Intermediates for preparing peptide boronic acid inhibitors of trypsin-like proteases
First Claim
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1. A compound of the formula ##STR10## wherein Y3 is 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, wherein the oxygen atoms of two of said hydroxy groups are bonded to B, said chain or ring comprising 1 to about 20 carbon atoms and optionally a heteroatom which can be N, S or O;
- R3 is a substituted alkyl selected from the group consisting of --(CH2)z -W1, --CH(CH3)--(CH2)2 -W1, --CH2 --CH(CH3)--CH2 -W1, --(CH2)2 --C(CH3)2 -W1 and --CH2)2 --CH(CH3)2 -W1 ;
W and W1, independently, are Cl or Br; and
z is 3 to 5.
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Abstract
Intermediates for the preparation of 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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2 Claims
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1. A compound of the formula ##STR10## wherein Y3 is 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, wherein the oxygen atoms of two of said hydroxy groups are bonded to B, 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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R3 is a substituted alkyl selected from the group consisting of --(CH2)z -W1, --CH(CH3)--(CH2)2 -W1, --CH2 --CH(CH3)--CH2 -W1, --(CH2)2 --C(CH3)2 -W1 and --CH2)2 --CH(CH3)2 -W1 ; W and W1, independently, are Cl or Br; and z is 3 to 5. - View Dependent Claims (2)
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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)Cintins, Marianne M.
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Assistant Examiner(s)PAGE, MARGARET
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Application NumberUS07/852,023Time in Patent Office575 DaysField of Search558/288, 558/289US Class Current558/288CPC Class CodesC07F 5/025 Boronic and borinic acid co...C07K 5/00 Peptides containing up to f...
