US 6,784,205 B2 · Compounds that modulate the activity of PTP-1B and TC-PTP

Abstract

The present invention relates to a new and improved method for treating diabetes and or its associated complications by modulating the activity of protein tryosin phosphatase 1B (“PTP-1B”). The inventive compounds modulate the activity PTP-1B by binding to a novel binding site referred herein as the PTP-1B exosite that is distal to the active site of PTP-1B. The present invention also relates to a new and improved method of treating immune system disorders by modulating the activity of T-cell protein tyrosine phosphatase (“TC-PTP”). The inventive compound modulate the activity of TC-PTP by binding to a novel binding site referred herein as the TC-PTP exosite that is distal to the active site of PTP-1B.

Claims24

Dependent claims

A compound having the structure

wherein:
R1 is hydrogen, methyl, ethyl, propyl;
R2 is hydrogen, —S(O2)R3, —NHC(═O)R3, —NHC(═O)CH2(C═O)OR3, —S(O2)NR4R5, or —NR4S(O2)R3 where R3 is C1-C5 alkyl, R4 is hydrogen, C4-C5 alkyl, unsubstituted cyclic moiety, or substituted cyclic moiety, and R5 is either hydrogen or R5 and R4 together form an unsubstituted cyclic moiety or a substituted cyclic moiety;
R6 is hydrogen or alternatively when R2 as —NR4S(O2)NR3, then R6 and R4 together form an unsubstituted cyclic moiety or substituted cyclic moiety;
and,
L is —NHS(O2)— or —S(O2)NR7CH2— where R7 is hydrogen or C4-C5 alkyl.

3 more elements

Dependencies are inferred from the claim text.

Compounds that modulate the activity of PTP-1B and TC-PTP

Life of this patent

Compounds that modulate the activity of PTP-1B and TC-PTP

Life of this patent

Abstract

Claims24