申请人:——
公开号:US20030013772A1
公开(公告)日:2003-01-16
The invention relates to the preparation of novel polyamines, such as derivatives of 1,3-bis-[(2′-aminoethyl)-amino]propane (2,3,2-tetramine) and 1,4,8,11-tetraazacyclotetradecane (cyclam), which can be used to treat mitochondrial and degenerative diseases.
Accordingly, in one aspect the invention is directed to compounds of the formula:
1
wherein
R
1
, R
2
, R
3
, R
4
, R
5
and R
6
may be the same or different and are hydrogen, alkyl, aryl, cycloalkyl, amino acid, glutathione, urate, ascorbate, estrogen, dehydroepiandrosterone, redox stabilizing substituents, a quinone, glutamate, succinate, —(CH
2
)
n
[XCH
2
)
n
]NH
2
— wherein n=3-6 and X=nitrogen, sulfur, phosporous or carbon, or heterocycle wherein R
1
to R
6
taken together are —(CH
2
XCH
2
)
n
— wherein n=3-6 and X=nitrogen, sulfur, phosporous or carbon.
M, n, and p may be the same or different and are bridging groups of variable length from 3-12 carbons.
X
1
and X
2
may be the same or different and are nitrogen, sulfur, phosporous or carbon.
本发明涉及制备新型聚胺,如1,3-双[(2'-氨基乙基)-氨基]丙烷(2,3,2-四胺)和1,4,8,11-四氮杂环十四烷(环戊二烯),可用于治疗线粒体和退行性疾病。因此,本发明在一个方面涉及以下式子的化合物:1其中R1、R2、R3、R4、R5和R6可以相同或不同,且为氢、烷基、芳香基、环烷基、氨基酸、谷胱甘肽、尿酸、抗坏血酸、雌激素、去氢表雄酮、氧化还原稳定取代基、醌、谷氨酸、琥珀酸、—(CH2)n[XCH2]nNH2—(其中n=3-6且X=氮、硫、磷或碳),或杂环,其中R1至R6一起为—(CH2XCH2)n—(其中n=3-6且X=氮、硫、磷或碳)。M、n和p可以相同或不同,且为可变长度的3-12个碳的桥接基团。X1和X2可以相同或不同,且为氮、硫、磷或碳。