Boronic ester and acid compounds, synthesis and uses
First Claim
Patent Images
1. A compound having the formula:
- ##STR51## or a pharmaceutically acceptable salt thereof;
wherein P is an amino protecting group;
A is 1;
B1 is CH;
X1 is --C(O)--NH--;
X2 is --C(O)--NH--;
R is hydrogen or alkyl;
R1 is hydrogen, C1-8 alkyl, C3-10 cycloalkyl, C6-10 aryl, or --CH2 --R5, where the ring portion of said aryl can be optionally substituted;
R2 is naphthylmethyl, pyridylmethyl or quinolinylmethyl;
R3 is C4 alkyl;
R5 is one of C6-10 aryl, C6-10 ar(C1-6)alkyl, C1-6 alk(C6-10)aryl, C3-10 cycloalkyl, C1-8 alkoxy or --W--R6, where W is a chalcogen and R6 is alkyl, where the ring portion of any of said aryl, aralkyl, or alkaryl can be optionally substituted; and
Z1 and Z2 are independently one of hydroxy, alkoxy, or aryloxy, or together Z1 and Z2 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 carbon atoms and, optionally, a heteroatom or heteroatoms which can be N, S, or O.
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Abstract
Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
152 Citations
12 Claims
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1. A compound having the formula:
- ##STR51## or a pharmaceutically acceptable salt thereof;
wherein P is an amino protecting group;A is 1; B1 is CH; X1 is --C(O)--NH--; X2 is --C(O)--NH--; R is hydrogen or alkyl; R1 is hydrogen, C1-8 alkyl, C3-10 cycloalkyl, C6-10 aryl, or --CH2 --R5, where the ring portion of said aryl can be optionally substituted; R2 is naphthylmethyl, pyridylmethyl or quinolinylmethyl; R3 is C4 alkyl; R5 is one of C6-10 aryl, C6-10 ar(C1-6)alkyl, C1-6 alk(C6-10)aryl, C3-10 cycloalkyl, C1-8 alkoxy or --W--R6, where W is a chalcogen and R6 is alkyl, where the ring portion of any of said aryl, aralkyl, or alkaryl can be optionally substituted; and Z1 and Z2 are independently one of hydroxy, alkoxy, or aryloxy, or together Z1 and Z2 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 carbon atoms and, optionally, a heteroatom or heteroatoms which can be N, S, or O. - View Dependent Claims (2, 3, 4, 5, 6, 8, 9, 10, 11, 12)
- ##STR51## or a pharmaceutically acceptable salt thereof;
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7. N-Acetyl-L-leucine-β
- -(1-naphthyl)-L-alanine-L-leucine boronic acid or a pharmaceutically acceptable salt or boronate ester therof.
Specification