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Items: 20

1.

3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma.

Xu R, Wang K, Rizzi JP, Huang H, Grina JA, Schlachter ST, Wang B, Wehn PM, Yang H, Dixon DD, Czerwinski RM, Du X, Ged EL, Han G, Tan H, Wong T, Xie S, Josey JA, Wallace EM.

J Med Chem. 2019 Aug 8;62(15):6876-6893. doi: 10.1021/acs.jmedchem.9b00719. Epub 2019 Jul 8.

PMID:
31282155
2.

Design and Activity of Specific Hypoxia-Inducible Factor-2α (HIF-2α) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385).

Wehn PM, Rizzi JP, Dixon DD, Grina JA, Schlachter ST, Wang B, Xu R, Yang H, Du X, Han G, Wang K, Cao Z, Cheng T, Czerwinski RM, Goggin BS, Huang H, Halfmann MM, Maddie MA, Morton EL, Olive SR, Tan H, Xie S, Wong T, Josey JA, Wallace EM.

J Med Chem. 2018 Nov 8;61(21):9691-9721. doi: 10.1021/acs.jmedchem.8b01196. Epub 2018 Oct 18.

PMID:
30289716
3.

Phase I Dose-Escalation Trial of PT2385, a First-in-Class Hypoxia-Inducible Factor-2α Antagonist in Patients With Previously Treated Advanced Clear Cell Renal Cell Carcinoma.

Courtney KD, Infante JR, Lam ET, Figlin RA, Rini BI, Brugarolas J, Zojwalla NJ, Lowe AM, Wang K, Wallace EM, Josey JA, Choueiri TK.

J Clin Oncol. 2018 Mar 20;36(9):867-874. doi: 10.1200/JCO.2017.74.2627. Epub 2017 Dec 19.

4.

Targeting renal cell carcinoma with a HIF-2 antagonist.

Chen W, Hill H, Christie A, Kim MS, Holloman E, Pavia-Jimenez A, Homayoun F, Ma Y, Patel N, Yell P, Hao G, Yousuf Q, Joyce A, Pedrosa I, Geiger H, Zhang H, Chang J, Gardner KH, Bruick RK, Reeves C, Hwang TH, Courtney K, Frenkel E, Sun X, Zojwalla N, Wong T, Rizzi JP, Wallace EM, Josey JA, Xie Y, Xie XJ, Kapur P, McKay RM, Brugarolas J.

Nature. 2016 Nov 3;539(7627):112-117. doi: 10.1038/nature19796. Epub 2016 Sep 5.

5.

On-target efficacy of a HIF-2α antagonist in preclinical kidney cancer models.

Cho H, Du X, Rizzi JP, Liberzon E, Chakraborty AA, Gao W, Carvo I, Signoretti S, Bruick RK, Josey JA, Wallace EM, Kaelin WG.

Nature. 2016 Nov 3;539(7627):107-111. doi: 10.1038/nature19795. Epub 2016 Sep 5.

6.

A Small-Molecule Antagonist of HIF2α Is Efficacious in Preclinical Models of Renal Cell Carcinoma.

Wallace EM, Rizzi JP, Han G, Wehn PM, Cao Z, Du X, Cheng T, Czerwinski RM, Dixon DD, Goggin BS, Grina JA, Halfmann MM, Maddie MA, Olive SR, Schlachter ST, Tan H, Wang B, Wang K, Xie S, Xu R, Yang H, Josey JA.

Cancer Res. 2016 Sep 15;76(18):5491-500. doi: 10.1158/0008-5472.CAN-16-0473. Epub 2016 Sep 6.

7.

Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.

Jiang Y, Andrews SW, Condroski KR, Buckman B, Serebryany V, Wenglowsky S, Kennedy AL, Madduru MR, Wang B, Lyon M, Doherty GA, Woodard BT, Lemieux C, Geck Do M, Zhang H, Ballard J, Vigers G, Brandhuber BJ, Stengel P, Josey JA, Beigelman L, Blatt L, Seiwert SD.

J Med Chem. 2014 Mar 13;57(5):1753-69. doi: 10.1021/jm400164c. Epub 2013 May 28.

PMID:
23672640
8.

Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.

Wang T, Lamb ML, Block MH, Davies AM, Han Y, Hoffmann E, Ioannidis S, Josey JA, Liu ZY, Lyne PD, MacIntyre T, Mohr PJ, Omer CA, Sjögren T, Thress K, Wang B, Wang H, Yu D, Zhang HJ.

ACS Med Chem Lett. 2012 Jul 26;3(9):705-9. doi: 10.1021/ml300074j. eCollection 2012 Sep 13.

9.

Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors.

Shiozaki M, Maeda K, Miura T, Kotoku M, Yamasaki T, Matsuda I, Aoki K, Yasue K, Imai H, Ubukata M, Suma A, Yokota M, Hotta T, Tanaka M, Hase Y, Haas J, Fryer AM, Laird ER, Littmann NM, Andrews SW, Josey JA, Mimura T, Shinozaki Y, Yoshiuchi H, Inaba T.

J Med Chem. 2011 Apr 28;54(8):2839-63. doi: 10.1021/jm101609j. Epub 2011 Mar 21.

PMID:
21417219
10.

Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors.

Shiozaki M, Imai H, Maeda K, Miura T, Yasue K, Suma A, Yokota M, Ogoshi Y, Haas J, Fryer AM, Laird ER, Littmann NM, Andrews SW, Josey JA, Mimura T, Shinozaki Y, Yoshiuchi H, Inaba T.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6213-7. doi: 10.1016/j.bmcl.2009.08.093. Epub 2009 Sep 3.

PMID:
19767207
11.

Non-nucleoside inhibitors of HCV NS5B polymerase. Part 1: Synthetic and computational exploration of the binding modes of benzothiadiazine and 1,4-benzothiazine HCV NS5b polymerase inhibitors.

Hendricks RT, Fell JB, Blake JF, Fischer JP, Robinson JE, Spencer SR, Stengel PJ, Bernacki AL, Leveque VJ, Le Pogam S, Rajyaguru S, Najera I, Josey JA, Harris JR, Swallow S.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3637-41. doi: 10.1016/j.bmcl.2009.04.119. Epub 2009 May 3.

PMID:
19447623
12.

Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors.

Shiozaki M, Maeda K, Miura T, Ogoshi Y, Haas J, Fryer AM, Laird ER, Littmann NM, Andrews SW, Josey JA, Mimura T, Shinozaki Y, Yoshiuchi H, Inaba T.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1575-80. doi: 10.1016/j.bmcl.2009.02.024. Epub 2009 Feb 11.

PMID:
19243944
13.

3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase.

Hendricks RT, Spencer SR, Blake JF, Fell JB, Fischer JP, Stengel PJ, Leveque VJ, Lepogam S, Rajyaguru S, Najera I, Josey JA, Swallow S.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):410-4. doi: 10.1016/j.bmcl.2008.11.060. Epub 2008 Nov 20.

PMID:
19070486
14.

Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227).

Seiwert SD, Andrews SW, Jiang Y, Serebryany V, Tan H, Kossen K, Rajagopalan PT, Misialek S, Stevens SK, Stoycheva A, Hong J, Lim SR, Qin X, Rieger R, Condroski KR, Zhang H, Do MG, Lemieux C, Hingorani GP, Hartley DP, Josey JA, Pan L, Beigelman L, Blatt LM.

Antimicrob Agents Chemother. 2008 Dec;52(12):4432-41. doi: 10.1128/AAC.00699-08. Epub 2008 Sep 29.

15.

Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.

Wang T, Lamb ML, Scott DA, Wang H, Block MH, Lyne PD, Lee JW, Davies AM, Zhang HJ, Zhu Y, Gu F, Han Y, Wang B, Mohr PJ, Kaus RJ, Josey JA, Hoffmann E, Thress K, Macintyre T, Wang H, Omer CA, Yu D.

J Med Chem. 2008 Aug 14;51(15):4672-84. doi: 10.1021/jm800343j. Epub 2008 Jul 23.

PMID:
18646745
19.

A nucleic acid triple helix formed by a peptide nucleic acid-DNA complex.

Betts L, Josey JA, Veal JM, Jordan SR.

Science. 1995 Dec 15;270(5243):1838-41.

PMID:
8525381
20.

Antisense and antigene properties of peptide nucleic acids.

Hanvey JC, Peffer NJ, Bisi JE, Thomson SA, Cadilla R, Josey JA, Ricca DJ, Hassman CF, Bonham MA, Au KG, et al.

Science. 1992 Nov 27;258(5087):1481-5.

PMID:
1279811

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