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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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Potent and Selective Agonists of Sphingosine 1‑Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2820-2840

2016

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Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1)

Bioorganic & medicinal chemistry letters, 2016-05, Vol.26 (10), p.2470-2474

2016

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Novel Tricyclic Inhibitors of IκB Kinase

Journal of medicinal chemistry, 2009-04, Vol.52 (7), p.1994-2005

2009

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Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy- N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5- d]pyrrolo[2,3- b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)

Bioorganic & medicinal chemistry letters, 2011-12, Vol.21 (23), p.7006-7012

2011

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Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: Synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis

Bioorganic & medicinal chemistry letters, 2011-01, Vol.21 (1), p.383-386

2011

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Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5- d]pyrrolo[2,3- b]pyridin-4-amine derived inhibitors of IκB kinase

Bioorganic & medicinal chemistry letters, 2009-05, Vol.19 (10), p.2646-2649

2009

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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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Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy-N-6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-ylmethyl acetamide (BMS-066)

Bioorganic & medicinal chemistry letters, 2011, Vol.21 (23), p.7006-7012

2011

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Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of I mu B kinase

Bioorganic & medicinal chemistry letters, 2009-05, Vol.19 (10), p.2646-2649

2009

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Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase

Bioorganic & medicinal chemistry letters, 2009-05, Vol.19 (10), p.2646-2649

2009

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Novel tricyclic inhibitors of IkappaB kinase

Journal of medicinal chemistry, 2009-04, Vol.52 (7), p.1994-2005

2009

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Stereoselective synthesis of hydroxylated bifenthrin isomers

Bioorganic & medicinal chemistry letters, 1992-12, Vol.2 (12), p.1585-1588

1992

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Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2

Journal of medicinal chemistry, 2021-01, Vol.64 (1), p.677-694

2021

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Organosilane insecticides. Part II: Chemistry and structure-activity relationships

Pesticide Science, 1990, Vol.28 (3), p.309-319

1990

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Potent and Selective Agonists of Sphingosine 1‑Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series

Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design

Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1)

Novel Tricyclic Inhibitors of IκB Kinase

Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy- N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5- d]pyrrolo[2,3- b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066)

Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: Synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5- d]pyrrolo[2,3- b]pyridin-4-amine derived inhibitors of IκB kinase

Novel tricyclic inhibitors of IKK2: Discovery and SAR leading to the identification of 2-methoxy-N-6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-ylmethyl acetamide (BMS-066)

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of I mu B kinase

Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase

Novel tricyclic inhibitors of IkappaB kinase

Stereoselective synthesis of hydroxylated bifenthrin isomers

Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2

Organosilane insecticides. Part II: Chemistry and structure-activity relationships

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