-
1
-
-
0036815962
-
Global epidemiology and burden of hepatitis C
-
Kim, W. R. Global epidemiology and burden of hepatitis C Microbes Infect. 2002, 4, 1219-1225
-
(2002)
Microbes Infect.
, vol.4
, pp. 1219-1225
-
-
Kim, W.R.1
-
2
-
-
0033544499
-
Hepatitis C global prevalence (update)
-
WHO Hepatitis C global prevalence (update) Wkly. Epidemiol. Rec. 1999, 74, 425-427
-
(1999)
Wkly. Epidemiol. Rec.
, vol.74
, pp. 425-427
-
-
Who1
-
3
-
-
84876149257
-
Global epidemiology of hepatits C virus infection: New estimates of age-specific antibody to HCV seroprevalence
-
Hanafiah, K. M.; Groeger, J.; Flaxman, A. D.; Wiersma, S. T. Global epidemiology of hepatits C virus infection: new estimates of age-specific antibody to HCV seroprevalence Hepatology 2013, 57, 1333-1342
-
(2013)
Hepatology
, vol.57
, pp. 1333-1342
-
-
Hanafiah, K.M.1
Groeger, J.2
Flaxman, A.D.3
Wiersma, S.T.4
-
4
-
-
84883445154
-
Epidemiology and natural history of HCV infection
-
Hajarazadeh, B.; Grebely, J.; Dore, G. J. Epidemiology and natural history of HCV infection Nat. Rev. Gastroenterol. Hepatol. 2013, 10, 553-562
-
(2013)
Nat. Rev. Gastroenterol. Hepatol.
, vol.10
, pp. 553-562
-
-
Hajarazadeh, B.1
Grebely, J.2
Dore, G.J.3
-
5
-
-
7044272621
-
Pathogenesis of hepatitis C-associated hepatocellular carcinoma
-
Liang, T. J.; Heller, T. Pathogenesis of hepatitis C-associated hepatocellular carcinoma Gastroenterology 2004, 127, S62-S71
-
(2004)
Gastroenterology
, vol.127
-
-
Liang, T.J.1
Heller, T.2
-
6
-
-
0842303291
-
Pathophysiology of hepatitis C virus infection and related liver disease
-
Pawlotsky, J.-M. Pathophysiology of hepatitis C virus infection and related liver disease Trends Microbiol. 2004, 12, 96-102
-
(2004)
Trends Microbiol.
, vol.12
, pp. 96-102
-
-
Pawlotsky, J.-M.1
-
7
-
-
0034120427
-
Clinical significance of hepatitis C virus genotypes
-
Zein, N. N. Clinical significance of hepatitis C virus genotypes Clin. Microbiol. Rev. 2000, 13, 223-235
-
(2000)
Clin. Microbiol. Rev.
, vol.13
, pp. 223-235
-
-
Zein, N.N.1
-
8
-
-
84855544169
-
An updated analysis of hepatitis C virus genotypes and subtypes based on the complete coding region
-
Nakano, T.; Lau, G. M. G.; Lau, G. M. L.; Sugiyama, M.; Mizokami, M. An updated analysis of hepatitis C virus genotypes and subtypes based on the complete coding region Liver Int. 2012, 32, 339-345
-
(2012)
Liver Int.
, vol.32
, pp. 339-345
-
-
Nakano, T.1
Lau, G.M.G.2
Lau, G.M.L.3
Sugiyama, M.4
Mizokami, M.5
-
9
-
-
33845449051
-
Peginterferon and ribavirin for chronic hepatitis C
-
Hoofnagle, J. H.; Seeff, L. B. Peginterferon and ribavirin for chronic hepatitis C N. Engl. J. Med. 2006, 355, 2444-2451
-
(2006)
N. Engl. J. Med.
, vol.355
, pp. 2444-2451
-
-
Hoofnagle, J.H.1
Seeff, L.B.2
-
10
-
-
54349107459
-
Extended-therapy duration for chronic hepatitis C genotype 1: The long and the short of it
-
Pearlman, B. L. Extended-therapy duration for chronic hepatitis C genotype 1: the long and the short of it World J. Gastroenterol. 2008, 14, 3621-3627
-
(2008)
World J. Gastroenterol.
, vol.14
, pp. 3621-3627
-
-
Pearlman, B.L.1
-
11
-
-
1542378867
-
Peginterferon-α2a and ribavirin combination therapy in chronic hepatitis C: A randomized study of treatment duration and ribavirin dose
-
PEGASYS International Study Group
-
Hadziyannis, S. J.; Sette, H.; Morgan, T. R.; Balan, V.; Diago, M.; Marcellin, P.; Ramadori, G.; Bodenheimer, H., Jr.; Bernstein, D.; Rizzetto, M.; Zeuzem, S.; Pockros, P. J.; Lin, A.; Ackrill, A. M.; PEGASYS International Study Group. Peginterferon-α2a and ribavirin combination therapy in chronic hepatitis C: a randomized study of treatment duration and ribavirin dose Ann. Intern. Med. 2004, 140, 346-355
-
(2004)
Ann. Intern. Med.
, vol.140
, pp. 346-355
-
-
Hadziyannis, S.J.1
Sette, H.2
Morgan, T.R.3
Balan, V.4
Diago, M.5
Marcellin, P.6
Ramadori, G.7
Bodenheimer Jr., H.8
Bernstein, D.9
Rizzetto, M.10
Zeuzem, S.11
Pockros, P.J.12
Lin, A.13
Ackrill, A.M.14
-
12
-
-
23944482649
-
Challenges and successes in developing new therapies for hepatitis C
-
De Francesco, R.; Migliaccio, G. Challenges and successes in developing new therapies for hepatitis C Nature 2005, 436, 953-960
-
(2005)
Nature
, vol.436
, pp. 953-960
-
-
De Francesco, R.1
Migliaccio, G.2
-
13
-
-
33644639990
-
SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells
-
Malcolm, B. A.; Liu, R.; Lahser, F.; Agrawal, S.; Belanger, B.; Butkiewicz, N.; Chase, R.; Gheyas, F.; Hart, A.; Hesk, D.; Ingravallo, P.; Jiang, C.; Kong, R.; Lu, J.; Pichardo, J.; Prongay, A.; Skelton, A.; Tong, X.; Venkatraman, S.; Xia, E.; Girijavallabhan, V.; Njoroge, F. G. SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells Antimicrob. Agents Chemother. 2006, 50, 1013-1020
-
(2006)
Antimicrob. Agents Chemother.
, vol.50
, pp. 1013-1020
-
-
Malcolm, B.A.1
Liu, R.2
Lahser, F.3
Agrawal, S.4
Belanger, B.5
Butkiewicz, N.6
Chase, R.7
Gheyas, F.8
Hart, A.9
Hesk, D.10
Ingravallo, P.11
Jiang, C.12
Kong, R.13
Lu, J.14
Pichardo, J.15
Prongay, A.16
Skelton, A.17
Tong, X.18
Venkatraman, S.19
Xia, E.20
Girijavallabhan, V.21
Njoroge, F.G.22
more..
-
14
-
-
33644636312
-
Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease
-
Perni, R. B.; Almquist, S. J.; Byrn, R. A.; Chandorkar, G.; Chaturvedi, P. R.; Courtney, L. F.; Decker, C. J.; Dinehart, K.; Gates, C. A.; Harbeson, S. L.; Heiser, A.; Kalkeri, G.; Kolaczkowski, E.; Lin, K.; Luong, Y.-P.; Rao, B. G.; Taylor, W. P.; Thomson, J. A.; Tung, R. D.; Wei, Y.; Kwong, A. D.; Lin, C. Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease Antimicrob. Agents Chemother. 2006, 50, 899-909
-
(2006)
Antimicrob. Agents Chemother.
, vol.50
, pp. 899-909
-
-
Perni, R.B.1
Almquist, S.J.2
Byrn, R.A.3
Chandorkar, G.4
Chaturvedi, P.R.5
Courtney, L.F.6
Decker, C.J.7
Dinehart, K.8
Gates, C.A.9
Harbeson, S.L.10
Heiser, A.11
Kalkeri, G.12
Kolaczkowski, E.13
Lin, K.14
Luong, Y.-P.15
Rao, B.G.16
Taylor, W.P.17
Thomson, J.A.18
Tung, R.D.19
Wei, Y.20
Kwong, A.D.21
Lin, C.22
more..
-
15
-
-
84865726171
-
New antiviral therapies in the management of HCV infection
-
Farnik, H.; Zeuzem, S. New antiviral therapies in the management of HCV infection Antiviral Ther 2012, 17, 771-783
-
(2012)
Antiviral Ther
, vol.17
, pp. 771-783
-
-
Farnik, H.1
Zeuzem, S.2
-
16
-
-
0036830454
-
Side effects of therapy of hepatitis C and their management
-
Fried, M. W. Side effects of therapy of hepatitis C and their management Hepatology 2002, 36, S237-S244
-
(2002)
Hepatology
, vol.36
-
-
Fried, M.W.1
-
17
-
-
84896270397
-
-
Incivek (telaprevir) in combination with drugs peginterferon alfa and ribavirin (Incivek combination treatment): drug safety communication - serious skin reactions. (posted by the FDA on December 19, 2012
-
Incivek (telaprevir) in combination with drugs peginterferon alfa and ribavirin (Incivek combination treatment): drug safety communication-serious skin reactions. http://www.fda.gov/Safety/MedWatch/SafetyInformation/ SafetyAlertsforHumanMedicalProducts/ucm332860.htm (posted by the FDA on December 19, 2012.
-
-
-
-
18
-
-
84872007723
-
Optimal treatment with boceprevir for chronic HCV infection
-
Maasoumy, B.; Manns, M. P. Optimal treatment with boceprevir for chronic HCV infection Liver Int. 2013, 33 (Suppl. 1) 14-22
-
(2013)
Liver Int.
, vol.33
, Issue.SUPPL. 1
, pp. 14-22
-
-
Maasoumy, B.1
Manns, M.P.2
-
19
-
-
84881314351
-
Novel therapies for hepatitis C - One pill fits all?
-
Manns, M. P.; von Hahn, T. Novel therapies for hepatitis C-One pill fits all? Nat. Rev. Drug Discovery 2013, 12, 595-610
-
(2013)
Nat. Rev. Drug Discovery
, vol.12
, pp. 595-610
-
-
Manns, M.P.1
Von Hahn, T.2
-
20
-
-
0032560602
-
Potent peptide inhibitors of human hepatitis C virus NS3 protease are obtained by optimizing the cleavage products
-
Ingallinella, P.; Altamura, S.; Bianchi, E.; Taliani, M.; Ingenito, R.; Cortese, R.; De Francesco, R.; Steinkuhler, C.; Pessi, A. Potent peptide inhibitors of human hepatitis C virus NS3 protease are obtained by optimizing the cleavage products Biochemistry 1998, 37, 8906-8914
-
(1998)
Biochemistry
, vol.37
, pp. 8906-8914
-
-
Ingallinella, P.1
Altamura, S.2
Bianchi, E.3
Taliani, M.4
Ingenito, R.5
Cortese, R.6
De Francesco, R.7
Steinkuhler, C.8
Pessi, A.9
-
21
-
-
0023653208
-
Extended binding inhibitors of chymotrypsin that interact with leaving group subsites S1′-S3′
-
Imperiali, B.; Abeles, R. H. Extended binding inhibitors of chymotrypsin that interact with leaving group subsites S1′-S3′ Biochemistry 1987, 26, 4474-4477
-
(1987)
Biochemistry
, vol.26
, pp. 4474-4477
-
-
Imperiali, B.1
Abeles, R.H.2
-
22
-
-
84896274193
-
-
World Patent Application WO 2000/0009543, February 24
-
Llinas-Brunet, M.; Bailey, M. D.; Cameron, D.; Faucher, A.-M; Ghiro, E.; Goudreau, N.; Halmos, T.; Poupart, M.-A.; Rancourt, J.; Tsantrizos, Y. S.; Wernic, D. M.; Simoneau, B. Preparation of hepatitis C inhibitory tripeptides. World Patent Application WO 2000/0009543, February 24, 2000.
-
(2000)
Preparation of Hepatitis C Inhibitory Tripeptides
-
-
Llinas-Brunet, M.1
Bailey, M.D.2
Cameron, D.3
Faucher, A.-M.4
Ghiro, E.5
Goudreau, N.6
Halmos, T.7
Poupart, M.-A.8
Rancourt, J.9
Tsantrizos, Y.S.10
Wernic, D.M.11
Simoneau, B.12
-
23
-
-
84896312851
-
-
World Patent Application WO-2002/060926 A2, August 8
-
Campbell, J. A.; Good, A. World Patent Application WO-2002/060926 A2, August 8, 2002.
-
(2002)
-
-
Campbell, J.A.1
Good, A.2
-
24
-
-
0018643960
-
Synthesis and biological activity of carboxyl-terminus modified prostaglandin analogues
-
Schaaf, T. K.; Hess, H.-J. Synthesis and biological activity of carboxyl-terminus modified prostaglandin analogues J. Med. Chem. 1979, 22, 1340-1346
-
(1979)
J. Med. Chem.
, vol.22
, pp. 1340-1346
-
-
Schaaf, T.K.1
Hess, H.-J.2
-
25
-
-
79955419410
-
Synopsis of some recent tactical applications of bioisosteres in drug design
-
Meanwell, N. A. Synopsis of some recent tactical applications of bioisosteres in drug design J. Med. Chem. 2011, 54, 2529-2591
-
(2011)
J. Med. Chem.
, vol.54
, pp. 2529-2591
-
-
Meanwell, N.A.1
-
26
-
-
80055009641
-
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors
-
Lu, X.; Zhang, H.; Li, X.; Chen, G.; Li, Q.-S.; Luo, Y.; Ruan, B.-F.; Chen, X.-W.; Zhu, H.-L. Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors Bioorg. Med. Chem. 2011, 19, 6827-6832
-
(2011)
Bioorg. Med. Chem.
, vol.19
, pp. 6827-6832
-
-
Lu, X.1
Zhang, H.2
Li, X.3
Chen, G.4
Li, Q.-S.5
Luo, Y.6
Ruan, B.-F.7
Chen, X.-W.8
Zhu, H.-L.9
-
27
-
-
84655161591
-
Novel HCV NS5B polymerase inhibitors: Discovery of indole C2 acyl sulfonamides
-
Anilkumar, G. N.; Selyutin, O.; Rosenblum, S. B.; Zeng, Q.; Jiang, Y.; Chan, T.-Y.; Pu, H.; Wang, L.; Bennett, F.; Chen, K. X; Lesburg, C. A.; Duca, J.; Gavalas, S.; Huang, Y.; Pinto, P.; Sannigrahi, M.; Velazquez, F.; Venkatraman, S.; Vibulbhan, B.; Agrawal, S.; Ferrari, E.; Jiang, C.-K.; Huang, H.-C.; Shih, N.-Y.; Njoroge, G. F; Kozlowski, J. A., II. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides Bioorg. Med. Chem. Lett. 2012, 22, 713-717
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 713-717
-
-
Anilkumar, G.N.1
Selyutin, O.2
Rosenblum, S.B.3
Zeng, Q.4
Jiang, Y.5
Chan, T.-Y.6
Pu, H.7
Wang, L.8
Bennett, F.9
Chen, K.X.10
Lesburg, C.A.11
Duca, J.12
Gavalas, S.13
Huang, Y.14
Pinto, P.15
Sannigrahi, M.16
Velazquez, F.17
Venkatraman, S.18
Vibulbhan, B.19
Agrawal, S.20
Ferrari, E.21
Jiang, C.-K.22
Huang, H.-C.23
Shih, N.-Y.24
Njoroge, G.F.25
Kozlowski, J.A.I.I.26
more..
-
28
-
-
84882586245
-
Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors
-
Glunz, P. W.; Zhang, X.; Zou, Y.; Delucca, I.; Nirschl, A. H.; Cheng, X.; Weigelt, C. A.; Cheney, D. L.; Wei, A.; Anumula, R.; Luettgen, J. M.; Rendina, A. R.; Harpel, M.; Luo, G.; Knabb, R.; Wong, P. C.; Wexler, R. R.; Priestley, E. S. Nonbenzamidine acylsulfonamide tissue factor-factor VIIa inhibitors Bioorg. Med. Chem. Lett. 2013, 23, 5244-5248
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 5244-5248
-
-
Glunz, P.W.1
Zhang, X.2
Zou, Y.3
Delucca, I.4
Nirschl, A.H.5
Cheng, X.6
Weigelt, C.A.7
Cheney, D.L.8
Wei, A.9
Anumula, R.10
Luettgen, J.M.11
Rendina, A.R.12
Harpel, M.13
Luo, G.14
Knabb, R.15
Wong, P.C.16
Wexler, R.R.17
Priestley, E.S.18
-
29
-
-
0034812103
-
The hepatitis C virus replicon system and its application to molecular studies
-
Pietschmann, T.; Bartenschlager, R. The hepatitis C virus replicon system and its application to molecular studies Curr. Opin. Drug Discovery Dev. 2001, 4, 657-664
-
(2001)
Curr. Opin. Drug Discovery Dev.
, vol.4
, pp. 657-664
-
-
Pietschmann, T.1
Bartenschlager, R.2
-
30
-
-
0037471233
-
Macrocyclic inhibitors of the NS3 protease as potential therapeutic agents of hepatitis C virus infection
-
Tsantrizos, Y. S.; Bolger, G.; Bonneau, P.; Cameron, D. R.; Goudreau, N.; Kukolj, G.; LaPlante, S. R.; Llinas-Brunet, M.; Nar, H.; Lamarre, D. Macrocyclic inhibitors of the NS3 protease as potential therapeutic agents of hepatitis C virus infection Angew. Chem., Int. Ed. 2003, 42, 1356-1360
-
(2003)
Angew. Chem., Int. Ed.
, vol.42
, pp. 1356-1360
-
-
Tsantrizos, Y.S.1
Bolger, G.2
Bonneau, P.3
Cameron, D.R.4
Goudreau, N.5
Kukolj, G.6
Laplante, S.R.7
Llinas-Brunet, M.8
Nar, H.9
Lamarre, D.10
-
31
-
-
10744231857
-
Inhibitors of hepatitis C virus NS3/4A protease 2. Warhead SAR and optimization
-
Perni, R. B.; Pitlik, J.; Britt, S. D.; Court, J. J.; Courtney, L. F.; Deininger, D. D.; Farmer, L. J.; Gates, C. A.; Harbeson, S. L.; Levin, R. B.; Lin, C.; Lin, K.; Moon, Y.-C.; Luong, Y.-P.; O'Malley, E. T.; Rao, B. G.; Thomson, J. A.; Tung, R. D.; Van Drie, J. H.; Wei, Y. Inhibitors of hepatitis C virus NS3/4A protease 2. Warhead SAR and optimization Bioorg. Med. Chem. Lett. 2004, 14, 1441-1446
-
(2004)
Bioorg. Med. Chem. Lett.
, vol.14
, pp. 1441-1446
-
-
Perni, R.B.1
Pitlik, J.2
Britt, S.D.3
Court, J.J.4
Courtney, L.F.5
Deininger, D.D.6
Farmer, L.J.7
Gates, C.A.8
Harbeson, S.L.9
Levin, R.B.10
Lin, C.11
Lin, K.12
Moon, Y.-C.13
Luong, Y.-P.14
O'Malley, E.T.15
Rao, B.G.16
Thomson, J.A.17
Tung, R.D.18
Van Drie, J.H.19
Wei, Y.20
more..
-
32
-
-
0037997042
-
Acyl sulfonamides as potent protease inhibitors of the hepatitis C virus full-length NS3 (protease-helicase/NTPase): A comparative study of different C-terminals
-
Johansson, A.; Poliakov, A.; Kerblom, E. A; Wiklund, K.; Lindeberg, G.; Winiwarter, S.; Danielson, U. H.; Samuelsson, B.; Hallberg, A. Acyl sulfonamides as potent protease inhibitors of the hepatitis C virus full-length NS3 (protease-helicase/NTPase): a comparative study of different C-terminals Bioorg. Med. Chem. 2003, 11, 2551-2568
-
(2003)
Bioorg. Med. Chem.
, vol.11
, pp. 2551-2568
-
-
Johansson, A.1
Poliakov, A.2
Kerblom, E.A.3
Wiklund, K.4
Lindeberg, G.5
Winiwarter, S.6
Danielson, U.H.7
Samuelsson, B.8
Hallberg, A.9
-
33
-
-
33845956650
-
Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors
-
Oertqvist, P.; Peterson, S. D.; Aakerblom, E.; Gossas, T.; Sabnis, Y. A.; Fransson, R.; Lindeberg, G.; Danielson, U. H.; Karlen, A.; Sandstroem, A. Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors Bioorg. Med. Chem. 2007, 15, 1448-1474
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 1448-1474
-
-
Oertqvist, P.1
Peterson, S.D.2
Aakerblom, E.3
Gossas, T.4
Sabnis, Y.A.5
Fransson, R.6
Lindeberg, G.7
Danielson, U.H.8
Karlen, A.9
Sandstroem, A.10
-
34
-
-
34247585525
-
Evaluation of a diverse set of potential P1 carboxylic acid bioisosteres in hepatitis C virus NS3 protease inhibitors
-
Roenn, R.; Gossas, T.; Sabnis, Y. A.; Daoud, H.; Aakerblom, E.; Danielson, U. H.; Sandstroem, A. Evaluation of a diverse set of potential P1 carboxylic acid bioisosteres in hepatitis C virus NS3 protease inhibitors Bioorg. Med. Chem. 2007, 15, 4057-4068
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 4057-4068
-
-
Roenn, R.1
Gossas, T.2
Sabnis, Y.A.3
Daoud, H.4
Aakerblom, E.5
Danielson, U.H.6
Sandstroem, A.7
-
35
-
-
34548837486
-
Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: Use of cyclopentane and cyclopentene P2-motifs
-
Baeck, M.; Johansson, P.-O.; Waangsell, F.; Thorstensson, F.; Kvarnstroem, I.; Ayesa, S.; Waehling, H.; Pelcman, M.; Jansson, K.; Lindstroem, S.; Wallberg, H.; Classon, B.; Rydergård, C.; Vrang, L.; Hamelink, E.; Hallberg, A.; Rosenquist, A.; Samuelsson, B. Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs Bioorg. Med. Chem. 2007, 15, 7184-7202
-
(2007)
Bioorg. Med. Chem.
, vol.15
, pp. 7184-7202
-
-
Baeck, M.1
Johansson, P.-O.2
Waangsell, F.3
Thorstensson, F.4
Kvarnstroem, I.5
Ayesa, S.6
Waehling, H.7
Pelcman, M.8
Jansson, K.9
Lindstroem, S.10
Wallberg, H.11
Classon, B.12
Rydergård, C.13
Vrang, L.14
Hamelink, E.15
Hallberg, A.16
Rosenquist, A.17
Samuelsson, B.18
-
36
-
-
44149085415
-
Potent triazolyl-proline-based inhibitors of HCV NS3 protease
-
Naud, J.; Lemke, C.; Goudreau, N.; Beaulieu, E.; White, P. D.; Llinas-Brunet, M.; Forgione, P. Potent triazolyl-proline-based inhibitors of HCV NS3 protease Bioorg. Med. Chem. Lett. 2008, 18, 3400-3404
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 3400-3404
-
-
Naud, J.1
Lemke, C.2
Goudreau, N.3
Beaulieu, E.4
White, P.D.5
Llinas-Brunet, M.6
Forgione, P.7
-
37
-
-
50049107010
-
Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350
-
Raboisson, P.; de Kock, H.; Rosenquist, A.; Nilsson, M.; Salvador-Oden, L.; Lin, T.-I.; Roue, N.; Ivanov, V.; Wahling, H.; Wickstrom, K.; Hamelink, E.; Edlund, M.; Vrang, L.; Vendeville, S.; Van de Vreken, W.; McGowan, D.; Tahri, A.; Hu, L.; Boutton, C.; Lenz, O.; Delouvroy, F.; Pille, G.; Surleraux, D.; Wigerinck, P.; Samuelsson, B.; Simmen, K. Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350 Bioorg. Med. Chem. Lett. 2008, 18, 4853-4858
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 4853-4858
-
-
Raboisson, P.1
De Kock, H.2
Rosenquist, A.3
Nilsson, M.4
Salvador-Oden, L.5
Lin, T.-I.6
Roue, N.7
Ivanov, V.8
Wahling, H.9
Wickstrom, K.10
Hamelink, E.11
Edlund, M.12
Vrang, L.13
Vendeville, S.14
Van De Vreken, W.15
McGowan, D.16
Tahri, A.17
Hu, L.18
Boutton, C.19
Lenz, O.20
Delouvroy, F.21
Pille, G.22
Surleraux, D.23
Wigerinck, P.24
Samuelsson, B.25
Simmen, K.26
more..
-
38
-
-
77649127624
-
Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target
-
Cummings, M. D.; Lindberg, J.; Lin, T.-I.; de Kock, H.; Lenz, O.; Lilja, E.; Fellander, S.; Baraznenok, V.; Nystrom, S.; Nilsson, M.; Vrang, L.; Edlund, M.; Rosenquist, A.; Samuelsson, B.; Raboisson, P.; Simmen, K. Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target Angew. Chem., Int. Ed. 2010, 49, 1652-1655
-
(2010)
Angew. Chem., Int. Ed.
, vol.49
, pp. 1652-1655
-
-
Cummings, M.D.1
Lindberg, J.2
Lin, T.-I.3
De Kock, H.4
Lenz, O.5
Lilja, E.6
Fellander, S.7
Baraznenok, V.8
Nystrom, S.9
Nilsson, M.10
Vrang, L.11
Edlund, M.12
Rosenquist, A.13
Samuelsson, B.14
Raboisson, P.15
Simmen, K.16
-
39
-
-
51349136109
-
Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors
-
Raboisson, P.; Lin, T.-I.; de Kock, H.; Vendeville, S.; Van de Vreken, W.; McGowan, D.; Tahri, A.; Hu, L.; Lenz, O.; Delouvroy, F.; Surleraux, D.; Wigerinck, P.; Nilsson, M.; Rosenquist, A.; Samuelsson, B.; Simmen, K. Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors Bioorg. Med. Chem. Lett. 2008, 18, 5095-5100
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 5095-5100
-
-
Raboisson, P.1
Lin, T.-I.2
De Kock, H.3
Vendeville, S.4
Van De Vreken, W.5
McGowan, D.6
Tahri, A.7
Hu, L.8
Lenz, O.9
Delouvroy, F.10
Surleraux, D.11
Wigerinck, P.12
Nilsson, M.13
Rosenquist, A.14
Samuelsson, B.15
Simmen, K.16
-
40
-
-
55549110737
-
Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors
-
Vendeville, S.; Nilsson, M.; de Kock, H.; Lin, T.-I.; Antonov, D.; Classon, B.; Ayesa, S.; Ivanov, V.; Johansson, P.-O.; Kahnberg, P.; Eneroth, A.; Wikstrom, K.; Vrang, L.; Edlund, M.; Lindström, S.; Van de Vreken, W.; McGowan, D.; Tahri, A.; Hu, L.; Lenz, O.; Delouvroy, F.; Van Dooren, M.; Kindermans, N.; Surleraux, D.; Wigerinck, P.; Rosenquist, A.; Samuelsson, B.; Simmen, K.; Raboisson, P. Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors Bioorg. Med. Chem. Lett. 2008, 18, 6189-6193
-
(2008)
Bioorg. Med. Chem. Lett.
, vol.18
, pp. 6189-6193
-
-
Vendeville, S.1
Nilsson, M.2
De Kock, H.3
Lin, T.-I.4
Antonov, D.5
Classon, B.6
Ayesa, S.7
Ivanov, V.8
Johansson, P.-O.9
Kahnberg, P.10
Eneroth, A.11
Wikstrom, K.12
Vrang, L.13
Edlund, M.14
Lindström, S.15
Van De Vreken, W.16
McGowan, D.17
Tahri, A.18
Hu, L.19
Lenz, O.20
Delouvroy, F.21
Van Dooren, M.22
Kindermans, N.23
Surleraux, D.24
Wigerinck, P.25
Rosenquist, A.26
Samuelsson, B.27
Simmen, K.28
Raboisson, P.29
more..
-
41
-
-
77953873770
-
Synthesis and SAR of potent inhibitors of the hepatitis C virus NS3/4A protease: Exploration of P2 quinazoline substituents
-
Nilsson, M.; Belfrage, A. K.; Lindstroem, S.; Waehling, H.; Lindquist, C.; Ayesa, S.; Kahnberg, P.; Pelcman, M.; Benkestock, K.; Agback, T.; Vrang, L.; Terelius, Y.; Wikström, K.; Hamelink, E.; RydergaÌŠrd, C.; Edlund, M.; Eneroth, A.; Raboisson, P.; Lin, T.-I.; de Kock, H.; Wigerinck, P.; Simmen, K.; Samuelsson, B.; Rosenquist, A. Synthesis and SAR of potent inhibitors of the hepatitis C virus NS3/4A protease: exploration of P2 quinazoline substituents Bioorg. Med. Chem. Lett. 2010, 20, 4004-4011
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 4004-4011
-
-
Nilsson, M.1
Belfrage, A.K.2
Lindstroem, S.3
Waehling, H.4
Lindquist, C.5
Ayesa, S.6
Kahnberg, P.7
Pelcman, M.8
Benkestock, K.9
Agback, T.10
Vrang, L.11
Terelius, Y.12
Wikström, K.13
Hamelink, E.14
Rydergaìšrd, C.15
Edlund, M.16
Eneroth, A.17
Raboisson, P.18
Lin, T.-I.19
De Kock, H.20
Wigerinck, P.21
Simmen, K.22
Samuelsson, B.23
Rosenquist, A.24
more..
-
42
-
-
77955314517
-
Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents
-
Lampa, A.; Ehrenberg, A. E.; Gustafsson, S. S.; Vema, A.; Aakerblom, E.; Lindeberg, G.; Karlen, A.; Danielson, U. H.; Sandstroem, A. Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents Bioorg. Med. Chem. 2010, 18, 5413-5424
-
(2010)
Bioorg. Med. Chem.
, vol.18
, pp. 5413-5424
-
-
Lampa, A.1
Ehrenberg, A.E.2
Gustafsson, S.S.3
Vema, A.4
Aakerblom, E.5
Lindeberg, G.6
Karlen, A.7
Danielson, U.H.8
Sandstroem, A.9
-
43
-
-
77955985523
-
Discovery of achiral inhibitors of the hepatitis C virus NS3 protease based on 2(1 H)-pyrazinones
-
Oertqvist, P.; Gising, J.; Ehrenberg, A. E.; Vema, A.; Borg, A.; Karlen, A.; Larhed, M.; Danielson, U. H; Sandstroem, A. Discovery of achiral inhibitors of the hepatitis C virus NS3 protease based on 2(1 H)-pyrazinones Bioorg. Med. Chem. 2010, 18, 6512-6525
-
(2010)
Bioorg. Med. Chem.
, vol.18
, pp. 6512-6525
-
-
Oertqvist, P.1
Gising, J.2
Ehrenberg, A.E.3
Vema, A.4
Borg, A.5
Karlen, A.6
Larhed, M.7
Danielson, U.H.8
Sandstroem, A.9
-
44
-
-
77957366855
-
Structure-activity relationships of HCV NS3 protease inhibitors evaluated on the drug-resistant variants A156T and D168V
-
Oertqvist, P.; Vema, A.; Ehrenberg, A. E.; Dahl, G.; Roenn, R.; Aekerblom, E.; Karlen, A.; Danielson, U. H.; Sandstroem, A. Structure-activity relationships of HCV NS3 protease inhibitors evaluated on the drug-resistant variants A156T and D168V Antiviral Ther. 2010, 15, 841-852
-
(2010)
Antiviral Ther.
, vol.15
, pp. 841-852
-
-
Oertqvist, P.1
Vema, A.2
Ehrenberg, A.E.3
Dahl, G.4
Roenn, R.5
Aekerblom, E.6
Karlen, A.7
Danielson, U.H.8
Sandstroem, A.9
-
45
-
-
78449289368
-
Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
-
Ding, C. Z.; Zhang, Y.-K.; Li, X.; Liu, Y.; Zhang, S.; Zhou, Y.; Plattner, J. J.; Baker, S. J.; Liu, L.; Duan, M.; Jarvest, R. L.; Ji, J.; Kazmierski, W. M.; Tallant, M. D.; Wright, L. L.; Smith, G. K.; Crosby, R. M.; Wang, A. A.; Ni, Z.-J.; Zoue, W.; Wright, J. Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease Bioorg. Med. Chem. Lett. 2010, 20, 7317-7322
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 7317-7322
-
-
Ding, C.Z.1
Zhang, Y.-K.2
Li, X.3
Liu, Y.4
Zhang, S.5
Zhou, Y.6
Plattner, J.J.7
Baker, S.J.8
Liu, L.9
Duan, M.10
Jarvest, R.L.11
Ji, J.12
Kazmierski, W.M.13
Tallant, M.D.14
Wright, L.L.15
Smith, G.K.16
Crosby, R.M.17
Wang, A.A.18
Ni, Z.-J.19
Zoue, W.20
Wright, J.21
more..
-
46
-
-
84862808848
-
Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease
-
Duan, M.; Kazmierski, W.; Crosby, R.; Gartland, M.; Ji, J.; Tallant, M.; Wang, A.; Hamatake, R.; Wright, L.; Wu, M.; Zhang, Y.-K.; Ding, C. Z.; Li, X.; Liu, Y.; Zhang, S.; Zhou, Y.; Plattner, J. J.; Baker, S. J. Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease Bioorg. Med. Chem. Lett. 2012, 22, 2993-2996
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 2993-2996
-
-
Duan, M.1
Kazmierski, W.2
Crosby, R.3
Gartland, M.4
Ji, J.5
Tallant, M.6
Wang, A.7
Hamatake, R.8
Wright, L.9
Wu, M.10
Zhang, Y.-K.11
Ding, C.Z.12
Li, X.13
Liu, Y.14
Zhang, S.15
Zhou, Y.16
Plattner, J.J.17
Baker, S.J.18
-
47
-
-
84859803083
-
Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants
-
Kazmierski, W. M.; Hamatake, R.; Duan, M.; Wright, L. L.; Smith, G. K.; Jarvest, R. L.; Ji, J.-J.; Cooper, J. P.; Tallant, M. D.; Crosby, R. M.; Creech, K.; Wang, A.; Li, X.; Zhang, S.; Zhang, Y.-Y.; Liu, Y.; Ding, C. Z.; Zhou, Y.; Plattner, J. J.; Baker, S. J.; Bu, W.; Liu, L. Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor- resistant mutants J. Med. Chem. 2012, 55, 3021-3026
-
(2012)
J. Med. Chem.
, vol.55
, pp. 3021-3026
-
-
Kazmierski, W.M.1
Hamatake, R.2
Duan, M.3
Wright, L.L.4
Smith, G.K.5
Jarvest, R.L.6
Ji, J.-J.7
Cooper, J.P.8
Tallant, M.D.9
Crosby, R.M.10
Creech, K.11
Wang, A.12
Li, X.13
Zhang, S.14
Zhang, Y.-Y.15
Liu, Y.16
Ding, C.Z.17
Zhou, Y.18
Plattner, J.J.19
Baker, S.J.20
Bu, W.21
Liu, L.22
more..
-
48
-
-
77949803029
-
Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor
-
McCauley, J. A.; McIntyre, C. J.; Rudd, M. T.; Nguyen, K. T.; Romano, J. J.; Butcher, J. W.; Gilbert, K. F.; Bush, K. J.; Holloway, M. K.; Swestock, J.; Wan, B.-L.; Carroll, S. S.; DiMuzio, J. M.; Graham, D. J.; Ludmerer, S. W.; Mao, S.-S.; Stahlhut, M. W.; Fandozzi, C. M.; Trainor, N.; Olsen, D. B.; Vacca, J. P.; Liverton, N. J. Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor J. Med. Chem. 2010, 53, 2443-2463
-
(2010)
J. Med. Chem.
, vol.53
, pp. 2443-2463
-
-
McCauley, J.A.1
McIntyre, C.J.2
Rudd, M.T.3
Nguyen, K.T.4
Romano, J.J.5
Butcher, J.W.6
Gilbert, K.F.7
Bush, K.J.8
Holloway, M.K.9
Swestock, J.10
Wan, B.-L.11
Carroll, S.S.12
Dimuzio, J.M.13
Graham, D.J.14
Ludmerer, S.W.15
Mao, S.-S.16
Stahlhut, M.W.17
Fandozzi, C.M.18
Trainor, N.19
Olsen, D.B.20
Vacca, J.P.21
Liverton, N.J.22
more..
-
49
-
-
41849092643
-
Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease
-
Liverton, N. J.; Holloway, M. K.; McCauley, J. A.; Rudd, M. T.; Butcher, J. W.; Carroll, S. S.; DiMuzio, J.; Fandozzi, C.; Gilbert, K. F.; Mao, S.-S.; McIntyre, C. J.; Nguyen, K. T.; Romano, J. J.; Stahlhut, M.; Wan, B.-L.; Olsen, D. B.; Vacca, J. P. Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease J. Am. Chem. Soc. 2008, 130, 4607-4609
-
(2008)
J. Am. Chem. Soc.
, vol.130
, pp. 4607-4609
-
-
Liverton, N.J.1
Holloway, M.K.2
McCauley, J.A.3
Rudd, M.T.4
Butcher, J.W.5
Carroll, S.S.6
Dimuzio, J.7
Fandozzi, C.8
Gilbert, K.F.9
Mao, S.-S.10
McIntyre, C.J.11
Nguyen, K.T.12
Romano, J.J.13
Stahlhut, M.14
Wan, B.-L.15
Olsen, D.B.16
Vacca, J.P.17
-
50
-
-
56249141811
-
Bismacrocyclic inhibitors of hepatitis C NS3/4a protease
-
McCauley, J. A.; Rudd, M. T.; Nguyen, K. T.; McIntyre, C. J.; Romano, J. J.; Bush, K. J.; Varga, S. L.; Ross, C. W., III; Carroll, S. S.; DiMuzio, J.; Stahlhut, M. W.; Olsen, D. B.; Lyle, T. A.; Vacca, J. P.; Liverton, N. J. Bismacrocyclic inhibitors of hepatitis C NS3/4a protease Angew. Chem., Int. Ed. 2008, 47, 9104-9107
-
(2008)
Angew. Chem., Int. Ed.
, vol.47
, pp. 9104-9107
-
-
McCauley, J.A.1
Rudd, M.T.2
Nguyen, K.T.3
McIntyre, C.J.4
Romano, J.J.5
Bush, K.J.6
Varga, S.L.7
Ross, C.W.8
Carroll, S.S.9
Dimuzio, J.10
Stahlhut, M.W.11
Olsen, D.B.12
Lyle, T.A.13
Vacca, J.P.14
Liverton, N.J.15
-
51
-
-
68549135158
-
Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: Discovery and optimization of a new series of P2-P4 macrocycles
-
Harper, S.; Ferrara, M.; Crescenzi, B.; Pompei, M.; Palumbi, M. C.; Di Muzio, J. M.; Donghi, M.; Fiore, F.; Koch, U.; Liverton, N. J.; Pesci, S.; Petrocchi, A.; Rowley, M.; Summa, V.; Gardelli, C. Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles J. Med. Chem. 2009, 52, 4820-4837
-
(2009)
J. Med. Chem.
, vol.52
, pp. 4820-4837
-
-
Harper, S.1
Ferrara, M.2
Crescenzi, B.3
Pompei, M.4
Palumbi, M.C.5
Di Muzio, J.M.6
Donghi, M.7
Fiore, F.8
Koch, U.9
Liverton, N.J.10
Pesci, S.11
Petrocchi, A.12
Rowley, M.13
Summa, V.14
Gardelli, C.15
-
52
-
-
71049182299
-
Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement
-
Di Francesco, M. E.; Dessole, G.; Nizi, E.; Pace, P.; Koch, U.; Fiore, F.; Pesci, S.; Di Muzio, J.; Monteagudo, E.; Rowley, M.; Summa, V. Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement J. Med. Chem. 2009, 52, 7014-7028
-
(2009)
J. Med. Chem.
, vol.52
, pp. 7014-7028
-
-
Di Francesco, M.E.1
Dessole, G.2
Nizi, E.3
Pace, P.4
Koch, U.5
Fiore, F.6
Pesci, S.7
Di Muzio, J.8
Monteagudo, E.9
Rowley, M.10
Summa, V.11
-
53
-
-
79952662135
-
Discovery of MK-1220: A macrocyclic inhibitor of hepatitis C virus NS3/4A protease with improved preclinical plasma exposure
-
Rudd, M. T.; McCauley, J. A.; Butcher, J. W.; Romano, J. J.; McIntyre, C. J.; Nguyen, K. T.; Gilbert, K. F.; Bush, K. J.; Holloway, M. K.; Swestock, J.; Wan, B.-L.; Carroll, S. S.; DiMuzio, J. M.; Graham, D. J.; Ludmerer, S. W.; Stahlhut, M. W.; Fandozzi, C. M.; Trainor, N.; Olsen, D. B.; Vacca, J. P.; Liverton, N. J. Discovery of MK-1220: a macrocyclic inhibitor of hepatitis C virus NS3/4A protease with improved preclinical plasma exposure ACS Med. Chem. Lett. 2011, 2, 207-212
-
(2011)
ACS Med. Chem. Lett.
, vol.2
, pp. 207-212
-
-
Rudd, M.T.1
McCauley, J.A.2
Butcher, J.W.3
Romano, J.J.4
McIntyre, C.J.5
Nguyen, K.T.6
Gilbert, K.F.7
Bush, K.J.8
Holloway, M.K.9
Swestock, J.10
Wan, B.-L.11
Carroll, S.S.12
Dimuzio, J.M.13
Graham, D.J.14
Ludmerer, S.W.15
Stahlhut, M.W.16
Fandozzi, C.M.17
Trainor, N.18
Olsen, D.B.19
Vacca, J.P.20
Liverton, N.J.21
more..
-
54
-
-
84859752422
-
Discovery of MK-5172, a macrocyclic hepatitis C virus NS3/4a protease inhibitor
-
Harper, S.; McCauley, J. A.; Rudd, M. T.; Ferrara, M.; DiFilippo, M.; Crescenzi, B.; Koch, U.; Petrocchi, A.; Holloway, M. K.; Butcher, J. W.; Romano, J. J.; Bush, K. J.; Gilbert, K. F.; McIntyre, C. J.; Nguyen, K. T.; Nizi, E.; Carroll, S. S.; Ludmerer, S. W.; Burlein, C.; DiMuzio, J. M.; Graham, D. J.; McHale, C. M.; Stahlhut, M. W.; Olsen, D. B.; Monteagudo, E.; Cianetti, S.; Giuliano, C.; Pucci, V.; Trainor, N.; Fandozzi, C. M.; Rowley, M.; Coleman, P. J.; Vacca, J. P.; Summa, V.; Liverton, N. J. Discovery of MK-5172, a macrocyclic hepatitis C virus NS3/4a protease inhibitor ACS Med. Chem. Lett. 2012, 3, 332-336
-
(2012)
ACS Med. Chem. Lett.
, vol.3
, pp. 332-336
-
-
Harper, S.1
McCauley, J.A.2
Rudd, M.T.3
Ferrara, M.4
Difilippo, M.5
Crescenzi, B.6
Koch, U.7
Petrocchi, A.8
Holloway, M.K.9
Butcher, J.W.10
Romano, J.J.11
Bush, K.J.12
Gilbert, K.F.13
McIntyre, C.J.14
Nguyen, K.T.15
Nizi, E.16
Carroll, S.S.17
Ludmerer, S.W.18
Burlein, C.19
Dimuzio, J.M.20
Graham, D.J.21
McHale, C.M.22
Stahlhut, M.W.23
Olsen, D.B.24
Monteagudo, E.25
Cianetti, S.26
Giuliano, C.27
Pucci, V.28
Trainor, N.29
Fandozzi, C.M.30
Rowley, M.31
Coleman, P.J.32
Vacca, J.P.33
Summa, V.34
Liverton, N.J.35
more..
-
55
-
-
84869083263
-
Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease
-
Rudd, M. T.; McCauley, J. A.; Romano, J. J.; Butcher, J. W.; Bush, K.; McIntyre, C. J.; Nguyen, K. T.; Gilbert, K. F.; Lyle, T. A.; Holloway, M. K; Wan, B.-L.; Vacca, J. P.; Summa, V.; Harper, S.; Rowley, M.; Carroll, S. S.; Burlein, C.; DiMuzio, J. M.; Gates, A.; Graham, D. J.; Huang, Q.; Ludmerer, S. W.; McClain, S.; McHale, C.; Stahlhut, M.; Fandozzi, C.; Taylor, A.; Trainor, N.; Olsen, D. B.; Liverton, N. J. Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease Bioorg. Med. Chem. Lett. 2012, 22, 7201-7206
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 7201-7206
-
-
Rudd, M.T.1
McCauley, J.A.2
Romano, J.J.3
Butcher, J.W.4
Bush, K.5
McIntyre, C.J.6
Nguyen, K.T.7
Gilbert, K.F.8
Lyle, T.A.9
Holloway, M.K.10
Wan, B.-L.11
Vacca, J.P.12
Summa, V.13
Harper, S.14
Rowley, M.15
Carroll, S.S.16
Burlein, C.17
Dimuzio, J.M.18
Gates, A.19
Graham, D.J.20
Huang, Q.21
Ludmerer, S.W.22
McClain, S.23
McHale, C.24
Stahlhut, M.25
Fandozzi, C.26
Taylor, A.27
Trainor, N.28
Olsen, D.B.29
Liverton, N.J.30
more..
-
56
-
-
84869083921
-
Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers
-
Rudd, M. T.; McIntyre, C. J.; Romano, J. J.; Butcher, J. W.; Holloway, M. K.; Bush, K.; Nguyen, K. T.; Gilbert, K. F.; Lyle, T. A.; Liverton, N. J.; Wan, B.-L; Summa, V.; Harper, S.; Rowley, M.; Vacca, J. P.; Carroll, S. S.; Burlein, C.; DiMuzio, J. M.; Gates, A.; Graham, D. J.; Huang, Q.; Ludmerer, S. W.; McClain, S.; McHale, C.; Stahlhut, M.; Fandozzi, C.; Taylor, A.; Trainor, N.; Olsen, D. B.; McCauley, J. A. Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers Bioorg. Med. Chem. Lett. 2012, 22, 7207-7213
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 7207-7213
-
-
Rudd, M.T.1
McIntyre, C.J.2
Romano, J.J.3
Butcher, J.W.4
Holloway, M.K.5
Bush, K.6
Nguyen, K.T.7
Gilbert, K.F.8
Lyle, T.A.9
Liverton, N.J.10
Wan, B.-L.11
Summa, V.12
Harper, S.13
Rowley, M.14
Vacca, J.P.15
Carroll, S.S.16
Burlein, C.17
Dimuzio, J.M.18
Gates, A.19
Graham, D.J.20
Huang, Q.21
Ludmerer, S.W.22
McClain, S.23
McHale, C.24
Stahlhut, M.25
Fandozzi, C.26
Taylor, A.27
Trainor, N.28
Olsen, D.B.29
McCauley, J.A.30
more..
-
57
-
-
84870243131
-
Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups
-
Li, X.; Liu, Y.; Zhang, Y.-K.; Plattner, J. J.; Baker, S. J.; Bu, W.; Liu, L.; Zhou, Y.; Ding, C. Z.; Zhang, S.; Kazmierski, W. M.; Hamatake, R.; Duan, M.; Wright, L. L.; Smith, G. K.; Jarvest, R. L.; Ji, J.-J.; Cooper, J. P.; Tallant, M. D.; Crosby, R. M.; Creech, K.; Wang, A. Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups Bioorg. Med. Chem. Lett. 2012, 22, 7351-7356
-
(2012)
Bioorg. Med. Chem. Lett.
, vol.22
, pp. 7351-7356
-
-
Li, X.1
Liu, Y.2
Zhang, Y.-K.3
Plattner, J.J.4
Baker, S.J.5
Bu, W.6
Liu, L.7
Zhou, Y.8
Ding, C.Z.9
Zhang, S.10
Kazmierski, W.M.11
Hamatake, R.12
Duan, M.13
Wright, L.L.14
Smith, G.K.15
Jarvest, R.L.16
Ji, J.-J.17
Cooper, J.P.18
Tallant, M.D.19
Crosby, R.M.20
Creech, K.21
Wang, A.22
more..
-
58
-
-
84879418857
-
Synthesis and optimization of a novel series of HCV NS3 protease inhibitors: 4-arylproline analogs
-
Bilodeau, F.; Bailey, M. D.; Bhardwaj, P. K.; Bordeleau, J.; Forgione, P.; Garneau, M.; Ghiro, E.; Gorys, V.; Halmos, T.; Jolicoeur, E. S.; Leblanc, M.; Lemke, C. T.; Naud, J.; O'Meara, J.; White, P. W.; Llinàs-Brunet, M. Synthesis and optimization of a novel series of HCV NS3 protease inhibitors: 4-arylproline analogs Bioorg. Med. Chem. Lett. 2013, 23, 4267-4271
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 4267-4271
-
-
Bilodeau, F.1
Bailey, M.D.2
Bhardwaj, P.K.3
Bordeleau, J.4
Forgione, P.5
Garneau, M.6
Ghiro, E.7
Gorys, V.8
Halmos, T.9
Jolicoeur, E.S.10
Leblanc, M.11
Lemke, C.T.12
Naud, J.13
O'Meara, J.14
White, P.W.15
Llinàs-Brunet, M.16
-
59
-
-
84879689214
-
Discovery of novel P2 substituted 4-biaryl proline inhibitors of hepatitis C virus NS3 serine protease
-
Bailey, M. D.; Halmos, T.; Lemke, C. T. Discovery of novel P2 substituted 4-biaryl proline inhibitors of hepatitis C virus NS3 serine protease Bioorg. Med. Chem. Lett. 2013, 23, 4436-4440
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 4436-4440
-
-
Bailey, M.D.1
Halmos, T.2
Lemke, C.T.3
-
60
-
-
84879688029
-
Peptide backbone replacement of hepatitis C virus NS3 serine protease C-terminal cleavage product analogs: Discovery of potent succinamide inhibitors
-
Bailey, M. D.; Bordeleau, J.; Garneau, M.; Leblanc, M.; Lemke, C. T.; O'Meara, J.; White, P. W.; Llinas-Brunet, M. Peptide backbone replacement of hepatitis C virus NS3 serine protease C-terminal cleavage product analogs: discovery of potent succinamide inhibitors Bioorg. Med. Chem. Lett. 2013, 23, 4447-4452
-
(2013)
Bioorg. Med. Chem. Lett.
, vol.23
, pp. 4447-4452
-
-
Bailey, M.D.1
Bordeleau, J.2
Garneau, M.3
Leblanc, M.4
Lemke, C.T.5
O'Meara, J.6
White, P.W.7
Llinas-Brunet, M.8
-
61
-
-
84896308671
-
Discovery of hepatitis C Virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution
-
DOI: 10.1021/jm400121t
-
Moreau, B.; O'Meara, J. A.; Bordeleau, J.; Garneau, M.; Godbout, C.; Gorys, V.; Leblanc, M.; Villemure, E.; White, P. W.; Llinas-Brunet, M. Discovery of hepatitis C Virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution. J. Med. Chem. 2013, DOI: 10.1021/jm400121t.
-
(2013)
J. Med. Chem.
-
-
Moreau, B.1
O'Meara, J.A.2
Bordeleau, J.3
Garneau, M.4
Godbout, C.5
Gorys, V.6
Leblanc, M.7
Villemure, E.8
White, P.W.9
Llinas-Brunet, M.10
-
62
-
-
57049176125
-
Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227)
-
Seiwert, S. D.; Andrews, S. W.; Jiang, Y.; Serebryany, V.; Tan, H.; Kossen, K.; Rajagopalan, P. T. R.; Misialek, S.; Stevens, S. K.; Stoycheva, A.; Hong, J.; Lim, S. R.; Qin, X.; Rieger, R.; Condroski, K. R.; Zhang, H.; Do, M. G.; Lemieux, C.; Hingorani, G. P.; Hartley, D. P.; Josey, J. A.; Pan, L.; Beigelman, L.; Blatt, L. M. Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227) Antimicrob. Agents Chemother. 2008, 52, 4432-4441
-
(2008)
Antimicrob. Agents Chemother.
, vol.52
, pp. 4432-4441
-
-
Seiwert, S.D.1
Andrews, S.W.2
Jiang, Y.3
Serebryany, V.4
Tan, H.5
Kossen, K.6
Rajagopalan, P.T.R.7
Misialek, S.8
Stevens, S.K.9
Stoycheva, A.10
Hong, J.11
Lim, S.R.12
Qin, X.13
Rieger, R.14
Condroski, K.R.15
Zhang, H.16
Do, M.G.17
Lemieux, C.18
Hingorani, G.P.19
Hartley, D.P.20
Josey, J.A.21
Pan, L.22
Beigelman, L.23
Blatt, L.M.24
more..
-
63
-
-
84896275496
-
Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent Inhibitor of hepatitis C virus (HCV) NS3/4A protease
-
10.1021/jm400164c
-
Jiang, Y.; Andrews, S. W.; Condroski, K. R.; Buckman, B.; Serebryany, V.; Wenglowsky, S.; Kennedy, A. L.; Madduru, M. R.; Wang, B.; Lyon, M.; Doherty, G. A.; Woodard, B. T.; Lemieux, C.; Geck Do, M.; Zhang, H.; Ballard, J.; Vigers, G.; Brandhuber, B. J.; Stengel, P.; Josey, J. A.; Beigelman, L.; Blatt, L.; Seiwert, S. D. Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent Inhibitor of hepatitis C virus (HCV) NS3/4A protease J. Med. Chem. 2014, 10.1021/jm400164c
-
(2014)
J. Med. Chem.
-
-
Jiang, Y.1
Andrews, S.W.2
Condroski, K.R.3
Buckman, B.4
Serebryany, V.5
Wenglowsky, S.6
Kennedy, A.L.7
Madduru, M.R.8
Wang, B.9
Lyon, M.10
Doherty, G.A.11
Woodard, B.T.12
Lemieux, C.13
Geck Do, M.14
Zhang, H.15
Ballard, J.16
Vigers, G.17
Brandhuber, B.J.18
Stengel, P.19
Josey, J.A.20
Beigelman, L.21
Blatt, L.22
Seiwert, S.D.23
more..
-
64
-
-
84871190914
-
Pharmacokinetics of new oral hepatitis C antiviral drugs
-
Vispo, E.; Barreiro, P.; Soriano, V. Pharmacokinetics of new oral hepatitis C antiviral drugs Expert Opin. Drug Metab. Toxicol. 2013, 9, 5-16
-
(2013)
Expert Opin. Drug Metab. Toxicol.
, vol.9
, pp. 5-16
-
-
Vispo, E.1
Barreiro, P.2
Soriano, V.3
-
65
-
-
84861127035
-
Pharmacokinetic/pharmacodynamic predictors of clinical potency for hepatitis C virus nonnucleoside polymerase and protease inhibitors
-
Reddy, M. B.; Morcos, P. N.; Le Pogam, S.; Ou, Y.; Frank, K.; Lave, T.; Smith, P. Pharmacokinetic/pharmacodynamic predictors of clinical potency for hepatitis C virus nonnucleoside polymerase and protease inhibitors Antimicrob. Agents Chemother. 2012, 56, 3144-3156
-
(2012)
Antimicrob. Agents Chemother.
, vol.56
, pp. 3144-3156
-
-
Reddy, M.B.1
Morcos, P.N.2
Le Pogam, S.3
Ou, Y.4
Frank, K.5
Lave, T.6
Smith, P.7
-
66
-
-
23944476834
-
Unravelling hepatitis C virus replication from genome to function
-
Lindenbach, B. D.; Rice, C. M. Unravelling hepatitis C virus replication from genome to function Nature 2005, 436, 933-938
-
(2005)
Nature
, vol.436
, pp. 933-938
-
-
Lindenbach, B.D.1
Rice, C.M.2
-
67
-
-
80052974259
-
Improving drug candidates by design: A focus on physicochemical properties as a means of improving compound disposition and safety
-
Meanwell, N. A. Improving drug candidates by design: a focus on physicochemical properties as a means of improving compound disposition and safety Chem. Res. Toxicol. 2011, 24, 1420-1456
-
(2011)
Chem. Res. Toxicol.
, vol.24
, pp. 1420-1456
-
-
Meanwell, N.A.1
-
68
-
-
10644231764
-
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: Discovery of potent and specific tripeptide inhibitors
-
Llinàs-Brunet, M.; Bailey, M. D.; Ghiro, E.; Gorys, V.; Halmos, T.; Poirier, M.; Rancourt, J.; Goudreau, N. A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors J. Med. Chem. 2004, 47 (26) 6584-6594
-
(2004)
J. Med. Chem.
, vol.47
, Issue.26
, pp. 6584-6594
-
-
Llinàs-Brunet, M.1
Bailey, M.D.2
Ghiro, E.3
Gorys, V.4
Halmos, T.5
Poirier, M.6
Rancourt, J.7
Goudreau, N.8
-
69
-
-
33748542524
-
Allylic strain in six-membered rings
-
Johnson, F. Allylic strain in six-membered rings Chem. Rev. 1968, 68, 375-413
-
(1968)
Chem. Rev.
, vol.68
, pp. 375-413
-
-
Johnson, F.1
-
70
-
-
0018456201
-
Methoxy group nonplanarity in o -dimethoxybenzenes. Simple predictive models for conformations and rotational barriers in alkoxyaromatics
-
Anderson, G. M., III; Kollman, P. A.; Domelsmith, L. N.; Houk, K. N. Methoxy group nonplanarity in o -dimethoxybenzenes. Simple predictive models for conformations and rotational barriers in alkoxyaromatics J. Am. Chem. Soc. 1979, 101, 2344-2352
-
(1979)
J. Am. Chem. Soc.
, vol.101
, pp. 2344-2352
-
-
Anderson III, G.M.1
Kollman, P.A.2
Domelsmith, L.N.3
Houk, K.N.4
-
71
-
-
0029745052
-
Cation-pi interactions in aromatics of biological and medicinal interest: Electrostatic potential surfaces as a useful qualitative guide
-
Mecozzi, S.; West, A. P.; Doughtery, D. A. Cation-pi interactions in aromatics of biological and medicinal interest: electrostatic potential surfaces as a useful qualitative guide Proc. Natl. Acad. Sci. U.S.A. 1996, 93, 10566-10571
-
(1996)
Proc. Natl. Acad. Sci. U.S.A.
, vol.93
, pp. 10566-10571
-
-
Mecozzi, S.1
West, A.P.2
Doughtery, D.A.3
-
72
-
-
0015816824
-
Aromatic substituent constants for structure-activity correlations
-
Hansch, C.; Leo, A.; Unger, S. H.; Kim, K. H.; Nikaitani, D.; Lien, E. J. Aromatic substituent constants for structure-activity correlations J. Med. Chem. 1973, 16, 1207-1216
-
(1973)
J. Med. Chem.
, vol.16
, pp. 1207-1216
-
-
Hansch, C.1
Leo, A.2
Unger, S.H.3
Kim, K.H.4
Nikaitani, D.5
Lien, E.J.6
-
73
-
-
84876275836
-
The cation-π interaction
-
Dougherty, D. A. The cation-π interaction Acc. Chem. Res. 2013, 46, 885-893
-
(2013)
Acc. Chem. Res.
, vol.46
, pp. 885-893
-
-
Dougherty, D.A.1
-
74
-
-
78649496901
-
Nitrile-containing pharmaceuticals: Efficacious roles of the nitrile pharmacophore
-
Fleming, F. F.; Yao, L.; Ravikumar, P. C.; Funk, L.; Shook, B. C. Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore J. Med. Chem. 2010, 53 (22) 7902-17
-
(2010)
J. Med. Chem.
, vol.53
, Issue.22
, pp. 7902-7917
-
-
Fleming, F.F.1
Yao, L.2
Ravikumar, P.C.3
Funk, L.4
Shook, B.C.5
-
75
-
-
84870203103
-
Understanding substituent effects in noncovalent interactions involving aromatic rings
-
Wheeler, S. E. Understanding substituent effects in noncovalent interactions involving aromatic rings Acc. Chem. Res. 2013, 46, 1029-1038
-
(2013)
Acc. Chem. Res.
, vol.46
, pp. 1029-1038
-
-
Wheeler, S.E.1
-
76
-
-
84884226479
-
P2′ benzene carboxylic acid moiety is associated with decrease in cellular uptake: Evaluation of novel nonpeptidic HIV-1 protease inhibitors containing P2 bis-tetrahydrofuran moiety
-
Yedidi, R. S.; Maeda, K.; Fyvie, W. S.; Steffey, M.; Davis, D. A.; Palmer, I.; Aoki, M.; Kaufman, J. D.; Stahl, S. J.; Garimella, H.; Das, D.; Wingfield, P. T.; Ghosh, A. K.; Mitsuya, H. P2′ benzene carboxylic acid moiety is associated with decrease in cellular uptake: evaluation of novel nonpeptidic HIV-1 protease inhibitors containing P2 bis-tetrahydrofuran moiety Antimicrob. Agents Chemother. 2013, 57 (10) 4920-4927
-
(2013)
Antimicrob. Agents Chemother.
, vol.57
, Issue.10
, pp. 4920-4927
-
-
Yedidi, R.S.1
Maeda, K.2
Fyvie, W.S.3
Steffey, M.4
Davis, D.A.5
Palmer, I.6
Aoki, M.7
Kaufman, J.D.8
Stahl, S.J.9
Garimella, H.10
Das, D.11
Wingfield, P.T.12
Ghosh, A.K.13
Mitsuya, H.14
-
77
-
-
77953784269
-
Transporter studies with the 3- O -sulfate conjugate of 17α-ethinylestradiol: Human liver drug transporters
-
Han, Y.; Busler, D.; Hong, Y.; Tian, Y.; Cliff Chen, C.; Rodrigues, D. A. Transporter studies with the 3- O -sulfate conjugate of 17α- ethinylestradiol: human liver drug transporters Drug Metab. Dispos. 2010, 38 (7) 1072-82
-
(2010)
Drug Metab. Dispos.
, vol.38
, Issue.7
, pp. 1072-1082
-
-
Han, Y.1
Busler, D.2
Hong, Y.3
Tian, Y.4
Cliff Chen, C.5
Rodrigues, D.A.6
-
78
-
-
84896267358
-
-
World Patent Application WO-2003/099274 A1, December 4
-
Wang, Z. A.; Sun, L.-Q.; Sit, S.-Y.; Sin, N.; Scola, P. M.; Hewawasam, P.; Good, A. C.; Chen, Y.; Campbell, J. A. Preparation of peptides as hepatitis C virus inhibitors. World Patent Application WO-2003/099274 A1, December 4, 2003.
-
(2003)
Preparation of Peptides As Hepatitis C Virus Inhibitors
-
-
Wang, Z.A.1
Sun, L.-Q.2
Sit, S.-Y.3
Sin, N.4
Scola, P.M.5
Hewawasam, P.6
Good, A.C.7
Chen, Y.8
Campbell, J.A.9
-
79
-
-
0037100307
-
Synthesis of novel substituted isoquinolones
-
Briet, N.; Brookes, M. H.; Davenport, R. J.; Galvin, F. C. A.; Gilbert, P. J.; Mack, S. R.; Sabin, V. Synthesis of novel substituted isoquinolones Tetrahedron 2002, 58, 5761-5766
-
(2002)
Tetrahedron
, vol.58
, pp. 5761-5766
-
-
Briet, N.1
Brookes, M.H.2
Davenport, R.J.3
Galvin, F.C.A.4
Gilbert, P.J.5
Mack, S.R.6
Sabin, V.7
-
80
-
-
0034675706
-
Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: Towards smaller inhibitors
-
Llinas-Brunet, M.; Bailey, M.; Fazal, G.; Ghiro, E.; Gorys, V.; Goulet, S.; Halmos, T.; Maurice, R.; Poirier, M.; Poupart, M.-A.; Rancourt, J.; Thibeault, D.; Wernic, D.; Lamarre, D. Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors Bioorg. Med. Chem. Lett. 2000, 10, 2267-2270
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 2267-2270
-
-
Llinas-Brunet, M.1
Bailey, M.2
Fazal, G.3
Ghiro, E.4
Gorys, V.5
Goulet, S.6
Halmos, T.7
Maurice, R.8
Poirier, M.9
Poupart, M.-A.10
Rancourt, J.11
Thibeault, D.12
Wernic, D.13
Lamarre, D.14
-
81
-
-
33645407171
-
A facile synthesis of 1-substituted cyclopropylsulfonamides
-
Li, J.; Smith, D.; Wong, H. S.; Campbell, J. A.; Meanwell, N. A.; Scola, P. M. A facile synthesis of 1-substituted cyclopropylsulfonamides Synlett 2006, 725-728
-
(2006)
Synlett
, pp. 725-728
-
-
Li, J.1
Smith, D.2
Wong, H.S.3
Campbell, J.A.4
Meanwell, N.A.5
Scola, P.M.6
-
82
-
-
84866334428
-
Preclinical profile and characterization of the hepatitis C virus NS3 protease inhibitor asunaprevir (BMS-650032)
-
McPhee, F.; Sheaffer, A. K.; Friborg, J.; Hernandez, D.; Falk, P.; Zhai, G.; Levine, S.; Chaniewski, S.; Yu, F.; Barry, D.; Chen, C.; Lee, M. S.; Mosure, K.; Sun, L.-Q.; Sinz, M.; Meanwell, N. A.; Colonno, R. J.; Knipe, J.; Scola, P. Preclinical profile and characterization of the hepatitis C virus NS3 protease inhibitor asunaprevir (BMS-650032) Antimicrob. Agents Chemother. 2012, 56, 5387-5396
-
(2012)
Antimicrob. Agents Chemother.
, vol.56
, pp. 5387-5396
-
-
McPhee, F.1
Sheaffer, A.K.2
Friborg, J.3
Hernandez, D.4
Falk, P.5
Zhai, G.6
Levine, S.7
Chaniewski, S.8
Yu, F.9
Barry, D.10
Chen, C.11
Lee, M.S.12
Mosure, K.13
Sun, L.-Q.14
Sinz, M.15
Meanwell, N.A.16
Colonno, R.J.17
Knipe, J.18
Scola, P.19
-
83
-
-
84856159009
-
Preliminary study of two antiviral agents for hepatitis C genotype 1
-
Lok, A. S.; Gardiner, D. F.; Lawitz, E.; Martorell, C.; Everson, G. T.; Ghalib, R.; Reindollar, R.; Rustgi, V.; McPhee, F.; Wind-Rotolo, M.; Persson, A.; Zhu, K.; Dimitrova, D. I.; Eley, T.; Guo, T.; Grasela, D. M.; Pasquinelli, C. Preliminary study of two antiviral agents for hepatitis C genotype 1 N. Engl. J. Med. 2012, 366, 216-224
-
(2012)
N. Engl. J. Med.
, vol.366
, pp. 216-224
-
-
Lok, A.S.1
Gardiner, D.F.2
Lawitz, E.3
Martorell, C.4
Everson, G.T.5
Ghalib, R.6
Reindollar, R.7
Rustgi, V.8
McPhee, F.9
Wind-Rotolo, M.10
Persson, A.11
Zhu, K.12
Dimitrova, D.I.13
Eley, T.14
Guo, T.15
Grasela, D.M.16
Pasquinelli, C.17
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