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Harnessing the Intrinsic Reactivity of 2‐Cyano‐Substituted Heteroarenes to Achieve Programmable Double Alkylation

Advanced synthesis & catalysis, 2020-04, Vol.362 (7), p.1502-1508

2020

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Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors

Bioorganic & medicinal chemistry letters, 2011-02, Vol.21 (4), p.1270-1274

2011

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Synthetic Approaches to the New Drugs Approved During 2015

Journal of medicinal chemistry, 2017-08, Vol.60 (15), p.6480-6515

2017

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Direct photochemical cross-coupling between aliphatic acids and BF3K salts

Chemical communications (Cambridge, England), 2020-01, Vol.56 (8), p.1294-1297

2020

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Discovery of 1‑{(3R,4R)‑3-[({5-Chloro-2-[(1-methyl‑1H‑pyrazol-4-yl)amino]‑7H‑pyrrolo[2,3‑d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

Journal of medicinal chemistry, 2016-03, Vol.59 (5), p.2005-2024

2016

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Synthetic approaches to the 2014 new drugs

Bioorganic & medicinal chemistry, 2016-05, Vol.24 (9), p.1937-1980

2016

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Synthetic approaches to the 2011 new drugs

Bioorganic & medicinal chemistry, 2013-06, Vol.21 (11), p.2795-2825

2013

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Synthetic approaches to the 2013 new drugs

Bioorganic & medicinal chemistry, 2015-05, Vol.23 (9), p.1895-1922

2015

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Identification of Cys255 in HIF‐1α as a novel site for development of covalent inhibitors of HIF‐1α/ARNT PasB domain protein–protein interaction

Protein science, 2012-12, Vol.21 (12), p.1885-1896

2012

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Synthetic approaches to the 2012 new drugs

Bioorganic & medicinal chemistry, 2014-04, Vol.22 (7), p.2005-2032

2014

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Targeting Small Cell Lung Cancer Harboring PIK3CA Mutation with a Selective Oral PI3K Inhibitor PF-4989216

Clinical cancer research, 2014-02, Vol.20 (3), p.631-643

2014

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Synthetic approaches to the 2009 new drugs

Bioorganic & medicinal chemistry, 2011-02, Vol.19 (3), p.1136-1154

2011

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Synthetic approaches to the 2010 new drugs

Bioorganic & medicinal chemistry, 2012-02, Vol.20 (3), p.1155-1174

2012

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Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors

Bioorganic & medicinal chemistry letters, 2012-08, Vol.22 (15), p.5114-5117

2012

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Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design

ACS medicinal chemistry letters, 2013-01, Vol.4 (1), p.91-97

2013

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Development of Scalable Syntheses of Selective PI3K inhibitors

Organic process research & development, 2011-05, Vol.15 (3), p.556-564

2011

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Synthetic approaches to the 2003 new drugs

Mini reviews in medicinal chemistry, 2004-12, Vol.4 (10), p.1105-1125

2004

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4-Methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors

Bioorganic & medicinal chemistry letters, 2010-10, Vol.20 (20), p.6096-6099

2010

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Design and synthesis of pyridazinone-based 5-HT2C agonists

Bioorganic & medicinal chemistry letters, 2009-10, Vol.19 (19), p.5791-5795

2009

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Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (1), p.266-271

2010

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Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity

ACS medicinal chemistry letters, 2011-11, Vol.2 (11), p.809-813

2011

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Synthetic approaches to the 2008 new drugs

Mini reviews in medicinal chemistry, 2009-12, Vol.9 (14), p.1655-1675

2009

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Short-acting 5-(trifluoromethyl)pyrido[4,3- d]pyrimidin-4(3 H)-one derivatives as orally-active calcium-sensing receptor antagonists

Bioorganic & medicinal chemistry letters, 2009-08, Vol.19 (16), p.4555-4559

2009

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Synthetic approaches to the 2007 new drugs

Mini reviews in medicinal chemistry, 2008-12, Vol.8 (14), p.1526-1548

2008

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Harnessing the Intrinsic Reactivity of 2‐Cyano‐Substituted Heteroarenes to Achieve Programmable Double Alkylation

Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors

Synthetic Approaches to the New Drugs Approved During 2015

Direct photochemical cross-coupling between aliphatic acids and BF3K salts

Discovery of 1‑{(3R,4R)‑3-[({5-Chloro-2-[(1-methyl‑1H‑pyrazol-4-yl)amino]‑7H‑pyrrolo[2,3‑d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

Synthetic approaches to the 2014 new drugs

Synthetic approaches to the 2011 new drugs

Synthetic approaches to the 2013 new drugs

Identification of Cys255 in HIF‐1α as a novel site for development of covalent inhibitors of HIF‐1α/ARNT PasB domain protein–protein interaction

Synthetic approaches to the 2012 new drugs

Targeting Small Cell Lung Cancer Harboring PIK3CA Mutation with a Selective Oral PI3K Inhibitor PF-4989216

Synthetic approaches to the 2009 new drugs

Synthetic approaches to the 2010 new drugs

Conformationally-restricted cyclic sulfones as potent and selective mTOR kinase inhibitors

Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design

Development of Scalable Syntheses of Selective PI3K inhibitors

Synthetic approaches to the 2003 new drugs

4-Methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors

Design and synthesis of pyridazinone-based 5-HT2C agonists

Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity

Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity

Synthetic approaches to the 2008 new drugs

Discovery Tactics To Mitigate Toxicity Risks Due to Reactive Metabolite Formation with 2-(2-Hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one Derivatives, Potent Calcium-Sensing Receptor Antagonists and Clinical Candidate(s) for the Treatment of Osteoporosis

Short-acting 5-(trifluoromethyl)pyrido[4,3- d]pyrimidin-4(3 H)-one derivatives as orally-active calcium-sensing receptor antagonists

Synthetic approaches to the 2007 new drugs

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