132980-20-2

Upstream product

• 24973-22-6 3-methoxy-4-methylbenzaldehyde 
• 134058-08-5 3-(3-methoxy-4-methylphenyl)-2-propenoic acid ethyl ester 

Downstream Products

• 802908-64-1 3-chloro-5-methoxy-6-methyl-benzo[b]thiophene-2-carbonyl chloride 
• 1012319-60-6 C₂₁H₁₇BrO₃ 
• 809281-52-5 3-chloro-5-methoxy-6-methyl-1-oxo-benzo[b]thiophene-2-carboxylic acid isopropyl ester 
• 1056047-21-2 3-chloro-5-methoxy-6-methyl-benzo[b]thiophene-2-carboxylic acid isopropyl ester 
• 136468-19-4 5-methoxy-6-methyl-2-aminoindan 
• 67199-60-4 3-(3-methoxy-4-methylphenyl)propanoic acid 

Relevant academic research and scientific papers

NOVEL BENZYLIDENEACETONE DERIVATIVE AND USE THEREOF

The present invention relates to novel benzylideneacetone derivatives or uses thereof, more specifically, the present invention relates to a pharmaceutical composition for preventing or treating, or food composition for ameliorating a cancer or a bone disease comprising a compound defined by Formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. Since compounds according to the present invention exhibit strong inhibitory activity on proliferation and differentiation of osteoclast, and activity on proliferation and differentiation of osteoblast, it can be usefully used to develop safe and effective anti-cancer agents, and therapeutic agents for preventing and treating or foods for ameliorating bone diseases including osteoporosis, and the like.

Benzylideneacetone Derivatives Inhibit Osteoclastogenesis and Activate Osteoblastogenesis Independently Based on Specific Structure-Activity Relationship

(E)-3,4-Dihydroxybenzylideneacetone (compound 1) inhibited receptor activator of NF-κB ligand-induced osteoclastogenesis of C57BL/6 bone marrow monocyte/macrophages with IC50 of 7.8 μM (IC50 of alendronate, 3.7 μM) while stimulating the differentiation of MC3T3-E1 osteoblastic cells, accompanied by the induction of Runt-related transcription factor 2, alkaline phosphatase, and osteocalcin. (E)-4-(3-Hydroxy-4-methoxyphenyl)-3-buten-2-one (compound 2c) showed a dramatically increased osteoclast-inhibitory potency with IC50 of 0.11 μM while sustaining osteoblast-stimulatory activity. (E)-4-(4-Hydroxy-3-methoxyphenyl)-3-buten-2-one (compound 2g) stimulated alkaline phosphatase production 2-fold at 50 μM without changing osteoclast-inhibitory activity, compared with compound 1. Oral administration of compounds 1, 2c, and 2g prevented ovariectomy-induced osteoporosis in ddY mice to a degree proportional to their osteoclastogenesis-inhibitory potencies. The administration of 1 (mg/kg)/d compound 2c ameliorated histomorphometry of osteoporotic bone to a degree comparable with 10 (mg/kg)/d alendronate. Conclusively, the in vitro capacity of a few benzylideneacetone derivatives to inhibit osteoclastogenesis supported by independent osteoblastogenesis activation was convincingly reflected in in vivo management of osteoporosis, suggesting a potential novel therapeutics for osteopenic diseases.

1,2,3-TRIAZOLO[4,5-D]PYRIMIDINES AS P2T RECEPTOR ANTAGONISTS

Compounds of formula having the following stereochemistrywherein R, R1, R2, R3 and R4 are as defined in the specification. The compounds are useful as P2T receptor antagonists