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Items: 35

1.

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G.

J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9.

PMID:
30130103
2.

Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.

Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R.

J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23.

PMID:
29298069
3.

Development of a high-throughput crystal structure-determination platform for JAK1 using a novel metal-chelator soaking system.

Caspers NL, Han S, Rajamohan F, Hoth LR, Geoghegan KF, Subashi TA, Vazquez ML, Kaila N, Cronin CN, Johnson E, Kurumbail RG.

Acta Crystallogr F Struct Biol Commun. 2016 Nov 1;72(Pt 11):840-845. Epub 2016 Oct 27.

4.

Imidazotriazines: Spleen Tyrosine Kinase (Syk) Inhibitors Identified by Free-Energy Perturbation (FEP).

Lovering F, Aevazelis C, Chang J, Dehnhardt C, Fitz L, Han S, Janz K, Lee J, Kaila N, McDonald J, Moore W, Moretto A, Papaioannou N, Richard D, Ryan MS, Wan ZK, Thorarensen A.

ChemMedChem. 2016 Jan 19;11(2):217-33. doi: 10.1002/cmdc.201500333. Epub 2015 Sep 18.

PMID:
26381330
5.

Results of bococizumab, a monoclonal antibody against proprotein convertase subtilisin/kexin type 9, from a randomized, placebo-controlled, dose-ranging study in statin-treated subjects with hypercholesterolemia.

Ballantyne CM, Neutel J, Cropp A, Duggan W, Wang EQ, Plowchalk D, Sweeney K, Kaila N, Vincent J, Bays H.

Am J Cardiol. 2015 May 1;115(9):1212-21. doi: 10.1016/j.amjcard.2015.02.006. Epub 2015 Feb 12.

6.

New spleen tyrosine kinase inhibitors: patent applications published during 2011-2013.

Thorarensen A, Kaila N.

Pharm Pat Anal. 2014 Sep;3(5):523-41. doi: 10.4155/ppa.14.34. Review.

PMID:
25374321
7.

Pharmacokinetics of ranibizumab after intravitreal administration in patients with retinal vein occlusion or diabetic macular edema.

Zhang Y, Yao Z, Kaila N, Kuebler P, Visich J, Maia M, Tuomi L, Ehrlich JS, Rubio RG, Campochiaro PA.

Ophthalmology. 2014 Nov;121(11):2237-46. doi: 10.1016/j.ophtha.2014.05.012. Epub 2014 Jul 4.

PMID:
25001159
8.

Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.

Kaila N, Follows B, Leung L, Thomason J, Huang A, Moretto A, Janz K, Lowe M, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E.

J Med Chem. 2014 Feb 27;57(4):1299-322. doi: 10.1021/jm401509e. Epub 2014 Feb 10.

PMID:
24512187
9.

Pharmacokinetic study in pigs and in vitro metabolic characterization in pig- and human-liver microsomes reveal marked differences in disposition and metabolism of tiletamine and zolazepam (Telazol).

Kumar A, Mann HJ, Remmel RP, Beilman GJ, Kaila N.

Xenobiotica. 2014 Apr;44(4):379-90. doi: 10.3109/00498254.2013.833362. Epub 2013 Sep 11.

PMID:
24020890
10.

Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.

Kaila N, Huang A, Moretto A, Follows B, Janz K, Lowe M, Thomason J, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E.

J Med Chem. 2012 Jun 14;55(11):5088-109. doi: 10.1021/jm300007n. Epub 2012 May 31.

PMID:
22651823
11.

The 2010 patent landscape for spleen tyrosine kinase inhibitors.

Moretto AF, Dehnhardt C, Kaila N, Papaioannou N, Thorarensen A.

Recent Pat Inflamm Allergy Drug Discov. 2012 May;6(2):97-120. Review.

PMID:
22292554
12.

Biophysical and mechanistic insights into novel allosteric inhibitor of spleen tyrosine kinase.

Hall J, Aulabaugh A, Rajamohan F, Liu S, Kaila N, Wan ZK, Ryan M, Magyar R, Qiu X.

J Biol Chem. 2012 Mar 2;287(10):7717-27. doi: 10.1074/jbc.M111.311993. Epub 2012 Jan 4.

13.

Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.

Huang A, Moretto A, Janz K, Lowe M, Bedard PW, Tam S, Di L, Clerin V, Sushkova N, Tchernychev B, Tsao DH, Keith JC, Shaw GD, Schaub RG, Wang Q, Kaila N.

J Med Chem. 2010 Aug 26;53(16):6003-17. doi: 10.1021/jm9013696.

PMID:
20718494
14.

Selectin inhibitors: a patent review.

Bedard PW, Kaila N.

Expert Opin Ther Pat. 2010 Jun;20(6):781-93. doi: 10.1517/13543771003767468. Review.

PMID:
20408735
15.

Bromodecarboxylation of quinoline salicylic acids: increasing the diversity of accessible substituted quinolines.

Janz K, Kaila N.

J Org Chem. 2009 Nov 20;74(22):8874-7. doi: 10.1021/jo9018232.

PMID:
19863103
16.

Selective inhibitors of tumor progression loci-2 (Tpl2) kinase with potent inhibition of TNF-alpha production in human whole blood.

Wu J, Green N, Hotchandani R, Hu Y, Condon J, Huang A, Kaila N, Li HQ, Guler S, Li W, Tam SY, Wang Q, Pelker J, Marusic S, Hsu S, Perry Hall J, Telliez JB, Cui J, Lin LL.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3485-8. doi: 10.1016/j.bmcl.2009.05.009. Epub 2009 May 7.

PMID:
19464884
17.

Prophylactic P-selectin inhibition with PSI-421 promotes resolution of venous thrombosis without anticoagulation.

Meier TR, Myers DD Jr, Wrobleski SK, Zajkowski PJ, Hawley AE, Bedard PW, Ballard NE, Londy FJ, Kaila N, Vlasuk GP, Schaub RG, Wakefield TW.

Thromb Haemost. 2008 Feb;99(2):343-51. doi: 10.1160/TH07-10-0608.

PMID:
18278184
18.

Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis.

Bedard PW, Clerin V, Sushkova N, Tchernychev B, Antrilli T, Resmini C, Keith JC Jr, Hennan JK, Kaila N, Debernardo S, Janz K, Wang Q, Crandall DL, Schaub RG, Shaw GD, Carter LL.

J Pharmacol Exp Ther. 2008 Feb;324(2):497-506. Epub 2007 Nov 16.

PMID:
18024786
19.

Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.

Green N, Hu Y, Janz K, Li HQ, Kaila N, Guler S, Thomason J, Joseph-McCarthy D, Tam SY, Hotchandani R, Wu J, Huang A, Wang Q, Leung L, Pelker J, Marusic S, Hsu S, Telliez JB, Hall JP, Cuozzo JW, Lin LL.

J Med Chem. 2007 Sep 20;50(19):4728-45. Epub 2007 Aug 23.

PMID:
17715908
20.

Identification of a novel class of selective Tpl2 kinase inhibitors: 4-Alkylamino-[1,7]naphthyridine-3-carbonitriles.

Kaila N, Green N, Li HQ, Hu Y, Janz K, Gavrin LK, Thomason J, Tam S, Powell D, Cuozzo J, Hall JP, Telliez JB, Hsu S, Nickerson-Nutter C, Wang Q, Lin LL.

Bioorg Med Chem. 2007 Oct 1;15(19):6425-42. Epub 2007 Jul 4.

PMID:
17664070
21.

Resolution of venous thrombosis using a novel oral small-molecule inhibitor of P-selectin (PSI-697) without anticoagulation.

Myers DD Jr, Wrobleski SK, Longo C, Bedard PW, Kaila N, Shaw GD, Londy FJ, Rohrer SE, Fex BA, Zajkowski PJ, Meier TR, Hawley AE, Farris DM, Ballard NE, Henke PK, Schaub RG, Wakefield TW.

Thromb Haemost. 2007 Mar;97(3):400-7.

PMID:
17334507
22.

2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid (PSI-697): identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists.

Kaila N, Janz K, Huang A, Moretto A, DeBernardo S, Bedard PW, Tam S, Clerin V, Keith JC Jr, Tsao DH, Sushkova N, Shaw GD, Camphausen RT, Schaub RG, Wang Q.

J Med Chem. 2007 Jan 11;50(1):40-64.

PMID:
17201409
23.

Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.

Kaila N, Janz K, DeBernardo S, Bedard PW, Camphausen RT, Tam S, Tsao DH, Keith JC Jr, Nickerson-Nutter C, Shilling A, Young-Sciame R, Wang Q.

J Med Chem. 2007 Jan 11;50(1):21-39.

PMID:
17201408
24.

Mixture models and subpopulation classification: a pharmacokinetic simulation study and application to metoprolol CYP2D6 phenotype.

Kaila N, Straka RJ, Brundage RC.

J Pharmacokinet Pharmacodyn. 2007 Apr;34(2):141-56. Epub 2006 Oct 12.

PMID:
17053980
25.

Inhibition of Tpl2 kinase and TNFalpha production with quinoline-3-carbonitriles for the treatment of rheumatoid arthritis.

Hu Y, Green N, Gavrin LK, Janz K, Kaila N, Li HQ, Thomason JR, Cuozzo JW, Hall JP, Hsu S, Nickerson-Nutter C, Telliez JB, Lin LL, Tam S.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6067-72. Epub 2006 Sep 14.

PMID:
16973359
26.

Treatment with an oral small molecule inhibitor of P selectin (PSI-697) decreases vein wall injury in a rat stenosis model of venous thrombosis.

Myers DD Jr, Henke PK, Bedard PW, Wrobleski SK, Kaila N, Shaw G, Meier TR, Hawley AE, Schaub RG, Wakefield TW.

J Vasc Surg. 2006 Sep;44(3):625-32.

27.

Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.

Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G, Cuozzo JW, Hall JP, Hsu S, Telliez JB, Lin LL.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92. Epub 2005 Sep 13.

PMID:
16165349
28.

Decreased venous thrombosis with an oral inhibitor of P selectin.

Myers DD Jr, Rectenwald JE, Bedard PW, Kaila N, Shaw GD, Schaub RG, Farris DM, Hawley AE, Wrobleski SK, Henke PK, Wakefield TW.

J Vasc Surg. 2005 Aug;42(2):329-36.

29.

Quinic acid derivatives as sialyl Lewis(x)-mimicking selectin inhibitors: design, synthesis, and crystal structure in complex with E-selectin.

Kaila N, Somers WS, Thomas BE, Thakker P, Janz K, DeBernardo S, Tam S, Moore WJ, Yang R, Wrona W, Bedard PW, Crommie D, Keith JC Jr, Tsao DH, Alvarez JC, Ni H, Marchese E, Patton JT, Magnani JL, Camphausen RT.

J Med Chem. 2005 Jun 30;48(13):4346-57.

PMID:
15974587
30.

Formulation development and stabililty testing of extemporaneous suspension prepared from dapsone tablets.

Kaila N, El-Ries M, Riga A, Alexander K, Dollimore Posthumously D.

Int J Pharm Compd. 2003 May-Jun;7(3):233-9.

PMID:
23979648
31.

Design and synthesis of sialyl Lewis(x) mimics as E- and P-selectin inhibitors.

Kaila N, Thomas BE 4th.

Med Res Rev. 2002 Nov;22(6):566-601. Review.

PMID:
12369089
32.

Beta-C-mannosides as selectin inhibitors.

Kaila N, Chen L, Thomas BE 4th, Tsao D, Tam S, Bedard PW, Camphausen RT, Alvarez JC, Ullas G.

J Med Chem. 2002 Apr 11;45(8):1563-6.

PMID:
11931610
33.

Identification and structural determination of a potent P-selectin inhibitor.

Kaila N, Xu GY, Camphausen RT, Xiang Y.

Bioorg Med Chem. 2001 Mar;9(3):801-6.

PMID:
11310615
34.

Design and synthesis of sialyl Lewis x mimics as E-selectin inhibitors.

Kaila N, Thomas BE 4th, Thakker P, Alvarez JC, Camphausen RT, Crommie D.

Bioorg Med Chem Lett. 2001 Jan 22;11(2):151-5.

PMID:
11206447
35.

Synthesis of the C'D' disaccharide of aureolic acid.

Franck RW, Kaila N.

Carbohydr Res. 1993 Feb 1;239:71-83.

PMID:
8458003

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