申请人:Van Nieuwenhze Michael S.
公开号:US20130345117A1
公开(公告)日:2013-12-26
The present invention provides a peptide-phospholipid conjugate of Formula 1:
wherein: X is selected from the group consisting of —CR
1
R
2
—, —R
3
—, —O—, —S—, and S
+
(R
3
)—; Y is selected from the group consisting of a bond, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, amino, ether, cycloamino, cycloether, aryl heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, to heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; Z is a peptide comprising 1 to 50 amino acids; R
1
and R
2
each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, amino, ether, cycloamino, cycloether, aryl, heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl; and R
3
is selected from the group consisting of alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, amino, ether, cycloamino, cycloether, aryl, heteroaryl, arylalkyl, heteroarylalkyl, hydroxyaryl, arylether, cycloalkyl, heterocycloalkyl, hydroxycycloalkyl, halocycloalkyl, and aminocycloalkyl.
本发明提供了一种式子为1的肽-磷脂共轭体:
其中:X选自CR1R2,R3,O,S和S+(R3)组成的群;Y选自键,烷基,烯基,炔基,卤代烷基,烷氧基烷基,羟基烷基,氨基,醚,环氨基,环醚,芳基杂芳基,芳基烷基,杂芳基烷基,羟基芳基,芳基醚,环烷基,对杂环烷基,羟基对杂环烷基,卤代对杂环烷基和氨基对杂环烷基;Z是由1到50个氨基酸组成的肽;R1和R2各自独立地选自氢,烷基,烯基,炔基,卤代烷基,烷氧基烷基,羟基烷基,氨基,醚,环氨基,环醚,芳基,杂芳基,芳基烷基,杂芳基烷基,羟基芳基,芳基醚,环烷基,对杂环烷基,羟基对杂环烷基,卤代对杂环烷基和氨基对杂环烷基;R3选自烷基,烯基,炔基,卤代烷基,烷氧基烷基,羟基烷基,氨基烷基,氨基,醚,环氨基,环醚,芳基,杂芳基,芳基烷基,杂芳基烷基,羟基芳基,芳基醚,环烷基,对杂环烷基,羟基对杂环烷基,卤代对杂环烷基和氨基对杂环烷基。