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Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Journal of medicinal chemistry, 2005-07, Vol.48 (15), p.5025-5037

2005

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Involvement of DPP‐IV catalytic residues in enzyme–saxagliptin complex formation

Protein science, 2008-02, Vol.17 (2), p.240-250

2008

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Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors

Bioorganic & medicinal chemistry letters, 2013-03, Vol.23 (6), p.1622-1625

2013

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Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes

Bioorganic & medicinal chemistry letters, 2010-08, Vol.20 (15), p.4395-4398

2010

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Optimization of Activity, Selectivity, and Liability Profiles in 5‑Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)‑2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo‑5H‑pyrrolo[3,4‑b]pyridin-6(7H)‑yl)‑N,N‑dimethylacetamide (BMS-767778)

Journal of medicinal chemistry, 2013-09, Vol.56 (18), p.7343-7357

2013

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Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

BMC pharmacology, 2012-04, Vol.12 (1), p.2-2, Article 2

2012

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Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors

Journal of medicinal chemistry, 2010-08, Vol.53 (15), p.5620-5628

2010

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DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues

Regulatory peptides, 2013-09, Vol.186, p.26-35

2013

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Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)

Archives of biochemistry and biophysics, 2006, Vol.445 (1), p.9-18

2006

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7-Oxopyrrolopyridine-derived DPP4 inhibitors—mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site

Bioorganic & medicinal chemistry letters, 2011-11, Vol.21 (22), p.6646-6651

2011

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Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors

Bioorganic & medicinal chemistry letters, 2010-11, Vol.20 (21), p.6273-6276

2010

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Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors

Bioorganic & medicinal chemistry, 2007-12, Vol.17 (23), p.6476-6480

2007

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Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors

Bioorganic & medicinal chemistry letters, 2005-09, Vol.15 (18), p.3992-3995

2005

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Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1

Bioorganic & medicinal chemistry letters, 2006-03, Vol.16 (6), p.1731-1734

2006

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Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach

Archives of biochemistry and biophysics, 2005-04, Vol.436 (2), p.367-376

2005

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Scorpion toxins targeted against the sarcoplasmic reticulum Ca(2+)-release channel of skeletal and cardiac muscle

Proceedings of the National Academy of Sciences - PNAS, 1992-12, Vol.89 (24), p.12185-12189

1992

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Two-photon-excitation fluorescence imaging of three-dimensional calcium-ion activity

Applied Optics, 1994-02, Vol.33 (4), p.662

1994

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Sodium/calcium exchanger in heart muscle: molecular biology, cellular function, and its special role in excitation-contraction coupling

Cardiovascular research, 1993-10, Vol.27 (10), p.1726-1734

1993

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Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate ( Sa )-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5 H -pyrrolo[3,4- b ]pyridin-6(7 H )-yl)- N , N -dimethylacetamide (BMS-767778)

Journal of medicinal chemistry, 2013-09, Vol.56 (18), p.7343-7357

2013

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Adriamycin cardiomyopathy in the rabbit: alterations in contractile proteins and myocyte function

Cardiovascular research, 1990-10, Vol.24 (10), p.834-842

1990

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Potassium efflux from the myocardium during hypoxia: role of lactate ions

Cardiovascular research, 1987-12, Vol.21 (12), p.886-891

1987

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Comparison of wet and dry growth in artificial and flight icing conditions

Journal of thermophysics and heat transfer, 1987-07, Vol.1 (3), p.215-221

1987

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Scorpion Toxins Targeted Against the Sarcoplasmic Reticulum Ca2+- Release Channel of Skeletal and Cardiac Muscle

Proceedings of the National Academy of Sciences - PNAS, 1992-12, Vol.89 (24), p.12185-12189

1992

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Measurement of ice growth during simulated and natural icing conditions using ultrasonic pulse-echo techniques

Journal of aircraft, 1986-06, Vol.23 (6), p.492-498

1986

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Measurement of ice accretion using ultrasonic pulse-echo techniques

Journal of aircraft, 1985-06, Vol.22 (6), p.530-535

1985

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Discovery and Preclinical Profile of Saxagliptin (BMS-477118): A Highly Potent, Long-Acting, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes

Involvement of DPP‐IV catalytic residues in enzyme–saxagliptin complex formation

Substituted piperidinyl glycinyl 2-cyano-4,5-methano pyrrolidines as potent and stable dipeptidyl peptidase IV inhibitors

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes

Optimization of Activity, Selectivity, and Liability Profiles in 5‑Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate (Sa)‑2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo‑5H‑pyrrolo[3,4‑b]pyridin-6(7H)‑yl)‑N,N‑dimethylacetamide (BMS-767778)

Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as Potent, Selective Dipeptidyl Peptidase-4 (DPP4) Inhibitors

DPP8 and DPP9 expression in cynomolgus monkey and Sprague Dawley rat tissues

Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)

7-Oxopyrrolopyridine-derived DPP4 inhibitors—mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site

Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors

Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors

Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors

Seco-prolinenitrile inhibitors of dipeptidyl peptidase IV define minimal pharmacophore requirements at P1

Probing prime substrate binding sites of human dipeptidyl peptidase-IV using competitive substrate approach

Scorpion toxins targeted against the sarcoplasmic reticulum Ca(2+)-release channel of skeletal and cardiac muscle

Two-photon-excitation fluorescence imaging of three-dimensional calcium-ion activity

Sodium/calcium exchanger in heart muscle: molecular biology, cellular function, and its special role in excitation-contraction coupling

Optimization of Activity, Selectivity, and Liability Profiles in 5-Oxopyrrolopyridine DPP4 Inhibitors Leading to Clinical Candidate ( Sa )-2-(3-(Aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5 H -pyrrolo[3,4- b ]pyridin-6(7 H )-yl)- N , N -dimethylacetamide (BMS-767778)

Adriamycin cardiomyopathy in the rabbit: alterations in contractile proteins and myocyte function

Potassium efflux from the myocardium during hypoxia: role of lactate ions

Comparison of wet and dry growth in artificial and flight icing conditions

Scorpion Toxins Targeted Against the Sarcoplasmic Reticulum Ca2+- Release Channel of Skeletal and Cardiac Muscle

Measurement of ice growth during simulated and natural icing conditions using ultrasonic pulse-echo techniques

Measurement of ice accretion using ultrasonic pulse-echo techniques

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