Claims Analysis
Total Claims: 31
Claim 1
Independent Claim
362 words
A pharmacologically active oligomeric peptide derivative which comprises (1) a polylysyl chain P which optionally includes branched chains formed of alanyl residues attached to the chain through the amino groups of lysyl groups in the chain not linked in the forming of said chain and (2) covalently linked to amino groups not linked into said chain P, muramyl peptide groups which comprise a glucopyranoside ring and linked thereto a peptide chain which chain comprises aminoacyl residues, the first of said aminoacyl residues being of an amino acid of the D-series and the second amino acyl residue being of D-glutamic acid, said oligomeric peptide derivative having the formula: ##STR6## in which the substituents R, R 1 , R 2 , R 4 , R 6 , X, Y, Z, x and n are defined as follows: R is either a hydrogen atom or alkyl group having from 1 to 4 carbon atoms, R 1 is hydrogen or alkyl having at most 4 carbon atoms or a simple or substituted aryl or alkyl-aryl having at most 10 carbon atoms, R 2 is hydrogen or alkyl, aryl or alkyl-aryl optionally substituted and having at most 22 carbon atoms, R 4 is hydrogen or acyl having at most 4 carbons, R 6 is hydrogen, a saturated or unsaturated acyl optionally branched having from 1 to about 90 carbon atoms and optionally having groups selected from the class consisting of hydroxyl, carboxyl, amino, cyclopropyl and methoxyl, X is an aminoacyl residue of the (D) series, selected from the class consisting of alanyl, arginyl, asparagyl, aspartyl, cystenyl, glutaminyl, glutamyl, histidyl, hydroxyprolyl, isoleucyl, leucyl, lysyl, methionyl, ornithyl, phenylalanyl, prolyl, seryl, threonyl, tryptophanyl, tyrosyl and valyl, Y is either --OH, or alkoxy having from 1 to 10 carbon atoms or --NH 2 group, of which one or the two hydrogens is optionally substituted by an alkyl having from 1 to 10 carbon atoms, Z is from 1 to 3 L- or D- identical or different aminoacyl residues, x is zero or an integer of 1 through 3, and n is a an integer other than zero, which integer is not more than the number of amino groups of chain P.
Claim 2
Dependent Claim
362 words
A pharmacologically active oligomeric peptide derivative which comprises (1) a polylysyl chain P which optionally includes branched chains formed of alanyl residues attached to the chain through the amino groups of lysyl groups in the chain not linked in the forming of said chain and (2) covalently linked to amino groups not linked into said chain P, muramyl peptide groups which comprise a glucopyranoside ring and linked thereto a peptide chain which chain comprises aminoacyl residues, the first of said aminoacyl residues being of an amino acid of the D-series and the second amino acyl residue being of D-glutamic acid, said oligomeric peptide derivative having the formula: ##STR6## in which the substituents R, R 1 , R 2 , R 4 , R 6 , X, Y, Z, x and n are defined as follows: R is either a hydrogen atom or alkyl group having from 1 to 4 carbon atoms, R 1 is hydrogen or alkyl having at most 4 carbon atoms or a simple or substituted aryl or alkyl-aryl having at most 10 carbon atoms, R 2 is hydrogen or alkyl, aryl or alkyl-aryl optionally substituted and having at most 22 carbon atoms, R 4 is hydrogen or acyl having at most 4 carbons, R 6 is hydrogen, a saturated or unsaturated acyl optionally branched having from 1 to about 90 carbon atoms and optionally having groups selected from the class consisting of hydroxyl, carboxyl, amino, cyclopropyl and methoxyl, X is an aminoacyl residue of the (D) series, selected from the class consisting of alanyl, arginyl, asparagyl, aspartyl, cystenyl, glutaminyl, glutamyl, histidyl, hydroxyprolyl, isoleucyl, leucyl, lysyl, methionyl, ornithyl, phenylalanyl, prolyl, seryl, threonyl, tryptophanyl, tyrosyl and valyl, Y is either --OH, or alkoxy having from 1 to 10 carbon atoms or --NH 2 group, of which one or the two hydrogens is optionally substituted by an alkyl having from 1 to 10 carbon atoms, Z is from 1 to 3 L- or D- identical or different aminoacyl residues, x is zero or an integer of 1 through 3, and n is a an integer other than zero, which integer is not more than the number of amino groups of chain P.
Claim 3
Dependent Claim
30 words
The oligomeric peptide derivative of claim 1 in which the chain P has branched peptide groups constituted of alanyl residues linked through the amino groups of the amino acyl residues.
Claim 4
Dependent Claim
34 words
The oligomeric peptide derivative of claim 2 in which the aminoacyl residues of the peptide groups are selected from amino acids of the group consisting of alanyl, alpha-aminobutyric acid, valyl, leucyl, isoleucyl or prolyl.
Claim 5
Dependent Claim
15 words
The oligomeric peptide derivative of claim 2 in which P consists of a polylysine chain.
Claim 6
Dependent Claim
15 words
The oligomeric peptide derivative of claim 1 in which the polymer is a L-lysyl polymer.
Claim 7
Dependent Claim
24 words
The oligomeric peptide derivative of claim 5 in which n is one integer less than the number of lysyl groups of the L-lysyl polymer.
Claim 8
Dependent Claim
24 words
The oligomeric peptide derivative of claim 1 in which the alnyl residues of the branched chains are of both the D- and L- series.
Claim 9
Dependent Claim
19 words
The oligomeric peptide derivative of claim 1 in which P includes L-polylysyl having linked thereto D- and/or L- alanyl.
Claim 10
Dependent Claim
43 words
The oligomeric peptide derivative of claim 8 in which the oligomeric peptide has an average molecular weight of 80,000 and the ratio of L-lysyl of P to the D- and L- alanyl of the branched chains linked thereto is between 1/10 to 1/30.
Claim 11
Dependent Claim
19 words
The oligomeric peptide derivative of claim 1 which has an average molecular weight from about 50,000 to about 250,000.
Claim 12
Dependent Claim
10 words
The oligomeric peptide derivative of claim 1 which is metabolizable.
Claim 13
Dependent Claim
26 words
The oligomeric peptide derivative of claim 1 wherein Y is --NH 2 , --OCH 3 , --OC 4 H 9 or OC 10 H 21 .
Claim 14
Dependent Claim
31 words
The oligomeric peptide derivative of claim 1 wherein x is 1 or 2 and Z is an aminoacyl residue selected from the group consisting of alanyl, glycyl, valyle, leucyle and isoleucyle.
Claim 15
Dependent Claim
13 words
The oligomeric peptide derivative of claim 1 wherein R is --CH 3 .
Claim 16
Dependent Claim
25 words
The oligomeric peptide derivative of claim 1 wherein R 1 , R 4 and R 6 are hydrogen and R 2 is --CH 3 .
Claim 17
Dependent Claim
14 words
The oligomeric peptide derivative of claim 9 wherein the muranyl peptide group are N-acetyl-muramyl-D-alanyl-D-isoglutaminyl.
Claim 18
Dependent Claim
20 words
The oligomeric peptide derivative of claim 1 wherein X is selected from the group consisting of D-prolyl, D-threonyl, and D-valyl.
Claim 19
Dependent Claim
14 words
The oligomeric peptide derivative of claim 1 wherein x is from 0 to 3.
Claim 20
Dependent Claim
13 words
The oligomeric peptide derivative of claim 1 wherein Y is --NH 2 .
Claim 21
Dependent Claim
30 words
The oligomeric peptide derivative of claim 1 wherein Y is selected from the group consisting of --OCH 3 , --OC 4 H 9 , or --OC 10 H 21 .
Claim 22
Dependent Claim
31 words
The oligomeric peptide derivative of claim 1 wherein R 2 is --CH 3 , R 1 , R 4 and R 6 are each hydrogen and R is --CH 3 .
Claim 23
Dependent Claim
15 words
The oligomeric peptide derivative of claim 1 wherein R is --C 2 H 5 .
Claim 24
Dependent Claim
22 words
The oligomeric peptide derivative of claim 1 wherein at least one of R 1 , R 4 and R 6 is hydrogen.
Claim 25
Dependent Claim
12 words
The oligomeric peptide derivative of claim 1 wherein R 4 is acetyl.
Claim 26
Dependent Claim
26 words
The oligomeric peptide derivative of claim 1 wherein R 6 is selected from the group consisting of acetyl of 1 to 4 carbons, mycolyl and corynomycolyl.
Claim 27
Dependent Claim
36 words
The oligomeric peptide derivative of claim 1 wherein R 1 , R 4 , and R 6 are hydrogen; R and R 2 are --CH 3 , X is D-alanyl and Y is --NH 2 .
Claim 28
Dependent Claim
10 words
The oligomeric peptide of claim 1 wherein X is D-alanyl.
Claim 29
Dependent Claim
62 words
A pharmaceutical composition for enhancing the resistance of a host against pathogens which comprises an effective amount of a biologically active oligomeric peptide derivative of any one of claims 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26 or 27 and a pharmaceutically acceptable carrier.
Claim 30
Independent Claim
65 words
The method for enhancing the resistance of a host against pathogens which comprises administering to said host an effective amount of a biologically active oligomeric peptide derivative of any one of claims 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, or 27 in a biologically acceptable carrier.
Claim 31
Dependent Claim
10 words
The oligomeric peptide derivative of claim 10 which is multi-poly-L-lysine.