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Details for Patent: 3,893,992

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Details for Patent: 3,893,992

Title: N-acylated peptides of amino aromatic sulfonic acids and their derivatives
Abstract:Polypeptides which are useful for evaluating pancreatic enzyme sufficiently in animal organisms have the formula RCO--A.sub.n --NHR'CO--B.sub.m --NHZ wherein R is a hydrogen atom; a phenyl group; a phenyl group substituted with one or more halogen atoms, (C.sub.1 --C.sub.4)alkyl groups, hydroxy groups, (C.sub.1 --C.sub.4)alkoxy groups, (C.sub.1 --C.sub.4)alkoxy carbonyl groups, or similar substituents which will not interfere with the test efficacy of the polypeptide; a (C.sub.1 --C.sub.12)alkyl group, preferably a (C.sub.1 --C.sub.6)alkyl group; a (C.sub.1 --C.sub.12)alkyl group substituted by one or more halogen atoms, (C.sub.1 --C.sub.4)alkoxy groups, hydroxy groups, acyloxy groups, preferably (C.sub.1 --C.sub.4)alkanoyloxy or benzoyloxy, polyalkoxyalkyl groups, phenyl groups, or similar substituents which will not interfere with the test efficacy of the polypeptide; a (C.sub.1 --C.sub.12)alkoxy group, preferably a (C.sub.1 --C.sub.6)alkoxy group; an aryloxy group having up to 10 carbon atoms; or a divalent alkylene group having up to 6 carbon atoms, in which case the formula would be written as R(--CO A.sub.n --NHR'CO--B.sub.m --NHZ).sub.2 or, when the blocking group is derived from oxalic acid, as (CO--A.sub.n --NHR'CO--B.sub.m --NHZ).sub.2 Nhr'co is the amino acid linkage derived from L-phenylalanine, L-tyrosine, L-leucine, L-methionine, L-tryptophan, L-arginine, or L-lysine; Z is a group of the formula ##SPC1## Wherein R" is a hydroxy group, a (C.sub.1 --C.sub.4)alkoxy group, a (C.sub.1 --C.sub.4)alkoxyalkoxy group, a (C.sub.1 --C.sub.8)aminoalkoxy group, an amino group, a (C.sub.1 --C.sub.4)monoalkylamino group, a (C.sub.1 --C.sub.4)dialkylamino group, a group of the formula --NHCH.sub.2 COR", or a salt, such as the sodium, potassium, or ammonium salt, of the group in which R" is a hydroxy group; Y is a group of the formula --CO-- or --SO.sub.2 --; X is a hydroxy group, a (C.sub.1 --C.sub.4)alkyl group, a halogen atom, a (C.sub.1 --C.sub.4)alkoxy group, or a similar substituent which will not interfere with the test efficacy of the polypeptide; and n' is 0, 1, or 2; A and B are the residues of low molecular weight amino acids, such as glycyl, alanyl, glycylglycyl, and the like, and n and m are 0, 1, or 2.
Inventor(s): De Benneville; Peter L. (Philadelphia, PA)
Assignee: Rohm and Haas Company (Philadelphia, PA)
Filing Date:Dec 12, 1973
Application Number:05/424,020
Claims:1. A compound of the formula

RCO--A.sub.n --NHR'CO--B.sub.m --NHZ

wherein R is a hydrogen atom; a phenyl group; a phenyl group substituted with one or more halogen atoms, (C.sub.1 --C.sub.4)alkyl groups, hydroxy groups, (C.sub.1 --C.sub.4)alkoxy groups, (C.sub.1 --C.sub.4)alkanoyloxy groups, or (C.sub.1 --C.sub.4)alkoxycarbonyl groups; a (C.sub.1 --C.sub.12)alkyl group; a (C.sub.1 --C.sub.12)alkyl group substituted with one or more halogen atoms, (C.sub.1 --C.sub.4)alkoxy groups, hydroxy groups, (C.sub.1 --C.sub.4)-- alkanoyloxy groups, polyalkoxyalkyl groups, or phenyl groups; a (C.sub.1 --C.sub.12)alkoxy group; an aralkoxy group of up to 10 carbon atoms; or a divalent alkylene group having up to 6 carbon atoms;

Nhr'co is an amino acid linkage derived from L-phenylalanine, L-tyrosine, L-leucine; L-methionine, L-tryptophan, L-arginine, or L-lysine;

Z is a group of the formula ##SPC3##

wherein

R" is a hydroxy group, a (C.sub.1 --C.sub.4)alkoxy group, a (C.sub.1 --C.sub.4)alkoxyalkoxy group, an amino group, a (C.sub.1 --C.sub.4)monoalkylamino group, a (C.sub.1 --C.sub.4)dialkylamino group, a group of the formula --NHCH.sub.2 COR", or a salt of the group in which R" is a hydroxy group;

X is a hydroxy group, a (C.sub.1 --C.sub.4)alkyl group, a halogen atom, or a (C.sub.1 --C.sub.4)alkoxy group; and

n' is 0, 1, or 2;

A and B are the residues of low molecular weight amino acids selected from the group consisting of glycyl, alanyl, and glycylglycyl; and

m and n are 0, 1, or 2.

2. A compound according to claim 1 wherein n and m are zero.

3. A compound according to claim 2 wherein R is a phenyl group.

4. A compound according to claim 2 wherein R is a (C.sub.1 --C.sub.4)alkyl group.

5. A compound according to claim 2 wherein R is a (C.sub.1 --C.sub.4)alkoxy group.

6. A compound according to claim 2 wherein NHR'CO is phenylalanyl, tyrosyl, or tryptophyl.

7. A compound according to claim 6 wherein R" is an amino group.

8. A compound according to claim 7 wherein the compound is N-benzoyl-L-phenylalanyl sulfanilamide.

9. A compound according to claim 7 wherein the compound is N-benzoyl-L-tyrosylsulfanilamide.

10. A compound according to claim 2 wherein the compound is N-benzoyl-L-tyrosyl-p-aminobenzene sulfonic acid, its sodium salt, or its ammonium salt.

11. A compound according to claim 6 wherein R" is an amino group, a (C.sub.1 --C.sub.4)alkoxy group, a hydroxy group or the sodium or ammonium salt of the group in which R" is a hydroxy group.
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