Compounds for stem cell differentiation
AssigneesSanford-Burnham Medical Research Institute, Human BioMolecular Research Institute, ChemRegen, Inc.
InventorsMARK MERCOLA, John Cashman, Marion Lanier, Erik Willems, Dennis Schade
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Abstract
Small molecule compounds and methods for stem cell differentiation are provided herein. An example of a class of compounds that may be used to practice the methods disclosed herein is represented by enantiomerically pure isomers of compounds of Formula I: or a chirally pure stereoisomer, pharmaceutically acceptable salt, or solvate thereof, wherein R1, R2, R3, R4, R5, R5′, R6, R6′, R7, R7′ are as described herein.
Claims24
A compound of Formula I:
- or a chirally pure stereoisomer, pharmaceutically acceptable salt or solvate thereof,
- wherein:
- R1 is independently hydrogen (C1-C6)alkyl or a moiety forming a salt;
- R2 is independently hydrogen or (C1-C6)alkyl;
- R3 is independently OR8 or NR13R13′;
- R4 is independently substituted or unsubstituted aryl, heteroalkyl, heterocycloalkyl, or heteroaryl substituted or unsubstituted pyridine, wherein phenyl or pyridine is optionally independently substituted with 1 to 3 R9 substituents;
- R5, R5′, R6, R6′, R7, and R7′ are each independently hydrogen or (C1-C6)alkyl;
- R8, R13, and R13′ are each independently hydrogen, (C1-C6)alkyl, (C3-C8)cycloalkyl, substituted or unsubstituted heterocyclyl, aryl, (C1-C6)alkylaryl, or (C1-C6)alkylNR10R10′;
- each R9 is independently hydrogen, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, cyclo(C1-C6)alkyl, substituted or unsubstituted phenyl, substituted or unsubstituted pyridine, substituted or unsubstituted indolyl;
- substituted or unsubstituted pyrrolidinyl, or substituted or unsubstituted piperidinyl, wherein phenyl, pyridine, indolyl, pyrrolidinyl and piperidinyl are each optionally independently substituted with hydrogen, halogen, or (C1-C6)alkyl;
- and
- R10 and R10′ are each independently hydrogen, (C1-C6)alkyl, aryl, or (C1-C6)alkylaryl.
A method for selectively inhibiting TGFb, comprising contacting TGFBR2 with a compound of structural Formula (I).
A method for the treatment of a disease or disorder associated with TGF, comprising administering to a subject in need thereof an effective amount of a compound of structural Formula (I).
Dependencies are inferred from the claim text.