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Items: 33

1.

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).

Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA.

J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29.

PMID:
30893553
2.

Siderophile element constraints on the thermal history of the H chondrite parent body.

Archer GJ, Walker RJ, Tino J, Blackburn T, Kruijer TS, Hellmann JL.

Geochim Cosmochim Acta. 2019 Jan 15;245:556-576. doi: 10.1016/j.gca.2018.11.012. Epub 2018 Nov 20.

PMID:
30846885
3.

Separation of Bruton's tyrosine kinase inhibitor atropisomers by supercritical fluid chromatography.

Yip SH, Wu DR, Li P, Sun D, Watterson SH, Zhao R, Tino J, Mathur A.

J Chromatogr A. 2019 Feb 8;1586:106-115. doi: 10.1016/j.chroma.2018.12.006. Epub 2018 Dec 14.

PMID:
30578026
4.

Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.

Liu Q, Batt DG, Chaudhry C, Lippy JS, Pattoli MA, Surti N, Xu S, Carter PH, Burke JR, Tino JA.

Bioorg Med Chem Lett. 2018 Oct 1;28(18):3080-3084. doi: 10.1016/j.bmcl.2018.07.041. Epub 2018 Jul 30.

PMID:
30097367
5.

Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care.

Gillooly KM, Pulicicchio C, Pattoli MA, Cheng L, Skala S, Heimrich EM, McIntyre KW, Taylor TL, Kukral DW, Dudhgaonkar S, Nagar J, Banas D, Watterson SH, Tino JA, Fura A, Burke JR.

PLoS One. 2017 Jul 24;12(7):e0181782. doi: 10.1371/journal.pone.0181782. eCollection 2017.

6.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA.

J Med Chem. 2017 Jun 22;60(12):5193-5208. doi: 10.1021/acs.jmedchem.7b00618. Epub 2017 Jun 5.

PMID:
28541707
7.

Identification of highly potent and selective PI3Kδ inhibitors.

Marcoux D, Qin LY, Ruan Z, Shi Q, Ruan Q, Weigelt C, Qiu H, Schieven G, Hynes J, Bhide R, Poss M, Tino J.

Bioorg Med Chem Lett. 2017 Jul 1;27(13):2849-2853. doi: 10.1016/j.bmcl.2017.01.077. Epub 2017 Feb 7.

PMID:
28209465
8.

Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.

Qin LY, Ruan Z, Cherney RJ, Dhar TGM, Neels J, Weigelt CA, Sack JS, Srivastava AS, Cornelius LAM, Tino JA, Stefanski K, Gu X, Xie J, Susulic V, Yang X, Yarde-Chinn M, Skala S, Bosnius R, Goldstein C, Davies P, Ruepp S, Salter-Cid L, Bhide RS, Poss MA.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):855-861. doi: 10.1016/j.bmcl.2017.01.016. Epub 2017 Jan 10.

PMID:
28108251
9.

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
10.

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
11.

Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARα Selective Agonist.

Shi Y, Li J, Kennedy LJ, Tao S, Hernández AS, Lai Z, Chen S, Wong H, Zhu J, Trehan A, Lim NK, Zhang H, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Muckelbauer J, Chang C, Krystek SR, Li YX, Hosagrahara V, Zhang L, Kadiyala P, Xu C, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA.

ACS Med Chem Lett. 2016 Apr 4;7(6):590-4. doi: 10.1021/acsmedchemlett.6b00033. eCollection 2016 Jun 9.

12.

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Liu Q, Batt DG, Lippy JS, Surti N, Tebben AJ, Muckelbauer JK, Chen L, An Y, Chang C, Pokross M, Yang Z, Wang H, Burke JR, Carter PH, Tino JA.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4265-9. doi: 10.1016/j.bmcl.2015.07.102. Epub 2015 Aug 6.

PMID:
26320619
13.

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

Shi Q, Tebben A, Dyckman AJ, Li H, Liu C, Lin J, Spergel S, Burke JR, McIntyre KW, Olini GC, Strnad J, Surti N, Muckelbauer JK, Chang C, An Y, Cheng L, Ruan Q, Leftheris K, Carter PH, Tino J, De Lucca GV.

Bioorg Med Chem Lett. 2014 May 1;24(9):2206-11. doi: 10.1016/j.bmcl.2014.02.075. Epub 2014 Mar 13.

PMID:
24685542
14.

X-ray crystal structure of bone marrow kinase in the x chromosome: a Tec family kinase.

Muckelbauer J, Sack JS, Ahmed N, Burke J, Chang CY, Gao M, Tino J, Xie D, Tebben AJ.

Chem Biol Drug Des. 2011 Nov;78(5):739-48. doi: 10.1111/j.1747-0285.2011.01230.x. Epub 2011 Sep 21.

PMID:
21883956
15.

Synthesis and structure-activity relationships of 2-aryl-4-oxazolylmethoxy benzylglycines and 2-aryl-4-thiazolylmethoxy benzylglycines as novel, potent PPARalpha selective activators- PPARalpha and PPARgamma selectivity modulation.

Ye XY, Chen S, Zhang H, Locke KT, O'Malley K, Zhang L, Srivastava R, Miao B, Meyers D, Monshizadegan H, Search D, Grimm D, Zhang R, Lippy J, Twamley C, Muckelbauer JK, Chang C, An Y, Hosagrahara V, Zhang L, Yang TJ, Mukherjee R, Cheng PT, Tino JA.

Bioorg Med Chem Lett. 2010 May 1;20(9):2933-7. doi: 10.1016/j.bmcl.2010.03.019. Epub 2010 Mar 7.

PMID:
20356736
16.

Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).

Li J, Kennedy LJ, Shi Y, Tao S, Ye XY, Chen SY, Wang Y, Hernández AS, Wang W, Devasthale PV, Chen S, Lai Z, Zhang H, Wu S, Smirk RA, Bolton SA, Ryono DE, Zhang H, Lim NK, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Kadiyala P, Hosagrahara V, Zhang L, Xu C, Li YX, Muckelbauer JK, Chang C, An Y, Krystek SR, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA.

J Med Chem. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812.

PMID:
20218621
17.

Enhanced gastrointestinal motility with orally active ghrelin receptor agonists.

Charoenthongtrakul S, Giuliana D, Longo KA, Govek EK, Nolan A, Gagne S, Morgan K, Hixon J, Flynn N, Murphy BJ, Hernández AS, Li J, Tino JA, Gordon DA, DiStefano PS, Geddes BJ.

J Pharmacol Exp Ther. 2009 Jun;329(3):1178-86. doi: 10.1124/jpet.108.150193. Epub 2009 Feb 27.

PMID:
19252061
18.

Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist.

Mukherjee R, Locke KT, Miao B, Meyers D, Monshizadegan H, Zhang R, Search D, Grimm D, Flynn M, O'Malley KM, Zhang L, Li J, Shi Y, Kennedy LJ, Blanar M, Cheng PT, Tino J, Srivastava RA.

J Pharmacol Exp Ther. 2008 Dec;327(3):716-26. doi: 10.1124/jpet.108.143271. Epub 2008 Sep 17.

PMID:
18799592
19.

Discovery and optimization of (R)-prolinol-derived agonists of the Growth Hormone Secretagogue receptor (GHSR).

Zhai W, Flynn N, Longhi DA, Tino JA, Murphy BJ, Slusarchyk D, Gordon DA, Pendri A, Shi S, Stoffel R, Ma B, Sofia MJ, Gerritz SW.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5083-6. doi: 10.1016/j.bmcl.2008.07.120. Epub 2008 Aug 3.

PMID:
18722770
20.

(D)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: synthesis and incorporation into the growth hormone secretagogues.

Li J, Chen SY, Murphy BJ, Flynn N, Seethala R, Slusarchyk D, Yan M, Sleph P, Zhang H, Humphreys WG, Ewing WR, Robl JA, Gordon D, Tino JA.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4072-4. doi: 10.1016/j.bmcl.2008.05.100. Epub 2008 Jun 12.

PMID:
18554903
21.

Tetrazole based amides as growth hormone secretagogues.

Li JJ, Wang H, Li J, Qu F, Swartz SG, Hernández AS, Biller SA, Robl JA, Tino JA, Slusarchyk D, Seethala R, Sleph P, Yan M, Grover G, Flynn N, Murphy BJ, Gordon D.

Bioorg Med Chem Lett. 2008 Apr 15;18(8):2536-9. doi: 10.1016/j.bmcl.2008.03.059. Epub 2008 Mar 22.

PMID:
18378446
22.

Design and synthesis of tetrazole-based growth hormone secretagogue: the SAR studies of the O-benzyl serine side chain.

Li J, Chen SY, Tao S, Wang H, Li JJ, Swartz S, Musial C, Hernandez AA, Flynn N, Murphy BJ, Beehler B, Dickinson KE, Giupponi L, Grover G, Seethala R, Sleph P, Slusarchyk D, Yan M, Humphreys WG, Zhang H, Ewing WR, Robl JA, Gordon D, Tino JA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1825-9. doi: 10.1016/j.bmcl.2008.02.021. Epub 2008 Feb 13.

PMID:
18295486
23.

Optimization of 1H-tetrazole-1-alkanenitriles as potent orally bioavailable growth hormone secretagogues.

Hernández AS, Swartz SG, Slusarchyk D, Yan M, Seethala RK, Sleph P, Grover G, Dickinson K, Giupponi L, Harper TW, Humphreys WG, Longhi DA, Flynn N, Murphy BJ, Gordon DA, Biller SA, Robl JA, Tino JA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2067-72. doi: 10.1016/j.bmcl.2008.01.100. Epub 2008 Jan 31.

PMID:
18282707
24.

Discovery of a tetrazole-based growth hormone secretagogue: 4-(hydroxybutyl)carbamic acid 2-{5-[1-(2-amino-2-methylpropionylamino)-2- benzyloxyethyl]tetrazol-1-yl}ethyl ester (BMS-317180).

Li J, Chen SY, Li JJ, Wang H, Hernandez AS, Tao S, Musial CM, Qu F, Swartz S, Chao ST, Flynn N, Murphy BJ, Slusarchyk DA, Seethala R, Yan M, Sleph P, Grover G, Smith MA, Beehler B, Giupponi L, Dickinson KE, Zhang H, Humphreys WG, Patel BP, Schwinden M, Stouch T, Cheng PT, Biller SA, Ewing WR, Gordon D, Robl JA, Tino JA.

J Med Chem. 2007 Nov 29;50(24):5890-3. Epub 2007 Oct 31.

PMID:
17973363
25.

Discovery, synthesis, and structure-activity studies of tetrazole based growth hormone secretagogues.

Hernández AS, Cheng PT, Musial CM, Swartz SG, George RJ, Grover G, Slusarchyk D, Seethala RK, Smith M, Dickinson K, Giupponi L, Longhi DA, Flynn N, Murphy BJ, Gordon DA, Biller SA, Robl JA, Tino JA.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5928-33. Epub 2007 Aug 23.

PMID:
17869100
26.

2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.

Li JJ, Wang H, Tino JA, Robl JA, Herpin TF, Lawrence RM, Biller S, Jamil H, Ponticiello R, Chen L, Chu CH, Flynn N, Cheng D, Zhao R, Chen B, Schnur D, Obermeier MT, Sasseville V, Padmanabha R, Pike K, Harrity T.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11. Epub 2007 Mar 12.

PMID:
17383874
27.

Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.

Li JJ, Wang H, Qu F, Musial C, Tino JA, Robl JA, Slusarchyk D, Golla R, Seethala R, Dickinson K, Giupponi L, Grover G, Sleph P, Flynn N, Murphy BJ, Gordon D, Kung M, Stoffel R.

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1799-802.

PMID:
15780609
28.

Discovery of a potent and novel motilin agonist.

Li JJ, Chao HG, Wang H, Tino JA, Lawrence RM, Ewing WR, Ma Z, Yan M, Slusarchyk D, Seethala R, Sun H, Li D, Burford NT, Stoffel RH, Salyan ME, Li CY, Witkus M, Zhao N, Rich A, Gordon DA.

J Med Chem. 2004 Mar 25;47(7):1704-8.

PMID:
15027861
29.

An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits.

Wetterau JR, Gregg RE, Harrity TW, Arbeeny C, Cap M, Connolly F, Chu CH, George RJ, Gordon DA, Jamil H, Jolibois KG, Kunselman LK, Lan SJ, Maccagnan TJ, Ricci B, Yan M, Young D, Chen Y, Fryszman OM, Logan JV, Musial CL, Poss MA, Robl JA, Simpkins LM, Slusarchyk WA, Sulsky R, Taunk P, Magnin DR, Tino JA, Lawrence RM, Dickson JK Jr, Biller SA.

Science. 1998 Oct 23;282(5389):751-4.

30.

Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.

Chen P, Cheng PT, Alam M, Beyer BD, Bisacchi GS, Dejneka T, Evans AJ, Greytok JA, Hermsmeier MA, Humphreys WG, Jacobs GA, Kocy O, Lin PF, Lis KA, Marella MA, Ryono DE, Sheaffer AK, Spergel SH, Sun CQ, Tino JA, Vite G, Colonno RJ, Zahler R, Barrish JC.

J Med Chem. 1996 May 10;39(10):1991-2007.

PMID:
8642558
31.

Antiviral properties of aminodiol inhibitors against human immunodeficiency virus and protease.

Bechtold CM, Patick AK, Alam M, Greytok J, Tino JA, Chen P, Gordon E, Ahmad S, Barrish JC, Zahler R, et al.

Antimicrob Agents Chemother. 1995 Feb;39(2):374-9.

32.

Synthesis and antiviral activity of novel isonucleoside analogs.

Tino JA, Clark JM, Field AK, Jacobs GA, Lis KA, Michalik TL, McGeever-Rubin B, Slusarchyk WA, Spergel SH, Sundeen JE, et al.

J Med Chem. 1993 Apr 30;36(9):1221-9.

PMID:
8387600
33.

Synthesis and antiviral activity of 1-cyclobutyl-5-(2-bromovinyl)uracil nucleoside analogues and related compounds.

Slusarchyk WA, Bisacchi GS, Field AK, Hockstein DR, Jacobs GA, McGeever-Rubin B, Tino JA, Tuomari AV, Yamanaka GA, Young MG, et al.

J Med Chem. 1992 May 15;35(10):1799-806.

PMID:
1316966

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