Peptide boronic acid inhibitors of trypsin-like proteases
First Claim
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1. A compound of the formula ##STR10## wherein Y1 and Y2, independently, are --OH or F or, taken together, form a moiety derived from a dihydroxy compound having at least two hydroxy groups separated by at least two connecting atoms in a chain or ring, said chain or ring comprising 1 to about 20 carbon atoms and, optionally, a heteroatom which can be N, S, or O;
- R2 is a substituted alkyl selected from the group consisting of --(CH2)z --X, --CH(CH3)--(CH2)2 --X, --CH2 --CH(CH3)--CH2 --X, --(CH2)2 --C(CH3)--X, and --(CH2)2 CH(CH3)2 --X, where X is --NH2, --NH--C(NH)--NH2 or --S--C(NH)--NH2, and z is 3 to 5;
n, o, p, and q are 1;
A1, A2 and A3, independently, are amino acids of L- or D-configuration selected from the group consisting of Ala, Arg, Asn, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr and Val; and
R1 is a peptide comprised of 1 to about 20 amino acids, said peptide optionally containing an N-terminal protecting group;
or a physiologically acceptable salt thereof.
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Abstract
Peptides comprising C-terminal boronic acid derivatives of lysine, ornithine, and arginine, homoarginine and corresponding isothiouronium analogs thereof, are reversible inhibitors of trypsin-like serine proteases such as thrombin, plasma kallikrein and plasmin.
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Citations
34 Claims
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1. A compound of the formula ##STR10## wherein Y1 and Y2, independently, are --OH or F or, taken together, form a moiety derived from a dihydroxy compound having at least two hydroxy groups separated by at least two connecting atoms in a chain or ring, said chain or ring comprising 1 to about 20 carbon atoms and, optionally, a heteroatom which can be N, S, or O;
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R2 is a substituted alkyl selected from the group consisting of --(CH2)z --X, --CH(CH3)--(CH2)2 --X, --CH2 --CH(CH3)--CH2 --X, --(CH2)2 --C(CH3)--X, and --(CH2)2 CH(CH3)2 --X, where X is --NH2, --NH--C(NH)--NH2 or --S--C(NH)--NH2, and z is 3 to 5; n, o, p, and q are 1; A1, A2 and A3, independently, are amino acids of L- or D-configuration selected from the group consisting of Ala, Arg, Asn, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr and Val; and R1 is a peptide comprised of 1 to about 20 amino acids, said peptide optionally containing an N-terminal protecting group; or a physiologically acceptable salt thereof. - View Dependent Claims (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, 27, 28, 29, 30, 31, 32, 33, 34)
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Specification
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Current AssigneeBristol-Myers Squibb Pharma Company (Bristol-Myers Squibb Company)
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Original AssigneeThe Dupont Merck Pharmaceutical Company
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InventorsKettner, Charles A., Shenvi, Ashokkumar B.
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Primary Examiner(s)Ramsuer, Robert W.
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Assistant Examiner(s)AMBROSE, MICHAEL GEORGE
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Application NumberUS07/848,296Time in Patent Office547 DaysField of Search514/18, 530/330US Class Current514/12.2CPC Class CodesC07F 5/025 Boronic and borinic acid co...C07K 5/00 Peptides containing up to f...
