Nonpeptide insulin receptor agonists
AssigneeTerrapin Technologies, Inc.
InventorsRichard Sportsman, Hugo O. Villar, Lawrence M. Kauvar, Wayne R. Spevak
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Abstract
Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula ##STR1## wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.
Claims25
A method to modulate the kinase activity of insulin receptor which method comprises contacting said insulin receptor or the kinase portion thereof with a compound of the formula ##STR6## wherein each A is independently a proton-accepting substituent;
- each R is independently a noninterfering substituent;
- each n is independently 0, 1, or 2;
- and
- each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--;
- said compound provided in an amount effective to modulate said kinase activity.
A method to potentiate the insulin activation of insulin receptor which method comprises contacting said insulin receptor or the kinase portion thereof with insulin and with a compound of the formula ##STR9## wherein each A is independently a proton-accepting substituent;
- each R is independently a noninterfering substituent;
- n is 0, 1, or 2;
- and
- each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--;
- said compound provided in an amount effective to potentiate said insulin activation.
A method to potentiate the stimulation by insulin of cellular glucose uptake which method comprises contacting cells displaying the insulin receptor with insulin and with a compound of the formula ##STR12## wherein each A is independently a proton-accepting substituent;
- each R is independently a noninterfering substituent;
- n is 0, 1, or 2;
- and
- each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--;
- said compound provided in an amount effective to potentiate said glucose uptake.
A method to stimulate the uptake of glucose in cells displaying the insulin receptor which method comprises contacting said cells with a compound of the formula ##STR15## wherein each A is independently a proton-accepting substituent;
- each R is independently a noninterfering substituent;
- n is 0, 1, or 2;
- and
- each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--;
- said compound provided in an amount effective to stimulate glucose uptake.
A method to lower blood glucose in a diabetic subject which method comprises administering to said subject a compound of the formula ##STR18## wherein each A is independently a proton-accepting substituent;
- each R is independently a noninterfering substituent;
- n is 0, 1, or 2;
- and
- each linker is independently an isostere of --NHCONH-- or of --N.dbd.N-- or of --NHCO--;
- said compound provided in an amount effective to lower blood glucose.
Dependencies are inferred from the claim text.