Method for inhibiting blood vessel blockage using octapeptide co

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 11, 514 12, 530311, C07K 726

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active

051478560

ABSTRACT:
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.

REFERENCES:
patent: 4485101 (1984-11-01), Coy et al.
patent: 4663309 (1987-05-01), Kaiser et al.
patent: 4853371 (1989-08-01), Coy et al.

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