申请人:——
公开号:US20040019021A1
公开(公告)日:2004-01-29
The invention relates to compounds of the following formula (I). In these compounds, R
1
, R
2
, R
3
and R
4
are each independently a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms, or hydrogen, substituted or unsubstituted alkyl, cycloalkyl, aryl, acyl, alkyloxycarbonyl, or alkylaminocarbonyl. At least two of R
1
, R
2
, R
3
and R
4
comprise the substituted or unsubstituted cyclitol. The linker can be any one of the following: —(CH2)
w
—, —(CH2)
x
—C6H4—(CH2)
x
—, —(CH2)
y
—NR5—(CH2)
y
—, and —(CH2)
z
—HCR6—(CH2)
z
—; wherein: w, x, y and z are independently an integer having a value of 0-10; R
5
is a substituted or unsubstituted cyclitol with a ring comprising six carbon atoms; and, R
6
is —OH, —OSO
3
Na, —OSO
3
Na substituted with alkyl, cycloalkyl or aryl, or substituted or unsubstituted alkyl, cycloalkyl or aryl. The compounds can also include substituted or unsubstituted cyclitol carbamides with the linker bond at the carbamide nitrogen. In other embodiments, the invention provides pharmaceutical compositions which include the compounds, and use of the compounds in the prevention or treatment in a mammalian subject of a disorder resulting from angiogenesis, metastasis, inflammation and/or coagulation/thrombosis.
1
本发明涉及以下式(I)的化合物。在这些化合物中,R1、R2、R3和R4分别独立地是带有六个碳原子环的取代或未取代的环己糖基,或者是氢、取代或未取代的烷基、环烷基、芳基、酰基、烷氧羰基或烷基
氨基羰基。至少有两个R1、R2、R3和R4包括取代或未取代的环己糖基。连接基可以是以下任何一种:-(
CH2)w-、-( )x-
C6H4-( )x-、-( )y-NR5-( )y-和-( )z-HCR6-( )z-;其中:w、x、y和z分别是0-10的整数;R5是带有六个碳原子环的取代或未取代的环己糖基;而R6是-OH、-OSO3Na、被烷基、环烷基或芳基取代的-OSO3Na,或者是取代或未取代的烷基、环烷基或芳基。这些化合物还可以包括连接基键在羰胺氮上的取代或未取代的环己糖基。在其他实施例中,本发明提供了包括这些化合物的制药组合物,并且利用这些化合物预防或治疗哺乳动物主体中因血管生成、转移、炎症和/或凝血/血栓形成而导致的疾病。