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Items: 1 to 20 of 96

1.

Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).

Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.

J Med Chem. 2011 Nov 24;54(22):7860-83. doi: 10.1021/jm200900q. Epub 2011 Oct 31.

PMID:
22039836
2.

JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia.

Manthey CL, Johnson DL, Illig CR, Tuman RW, Zhou Z, Baker JF, Chaikin MA, Donatelli RR, Franks CF, Zeng L, Crysler C, Chen Y, Yurkow EJ, Boczon L, Meegalla SK, Wilson KJ, Wall MJ, Chen J, Ballentine SK, Ott H, Baumann C, Lawrence D, Tomczuk BE, Molloy CJ.

Mol Cancer Ther. 2009 Nov;8(11):3151-61. doi: 10.1158/1535-7163.MCT-09-0255. Epub 2009 Nov 3.

3.

Synthesis, structure-activity relationship and in vivo antiinflammatory efficacy of substituted dipiperidines as CCR2 antagonists.

Xia M, Hou C, DeMong DE, Pollack SR, Pan M, Brackley JA, Jain N, Gerchak C, Singer M, Malaviya R, Matheis M, Olini G, Cavender D, Wachter M.

J Med Chem. 2007 Nov 15;50(23):5561-3. Epub 2007 Oct 11.

PMID:
17929797
4.

Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.

Illig CR, Chen J, Wall MJ, Wilson KJ, Ballentine SK, Rudolph MJ, DesJarlais RL, Chen Y, Schubert C, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1642-8. doi: 10.1016/j.bmcl.2008.01.059. Epub 2008 Jan 19.

PMID:
18242992
5.

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
6.

Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors.

Illig CR, Manthey CL, Meegalla SK, Wall MJ, Chen J, Wilson KJ, DesJarlais RL, Ballentine SK, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6363-9. doi: 10.1016/j.bmcl.2013.09.061. Epub 2013 Oct 1.

PMID:
24138939
7.

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
8.

Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.

Wall MJ, Chen J, Meegalla S, Ballentine SK, Wilson KJ, DesJarlais RL, Schubert C, Chaikin MA, Crysler C, Petrounia IP, Donatelli RR, Yurkow EJ, Boczon L, Mazzulla M, Player MR, Patch RJ, Manthey CL, Molloy C, Tomczuk B, Illig CR.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2097-102. doi: 10.1016/j.bmcl.2008.01.088. Epub 2008 Jan 30.

PMID:
18289848
9.

Design, synthesis, and activity of 2-imidazol-1-ylpyrimidine derived inducible nitric oxide synthase dimerization inhibitors.

Davey DD, Adler M, Arnaiz D, Eagen K, Erickson S, Guilford W, Kenrick M, Morrissey MM, Ohlmeyer M, Pan G, Paradkar VM, Parkinson J, Polokoff M, Saionz K, Santos C, Subramanyam B, Vergona R, Wei RG, Whitlow M, Ye B, Zhao ZS, Devlin JJ, Phillips G.

J Med Chem. 2007 Mar 22;50(6):1146-57. Epub 2007 Feb 23.

PMID:
17315988
10.

An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.

McKenna JM, Halley F, Souness JE, McLay IM, Pickett SD, Collis AJ, Page K, Ahmed I.

J Med Chem. 2002 May 23;45(11):2173-84.

PMID:
12014955
11.

Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.

Martin MW, Newcomb J, Nunes JJ, Boucher C, Chai L, Epstein LF, Faust T, Flores S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Kim JL, Middleton S, Morgenstern K, Oliveira-dos-Santos A, Patel VF, Powers D, Rose P, Tudor Y, Turci SM, Welcher AA, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Ermann M, Johnston D, Saluste CG.

J Med Chem. 2008 Mar 27;51(6):1637-48. doi: 10.1021/jm701095m. Epub 2008 Feb 16.

PMID:
18278858
12.

Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.

Almansa C, Alfón J, de Arriba AF, Cavalcanti FL, Escamilla I, Gómez LA, Miralles A, Soliva R, Bartrolí J, Carceller E, Merlos M, García-Rafanell J.

J Med Chem. 2003 Jul 31;46(16):3463-75.

PMID:
12877584
13.

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.

Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ, Gillooly KM, Behnia K, Schieven GL, Wityak J, Barrish JC.

J Med Chem. 2006 Nov 16;49(23):6819-32.

PMID:
17154512
14.

Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents.

Patch RJ, Brandt BM, Asgari D, Baindur N, Chadha NK, Georgiadis T, Cheung WS, Petrounia IP, Donatelli RR, Chaikin MA, Player MR.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6070-4. Epub 2007 Sep 19.

PMID:
17904845
15.

Rational design of non-nucleoside, potent, and orally bioavailable adenosine deaminase inhibitors: predicting enzyme conformational change and metabolism.

Terasaka T, Tsuji K, Kato T, Nakanishi I, Kinoshita T, Kato Y, Kuno M, Inoue T, Tanaka K, Nakamura K.

J Med Chem. 2005 Jul 28;48(15):4750-3.

PMID:
16033254
16.
17.

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
18.

Pyrido[2,3-d]pyrimidin-5-ones: a novel class of antiinflammatory macrophage colony-stimulating factor-1 receptor inhibitors.

Huang H, Hutta DA, Rinker JM, Hu H, Parsons WH, Schubert C, DesJarlais RL, Crysler CS, Chaikin MA, Donatelli RR, Chen Y, Cheng D, Zhou Z, Yurkow E, Manthey CL, Player MR.

J Med Chem. 2009 Feb 26;52(4):1081-99. doi: 10.1021/jm801406h.

PMID:
19193011
19.

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
20.

Structure-based optimization of a potent class of arylamide FMS inhibitors.

Meegalla SK, Wall MJ, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Illig CR.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3632-7. doi: 10.1016/j.bmcl.2008.04.059. Epub 2008 Apr 26.

PMID:
18495479

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