RU2017103943A - Производные 6-амино-5,6,7,8-тетрагидронафтален-2-ила или 3-аминохроман-7-ила в качестве модуляторов taar - Google Patents

Производные 6-амино-5,6,7,8-тетрагидронафтален-2-ила или 3-аминохроман-7-ила в качестве модуляторов taar Download PDF

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RU2017103943A
RU2017103943A RU2017103943A RU2017103943A RU2017103943A RU 2017103943 A RU2017103943 A RU 2017103943A RU 2017103943 A RU2017103943 A RU 2017103943A RU 2017103943 A RU2017103943 A RU 2017103943A RU 2017103943 A RU2017103943 A RU 2017103943A
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amino
tetrahydronaphthalen
carboxamide
tetrahydronaphthalene
disorders
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RU2017103943A
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RU2017103943A3 (ru
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Джузеппе ЧЕЧЕРЕ
Гуидо Галлей
Анник ГЁРГЛЕ
Роджер НОРКРОСС
Филипп ПФЛИГЕР
Алина ТИРЛА
Филипп ШМИД
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Ф. Хоффманн-Ля Рош Аг
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Publication of RU2017103943A3 publication Critical patent/RU2017103943A3/ru

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Claims (123)

1. Соединение формулы
Figure 00000001
где
L представляет собой -C(O)NH-, -NHC(O)-, -NH- или -NHC(O)NH-;
Ar представляет собой фенил, бензил, нафтил или гетероарил, выбранный из группы, состоящей из пиридинила, пиразолила, пиримидинила, изоксазолила или пиразинила, где Ar может быть возможно замещен одним, двумя или тремя R1;
R1 представляет собой водород, С1-7 алкил, С1-7 алкокси, галоген, циано, циклоалкил, NHC(O)-C1-7 алкил, С1-7 алкокси замещенный галогеном, С1-7 алкил замещенный галогеном, или представляет собой фенил возможно замещенный одним или двумя атомами галогена, CF3O или С1-7 алкилом, или представляет собой фуранил, тиазолил или тиофенил, возможно замещенный галогеном или С1-7 алкилом;
X представляет собой СН2 или О;
R представляет собой водород или галоген;
или его фармацевтически приемлемые кислотно-аддитивные соли, все рацемические смеси, их соответствующие энантиомер и/или оптические изомеры.
2. Соединение формулы I по п. 1, где L представляет собой -C(O)NH-,
3. Соединение формулы I по п. 2, которое представляет собой
N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-(трифторметил)изоникотинамид
N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-4-бромо-5-циклопропил-1Н-пиразол-3-карбоксамид
N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-1-(2,2-дифторэтил)-5-пропил-1Н-пиразол-3-карбоксамид
(R)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-1-(2,2-дифторэтил)-5-пропил-1Н-пиразол-3-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-1-(2,2-дифторэтил)-5-пропил-1Н-пиразол-3-карбоксамид
(R)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-6-метил-2-(трифторметил)-пиримидин-4-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-6-метил-2-(трифторметил)-пиримидин-4-карбоксамид
N-(3-аминохроман-7-ил)-1-(2,2-дифторэтил)-5-пропил-1Н-пиразол-3-карбоксамид
N-(3-аминохроман-7-ил)-6-метил-2-(трифторметил)пиримидин-4-карбоксамид
(R)-N-(3-аминохроман-7-ил)-1-(2,2-дифторэтил)-5-пропил-1Н-пиразол-3-карбоксамид
(S)-N-(3-аминохроман-7-ил)-1-(2,2-дифторэтил)-5-пропил-1Н-пиразол-3-карбоксамид
(R)-N-(3-аминохроман-7-ил)-6-метил-2-(трифторметил)пиримидин-4-карбоксамид
(S)-N-(3-аминохроман-7-ил)-6-метил-2-(трифторметил)пиримидин-4-карбоксамид
(R)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-4-хлорбензамид
(R)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-хлорбензамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-метилизоникотинамид
(S)-2-ацетамидо-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)изоникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-этоксиизоникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-6-(трифторметил)никотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-6-метоксиникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-6-(2,2,2-трифторэтокси)никотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-4-хлор-3-(5-хлорофуран-2-ил)-1Н-пиразол-5-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-4-хлор-5-метилизоксазол-3-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-1-р-толил-1Н-пиразол-4-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-1-(3,4-дихлорфенил)-1Н-пиразол-4-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-1-(4-(трифторметокси)фенил)-1Н-пиразол-4-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-фторникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-6-хлорникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-5,6-дихлорникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3,4-дифторбензамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-нафтамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-(трифторметил)изоникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2,6-дихлоризоникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-5-хлорникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-2-хлор-6-метилизоникотинамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-этил-4-метил-1Н-пиразол-5-карбоксамид
(S)-N-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-4-бромо-5-(2,2-дифторэтокси)-1-этил-1Н-пиразол-3-карбоксамид
(S)-N-(6-амино-1-хлор-5,6,7,8-тетрагидронафтален-2-ил)-6-хлорникотинамид
(R)-N-(3-аминохроман-7-ил)-5-этокси-4-метил-1Н-пиразол-3-карбоксамид
(R)-N-(3-аминохроман-7-ил)-4-хлорпиримидин-2-карбоксамид
(R)-N-(3-аминохроман-7-ил)-4-(2-метилтиазол-4-ил)бензамид
(R)-N-(3-аминохроман-7-ил)-5-(трифторметил)пиримидин-2-карбоксамид
(R)-N-(3-аминохроман-7-ил)-1-метил-5-(тиофен-2-ил)-1Н-пиразол-3-карбоксамид
(R)-N-(3-аминохроман-7-ил)-4-циано-3-фторбензамид
(R)-N-(3-аминохроман-7-ил)-3,4-дифторбензамид
(R)-N-(3-аминохроман-7-ил)-3-этил-4-метил-1Н-пиразол-5-карбоксамид
(R)-N-(3-аминохроман-7-ил)-2-хлор-6-метилизоникотинамид
(R)-N-(3-аминохроман-7-ил)-2-(трифторметил)изоникотинамид
(R)-N-(3-аминохроман-7-ил)-2,6-дихлоризоникотинамид или
(R)-N-(3-аминохроман-7-ил)-4-бромо-5-(2,2-дифторэтокси)-1-этил-1Н-пиразол-3-карбоксамид.
4. Соединение формулы I по п. 1, где L представляет собой -NHC(O)-.
5. Соединение формулы I по п. 4, которое представляет собой
6-амино-N-(6-этоксипиридин-3-ил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(2-циклопропилпиримидин-5-ил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(5-(трифторметил)пиразин-2-ил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(4-(трифторметил)фенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(4-(трифторметил)бензил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-((6-хлорпиридин-3-ил)метил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(6-хлорпиридин-3-ил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(3-метоксифенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(3-(трифторметокси)фенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(4-этилфенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(4-хлорфенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(4-фторфенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(3-хлорфенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(4-циклопропилфенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
6-амино-N-(4-цианофенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид
(R)-6-амино-N-(3-(трифторметокси)фенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид или
(S)-6-амино-N-(3-(трифторметокси)фенил)-5,6,7,8-тетрагидронафтален-2-карбоксамид.
6. Соединение формулы I по п. 1, где L представляет собой NH-.
7. Соединение формулы I по п. 6, которое представляет собой
(S)-N6-(5-(трифторметил)пиримидин-2-ил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(5-хлорпиримидин-2-ил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(5-(трифторметил)пиридин-2-ил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(4-(трифторметил)фенил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-4-(6-амино-5,6,7,8-тетрагидронафтален-2-иламино)бензонитрил
(S)-N6-(4-хлорфенил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(4-этилфенил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(3-(трифторметокси)фенил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(4-фторфенил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(3-хлорфенил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(4-циклопропилфенил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(S)-N6-(4-хлорбензил)-1,2,3,4-тетрагидронафтален-2,6-диамин
(R)-N7-(5-(трифторметил)пиримидин-2-ил)хроман-3,7-диамин
(R)-N7-(5-хлорпиримидин-2-ил)хроман-3,7-диамин или
(S)-N6-(3-метоксифенил)-1,2,3,4-тетрагидронафтален-2,6-диамин.
8. Соединение формулы I по п. 1, где L представляет собой -NHC(O)NH-.
9. Соединение формулы I по п. 8, которое представляет собой
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(6-(трифторметил)пиридин-3-ил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(4-(трифторметил)фенил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-((5-хлорпиридин-2-ил)метил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(3-(трифторметокси)бензил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(4-этилфенил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(4-(трифторметокси)фенил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(3-метоксифенил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(4-хлорбензил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(4-цианофенил)мочевина
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(4-циклопропилфенил)мочевина или
(S)-1-(6-амино-5,6,7,8-тетрагидронафтален-2-ил)-3-(4-хлорфенил)мочевина.
10. Способ получения соединения формулы I по любому из пп. 1-9, который содержит
а) отщепление N-защитной группы (PG) от соединений формулы
Figure 00000002
до соединения формулы
Figure 00000003
где PG представляет собой N-защитную группу, выбранную из -С(O)O-трет-бутил (ВОС), и другие определения являются такими, как описано в п. 1, и,
если необходимо, конвертирование полученных соединений в фармацевтически приемлемые кислотно-аддитивные соли.
11. Соединение по любому из пп. 1-9, полученное способом по п. 10.
12. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-9 и фармацевтически приемлемый носитель и/или адъювант.
13. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-9 и фармацевтически приемлемый носитель и/или адъювант для применения при лечении депрессии, тревожных расстройств, биполярного расстройства, синдрома дефицита внимания и гиперактивности (СДВГ), расстройств, вызванных стрессом, психотических расстройств, шизофрении, неврологических заболеваний, болезни Паркинсона, нейродегенеративных расстройств, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, вызывающими зависимость, метаболических расстройств, нарушения питания, диабета, диабетических осложнений, ожирения, дислипидемии, расстройств потребления и ассимиляции энергии, расстройств и нарушений температурного гомеостаза, нарушений сна и циркадного ритма и сердечно-сосудистых расстройств.
14. Соединение по любому из пп. 1-9 для применения в качестве терапевтически активных веществ.
15. Соединения по любому из пп. 1-9 для применения в качестве терапевтически активных веществ для лечения депрессии, тревожных расстройств, биполярного расстройства, синдрома дефицита внимания и гиперактивности (СДВГ), расстройств, вызванных стрессом, психотических расстройств, шизофрении, неврологических заболеваний, болезни Паркинсона, нейродегенеративных расстройств, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, вызывающими зависимость, метаболических расстройств, нарушения питания, диабета, диабетических осложнений, ожирения, дислипидемии, расстройств потребления и ассимиляции энергии, расстройств и нарушений температурного гомеостаза, нарушений сна и циркадного ритма и сердечно-сосудистых расстройств.
16. Применение соединения по любому из пп. 1-9 для изготовления лекарственного средства для терапевтического и/или профилактического лечения депрессии, тревожных расстройств, биполярного расстройства, синдрома дефицита внимания и гиперактивности (СДВГ), расстройств, вызванных стрессом, психотических расстройств, шизофрении, неврологических заболеваний, болезни Паркинсона, нейродегенеративных расстройств, болезни Альцгеймера, эпилепсии, мигрени, гипертензии, злоупотребления веществами, вызывающими зависимость, метаболических расстройств, нарушения питания, диабета, диабетических осложнений, ожирения, дислипидемии, расстройств потребления и ассимиляции энергии, расстройств и нарушений температурного гомеостаза, нарушений сна и циркадного ритма и сердечно-сосудистых расстройств.
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