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Phase I Dose-Escalation Trial of PT2385, a First-in-Class Hypoxia-Inducible Factor-2α Antagonist in Patients With Previously Treated Advanced Clear Cell Renal Cell Carcinoma

Journal of clinical oncology, 2018-03, Vol.36 (9), p.867-874

2018

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On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models

Nature (London), 2016-11, Vol.539 (7627), p.107-111

2016

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Targeting renal cell carcinoma with a HIF-2 antagonist

Nature (London), 2016-11, Vol.539 (7627), p.112-117

2016

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3‑[(1S,2S,3R)‑2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma

Journal of medicinal chemistry, 2019-08, Vol.62 (15), p.6876-6893

2019

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A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma

Cancer research (Chicago, Ill.), 2016-09, Vol.76 (18), p.5491-5500

2016

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Discovery of Danoprevir (ITMN-191/R7227), a Highly Selective and Potent Inhibitor of Hepatitis C Virus (HCV) NS3/4A Protease

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.1753-1769

2014

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Preclinical Characteristics of the Hepatitis C Virus NS3/4A Protease Inhibitor ITMN-191 (R7227)

Antimicrobial Agents and Chemotherapy, 2008-12, Vol.52 (12), p.4432-4441

2008

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Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→πAr interaction

Medicinal chemistry research, 2023-07, Vol.32 (7), p.1510-1531

2023

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Discovery of (1S,2R,3R)-2,3-Dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: Novel and Highly Selective Aggrecanase Inhibitors

Journal of medicinal chemistry, 2011-04, Vol.54 (8), p.2839-2863

2011

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Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases

Journal of medicinal chemistry, 2008-08, Vol.51 (15), p.4672-4684

2008

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A Nucleic Acid Triple Helix Formed by a Peptide Nucleic Acid-DNA Complex

Science (American Association for the Advancement of Science), 1995-12, Vol.270 (5243), p.1838-1841

1995

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A New Resin-Bound Universal Isonitrile for the Ugi 4CC Reaction: Preparation and Applications to the Synthesis of 2,5-Diketopiperazines and 1,4-Benzodiazepine-2,5-diones

Organic letters, 2002-04, Vol.4 (7), p.1167-1170

2002

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Crystal structures of H-2Db in complex with the LCMV-derived peptides GP92 and GP392 explain pleiotropic effects of glycosylation on antigen presentation and immunogenicity

PloS one, 2017, Vol.12 (12), p.e0189584-e0189584

2017

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3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase

Bioorganic & medicinal chemistry letters, 2009-01, Vol.19 (2), p.410-414

2009

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Discovery of Disubstituted Imidazo[4,5‑b]pyridines and Purines as Potent TrkA Inhibitors

ACS medicinal chemistry letters, 2012-09, Vol.3 (9), p.705-709

2012

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Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase inhibitors

Bioorganic & medicinal chemistry letters, 2009-07, Vol.19 (13), p.3637-3641

2009

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Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (6), p.1575-1580

2009

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Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors

Bioorganic & medicinal chemistry letters, 2009-11, Vol.19 (21), p.6213-6217

2009

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General Method for the Synthesis of Phospholipid Derivatives of 1,2-O-Diacyl-sn-Glycerols

Journal of organic chemistry, 1994-08, Vol.59 (17), p.4805-4820

1994

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Antisense and Antigene Properties of Peptide Nucleic Acids

Science (American Association for the Advancement of Science), 1992-11, Vol.258 (5087), p.1481-1485

1992

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Efficient, Stereoselective Synthesis of Oxazolo[3,2-a]pyrazin-5-ones: Novel Bicyclic Lactam Scaffolds from the Bicyclocondensation of 3-Aza-1,5-ketoacids and Amino Alcohols

Organic letters, 2003-07, Vol.5 (15), p.2727-2730

2003

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Novel linker for the solid-phase synthesis of guanidines

Tetrahedron letters, 1998-08, Vol.39 (33), p.5899-5902

1998

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Abstract 4022: PT2385, a novel HIF-2 antagonist, combines with checkpoint inhibitor antibodies to inhibit tumor growth in preclinical models by modulating myeloid cells and enhancing T cell infiltration

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.4022-4022

2016

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Phase I Dose-Escalation Trial of PT2385, a First-in-Class Hypoxia-Inducible Factor-2α Antagonist in Patients With Previously Treated Advanced Clear Cell Renal Cell Carcinoma

On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models

Targeting renal cell carcinoma with a HIF-2 antagonist

3‑[(1S,2S,3R)‑2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma

A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate (S)‑3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro‑1H‑inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385)

Discovery of Danoprevir (ITMN-191/R7227), a Highly Selective and Potent Inhibitor of Hepatitis C Virus (HCV) NS3/4A Protease

Preclinical Characteristics of the Hepatitis C Virus NS3/4A Protease Inhibitor ITMN-191 (R7227)

Lead change of a HIF-2α antagonist guided by multiparameter optimization and utilization of an Olp→πAr interaction

Discovery of (1S,2R,3R)-2,3-Dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: Novel and Highly Selective Aggrecanase Inhibitors

Identification of 4-Aminopyrazolylpyrimidines as Potent Inhibitors of Trk Kinases

A Nucleic Acid Triple Helix Formed by a Peptide Nucleic Acid-DNA Complex

A New Resin-Bound Universal Isonitrile for the Ugi 4CC Reaction: Preparation and Applications to the Synthesis of 2,5-Diketopiperazines and 1,4-Benzodiazepine-2,5-diones

Crystal structures of H-2Db in complex with the LCMV-derived peptides GP92 and GP392 explain pleiotropic effects of glycosylation on antigen presentation and immunogenicity

3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase

Discovery of Disubstituted Imidazo[4,5‑b]pyridines and Purines as Potent TrkA Inhibitors

Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase inhibitors

Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors

Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors

General Method for the Synthesis of Phospholipid Derivatives of 1,2-O-Diacyl-sn-Glycerols

Antisense and Antigene Properties of Peptide Nucleic Acids

Efficient, Stereoselective Synthesis of Oxazolo[3,2-a]pyrazin-5-ones: Novel Bicyclic Lactam Scaffolds from the Bicyclocondensation of 3-Aza-1,5-ketoacids and Amino Alcohols

Novel linker for the solid-phase synthesis of guanidines

Abstract 4022: PT2385, a novel HIF-2 antagonist, combines with checkpoint inhibitor antibodies to inhibit tumor growth in preclinical models by modulating myeloid cells and enhancing T cell infiltration

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