RU2007116039A - Сульфонилзамещенные бициклические соединеия в качестве модуляторов ppar - Google Patents
Сульфонилзамещенные бициклические соединеия в качестве модуляторов ppar Download PDFInfo
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Abstract
1. Соединение, имеющее структурную формулу, выбранную из группы, состоящей из формулы II, формулы III и формулы IVиили его соль, сложный эфир или пролекарство,где Gвыбран из группы, включающей -(CRR)-, -Z(CRR)-, -(CRR)Z-, -(CRR)Z(CRR)-;Z является О, S или NR;n равно О, 1 или 2;r и s независимо выбраны из 0 и 1;Rи Rнезависимо выбраны из группы, включающей водород, гало, необязательно замещенный низший алкил, необязательно замещенный низший гетероалкил, необязательно замещенный низший алкокси и низший пергалоалкил, или вместе могут образовывать необязательно замещенный циклоалкил;X, X, и Хнезависимо выбраны из группы, включающей водород, необязательно замещенный низший алкил, необязательно замещенный циклоалкил, галоген, пергалоалкил, гидрокси, необязательно замещенный низший алкокси, нитро, циано и NH;Gвыбран из группы, включающей насыщенный или ненасыщенный циклоалкил или гетероциклоалкильный линкер, необязательно замещенный Хи Х;Хи Xнезависимо выбраны из группы, включающей водород, необязательно замещенный низший алкил, галоген, низший пергалоалкил, гидрокси, необязательно замещенный низший алкокси, нитро, циано, NHи COR, или Хи Хвместе могут образовывать углеродный цикл;R выбран из группы, состоящей из необязательно замещенного низшего алкила и водорода;Gвыбран из группы, включающей связь, двойную связь, -(CRR)-, карбонил и -(CRR)CR=CR-;m равно 0, 1 или 2;Rи Rнезависимо выбраны из группы, включающей водород, необязательно замещенный низший алкил, необязательно замещенный низший алкокси, необязательно замещенный арил, низший пергалоалкил, циано и нитро;Gвыбран из группы, включающей водород, необязательно замещенный арил, необязательно замещенный гетероарил
Claims (9)
1. Соединение, имеющее структурную формулу, выбранную из группы, состоящей из формулы II, формулы III и формулы IV
или его соль, сложный эфир или пролекарство,
где G1 выбран из группы, включающей -(CR1R2)n-, -Z(CR1R2)n-, -(CR1R2)nZ-, -(CR1R2)rZ(CR1R2)s-;
Z является О, S или NR;
n равно О, 1 или 2;
r и s независимо выбраны из 0 и 1;
R1 и R2 независимо выбраны из группы, включающей водород, гало, необязательно замещенный низший алкил, необязательно замещенный низший гетероалкил, необязательно замещенный низший алкокси и низший пергалоалкил, или вместе могут образовывать необязательно замещенный циклоалкил;
X1, X2, и Х3 независимо выбраны из группы, включающей водород, необязательно замещенный низший алкил, необязательно замещенный циклоалкил, галоген, пергалоалкил, гидрокси, необязательно замещенный низший алкокси, нитро, циано и NH2;
G2 выбран из группы, включающей насыщенный или ненасыщенный циклоалкил или гетероциклоалкильный линкер, необязательно замещенный Х4 и Х5;
Х4 и X5 независимо выбраны из группы, включающей водород, необязательно замещенный низший алкил, галоген, низший пергалоалкил, гидрокси, необязательно замещенный низший алкокси, нитро, циано, NH2 и CO2R, или Х4 и Х5 вместе могут образовывать углеродный цикл;
R выбран из группы, состоящей из необязательно замещенного низшего алкила и водорода;
G3 выбран из группы, включающей связь, двойную связь, -(CR3R4)m-, карбонил и -(CR3R4)mCR3=CR4-;
m равно 0, 1 или 2;
R3 и R4 независимо выбраны из группы, включающей водород, необязательно замещенный низший алкил, необязательно замещенный низший алкокси, необязательно замещенный арил, низший пергалоалкил, циано и нитро;
G4 выбран из группы, включающей водород, необязательно замещенный арил, необязательно замещенный гетероарил, необязательно замещенный циклоалкил, необязательно замещенный циклогетероалкил, необязательно замещенный циклогетероарил, необязательно замещенный циклоалкенил и -N=(CR5R6); и
R5 и R6 независимо выбраны из группы, включающей водород, необязательно замещенный алкил, необязательно замещенный арил, необязательно замещенный гетероарил, необязательно замещенный циклоалкил, необязательно замещенный циклоалкенил и необязательно замещенный циклогетероалкил.
2. Соединение по п.1, имеющее структурную формулу, выбранную из группы, состоящей из
где G1 выбран из группы, включающей -(CR1R2)n- и -(CR1R2)nO-;
Z является О, S или NR;
n равно 0 или 1;
G2 имеет структуру
X1, X2, и Х3 - водород;
Х4 и X5 независимо выбраны из группы, включающей водород и низший алкил;
р равно 1, 2 или 3;
W выбран из группы, состоящей из -CX4Х5- и N-X7;
Х6 выбран из группы, включающей водород, алкил, гидрокси, алкокси, циано, галоген, низший пергалоалкил и NH2, или же не является ничем при образовании двойной связи с атомом соседнего кольца;
X7 выбран из группы, включающей водород, алкил, гидрокси и низший пергалоалкил, или же не является ничем при образовании двойной связи с Y2;
G3 выбран из группы, включающей связь и -(CR3R4)m-; и
R3 и R4 независимо выбраны из группы, включающей водород и низший алкил.
3. Соединение по п.2, отличающееся тем, что
р равно 2;
W является CX4Х5;
Х4 и X5 независимо выбраны из группы, включающей водород и метил;
Y1 является N;
G1 является -(CR1R2)n-;
R1 и R2 являются водородом и
G4 является арилом или гетероарилом, любой из которых может быть замещен галогеном, низшим алкилом, низшим пергалоалкилом, низшим пергалоалкокси, моно- или дигалоалкокси.
4. Соединение по п.3, отличающееся тем, что
G3 выбран из группы, включающей связь и -СН2-;
G4 является фенилом или пиридинилом, любой из которых единожды или дважды замещен галогеном, низшим алкилом, низшим пергалоалкилом, низшим пергалоалкокси, моно- или дигалоалкокси; и
Y2 является N.
5. Соединение по п.4, отличающееся тем, что Х4 и X5 являются метилом и присоединены к пиперазиновому кольцу в положениях 2 и 6; и
G4 является фенилом, паразамещенным заместителем, выбранным из группы, включающей трифторметил и трифторметокси.
6. Соединение, выбранное из группы, состоящей из соединений, описанных в примерах 1-107 и 110-117.
7. Соединение, выбранное из группы, состоящей из (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-фенил)-пиперазин-1-сульфонил]-индан-2-уксусной кислоты и (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-бензил)-пиперазин-1-сульфонил]-индан-2-уксусной кислоты, или его соль.
8. Соль, выбранная из группы, состоящей из тозилата (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-фенил)-пиперазин-1-сульфонил]-индан-2-уксусной кислоты и тозилата (S)-4-[цис-2,6-диметил-4-(4-трифторметокси-бензил)-пиперазин-1-сульфонил]-индан-2-уксусной кислоты.
9. Фармацевтическая композиция, включающая соединение по любому из пп.1-8 и фармацевтически приемлемый носитель.
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AU2005307006A1 (en) | 2006-05-26 |
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US7915253B2 (en) | 2011-03-29 |
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