются такими, как указано в п.1,
для получения соединения формулы
Figure 00000004
и, если желательно, превращение соединения формулы I в фармацевтически приемлемую соль.
13. Соединение формулы I по любому из пп.1-11, полученное способом по п.12.
14. Лекарственное средство, содержащее одно или несколько соединений по любому из пп.1-11 и фармацевтически приемлемые наполнители, предназначенное для лечения и предупреждения заболеваний, опосредованных ингибиторами моноаминоксидазы В.
15. Лекарственное средство, содержащее одно или несколько соединений по любому из пп.1-11 и фармацевтически приемлемые наполнители, предназначенное для лечения и предупреждения болезни Альцгеймера и старческого слабоумия.
16. Соединение формулы I по любому из пп.1-11, а также его фармацевтически приемлемые соли для лечения или предупреждения заболеваний.
17. Применение соединения формулы I по любому из пп.1-11, а также его фармацевтически приемлемых солей для производства лекарственных средств, предназначенных для лечения и предупреждения заболеваний, опосредованных ингибиторами моноаминоксидазы В.
18. Применение по п.17, когда заболеванием является болезнь Альцгеймера или старческое слабоумие.
RU2004126861/04A 2002-02-04 2003-01-27 Производные пиридинамидов и лекарственное средство на их основе RU2309950C2 (ru)

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IT1404729B1 (it) * 2011-01-27 2013-11-29 Univ Pisa Inibitori altamente selettivi dell'attivita' di adams
KR101746060B1 (ko) 2015-09-18 2017-06-12 한국과학기술연구원 항비만 치료용 가역적 마오비 저해제
CN105601563B (zh) * 2015-12-17 2018-05-08 浙江工业大学 6-氯-n-(4-(6-氯烟酰胺)苄基)烟酰胺及其制备和应用
CN108912029B (zh) * 2017-08-25 2021-10-01 广东东阳光药业有限公司 含氮杂环酰胺衍生物及其用途
CN107903289B (zh) * 2017-11-08 2020-07-31 中国科学院烟台海岸带研究所 一种基于花菁的有机化合物及其应用

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