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Mosser SD, DeSolms SJ, Giuliani EA, Pompliano DL, Grahm SL, Smith RL, Scolnick EM, Oliff A, Gibbs JB: Selective Inhibition of Ras-dependent Transformation by A Farnesyltransferase Inhibitor. Science
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Kohl N E, Wilson F R, Mosser SD Giuliani E, DeSolms SJ, Conner MW, Anthony NJ, Holtz WJ, Gomez RP, Lee T-J, Smith RL, Grahm SL, Hartman GD, Gibbs JB, Oliff A: Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice. Proc Nail AcadSei(75/1(1994) 91:9141-9145.
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Graham SL, Hartman GD, Koblan KS, Kohl NE, Orner ÇA, Oliff A: Farnesyltranferase Inhibitors Versus Ras Inhibitors. Curr Opin Chem Biol
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Gibbs, J.B.1
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14
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Ashar HR, Armstrong L, James U, Carr DM, Gray K, Taveras A, Doll RJ, Bishop WR, Kirschmeier P T: Biological effects and mechanism of action of farnesyl transferase inhibitors. Chem Res Toxicol (2000) 13:949-952.
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Patnaik, A.1
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22
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33746744904
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90th (Philadelphia): Abs 3413
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Soignet S, Yao S-L, Britten C, Spriggs D, Pezzulli S, McCreery H, Mazina K, Deutsch P, Lee Y, Lobell R, Rosen N, Rowinsky E: Pharmacokinetics and pharmacodynamics of the farnesyl protein transferase inhibitor (L-778,123) in solid tumors. A AC R. (1999) 90th (Philadelphia): Abs 3413
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Yao S-L, Britten C, Spriggs D, Pezzulli S, McCreery H, Mazina K, Deutsch P, Lee Y, Lobell R, Rosen N, Rowinsky E: Pharmacokinetics and Pharmacodynamics of the Farnesyl Protein Transferase Inhibitor (L-778,123) in Solid Tumors. A AC R. (1999)
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Soignet, S.1
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23
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33746719196
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35th (Atlanta): Abs 597.
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Britten CD, Rowinsky E, Yao S-L, Rosen N, Eckhardt SG, Drengler R, Hammond L, Siu LL, Smith L, McCreery H, Pezzulli S, Lee Y, Lobell R, Deutsch P, Von Hoff D, Spriggs D: The farnesyl protein transferase (FPTase) inhibitor L-778,123 in patients with solid tumors. ASCO. (1999) 35th (Atlanta): Abs 597.
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Rowinsky E, Yao S-L, Rosen N, Eckhardt SG, Drengler R, Hammond L, Siu LL, Smith L, McCreery H, Pezzulli S, Lee Y, Lobell R, Deutsch P, von Hoff D, Spriggs D: the Farnesyl Protein Transferase (FPTase) Inhibitor L-778,123 in Patients with Solid Tumors. ASCO. (1999)
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Britten, C.D.1
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24
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33746780556
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219th (San Francisco): MEDI 292.
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Gibbs JB, Anthony NJ, Buser CA, deSolms SJ, Graham SL, Hartman GD, Heimbrook DC, Lobell RB, Koblan KS, Kohl NE, Williams TM: Farnesyltransferase inhibitors as potential anticancer agents. ACS (2000) 219th (San Francisco): MEDI 292.
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Anthony NJ, Buser CA, DeSolms SJ, Graham SL, Hartman GD, Heimbrook DC, Lobell RB, Koblan KS, Kohl NE, Williams TM: Farnesyltransferase Inhibitors As Potential Anticancer Agents. ACS (2000)
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Gibbs, J.B.1
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25
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33746739971
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222nd (Chicago): MED11.
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Williams TM, Dinsmore MJ, Bogusky JM, Bergman JM, Nguyen DN, Stump CA, Zartman CB, Busher CA, Huber DD, Koblan KS, Kohi NE, Lobell RB, Kassahun K, Rodrigues DD, Gibbs JB, Heimbrook DC, Hartman GD, Huff JR, Graham SL: Macrocycle and other constrained analogues of the FTIL-778123. /CS(2001) 222nd (Chicago): MED11.
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Dinsmore MJ, Bogusky JM, Bergman JM, Nguyen DN, Stump CA, Zartman CB, Busher CA, Huber DD, Koblan KS, Kohi NE, Lobell RB, Kassahun K, Rodrigues DD, Gibbs JB, Heimbrook DC, Hartman GD, Huff JR, Graham SL: Macrocycle and Other Constrained Analogues of the FTIL-778123. /CS(2001)
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Williams, T.M.1
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26
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33746736770
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89th (New Orleans): Abs 1847. .
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End D, Skrzat SG, Devine A, Angibaud P, Venet M, Sanz G, Bowden C: R115777, a novel imidazole farnesyl protein transferase inhibitor (FTI): biochemical and cellular effects in H-ras and K-ras dominant systems. AACR (1998) 89th (New Orleans): Abs 1847. .
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Skrzat SG, Devine A, Angibaud P, Venet M, Sanz G, Bowden C: R115777, A Novel Imidazole Farnesyl Protein Transferase Inhibitor (FTI): Biochemical and Cellular Effects in H-ras and K-ras Dominant Systems. AACR (1998)
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End, D.1
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27
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61:131-137.
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End DW, Smets G, Todd AV, Applegate TL, Fuery CJ, Angibaud P, Vemet M, Sanz G, Poignet H, Skrzat S, Devine A, Wouters W, Bowden C: Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 In vivo and in vitro. Cancer Res (2001) 61:131-137.
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Smets G, Todd AV, Applegate TL, Fuery CJ, Angibaud P, Vemet M, Sanz G, Poignet H, Skrzat S, Devine A, Wouters W, Bowden C: Characterization of the Antitumor Effects of the Selective Farnesyl Protein Transferase Inhibitor R115777 in Vivo and in Vitro. Cancer Res (2001)
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End, D.W.1
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28
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11:533.
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Holden SN, Cohen R, Persky M, Mikule C, Morrow M, Richards H, Rodriguez S, Eckhardt, SG: A Phase I pharmacological and biological study of the farnesyl transferase inhibitor (FTI) R115777 and capecitabine in patients (pts) with advanced solid malignancies. MCI EORTC Symp New Drugs Cancer Ther (2000) 11:533.
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Cohen R, Persky M, Mikule C, Morrow M, Richards H, Rodriguez S, Eckhardt, SG: A Phase i Pharmacological and Biological Study of the Farnesyl Transferase Inhibitor (FTI) R115777 and Capecitabine in Patients (Pts) with Advanced Solid Malignancies. MCI EORTC Symp New Drugs Cancer Ther (2000)
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Holden, S.N.1
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29
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33746686821
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36th (New Orleans): 318..-
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Johnson SR, Ellis PA, Houston S, Hickish T, Howes AJ, Palmer P, Horak I: A phase II study of the farnesyltransferase inhibitor R115777 in patients with advanced breast cancer. ASCO (2000) 36th (New Orleans): 318..-
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Ellis PA, Houston S, Hickish T, Howes AJ, Palmer P, Horak I: A Phase II Study of the Farnesyltransferase Inhibitor R115777 in Patients with Advanced Breast Cancer. ASCO (2000)
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Johnson, S.R.1
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30
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18544412314
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18:927-941.
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Zujewski J, Horak ID, Bol CJ, Woestenborghs R, Bowden C, End DW, Piotrovsky VK, Chiao J, Belly RT, Todd A, Kopp WC, Kohler DR, Chow C, Noone M, Hakim FT, Larkin G, Gress RE, Nussenblatt PB, Kremer AB, Cowan KH: Phase I and pharmacokinetic study of farnesyl protein transferase inhibitor R11577 in advanced cancer. J Clin Onco/(2000) 18:927-941.
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Horak ID, Bol CJ, Woestenborghs R, Bowden C, End DW, Piotrovsky VK, Chiao J, Belly RT, Todd A, Kopp WC, Kohler DR, Chow C, Noone M, Hakim FT, Larkin G, Gress RE, Nussenblatt PB, Kremer AB, Cowan KH: Phase i and Pharmacokinetic Study of Farnesyl Protein Transferase Inhibitor R11577 in Advanced Cancer. J Clin Onco/(2000)
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Zujewski, J.1
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32
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7844233665
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3,10-dibromo-6,11-dihydro5H-benzo[5,6]cyclohepta[1,2-b]-pyridin-11 (R)-yl-1 -piperidinylJ-2oxo-ethyl-1-piperidinecarboxamlde (SCH-66336): A very potent farnesyl protein transferase inhibitor as a novel antitumor agent J Med Chem (1998) 41:4890-902.
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Njoroge FG, Taveras AG, Kelly J, Remiszewski S, Mallams AK, Wolin R, Afonso A, Cooper AB, Rane DF, U'u Y-T, Wong J, Vibulbhan B, Pinto P, Deskus J, Alvarez CS, del Rosario J, Connolly M, Wang J, Desai J, Rossman RR, Bishop WR, Patton R, Wang L, Kirschmeier P, Bryant MS, Nomeir AA, Un C-C, Liu M, McPhail AT, Doll RJ, Girijavallabhan VM, Ganguly AK: (+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro5H-benzo[5,6]cyclohepta[1,2-b]- pyridin-11 (R)-yl)-1 -piperidinylJ-2oxo-ethyl]-1-piperidinecarboxamlde (SCH-66336): A very potent farnesyl protein transferase inhibitor as a novel antitumor agent J Med Chem (1998) 41:4890-902.
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Taveras AG, Kelly J, Remiszewski S, Mallams AK, Wolin R, Afonso A, Cooper AB, Rane DF, U'u Y-T, Wong J, Vibulbhan B, Pinto P, Deskus J, Alvarez CS, Del Rosario J, Connolly M, Wang J, Desai J, Rossman RR, Bishop WR, Patton R, Wang L, Kirschmeier P, Bryant MS, Nomeir AA, un C-C, Liu M, McPhail AT, Doll RJ, Girijavallabhan VM, Ganguly AK: (+)-4-2-4-8-Chloro
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Njoroge, F.G.1
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33
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0035865305
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66336 given twice daily to patients with advanced solid tumors. J Clin Oncol (2001 ) 15:1167-1175.
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Eskens FA, Awada A, Cutler DL, de Jonge MJ, Luyten GP, Faber MN, Statkevich P, Sparreboom A, Verweij J, Hanauske AR, Piccart M: Phase I and pharmacokinetic study of the oral farnesyl transferase inhibitor SCH 66336 given twice daily to patients with advanced solid tumors. J Clin Oncol (2001 ) 15:1167-1175.
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Awada A, Cutler DL, de Jonge MJ, Luyten GP, Faber MN, Statkevich P, Sparreboom A, Verweij J, Hanauske AR, Piccart M: Phase i and Pharmacokinetic Study of the Oral Farnesyl Transferase Inhibitor SCH
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Eskens, F.A.1
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34
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33746746339
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92nd (New Orleans): Abs 2629.
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Kirn E, Glisson BS, Meyers ML, Herbst RS, Shin DM, Statkevich P, Bangert S, Hong WK, Khuri FR: A Phase l/ll study of the farnesyl transferase inhibitor (FD) SCH66336 with Paclitaxel in patients with solid tumors. AACR (2001) 92nd (New Orleans): Abs 2629.
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Glisson BS, Meyers ML, Herbst RS, Shin DM, Statkevich P, Bangert S, Hong WK, Khuri FR: A Phase L/ll Study of the Farnesyl Transferase Inhibitor (FD) SCH66336 with Paclitaxel in Patients with Solid Tumors. AACR (2001)
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Kirn, E.1
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35
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0034609805
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2,3,4,5-tetrahydro-1-(1W-imidazol-4-ylmethyl)-3-(phenylmethyl)4-(2- thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent anti-tumor activity. J Med Chem (2000) 43: 3587-3595.
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Hunt JT, Ding CZ, Batorsky R, Bednarz M, Bhide R, Cho Y, Chong S, Chao S, Gullo-Brown J, Guo P, Kirn SH, Lee RYF, Leftheris K, Miller A, Mitt T, Patel M, Penhallow BA, Ricca C, Rose WC, Schmidt R, Slusarchyk WA, Vite G, Manne V: Discovery of (R)-7-cyano2,3,4,5-tetrahydro-1-(1W-imidazol-4-ylmethyl)-3-(phenylmethyl)4-(2- thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent anti-tumor activity. J Med Chem (2000) 43: 3587-3595.
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Ding CZ, Batorsky R, Bednarz M, Bhide R, Cho Y, Chong S, Chao S, Gullo-Brown J, Guo P, Kirn SH, Lee RYF, Leftheris K, Miller A, Mitt T, Patel M, Penhallow BA, Ricca C, Rose WC, Schmidt R, Slusarchyk WA, Vite G, Manne V: Discovery of (R)-7-cyano
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Hunt, J.T.1
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36
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33746729658
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37th (San Francisco): Pt 1,315.
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Mackay HJ, Hoekstra R, Eskens F, Devlin M, Sonnicchsen D, Voi M, Evans TR, Van Vreckem A, Verweij J: A Phase I dose escalating study of BMS-214662 in combination with cisplatin in patients with advanced solid tumors. ASCO (2001) 37th (San Francisco): Pt 1,315.
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Hoekstra R, Eskens F, Devlin M, Sonnicchsen D, Voi M, Evans TR, Van Vreckem A, Verweij J: A Phase i Dose Escalating Study of BMS-214662 in Combination with Cisplatin in Patients with Advanced Solid Tumors. ASCO (2001)
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Mackay, H.J.1
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37
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33746768655
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37th (San Francisco): Pt 1, 311.
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Camacho LH, Soignet SL, Pezzulli S, Canales C, Aghajanian C, Spriggs DS, Damie B, Sonnichsen D: Dose escalation study of oral farnesyl transferase inhibitor (FTI) BMS-214662 with solid tumors. ASCO (2001) 37th (San Francisco): Pt 1, 311.
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Soignet SL, Pezzulli S, Canales C, Aghajanian C, Spriggs DS, Damie B, Sonnichsen D: Dose Escalation Study of Oral Farnesyl Transferase Inhibitor (FTI) BMS-214662 with Solid Tumors. ASCO (2001)
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Camacho, L.H.1
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38
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33746747415
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1-hour infusion in patients with solid tumors: Clinical findings. /1SCO(2001) 37th (San Francisco):?l 1, 312.
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Voi M, Tabemero J, Cooper MR, Marimon I, Van Verckem A, Albanell J, Valverde S, Carreras J, Baselga J: A Phase I study of the farnesyltransferase (FT) inhibitor BMS-214662 administered as a weekly 1-hour infusion in patients with solid tumors: Clinical findings. /1SCO(2001) 37th (San Francisco):?l 1, 312.
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Tabemero J, Cooper MR, Marimon I, Van Verckem A, Albanell J, Valverde S, Carreras J, Baselga J: A Phase i Study of the Farnesyltransferase (FT) Inhibitor BMS-214662 Administered As A Weekly
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Voi, M.1
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39
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33746763620
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37th (San Francisco): Pt 1, 313.
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Kim KB, Shin DM, Summey CC, Kurie JM, Fossella FV, Lee JS, Zinner RG, Glisson BS, Kies MS, Hong WK, Abbaizzese JL, Khuri FR: Phase I study of farnesyl transferase inhibitor, BMS-214662 in solid tumors. ASCO (2001) 37th (San Francisco): Pt 1, 313.
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Shin DM, Summey CC, Kurie JM, Fossella FV, Lee JS, Zinner RG, Glisson BS, Kies MS, Hong WK, Abbaizzese JL, Khuri FR: Phase i Study of Farnesyl Transferase Inhibitor, BMS-214662 in Solid Tumors. ASCO (2001)
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Kim, K.B.1
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40
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33746712131
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37th (San Francisco): Pt 1,314.
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Bailey HH, Mamocha R, Arzoomanian R, Alberti D, Binger K, Volkman J, Feierabend C, Ellingen S, Black S, Hampton K, Cooper M et at Phase I trial of weekly paclitaxel and BMS-214662 in patients with advanced solid tumors. ASCO (2001) 37th (San Francisco): Pt 1,314.
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Mamocha R, Arzoomanian R, Alberti D, Binger K, Volkman J, Feierabend C, Ellingen S, Black S, Hampton K, Cooper M et at Phase i Trial of Weekly Paclitaxel and BMS-214662 in Patients with Advanced Solid Tumors. ASCO (2001)
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Bailey, H.H.1
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41
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33746726328
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37th (San Francisco): Pt 1, 304.
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Tabemero J, Sonnichsen D, Albanell J, DamieB, Rojo F; Christopher L, Marimon I, Dendler R, Trigo JM, Manne S, Garcia M et ah A phase I pharmacokinetic (PK) and serial tumor and PBMC pharmacodynamic study of weekly BMS-214662, a farnesyltransferase (FT) Inhibitor, in patients with advanced solid tumors. ASCO (2001) 37th (San Francisco): Pt 1, 304.
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Sonnichsen D, Albanell J, DamieB, Rojo F; Christopher L, Marimon I, Dendler R, Trigo JM, Manne S, Garcia M et Ah A Phase i Pharmacokinetic (PK) and Serial Tumor and PBMC Pharmacodynamic Study of Weekly BMS-214662, A Farnesyltransferase (FT) Inhibitor, in Patients with Advanced Solid Tumors. ASCO (2001)
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Tabemero, J.1
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42
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33746730931
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222nd (Chicago):MEDI 4.
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Baudoin B, Brealy B, Clerc J-C, Dereu N, El Ahmad Y et at. High throughput organic synthesis, crystallography and early ADME integration applied to the discovery of potent and orally bioavailable chromane and benzoxazine farnesyltransferase inhibitors. ACS (2001) 222nd (Chicago):MEDI 4.
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Brealy B, Clerc J-C, Dereu N, El Ahmad y et At. High Throughput Organic Synthesis, Crystallography and Early ADME Integration Applied to the Discovery of Potent and Orally Bioavailable Chromane and Benzoxazine Farnesyltransferase Inhibitors. ACS (2001)
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Baudoin, B.1
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43
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33746753838
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222nd (Chicago):MEDI 3.
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Taveras AG, Chao J, Aki C, Cooper AB, Strickland C, Gray K, Patton R, Kirschmeier P, Liu M, Nomeir A, Doll RJ, Girijavallabhan VM: SCH66336 and beyond: discovering next generation inhibitors of farnesyl protein transferase. ACS (2001) 222nd (Chicago):MEDI 3.
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Chao J, Aki C, Cooper AB, Strickland C, Gray K, Patton R, Kirschmeier P, Liu M, Nomeir A, Doll RJ, Girijavallabhan VM: SCH66336 and Beyond: Discovering next Generation Inhibitors of Farnesyl Protein Transferase. ACS (2001)
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Taveras, A.G.1
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44
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Yokoyama, K.1
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1-{3-chlorophenyl-4-1-(4-cyanobenzyr)-5-iiTiidazorylmettiyl}-2- piperazinone. WO-00107437 (2001).
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MERCK & Co INC (Varsdona RJ, McCauley JA): Crystal forms of 1-{3-chlorophenyl)-4-[1-(4-cyanobenzyr)-5-iiTiidazorylmettiyl}-2-piperazinone. WO-00107437 (2001).
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8-carbonyl chroman derivatives, preparation and therapeutic use thereof. WO-00109112(2001).
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AVENTIS PHARMA SA (Baudoin B, Jimonet P, Laoui A): Novel 8-carbonyl chroman derivatives, preparation and therapeutic use thereof. WO-00109112(2001).
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59
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8-carbamyl chroman derivatives, preparation and therapeutic use thereof. WO-00109124 (2001).
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AVENTIS PHARMA SA (Baudoin B, Jimonet P): Novel 8-carbamyl chroman derivatives, preparation and therapeutic use thereof. WO-00109124 (2001).
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60
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8-carbonyl chroman derivatives, preparation and therapeutic use thereof. WO-00109125 (2001).
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AVENTIS PHARMA SA (Baudoin B, Jimonet P, Maignan S, Achard D, Mailliet P, Laoui A, Nemecek C): Novel 8-carbonyl chroman derivatives, preparation and therapeutic use thereof. WO-00109125 (2001).
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SA (Baudoin B, Jimonet P, Maignan S, Achard D, Mailliet P, Laoui A, Nemecek C): Novel
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Pharma, A.1
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65
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SCHERING CORPORATION (Afonso A, Baldwin JJ, Doll RJ, Li G, Mallams AK, Njoroge FG, Pane DF, Reader JC, Rossman RR): Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferate diseases. US-06214827 (2001).
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(Afonso A, Baldwin JJ, Doll RJ, Li G, Mallams AK, Njoroge FG, Pane DF, Reader JC, Rossman RR): Tricyclic Compounds Useful for Inhibition of G-protein Function and for Treatment of Proliferate Diseases. US-06214827 (2001).
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Corporation, S.1
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67
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SCHERING CORPORATION (Bishop WR, Doll RJ, Mallams AK, Njoroge FG, Pétrin JM, Piwinski JJ, Wolin RL, Taveras AG, Remiszewski SW): Tricyclic amide and urea compounds useful for Inhibition of Gprotein function and for treatment of proliferative diseases. US06242458 (2001).
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(Bishop WR, Doll RJ, Mallams AK, Njoroge FG, Pétrin JM, Piwinski JJ, Wolin RL, Taveras AG, Remiszewski SW): Tricyclic Amide and Urea Compounds Useful for Inhibition of Gprotein Function and for Treatment of Proliferative Diseases. US06242458 (2001).
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Corporation, S.1
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68
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SCHERING CORPORATION (Doll RJ, Kelly MK, Mallams AK, Njoroge FG, Remiszewski SW, Taveras AG): Tricyclic amides useful for inhibition of G-protein function and for treatment of proliferative diseases. US-06214828 (2001).
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(Doll RJ, Kelly MK, Mallams AK, Njoroge FG, Remiszewski SW, Taveras AG): Tricyclic Amides Useful for Inhibition of G-protein Function and for Treatment of Proliferative Diseases. US-06214828 (2001).
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