Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
374 words
A compound selected from the group consisting of those having (i) the structural formula wherein X is O, S, or NR 5 ; R 1 S is the residue of any biologically active agent R 1 SH ; R 2 is selected from the group consisting of straight or branched chain alkyl having from 1 to 20 carbon atoms; aryl having from 6 to 10 carbon atoms; cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 2 to 20 carbon atoms; cycloalkenyl having from 4 to 8 carbon atoms; alkynyl having from 2 to 20 carbon atoms; aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweracyloxyalkyl, and carboxyalkyl, wherein alkyl, aryl, alkenyl and alkynyl are as defined above saturated or unsaturated monoheterocyclic or polyheterocyclic, or fused heterocyclic, either directly bonded to the carbonyl function or linked thereto via an alkylene bridge, containing from 1 to 3 of any one or more of the hetero atoms N, S or O in each heterocyclic ring thereof and each such ring being from 3- to 8- membered; and mono- or polysubstituted derivatives of the above, each of said substituents being selected from the group consisting of lower alkyl, lower alkoxy, lower acyl, lower acyloxy, lower acyl, lower acyloxy, halo, haloloweralkyl, cyano, carbethoxy, loweralkylthio, amino, nitro, loweralkylamino, diloweralkylamino, carboxyl, carbamyl, loweralkylcarbamyl, and wherein R 4 is hydrogen or alkyl having from 1 to 10 carbons; R 3 is hydrogen, R 2 , lower acyl, cyano, haloloweralkyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl, -CH 2 ONO 2 and -CH 2 OCOR 2 ; R 5 is hydrogen or lower alkyl; and further wherein R 2 and R 3 may be taken together to form a cyclizing moiety selected from the group consisting of with the provision that when R 1 S is the residue of a sulfur containing amino acid, then x cannot be NR 5 ; (ii) the structural formula (I) wherein R 2_ C - is the residue of any naturally occurring protein amino acid, the residue of any N-substituted naturally occurring amino acid, which N-substituent is lower alkyl or any amino acid protective group cleavable via hydrogenolysis or hydrolysis, or the residue of an N,N-lower dialkyl or C -C cycloalkylamino acid; and (iii) the non-toxic, pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
374 words
A compound selected from the group consisting of those having (i) the structural formula wherein X is O, S, or NR 5 ; R 1 S is the residue of any biologically active agent R 1 SH ; R 2 is selected from the group consisting of straight or branched chain alkyl having from 1 to 20 carbon atoms; aryl having from 6 to 10 carbon atoms; cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 2 to 20 carbon atoms; cycloalkenyl having from 4 to 8 carbon atoms; alkynyl having from 2 to 20 carbon atoms; aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweracyloxyalkyl, and carboxyalkyl, wherein alkyl, aryl, alkenyl and alkynyl are as defined above saturated or unsaturated monoheterocyclic or polyheterocyclic, or fused heterocyclic, either directly bonded to the carbonyl function or linked thereto via an alkylene bridge, containing from 1 to 3 of any one or more of the hetero atoms N, S or O in each heterocyclic ring thereof and each such ring being from 3- to 8- membered; and mono- or polysubstituted derivatives of the above, each of said substituents being selected from the group consisting of lower alkyl, lower alkoxy, lower acyl, lower acyloxy, lower acyl, lower acyloxy, halo, haloloweralkyl, cyano, carbethoxy, loweralkylthio, amino, nitro, loweralkylamino, diloweralkylamino, carboxyl, carbamyl, loweralkylcarbamyl, and wherein R 4 is hydrogen or alkyl having from 1 to 10 carbons; R 3 is hydrogen, R 2 , lower acyl, cyano, haloloweralkyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl, -CH 2 ONO 2 and -CH 2 OCOR 2 ; R 5 is hydrogen or lower alkyl; and further wherein R 2 and R 3 may be taken together to form a cyclizing moiety selected from the group consisting of with the provision that when R 1 S is the residue of a sulfur containing amino acid, then x cannot be NR 5 ; (ii) the structural formula (I) wherein R 2_ C - is the residue of any naturally occurring protein amino acid, the residue of any N-substituted naturally occurring amino acid, which N-substituent is lower alkyl or any amino acid protective group cleavable via hydrogenolysis or hydrolysis, or the residue of an N,N-lower dialkyl or C -C cycloalkylamino acid; and (iii) the non-toxic, pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
46 words
A compound as defined by Claim 1 wherein the R 1 S residue is selected from the group consisting of N-(2-methyl-3-thiopropionyl)proline and its ester, amide, mono- or di-loweralkyl- amide, N-acetyl cystein, penicillamine, cysteine methyl ester, dimercaprol, glutathione, 2-thiopyridine N-oxide, thiopental, 2-thiouracil, 6-mercaptopurine, 6-thio-guanine, 6-thioguanosine, 6-mercaptopurineriboside, methimazole.
Claim 4
Dependent Claim
18 words
A compound as defined by Claim 2 wherein R 1 S residue is N-(2-methyl-3-thiopropionyl)- ' proline lower alkylester.
Claim 5
Dependent Claim
14 words
A compound as defined by Claim 1, wherein the R 1 S residue is
Claim 8
Dependent Claim
24 words
A compound as defined by any one of claims 1 to 4 wherein R 2 is aryl having from 6 to 10 carbon atoms.
Claim 9
Dependent Claim
17 words
A compound as defined by any one of claims 1 to 5 wherein R 3 is trichloromethyl.
Claim 10
Dependent Claim
24 words
A therapeutically effective composition of matter comprising an effective amount of a compound as defined by Claim 1, and a pharmaceutically effective carrier therefor.
Claim 11
Dependent Claim
49 words
A process for the preparation of a compound according to claim 1 comprising reacting a mercapto compound of the formula: with a compound of the formula wherein Z is a leaving group, and R 1 , R 2 , R 3 and X are as defined in Claim 1.