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Items: 1 to 50 of 102

1.

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
2.

Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.

Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH.

ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14.

PMID:
30891130
3.

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.

Gong H, Weinstein DS, Lu Z, Duan JJ, Stachura S, Haque L, Karmakar A, Hemagiri H, Raut DK, Gupta AK, Khan J, Camac D, Sack JS, Pudzianowski A, Wu DR, Yarde M, Shen DR, Borowski V, Xie JH, Sun H, D'Arienzo C, Dabros M, Galella MA, Wang F, Weigelt CA, Zhao Q, Foster W, Somerville JE, Salter-Cid LM, Barrish JC, Carter PH, Dhar TGM.

Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93. doi: 10.1016/j.bmcl.2017.12.006. Epub 2017 Dec 5.

PMID:
29233651
4.

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
5.

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
6.

Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor.

Ye XY, Chen SY, Wu S, Yoon DS, Wang H, Hong Z, O'Connor SP, Li J, Li JJ, Kennedy LJ, Walker SJ, Nayeem A, Sheriff S, Camac DM, Ramamurthy V, Morin PE, Zebo R, Taylor JR, Morgan NN, Ponticiello RP, Harrity T, Apedo A, Golla R, Seethala R, Wang M, Harper TW, Sleczka BG, He B, Kirby M, Leahy DK, Li J, Hanson RL, Guo Z, Li YX, DiMarco JD, Scaringe R, Maxwell B, Moulin F, Barrish JC, Gordon DA, Robl JA.

J Med Chem. 2017 Jun 22;60(12):4932-4948. doi: 10.1021/acs.jmedchem.7b00211. Epub 2017 Jun 5.

PMID:
28537398
7.

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.

Jurica EA, Wu X, Williams KN, Hernandez AS, Nirschl DS, Rampulla RA, Mathur A, Zhou M, Cao G, Xie C, Jacob B, Cai H, Wang T, Murphy BJ, Liu H, Xu C, Kunselman LK, Hicks MB, Sun Q, Schnur DM, Sitkoff DF, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Flynn NA, Maxwell BD, Hong Y, Tian Y, Wilkes JJ, Zinker BA, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2017 Feb 23;60(4):1417-1431. doi: 10.1021/acs.jmedchem.6b01559. Epub 2017 Feb 9.

PMID:
28112924
8.

Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.

Yang MG, Xiao Z, Dhar TG, Xiao HY, Gilmore JL, Marcoux D, Xie JH, McIntyre KW, Taylor TL, Borowski V, Heimrich E, Li YW, Feng J, Fernandes A, Yang Z, Balimane P, Marino AM, Cornelius G, Warrack BM, Mathur A, Wu DR, Li P, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Lehman-McKeeman LD, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

J Med Chem. 2016 Dec 22;59(24):11138-11147. doi: 10.1021/acs.jmedchem.6b01433. Epub 2016 Dec 7.

PMID:
28002964
9.

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

Xiao HY, Watterson SH, Langevine CM, Srivastava AS, Ko SS, Zhang Y, Cherney RJ, Guo WW, Gilmore JL, Sheppeck JE 2nd, Wu DR, Li P, Ramasamy D, Arunachalam P, Mathur A, Taylor TL, Shuster DJ, McIntyre KW, Shen DR, Yarde M, Cvijic ME, Marino AM, Balimane PV, Yang Z, Banas DM, Cornelius G, D'Arienzo CJ, Warrack BM, Lehman-McKeeman L, Salter-Cid LM, Xie J, Barrish JC, Carter PH, Dyckman AJ, Dhar TG.

J Med Chem. 2016 Nov 10;59(21):9837-9854. Epub 2016 Oct 20.

PMID:
27726358
10.

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.

Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA.

J Med Chem. 2016 Oct 13;59(19):9173-9200. Epub 2016 Sep 19.

PMID:
27583770
11.

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).

De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA.

J Med Chem. 2016 Sep 8;59(17):7915-35. doi: 10.1021/acs.jmedchem.6b00722. Epub 2016 Aug 26.

PMID:
27531604
12.

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ.

J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1.

PMID:
27309907
13.

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

Guo J, Watterson SH, Spergel SH, Kempson J, Langevine CM, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

Bioorg Med Chem Lett. 2016 May 15;26(10):2470-2474. doi: 10.1016/j.bmcl.2016.03.105. Epub 2016 Apr 1.

PMID:
27055941
14.

Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.

Dhar TG, Xiao HY, Xie J, Lehman-McKeeman LD, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Warrack B, Shi H, Levesque PC, Zhu JL, Hennan J, Balimane P, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Shen DR, Cvijic ME, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

ACS Med Chem Lett. 2016 Jan 19;7(3):283-8. doi: 10.1021/acsmedchemlett.5b00448. eCollection 2016 Mar 10.

15.

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

Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.

J Med Chem. 2016 Mar 24;59(6):2820-40. doi: 10.1021/acs.jmedchem.6b00089. Epub 2016 Mar 10.

PMID:
26924461
16.

Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.

Brown GD, Shi Q, Delucca GV, Batt DG, Galella MA, Cvijic ME, Liu RQ, Qiu F, Zhao Q, Barrish JC, Carter PH.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):662-666. doi: 10.1016/j.bmcl.2015.11.051. Epub 2015 Nov 17.

PMID:
26631321
17.

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
18.

Improving the pharmacokinetic and CYP inhibition profiles of azaxanthene-based glucocorticoid receptor modulators-identification of (S)-5-(2-(9-fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)-5H-chromeno[2,3-b]pyridin-5-yl)-2-methylpropanamido)-N-(tetrahydro-2H-pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341).

Yang MG, Dhar TG, Xiao Z, Xiao HY, Duan JJ, Jiang B, Galella MA, Cunningham M, Wang J, Habte S, Shuster D, McIntyre KW, Carman J, Holloway DA, Somerville JE, Nadler SG, Salter-Cid L, Barrish JC, Weinstein DS.

J Med Chem. 2015 May 28;58(10):4278-90. doi: 10.1021/acs.jmedchem.5b00257. Epub 2015 May 7.

PMID:
25905990
19.

Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.

Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S, Mo R, Nelson DJ, Pang J, Rose AV, Santella JB 3rd, Tebben AJ, Traeger SC, Xu S, Zhao Q, Barrish JC.

ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. doi: 10.1021/ml500505q. eCollection 2015 Apr 9.

20.

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
21.

Identification of a nonbasic melanin hormone receptor 1 antagonist as an antiobesity clinical candidate.

Washburn WN, Manfredi M, Devasthale P, Zhao G, Ahmad S, Hernandez A, Robl JA, Wang W, Mignone J, Wang Z, Ngu K, Pelleymounter MA, Longhi D, Zhao R, Wang B, Huang N, Flynn N, Azzara AV, Barrish JC, Rohrbach K, Devenny JJ, Rooney S, Thomas M, Glick S, Godonis HE, Harvey SJ, Cullen MJ, Zhang H, Caporuscio C, Stetsko P, Grubb M, Maxwell BD, Yang H, Apedo A, Gemzik B, Janovitz EB, Huang C, Zhang L, Freeden C, Murphy BJ.

J Med Chem. 2014 Sep 25;57(18):7509-22. doi: 10.1021/jm500026w. Epub 2014 Sep 9.

PMID:
25165888
22.

Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.

Santella JB 3rd, Gardner DS, Duncia JV, Wu H, Dhar M, Cavallaro C, Tebben AJ, Carter PH, Barrish JC, Yarde M, Briceno SW, Cvijic ME, Grafstrom RR, Liu R, Patel SR, Watson AJ, Yang G, Rose AV, Vickery RD, Caceres-Cortes J, Caporuscio C, Camac DM, Khan JA, An Y, Foster WR, Davies P, Hynes J Jr.

J Med Chem. 2014 Sep 25;57(18):7550-64. doi: 10.1021/jm5003167. Epub 2014 Sep 3.

PMID:
25101488
23.

Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.

Gong H, Yang M, Xiao Z, Doweyko AM, Cunningham M, Wang J, Habte S, Holloway D, Burke C, Shuster D, Gao L, Carman J, Somerville JE, Nadler SG, Salter-Cid L, Barrish JC, Weinstein DS.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3268-73. doi: 10.1016/j.bmcl.2014.06.010. Epub 2014 Jun 13.

PMID:
24980053
24.

Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Yang MG, Xiao Z, Zhao Q, Mandlekar S, Cvijic ME, Charo IF, Barrish JC, Decicco CP, Carter PH.

Bioorg Med Chem Lett. 2014 Apr 1;24(7):1843-5. doi: 10.1016/j.bmcl.2014.02.013. Epub 2014 Feb 21.

25.

Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core.

Xiao HY, Wu DR, Sheppeck JE 2nd, Habte SF, Cunningham MD, Somerville JE, Barrish JC, Nadler SG, Dhar TG.

Bioorg Med Chem Lett. 2013 Oct 15;23(20):5571-4. doi: 10.1016/j.bmcl.2013.08.049. Epub 2013 Aug 16.

PMID:
24011644
26.

Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.

Sheppeck JE 2nd, Gilmore JL, Xiao HY, Dhar TG, Nirschl D, Doweyko AM, Sack JS, Corbett MJ, Malley MF, Gougoutas JZ, Mckay L, Cunningham MD, Habte SF, Dodd JH, Nadler SG, Somerville JE, Barrish JC.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5442-7. doi: 10.1016/j.bmcl.2013.06.089. Epub 2013 Jul 9.

PMID:
23953070
27.

Synthesis and structure-activity relationships of novel indazolyl glucocorticoid receptor partial agonists.

Gilmore JL, Sheppeck JE 2nd, Wang J, Dhar TG, Cavallaro C, Doweyko AM, Mckay L, Cunningham MD, Habte SF, Nadler SG, Dodd JH, Somerville JE, Barrish JC.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5448-51. doi: 10.1016/j.bmcl.2013.06.085. Epub 2013 Jul 4.

PMID:
23916594
28.

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
29.

Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor.

Liu C, Lin J, Everlof G, Gesenberg C, Zhang H, Marathe PH, Malley M, Galella MA, McKinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2013 May 15;23(10):3028-33. doi: 10.1016/j.bmcl.2013.03.022. Epub 2013 Mar 15.

PMID:
23578688
30.

Benzimidazoles as benzamide replacements within cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Meyer DT, Pechulis AD, Guaciaro MA, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Cvijic ME, Barrish JC, Decicco CP, Carter PH.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6181-4. doi: 10.1016/j.bmcl.2012.08.002. Epub 2012 Aug 10.

PMID:
22939233
31.

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

Yang MG, Xiao Z, Shi Q, Cherney RJ, Tebben AJ, De Lucca GV, Santella JB 3rd, Mo R, Cvijic ME, Zhao Q, Barrish JC, Carter PH.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1384-7. doi: 10.1016/j.bmcl.2011.12.057. Epub 2011 Dec 16.

PMID:
22225639
32.

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).

Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5.

PMID:
22018461
33.

Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791826).

Weinstein DS, Gong H, Doweyko AM, Cunningham M, Habte S, Wang JH, Holloway DA, Burke C, Gao L, Guarino V, Carman J, Somerville JE, Shuster D, Salter-Cid L, Dodd JH, Nadler SG, Barrish JC.

J Med Chem. 2011 Oct 27;54(20):7318-33. doi: 10.1021/jm200879j. Epub 2011 Oct 3.

PMID:
21899328
34.

Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.

Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly KM, Shuster DJ, Doweyko AM, Sack JS, Kish K, Kiefer SE, Newitt JA, Zhang H, Marathe PH, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4633-7. doi: 10.1016/j.bmcl.2011.05.091. Epub 2011 May 30.

PMID:
21705217
35.

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.

Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31.

PMID:
21087862
36.

Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.

Yang BV, Weinstein DS, Doweyko LM, Gong H, Vaccaro W, Huynh T, Xiao HY, Doweyko AM, McKay L, Holloway DA, Somerville JE, Habte S, Cunningham M, McMahon M, Townsend R, Shuster D, Dodd JH, Nadler SG, Barrish JC.

J Med Chem. 2010 Dec 9;53(23):8241-51. doi: 10.1021/jm100957a. Epub 2010 Nov 12.

PMID:
21073190
37.

5-amino-pyrazoles as potent and selective p38α inhibitors.

Das J, Moquin RV, Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Newitt JA, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6886-9. doi: 10.1016/j.bmcl.2010.10.034. Epub 2010 Oct 13.

PMID:
21035336
38.

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
39.

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
40.

Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).

Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG.

J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u.

PMID:
20405922
41.

gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.

Cherney RJ, Mo R, Meyer DT, Voss ME, Yang MG, Santella JB 3rd, Duncia JV, Lo YC, Yang G, Miller PB, Scherle PA, Zhao Q, Mandlekar S, Cvijic ME, Barrish JC, Decicco CP, Carter PH.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2425-30. doi: 10.1016/j.bmcl.2010.03.035. Epub 2010 Mar 10.

PMID:
20346664
42.

An LFA-1 (alphaLbeta2) small-molecule antagonist reduces inflammation and joint destruction in murine models of arthritis.

Suchard SJ, Stetsko DK, Davis PM, Skala S, Potin D, Launay M, Dhar TG, Barrish JC, Susulic V, Shuster DJ, McIntyre KW, McKinnon M, Salter-Cid L.

J Immunol. 2010 Apr 1;184(7):3917-26. doi: 10.4049/jimmunol.0901095. Epub 2010 Feb 26.

43.

The antiangiogenic activity in xenograft models of brivanib, a dual inhibitor of vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinases.

Bhide RS, Lombardo LJ, Hunt JT, Cai ZW, Barrish JC, Galbraith S, Jeyaseelan R Sr, Mortillo S, Wautlet BS, Krishnan B, Kukral D, Malone H, Lewin AC, Henley BJ, Fargnoli J.

Mol Cancer Ther. 2010 Feb;9(2):369-78. doi: 10.1158/1535-7163.MCT-09-0472. Epub 2010 Jan 26.

44.

Novel synthesis of the hexahydroimidazo[1,5b]isoquinoline scaffold: application to the synthesis of glucocorticoid receptor modulators.

Xiao HY, Wu DR, Malley MF, Gougoutas JZ, Habte SF, Cunningham MD, Somerville JE, Dodd JH, Barrish JC, Nadler SG, Dhar TG.

J Med Chem. 2010 Feb 11;53(3):1270-80. doi: 10.1021/jm901551w.

PMID:
20047280
45.

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.

Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, Langevine CM, Dyckman AJ, Pattoli M, Burke JR, Yang X, Gillooly KM, McIntyre KW, Chen L, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.

Bioorg Med Chem Lett. 2009 May 15;19(10):2646-9. doi: 10.1016/j.bmcl.2009.03.159. Epub 2009 Apr 5.

PMID:
19376699
46.

Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.

Yang BV, Vaccaro W, Doweyko AM, Doweyko LM, Huynh T, Tortolani D, Nadler SG, McKay L, Somerville J, Holloway DA, Habte S, Weinstein DS, Barrish JC.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2139-43. doi: 10.1016/j.bmcl.2009.03.006. Epub 2009 Mar 9.

PMID:
19321341
47.

Novel tricyclic inhibitors of IkappaB kinase.

Kempson J, Spergel SH, Guo J, Quesnelle C, Gill P, Belanger D, Dyckman AJ, Li T, Watterson SH, Langevine CM, Das J, Moquin RV, Furch JA, Marinier A, Dodier M, Martel A, Nirschl D, Van Kirk K, Burke JR, Pattoli MA, Gillooly K, McIntyre KW, Chen L, Yang Z, Marathe PH, Wang-Iverson D, Dodd JH, McKinnon M, Barrish JC, Pitts WJ.

J Med Chem. 2009 Apr 9;52(7):1994-2005. doi: 10.1021/jm8015816.

PMID:
19267461
48.

Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer.

Dhar TG, Yang G, Davies P, Malley MF, Gougoutas JZ, Wu DR, Barrish JC, Carter PH.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):96-9. doi: 10.1016/j.bmcl.2008.11.002. Epub 2008 Nov 6.

PMID:
19010676
49.

(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.

Ahmad S, Madsen CS, Stein PD, Janovitz E, Huang C, Ngu K, Bisaha S, Kennedy LJ, Chen BC, Zhao R, Sitkoff D, Monshizadegan H, Yin X, Ryan CS, Zhang R, Giancarli M, Bird E, Chang M, Chen X, Setters R, Search D, Zhuang S, Nguyen-Tran V, Cuff CA, Harrity T, Darienzo CJ, Li T, Reeves RA, Blanar MA, Barrish JC, Zahler R, Robl JA.

J Med Chem. 2008 May 8;51(9):2722-33. doi: 10.1021/jm800001n. Epub 2008 Apr 15.

PMID:
18412317
50.

Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.

Ruel R, Thibeault C, L'Heureux A, Martel A, Cai ZW, Wei D, Qian L, Barrish JC, Mathur A, D'Arienzo C, Hunt JT, Kamath A, Marathe P, Zhang Y, Derbin G, Wautlet B, Mortillo S, Jeyaseelan R Sr, Henley B, Tejwani R, Bhide RS, Trainor GL, Fargnoli J, Lombardo LJ.

Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. doi: 10.1016/j.bmcl.2008.03.057. Epub 2008 Mar 22.

PMID:
18395443

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