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Discovery of 6‑Fluoro-5‑(R)‑(3‑(S)‑(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)‑yl)-2-methylphenyl)-2‑(S)‑(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro‑1H‑carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.9173-9200

2016

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Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7‑(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]‑9H‑carbazole-1-carboxamide (BMS-935177)

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.7915-7935

2016

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Purine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors for autoimmune diseases

Bioorganic & medicinal chemistry letters, 2014-05, Vol.24 (9), p.2206-2211

2014

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Discovery and Structure−Activity Relationship of N-(Ureidoalkyl)-Benzyl-Piperidines As Potent Small Molecule CC Chemokine Receptor-3 (CCR3) Antagonists

Journal of medicinal chemistry, 2002-08, Vol.45 (17), p.3794-3804

2002

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Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2)

Bioorganic & medicinal chemistry letters, 2012-02, Vol.22 (3), p.1384-1387

2012

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Stereospecific Synthesis, Structure−Activity Relationship, and Oral Bioavailability of Tetrahydropyrimidin-2-one HIV Protease Inhibitors

Journal of medicinal chemistry, 1999-01, Vol.42 (1), p.135-152

1999

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Cyclic HIV protease inhibitors capable of displacing the active site structural water molecule

Drug discovery today, 1997, Vol.2 (1), p.6-18

1997

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Preparation and Structure−Activity Relationship of Novel P1/P1‘-Substituted Cyclic Urea-Based Human Immunodeficiency Virus Type-1 Protease Inhibitors

Journal of medicinal chemistry, 1996-05, Vol.39 (11), p.2156-2169

1996

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Stereospecific, Stereoselective Rearrangement of Hexahydro-1,3-diazepin-2-ones to Tetrahydropyrimidin-2-ones and Imidazolidin-2-ones, a Useful Route for the Synthesis of HIV Protease Inhibitors

Journal of organic chemistry, 1998-07, Vol.63 (14), p.4755-4766

De Lucca, George V

1998

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Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9 H -carbazole-1-carboxamide (BMS-935177)

Journal of medicinal chemistry, 2016-09, Vol.59 (17), p.7915-7935

2016

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Nonsymmetric P2/P2‘ Cyclic Urea HIV Protease Inhibitors. Structure−Activity Relationship, Bioavailability, and Resistance Profile of Monoindazole-Substituted P2 Analogues

Journal of medicinal chemistry, 1998-06, Vol.41 (13), p.2411-2423

1998

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Design, Synthesis, and Evaluation of Tetrahydropyrimidinones as an Example of a General Approach to Nonpeptide HIV Protease Inhibitors

Journal of medicinal chemistry, 1997-05, Vol.40 (11), p.1707-1719

1997

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Discovery of 6-Fluoro-5-( R )-(3-( S )-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4 H )-yl)-2-methylphenyl)-2-( S )-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1 H -carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.9173-9200

2016

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Calculated and Experimental Low-Energy Conformations of Cyclic Urea HIV Protease Inhibitors

Journal of the American Chemical Society, 1998-05, Vol.120 (19), p.4570-4581

1998

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Recent developments in CCR3 antagonists

Current opinion in drug discovery & development, 2006-07, Vol.9 (4), p.516

De Lucca, George V

2006

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Discovery of CC Chemokine Receptor-3 (CCR3) Antagonists with Picomolar Potency

Journal of medicinal chemistry, 2005-03, Vol.48 (6), p.2194-2211

2005

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Synthesis and evaluation of delta lactams as nonpeptide HIV-protease inhibitors

Bioorganic & medicinal chemistry letters, 1997-03, Vol.7 (5), p.501-504

De Lucca, George V.

1997

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Does a diol cyclic urea inhibitor of HIV-1 protease bind tighter than its corresponding alcohol form? A study by free energy perturbation and continuum electrostatics calculations

Journal of computer-aided molecular design, 2001-02, Vol.15 (2), p.145-156

2001

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Synthesis and evaluation of imidazolidinones as nonpeptide HIV-protease inhibitors

Bioorganic & medicinal chemistry letters, 1997-03, Vol.7 (5), p.495-500

De Lucca, George V.

1997

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Synthesis and anti-HIV activity of pyrrolo-[1,2-d]-(1,4)-benzodiazepin-6-ones

Bioorganic & medicinal chemistry letters, 1992-12, Vol.2 (12), p.1639-1644

1992

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ChemInform Abstract: Stereospecific Synthesis, Structure-Activity Relationship, and Oral Bioavailability of Tetrahydropyrimidin-2-one HIV Protease Inhibitors

ChemInform, 1999-05, Vol.30 (21), p.no-no

1999

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Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7‑(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]‑9H‑carbazole-1-carboxamide (BMS-935177)

Purine derivatives as potent Bruton’s tyrosine kinase (BTK) inhibitors for autoimmune diseases

Discovery and Structure−Activity Relationship of N-(Ureidoalkyl)-Benzyl-Piperidines As Potent Small Molecule CC Chemokine Receptor-3 (CCR3) Antagonists

Synthesis of 3-phenylsulfonylmethyl cyclohexylaminobenzamide-derived antagonists of CC chemokine receptor 2 (CCR2)

Stereospecific Synthesis, Structure−Activity Relationship, and Oral Bioavailability of Tetrahydropyrimidin-2-one HIV Protease Inhibitors

Cyclic HIV protease inhibitors capable of displacing the active site structural water molecule

Preparation and Structure−Activity Relationship of Novel P1/P1‘-Substituted Cyclic Urea-Based Human Immunodeficiency Virus Type-1 Protease Inhibitors

Stereospecific, Stereoselective Rearrangement of Hexahydro-1,3-diazepin-2-ones to Tetrahydropyrimidin-2-ones and Imidazolidin-2-ones, a Useful Route for the Synthesis of HIV Protease Inhibitors

Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9 H -carbazole-1-carboxamide (BMS-935177)

Nonsymmetric P2/P2‘ Cyclic Urea HIV Protease Inhibitors. Structure−Activity Relationship, Bioavailability, and Resistance Profile of Monoindazole-Substituted P2 Analogues

Design, Synthesis, and Evaluation of Tetrahydropyrimidinones as an Example of a General Approach to Nonpeptide HIV Protease Inhibitors

Calculated and Experimental Low-Energy Conformations of Cyclic Urea HIV Protease Inhibitors

Recent developments in CCR3 antagonists

Discovery of CC Chemokine Receptor-3 (CCR3) Antagonists with Picomolar Potency

Synthesis and evaluation of delta lactams as nonpeptide HIV-protease inhibitors

Does a diol cyclic urea inhibitor of HIV-1 protease bind tighter than its corresponding alcohol form? A study by free energy perturbation and continuum electrostatics calculations

Synthesis and evaluation of imidazolidinones as nonpeptide HIV-protease inhibitors

Synthesis and anti-HIV activity of pyrrolo-[1,2-d]-(1,4)-benzodiazepin-6-ones

ChemInform Abstract: Stereospecific Synthesis, Structure-Activity Relationship, and Oral Bioavailability of Tetrahydropyrimidin-2-one HIV Protease Inhibitors

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