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CHROMENE DERIVATIVES AS INHIBITORS OF TCR-NCK INTERACTION
专利权人:
ARTAKS BIOFARMA INK.
发明人:
GAKHETE MATEOS Andres (US),ГАХЕТЕ МАТЕОС Андрес (US),KASTRO PALOMINO Khulio (ES),КАСТРО ПАЛОМИНО Хулио (ES),MARTI KLAUSEL Luk (US),МАРТИ КЛАУСЕЛЬ Лук (US),TORMO KARULYA Damiya (US),ТОРМО КАРУЛЬЯ Дамия,GAKHETE MATEOS Andres,ГАХЕТЕ МАТЕОС Андрес,KASTRO PALOMINO Khulio,КАСТРО ПАЛОМИНО Хулио,MARTI KLAUSEL Luk,МАРТИ КЛАУСЕЛЬ Лук,TORMO KARULYA Damiya
申请号:
RU2016118038
公开号:
RU0002665709C2
申请日:
2014.10.20
申请国别(地区):
RU
年份:
2018
代理人:
摘要:
FIELD: organic chemistry.SUBSTANCE: invention relates to a group of compounds of formula (I) containing a chromene nucleus or pharmaceutically acceptable salts thereof, wherein: R1 is unsubstituted C1-C6 alkyl or C1-C6 alkyl substituted with C3-C6 cycloalkyl; X is selected from -OH or -N(R2)(R3); R2 and R3 are independently selected from hydrogen, unsubstituted C1-C6 alkyl, C1-C6 alkyl substituted with -N(R')(R''), where R' and R'' are independently selected from H or C1-C4 alkyl, or a saturated 6-membered heterocycle that contains an N atom that is unsubstituted or substituted with C1-C4 alkyl; or R2 and R3 together with the nitrogen atom to which they are attached form a 5- or 6-membered saturated heterocycle, wherein said heterocycle contains at least one heteroatom selected from nitrogen, oxygen or sulphur, and wherein the heterocycle is optionally substituted with C1-C4 alkyl; R4 is a halogen, as well as a process for their preparation. .EFFECT: said compounds have the ability to inhibit the proliferation of lymphocytes mediated by the interaction of TCR with Nck, and therefore the present invention also relates to pharmaceutical compositions based thereon and the use of these compounds for the treatment of diseases or conditions, in which said interaction causes complications, such as graft rejection reactions, immune or autoimmune diseases, inflammatory diseases or proliferative diseases.36 cl, 2 dwg, 3 exИзобретение относится к группе соединений формулы (I), содержащих хроменовое ядро, или их фармацевтически приемлемым солям, где: R1 представляет собой незамещенный C1-C6 алкил или C1-C6 алкил, замещенный посредством С3-C6 циклоалкила; X выбран из -ОН или -N(R2)(R3); R2 и R3 независимо выбраны из водорода, незамещенного C1-C6 алкила, C1-C6 алкила, замещенного посредством -N(R')(R''), причем R' и R'' независимо выбраны из Н или С1-С4 алкила, или насыщенного 6-членного гетероцикла, который содержит атом N, незамещенный или замещенный посредством С1-С4 алкила; и
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