261175-36-4

Upstream product

• 261176-45-8 Di(tert-butyl)[4-(2-{4-[[di(tert-butoxy)phosphoryl](difluoro)methyl]benzyl}-3-oxo-2,3-diphenylpropyl)phenyl](difluoro)methylphosphonate 
• 451-40-1 phenyl benzyl ketone 
• 261176-00-5 (4-bromomethylphenyl) difluoromethylphosphonic acid di-tert-butyl ester 
• 345953-50-6 di(tert-butyl)difluoro[4-(3-oxo-2,3-diphenylpropyl)phenyl]methylphosphonate 

Downstream Products

• 261175-47-7 (4-{2-{4-[difluoro(phosphono)methyl]benzyl}-3-(4-fluorophenyl)-2-[4-(methylsulfanyl)phenyl]-3-oxopropyl}phenyl)(difluoro)methylphosphonic acid 
• 261175-39-7 (4-{2-{4-[difluoro(phosphono)methyl]benzyl}-3-(3-fluorophenyl)-2-[4-(methylsulfanyl)phenyl]-3-oxopropyl}phenyl)(difluoro)methyl phosphonic acid 

Relevant academic research and scientific papers

The development of potent non-peptidic PTP-1B inhibitors

The SAR from our peptide libraries was exploited to design a series of potent deoxybenzoin PTP-1B inhibitors. The introduction of an ortho bromo substituent next to the difluoromethylphosphonate warhead gave up to 20-fold increase in potency compared to the desbromo analogues. In addition, these compounds were orally bioavailable and active in the animal models of non-insulin dependent diabetes mellitus (NIDDM).

Phosphonic acids derivatives as inhibitors of protein tyrosine phosphate 1B (PTP-1B)

The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.