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RU2017145924A - МОДУЛЯТОРЫ ROR ГАММА (RORy) - Google Patents

МОДУЛЯТОРЫ ROR ГАММА (RORy) Download PDF

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Publication number
RU2017145924A
RU2017145924A RU2017145924A RU2017145924A RU2017145924A RU 2017145924 A RU2017145924 A RU 2017145924A RU 2017145924 A RU2017145924 A RU 2017145924A RU 2017145924 A RU2017145924 A RU 2017145924A RU 2017145924 A RU2017145924 A RU 2017145924A
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Russia
Prior art keywords
acetamido
cyclopropylmethanesulfonylphenyl
benzamide
phenyl
ethyl
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RU2017145924A
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English (en)
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RU2017145924A3 (ru
RU2727698C2 (ru
Inventor
Йосеф Мария Герардус Барбара Калс
Вера ДЕ КИМПЕ
Сандер Бернардус Набююрс
Original Assignee
Лид Фарма Холдинг Б.В.
Санофи
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Publication of RU2017145924A publication Critical patent/RU2017145924A/ru
Publication of RU2017145924A3 publication Critical patent/RU2017145924A3/ru
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Publication of RU2727698C2 publication Critical patent/RU2727698C2/ru

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    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07C311/20—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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    • C07D213/04—Heterocyclic 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
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Claims (194)

1. Соединение формулы I
Figure 00000001
(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 A 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 R6 и R7 вместе являются карбонилом, все алкильные группы, если присутствуют, необязательно замещены одним или более F;
- R8 является H или C(1-6)алкилом;
- A9-A12 являются N или CR9-CR12, соответственно, при условии, что не более двух из четырех положений A в A9-A12 одновременно могут быть N;
- R9-R12 независимо являются H, галогеном, амино, C(1-3)алкокси, (ди)C(1-3)алкиламино или C(1-6)алкилом;
- R13 является H, C(1-6)алкилом, C(2-6)алкенилом, C(3-6)циклоалкилом, C(3-6)циклоалкил-C(1-4)алкилом, C(2-5)гетероциклоалкилом, C(2-5)гетероциклоалкил-C(1-4)алкилом, C(6-10)арилом, C(6-10)арил-C(1-4)алкилом, C(1-9)гетероарилом или C(1-9)гетероарил-C(1-4)алкилом, все группы необязательно замещены одним или более галогеном, амино, гидроксилом, циано, C(1-3)алкокси, C(1-3)алкоксикарбонилом, (ди)C(1-3)алкиламино или C(1-3)алкилом; и
- R14 является H, C(1-6)алкилом, C(2-6)алкенилом, C(3-6)циклоалкилом, C(3-6)циклоалкил-C(1-4)алкилом, C(2-5)гетероциклоалкилом, C(2-5)гетероциклоалкил-C(1-4)алкилом, C(6-10)арилом, C(6-10)арил-C(1-4)алкилом, C(1-9)гетероарилом или C(1-9)гетероарил-C(1-4)алкилом, все группы необязательно замещены одним или более галогеном, амино, гидроксилом, циано, C(1-3)алкокси, C(1-3)алкоксикарбонилом, (ди)C(1-3)алкиламино или C(1-3)алкилом;
- или R13 и R14 конденсированы и образуют кольцо, содержащее от 5 до 7 атомов объединением R13, являющимся C(1-6)алкилом или C(2-6)алкенилом, ч независимым заместителем в пределах определения R14, все группы необязательно замещены одним или более галогеном, амино, гидрокси, циано, C(1-3)алкокси, C(1-3)алкоксикарбонилом, (ди)C(1-3)алкиламино или C(1-3)алкилом.
2. Соединение по п. 1, где A1 является CR1 и R1 является водородом.
3. Соединение по п. 1, где A1 является NR1 и R1 является водородом.
4. Соединение по п. 1-3, где все положения А в A2-A5 являются углеродом и все положения R в R2-R5 являются H.
5. Соединение по пп. 1-4, где R6 и R7 независимо являются H, метилом или гидроксилом.
6. Соединение по пп. 1-5, где R8 является H.
7. Соединение по пп. 1-6, где все положения А в A9-A12 являются углеродом или где положение A в любом из A9 или A10 является азотом и оставшиеся положения A в A9-A12 являются углеродом.
8. Соединение по пп. 1-7, где R9-R12 независимо являются H, галогеном, метилом или метокси.
9. Соединение по пп. 1-8, где R13 и R14 независимо являются H, C(1-6)алкилом, C(2-6)алкенилом, C(3-6)циклоалкилом, C(3-6)циклоалкил-C(1-4)алкилом, C(2-5)гетероциклоалкилом, C(2-5)гетероциклоалкил-C(1-4)алкилом, C(6-10)арилом, C(6-10)арил-C(1-4)алкилом, C(1-9)гетероарилом или C(1-9)гетероарил-C(1-4)алкилом, все группы необязательно замещены одним или более галогеном, гидроксилом, циано, C(1-3)алкокси, C(1-3)алкоксикарбонилом или C(1-3)алкилом.
10. Соединение по пп. 1-8, где R13 и R14 конденсированы и образуют кольцо, включающее от 5 до 7 атомов объединением C(1-6)алкила или C(2-6)алкенила в положении R13 с заместителем в положении R14, выбранным из C(1-6)алкила, C(2-6)алкенила, C(3-6)циклоалкила, C(3-6)циклоалкил-C(1-4)алкила, C(2-5)гетероциклоалкила, C(2-5)гетероциклоалкил-C(1-4)алкила, C(6)арила, C(6)арил-C(1-4)алкила, C(1-5)гетероарила или C(1-5)гетероарил-C(1-4)алкила, где все группы необязательно замещены одним или более галогеном, гидрокси, циано, C(1-3)алкокси, C(1-3)алкоксикарбонилом или C(1-3)алкилом.
11. Соединение по п. 1, которое выбирают из группы, включающей:
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-пропилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N,N-диметилбензамид;
N-бензил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2-фенилпропан-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-пропилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-(2-метилпропил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(циклопропилметил)-N-пропилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-(2-фенилэтил)бензамид;
N-трет-бутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамид;
N,N-дибензил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамид;
N-бензил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1-фенилэтил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N,N-бис(2-метилпропил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-(пиридин-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-[(1S)-1-фенилэтил]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенил-N-пропилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-пропил-N-(пиридин-3-ил)бензамид;
N-бензил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-пропилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-фенил-N-пропилбензамид;
N-бензил-4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-пропилбензамид;
N,N-дибензил-4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}бензамид;
этил 1-{4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензоил}пиперидин-3-карбоксилат;
N-трет-бутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метилбензамид;
N,N-дициклобутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(2-метилпиперидин-1-карбонил)фенил]ацетамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(4-метилфенил)бензамид;
метил 3-{N-этил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамидо} бензоат;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(3-метилфенил)бензамид;
этил 2-(N-бензил-1-{4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]фенил}формамидо)ацетат;
этил 6-{4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензоил}-4H,5H,6H,7H-тиено[2,3-c]пиридин-2-карбоксилат;
N-циклогексил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метилбензамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(2-фенилпирролидин-1-карбонил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(пиперидин-1-карбонил)фенил]ацетамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2-метилпропил)-N-фенилбензамид;
этил 2-(1-{4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензоил}пирролидин-2-ил)-1,3-тиазол-4-карбоксилат;
2-(4-циклопропилметансульфонилфенил)-N-{4-[2-(морфолин-4-илметил)пиперидин-1-карбонил]фенил}ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(1,2,3,4-тетрагидрохинолин-1-карбонил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(2,3-дигидро-1H-индол-1-карбонил)фенил]ацетамид;
N-бензил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-фенилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-метил-N-фенилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-(4-метилфенил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-(3-метилфенил)бензамид;
метил 3-(N-этил-4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}бензамидо)бензоат;
2-(4-циклопропилметансульфонилфенил)-N-[4-(3-фенилпиперидин-1-карбонил)фенил]ацетамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(2-фенилпиперидин-1-карбонил)фенил]ацетамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-(пиридин-3-ил)бензамид;
6-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-фенилпиридин-3-карбоксамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(пиридин-3-ил)бензамид;
3-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-фенилбензамид;
6-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-фенилпиридин-3-карбоксамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(1,2,3,4-тетрагидроизохинолин-2-карбонил)фенил]ацетамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-[(5-метил-1,2-оксазол-3-ил)метил]бензамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(4-метил-2-фенилпиперазин-1-карбонил)фенил]ацетамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-2-метокси-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(фуран-2-илметил)-N-метилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-[2-метил-1-(морфолин-4-ил)пропан-2-ил]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N,N-бис(проп-2-ен-1-ил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N,N-бис(2-метилпропил)бензамид;
2-(4-циклопропилметансульфонилфенил)-N-[4-(2,3,4,5-тетрагидро-1H-1-бензазепин-1-карбонил)фенил]ацетамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(4-метил-5-метил-1,3-тиазол-2-ил)-N-этилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-пропил-N-(пиридин-3-ил)бензамид;
2-[4-(циклопропилсульфамоил)фенил]-N-[4-(2-фенилпиперидин-1-карбонил)фенил]ацетамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-(пиридин-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-[2-(пиридин-3-ил)пропан-2-ил]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-[(2R)-1,1,1-трифтор-3-метилбутан-2-ил]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-[(1S)-1-(2-метоксифенил)этил]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-[(1S)-1-(2-фторфенил)этил]бензамид;
N-[циано(тиофен-2-ил)метил]-4-[2-(4-циклопропилметансульфонилфенил) ацетамидо]бензамид;
N-[циано(фенил)метил]-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-[2-(трифторметокси)фенил]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2,6-диметилфенил)бензамид;
N-[(1R)-1-(4-хлорфенил)-2,2,2-трифторэтил]-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамид;
N-циклопропил-4-[[2-[4-(циклопропилметилсульфонил)фенил]ацетил]амино]-N-(2-гидроксиэтил)бензамид;
N-циклопропил-4-[[2-[4-(циклопропилметилсульфонил)фенил]ацетил]амино]-N-[(1-гидроксициклобутил)метил]бензамид;
N-циклопропил-4-[[2-[4-(циклопропилметилсульфонил)фенил]ацетил]амино]-N-(2-метоксиэтил)бензамид;
N-циклопропил-4-[[2-[4-(циклопропилметилсульфонил)фенил]ацетил]амино]-N-тетрагидропиран-4-ил-бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-пропил-N-(тиофен-3-ил)бензамид;
N-бутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1,3-тиазол-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-пропил-N-(1,3-тиазол-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(1,3-тиазол-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-(1,3-тиазол-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1,3-диметил-1H-пиразол-5-ил)-N-пропилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(5-метил-1,2-оксазол-3-ил)-N-пропилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1,3-диметил-1H-пиразол-5-ил)-N-этилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(5-метил-1,2-оксазол-3-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-(5-метил-1,2-оксазол-3-ил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-метил-N-(5-метил-1,2-оксазол-3-ил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-(1,3-диметил-1H-пиразол-5-ил)-N-пропилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-(5-метил-1,2-оксазол-3-ил)-N-пропилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(3-метил-1,2-оксазол-5-ил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-(3-метил-1,2-оксазол-5-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(5-метил-1,3,4-тиадиазол-2-ил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-(5-метил-1,3,4-тиадиазол-2-ил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-3-метокси-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-2-фтор-N-фенилбензамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-3-метокси-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-3-фтор-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(1,2-оксазол-3-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенил-N-(2,2,2-трифторэтил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-3-метил-N-фенилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-3-метил-N-фенилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-(4-метил-5-метил-1,3-тиазол-2-ил)-N-этилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(диметил-1,2-оксазол-4-ил)-N-этилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-фенил-N-(2,2,2-трифторэтил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-(диметил-1,2-оксазол-4-ил)-N-этилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-2-фтор-N-фенилбензамид;
2-хлор-4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-этил-N-фенилбензамид;
N-бензил-N-трет-бутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1-метилпиперидин-4-ил)-N-фенилбензамид;
N-(4-бромфенил)-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-2-фтор-N-метил-N-(2-метилфенил)бензамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-метил-N-(2-метилфенил)бензамид;
N-(2-хлорфенил)-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-2-фторбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2,3-диметилфенил)-N-этил-2-фторбензамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2,3-диметилфенил)-N-этилбензамид;
N-[4-(3-трет-бутил-3,4-дигидро-2H-1,4-бензоксазин-4-карбонил)фенил]-2-(4-циклопропилметансульфонилфенил)ацетамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2-метоксифенил)-N,2-диметилбензамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенил-N-(2,2,2-трифторэтил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-2-фтор-N-(2-метоксифенил)-N-метилбензамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2-метоксифенил)-N-метилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-2-фтор-N-(2-фторфенил)-N-метилбензамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2-фторфенил)-N-метилбензамид;
2-хлор-N-(2-хлорфенил)-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этилбензамид;
2-хлор-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-N-(2-метилфенил)бензамид;
N-трет-бутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенилбензамид;
N-трет-бутил-4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-фенилбензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-(4-метилфенил)-N-[2-(оксолан-2-ил)пропан-2-ил]бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(4-метилфенил)-N-[2-(оксолан-2-ил)пропан-2-ил]бензамид;
N-трет-бутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-3-фтор-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-[2-(оксолан-2-ил)пропан-2-ил]-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(оксолан-3-ил)-N-(пиридин-2-ил)бензамид;
N-циклопропил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(пиридин-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1-гидрокси-2-метилпропан-2-ил)-N-фенилбензамид;
N-циклобутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(пиридин-2-ил)бензамид;
N-циклопропил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенилбензамид;
N-циклобутил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1-метилциклопропил)-N-фенилбензамид;
N-циклопропил-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(пиридин-3-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(3,3-дифторциклобутил)-N-фенилбензамид;
метил 2-(1-{4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]фенил}-N-фенилформамидо)-2-метилпропаноат;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-фенил-N-(1,1,1-трифторпропан-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2,6-дихлорфенил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-фенил-N-(1,1,1-трифторпропан-2-ил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(оксетан-3-ил)-N-фенилбензамид;
N-(4-(7-окса-4-азаспиро[2.5]октан-4-карбонил)фенил)-2-(4-((циклопропилметил)сульфонил)фенил)ацетамид;
N-(трет-бутил)-4-(2-(4-((циклопропилметил)сульфонил)фенил)ацетамидо)-N-(2-гидроксиэтил)бензамид;
4-(2-(4-((циклопропилметил)сульфонил)фенил)ацетамидо)-N-(2-гидроксиэтил)-N-изобутилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(1-гидрокси-2-метилпропан-2-ил)-N-(4-метилфенил)бензамид;
4-{2-[4-(циклопропилсульфамоил)фенил]ацетамидо}-N-(1-гидрокси-2-метилпропан-2-ил)-N-(4-метилфенил)бензамид;
4-[2-(6-циклопропилметансульфонилпиридин-3-ил)ацетамидо]-N-фенил-N-(2,2,2-трифторэтил)бензамид;
4-[2-(6-циклопропилметансульфонилпиридин-3-ил)ацетамидо]-N-этил-2-фтор-N-фенилбензамид;
2-хлор-4-[2-(6-циклопропилметансульфонилпиридин-3-ил)ацетамидо]-N-этил-N-фенилбензамид;
N-трет-бутил-4-[2-(6-циклопропилметансульфонилпиридин-3-ил)ацетамидо]-N-фенилбензамид;
N-трет-бутил-4-[2-(6-циклопропилметансульфонилпиридин-3-ил)ацетамидо]-3-фтор-N-фенилбензамид;
4-[2-(6-циклопропилметансульфонилпиридин-3-ил)ацетамидо]-N-[2-(оксолан-2-ил)пропан-2-ил]-N-фенилбензамид;
4-[2-(6-циклопропилметансульфонилпиридин-3-ил)ацетамидо]-N-(1-гидрокси-2-метилпропан-2-ил)-N-(4-метилфенил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-2-метил-N-фенилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N,2-диметил-N-(2-метилфенил)бензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2,3-диметилфенил)-N-этил-2-метилбензамид;
4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-(2-фторфенил)-N,2-диметилбензамид и
N-(2-хлорфенил)-4-[2-(4-циклопропилметансульфонилфенил)ацетамидо]-N-этил-2-метилбензамид.
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.
RU2017145924A 2015-06-05 2016-06-03 МОДУЛЯТОРЫ ROR ГАММА (RORγ) RU2727698C2 (ru)

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