Therapeutic somatostatin analogs

Details Therapeutic somatostatin analogs Therapeutic somatostatin analogs

1988-06-22

1989-08-01

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530311, 514806, H61K 3724, C07K 726

Patent

active

048533718

ABSTRACT:
An octapeptide of 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, 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 p-substituted X-Phe (where X is a halogen, H, NO.sub.2, OH, NH.sub.2, or C.sub.1-3 alkyl), pentafluoro-Phe, or .alpha.-Nal; A.sub.5 is Thr, Ser, Phe, Val, .alpha.-aminobutyric acid, or Ile, provided that when A.sub.3 is phenyl, A.sub.1 is H, and A.sub.2 is H, A.sub.5 cannot be Val; and A.sub.7 is Thr, Trp, or .beta.-Nal; or a pharmaceutically acceptable salt thereof.

REFERENCES:
patent: 4282143 (1981-08-01), Sarantakis
patent: 4291022 (1981-09-01), Sandrin
patent: 4328135 (1982-05-01), Sarantakis
patent: 4395403 (1983-07-01), Bauer
patent: 4435385 (1984-03-01), Bauer
patent: 4485101 (1984-11-01), Coy
Veber et al., (1984), Life Sciences 34 (14), 1371.
Cai et al., (Jul 1985), Proc. 9th Ann. Peptide, Symposium Abstract.
Torres-Alman, (Abstract), Chemical Abstracts, 102:160733, (1985).
Murphy et al., Chemical Abstracts, 104:28911x, (1986).

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