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Method for inhibiting angiogenesis using squalamine and squalamine steroid derivatives

机译:使用角鲨胺和角鲨胺类固醇衍生物抑制血管生成的方法

摘要

A method of inhibiting angiogenesis in a patient includes administering to the patient an effective amount of squalamine or a pharmaceutically acceptable salt of squalamine. Alternatively, a compound according to the following Formula (III) (or a pharmaceutically acceptable salt thereof) can be administered: ##STR1## wherein Z.sub.5 is -H or -H; each of the substituents Z.sub.7 is selected from the group of --H, --OH, --SH, --NH.sub.2, --F, --(C.sub.1 -C.sub.3)-alkyl, and --(C.sub.1 -C.sub.3)-alkoxy; and one of the substituents Z.sub.12 is - -H and the other is --H or --OH. X' is a polyamine side chain of the formula --X.sub.1 --(CH.sub.2).sub.p --X.sub.2 --(CH.sub.2).sub.q --N(R. sup.II)(R.sup.III), wherein one of X.sub.1 and X.sub.2 is --N(R.sup.IV) and the other is selected from the group of --N(R.sup.V), --O, --S, and -- CH.sub.2. R.sup.IV and R.sup.V are each --H or --(C.sub.1 -C.sub.3)- alkyl, p and q are each an integer of from 0 to 5 (but both are not 0). R. sup. II and R.sup.III in the formula for X' are each --H, --(C.sub.1 -C. sub.3)- alkyl, or --(CH.sub.2).sub.r --N(R.sub.10)(R.sub.11) wherein r is an integer from 2 to 5 and R.sub.10 and R.sub.11 are each --H or --(C.sub. 1 - C.sub.3)-alkyl. R' in Formula (III) is --H or --(C.sub.1 -C.sub.3)- alkyl, and Y' is --(C.sub.1 -C.sub.10)-alkyl, unsubstituted or substituted with - -CO.sub.2 H, --OH, --NH--SO.sub.2 CF.sub.3, --SO.sub.3 H, --PO.sub.3 H. sub.2, --OSO.sub.3 H, --CF.sub.3, --F, ##STR2##
机译:抑制患者血管新生的方法包括向患者施用有效量的角鲨胺或角鲨胺的药学上可接受的盐。或者,可以施用根据下式(III)的化合物(或其药学上可接受的盐):其中Z 5是-H或-H;或者每个取代基Z 7选自-H,-OH,-SH,-NH 2,-F,-(C 1 -C。 sub.3)-烷基和-(C.sub.1 -C.sub.3)-烷氧基;取代基Z 12之一是-H,另一个是-H或-OH。 X′是式--X.sub.1-(CH.sub.2).sub.p --X.sub.2-(CH.sub.2).q的多胺侧链--N(R.sup.II)(R.sup.III),其中X.sub.1和X.sub.2中的一个是--N(R.sup.IV),另一个选自--N(R.sup.V),-O,-S和-CH.sub.2组。 Rsv IV和Rsv分别为--H或-(C1-C3)烷基,p和q均为0至5的整数(但两者不为0)。 R. X′的式中的II和R III分别是-H,-(C 1 -C 3)-烷基或-(CH 2)。 r --N(R.sub.10)(R.sub.11)其中r是2到5的整数,R.sub.10和R.sub.11分别是--H或-(C。 1-C 3)-烷基。式(III)中的R'为-H或-(C 1 -C 3)-烷基,且Y'为-(C 1 -C 10)-未取代或被--CO.sub.2 H,-OH,-NH-SO.sub.2 CF.sub.3,-SO.sub.3 H,-PO.sub。 3 H.sub.2,--OSO.sub.3 H,--CF.sub.3,--F,## STR2 ##

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