RU2219167C2 - N-замещенные аминотетралины как лиганды для рецептора y5 нейропептида y, полезные при лечении ожирения и других расстройств - Google Patents

N-замещенные аминотетралины как лиганды для рецептора y5 нейропептида y, полезные при лечении ожирения и других расстройств Download PDF

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RU2219167C2
RU2219167C2 RU2000127036/04A RU2000127036A RU2219167C2 RU 2219167 C2 RU2219167 C2 RU 2219167C2 RU 2000127036/04 A RU2000127036/04 A RU 2000127036/04A RU 2000127036 A RU2000127036 A RU 2000127036A RU 2219167 C2 RU2219167 C2 RU 2219167C2
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Скотт Л. Дакс
Тимоти Уолтер ЛАВЕНБЕРГ
Джеймс Дж. МАКНЭЛЛИ
Аллен Б. Рейтц
Марк Эндрю ЯНГМЭН
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Abstract

Изобретение относится к N-замещенным аминотетралинам формулы 1
Figure 00000001

где R1 независимо выбирают из группы, состоящей из водорода; гидрокси; галогена; C1-8-алкокси; замещенного C1-8-алкокси, где заместитель представляет собой галоген; n равен 0-2; Y представляет собой метилен; m равен 0-3; В1 означает водород; В2 означает водород; R2 выбирают из группы, состоящей из водорода; гидрокси; C1-6-алкила; C1-6-алкенила; фенила; замещенного фенила, где заместитель выбирают из галогена, C1-6-алкила, С1-6-алкокси, трифтор-С1-6-алкила, нитро; нафтила и пиридила; L выбирают из группы, состоящей из C1-8-алкилена; С1-4-алкилен-С3-7-циклоалкил-С1-4-алкилена; С1-4-алкилен-арил-С1-4-алкилена; R3 выбирают из фенила; замещенного фенила, где заместитель выбирают из галогена, нитро, C1-8-алкокси, трифторметила и амино-С1-8-алкила; нафтила; и тиенила и их энантиомеры, диастереомеры и фармацевтически приемлемые соли. Соединения 1 являются лигандами рецептора Y5 нейропептида Y, что позволяет использовать их в фармацевтической композиции для лечения болезней и расстройств, связанных с ингибированием подтипа Y5 рецептора NPY. 3 с. и 17 з.п. ф-лы, 3 табл.

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Claims (20)

1. N-Замещенные аминотетралины формулы 1
Figure 00000098
где R1 независимо выбирают из группы, состоящей из водорода; гидрокси; галогена; C1-8-алкокси; замещенного C1-8-алкокси, где заместитель представляет собой галоген;
n = 0-2;
Y - метилен;
m = 0-3;
B1 - водород;
В2 - водород;
R2 выбирают из группы, состоящей из водорода; гидрокси; C1-6-алкила; C1-6-алкенила; фенила; замещенного фенила, где заместитель выбирают из галогена, С1-6-алкила, C1-6-алкокси, трифтор-С1-6-алкила, нитро; нафтила и пиридила;
L выбирают из группы, состоящей из C1-8-алкилена; C1-4-алкилен-С3-7-циклоалкил-С1-4-алкилена; C1-4-алкилен-арил-C1-4-алкилена;
R3 выбирают из фенила; замещенного фенила, где заместитель выбирают из галогена, нитро, C1-8-алкокси, трифторметила и амино-С1-8-алкила; нафтила и тиенила;
и их энантиомеры, диастереомеры и фармацевтически приемлемые соли.
2. Соединение по п.1, выбранное из группы, в которую входят
рац-[lα,2α(транс)]-N-[[[[[1,2,3,4-тетрагидро-6-метокси-1-(фенилметил)-2-нафталинил]амино]метил]-4-циклогексил]метил]-2-нафталинсульфонамид;
рац-[1α,2α(транс)]-N-[[[1,2,3,4-тетрагидро-6-метокси-1-(фенилметил)-2-нафталинил]амино]-5-пентил]-2-нафталинсульфонамид;
рац-[1α,2α(транс)]-N-[[[[[1,2,3,4-тетрагидро-6-метокси-1-(3-пиридинилметил)-2-нафталинил]амино]метил]-4-циклогексил]метил]-2-нафталинсульфонамид;
рац-[1α,2α(транс)]-N-[[[[[1,2,3,4-тетрагидро-6-фтор-1-(фенилметил)-2-нафталинил]амино]метил]-4-циклогексил]метил]-2-фторбензолсульфонамид;
рац-[1α,2α(транс)]-N-[[[[[1,2,3,4-тетрагидро-6-фтор-1-фенил-2-нафталинил]амино]метил]-4-циклогексил]метил]-2-наф-талинсульфонамид;
рац-[1α,2α(транс)]-N-[[[[[1,2,3,4-тетрагидро-6-метокси-1-(1-пропен-3-ил)-2-нафталинил]амино]метил]-4-циклогексил]-метил]бензолсульфонамид;
рац-[1α,2α(транс)]-N-[[[[[1,2,3,4-тетрагидро-6-метокси-1-(3-гидроксипропил)-2-нафталинил]амино]метил]-4-циклогек-сил]метил]бензолсульфонамид и
рац-[1α,2α(транс)]-N-[[[[[1,2,3,4-тетрагидро-6-метокси-1-(н-пропил)-2-нафталинил]амино]метил]-4-циклогексил]метил]-бензолсульфонамид.
3. Соединение по п.1, где соль представляет собой гидрохлорид.
4. Соединение по п.1, где R1 - водород, C1-8-алкокси, галоген, или гидрокси; B1 и В2 - водород; m = 0-3; n = 1-2; R2 - фенил, замещенный фенил, нафтил или пиридил; L = C1-8алкилен или С1-4-алкилен-С3-7-циклоалкил-С1-4-алкилен; R3 - фенил, замещенный фенил, нафтил или тиенил, и его энантиомеры, диастереомеры и фармацевтически приемлемые соли.
5. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000099
Figure 00000100
Figure 00000101
Figure 00000102
Figure 00000103
6. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000104
Figure 00000105
Figure 00000106
Figure 00000107
Figure 00000108
Figure 00000109
Figure 00000110
7. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000111
Figure 00000112
Figure 00000113
Figure 00000114
Figure 00000115
Figure 00000116
Figure 00000117
8. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000118
Figure 00000119
Figure 00000120
Figure 00000121
Figure 00000122
Figure 00000123
Figure 00000124
9. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000125
Figure 00000126
Figure 00000127
Figure 00000128
Figure 00000129
Figure 00000130
Figure 00000131
10. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000132
Figure 00000133
Figure 00000134
Figure 00000135
Figure 00000136
Figure 00000137
11. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000138
Figure 00000139
Figure 00000140
Figure 00000141
Figure 00000142
Figure 00000143
12. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000144
Figure 00000145
Figure 00000146
Figure 00000147
Figure 00000148
Figure 00000149
13. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000150
Figure 00000151
Figure 00000152
14. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000153
Figure 00000154
Figure 00000155
Figure 00000156
Figure 00000157
Figure 00000158
Figure 00000159
15. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000160
Figure 00000161
16. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000162
Figure 00000163
17. Соединение по п.1, выбранное из группы, состоящей из
Figure 00000164
Figure 00000165
18. Способ лечения расстройств и болезней, связанных с ингибированием подтипа Y5 рецептора NPY, включающий введение млекопитающему, нуждающемуся в таком лечении, терапевтически эффективного количества соединения по п.1.
19. Фармацевтическая композиция для лечения болезней и расстройств, связанных с ингибированием подтипа Y5 рецептора NPY, содержащая терапевтически эффективное количество соединения по п.1 и фармацевтически приемлемый носитель.
20. Фармацевтическая композиция по п. 21 для лечения ожирения, связанного с ингибированием подтипа Y5 рецептора NPY.
RU2000127036/04A 1998-04-29 1999-04-12 N-замещенные аминотетралины как лиганды для рецептора y5 нейропептида y, полезные при лечении ожирения и других расстройств RU2219167C2 (ru)

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US60/083,415 1998-04-29
US09/290,651 US6140354A (en) 1998-04-29 1999-04-12 N-substituted aminotetralins as ligands for the neuropeptide Y Y5 receptor useful in the treatment of obesity and other disorders
US09/290,651 1999-04-12

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PT1076644E (pt) 2004-10-29
DE69918296T2 (de) 2005-08-04
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US6140354A (en) 2000-10-31
CN1289475C (zh) 2006-12-13
PL194839B1 (pl) 2007-07-31
WO1999055667A1 (en) 1999-11-04
IL139227A0 (en) 2001-11-25
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AU3640099A (en) 1999-11-16
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JP2004503462A (ja) 2004-02-05
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EP1076644A1 (en) 2001-02-21
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AU759313B2 (en) 2003-04-10
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ATE269846T1 (de) 2004-07-15
TR200100137T2 (tr) 2001-05-21
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