Back to results
US 6,066,730 AGranted
Boronic ester and acid compounds, synthesis and uses
AssigneeProScript, Inc.
InventorsJulian Adams, Yu-Ting Ma, Ross Stein, Matthew Baevsky, Louis Grenier, Louis Plamondon
Life of this patent
Estimating the term…
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.
Claims12
A compound having the formula:
- ##STR51## or a pharmaceutically acceptable salt thereof;
- wherein P is an amino protecting group;
- A is 1;
- B.sup.1 is CH;
- X.sup.1 is --C(O)--NH--;
- X.sup.2 is --C(O)--NH--;
- R is hydrogen or alkyl;
- R.sup.1 is hydrogen, C.sub.1-8 alkyl, C.sub.3-10 cycloalkyl, C.sub.6-10 aryl, or --CH.sub.2 --R.sup.5, where the ring portion of said aryl can be optionally substituted;
- R.sup.2 is naphthylmethyl, pyridylmethyl or quinolinylmethyl;
- R.sup.3 is C.sub.4 alkyl;
- R.sup.5 is one of C.sub.6-10 aryl, C.sub.6-10 ar(C.sub.1-6)alkyl, C.sub.1-6 alk(C.sub.6-10)aryl, C.sub.3-10 cycloalkyl, C.sub.1-8 alkoxy or --W--R.sup.6, where W is a chalcogen and R.sup.6 is alkyl, where the ring portion of any of said aryl, aralkyl, or alkaryl can be optionally substituted;
- and
- Z.sup.1 and Z.sup.2 are independently one of hydroxy, alkoxy, or aryloxy, or together Z.sup.1 and Z.sup.2 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.
10 more elements
N-Acetyl-L-leucine-.beta.-(1-naphthyl)-L-alanine-L-leucine boronic acid or a pharmaceutically acceptable salt or boronate ester therof.
Dependencies are inferred from the claim text.