β- and γ-diketones and γ-hydroxyketones as
The present invention discloses β-diketones, γ-diketones or γ-hydroxyketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
1. A compound or pharmaceutically acceptable salt thereof having the structure of Formula I:
wherein R 1 is a substituted or unsubstituted heteroaryl, wherein the heteroaryl is selected from the group consisting of
with the proviso that a carbon atom of the R 1 heteroaryl is attached to the carbonyl;
R 2 is a substituted or unsubstituted
and
R 3 , R 4 , R 3 and R 6 are H.
2. The compound of claim 1 , wherein R 1 is a substituted or unsubstituted
3. The compound of claim 1 , wherein R 1 is a substituted or unsubstituted
4. The compound of claim 1 , wherein R 1 is a substituted or unsubstituted
5. The compound of claim 1 , wherein R 1 is a substituted or unsubstituted
6. The compound of claim 1 , wherein R 2 is an unsubstituted
7. A compound or pharmaceutically acceptable salt thereof having the structure of Formula I:
wherein R 1 is an unsubstituted heteroaryl, wherein the heteroaryl is selected from the group consisting of
with the proviso that a carbon atom of the R 1 heteroaryl is attached to the carbonyl;
R 2 is a substituted or unsubstituted
and
R 3 , R 4 , R 5 and R 6 are H.
8. A compound or pharmaceutically acceptable salt thereof having the structure of Formula I:
wherein R 1 is an unsubstituted heteroaryl, wherein the heteroaryl is selected from the group consisting of
with the proviso that a carbon atom of the R 1 heteroaryl is attached to the carbonyl;
R 2 is an unsubstituted
and
R 3 , R 4 , R 5 and R 6 are H.
9. A pharmaceutical composition comprising a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof having the structure of Formula I:
wherein R 1 is a substituted or unsubstituted heteroaryl, wherein the heteroaryl is selected from the group consisting of
with the proviso that a carbon atom of the R 1 heteroaryl is attached to the carbonyl;
R 2 is a substituted or unsubstituted
and
R 3 , R 4 , R 5 and R 6 are H;
and a pharmaceutically acceptable excipient.
10. The pharmaceutical composition of claim 9 , wherein R 1 is a substituted or unsubstituted
11. The pharmaceutical composition of claim 9 , wherein R 1 is a substituted or unsubstituted
12. The pharmaceutical composition of claim 9 , wherein R 1 is a substituted or unsubstituted
13. The pharmaceutical composition of claim 9 , wherein R 1 is a substituted or unsubstituted
14. The pharmaceutical composition of claim 9 , wherein R 2 is an unsubstituted