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Items: 23

1.

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain.

Burke JR, Cheng L, Gillooly KM, Strnad J, Zupa-Fernandez A, Catlett IM, Zhang Y, Heimrich EM, McIntyre KW, Cunningham MD, Carman JA, Zhou X, Banas D, Chaudhry C, Li S, D'Arienzo C, Chimalakonda A, Yang X, Xie JH, Pang J, Zhao Q, Rose SM, Huang J, Moslin RM, Wrobleski ST, Weinstein DS, Salter-Cid LM.

Sci Transl Med. 2019 Jul 24;11(502). pii: eaaw1736. doi: 10.1126/scitranslmed.aaw1736.

PMID:
31341059
2.

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165.

Wrobleski ST, Moslin R, Lin S, Zhang Y, Spergel S, Kempson J, Tokarski JS, Strnad J, Zupa-Fernandez A, Cheng L, Shuster D, Gillooly K, Yang X, Heimrich E, McIntyre KW, Chaudhry C, Khan J, Ruzanov M, Tredup J, Mulligan D, Xie D, Sun H, Huang C, D'Arienzo C, Aranibar N, Chiney M, Chimalakonda A, Pitts WJ, Lombardo L, Carter PH, Burke JR, Weinstein DS.

J Med Chem. 2019 Jul 18. doi: 10.1021/acs.jmedchem.9b00444. [Epub ahead of print]

PMID:
31318208
3.

Identification of N-Methyl Nicotinamide and N-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2).

Moslin R, Zhang Y, Wrobleski ST, Lin S, Mertzman M, Spergel S, Tokarski JS, Strnad J, Gillooly K, McIntyre KW, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Heimrich E, Yang X, Muckelbauer JK, Chang C, Tredup J, Mulligan D, Xie D, Aranibar N, Chiney M, Burke JR, Lombardo L, Carter PH, Weinstein DS.

J Med Chem. 2019 Jul 17. doi: 10.1021/acs.jmedchem.9b00443. [Epub ahead of print]

PMID:
31314518
4.

Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.

Spergel SH, Mertzman ME, Kempson J, Guo J, Stachura S, Haque L, Lippy JS, Zhang RF, Galella M, Pitt S, Shen G, Fura A, Gillooly K, McIntyre KW, Tang V, Tokarski J, Sack JS, Khan J, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Schieven GL, Wrobleski ST, Pitts WJ.

ACS Med Chem Lett. 2019 Feb 13;10(3):306-311. doi: 10.1021/acsmedchemlett.8b00508. eCollection 2019 Mar 14.

PMID:
30891131
5.

Discovery of highly potent, selective, covalent inhibitors of JAK3.

Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J Jr, Wu H, Tokarski J, Sack JS, Khan J, Schieven G, Blatt Y, Chaudhry C, Salter-Cid LM, Fura A, Barrish JC, Carter PH, Pitts WJ.

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11.

PMID:
28927786
6.

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

Hynes J Jr, Wu H, Kempson J, Duan JJ, Lu Z, Jiang B, Stachura S, Tokarski JS, Sack JS, Khan JA, Lippy JS, Zhang RF, Pitt S, Shen G, Gillooly K, McIntyre K, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Fura A, Schieven GL, Pitts WJ, Wrobleski ST.

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. doi: 10.1016/j.bmcl.2017.05.043. Epub 2017 May 15.

PMID:
28539220
7.

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

Liu C, Lin J, Hynes J, Wu H, Wrobleski ST, Lin S, Dhar TG, Vrudhula VM, Sun JH, Chao S, Zhao R, Wang B, Chen BC, Everlof G, Gesenberg C, Zhang H, Marathe PH, McIntyre KW, Taylor TL, Gillooly K, Shuster DJ, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

J Med Chem. 2015 Oct 8;58(19):7775-84. doi: 10.1021/acs.jmedchem.5b00839. Epub 2015 Sep 22.

PMID:
26359680
8.

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J Jr, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, Pitt S, Shen G, Pitts WJ, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, McKinnon M, Fura A, Schieven GL, Wrobleski ST.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5721-5726. doi: 10.1016/j.bmcl.2014.10.061. Epub 2014 Oct 24.

PMID:
25453808
9.

The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.

Wrobleski ST, Lin S, Dhar TG, Dyckman AJ, Li T, Pitt S, Zhang R, Fan Y, Doweyko AM, Tokarski JS, Kish KF, Kiefer SE, Sack JS, Newitt JA, Witmer MR, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4120-6. doi: 10.1016/j.bmcl.2013.05.047. Epub 2013 May 23.

PMID:
23746475
10.

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.

Liu C, Lin J, Wrobleski ST, Lin S, Hynes J, Wu H, Dyckman AJ, Li T, Wityak J, Gillooly KM, Pitt S, Shen DR, Zhang RF, McIntyre KW, Salter-Cid L, Shuster DJ, Zhang H, Marathe PH, Doweyko AM, Sack JS, Kiefer SE, Kish KF, Newitt JA, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

J Med Chem. 2010 Sep 23;53(18):6629-39. doi: 10.1021/jm100540x.

PMID:
20804198
11.

Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors.

Lin S, Wrobleski ST, Hynes J Jr, Pitt S, Zhang R, Fan Y, Doweyko AM, Kish KF, Sack JS, Malley MF, Kiefer SE, Newitt JA, McKinnon M, Trzaskos J, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5864-8. doi: 10.1016/j.bmcl.2010.07.102. Epub 2010 Jul 30.

PMID:
20732813
12.

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

Wrobleski ST, Lin S, Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, McKinnon M, Dodd J, Barrish JC, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2739-44. doi: 10.1016/j.bmcl.2008.02.067. Epub 2008 Mar 4.

PMID:
18364256
13.

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.

Hynes J Jr, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K, Zhang H, Marathe PH, Doweyko AM, Tokarski JS, Sack JS, Pokross M, Kiefer SE, Newitt JA, Barrish JC, Dodd J, Schieven GL, Leftheris K.

J Med Chem. 2008 Jan 10;51(1):4-16. Epub 2007 Dec 12.

PMID:
18072718
14.

Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.

Murali Dhar TG, Wrobleski ST, Lin S, Furch JA, Nirschl DS, Fan Y, Todderud G, Pitt S, Doweyko AM, Sack JS, Mathur A, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5019-24. Epub 2007 Jul 21.

PMID:
17664068
15.

Toward the development of a general chiral auxiliary. A total synthesis of (+)-tetronolide via a tandem ketene-trapping [4 + 2] cycloaddition strategy.

Boeckman RK Jr, Shao P, Wrobleski ST, Boehmler DJ, Heintzelman GR, Barbosa AJ.

J Am Chem Soc. 2006 Aug 16;128(32):10572-88.

PMID:
16895426
16.

5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.

Liu C, Wrobleski ST, Lin J, Ahmed G, Metzger A, Wityak J, Gillooly KM, Shuster DJ, McIntyre KW, Pitt S, Shen DR, Zhang RF, Zhang H, Doweyko AM, Diller D, Henderson I, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

J Med Chem. 2005 Oct 6;48(20):6261-70.

PMID:
16190753
17.

Total synthesis of (+)-amphidinolide A. Structure elucidation and completion of the synthesis.

Trost BM, Harrington PE, Chisholm JD, Wrobleski ST.

J Am Chem Soc. 2005 Oct 5;127(39):13598-610.

PMID:
16190725
18.

Total synthesis of (+)-amphidinolide A. Assembly of the fragments.

Trost BM, Wrobleski ST, Chisholm JD, Harrington PE, Jung M.

J Am Chem Soc. 2005 Oct 5;127(39):13589-97.

PMID:
16190724
19.
20.

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

Leftheris K, Ahmed G, Chan R, Dyckman AJ, Hussain Z, Ho K, Hynes J Jr, Letourneau J, Li W, Lin S, Metzger A, Moriarty KJ, Riviello C, Shimshock Y, Wen J, Wityak J, Wrobleski ST, Wu H, Wu J, Desai M, Gillooly KM, Lin TH, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Zhang R, Diller D, Doweyko A, Sack J, Baldwin J, Barrish J, Dodd J, Henderson I, Kanner S, Schieven GL, Webb M.

J Med Chem. 2004 Dec 2;47(25):6283-91.

PMID:
15566298
21.

Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.

Wrobleski ST, Chen P, Hynes J Jr, Lin S, Norris DJ, Pandit CR, Spergel S, Wu H, Tokarski JS, Chen X, Gillooly KM, Kiener PA, McIntyre KW, Patil-Koota V, Shuster DJ, Turk LA, Yang G, Leftheris K.

J Med Chem. 2003 May 22;46(11):2110-6.

PMID:
12747783
22.

Ruthenium-catalyzed alkene-alkyne coupling: synthesis of the proposed structure of amphidinolide A.

Trost BM, Chisholm JD, Wrobleski ST, Jung M.

J Am Chem Soc. 2002 Oct 23;124(42):12420-1.

PMID:
12381177

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