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RU2397168C2 - Производные тиофена в качестве ингибиторов снк 1 - Google Patents

Производные тиофена в качестве ингибиторов снк 1 Download PDF

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RU2397168C2
RU2397168C2 RU2006128426/04A RU2006128426A RU2397168C2 RU 2397168 C2 RU2397168 C2 RU 2397168C2 RU 2006128426/04 A RU2006128426/04 A RU 2006128426/04A RU 2006128426 A RU2006128426 A RU 2006128426A RU 2397168 C2 RU2397168 C2 RU 2397168C2
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Сьюсан АШУЭЛЛ (US)
Сьюсан АШУЭЛЛ
Томас ДЖЕРО (US)
Томас Джеро
Стефанос ИОАННИДИС (US)
Стефанос ИОАННИДИС
Джеймс ДЖЕЙНЕТКА (US)
Джеймс ДЖЕЙНЕТКА
Пол ЛАЙН (US)
Пол Лайн
Мэй СУ (US)
Мэй СУ
Дорин ТОДЕР (US)
Дорин ТОДЕР
Динвэй Ю (US)
Динвэй Ю
Янь Ю (US)
Янь Ю
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Abstract

Настоящее изобретение относится к соединениям формулы (II) и их фармацевтически приемлемым солям. Соединения настоящего изобретения обладают свойствами ингибитора киназы СНК1. В формуле (II)
Figure 00000143
,
Figure 00000144
R1 обозначает фенил, который необязательно замещен на одном или нескольких атомах углерода одним или несколькими R9; где R9 выбирают из галогена, амино, C1-6алкила и C1-6алкокси, один из R2 и R3 представляет собой -С(=O)NR6R7, а другой представляет собой -NHC(=O)NHR4; R4 и R6 представляют собой Н, а R7 представляет собой пиперидин-3-ил. Изобретение также относится к фармацевтической композиции, содержащей соединение изобретения, к применению соединения для приготовления лекарственного средства, а также к промежуточному соединению формулы (XI) или его соли, где А представляет собой тиенильное кольцо. 4 н. и 3 з. п. ф-лы, 1 табл.

Description

Текст описания приведен в факсимильном виде.
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Claims (7)

1. Соединение формулы (II) или его фармацевтически приемлемая соль
Figure 00000141
,
в которой R1 обозначает фенил, который необязательно замещен на одном или нескольких атомах углерода одним или несколькими R9; где R9 выбирают из галогена, амино, C1-6алкила и С1-6алкокси,
один из R2 и R3 представляет собой -С(=O)NR6R7, а другой представляет собой -NHC(=O)NHR4;
R4 и R6 представляют собой Н, а
R7 представляет собой пиперидин-3-ил.
2. Соединение по п.1 или его фармацевтически приемлемая соль, где R2 представляет собой -NHC(=O)NHR4, a R3 представляет собой -C(=O)NR6R7.
3. Соединение по п.1, которое представляет собой (S)-пиперидин-3-иламид 5-(3-фтор-фенил)-3-уреидо-тиофен-2-карбоновой кислоты или его фармацевтически приемлемую соль.
4. Соединение по п.1, которое представляет собой (S)-пиперидин-3-иламид 5-фенил-2-уреидо-тиофен-3-карбоновой кислоты или его фармацевтически приемлемую соль.
5. Фармацевтическая композиция, обладающая свойствами ингибитора киназы СНК 1, содержащая соединение формулы (II) или его фармацевтически приемлемую соль по любому из пп.1-4 совместно с по меньшей мере одним фармацевтически приемлемым носителем, разбавителем или наполнителем.
6. Применение соединения формулы (II) или его фармацевтически приемлемой соли по любому из пп.1-4 для приготовления лекарственного средства, используемого при ингибировании активности киназы СНК 1.
7. Промежуточное соединение формулы (XI) или его соли
Figure 00000142

где R1 обозначает фенил, который необязательно замещен на одном или нескольких атомах углерода одним или несколькими R9; где R9 выбирают из галогена, амино, С1-6алкила и С1-6алкокси,
R6 представляют собой Н,
R7 представляет собой пиперидин-3-ил, а
А представляет собой тиенильное кольцо для получения соединения формулы (II) по любому из пп.1-4.
RU2006128426/04A 2004-01-05 2004-12-24 Производные тиофена в качестве ингибиторов снк 1 RU2397168C2 (ru)

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US55330504P 2004-03-15 2004-03-15
US60/553,305 2004-03-15

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US (1) US20070010556A1 (ru)
EP (2) EP1732920B1 (ru)
JP (1) JP2007517843A (ru)
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CN (1) CN100584840C (ru)
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MX (1) MXPA06007692A (ru)
MY (1) MY142018A (ru)
NO (1) NO20063449L (ru)
RU (1) RU2397168C2 (ru)
SA (1) SA05250449B1 (ru)
TW (1) TW200536849A (ru)
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