申请人:Guilford Pharmaceuticals Inc.
公开号:US20020156050A1
公开(公告)日:2002-10-24
A compound of formula I:
1
or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof; wherein:
Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, carbocyclic or N-containing heterocyclic ring, wherein Y and any heteroatom(s) therein are unsubstituted or independently substituted by at least one non-interfering alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, carboxy or halo substituent;
X is at the 1-position of ring Y and is —COOR
5
or a substituted or unsubstituted moiety selected from the group consisting of
2
wherein
R
7
is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group;
R
1
is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkenyl, and is itself either unsubstituted or substituted with an alkyl, alkenyl, cycloalkyl or cycloalkenyl group;
R
2
, R
3
, R
4
and R
5
are independently hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl, and are either unsubstituted or substituted with a moiety selected from the group consisting of alkyl, alkenyl, alkoxy, phenoxy, benzyloxy, cycloalkyl, cycloalkenyl, hydroxy, carboxy, carbonyl, amino, amido, cyano, isocyano, nitro, nitroso, nitrilo, isonitrilo, imino, azo, diazo, sulfonyl, sulfoxy, thio, thiocarbonyl, sulfhydryl, halo, haloalkyl, trifluoromethyl and aryl.
式 I 的化合物:
1
或其药学上可接受的盐、水合物、酯、溶液剂、原药、代谢物、立体异构体或混合物;其中
Y 代表形成融合的 5 至 6 元、芳香族或非芳香族、碳环或含 N 的杂环所需的原子,其中 Y 及其中的任何杂原子未被取代或独立地被至少一个无干扰的烷基、烯基、环烷基、环烯基、芳基、芳基、羧基或卤代取代基取代;
X 位于环 Y 的 1 位,并且是 -COOR
5
或选自以下组别的取代或未取代分子
2
其中
R
7
是氢、烷基、烯基、环烷基或环烯基,且本身未被取代或被烷基、烯基、环烷基或环烯基取代;
R
1
是氢、烷基、烯基、环烷基或环烯基,且本身未被取代或被烷基、烯基、环烷基或环烯基取代;
R
2
, R
3
, R
4
和 R
5
环烷基、环烯基、羟基、羧基、羰基、氨基、酰胺基、氰基、异氰基、硝基、亚硝基、 尼基、异尼基、亚氨基、偶氮、重氮、磺酰基、磺氧、硫代、硫代羰基、巯基、卤代、 卤代烷基、三氟甲基和芳基。