Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Tripeptides – e.g. – tripeptide thyroliberin – etc.
Patent
1987-03-13
1990-11-13
Lee, Lester L.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Tripeptides, e.g., tripeptide thyroliberin , etc.
C07K 500
Patent
active
049702971
ABSTRACT:
This invention is directed to compounds of the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:
n is 0, 1 or 2;
p and q are independently 0, 1 or 2 and the sum of (p+q) is less than or equal to 3;
X is selected from the group consisting of: halo; --OR.sup.2, --SR.sup.2, --S(O)R.sup.2, --S(O).sub.2 R.sup.2, and --S(O).sub.2 NHR.sup.2, wherein R.sup.2 is lower alkyl, mono-, di- or tri-fluoro alkyl of 2 or 3 carbon atoms, optionally substituted aryl;
R is H or an N-protecting group;
R.sup.1 is alkylthio, arylthio, amino, alkylamino, optionally substituted arylamino, or optionally substituted aralkylamino; and when the sum of n+p+q is greater than or equal to one, R.sup.1 is also hydroxy, alkoxy, or aralkoxy; and
each (aa) is independently an .alpha.-amino acid residue with an optionally protected amino acid side chain.
REFERENCES:
patent: 4128542 (1978-12-01), Atherton et al.
patent: 4276288 (1981-06-01), Etschenberg et al.
patent: 4305852 (1981-12-01), Garsky
patent: 4397853 (1983-08-01), Kawakita et al.
patent: 4593024 (1986-06-01), Lu et al.
patent: 4657899 (1987-04-01), Rzeszotarski et al.
patent: 4694016 (1987-09-01), Lu et al.
J. Med. Chem. (1985), 28(5),668-672, Lauridsen et al.
Cancer Chemotherapy Reports, vol. 58, 6 (1974), Cooney et al.
Chem. Abs., vol. 102, 1985, 20 3802 k.
Chem. Abs., vol. 94, 1981, 16038v.
Chem. Abs., vol. 82, 1975, 149188t.
Organic Chemistry, vol. 6, 2nd, pp. 140-141.
Organic Chemistry, 3rd ed., Chap. 36, p. 1152.
Castelhano Arlindo L.
Pliura Diana H.
Venuti Michael C.
Johnson Lester E.
Lee Lester L.
Moran Tom M.
Syntex (U.S.A.) Inc.
Toth Liza K.
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