345953-48-2Relevant academic research and scientific papers
The development of potent non-peptidic PTP-1B inhibitors
Dufresne, Claude,Roy, Patrick,Wang, Zhaoyin,Asante-Appiah, Ernest,Cromlish, Wanda,Boie, Yves,Forghani, Farnaz,Desmarais, Sylvie,Wang, Qingping,Skorey, Kathryn,Waddleton, Deena,Ramachandran, Chidambaram,Kennedy, Brian P.,Xu, Lijing,Gordon, Robert,Chan, Chi Chung,Leblanc, Yves
, p. 1039 - 1042 (2007/10/03)
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).
Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
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, (2008/06/13)
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, including diabetes, obesity, and diabetes-related diseases.
Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
-
, (2008/06/13)
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, including diabetes, obesity, and diabetes-related diseases.
Protein tyrosine phosphatase 1B (PTP-1B) inhibitors containing two ortho-substituted aromatic phosphonates
-
, (2008/06/13)
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, including diabetes, obesity, and diabetes-related diseases.
