Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...
Patent
1992-11-16
1996-05-14
Saunders, David
Chemistry: molecular biology and microbiology
Measuring or testing process involving enzymes or...
Involving antigen-antibody binding, specific binding protein...
424 169, 435 78, 530324, 530325, 530326, 530327, C07K 708, C07K 1400, G01N 33534
Patent
active
055166423
ABSTRACT:
Disclosed herein are polypeptides of the formula
R.sup.1 --AA--A.sup.1 --A.sup.2 --A.sup.3 --A.sup.4 --A.sup.5 --A.sup.6 --A.sup.7 --A.sup.8 --A.sup.9 --A.sup.10 --A.sup.11 --A.sup.12 --A.sup.13 --R.sup.2 that are useful in treatment of diabetes mellitus, wherein:
AA is a single bond or a polypeptide chain of 1 to 12 natural amino acid residues;
A.sup.1 is seryl, A.sup.2 is phenylalanyl, A.sup.3 is arginyl, A.sup.4 is valyl, A.sup.5 is aspartyl, A.sup.6 is leucyl, A.sup.7 is arginyl, A.sup.8 is threonyl, A.sup.9 is leucyl, A.sup.10 is leucyl, A.sup.11 is arginyl, and A.sup.12 is tyrosyl, wherein one of A.sup.1 through A.sup.12 may be replaced with a natural amino acid residue, and wherein when A.sup.12 is phenylalanyl, tyrosyl or tryptophyl, its aromatic ring may be substituted with 1 or 2 iodo atoms;
A.sup.13 is a natural amino acid residue other than tyrosyl, the D-form of a natural amino acid residue, --N(R.sup.4)--CH(R.sup.3)--C(O)--, or --N(R.sup.4)--CH(R.sup.3)--CH.sub.2 --;
R.sup.1 is hydrogen, lower alkyl, R.sup.5 --C(O)--, aryl, aryl(lower alkyl), cycloalkyl, cycloalkyl(lower alkyl), aryl(lower alkoxy), cycloalkyl(lower alkoxy), or arylsulfenyl, wherein the aryl or cycloalkyl may be substituted with 1 to 5 substituents selected from 1 to 5 halo, 1 to 3 nitro, 1 to 5 lower alkyl, and 1 to 5 lower alkoxy groups;
R.sup.2 is hydrogen, lower alkyl, aryl, aryl(lower alkyl), cycloalkyl, cycloalkyl(lower alkyl), hydroxyl, lower alkoxy, aryloxy, aryl(lower alkoxy), cycloalkyloxy, cycloalkyl(lower alkoxy), N.sub.3, --NR.sup.6 R.sup.7, or --N(R.sup.8)--NR.sup.6 R.sup.7 ;
R.sup.3 is hydrogen, --R.sup.9 --R.sup.10, or --NR.sup.6 R.sup.7, and R.sup.4 is hydrogen or alkyl, or R.sup.3 and R.sup.4 together are alkylene;
and the remaining symbols are as defined in the specification.
REFERENCES:
patent: 5073540 (1991-12-01), Olsson
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Mapelli Claudio
Meyers Chester A.
Bristol--Myers Squibb Company
Gaul Timothy J.
Saunders David
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