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    • 4. 发明授权
    • Method for inhibiting blood vessel blockage using octapeptide
compositions
    • 使用八肽组合物抑制血管阻塞的方法
    • US5147856A
    • 1992-09-15
    • US329854
    • 1989-03-28
    • Peter W. RamwellPierre Braquet
    • Peter W. RamwellPierre Braquet
    • A61K38/00C07K14/655
    • C07K14/6555A61K38/00
    • A method for inhibiting blood vessel blockage in a mammal particularly after a procedure such as angioplasty, an arterial bypass operation or an allograft transplant operation which comprises: administering to a mammal before, during and/or after the procedure an effective blood vessel blockage inhibiting amount of an octapeptide having the formula ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H; A.sub.3 is CH.sub.2 A.sub.6 (where A.sub.6 is pentafluorophenyl, naphthyl, pyridyl, or phenyl); A.sub.4 is o-, m- or, more preferably, p-substituted X-Phe (where X is a halogen, H, NH.sub.2, NO.sub.2, OH , or C.sub.1-13 alkyl), pentafluoro-Phe, or .beta.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile; A.sub.7 is Thr, Trp, or .beta.-Nal (and can be either the D- or L-isomer); and Z is NH.sub.2 or OH; or a pharmaceutically acceptable salt thereof.
    • 一种抑制哺乳动物血管阻塞的方法,特别是在诸如血管成形术,动脉旁路操作或同种异体移植手术的手术之后,包括:在手术之前,期间和/或之后向哺乳动物施用有效的血管阻塞抑制量 具有式 + TR LA7Z的八肽,其中每个A1和A2独立地是H,C1-12烷基,C7-10苯基烷基,R1CO(其中R1是C1-20烷基,C3-20烯基,C3- 20个炔基,苯基,萘基或C7-10苯基烷基)或R2OCO(其中R2是C1-10烷基或C7-10苯基烷基),条件是当A1或A2之一为R1CO或R2OCO时,另一个必须为H; A3是CH2A6(其中A6是五氟苯基,萘基,吡啶基或苯基); A4是邻 - ,间 - 或更优选对取代的X-Phe(其中X是卤素,H,NH 2,NO 2,OH或C 1-13烷基),五氟-Phe或β-Nal; A5是Thr,Ser,Phe,Val,α-氨基丁酸或Ile; A7是Thr,Trp或β-Nal(并且可以是D-或L-异构体); Z是NH 2或OH; 或其药学上可接受的盐。