The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Oct. 29, 1996

Filed:

Dec. 08, 1994
Applicant:
Inventors:

David H Coy, New Orleans, LA (US);

John E Taylor, Upton, MA (US);

Assignees:
Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K / ; C07K / ; C07K / ; C07K / ;
U.S. Cl.
CPC ...
530311 ; 530317 ; 530328 ;
Abstract

A cyclic octapeptide of the formula: ##STR1## wherein: A.sup.1 is D-Nal or D-Trp; A.sup.3 is Phe, F.sub.5 -Phe, or X-Phe wherein X is a halogen, NO.sub.2, CH.sub.3, or OH; A.sup.5 is --NH--CH(Y)--CO-- wherein Y is (CH.sub.2).sub.m --R.sub.4 --N(R.sub.5)(R.sub.6) or (CH.sub.2).sub.n --R.sub.4 --NH--C(R.sub.7)--N(R.sub.5) (R.sub.6); A.sup.6 is the D-- or L-- isomer of Thr, Leu, Ile, Nle, Val, and Abu; A.sup.8 is Nal or Trp; m is 1, 2, or 3; n is 1, 2, 3, 4 or 5; each of R.sub.1 and R.sub.2, independently, is H, E, COE, or COOE wherein E is C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, phenyl, naphthyl, C.sub.7-12 phenylalkyl or alkylphenyl, C.sub.8-12 phenylalkenyl or alkenylphenyl, C.sub.8-12 phenylalkynyl or alkynylphenyl, C.sub.11-20 naphthylalkyl or alkylnaphthyl, C.sub.12-20 naphthylalkenyl or alkenylnaphthyl, or C.sub.12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R.sub.1 or R.sub.2 is COE or COOE, the other must be H; R.sub.4 is C.sub.6 H.sub.4 or absent; R.sub.7 is .dbd.NR.sub.8, .dbd.S, or .dbd.O; and each of R.sub.3, R.sub.5, R.sub.6, and R.sub.8, independently, is H or E.


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