RU2016117941A - Фениколовые противобактериальные средства - Google Patents

Фениколовые противобактериальные средства Download PDF

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RU2016117941A
RU2016117941A RU2016117941A RU2016117941A RU2016117941A RU 2016117941 A RU2016117941 A RU 2016117941A RU 2016117941 A RU2016117941 A RU 2016117941A RU 2016117941 A RU2016117941 A RU 2016117941A RU 2016117941 A RU2016117941 A RU 2016117941A
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phenyl
pyridin
fluoro
acetamide
hydroxy
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RU2016117941A
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Майкл КЕРТИС
Брайан А. ДУКЛОС
Ричард А. ЭВИН
Пол Д. ДЖОНСОН
Тимоти А. ДЖОНСОН
Раджендран ВЭРАГУНДАР
Денис Биллен
Ричард М. ГУДВИН
Андреа К. ХЭЙБЕР-СТАК
Грэм М. КАЙН
Сьюзан М.К. ШИХАН
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ЗОИТИС ЭлЭлСи
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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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Claims (28)

1. Соединение, выбранное из группы, состоящей из:
2,2-дифтор-N-{(1S,2R)-1-фторметил-2-гидрокси-2-[4-(6-пирролидин-2-ил-пиридин-3-ил)-фенил]-этил}-ацетамида;
2,2-дихлор-N-{(1S,2R)-1-(фторметил)-2-гидрокси-2-[4-(6-пирролидин-2-илпиридин-3-ил)-фенил]-этил}-ацетамида;
N-((1R,2S)-1-(4-(6-((S)-1-амино-2-гидроксиэтил)-пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида;
2,2-дихлор-N-((1R,2S)-3-фтор-1-гидрокси-1-(4-(6-(метилсульфонамидометил)пиридин-3-ил)фенил)пропан-2-ил)ацетамида;
2,2-дихлор-N-((1R,2S)-3-фтор-1-гидрокси-1-(4-(6-(1-(метилсульфонил)пирролидин-2-ил)пиридин-3-ил)фенил)пропан-2-ил)-ацетамида;
2,2-дихлор-N-((1R,2S)-3-фтор-1-гидрокси-1-(4-(6-(1-(метилсульфонамидо)этил)пиридин-3-ил)фенил)пропан-2-ил)ацетамида;
2,2-дифтор-N-((1R,2S)-3-фтор-1-гидрокси-1-(4-(6-(метилсульфонамидометил)пиридин-3-ил)фенил)пропан-2-ил)ацетамида;
2,2-дифтор-N-[(1R,2R)-1-фторметил-2-(4-{6-[(3-фтор-пропиламино)-метил]-пиридин-3-ил}-фенил)-2-гидрокси-этил]-ацетамида;
N-((1S,2R)-2-{4-[6-(1-амино-2,2,2-трифтор-этил)-пиридин-3-ил]-фенил}-1-фторметил-2-гидрокси-этил)-2,2-дифторацетамида;
2,2-дифтор-N-((1S,2R)-1-фторметил-2-гидрокси-2-{4-[6-(1-морфолин-4-ил-этил)-пиридин-3-ил]-фенил}-этил)-ацетамида;
2,2-дифтор-N-((1S,2R)-1-фторметил-2-гидрокси-2-{4-[6-(1-метиламино-этил)-пиридин-3-ил]-фенил}-этил)-ацетамида;
2,2-дифтор-N-[(1S,2R)-2-(4-{6-[1-(2-фтор-этиламино)-этил]-пиридин-3-ил}-фенил)-1-фторметил-2-гидрокси-этил]-ацетамида;
N-((1R,2S)-1-(4-(6-(3-аминооксетан-3-ил)пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида;
2,2-дифтор-N-((1R,2S)-3-фтор-1-гидрокси-1-(4-(6-(1-(метилсульфонамидо)циклопропил)пиридин-3-ил)фенил)пропан-2-ил)ацетамида;
N-((1R,2S)-1-(4-(5-(1-аминоэтил)тиофен-2-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дихлорацетамида;
2,2-дифтор-N-((1R,2S)-3-фтор-1-гидрокси-1-(4-(6-((RS)-1-(метилсульфонамидо)этил)пиридин-3-ил)фенил)пропан-2-ил)ацетамида;
2,2-дифтор-N-((1R,2S)-3-фтор-1-гидрокси-1-(4-(6-(морфолин-3-ил)пиридин-3-ил)фенил)пропан-2-ил)ацетамида;
N-((1R,2S)-1-(4-(6-(1-амино-2-метоксиэтил)-пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида;
N-((1S,2R)-2-{4-[6-(1-амино-2-циано-этил)-пиридин-3-ил]-фенил}-1-фторметил-2-гидрокси-этил)-2,2-дифторацетамида;
N-((1R,2S)-1-(4-(6-(2-амино-1-гидроксипропан-2-ил)пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида;
N-((1R,2S)-1-(4-(2-(1-аминоэтил)тиазол-5-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дихлорацетамида;
N-((1R,2S)-1-(4-(6-(1-аминопропил)пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида;
N-((1R,2S)-1-(4-(6-(амино(циклопропил)метил)пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида;
N-((1R,2S)-1-(4-(6-(1-амино-2-гидроксипропил)пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида; и
N-((1R,2S)-1-(4-(6-(азетидин-2-ил)пиридин-3-ил)фенил)-3-фтор-1-гидроксипропан-2-ил)-2,2-дифторацетамида, его энантиомеры, диастереомеры или фармацевтически приемлемая соль.
2. Фармацевтическая композиция, содержащая соединение по п. 1, его энантиомеры, диастереомеры или фармацевтически приемлемую соль и фармацевтически приемлемый носитель.
3. Способ контролирования или лечения инфекций у домашнего скота, включающий введение нуждающемуся в этом животному терапевтически эффективного количества соединения по п. 1, его энантиомеров, диастереомеров или фармацевтически приемлемой соли.
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