RU2015133177A - Модуляторы ship1 и связанные с ними способы - Google Patents

Модуляторы ship1 и связанные с ними способы Download PDF

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RU2015133177A
RU2015133177A RU2015133177A RU2015133177A RU2015133177A RU 2015133177 A RU2015133177 A RU 2015133177A RU 2015133177 A RU2015133177 A RU 2015133177A RU 2015133177 A RU2015133177 A RU 2015133177A RU 2015133177 A RU2015133177 A RU 2015133177A
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compound
optionally substituted
pharmaceutically acceptable
acceptable salt
stereoisomer
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RU2015133177A
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Ллойд Ф. МАККЕНЗИ
Томас Б. МАКРУРИ
Кертис ХАРВИГ
Дэвид БОГУЦКИ
Джеффри Р. РЭЙМОНД
Джереми Д. ПЕТТИГРЮ
Владимир Хлебников
Рудонг ШАН
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Экуинокс Фармасьютикалз (Кэнэда) Инк.
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Publication of RU2015133177A publication Critical patent/RU2015133177A/ru

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Claims (123)

1. Соединение формулы (I)
Figure 00000001
где
Figure 00000002
выбран из
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
или
Figure 00000011
n равно 1, 2, 3, 4, 5 или 6;
R1 представляет собой -R9a-C(R10)2-R9b-, -R9a-C(О)-R9b-, -R9a-S(O)t-R9b- (где t равно 0, 1 или 2), -R9a-O-R9b-, -R9a-C(О)N(R11a)-R9b-, -R9a-N(R11a)C(O)-R9b- или -R9a-N(R11a)-R9b-;
каждый R2 и R3 независимо выбран из водорода, алкила или -R9-OR11, при условии, что по меньшей мере один из R2 и R3 представляет собой -R9-OR11, где R6 представляет собой водород;
каждый R4a и R4b независимо выбран из водорода, алкила, -R9-OR11 или -С(О)OR11,
или R4a выбран из водорода, алкила, -R9-OR11 или -C(O)OR11, и R4b представляет собой прямую связь к углероду с номером 1 или представляет собой прямую связь к углероду с номером 3;
R5 независимо выбран из водорода, оксо, циано, нитро, галогена, алкила, галогеналкила, необязательно замещенного циклоалкила, необязательно замещенного циклоалкилалкила, необязательно замещенного арила, необязательно замещенного аралкила, необязательно замещенного гетероциклила, необязательно замещенного гетероциклилалкила, необязательно замещенного гетероарила, необязательно замещенного гетероарилалкила, -R9-OR11, -R9-C(O)R11, -R9-C(O)OR11, -R9-N(R11)R12, -R9-C(O)N(R11)R12, -R9-N(R11)C(O)R12, -R9-N(R11)-R14-N(R11)R12, -R9-N(R11)C(O)-R9-N(R11)R12, -R9-N(R11)C(O)N(R11)-OR12, -R9-N(R11)C(=NR11)N(R11)R12, -R9-N(R11)S(O)pR11 (где p равно 1 или 2), -R9-N(R11)C(S)N(R11)R12 или -R9-N(R11)C(O)-R9-N(R11)S(O)pR12 (где p равно 1 или 2);
каждый R6 и R8 независимо выбран из водорода, алкила, галогена или галогеналкила;
R7 представляет собой водород, алкил, галоген или галогеналкил;
каждый R9, R9a и R9b независимо представляет собой прямую связь или неразветвленную или разветвленную алкиленовую цепь;
каждый R10 независимо представляет собой водород, алкил, -OR11, -C(O)OR11, -C(O)N(R11)R12, -N(R11)R12 или -N(R11)C(O)R11;
каждый R11, R11a и R12 независимо представляет собой водород, алкил, алкенил, галогеналкил, необязательно замещенный циклоалкил, необязательно замещенный циклоалкилалкил, необязательно замещенный арил, необязательно замещенный аралкил, необязательно замещенный гетероциклил, необязательно замещенный гетероциклилалкил, необязательно замещенный гетероарил или необязательно замещенный гетероарилалкил; и
R14 представляет собой неразветвленную или разветвленную алкиленовую цепь;
или его стереоизомер или его фармацевтически приемлемая соль;
при условии, что соединения формулы (I) не включают следующие соединения:
(1S,2S,4aS,8aR)-декагидро-1-[2-(3-метоксифенил)этил]-5,5,8а-триметил-2-нафталинкарбоновая кислота;
(1S,2S,4aS,8aR)-декагидро-1-[2-(3-метоксифенил)этил]-5,5,8а-триметил-2-нафталинметанол;
α-(3,5-диметоксифенил)декагидро-2-гидрокси-2,5,5,8а-тетраметил-1-нафталинметанол;
(4aS,8aS)-3,4,4а,5,6,7,8,8а-октагидро-α-(3-метокси-5-метилфенил)-2,5,5,8а-тетраметил-1-нафталинметанол;
(1S,2R,4aS,8aS)-декагидро-2-гидрокси-α-(3-метокси-5-метилфенил)-2,5,5,8а-тетраметил-1-нафталинметанол;
(1R,2R,4aS,8aS)-декагидро-1-[(3-метокси-5-метилфенил)метил]-2,5,5,8а-тетраметил-2-нафталенол;
(1S,2R,4aS,8aS)-1-(3-метокси-5-метилфеноксиметил)-2,5,5,8a-тетраметилдекагидронафтален-2-ол;
(1S,2R,4aS,8aS)-1-(3,5-диметоксифеноксиметил)-2,5,5,8a-тетраметилдекагидронафтален-2-ол;
(1S,2R,4aS,8aS)-1-[3,5-бис(пропан-2-илокси)феноксиметил]-2,5,5,8а-тетраметилдекагидронафтален-2-ол;
(1R,2R,8aS)-1-((3,5-диметоксифенилсульфонил)метил)-2,5,5,8а-тетраметилдекагидронафтален-2-ол;
(1R,2R,4aS,8aS)-1-{[(3-метокси-5-метилфенил)сульфанил]метил}-2,5,5,8а-тетраметилдекагидронафтален-2-ол;
(1R,2R,4aS,8aS)-1-{[(3-метоксифенил)сульфанил]метил}-2,5,5,8а-тетраметилдекагидронафтален-2-ол; и
(1R,2R,4aS,8aS)-1-{[(3,5-диметоксифенил)сульфанил]метил}2,5,5,8а-тетраметилдекагидронафтален-2-ол.
2. Соединение по п. 1 формулы (Iа)
Figure 00000012
где n, R1, R2, R3, R4a, R4b, R5, R6, R7 и R8 такие, как определено в п. 1,
или его стереоизомер или его фармацевтически приемлемая соль.
3. Соединение по п. 2, где R1 представляет собой -R9a-C(O)-R9b-, т.е. соединение формулы (Ia1)
Figure 00000013
где R9a и R9b такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
4. Соединение по п. 2, где R1 представляет собой -R9a-C(R10)2-R9b-, т.е. соединение формулы (Iа2):
Figure 00000014
где R9a, R9b и R10 такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
5. Соединение по п. 2, где R1 представляет собой -R9-S(O)t-R9-, т.е. соединение формулы (Iа3)
Figure 00000015
где t, R9a и R9b такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
6. Соединение по п. 2, где R1 представляет собой -R9a-O-R9b-, т.е. соединение формулы (Iа4)
Figure 00000016
где R9a и R9b такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
7. Соединение по п. 2, где R1 представляет собой -R9a-С(О)N(R11a)-R9b-, т.е. соединение формулы (Iа5)
Figure 00000017
где R9a, R9b и R11a такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
8. Соединение по п. 2, где R1 представляет собой -R9a-N(R11a)С(О)-R9b-, т.е. соединение формулы (Iа6)
Figure 00000018
где R9a, R9b и R11a такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
9. Соединение по п. 2, где R1 представляет собой -R9a-N(R11a)-R9b-, т.е. соединение формулы (Iа7)
Figure 00000019
где R9a, R9b и R11a такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
10. Соединение по п. 1 формулы (Iс)
Figure 00000020
где n, R1, R4a, R4b, R5, R6, R7 и R8 такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
11. Соединение по п. 10, где R1 представляет собой -R9a-N(R11a)С(О)-R9b-, т.е. соединение формулы (Ic1)
Figure 00000021
где R9a, R9b и R11a такие, как определено в п. 1,
или его стереоизомер или его фармацевтически приемлемая соль.
12. Соединение по п. 1 формулы (Id)
Figure 00000022
где n, R1, R4a, R4b, R5, R6, R7 и R8 такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
13. Соединение по п. 12, где R1 представляет собой R1 представляет собой -R9a-C(R10)2-R9b-, т.е. соединение формулы (Id1)
Figure 00000023
где R9a, R9b и R10 такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
14. Соединение по п. 1 формулы (Iе)
Figure 00000024
где n, R1, R4a, R4b, R5, R6, R7 и R8 такие, как определено в п. 1,
или его стереоизомер или его фармацевтически приемлемая соль.
15. Соединение по п. 14, где R1 представляет собой -R9a-С(R10)2-R9b-, т.е. соединение формулы (Ie1)
Figure 00000025
где R9a, R9b и R10 такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемая соль.
16. Соединение по п. 1 формулы (If)
Figure 00000026
где n, R1, R4a, R4b, R5, R6, R7 и R8 такие, как определено в п. 1,
или его стереоизомер, или его фармацевтически приемлемую соль.
17. Соединение по п. 16, где R1 представляет собой -R9a-С(R10)2-R9b-, т.е. соединение формулы (If1)
Figure 00000027
где R9a, R9b и R10 такие, как определено в п. 1,
или его стереоизомер или его фармацевтически приемлемая соль.
18. Соединение по п. 1, где
Figure 00000028
выбран из
Figure 00000029
Figure 00000030
Figure 00000031
или
Figure 00000032
n равно 1, 2, 3, 4, 5 или 6;
R1 представляет собой -R9a-C(R10)2-R9b-, -R9a-C(О)-R9b-, -R9a-S(O)t-R9b- (где t равно 0, 1 или 2), -R9a-O-R9b-, или -R9a-С(O)N(R11a)-R9b- или -R9a-N(R11a)C(O)-R9b-;
каждый R4a и R4b независимо выбран из водорода, алкила, -R9-OR11 или -С(О)OR11,
или R4a выбран из водорода, алкила, -R9-OR11 или -С(О)OR11, и R4b представляет собой прямую связь к углероду с номером 1 или представляет собой прямую связь к углероду с номером 3;
R5 независимо выбран из водорода, оксо, циано, нитро, галогена, алкила, галогеналкила, необязательно замещенного циклоалкила, необязательно замещенного циклоалкилалкила, необязательно замещенного арила, необязательно замещенного аралкила, необязательно замещенного гетероциклила, необязательно замещенного гетероциклилалкила, необязательно замещенного гетероарила, необязательно замещенного гетероарилалкила, -R9-OR11, -R9-C(O)R11, -R9-C(O)OR11, -R9-N(R11)R12, -R9-C(O)N(R11)R12, -R9-N(R11)C(O)R12, -R9-N(R11)-R14-N(R11)R12, -R9-N(R11)C(O)-R9-N(R11)R12, -R9-N(R11)C(O)N(R11)-OR12, -R9-N(R11)C(=NR11)N(R11)R12, -R9-N(R11)S(O)pR11 (где p равно 1 или 2), -R9-N(R11)C(S)N(R11)R12 или -R9-N(R11)C(O)-R9-N(R11)S(O)pR12 (где p равно 1 или 2);
каждый R6 и R8 независимо выбран из водорода, алкила, галогена или галогеналкила;
R7 представляет собой водород, алкил, галоген или галогеналкил;
каждый R9, R9a и R9b независимо представляет собой прямую связь или неразветвленную или разветвленную алкиленовую цепь;
каждый R10 независимо представляет собой водород, алкил, -OR11, -С(О)OR11, -C(O)N(R11)R12, -Ν(R11)R12 или -Ν(R11)С(O)R11;
каждый R11, R11a и R12 независимо представляет собой водород, алкил, алкенил, галогеналкил, необязательно замещенный циклоалкил, необязательно замещенный циклоалкилалкил, необязательно замещенный арил, необязательно замещенный аралкил, необязательно замещенный гетероциклил, необязательно замещенный гетероциклилалкил, необязательно замещенный гетероарил или необязательно замещенный гетероарилалкил; и
R14 представляет собой неразветвленную или разветвленную алкиленовую цепь;
или его стереоизомер, или его фармацевтически приемлемая соль.
19. Соединение, выбранное из группы, состоящей из:
(2R,4R,4aS,8aS)-4-[(3,5-диметоксифенил)карбонил]-4а,8,8-триметил-3-метилидендекагидронафтален-2-ола;
(4aS,5S,8aS)-5-[(3-метокси-5-метилфенил)метил]-1,1,4а-триметил-6-метилидендекагидронафталена;
N-((2R,3S,4S,4aS)-4-((фуран-2-карбоксамидо)метил)-3,4а,8,8-тетраметилдекагидронафтален-2-ил)никотинамида;
N-((2R,3S,4S,4aS)-4-((фуран-2-карбоксамидо)метил)-3,4а,8,8-тетраметилдекагидронафтален-2-ил)-4-метилпиперазин-1-карбоксамида и
N-((2R,3S,4S,4aR)-4-(2-(фуран-2-карбоксамидо)этил)-3,4а,8,8-тетраметилдекагидронафтален-2-ил)-4-метилпиперазин-1-карбоксамида;
или его фармацевтически приемлемая соль.
20. Композиция, содержащая соединение по п. 1 или п. 19, или его стереоизомер или его фармацевтически приемлемую соль, и фармацевтически приемлемый эксципиент.
21. Способ модуляции SHIP1, включающий введение эффективного количества соединения по п. 1 или 19, или его фармацевтически приемлемой соли, или стереоизомера, или композиции по п. 20 млекопитающему, при необходимости.
22. Способ лечения заболевания, нарушения или состояния, включающий введение эффективного количества соединения по п. 1 или 19, или его фармацевтически приемлемой соли, или стереоизомера, или композиции по п. 20 млекопитающему, при необходимости, где заболевание, нарушение или состояние, представляет собой аутоиммунное заболевание, нарушение или состояние, воспалительное заболевание, нарушение или состояние, или неопластическое или клеточно-пролиферативное заболевание, нарушение или состояние.
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