申请人：Kuo Sheng-Chu
公开号：US20120015908A1
公开（公告）日：2012-01-19
A compound of Formula I is disclosed as follows:
or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein
R is hydrogen, P(═O)(OH)
2
, P(═O)(O(C
1
-C
18
)alkylene(C
6
-C
20
)aryl)
2
, P(═O)(OH)(OM), P(═O)(OM)
2
, P═O(O
2
M), S(═O)(OH)
2
, S(═O)(O(C
1
-C
18
)alkylene(C
6
-C
20
)aryl)
2
, S(═O)(OH)(OM), S(═O)(OM)
2
;
M is a monovalent or divalent metal ion, or alkylammonium ion;
W is (C
6
-C
20
)aryl, (C
6
-C
20
)heteroaryl, (C
1
-C
18
)alkyl(C
6
-C
20
)aryl, (C
1
-C
18
)alkyl(C
6
-C
20
)heteroaryl, hydroxy(C
6
-C
20
)aryl, hydroxy(C
6
-C
20
)heteroaryl, (C
1
-C
18
)alkoxy(C
6
-C
20
)aryl, (C
1
-C
18
)alkoxy(C
6
-C
20
)heteroaryl, (C
1
-C
18
)alkylenedioxy(C
6
-C
20
)aryl, (C
1
-C
18
)alkylenedioxy(C
6
-C
20
)heteroaryl, halo(C
6
-C
20
)aryl, halo(C
6
-C
20
)heteroaryl, (C
1
-C
18
)alkylamino(C
6
-C
20
)aryl, (C
1
-C
18
)alkylamino(C
6
-C
20
)heteroaryl, (C
1
-C
18
)cycloalkylamino(C
6
-C
20
)aryl, or (C
1
-C
18
)cycloalkylamino(C
6
-C
20
)heteroaryl, and their OR
8
substutes;
R
5
is (C
1
-C
18
alkoxy, hydrogen, hydroxyl, O—(C
1
-C
18
)alkyl(C
6
-C
20
)aryl, halo or OR
8
, or R
5
and R
6
are (C
1
-C
18
)dioxy provided that R
7
is hydrogen;
R
6
is hydroxyl, O—(C
1
-C
18
)alkyl(C
6
-C
20
)aryl, halo or OR
R
, (C
1
-C
18
)alkoxy, (C
1
-C
18
)alkylamino, or (C
1
-C
18
)cycloalkylamino, or R
6
and R
7
are (C
1
-C
18
)dioxy provided that R
5
is hydrogen;
R
7
is hydrogen, halo or OR
8
, hydroxyl, or O—(C
1
-C
18
)alkyl(C
6
-C
20
)aryl; and
R
8
is P(═O)(OH)
2
, P(═O)(O(C
1
-C
18
)alkyl(C
6
-C
20
)aryl)
2
, P(═O)(OH)(OM), or P(═O)(OM)
2
, P═O(O
2
M).
根据以下公式披露了一种化合物：或其药学上可接受的盐、前药、溶剂合物或代谢物，其中R为氢、P(═O)(OH)2、P(═O)(O(C1-C18)烷基(C6-C20)芳基)2、P(═O)(OH)(OM)、P(═O)(OM)2、P═O(O2M)、S(═O)(OH)2、S(═O)(O(C1-C18)烷基(C6-C20)芳基)2、S(═O)(OH)(OM)、S(═O)(OM)2；M为一价或二价金属离子，或烷基铵离子；W为(C6-C20)芳基、(C6-C20)杂芳基、(C1-C18)烷基(C6-C20)芳基、(C1-C18)烷基(C6-C20)杂芳基、羟基(C6-C20)芳基、羟基(C6-C20)杂芳基、(C1-C18)烷氧基(C6-C20)芳基、(C1-C18)烷氧基(C6-C20)杂芳基、(C1-C18)烷二氧基(C6-C20)芳基、(C1-C18)烷二氧基(C6-C20)杂芳基、卤代(C6-C20)芳基、卤代(C6-C20)杂芳基、(C1-C18)烷基氨基(C6-C20)芳基、(C1-C18)烷基氨基(C6-C20)杂芳基、(C1-C18)环烷基氨基(C6-C20)芳基，或(C1-C18)环烷基氨基(C6-C20)杂芳基，以及它们的OR8取代基；R5为(C1-C18)烷氧基、氢、羟基、O—(C1-C18)烷基(C6-C20)芳基、卤素或OR8，或R5和R6为(C1-C18)二氧基，前提是R7为氢；R6为羟基、O—(C1-C18)烷基(C6-C20)芳基、卤素或ORR、(C1-C18)烷氧基、(C1-C18)烷基氨基，或(C1-C18)环烷基氨基，或R6和R7为(C1-C18)二氧基，前提是R5为氢；R7为氢、卤素或OR8、羟基，或O—(C1-C18)烷基(C6-C20)芳基；R8为P(═O)(OH)2、P(═O)(O(C1-C18)烷基(C6-C20)芳基)2、P(═O)(OH)(OM)、或P(═O)(OM)2、P═O(O2M)。
