RU2017145929A - МОДУЛЯТОРЫ ROR ГАММА(RORγ) - Google Patents
МОДУЛЯТОРЫ ROR ГАММА(RORγ) Download PDFInfo
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- RU2017145929A RU2017145929A RU2017145929A RU2017145929A RU2017145929A RU 2017145929 A RU2017145929 A RU 2017145929A RU 2017145929 A RU2017145929 A RU 2017145929A RU 2017145929 A RU2017145929 A RU 2017145929A RU 2017145929 A RU2017145929 A RU 2017145929A
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- phenyl
- acetamide
- cyclopropylmethanesulfonylphenyl
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- methyl
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- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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Claims (106)
1. Соединение формулы I
(формула I)
или его фармацевтически приемлемая соль, где:
A1 является NR1 или CR1, где R1 является H или метилом, где метил, если присутствует, необязательно замещен одним или более F;
циклопропильная часть может быть необязательно замещена одним или более метилом и одним или более F;
A2-A5 являются N или CR2-CR5, соответственно, при условии, что не более двух из четырех положений А в A2-A5 одновременно могут быть N;
R2-R5 независимо являются H, галогеном, амино, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-6)алкилом;
R6 и R7 независимо являются H, F, метилом, этилом, гидроксилом или метокси, или R2 и R3 вместе являются карбонилом, все алкильные группы, если присутствуют, необязательно замещены одним или более F;
R8 является Н или C(1-6)алкилом;
R
9
выбирают из группы, включающей формулу II, III, IV и V
(формула II)
где:
A10-A13 являются N или CR10-CR13, соответственно, при условии, что не более двух из четырех положений А в A10-A13 одновременно могут быть N;
R10-R13 независимо являются H, галогеном, амино, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-6)алкилом;
X14 является либо C(6-10)арилом, либо C(1-9)гетероарилом, где все атомы углерода необязательно замещены галогеном, амино, циано, C(1-3)алкокси, (ди)C(1 3)алкиламино или C(1-3)алкилом;
(формула III)
где:
A20-A27 являются N или CR20-CR27, соответственно, при условии, что не более двух из трех положений А в A20-A22 одновременно могут быть N, и что не более трех из пяти положений А в A23-A27 одновременно могут быть N;
R20-R22 независимо являются H, галогеном, амино, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-6)алкилом;
R23-R27 независимо являются H, галогеном, амино, циано, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-3)алкилом;
X28 является либо C(6-10)арилом, либо C(1-9)гетероарилом, где все атомы углерода необязательно замещены галогеном, амино, циано, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-3)алкилом;
где:
A30 является N или C;
A31 является O, карбонилом, NR31 или CR32;
R31 является Н или C(1-6)алкилом;
R32 является либо H, OH, либо C(1-3)алкилом, где все алкильные группы необязательно замещены одним или более F или OH;
A33-A42 являются N или CR33-CR42, соответственно, при условии, что не более трех из пяти положений А в A33-A37 одновременно могут быть N, и что не более трех из пяти положений А в A38-A42 одновременно могут быть N;
R33-R42 независимо являются H, галогеном, амино, циано, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-3)алкилом.
2. Соединение по п. 1, где A1 является CR1.
3. Соединение по п. 1, где A1 является NR1.
4. Соединение по пп. 1-3, где R1 является водородом.
5. Соединение по пп. 1-4, где R6 и R7 оба являются H.
6. Соединение по пп. 1-5, где R8 является H.
7. Соединение по пп. 1-6, где все положения А в A2-A5 являются CR2-R5 и все положения R в R2-R5 являются H.
8. Соединение по пп. 1-7, где R9 имеет формулу II, где:
A10-A13 являются N или CR10-CR13, соответственно, при условии, что не более двух из четырех положений А в A10-A13 одновременно могут быть N;
R10-R13 независимо являются H, амино, галогеном, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-6)алкилом;
X14 является либо C(6)арилом, либо C(1-5)гетероарилом, где все атомы углерода необязательно замещены галогеном, циано, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-3)алкилом.
9. Соединение по пп. 1-7, где R9 имеет формулу III, где:
A20-A27 являются N или CR20-CR27 соответственно, при условии, что не более двух из трех положений А в A20-A22 одновременно могут быть N, и что не более трех из пяти положений А в A23-A27 одновременно могут быть N;
R20-R22 независимо являются H, галогеном, амино, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-6)алкилом;
R23-R27 независимо являются H, галогеном, циано, амино, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-3)алкилом;
X28 является либо C(6)арилом или C(1-5)гетероарилом, где все атомы углерода необязательно замещены галогеном, циано, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-3)алкилом.
10. Соединение по пп. 1-7, где R9 имеет формулу IV или V, где:
A30 является N или C;
A31 является O, карбонилом, NR31 или CR32;
R31 является Н или C(1-6)алкилом;
R32 является H, OH или C(1-6)алкилом, где все алкильные группы необязательно замещены одним или более F или OH;
A33-A42 являются N или CR33-CR42, соответственно, при условии, что не более трех из пяти положений A33-A37 одновременно могут быть N, и что не более трех из пяти положений A38-A42 одновременно могут быть N;
R33-R42 независимо являются H, галогеном, циано, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-3)алкилом.
11. Соединение по п. 1, которое выбирают из группы:
2-(4-циклопропилметансульфонилфенил)-N-(3-фенокси-4-фенилфенил)ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(3-фторфенил)-3-(3-метоксифенокси)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[3-(3-метоксифенокси)-4-(4-метил-1H-имидазол-1-ил)фенил]ацетамид;
N-[3-(3-хлорфенокси)-4-(3-фторфенил)фенил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
N-[3-(3-хлорфенокси)-4-(3,4-дифторфенил)фенил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
N-[3-(3-цианофенокси)-4-(3,4-дифторфенил)фенил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[3-(3-метоксифенокси)-4-(5-метил-1H-пиразол-1-ил)фенил]ацетамид;
N-[3-(3-хлорфенокси)-4-(3,5-дифторфенил)фенил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
N-[4-(4-цианофенил)-3-(3-фторфенокси)фенил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
N-[3-(3-хлорфенокси)-4-(3-цианофенил)фенил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(3-фторфенил)-3-[3-(трифторметил)фенокси]фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[3-(3-фторфенокси)-4-(4-фторфенил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[3-(3,5-дифторфенокси)-4-(3-фторфенил)фенил]ацетамид;
2-[4-(циклопропилсульфамоил)фенил]-N-[3-(3-метоксифенокси)-4-(4-метил-1H-имидазол-1-ил)фенил]ацетамид;
2-[4-(циклопропилсульфамоил)фенил]-N-[3-(3-метоксифенокси)-4-(5-метил-1H-пиразол-1-ил)фенил]ацетамид;
2-[4-(циклопропилсульфамоил)фенил]-N-[4-(3-фторфенил)-3-(3-метоксифенокси)фенил]ацетамид;
N-[3-(3-хлорфенокси)-4-(3-фторфенил)фенил]-2-[4-(циклопропилсульфамоил)фенил]ацетамид;
N-[3-(3-хлорфенокси)-4-(3,4-дифторфенил)фенил]-2-[4-(циклопропилсульфамоил)фенил]ацетамид;
2-[4-(циклопропилсульфамоил)фенил]-N-[4-(3-фторфенил)-3-[3-(трифторметил)фенокси]фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-(5-фенокси-4-фенил-1,3-тиазол-2-ил)ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-фенил-5-(пиридин-3-илокси)-1,3-тиазол-2-ил]ацетамид;
N-(5-бензоил-4-фенил-1,3-тиазол-2-ил)-2-(4-циклопропилметансульфонилфенил)ацетамид;
N-[5-(4-хлорбензоил)-4-(3-хлорфенил)-1,3-тиазол-2-ил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-(4-фенилтиофен-2-ил)ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(пиридин-3-ил)тиофен-2-ил]ацетамид;
N-(5-бензоил-4-фенил-1,3-тиазол-2-ил)-2-[4-(циклопропилсульфамоил)фенил]ацетамид;
N-(5-бензоил-4-фенилтиофен-2-ил)-2-(4-циклопропилметансульфонилфенил)ацетамид;
N-{3-хлор-4-[2-(трифторметокси)фенил]фенил}-2-(4-циклопропилметансульфонилфенил)ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-{3-метил-4-[2-(трифторметокси)фенил]фенил}ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-{3,5-дихлор-4-[2-(трифторметокси)фенил]фенил}ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-{4-метил-5-[2-(трифторметокси)фенил]пиридин-2-ил}ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-{6-метил-5-[2-(трифторметокси)фенил]пиридин-2-ил}ацетамид;
N-{3-хлор-4-[2-(трифторметокси)фенил]фенил}-2-[4-(циклопропилсульфамоил)фенил]ацетамид;
2-[4-(циклопропилсульфамоил)фенил]-N-{6-метил-5-[2-(трифторметокси)фенил]пиридин-2-ил}ацетамид;
2-[4-(циклопропилсульфамоил)фенил]-N-{4-метил-5-[2-(трифторметокси)фенил]пиридин-2-ил}ацетамид;
2-[4-(циклопропилсульфамоил)фенил]-N-{3-метил-4-[2-(трифторметокси)фенил]фенил}ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-{4,6-диметил-5-[2-(трифторметокси)фенил]пиридин-2-ил}ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(4-метил-1H-имидазол-1-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(5-метил-1H-имидазол-1-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(3-метил-1H-пиразол-1-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(5-метил-1H-пиразол-1-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(4-метил-1H-пиразол-1-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(1,3-оксазол-5-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(1H-пиразол-1-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(1H-имидазол-1-ил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(1H-1,2,4-триазол-1-ил)фенил]ацетамид и
2-(4-циклопропилметансульфонилфенил)-N-[4-(1,2,4-оксадиазол-3-ил)фенил]ацетамид.
12. Соединение по любому из пп. 1-11 или его фармацевтически приемлемая соль для применения в терапии.
13. Соединение по любому из пп. 1-11 или его фармацевтически приемлемая соль для лечения RORγ-медиированных заболеваний или состояний.
14. Фармацевтическая композиция, которая содержит соединение формулы I по любому из пп. 1-11 или его фармацевтически приемлемую соль и один или более фармацевтически приемлемых наполнителей.
15. Фармацевтическая композиция по п. 14, которая также содержит, по крайней мере, один терапевтически активный агент.
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AU2016272018A1 (en) | 2018-01-04 |
WO2016193470A1 (en) | 2016-12-08 |
BR112017026224A2 (pt) | 2018-09-11 |
CN108430973B (zh) | 2021-09-21 |
CN108430973A (zh) | 2018-08-21 |
ES2794751T3 (es) | 2020-11-19 |
CA2988008A1 (en) | 2016-12-08 |
AU2016272018B2 (en) | 2020-08-27 |
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