Back to results
US 2013/0172340 A1Published application
Substituted 2-(9h-purin-9-yl) acetic acid analogues as inhibitors of stat3
AssigneeUniversity of Central Flordia Research Foundation, Inc.
InventorsJames Turkson, Patrick Gunning
Life of this patent
Estimating the term…
Abstract
In one aspect, the invention relates to substituted purine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Claims20
A compound having a structure represented by a formula:
- wherein R1 is selected from H and (CH2)mC═OR5, wherein m is an integer from 0-3;
- wherein R5 is selected from OR6 and NR7R8;
- wherein R6 is selected from hydrogen and C1-C8 alkyl;
- wherein each of R7 and R8 is independently selected from hydrogen and C1-C8 alkyl;
- wherein R2 is selected from halogen, OR9, and NR10R11;
- wherein R9 is an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, (CH2)nR12, and Ar1;
- wherein n is an integer from 0-3;
- wherein R12 is an optionally substituted group selected from Ar1, C3-C6 cycloalkyl and C3-C6 heterocycloalkyl;
- wherein Ar1 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R10 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, (CH2)pR13, and Ar2;
- wherein n is an integer from 0-3;
- wherein R13 is an optionally substituted group selected from Ar2, C3-C6 cycloalkyl and C3-C6 heterocycloalkyl;
- wherein Ar2 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R11 is selected from hydrogen and C1-C8 alkyl;
- wherein R3 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, (CH2)qR14, and C═O(CH2)qR14;
- wherein q is an integer from 0-3;
- wherein R14 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, and Ar3;
- wherein Ar3 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R4 is selected from hydrogen and C═OOR15;
- wherein R15 is selected from hydrogen and optionally substituted C1-C8 alkyl;
- wherein R3 and R4 are optionally covalently bonded and, together with the intermediate carbon, comprise an optionally substituted 3- to 7-membered heterocycloalkyl;
- and
- wherein R10 and R11 are optionally covalently bonded and, together with the intermediate carbon, comprise an optionally substituted 3- to 7-membered heterocycloalkyl;
- or a pharmaceutically acceptable salt, hydrate, solvate, or polymorph thereof.
21 more elements
A method for the treatment of a disorder associated with STAT activity in a mammal comprising the step of administering to the mammal a therapeutically effective amount of a compound having a structure represented by a formula:
- wherein R1 is selected from H and (CH2)mC═OR5, wherein m is an integer from 0-3;
- wherein R5 is selected from OR6 and NR7R8;
- wherein R6 is selected from hydrogen and C1-C8 alkyl;
- wherein each of R7 and R8 is independently selected from hydrogen and C1-C8 alkyl;
- wherein R2 is selected from halogen, OR9, and NR10R11;
- wherein R9 is an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, (CH2)nR12, and Ar1;
- wherein n is an integer from 0-3;
- wherein R12 is an optionally substituted group selected from Ar1, C3-C6 cycloalkyl and C3-C6 heterocycloalkyl;
- wherein Ar1 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R10 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, (CH2)pR13, and Ar2;
- wherein n is an integer from 0-3;
- wherein R13 is an optionally substituted group selected from Ar2, C3-C6 cycloalkyl and C3-C6 heterocycloalkyl;
- wherein Ar2 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R11 is selected from hydrogen and C1-C8 alkyl;
- wherein R3 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, (CH2)qR14, and C═O(CH2)qR14;
- wherein q is an integer from 0-3;
- wherein R14 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, and Ar3;
- wherein Ar3 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R4 is selected from hydrogen and C═OOR15;
- wherein R15 is selected from hydrogen and optionally substituted C1-C8 alkyl;
- wherein R3 and R4 are optionally covalently bonded and, together with the intermediate carbon, comprise an optionally substituted 3- to 7-membered heterocycloalkyl;
- and
- wherein R10 and R11 are optionally covalently bonded and, together with the intermediate carbon, comprise an optionally substituted 3- to 7-membered heterocycloalkyl;
- or a pharmaceutically acceptable salt, hydrate, solvate, or polymorph thereof.
21 more elements
A method for inhibiting STAT activity in at least one cell, comprising the step of contacting the at least one cell with an effective amount of least one compound having a structure represented by a formula:
- wherein R1 is selected from H and (CH2)mC═OR5, wherein m is an integer from 0-3;
- wherein R5 is selected from OR6 and NR7R8;
- wherein R6 is selected from hydrogen and C1-C8 alkyl;
- wherein each of R7 and R8 is independently selected from hydrogen and C1-C8 alkyl;
- wherein R2 is selected from halogen, OR9, and NR10R11;
- wherein R9 is an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, (CH2)nR12, and Ar1;
- wherein n is an integer from 0-3;
- wherein R12 is an optionally substituted group selected from Ar1, C3-C6 cycloalkyl and C3-C6 heterocycloalkyl;
- wherein Ar1 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R10 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, (CH2)pR13, and Ar2;
- wherein n is an integer from 0-3;
- wherein R13 is an optionally substituted group selected from Ar2, C3-C6 cycloalkyl and C3-C6 heterocycloalkyl;
- wherein Ar2 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R11 is selected from hydrogen and C1-C8 alkyl;
- wherein R3 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, (CH2)qR14, and C═O(CH2)qR14;
- wherein q is an integer from 0-3;
- wherein R14 is selected from hydrogen and an optionally substituted group selected from C1-C8 alkyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, and Ar3;
- wherein Ar3 is selected from an optionally substituted monocyclic aryl and monocyclic heteroaryl;
- wherein R4 is selected from hydrogen and C═OOR15;
- wherein R15 is selected from hydrogen and optionally substituted C1-C8 alkyl;
- wherein R3 and R4 are optionally covalently bonded and, together with the intermediate carbon, comprise an optionally substituted 3- to 7-membered heterocycloalkyl;
- and
- wherein R10 and R11 are optionally covalently bonded and, together with the intermediate carbon, comprise an optionally substituted 3- to 7-membered heterocycloalkyl;
- or a pharmaceutically acceptable salt, hydrate, solvate, or polymorph thereof.
21 more elements
Dependencies are inferred from the claim text.