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ARYLSULPHONAMIDE CCR3 ANTAGONISTS
专利权人:
INK.;AKSIKIN FARMASJUTIKALZ;AKSIKIN FARMAS'JUTIKALZ
发明人:
LAJ Taj Vehj (US),ЛАЙ Тай Вэй (US),FORRESTER Dzhared Ehndrju (US),ФОРРЕСТЕР Джаред Эндрю (US),LAJ TAJ VEHJ,ЛАЙ Тай Вэй,FORRESTER DZHARED EHNDRJU,ФОРРЕСТЕР Джаред Эндрю
申请号:
RU2011147192/04
公开号:
RU0002539591C2
申请日:
2010.04.21
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula , where: R1, R2, R3, R4, R5 and R6, each independently, denote hydrogen, halogen, cyano, nitro or C1-6alkyl; X denotes O or S; RYa denotes -C(O)R1a, -C(O)OR1a, -C(O)NR1bR1c, -C(S)NR1bR1c, -C(NNO2)NR1bR1c, -S(O)2R1a or -S(O)2NR1bR1c; under the condition that RYa is not -C(O)O-tert-butyl; and each R1a, R1b and R1c independently denotes hydrogen, C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, C6-14aryl, 5-10-member heteroaryl containing one, two or three heteroatoms selected from O, N or S, or morpholinyl; or each pair of R1b and R1c, together with the N atom to which they are bonded, independently forms morpholinyl; under the condition that the compound is not 4-(2-(3,5-dimethylphenoxy)-5-nitrophenylsulphonyl)piperazine-1-carbaldehyde; wherein each alkyl, alkenyl, aryl and 5-10-member heteroaryl, containing one, two or three heteroatoms selected from O, N or S, is optionally substituted with one or more groups, each independently selected from (a) cyano, halogen and nitro; (b) C1-6alkyl, C6-14aryl, furanyl and morpholinyl, each optionally substituted with one or more substitutes Q; (c) -C(O)Ra, -C(O)ORa, -ORa and -SRa, wherein each Q is independently selected from a group consisting of (a) cyano, halogen and nitro; (b) C1-6alkyl and C2-6alkenyl; and (c) -C(O)Re, -C(O)ORe, and -SRe; where each Re, Rf and Rg independently denotes (i) hydrogen; (ii) C1-6alkyl or C2-6alkenyl, which are suitable for modulating CCR3 activity.EFFECT: obtaining compounds which are suitable for modulating CCR3 activity.41 cl, 1 tbl, 4 exИзобретение относится к соединениям формулы I:где: R1, R2, R3, R4, R5 и R6, каждый независимо, обозначает водород, галоген, циано, нитро или C1-6алкил; X обозначает О или S; RYa обозначает -C(O)R1a, -C(O)OR1a, -С(О)NR1bR1c, -С(S)NR1bR1c, -С(NNO2)NR1bR1c, -S(O)2R1a или -S(О)2NR1bR1c; при условии, что RYa не является -С(О)О-трет-бутилом; и каждый R1a, R1b и R1c независимо обозначает водород, С1-6алк
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