Analogs of terpene trilactones from ginkgo biloba and related compounds and uses thereof
申请人:Stromgaard Kristian
公开号:US20070098632A1
公开(公告)日:2007-05-03
The subject invention provides compounds having the structure:
wherein R
1
is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R
2
is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R
3
is H or OH; R
4
is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R
1
, R
2
, R
3
, or R
4
is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C
1
-C
5
) alkyl group, (C
2
-C
5
) alkenyl, or a (C
2
-C
5
) alkynyl, (C
1
-C
5
) alkoxy, (C
2
-C
5
) alkenyloxy, or (C
2
-C
5
) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C
1
-C
5
) alkyl, (C
2
-C
5
) alkenyl, or (C
2
-C
5
) alkynyl, or a cycloalkyl or aryl group having 3 to 10 carbon atoms; R3 is H or OH; R4 is H, (C1-C10) alkyl, (C1-C10) alkenyl, (C1-C10) alkynyl, -A-Ar, -A-Z-Ar, —SO
2
—Ar, or -A-NR
5
, or —R
7
, where A, Z and Ar are as defined herein, and the use of the compounds for detecting or identifying a receptor which binds the compounds of the invention or for treating a PAF associated condition in a subject.
该发明涉及具有以下结构的化合物:其中R1为H,OH,光活性基团,荧光基团或放射性基团;R2为H,OH,光活性基团,荧光基团或放射性基团;R3为H或OH;R4为H,OH,光活性基团,荧光基团或放射性基团;且其中至少一个R1,R2,R3或R4为光活性基团,荧光基团或放射性基团,或该化合物的光学纯对映体,或其中R1为H或OH;R2为H,OH,卤素,未取代或取代,直链或支链(C1-C5)烷基,(C2-C5)烯基或(C2-C5)炔基,(C1-C5)烷氧基,(C2-C5)烯氧基或(C2-C5)炔氧基,-N3,-COR5,-CONR5R6,-CO2R5,-OCOR5,-NH(OH),-NR5R6,-NHCOR5,-N(OH)COR5,-CH2OR5,-OCH2CO2R5,-CH2SR5,-CH2NR5R6,-SR5,-OSR5或-NR5SO2R6,其中R5和R6各自独立地为氢,取代或未取代的(C1-C5)烷基,(C2-C5)烯基或(C2-C5)炔基,或具有3至10个碳原子的环烷基或芳基;R3为H或OH;R4为H,(C1-C10)烷基,(C1-C10)烯基,(C1-C10)炔基,-A-Ar,-A-Z-Ar,-SO2-Ar或-A-NR5,或-R7,其中A,Z和Ar如本文所定义,并且使用这些化合物用于检测或识别结合该发明化合物的受体或用于治疗与PAF相关的疾病。