-
1
-
-
68149096799
-
The pharmacology of mTOR inhibition
-
Guertin DA, Sabatini DM: The pharmacology of mTOR inhibition. Sci Signal (2009)2(67):pe24.
-
(2009)
Sci. Signal
, vol.2
, Issue.67
-
-
Guertin, D.A.1
Sabatini, D.M.2
-
2
-
-
34250619165
-
The mammalian target of rapamycin signaling pathway: Twists and turns in the road to cancer therapy
-
Provides a detailed description of the PI3K/Akt/mTOR pathway
-
Abraham RT, Gibbons JJ: The mammalian target of rapamycin signaling pathway: Twists and turns in the road to cancer therapy. Clin Cancer Res (2007)13(11):3109-3114. • Provides a detailed description of the PI3K/Akt/mTOR pathway.
-
(2007)
Clin. Cancer Res.
, vol.13
, Issue.11
, pp. 3109-3114
-
-
Abraham, R.T.1
Gibbons, J.J.2
-
3
-
-
67349241955
-
Deptor is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival
-
Peterson TR, Laplante M, Thoreen CC, Sancak Y, Kang SA, Kuehl WM, Gray NS, Sabatini DM: Deptor is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival. Cell (2009)137(5):873-886.
-
(2009)
Cell.
, vol.137
, Issue.5
, pp. 873-886
-
-
Peterson, T.R.1
Laplante, M.2
Thoreen, C.C.3
Sancak, Y.4
Kang, S.A.5
Kuehl, W.M.6
Gray, N.S.7
Sabatini, D.M.8
-
4
-
-
70350418625
-
MTOR signaling at a glance
-
Laplante M, Sabatini DM: mTOR signaling at a glance. J Cell Sci (2009)122(Pt 20):3589-3594.
-
(2009)
J. Cell. Sci.
, vol.122
, Issue.20
, pp. 3589-3594
-
-
Laplante, M.1
Sabatini, D.M.2
-
5
-
-
0029071264
-
TOR kinase domains are required for two distinct functions, only one of which is inhibited by rapamycin
-
Zheng XF, Florentino D, Chen J, Crabtree GR, Schreiber SL: TOR kinase domains are required for two distinct functions, only one of which is inhibited by rapamycin. Cell (1995)82(1):121-130.
-
(1995)
Cell.
, vol.82
, Issue.1
, pp. 121-130
-
-
Zheng, X.F.1
Florentino, D.2
Chen, J.3
Crabtree, G.R.4
Schreiber, S.L.5
-
6
-
-
57449111076
-
MTOR pathway and mTOR inhibitors as agents for cancer therapy
-
Baldo P, Cecco S, Giacomin E, Lazzarini R, Ros B, Marastoni S: mTOR pathway and mTOR inhibitors as agents for cancer therapy. Curr Cancer Drug Targets (2008)8(8):647-665.
-
(2008)
Curr. Cancer Drug Targets
, vol.8
, Issue.8
, pp. 647-665
-
-
Baldo, P.1
Cecco, S.2
Giacomin, E.3
Lazzarini, R.4
Ros, B.5
Marastoni, S.6
-
7
-
-
51449095342
-
Targeting the PI3K-Akt-mTOR pathway: Progress, pitfalls, and promises
-
Yap TA, Garrett MD, Walton MI, Raynaud F, de Bono JS, Workman P: Targeting the PI3K-Akt-mTOR pathway: Progress, pitfalls, and promises. Curr Opin Pharmacol (2008)8(4):393-412.
-
(2008)
Curr. Opin. Pharmacol.
, vol.8
, Issue.4
, pp. 393-412
-
-
Yap, T.A.1
Garrett, M.D.2
Walton, M.I.3
Raynaud, F.4
De Bono, J.S.5
Workman, P.6
-
8
-
-
59749091850
-
A complex interplay between Akt, TSC2 and the two mTOR complexes
-
Huang J, Manning BD: A complex interplay between Akt, TSC2 and the two mTOR complexes. Biochem Soc Trans (2009)37(Pt 1):217-222.
-
(2009)
Biochem. Soc. Trans
, vol.37
, Issue.1
, pp. 217-222
-
-
Huang, J.1
Manning, B.D.2
-
9
-
-
65549145048
-
An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycinresistant functions of mTORC1
-
Describes the ATP-competitive mTOR inhibitor Torin1, which displays antiproliferative properties that are superior to those observed with sirolimus. This superiority is attributed to the ability of Torin1 to inhibit the phosphorylation of 4E-BP1
-
Thoreen CC, Kang SA, Chang JW, Liu Q, Zhang J, Gao Y, Reichling LJ, Sim T, Sabatini DM, Gray NS: An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycinresistant functions of mTORC1. J Biol Chem (2009)284(12):8023-8032. •• Describes the ATP-competitive mTOR inhibitor Torin1, which displays antiproliferative properties that are superior to those observed with sirolimus. This superiority is attributed to the ability of Torin1 to inhibit the phosphorylation of 4E-BP1.
-
(2009)
J. Biol. Chem.
, vol.284
, Issue.12
, pp. 8023-8032
-
-
Thoreen, C.C.1
Kang, S.A.2
Chang, J.W.3
Liu, Q.4
Zhang, J.5
Gao, Y.6
Reichling, L.J.7
Sim, T.8
Sabatini, D.M.9
Gray, N.S.10
-
10
-
-
76549107351
-
Beyond rapalog therapy: Preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2
-
Yu K, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK et al: Beyond rapalog therapy: Preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. Cancer Res (2010)70(2):621-631.
-
(2010)
Cancer Res.
, vol.70
, Issue.2
, pp. 621-631
-
-
Yu, K.1
Shi, C.2
Toral-Barza, L.3
Lucas, J.4
Shor, B.5
Kim, J.E.6
Zhang, W.G.7
Mahoney, R.8
Gaydos, C.9
Tardio, L.10
Kim, S.K.11
-
11
-
-
68249093818
-
Targeting the phosphoinositide 3-kinase pathway in cancer
-
Liu P, Cheng H, Roberts TM, Zhao JJ: Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov (2009)8(8):627-644.
-
(2009)
Nat. Rev. Drug Discov.
, vol.8
, Issue.8
, pp. 627-644
-
-
Liu, P.1
Cheng, H.2
Roberts, T.M.3
Zhao, J.J.4
-
12
-
-
51849098272
-
Drug discovery approaches targeting the PI3K/Akt pathway in cancer
-
Garcia-Echeverria C, Sellers WR: Drug discovery approaches targeting the PI3K/Akt pathway in cancer. Oncogene (2008)27(41):5511-5526.
-
(2008)
Oncogene
, vol.27
, Issue.41
, pp. 5511-5526
-
-
Garcia-Echeverria, C.1
Sellers, W.R.2
-
13
-
-
73849094834
-
The biological effects of isoform-specific PI3-kinase inhibition
-
Ihle NT, Powis G: The biological effects of isoform-specific PI3-kinase inhibition. Curr Opin Drug Discov Devel (2010)13(1):41-49.
-
(2010)
Curr. Opin. Drug Discov. Devel
, vol.13
, Issue.1
, pp. 41-49
-
-
Ihle, N.T.1
Powis, G.2
-
14
-
-
77954653578
-
-
KuDOS Pharmaceuticals Ltd AstraZeneca plc,:, WO-2006090169
-
KuDOS Pharmaceuticals Ltd [AstraZeneca plc] (Hummersone MG, Gomez S, Menear KA, Cockroft FX, Edwards P, Loh VJML, Smith GCM): 2, 4-diamino- pyridopyrimidine derivatives and their use as mTOR inhibitors. WO-2006090169 (2006).
-
(2006)
2, 4-diamino-pyridopyrimidine Derivatives and Their use as MTOR Inhibitors
-
-
Hummersone, M.G.1
Gomez, S.2
Menear, K.A.3
Cockroft, F.X.4
Edwards, P.5
Loh, V.J.M.L.6
Smith, G.C.M.7
-
15
-
-
77954630881
-
-
KuDOS Pharmaceuticals Ltd AstraZeneca plc,:, WO-2007060404
-
KuDOS Pharmaceuticals Ltd [AstraZeneca plc] (Hummersone MG, Gomez S, Menear KA, Smith GCM, Malagu K, Duggan HME, Cockroft FX, Hermann GJ): Pyrido-, pyrazo-, and pyrimidopyrimidine derivatives as mTOR inhibitors. WO-2007060404 (2007).
-
(2007)
Pyrido-, Pyrazo-, and Pyrimidopyrimidine Derivatives as MTOR Inhibitors
-
-
Hummersone, M.G.1
Gomez, S.2
Menear, K.A.3
Smith, G.C.M.4
Malagu, K.5
Duggan, H.M.E.6
Cockroft, F.X.7
Hermann, G.J.8
-
16
-
-
77954632015
-
-
KuDOS Pharmaceuticals Ltd AstraZeneca plc,:, WO-2008023161
-
KuDOS Pharmaceuticals Ltd [AstraZeneca plc] (Duggan HME, Leroux FGM, Malagu K, Martin NMB, Menear KA, Smith GCM): 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mTOR inhibitors. WO-2008023161 (2008).
-
(2008)
2-methylmorpholine Pyrido-, Pyrazo- and Pyrimido-pyrimidine Derivatives as MTOR Inhibitors
-
-
Duggan, H.M.E.1
Leroux, F.G.M.2
Malagu, K.3
Martin, N.M.B.4
Menear, K.A.5
Smith, G.C.M.6
-
17
-
-
75149112670
-
AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity
-
Describes the efficacy of AZD-8055, one of the first selective mTOR inhibitors to enter clinical trials, in a variety of xenograft models
-
Chresta CM, Davies BR, Hickson I, Harding T, Cosulich S, Critchlow SE, Vincent JP, Ellston R, Jones D, Sini P, James D et al: AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity. Cancer Res (2010)70(1):288-298. •• Describes the efficacy of AZD-8055, one of the first selective mTOR inhibitors to enter clinical trials, in a variety of xenograft models.
-
(2010)
Cancer Res.
, vol.70
, Issue.1
, pp. 288-298
-
-
Chresta, C.M.1
Davies, B.R.2
Hickson, I.3
Harding, T.4
Cosulich, S.5
Critchlow, S.E.6
Vincent, J.P.7
Ellston, R.8
Jones, D.9
Sini, P.10
James, D.11
-
18
-
-
77954648257
-
OSI-027, a selective dual mTORC1/TORC2 kinase inhibitor displays broad spectrum anti-tumor activity in preclinical models of human cancer
-
Abs
-
Gokhale PC, Bhagwat SV, Crew AP, Cooke A, Mantis C, Workman JC, Landfair D, Bittner M, Epstein DM, Pachter JA, Wild R: OSI-027, a selective dual mTORC1/TORC2 kinase inhibitor displays broad spectrum anti-tumor activity in preclinical models of human cancer. American Association for Cancer Research Annual Meeting, Washington DC, USA (2010) 101: Abs 4486.
-
(2010)
American Association for Cancer Research Annual Meeting, Washington DC, USA
, vol.101
, pp. 4486
-
-
Gokhale, P.C.1
Bhagwat, S.V.2
Crew, A.P.3
Cooke, A.4
Mantis, C.5
Workman, J.C.6
Landfair, D.7
Bittner, M.8
Epstein, D.M.9
Pachter, J.A.10
Wild, R.11
-
19
-
-
79952489138
-
OSI-027, a potent and selective small molecule mTORC1/mTORC2 kinase inhibitor is mechanistically distinct from rapamycin
-
Abs
-
Bhagwat SV, Crew AP, Gokhale PC, Yao Y, Kahler J, Epstein DM, Wild R, Pachter JA: OSI-027, a potent and selective small molecule mTORC1/mTORC2 kinase inhibitor is mechanistically distinct from rapamycin. American Association for Cancer Research Annual Meeting, Washington DC, USA (2010) 101: Abs 4487.
-
(2010)
American Association for Cancer Research Annual Meeting, Washington DC, USA
, vol.101
, pp. 4487
-
-
Bhagwat, S.V.1
Crew, A.P.2
Gokhale, P.C.3
Yao, Y.4
Kahler, J.5
Epstein, D.M.6
Wild, R.7
Pachter, J.A.8
-
20
-
-
84924280752
-
-
INK128: Intellikine Inc, La Jolla, CA, USA 2009
-
INK128: Intellikine Inc, La Jolla, CA, USA (2009). www.intellikine.com/ pipeline/ink128.html
-
-
-
-
21
-
-
77954630882
-
Novel small molecule inhibitors targeting the mTOR complex in cancer
-
Denver, CO, USA
-
Rommel C: Novel small molecule inhibitors targeting the mTOR complex in cancer. American Association for Cancer Research Annual Meeting, Denver, CO, USA (2009) 100.
-
(2009)
American Association for Cancer Research Annual Meeting
, pp. 100
-
-
Rommel, C.1
-
22
-
-
67650312583
-
KU-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR)
-
Describes the in vitro properties of KU-0063794, a selective mTOR inhibitor that significantly increased the levels of desphosphoyrlated 4E-BP1 compared with sirolimus, demonstrating that dual mTORC1/mTORC2 inhibitors may have a distinct mechanism of action from sirolimus and the rapalogs
-
García-Martínez JM, Moran J, Clarke RG, Gray A, Cosulich SC, Chresta CM, Alessi DR: KU-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem J (2009)421(1):29-42. •• Describes the in vitro properties of KU-0063794, a selective mTOR inhibitor that significantly increased the levels of desphosphoyrlated 4E-BP1 compared with sirolimus, demonstrating that dual mTORC1/mTORC2 inhibitors may have a distinct mechanism of action from sirolimus and the rapalogs.
-
(2009)
Biochem. J.
, vol.421
, Issue.1
, pp. 29-42
-
-
García-Martínez, J.M.1
Moran, J.2
Clarke, R.G.3
Gray, A.4
Cosulich, S.C.5
Chresta, C.M.6
Alessi, D.R.7
-
23
-
-
70349256453
-
The discovery and optimisation of pyrido[2, 3-d]pyrimidine-2, 4-diamines as potent and selective inhibitors of mTOR kinase
-
Reports the mTOR inhibitory activity of KU-0063794 and its selectivity for mTOR over other PI3K isoforms, and describes the antiproliferative activity of the compound in a glioblastoma mouse xenograft model
-
Malagu K, Duggan H, Menear K, Hummersone M, Gomez S, Bailey C, Edwards P, Drzewiecki J, Leroux F, Quesada MJ, Hermann G et al: The discovery and optimisation of pyrido[2, 3-d]pyrimidine-2, 4-diamines as potent and selective inhibitors of mTOR kinase. Bioorg Med Chem Lett (2009)19(20):5950-5953. • Reports the mTOR inhibitory activity of KU-0063794 and its selectivity for mTOR over other PI3K isoforms, and describes the antiproliferative activity of the compound in a glioblastoma mouse xenograft model.
-
(2009)
Bioorg Med. Chem. Lett.
, vol.19
, Issue.20
, pp. 5950-5953
-
-
Malagu, K.1
Duggan, H.2
Menear, K.3
Hummersone, M.4
Gomez, S.5
Bailey, C.6
Edwards, P.7
Drzewiecki, J.8
Leroux, F.9
Quesada, M.J.10
Hermann, G.11
-
24
-
-
77954641882
-
-
OSI Pharmaceuticals Inc Astellas Pharma Inc,WO-2007061737
-
OSI Pharmaceuticals Inc [Astellas Pharma Inc] (Chen X, Coate H, Crew AP, Dong HQ, Honda A, Mulvihill JM, Tavares RAP, Wang J, Werner SD, Mulvihill MK, Siu WK et al Fused bicyclic mTOR inhibitors. WO-2007061737 (2007).
-
(2007)
Fused Bicyclic MTOR Inhibitors
-
-
Chen, X.1
Coate, H.2
Crew, A.P.3
Dong, H.Q.4
Honda, A.5
Mulvihill, J.M.6
Tavares, R.A.P.7
Wang, J.8
Werner, S.D.9
Mulvihill, M.K.10
Siu, W.K.11
-
25
-
-
77954642343
-
-
OSI Pharmaceuticals Inc Astellas Pharma Inc,WO-2007064993
-
OSI Pharmaceuticals Inc [Astellas Pharma Inc] (Crew PA, Dong HQ, Mulvihill JM, Werner DS, Kadalbajoo M, Lauffer R Bicyclic protein kinase inhibitors. WO-2007064993 (2007).
-
(2007)
Bicyclic Protein Kinase Inhibitors
-
-
Crew, P.A.1
Dong, H.Q.2
Mulvihill, J.M.3
Werner, D.S.4
Kadalbajoo, M.5
Lauffer, R.6
-
27
-
-
70450247170
-
High-throughput screening for mTORC1/mTORC2 kinase inhibitors using a chemiluminescence-based ELISA assay
-
Bhagwat SV, Kahler J, Yao Y, Maresca P, Brooks M, Crew A, Boisclair M, Pachter JA: High-throughput screening for mTORC1/mTORC2 kinase inhibitors using a chemiluminescence-based ELISA assay. Assay Drug Dev Technol (2009)7(5):471-478.
-
(2009)
Assay Drug Dev. Technol.
, vol.7
, Issue.5
, pp. 471-478
-
-
Bhagwat, S.V.1
Kahler, J.2
Yao, Y.3
Maresca, P.4
Brooks, M.5
Crew, A.6
Boisclair, M.7
Pachter, J.A.8
-
28
-
-
77954628674
-
-
Intellikine Inc,WO-2009114870
-
Intellikine Inc (Liu Y, Ren P, Li L, Chan K, Wilson ET Kinase inhibitors and methods of use. WO-2009114870 (2009).
-
(2009)
Kinase Inhibitors and Methods of use
-
-
Liu, Y.1
Ren, P.2
Li, L.3
Chan, K.4
Wilson, E.T.5
-
29
-
-
77954652766
-
-
Intellikine Inc,WO-2009114874
-
Intellikine Inc (Ren P, Liu Y, Li L, Chan K, Wilson ET Benzothiazole kinase inhibitors and methods of use. WO-2009114874 (2009).
-
(2009)
Benzothiazole Kinase Inhibitors and Methods of use
-
-
Ren, P.1
Liu, Y.2
Li, L.3
Chan, K.4
Wilson, E.T.5
-
31
-
-
84924232510
-
-
Intellikine Inc/University of California,WO-2010006072
-
Intellikine Inc/University of California (Shokat KM, Fruman D, Ren P, Wilson ET, Li L, Hsieh A, Feldman M, Apsel B, Liu Y, Rommel C, Chan K et al mTOR modulators and uses thereof. WO-2010006072 (2010).
-
(2010)
MTOR Modulators and Uses Thereof
-
-
Shokat, K.M.1
Fruman, D.2
Ren, P.3
Wilson, E.T.4
Li, L.5
Hsieh, A.6
Feldman, M.7
Apsel, B.8
Liu, Y.9
Rommel, C.10
Chan, K.11
-
32
-
-
77954640336
-
-
Intellikine Inc,WO-2010006086
-
Intellikine Inc (Ren P, Liu Y, Li L, Chan K, Wilson ET, Martin M, Rommel C Kinase inhibitors and methods of use. WO-2010006086 (2010).
-
(2010)
Kinase Inhibitors and Methods of use
-
-
Ren, P.1
Liu, Y.2
Li, L.3
Chan, K.4
Wilson, E.T.5
Martin, M.6
Rommel, C.7
-
33
-
-
54249162351
-
Targeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases
-
Describes several mTOR-selective, PI3K-selective and dual mTOR/PI3K inhibitors, and reports their ability to inhibit biomarkers in the mTOR/PI3K pathway. Describes one of the earliest ATP-competitive, selective mTOR inhibitors to be reported, PP-242
-
Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA: Targeted polypharmacology: Discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol (2008)4(11):691-699. •• Describes several mTOR-selective, PI3K-selective and dual mTOR/PI3K inhibitors, and reports their ability to inhibit biomarkers in the mTOR/PI3K pathway. Describes one of the earliest ATP-competitive, selective mTOR inhibitors to be reported, PP-242.
-
(2008)
Nat. Chem. Biol.
, vol.4
, Issue.11
, pp. 691-699
-
-
Apsel, B.1
Blair, J.A.2
Gonzalez, B.3
Nazif, T.M.4
Feldman, M.E.5
Aizenstein, B.6
Hoffman, R.7
Williams, R.L.8
Shokat, K.M.9
Knight, Z.A.10
-
34
-
-
61349141302
-
Active-site inhibitors of mTOR target rapamycinresistant outputs of mTORC1 and mTORC2
-
Describes the biological effects of PP-242 and related compounds, and their ability to inhibit both mTORC1 and mTORC2. Notably, these ATP-competitive inhibitors are distinguished from sirolimus by their ability to inhibit certain mTORC1 functions specifically cap-dependent translation to a greater extent
-
Feldman ME, Apsel B, Uotila A, Loewith R, Knight ZA, Ruggero D, Shokat KM: Active-site inhibitors of mTOR target rapamycinresistant outputs of mTORC1 and mTORC2. PLoS Biol (2009)7(2):e38. •• Describes the biological effects of PP-242 and related compounds, and their ability to inhibit both mTORC1 and mTORC2. Notably, these ATP-competitive inhibitors are distinguished from sirolimus by their ability to inhibit certain mTORC1 functions (specifically cap-dependent translation) to a greater extent.
-
(2009)
PLoS Biol.
, vol.7
, Issue.2
-
-
Feldman, M.E.1
Apsel, B.2
Uotila, A.3
Loewith, R.4
Knight, Z.A.5
Ruggero, D.6
Shokat, K.M.7
-
35
-
-
76349104427
-
Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor
-
Janes MR, Limon JJ, So L, Chen J, Lim RJ, Chavez MA, Vu C, Lilly MB, Mallya S, Ong ST, Konopleva M et al: Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat Med (2010)16(2):205-213.
-
(2010)
Nat. Med.
, vol.16
, Issue.2
, pp. 205-213
-
-
Janes, M.R.1
Limon, J.J.2
So, L.3
Chen, J.4
Lim, R.J.5
Chavez, M.A.6
Vu, C.7
Lilly, M.B.8
Mallya, S.9
Ong, S.T.10
Konopleva, M.11
-
36
-
-
13844312400
-
Phosphorylation and regulation of Akt/PKB by the Rictor-mTOR complex
-
Sarbassov DD, Guertin DA, Ali SM, Sabatini DM: Phosphorylation and regulation of Akt/PKB by the Rictor-mTOR complex. Science (2005)307(5712):1098- 1101.
-
(2005)
Science
, vol.307
, Issue.5712
, pp. 1098-1101
-
-
Sarbassov, D.D.1
Guertin, D.A.2
Ali, S.M.3
Sabatini, D.M.4
-
37
-
-
0035882103
-
The PIF-binding pocket in PDK1 is essential for activation of S6K and SGK, but not PKB
-
Biondi RM, Kieloch A, Currie RA, Deak M, Alessi DR: The PIF-binding pocket in PDK1 is essential for activation of S6K and SGK, but not PKB. EMBO J (2001)20(16):4380-4390.
-
(2001)
EMBO J.
, vol.20
, Issue.16
, pp. 4380-4390
-
-
Biondi, R.M.1
Kieloch, A.2
Currie, R.A.3
Deak, M.4
Alessi, D.R.5
-
38
-
-
0036333737
-
Multiple phosphoinositide 3-kinase-dependent steps in activation of protein kinase B
-
Scheid MP, Marignani PA, Woodgett JR: Multiple phosphoinositide 3-kinase-dependent steps in activation of protein kinase B. Mol Cell Biol (2002)22(17):6247-6260.
-
(2002)
Mol. Cell. Biol.
, vol.22
, Issue.17
, pp. 6247-6260
-
-
Scheid, M.P.1
Marignani, P.A.2
Woodgett, J.R.3
-
39
-
-
68049137608
-
Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin
-
Describes biomarker and efficacy studies for several pyrazolopyrimidine inhibitors and highlights mechanistic differences between rapalogs and ATP-competitive mTOR inhibitors
-
Yu K, Toral-Barza L, Shi C, Zhang WG, Lucas J, Shor B, Kim J, Verheijen J, Curran K, Malwitz DJ, Cole DC et al: Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res (2009)69(15):6232-6240. •• Describes biomarker and efficacy studies for several pyrazolopyrimidine inhibitors and highlights mechanistic differences between rapalogs and ATP-competitive mTOR inhibitors.
-
(2009)
Cancer Res.
, vol.69
, Issue.15
, pp. 6232-6240
-
-
Yu, K.1
Toral-Barza, L.2
Shi, C.3
Zhang, W.G.4
Lucas, J.5
Shor, B.6
Kim, J.7
Verheijen, J.8
Curran, K.9
Malwitz, D.J.10
Cole, D.C.11
-
40
-
-
73249124369
-
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3, 4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituent
-
Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J et al: Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3, 4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituent. J Med Chem (2009)52(24):8010- 8024.
-
(2009)
J. Med. Chem.
, vol.52
, Issue.24
, pp. 8010-8024
-
-
Verheijen, J.C.1
Richard, D.J.2
Curran, K.3
Kaplan, J.4
Lefever, M.5
Nowak, P.6
Malwitz, D.J.7
Brooijmans, N.8
Toral-Barza, L.9
Zhang, W.G.10
Lucas, J.11
-
41
-
-
0033634827
-
Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine
-
Walker EH, Pacold ME, Perisic O, Stephens L, Hawkins PT, Wymann MP, Williams RL: Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine. Mol Cell (2000)6(4):909-919.
-
(2000)
Mol. Cell.
, vol.6
, Issue.4
, pp. 909-919
-
-
Walker, E.H.1
Pacold, M.E.2
Perisic, O.3
Stephens, L.4
Hawkins, P.T.5
Wymann, M.P.6
Williams, R.L.7
-
42
-
-
33646447708
-
Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor
-
Yaguchi S, Fukui Y, Koshimizu I, Yoshimi H, Matsuno T, Gouda H, Hirono S, Yamazaki K, Yamori T: Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor. J Nat Cancer Inst (2006)98(8):545-556.
-
(2006)
J. Nat. Cancer Inst.
, vol.98
, Issue.8
, pp. 545-556
-
-
Yaguchi, S.1
Fukui, Y.2
Koshimizu, I.3
Yoshimi, H.4
Matsuno, T.5
Gouda, H.6
Hirono, S.7
Yamazaki, K.8
Yamori, T.9
-
43
-
-
68049134057
-
-
Wyeth Pfzer Inc,WO-2008115974
-
Wyeth [Pfzer Inc] (Zask A, Nowak PW, Verheijen J, Curran KJ, Kaplan J, Malwitz D, Bursavich MG, Cole DC, Ayral-Kaloustian S, Yu K, Richard DJ et al Pyrazolopyrimidine analogs and their use as mTOR kinase and PI3 kinase inhibitors. WO-2008115974 (2008).
-
(2008)
Pyrazolopyrimidine Analogs and Their use as MTOR Kinase and PI3 Kinase Inhibitors
-
-
Zask, A.1
Nowak, P.W.2
Verheijen, J.3
Curran, K.J.4
Kaplan, J.5
Malwitz, D.6
Bursavich, M.G.7
Cole, D.C.8
Ayral-Kaloustian, S.9
Yu, K.10
Richard, D.J.11
-
44
-
-
76549113435
-
-
Wyeth,WO-2009052145
-
Wyeth (Zask A, Kaplan JA, Verheijen JC, Curran KJ, Richard DJ, Ayral-Kaloustian S Thienopyrimidine and pyrazolopyrimidine compounds and their use as mTOR kinase and PI3 kinase inhibitors. WO-2009052145 (2009).
-
(2009)
Thienopyrimidine and Pyrazolopyrimidine Compounds and Their use as MTOR Kinase and PI3 Kinase Inhibitors
-
-
Zask, A.1
Kaplan, J.A.2
Verheijen, J.C.3
Curran, K.J.4
Richard, D.J.5
Ayral-Kaloustian, S.6
-
45
-
-
77954634957
-
-
Wyeth,US-2009192176
-
Wyeth (Zask A, Dehnhardt CM, Kaplan JA, Delos Santos EG, Venkatesan AM, Verheijen JC 1H-Pyrazolo[3, 4-d]pyrimidine, purine, 7H-purin-8 (9H)-one, 3H-[1, 2, 3]triazolo[4, 5-d] pyrimidine, and thieno[3, 2-d]pyrimidine compounds as mTOR kinase and PI3 kinase inhibitors, and their syntheses. US-2009192176 (2009).
-
(2009)
1H-Pyrazolo[3, 4-d]pyrimidine, Purine, 7H-purin-8 (9H)-one, 3H-[1, 2, 3]triazolo[4, 5-d] Pyrimidine, and Thieno[3, 2-d]pyrimidine Compounds as MTOR Kinase and PI3 Kinase Inhibitors, and Their Syntheses
-
-
Zask, A.1
Dehnhardt, C.M.2
Kaplan, J.A.3
Santos, E.G.D.4
Venkatesan, A.M.5
Verheijen, J.C.6
-
46
-
-
70949092751
-
Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase
-
Nowak P, Cole DC, Brooijmans N, Bursavich MG, Curran KJ, Ellingboe JW, Gibbons JJ, Hollander I, Hu Y, Kaplan J, Malwitz DJ et al: Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase. J Med Chem (2009)52(22):7081-7089.
-
(2009)
J. Med. Chem.
, vol.52
, Issue.22
, pp. 7081-7089
-
-
Nowak, P.1
Cole, D.C.2
Brooijmans, N.3
Bursavich, M.G.4
Curran, K.J.5
Ellingboe, J.W.6
Gibbons, J.J.7
Hollander, I.8
Hu, Y.9
Kaplan, J.10
Malwitz, D.J.11
-
47
-
-
72249113146
-
Novel purine and pyrazolo[3, 4-d]pyrimidine inhibitors of PI3 kinase-α: Hit to lead studies
-
Gilbert AM, Nowak P, Brooijmans N, Bursavich MG, Dehnhardt C, Santos ED, Feldberg LR, Hollander I, Kim S, Lombardi S, Park K et al: Novel purine and pyrazolo[3, 4-d]pyrimidine inhibitors of PI3 kinase-α: Hit to lead studies. Bioorg Med Chem Lett (2010)20(2):636-639.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.2
, pp. 636-639
-
-
Gilbert, A.M.1
Nowak, P.2
Brooijmans, N.3
Bursavich, M.G.4
Dehnhardt, C.5
Santos, E.D.6
Feldberg, L.R.7
Hollander, I.8
Kim, S.9
Lombardi, S.10
Park, K.11
-
48
-
-
69049087738
-
ATP-competitive inhibitors of the mammalian target of rapamycin: Design and synthesis of highly potent and selective pyrazolopyrimidines
-
The first report of the arylureiodphenyl-pyrazolopyrimidines as mTOR inhibitors. Describes how modification of the urea moiety affects mTOR potency and selectivity over PI3K, and presents a binding model for this class of compounds
-
Zask A, Verheijen JC, Curran K, Kaplan J, Richard DJ, Nowak P, Malwitz DJ, Brooijmans N, Bard J, Svenson K, Lucas J et al: ATP-competitive inhibitors of the mammalian target of rapamycin: Design and synthesis of highly potent and selective pyrazolopyrimidines. J Med Chem (2009)52(16):5013-5016. •• The first report of the arylureiodphenyl-pyrazolopyrimidines as mTOR inhibitors. Describes how modification of the urea moiety affects mTOR potency and selectivity over PI3K, and presents a binding model for this class of compounds.
-
(2009)
J. Med. Chem.
, vol.52
, Issue.16
, pp. 5013-5016
-
-
Zask, A.1
Verheijen, J.C.2
Curran, K.3
Kaplan, J.4
Richard, D.J.5
Nowak, P.6
Malwitz, D.J.7
Brooijmans, N.8
Bard, J.9
Svenson, K.10
Lucas, J.11
-
49
-
-
75449120554
-
Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent
-
Curran KJ, Verheijen JC, Kaplan J, Richard DJ, Toral-Barza L, Hollander I, Lucas J, Ayral-Kaloustian S, Yu K, Zask A: Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent. Bioorg Med Chem Lett (2010)20(4):1440-1444.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.4
, pp. 1440-1444
-
-
Curran, K.J.1
Verheijen, J.C.2
Kaplan, J.3
Richard, D.J.4
Toral-Barza, L.5
Hollander, I.6
Lucas, J.7
Ayral-Kaloustian, S.8
Yu, K.9
Zask, A.10
-
50
-
-
72249090391
-
Discovery of 3, 6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3, 4-d] pyrimidines and 2-arylthieno[3, 2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
-
Kaplan J, Verheijen JC, Brooijmans N, Toral-Barza L, Hollander I, Yu K, Zask A: Discovery of 3, 6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3, 4-d] pyrimidines and 2-arylthieno[3, 2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Bioorg Med Chem Lett (2010)20(2):640-643.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.2
, pp. 640-643
-
-
Kaplan, J.1
Verheijen, J.C.2
Brooijmans, N.3
Toral-Barza, L.4
Hollander, I.5
Yu, K.6
Zask, A.7
-
51
-
-
73249140565
-
Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors
-
Provides an initial report of the dramatic effect of structural modifications to the morpholine moiety on selectivity for mTOR over PI3K
-
Zask A, Kaplan J, Verheijen JC, Richard DJ, Curran K, Brooijmans N, Bennett EM, Toral-Barza L, Hollander I, Ayral-Kaloustian S, Yu K: Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors. J Med Chem (2009)52(24):7942-7945. •• Provides an initial report of the dramatic effect of structural modifications to the morpholine moiety on selectivity for mTOR over PI3K.
-
(2009)
J. Med. Chem.
, vol.52
, Issue.24
, pp. 7942-7945
-
-
Zask, A.1
Kaplan, J.2
Verheijen, J.C.3
Richard, D.J.4
Curran, K.5
Brooijmans, N.6
Bennett, E.M.7
Toral-Barza, L.8
Hollander, I.9
Ayral-Kaloustian, S.10
Yu, K.11
-
52
-
-
71849089048
-
Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: Discovery of highly potent and selective analogs with improved human microsomal stability
-
Describes the enhancement of human microsomal stability and cellular activity resulting from the attachment of water-solubilizing groups to the urea group of pyrazolopyrimidines
-
Richard DJ, Verheijen JC, Curran K, Kaplan J, Toral-Barza L, Hollander I, Lucas J, Yu K, Zask A: Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: Discovery of highly potent and selective analogs with improved human microsomal stability. Bioorg Med Chem Lett (2009)19(24):6830-6835. • Describes the enhancement of human microsomal stability and cellular activity resulting from the attachment of water-solubilizing groups to the urea group of pyrazolopyrimidines.
-
(2009)
Bioorg Med. Chem. Lett.
, vol.19
, Issue.24
, pp. 6830-6835
-
-
Richard, D.J.1
Verheijen, J.C.2
Curran, K.3
Kaplan, J.4
Toral-Barza, L.5
Hollander, I.6
Lucas, J.7
Yu, K.8
Zask, A.9
-
54
-
-
70350518100
-
Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases
-
Link W, Oyarzabal J, Serelde BG, Albarran MI, Rabal O, Cebriá A, Alfonso P, Fominaya J, Renner O, Peregrina S, Soilán D et al: Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. J Biol Chem (2009)284(41):28392-28400.
-
(2009)
J. Biol. Chem.
, vol.284
, Issue.41
, pp. 28392-28400
-
-
Link, W.1
Oyarzabal, J.2
Serelde, B.G.3
Albarran, M.I.4
Rabal, O.5
Cebriá, A.6
Alfonso, P.7
Fominaya, J.8
Renner, O.9
Peregrina, S.10
Soilán, D.11
-
55
-
-
77954631542
-
-
Genentech Inc Roche Holding AG/F Hoffman-La Roche Ltd,WO-2009097446
-
Genentech Inc [Roche Holding AG]/F Hoffman-La Roche Ltd (Dotson J, Heffron T, Olivero A, Sutherlin DP, Wang S, Zhu B, Chuckowree I, Folkes A, Wan NC Pyrazolopyrimidine PI3K inhibitor compounds and methods of use. WO-2009097446 (2009).
-
(2009)
Pyrazolopyrimidine PI3K Inhibitor Compounds and Methods of use
-
-
Dotson, J.1
Heffron, T.2
Olivero, A.3
Sutherlin, D.P.4
Wang, S.5
Zhu, B.6
Chuckowree, I.7
Folkes, A.8
Wan, N.C.9
-
56
-
-
77954647261
-
-
Wyeth Pfizer Inc,WO-2009091788
-
Wyeth [Pfizer Inc] (Dehnhardt CM, Venkatesan AM, Delos Santos EG, Chen Z, Dos Santos O, Brooijmans N, Zask A, Verheijen JC, Ayral-Kaloustian S 3H-[1, 2, 3]Triazolo[4, 5-d] pyrimidine compounds, their use as mTOR kinase and PI3 kinase inhibitors, and their syntheses. WO-2009091788 (2009).
-
(2009)
3H-[1, 2, 3]Triazolo[4, 5-d] Pyrimidine Compounds, Their use as MTOR Kinase and PI3 Kinase Inhibitors, and Their Syntheses
-
-
Dehnhardt, C.M.1
Venkatesan, A.M.2
Santos, E.G.D.3
Chen, Z.4
Santos, O.D.5
Brooijmans, N.6
Zask, A.7
Verheijen, J.C.8
Ayral-Kaloustian, S.9
-
57
-
-
77249098372
-
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: Discovery of PKI-402
-
Dehnhardt CM, Venkatesan AM, Delos Santos E, Chen Z, Santos O, Ayral-Kaloustian S, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J et al: Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: Discovery of PKI-402. J Med Chem (2010)53(2):798-810.
-
(2010)
J. Med. Chem.
, vol.53
, Issue.2
, pp. 798-810
-
-
Dehnhardt, C.M.1
Venkatesan, A.M.2
Santos, E.D.3
Chen, Z.4
Santos, O.5
Ayral-Kaloustian, S.6
Brooijmans, N.7
Mallon, R.8
Hollander, I.9
Feldberg, L.10
Lucas, J.11
-
58
-
-
84924229598
-
-
Wyeth Pfizer Inc,WO-2008116129
-
Wyeth [Pfizer Inc] (Bursavich MG, Venkatesan AM, Nowak PW, Lombardi S, Gilbert AM, Dehnhardt CM, Dos Santos O, Denos Santos EG, Brooijmans N, Ayral-Kaloustian S, Chen Z et al Imidazolopyrimidine analogs and their use as PI3 kinase and mTOR inhibitors. WO-2008116129 (2008).
-
(2008)
Imidazolopyrimidine Analogs and Their use as PI3 Kinase and MTOR Inhibitors
-
-
Bursavich, M.G.1
Venkatesan, A.M.2
Nowak, P.W.3
Lombardi, S.4
Gilbert, A.M.5
Dehnhardt, C.M.6
Santos, O.D.7
Santos, E.G.D.8
Brooijmans, N.9
Ayral-Kaloustian, S.10
Chen, Z.11
-
59
-
-
72249111293
-
Novel imidazolopyrimidines as dual PI3-kinase/mTOR inhibitors
-
Venkatesan AM, Dehnhardt CM, Chen Z, Santos ED, Dos Santos O, Bursavich M, Gilbert AM, Ellingboe JW, Ayral-Kaloustian S, Khafizova G, Brooijmans N et al: Novel imidazolopyrimidines as dual PI3-kinase/mTOR inhibitors. Bioorg Med Chem Lett (2010)20(2):653-656.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.2
, pp. 653-656
-
-
Venkatesan, A.M.1
Dehnhardt, C.M.2
Chen, Z.3
Santos, E.D.4
Santos, O.D.5
Bursavich, M.6
Gilbert, A.M.7
Ellingboe, J.W.8
Ayral-Kaloustian, S.9
Khafizova, G.10
Brooijmans, N.11
-
63
-
-
84924235041
-
Novel potent and selective mTOR/PI3K inhibitors that inhibit tumor growth in animal models through efficient and sustained shut down of the PI3K/Akt signaling pathway
-
Denver, CO, USA, Abs
-
Bonday Z, Williams M, Nagaraj H, Poulsen A, Hentze H, Chen DZ, Blanchard S, Hart S, Goh KC, Goh KL, Goh MK et al: Novel potent and selective mTOR/PI3K inhibitors that inhibit tumor growth in animal models through efficient and sustained shut down of the PI3K/Akt signaling pathway. American Association for Cancer Research Annual Meeting, Denver, CO, USA (2009) 100: Abs 3710.
-
(2009)
American Association for Cancer Research Annual Meeting
, vol.100
, pp. 3710
-
-
Bonday, Z.1
Williams, M.2
Nagaraj, H.3
Poulsen, A.4
Hentze, H.5
Chen, D.Z.6
Blanchard, S.7
Hart, S.8
Goh, K.C.9
Goh, K.L.10
Goh, M.K.11
-
64
-
-
77954639869
-
-
Wyeth Pfizer Inc,WO-2009111547
-
Wyeth [Pfizer Inc] (Venkatesan AM, Chen Z, Dos Santos O, Brooijmans N, Gopalsamy M 7H-Pyrrolo[2, 3-h]quinazoline compounds, their use as mTOR kinase and PI3 kinase inhibitors, and their synthesis. WO-2009111547 (2009).
-
(2009)
7H-Pyrrolo[2, 3-h]quinazoline Compounds, Their use as MTOR Kinase and PI3 Kinase Inhibitors, and Their Synthesis
-
-
Venkatesan, A.M.1
Chen, Z.2
Santos, O.D.3
Brooijmans, N.4
Gopalsamy, M.5
-
65
-
-
77954654348
-
-
Wyeth Pfizer Inc,WO-2009070524
-
Wyeth [Pfizer Inc] (Chen Z, Venkatesan AM, Dehnhardt CM, Ayral-Kaloustian S, Mansour TS, Zask A, Verheijen JC Pyrrolo[3, 2-d]pyrimidine compounds and their use as PI3 kinase and mTOR kinase inhibitors. WO-2009070524 (2009).
-
(2009)
Pyrrolo[3, 2-d]pyrimidine Compounds and Their use as PI3 Kinase and MTOR Kinase Inhibitors
-
-
Chen, Z.1
Venkatesan, A.M.2
Dehnhardt, C.M.3
Ayral-Kaloustian, S.4
Mansour, T.S.5
Zask, A.6
Verheijen, J.C.7
-
66
-
-
77951096315
-
Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors
-
Chen Z, Venkatesan AM, Dehnhardt CM, Ayral-Kaloustian S, Brooijmans N, Mallon R, Feldberg L, Hollander I, Lucas J, Yu K, Kong F et al: Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors. J Med Chem (2010)53(8):3169-3182.
-
(2010)
J. Med. Chem.
, vol.53
, Issue.8
, pp. 3169-3182
-
-
Chen, Z.1
Venkatesan, A.M.2
Dehnhardt, C.M.3
Ayral-Kaloustian, S.4
Brooijmans, N.5
Mallon, R.6
Feldberg, L.7
Hollander, I.8
Lucas, J.9
Yu, K.10
Kong, F.11
-
67
-
-
77954646271
-
-
Chugai Pharmaceutical Co Ltd Roche Holding AG,WO-2008018426
-
Chugai Pharmaceutical Co Ltd [Roche Holding AG] (Shimma N, Ebiike H, Ohwada J, Kawada H, Morikami K, Nakamura M, Yoshida M, Ishii N, Hasegawa M, Yamamoto S, Koyama K Pyrimidine derivative as PI3K inhibitor and use thereof. WO-2008018426 (2008).
-
(2008)
Pyrimidine Derivative as PI3K Inhibitor and use Thereof
-
-
Shimma, N.1
Ebiike, H.2
Ohwada, J.3
Kawada, H.4
Morikami, K.5
Nakamura, M.6
Yoshida, M.7
Ishii, N.8
Hasegawa, M.9
Yamamoto, S.10
Koyama, K.11
-
68
-
-
77954642494
-
-
Chugai Pharmaceutical Co Ltd Roche Holding AG,WO-2009099163
-
Chugai Pharmaceutical Co Ltd [Roche Holding AG] (Ebiike H, Ohwada J, Koyama K, Murata T, Hong WS Pyrrolopyrimidin derivative for use as PI3K inhibitor, and use thereof. WO-2009099163 (2009).
-
(2009)
Pyrrolopyrimidin Derivative for use as PI3K Inhibitor, and use Thereof
-
-
Ebiike, H.1
Ohwada, J.2
Koyama, K.3
Murata, T.4
Hong, W.S.5
-
69
-
-
77954038469
-
-
F Hoffman-La Roche Ltd,WO-2008152387
-
F Hoffman-La Roche Ltd (Baker SJ, Hancox TC, Pegg NA, Nadin AJ, Price S Quinazoline derivatives as PI3 kinase inhibitors. WO-2008152387 (2008).
-
(2008)
Quinazoline Derivatives as PI3 Kinase Inhibitors
-
-
Baker, S.J.1
Hancox, T.C.2
Pegg, N.A.3
Nadin, A.J.4
Price, S.5
-
70
-
-
77954647749
-
-
F Hoffman-La Roche Ltd,WO-2008152390
-
F Hoffman-La Roche Ltd (Hancox TC, Pegg NA, Beswick MC, Blench TJ, Dechaux EA, Kulagowski JJ, Nadin AJ, Price S Thiazolopyrimidines and their uses as inhibitors of phosphatidylinositol-3 kinase. WO-2008152390 (2008).
-
(2008)
Thiazolopyrimidines and Their Uses as Inhibitors of Phosphatidylinositol- 3 Kinase
-
-
Hancox, T.C.1
Pegg, N.A.2
Beswick, M.C.3
Blench, T.J.4
Dechaux, E.A.5
Kulagowski, J.J.6
Nadin, A.J.7
Price, S.8
-
72
-
-
84947733332
-
-
F Hoffman-La Roche Ltd,WO-2009053716
-
F Hoffman-La Roche Ltd (Goldsmith P, Hancox TC, Hudson A, Pegg NA, Neil A, Kulagowski JJ, Nadin AJ, Price S Purine derivatives useful as PI3 kinase inhibitors. WO-2009053716 (2009).
-
(2009)
Purine Derivatives Useful as PI3 Kinase Inhibitors
-
-
Goldsmith, P.1
Hancox, T.C.2
Hudson, A.3
Pegg, N.A.4
Neil, A.5
Kulagowski, J.J.6
Nadin, A.J.7
Price, S.8
-
73
-
-
77954628364
-
-
Genentech Inc Roche Holding AG/F Hoffman-La Roche Ltd,WO-2009146406
-
Genentech Inc [Roche Holding AG]/F Hoffman-La Roche Ltd (Castanedo G, Chuckowree I, Folkes A, Sutherlin DP, Wan NC Purine PI3K inhibitor compounds and methods of use. WO-2009146406 (2009).
-
(2009)
Purine PI3K Inhibitor Compounds and Methods of use
-
-
Castanedo, G.1
Chuckowree, I.2
Folkes, A.3
Sutherlin, D.P.4
Wan, N.C.5
-
74
-
-
77954637046
-
-
Genentech Inc Roche Holding AG/F Hoffman-La Roche Ltd,WO-2009042607
-
Genentech Inc [Roche Holding AG]/F Hoffman-La Roche Ltd (Castanedo G, Gunzner JL, Malesky K, Mathieu S, Olivero AG, Sutherin DP, Wang S, Zhu B, Chuckowree I, Folkes A, Oxenford S et al Thiazolopyrimidine PI3K inhibitor compounds and methods of use. WO-2009042607 (2009).
-
(2009)
Thiazolopyrimidine PI3K Inhibitor Compounds and Methods of use
-
-
Castanedo, G.1
Gunzner, J.L.2
Malesky, K.3
Mathieu, S.4
Olivero, A.G.5
Sutherin, D.P.6
Wang, S.7
Zhu, B.8
Chuckowree, I.9
Folkes, A.10
Oxenford, S.11
-
75
-
-
77954631213
-
-
Genentech Inc Roche Holding AG,WO-2010014939
-
Genentech Inc [Roche Holding AG] (Bergeron P, Cohen F, Estrada A, Koehler MFT, Lau KHL, Ly C, Lyssikatos JP, Ortwine DF, Pei Z, Zhao X Pyrimidine compounds, compositions and methods of use. WO-2010014939 (2010).
-
(2010)
Pyrimidine Compounds, Compositions and Methods of use
-
-
Bergeron, P.1
Cohen, F.2
Estrada, A.3
Koehler, M.F.T.4
Lau, K.H.L.5
Ly, C.6
Lyssikatos, J.P.7
Ortwine, D.F.8
Pei, Z.9
Zhao, X.10
-
76
-
-
80054122335
-
-
Takeda Pharmaceutical Co Ltd,WO-2010008847
-
Takeda Pharmaceutical Co Ltd (Dong Q, Gong X, Hirose M, Jin B, Zhou F PI3K/mTOR inhibitors. WO-2010008847 (2010).
-
(2010)
PI3K/mTOR Inhibitors
-
-
Dong, Q.1
Gong, X.2
Hirose, M.3
Jin, B.4
Zhou, F.5
-
77
-
-
77954637193
-
-
Piramed Pharma Roche Holding AG,WO-2007122410
-
Piramed Pharma [Roche Holding AG] (Baker SJ, Goldsmith PJ, Hancox TC, Pegg NA, Price S, Shuttleworth SJ, Sohal S Pyrimidine derivatives as PI3K inhibitors. WO-2007122410 (2007).
-
(2007)
Pyrimidine Derivatives as PI3K Inhibitors
-
-
Baker, S.J.1
Goldsmith, P.J.2
Hancox, T.C.3
Pegg, N.A.4
Price, S.5
Shuttleworth, S.J.6
Sohal, S.7
-
78
-
-
77954629969
-
-
Piramed Pharma Roche Holding AG,WO-2007132171
-
Piramed Pharma [Roche Holding AG] (Chuckowree IS, Folkes AJ, Goldsmith P, Hancox TC, Shuttleworth SJ Pharmaceutical compounds. WO-2007132171 (2007).
-
(2007)
Pharmaceutical Compounds
-
-
Chuckowree, I.S.1
Folkes, A.J.2
Goldsmith, P.3
Hancox, T.C.4
Shuttleworth, S.J.5
-
79
-
-
77954629969
-
-
Piramed Pharma Roche Holding AG/Genentech Inc Roche Holding AG,WO-2007127175
-
Piramed Pharma [Roche Holding AG]/Genentech Inc [Roche Holding AG] (Folkes A, Shuttleworth S, Chuckowree I, Oxenford S, Wan NC, Castanedo G, Gunzner J, Heffron T, Mathieu S, Olivero A, Sutherlin DP et al Pharmaceutical compounds. WO-2007127175 (2007).
-
(2007)
Pharmaceutical Compounds
-
-
Folkes, A.1
Shuttleworth, S.2
Chuckowree, I.3
Oxenford, S.4
Wan, N.C.5
Castanedo, G.6
Gunzner, J.7
Heffron, T.8
Mathieu, S.9
Olivero, A.10
Sutherlin, D.P.11
-
80
-
-
84924243803
-
-
Piramed Pharma Roche Holding AG/Genentech Inc Roche Holding AG,WO-2007127183
-
Piramed Pharma [Roche Holding AG]/Genentech Inc [Roche Holding AG] (Castanedo G, Goldsmith G, Gunzner J, Heffron T, Malesky K, Mathieu S, Olivero A, Sutherlin DP, Tsui V, Wang S, Weismann C et al Phosphoinositide 3 kinase inhibitor compounds and pharmaceutical compositions containing them. WO-2007127183 (2007).
-
(2007)
Phosphoinositide 3 Kinase Inhibitor Compounds and Pharmaceutical Compositions Containing Them
-
-
Castanedo, G.1
Goldsmith, G.2
Gunzner, J.3
Heffron, T.4
Malesky, K.5
Mathieu, S.6
Olivero, A.7
Sutherlin, D.P.8
Tsui, V.9
Wang, S.10
Weismann, C.11
-
82
-
-
77954632676
-
-
Piramed Pharma Roche Holding AG/Genentech Inc Roche Holding AG,WO-2008070740
-
Piramed Pharma [Roche Holding AG]/Genentech Inc [Roche Holding AG] (Bayliss T, Chuckowree I, Folkes A, Oxenford S, Wan NC, Castanedo G, Goldsmith R, Gunzner J, Heffron T, Mathieu S, Olivero A et al Phosphoinositide 3-kinase inhibitor compounds and methods of use. WO-2008070740 (2008).
-
(2008)
Phosphoinositide 3-kinase Inhibitor Compounds and Methods of use
-
-
Bayliss, T.1
Chuckowree, I.2
Folkes, A.3
Oxenford, S.4
Wan, N.C.5
Castanedo, G.6
Goldsmith, R.7
Gunzner, J.8
Heffron, T.9
Mathieu, S.10
Olivero, A.11
-
83
-
-
77954645651
-
-
Piramed Pharma Roche Holding AG/Genentech Inc Roche Holding AG,WO-2008073785
-
Piramed Pharma [Roche Holding AG]/Genentech Inc [Roche Holding AG] (Castanedo G, Dotson J, Goldsmith R, Gunzner J, Heffron T, Mathieu S, Olivero A, Staben S, Sutherlin DP, Tsui V, Wang S et al Phosphoinositide 3-kinase inhibitor compounds and methods of use. WO-2008073785 (2008).
-
(2008)
Phosphoinositide 3-kinase Inhibitor Compounds and Methods of use
-
-
Castanedo, G.1
Dotson, J.2
Goldsmith, R.3
Gunzner, J.4
Heffron, T.5
Mathieu, S.6
Olivero, A.7
Staben, S.8
Sutherlin, D.P.9
Tsui, V.10
Wang, S.11
-
84
-
-
77954650115
-
-
Genentech Inc Roche Holding AG/F Hoffmann-La Roche Ltd,WO-2009036082
-
Genentech Inc [Roche Holding AG]/F Hoffmann-La Roche Ltd (Belvin M, Friedman L, Hoeflich K, Sampath D, Vijapurkar U, Wallin J, Johnson L, Singh M, Patel S Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use. WO-2009036082 (2009).
-
(2009)
Combinations of Phosphoinositide 3-kinase Inhibitor Compounds and Chemotherapeutic Agents, and Methods of use
-
-
Belvin, M.1
Friedman, L.2
Hoeflich, K.3
Sampath, D.4
Vijapurkar, U.5
Wallin, J.6
Johnson, L.7
Singh, M.8
Patel, S.9
-
85
-
-
52449106253
-
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin- 1-ylmethyl)-4-morpholin-4-ylthieno[3, 2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer
-
Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS et al: The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl) -4-morpholin-4-ylthieno[3, 2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. J Med Chem (2008)51(18):5522-5532.
-
(2008)
J. Med. Chem.
, vol.51
, Issue.18
, pp. 5522-5532
-
-
Folkes, A.J.1
Ahmadi, K.2
Alderton, W.K.3
Alix, S.4
Baker, S.J.5
Box, G.6
Chuckowree, I.S.7
Clarke, P.A.8
Depledge, P.9
Eccles, S.A.10
Friedman, L.S.11
-
86
-
-
77249137785
-
Discovery of (thienopyrimidin-2-yl) aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer
-
Sutherlin DP, Sampath D, Berry M, Castanedo G, Chang Z, Chuckowree I, Dotson J, Folkes A, Friedman L, Goldsmith R, Heffron T et al: Discovery of (thienopyrimidin-2-yl) aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem (2010)53(3):1086-1097.
-
(2010)
J. Med. Chem.
, vol.53
, Issue.3
, pp. 1086-1097
-
-
Sutherlin, D.P.1
Sampath, D.2
Berry, M.3
Castanedo, G.4
Chang, Z.5
Chuckowree, I.6
Dotson, J.7
Folkes, A.8
Friedman, L.9
Goldsmith, R.10
Heffron, T.11
-
88
-
-
72049122106
-
Discovery of 2-arylthieno[3, 2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K
-
Verheijen JC, Yu K, Toral-Barza I, Hollander I, Zask A: Discovery of 2-arylthieno[3, 2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K. Bioorg Med Chem Lett (2010)20(1):375-379.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.1
, pp. 375-379
-
-
Verheijen, J.C.1
Yu, K.2
Toral-Barza, I.3
Hollander, I.4
Zask, A.5
-
89
-
-
84924238987
-
-
Wyeth,WO-2009143313
-
Wyeth (Venkatesan AM, Chen Z, Dehnhardt CM, Dos Santos O, Delos Santos EG, Zask A, Verheijen JC, Kaplan JA, Richard DJ, Ayral-Kaloustian S, Mansour TS et al Triazine compounds as PI3 kinase and mTOR inhibitors. WO-2009143313 (2009).
-
(2009)
Triazine Compounds as PI3 Kinase and MTOR Inhibitors
-
-
Venkatesan, A.M.1
Chen, Z.2
Dehnhardt, C.M.3
Santos, O.D.4
Santos, E.G.D.5
Zask, A.6
Verheijen, J.C.7
Kaplan, J.A.8
Richard, D.J.9
Ayral-Kaloustian, S.10
Mansour, T.S.11
-
90
-
-
84924238987
-
-
Wyeth,WO-2009143317
-
Wyeth (Venkatesan AM, Chen Z, Dehnhardt CM, Dos Santos O, Delos Santos EG, Zask A, Verheijen JC, Kaplan JA, Richard DJ, Ayral-Kaloustian S, Mansour TS et al Triazine compounds as PI3 kinase and mTOR inhibitors. WO-2009143317 (2009).
-
(2009)
Triazine Compounds as PI3 Kinase and MTOR Inhibitors
-
-
Venkatesan, A.M.1
Chen, Z.2
Dehnhardt, C.M.3
Santos, O.D.4
Santos, E.G.D.5
Zask, A.6
Verheijen, J.C.7
Kaplan, J.A.8
Richard, D.J.9
Ayral-Kaloustian, S.10
Mansour, T.S.11
-
91
-
-
77949785193
-
Bis (morpholino-1, 3, 5-triazine) derivatives: Potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: Discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor
-
Describes the discovery of the triazine dual mTOR/PI3K inhibitor PKI-587
-
Venkatesan AM, Dehnhardt CM, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L et al: Bis (morpholino-1, 3, 5-triazine) derivatives: Potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: Discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem (2010)53(6):2636-2645. • Describes the discovery of the triazine dual mTOR/PI3K inhibitor PKI-587.
-
(2010)
J Med. Chem.
, vol.53
, Issue.6
, pp. 2636-2645
-
-
Venkatesan, A.M.1
Dehnhardt, C.M.2
Santos, E.D.3
Chen, Z.4
Santos, O.D.5
Ayral-Kaloustian, S.6
Khafizova, G.7
Brooijmans, N.8
Mallon, R.9
Hollander, I.10
Feldberg, L.11
-
92
-
-
77950055909
-
Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors
-
Reports the design, synthesis and mTOR inhibitory properties of phenylureidotriazine derivatives bearing two bridged morpholine moieties
-
Zask A, Verheijen JC, Richard DJ, Kaplan J, Curran K, Toral-Barza L, Lucas J, Hollander I, Yu K: Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors. Bioorg Med Chem Lett (2010)20(8):2644-2647. • Reports the design, synthesis and mTOR inhibitory properties of phenylureidotriazine derivatives bearing two bridged morpholine moieties.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.8
, pp. 2644-2647
-
-
Zask, A.1
Verheijen, J.C.2
Richard, D.J.3
Kaplan, J.4
Curran, K.5
Toral-Barza, L.6
Lucas, J.7
Hollander, I.8
Yu, K.9
-
93
-
-
77950031107
-
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl) triazines as highly potent and selective ATP competitive mTOR inhibitors: Optimization of human microsomal stability
-
Verheijen JC, Richard DJ, Curran K, Kaplan J, Yu K, Zask A: 2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl) triazines as highly potent and selective ATP competitive mTOR inhibitors: Optimization of human microsomal stability. Bioorg Med Chem Lett (2010)20(8):2648-2653.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.8
, pp. 2648-2653
-
-
Verheijen, J.C.1
Richard, D.J.2
Curran, K.3
Kaplan, J.4
Yu, K.5
Zask, A.6
-
94
-
-
77950050825
-
Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kα
-
Richard DJ, Verheijen JC, Yu K, Zask A: Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kα. Bioorg Med Chem Lett (2010)20(8):2654-2657.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.8
, pp. 2654-2657
-
-
Richard, D.J.1
Verheijen, J.C.2
Yu, K.3
Zask, A.4
-
95
-
-
70349199015
-
Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR
-
Menear KA, Gomez S, Malagu K, Bailey C, Blackburn K, Cockcroft XL, Ewen S, Fundo A, Le Gall A, Hermann G, Sebastian L et al: Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR. Bioorg Med Chem Lett (2009)19(20):5898-5901.
-
(2009)
Bioorg Med. Chem. Lett.
, vol.19
, Issue.20
, pp. 5898-5901
-
-
Menear, K.A.1
Gomez, S.2
Malagu, K.3
Bailey, C.4
Blackburn, K.5
Cockcroft, X.L.6
Ewen, S.7
Fundo, A.8
Le Gall, A.9
Hermann, G.10
Sebastian, L.11
-
96
-
-
77954633177
-
-
F Hoffman-La Roche Ltd/Genentech Inc Roche Holding AG,WO-2009066084
-
F Hoffman-La Roche Ltd/Genentech Inc [Roche Holding AG] (Chuckowree I, Folkes A, Oxenford S, Olivero A, Sutherlin DP, Zhu B 2-morpholinopyrimidines and their use as PI3 kinaseinhibitors. WO-2009066084 (2009).
-
(2009)
2-morpholinopyrimidines and Their use as PI3 Kinaseinhibitors
-
-
Chuckowree, I.1
Folkes, A.2
Oxenford, S.3
Olivero, A.4
Sutherlin, D.P.5
Zhu, B.6
-
97
-
-
77954646116
-
-
Piramed Pharma Roche Holding AG/Astellas Pharma Inc/Institute of Cancer Research UK/Ludwig Institute for Cancer Research/Cancer Research Technology Ltd Cancer Research UK,WO-2007042806
-
Piramed Pharma [Roche Holding AG]/Astellas Pharma Inc/Institute of Cancer Research UK/Ludwig Institute for Cancer Research/Cancer Research Technology Ltd [Cancer Research UK] (McDonald E, Large JM, Folkes A, Shuttleworth SJ, Wan NC Pyrimidine derivatives for the treatment of cancer. WO-2007042806 (2007).
-
(2007)
Pyrimidine Derivatives for the Treatment of Cancer
-
-
McDonald, E.1
Large, J.M.2
Folkes, A.3
Shuttleworth, S.J.4
Wan, N.C.5
-
98
-
-
77954646116
-
-
Piramed Ltd/Astellas Pharma Inc/Institute of Cancer Research UK/Ludwig Institute for Cancer Research/Cancer Research Technology Ltd,WO-2007042810
-
Piramed Ltd/Astellas Pharma Inc/Institute of Cancer Research UK/Ludwig Institute for Cancer Research/Cancer Research Technology Ltd (McDonald E, Large JM, Folkes A, Shuttleworth SJ Pyrimidine derivatives for the treatment of cancer. WO-2007042810 (2007).
-
(2007)
Pyrimidine Derivatives for the Treatment of Cancer
-
-
McDonald, E.1
Large, J.M.2
Folkes, A.3
Shuttleworth, S.J.4
-
99
-
-
77954626646
-
-
Piramed Pharma Roche Holding AG/Institute of Cancer Research UK,WO-2008125839
-
Piramed Pharma [Roche Holding AG]/Institute of Cancer Research UK (Goldsmith PJ, Hancox TC, Pegg NA, Shuttleworth SJ, Dechaux EA, Price S, Large JM, McDonald E Pharmaceutical compounds. WO-2008125839 (2008).
-
(2008)
Pharmaceutical Compounds
-
-
Goldsmith, P.J.1
Hancox, T.C.2
Pegg, N.A.3
Shuttleworth, S.J.4
Dechaux, E.A.5
Price, S.6
Large, J.M.7
McDonald, E.8
-
100
-
-
77954634171
-
-
Piramed Pharma Roche Holding AG/Institute of Cancer Research UK,WO-2008125835
-
Piramed Pharma [Roche Holding AG]/Institute of Cancer Research UK (Goldsmith PJ, Hancox TC, Pegg NA, Shuttleworth SJ, Large JM, McDonald E 2-Morpholin-4-yl-pyrimidines as PI3K inhibitors. WO-2008125835 (2008).
-
(2008)
2-Morpholin-4-yl-pyrimidines as PI3K Inhibitors
-
-
Goldsmith, P.J.1
Hancox, T.C.2
Pegg, N.A.3
Shuttleworth, S.J.4
Large, J.M.5
McDonald, E.6
-
101
-
-
77954626646
-
-
Piramed Pharma Roche Holding AG/Institute of Cancer Research UK,WO-2008125833
-
Piramed Pharma [Roche Holding AG]/Institute of Cancer Research UK (Baker S, Goldsmith PJ, Hancox TC, Pegg NA, Shuttleworth SJ, Dechaux EA, Krintel SL, Price S, Large JM, McDonald E Pharmaceutical compounds. WO-2008125833 (2008).
-
(2008)
Pharmaceutical Compounds
-
-
Baker, S.1
Goldsmith, P.J.2
Hancox, T.C.3
Pegg, N.A.4
Shuttleworth, S.J.5
Dechaux, E.A.6
Krintel, S.L.7
Price, S.8
Large, J.M.9
McDonald, E.10
-
103
-
-
33750498138
-
-
Chiron Corp Novartis AG,WO-2004048365
-
Chiron Corp [Novartis AG] (Nuss JM, Pecchi S, Renhowe PA 2, 4, 6-Trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer. WO-2004048365 (2004).
-
(2004)
2, 4, 6-Trisubstituted Pyrimidines as Phosphotidylinositol (PI) 3-kinase Inhibitors and Their use in the Treatment of Cancer
-
-
Nuss, J.M.1
Pecchi, S.2
Renhowe, P.A.3
-
104
-
-
77954631541
-
-
*Bio Pte Ltd,WO-2009093981
-
*Bio Pte Ltd (Lee CHA, Nagaraj HKM, William AD, Williams M, Xiong Z Triazine compounds as kinase inhibitors. WO-2009093981 (2009).
-
(2009)
Triazine Compounds as Kinase Inhibitors
-
-
Lee, C.H.A.1
Nagaraj, H.K.M.2
William, A.D.3
Williams, M.4
Xiong, Z.5
-
105
-
-
77954631212
-
-
AstraZeneca UK Ltd/AstraZeneca AB,WO-2009007748
-
AstraZeneca UK Ltd/AstraZeneca AB (Morris JJ, Pike KG Compounds 945. WO-2009007748 (2009).
-
(2009)
Compounds
, vol.945
-
-
Morris, J.J.1
Pike, K.G.2
-
106
-
-
77954655518
-
-
AstraZeneca UK Ltd/AstraZeneca AB,WO-2009007749
-
AstraZeneca UK Ltd/AstraZeneca AB (Finlay MRV Compounds 947. WO-2009007749 (2009).
-
(2009)
Compounds
, vol.947
-
-
Finlay, M.R.V.1
-
108
-
-
77954645027
-
-
AstraZeneca UK Ltd/AstraZeneca AB,WO-2009007751
-
AstraZeneca UK Ltd/AstraZeneca AB (Finlay MRV, Pike KG Compound - 946. WO-2009007751 (2009).
-
(2009)
Compound
, vol.946
-
-
Finlay, M.R.V.1
Pike, K.G.2
-
109
-
-
69249164134
-
Synthesis of 4-(5-benzyl-2-phenylpyrimid-4-yl) morpholines as novel PI3K inhibitors via acetates of Baylis-Hillman adducts and benzamidines
-
Yang C, Yu H, Yang N, Meng L, Xu J, Zhang R, Xie Y, Ding J: Synthesis of 4-(5-benzyl-2-phenylpyrimid-4-yl) morpholines as novel PI3K inhibitors via acetates of Baylis-Hillman adducts and benzamidines. Lett Org Chem (2009)6(2):134-140.
-
(2009)
Lett. Org Chem.
, vol.6
, Issue.2
, pp. 134-140
-
-
Yang, C.1
Yu, H.2
Yang, N.3
Meng, L.4
Xu, J.5
Zhang, R.6
Xie, Y.7
Ding, J.8
-
110
-
-
84924243808
-
-
Novartis AG,WO-2007084786
-
Novartis AG (Pick T, Barsanti P, Iwanowicz E, Fantl W, Hendryckson T, Knapp M, Meritt H, Voliva C, Weismann M, Xin X, Burger M et al Pyrimidine derivatives used as PI-3 kinase inhibitors. WO-2007084786 (2007).
-
(2007)
Pyrimidine Derivatives Used as PI-3 Kinase Inhibitors
-
-
Pick, T.1
Barsanti, P.2
Iwanowicz, E.3
Fantl, W.4
Hendryckson, T.5
Knapp, M.6
Meritt, H.7
Voliva, C.8
Weismann, M.9
Xin, X.10
Burger, M.11
-
111
-
-
84924275094
-
-
Novartis Vaccines & Diagnostics,WO-2008098058
-
Novartis Vaccines & Diagnostics (Pecchi S, Ni Z, Burger M, Wagman A, Atallah G, Bartulis S, Ng S, Pfister KB, Smith A, Zhang Y, Merritt H et al PI3-kinase inhibitors and methods of their use. WO-2008098058 (2008).
-
(2008)
PI3-kinase Inhibitors and Methods of Their use
-
-
Pecchi, S.1
Ni, Z.2
Burger, M.3
Wagman, A.4
Atallah, G.5
Bartulis, S.6
Ng, S.7
Pfister, K.B.8
Smith, A.9
Zhang, Y.10
Merritt, H.11
-
112
-
-
84930157798
-
-
Wyeth Pfizer Inc,WO-2009155042
-
Wyeth [Pfizer Inc] (Bursavich MG, Zhang N, Ayral-Kaloustian S, Anderson JT, Nguyen TH, Lombardi S, Malwitz D, Brooijmans N, Cole DC, Gilbert AM, Nowak PW, Park K et al 3-Substituted-1H-indole compounds, their use as mTOR kinase and PI3 kinase inhibitors, and their syntheses. WO-2009155042 (2009).
-
(2009)
3-Substituted-1H-indole Compounds, Their use as MTOR Kinase and PI3 Kinase Inhibitors, and Their Syntheses
-
-
Bursavich, M.G.1
Zhang, N.2
Ayral-Kaloustian, S.3
Anderson, J.T.4
Nguyen, T.H.5
Lombardi, S.6
Malwitz, D.7
Brooijmans, N.8
Cole, D.C.9
Gilbert, A.M.10
Nowak, P.W.11
Park, K.12
-
113
-
-
77954626176
-
-
Wyeth Pfizer Inc,WO-2009155052
-
Wyeth [Pfizer Inc] (Tsou H, Birnberg GH, MacEwan GJ, Ayral-Kaloustian S, Bursavich MG, Lombardi S, Zhang N, Gilbert AM, Grosu GT, Brooijmans N, Nguyen TH 3-Substituted-1H-pyrrolo[2, 3-b]pyridine and 3-substituted-1H-pyrrolo[3, 2-b] pyridine compounds, their use as mTOR kinase and PI3 kinase inhibitors, and their synthesis. WO-2009155052 (2009).
-
(2009)
3-Substituted-1H-Pyrrolo[2, 3-b]pyridine and 3-substituted-1H-pyrrolo[3, 2-b] Pyridine Compounds, Their use as MTOR Kinase and PI3 Kinase Inhibitors, and Their Synthesis
-
-
Tsou, H.1
Birnberg, G.H.2
MacEwan, G.J.3
Ayral-Kaloustian, S.4
Bursavich, M.G.5
Lombardi, S.6
Zhang, N.7
Gilbert, A.M.8
Grosu, G.T.9
Brooijmans, N.10
Nguyen, T.H.11
-
114
-
-
77950169471
-
Novel benzofuran-3-one indole inhibitors of PI3 kinase-α and the mammalian target of rapamycin: Hit to lead studies
-
Bursavich MG, Brooijmans N, Feldberg L, Hollander I, Kim S, Lombardi S, Park K, Mallon R, Gilbert AM: Novel benzofuran-3-one indole inhibitors of PI3 kinase-α and the mammalian target of rapamycin: Hit to lead studies. Bioorg Med Chem Lett (2010)20(8):2586-2590.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.8
, pp. 2586-2590
-
-
Bursavich, M.G.1
Brooijmans, N.2
Feldberg, L.3
Hollander, I.4
Kim, S.5
Lombardi, S.6
Park, K.7
Mallon, R.8
Gilbert, A.M.9
-
115
-
-
77949492415
-
Discovery and optimization of 2-(4-substituted-pyrrolo[2, 3-b]pyridin-3-yl) methylene-4-hydroxybenzofuran-3 (2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
-
Tsou HR, MacEwan G, Birnberg G, Grosu G, Bursavich MG, Bard J, Brooijmans N, Toral-Barza L, Hollander I, Mansour TS, Ayral-Kaloustian S et al: Discovery and optimization of 2-(4-substituted-pyrrolo[2, 3-b]pyridin-3-yl) methylene-4-hydroxybenzofuran-3 (2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Bioorg Med Chem Lett (2010)20(7):2321-2325.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.7
, pp. 2321-2325
-
-
Tsou, H.R.1
MacEwan, G.2
Birnberg, G.3
Grosu, G.4
Bursavich, M.G.5
Bard, J.6
Brooijmans, N.7
Toral-Barza, L.8
Hollander, I.9
Mansour, T.S.10
Ayral-Kaloustian, S.11
-
116
-
-
77949489853
-
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)
-
Tsou HR, MacEwan G, Birnberg G, Zhang N, Brooijmans N, Toral-Barza L, Hollander I, Ayral-Kaloustian S, Yu K: 4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR). Bioorg Med Chem Lett (2010)20(7):2259-2263.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.7
, pp. 2259-2263
-
-
Tsou, H.R.1
MacEwan, G.2
Birnberg, G.3
Zhang, N.4
Brooijmans, N.5
Toral-Barza, L.6
Hollander, I.7
Ayral-Kaloustian, S.8
Yu, K.9
-
117
-
-
77954213226
-
5-Ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-α and mTOR for the treatment of breast cancer
-
Zhang N, Ayral-Kaloustian S, Anderson JT, Nguyen T, Das S, Venkatesan AM, Brooijmans N, Lucas J, Yu K, Hollander I, Mallon R: 5-Ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-α and mTOR for the treatment of breast cancer. Bioorg Med Chem Lett (2010)20(12):3526-3529.
-
(2010)
Bioorg Med. Chem. Lett.
, vol.20
, Issue.12
, pp. 3526-3529
-
-
Zhang, N.1
Ayral-Kaloustian, S.2
Anderson, J.T.3
Nguyen, T.4
Das, S.5
Venkatesan, A.M.6
Brooijmans, N.7
Lucas, J.8
Yu, K.9
Hollander, I.10
Mallon, R.11
-
118
-
-
77954626329
-
-
Piramal Life Sciences Ltd,WO-2009019656
-
Piramal Life Sciences Ltd (Kumar S, Josh KS, Deore V, Bhonde MR, Yewalkar NN, Padgaonkar AA, Rathos MG, Kulkarni-Almeida AA, Parikh S, Dagia NM Pyridyl derivatives, their preparation and use. WO-2009019656 (2009).
-
(2009)
Pyridyl Derivatives, Their Preparation and use
-
-
Kumar, S.1
Josh, K.S.2
Deore, V.3
Bhonde, M.R.4
Yewalkar, N.N.5
Padgaonkar, A.A.6
Rathos, M.G.7
Kulkarni-Almeida, A.A.8
Parikh, S.9
Dagia, N.M.10
-
119
-
-
65549160091
-
Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors
-
Deore V, Yewalkar N, Bhatia D, Desai N, Gupte RD, Dadarkar SS, Jadhav MG, Tannu AA, Bhatt P, Nemmani KV, Vishwakarma RA et al: Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors. Bioorg Med Chem Lett (2009)19(11):2949-2952.
-
(2009)
Bioorg Med. Chem. Lett.
, vol.19
, Issue.11
, pp. 2949-2952
-
-
Deore, V.1
Yewalkar, N.2
Bhatia, D.3
Desai, N.4
Gupte, R.D.5
Dadarkar, S.S.6
Jadhav, M.G.7
Tannu, A.A.8
Bhatt, P.9
Nemmani, K.V.10
Vishwakarma, R.A.11
-
120
-
-
57349119998
-
A novel mTOR inhibitor is efficacious in a murine model of colitis
-
Bhonde MR, Gupte RD, Dadarkar SD, Jadhav MG, Tannu AA, Bhatt P, Bhatia DR, Desai NK, Deore V, Yewalkar N, Vishwakarma RA et al: A novel mTOR inhibitor is efficacious in a murine model of colitis. Am J Physiol Gastrointest Liver Physiol (2008)295(6):G1237-G1245.
-
(2008)
Am. J. Physiol. Gastrointest Liver Physiol.
, vol.295
, Issue.6
-
-
Bhonde, M.R.1
Gupte, R.D.2
Dadarkar, S.D.3
Jadhav, M.G.4
Tannu, A.A.5
Bhatt, P.6
Bhatia, D.R.7
Desai, N.K.8
Deore, V.9
Yewalkar, N.10
Vishwakarma, R.A.11
-
121
-
-
79959987654
-
XL388: A novel, selective, orally bioavailable mTORC1 and mTORC2 inhibitor that demonstrates pharmacodynamic antitumor activity in multiple human cancer xenograft models
-
Boston, MA, USA, Abs
-
Miller N: XL388: A novel, selective, orally bioavailable mTORC1 and mTORC2 inhibitor that demonstrates pharmacodynamic antitumor activity in multiple human cancer xenograft models. AACR/NCI/EORTC International Conference on Molecular Targets and Cancer Therapeutics: Discovery, Biology, and Clinical Applications, Boston, MA, USA (2009): Abs B146.
-
(2009)
AACR/NCI/EORTC International Conference on Molecular Targets and Cancer Therapeutics: Discovery, Biology, and Clinical Applications
-
-
Miller, N.1
-
122
-
-
77954629282
-
-
Amgen Inc,WO-2009155121
-
Amgen Inc (Bo YY, Booker S, Bryan M, Deak HL, Liu L, Andrews K, Nishimura N, Norman MH, Panter K, Schenkel L, Siegmund AC et al Inhibitors of PI3 kinase. WO-2009155121 (2009).
-
(2009)
Inhibitors of PI3 Kinase
-
-
Bo, Y.Y.1
Booker, S.2
Bryan, M.3
Deak, H.L.4
Liu, L.5
Andrews, K.6
Nishimura, N.7
Norman, M.H.8
Panter, K.9
Schenkel, L.10
Siegmund, A.C.11
-
123
-
-
85006834271
-
AEZS-126, a new orally bioavailable PI3K inhibitor with antitumor effects
-
Abs
-
Seipelt I, Baasner S, Gerlac M, Teifel M, Fensterle J, Blumenstein L, Mueller G, Guenther E: AEZS-126, a new orally bioavailable PI3K inhibitor with antitumor effects. American Association for Cancer Research Annual Meeting, Denver, CO, USA (2009) 100: Abs 3705.
-
(2009)
American Association for Cancer Research Annual Meeting, Denver, CO, USA
, vol.100
, pp. 3705
-
-
Seipelt, I.1
Baasner, S.2
Gerlac, M.3
Teifel, M.4
Fensterle, J.5
Blumenstein, L.6
Mueller, G.7
Guenther, E.8
-
124
-
-
44649152229
-
Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway
-
Lohar MV, Mundada R, Bhonde M, Padgaonkar A, Deore V, Yewalkar N, Bhatia D, Rathos M, Joshi K, Vishwakarma RA, Kumar S: Design and synthesis of novel furoquinoline based inhibitors of multiple targets in the PI3K/Akt-mTOR pathway. Bioorg Med Chem Lett (2008)18(12):3603-3606.
-
(2008)
Bioorg Med. Chem. Lett.
, vol.18
, Issue.12
, pp. 3603-3606
-
-
Lohar, M.V.1
Mundada, R.2
Bhonde, M.3
Padgaonkar, A.4
Deore, V.5
Yewalkar, N.6
Bhatia, D.7
Rathos, M.8
Joshi, K.9
Vishwakarma, R.A.10
Kumar, S.11
-
126
-
-
77954630112
-
-
Semafore Pharmaceuticals Inc, WO-2009094560
-
Semafore Pharmaceuticals Inc (Morales GA, Weber KT, Newblom JM, Peng X, Su J, Garlich GR): Thienopyranones as kinase inhibitors. WO-2009094560 (2009).
-
(2009)
Thienopyranones as Kinase Inhibitors
-
-
Morales, G.A.1
Weber, K.T.2
Newblom, J.M.3
Peng, X.4
Su, J.5
Garlich, G.R.6
-
127
-
-
77954638677
-
Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin
-
Knight SD, Adams ND, Burgess JL, Chaudhari AM, Darcy MG, Donatelli CA, Luengo JI, Newlander KA, Parrish CA, Ridgers LH, Sarpong MA et al: Discovery of GSK2126458, a highly potent inhibitor of PI3K and the mammalian target of rapamycin. ACS Med Chem Lett (2010)1(1):39-43.
-
(2010)
ACS Med. Chem. Lett.
, vol.1
, Issue.1
, pp. 39-43
-
-
Knight, S.D.1
Adams, N.D.2
Burgess, J.L.3
Chaudhari, A.M.4
Darcy, M.G.5
Donatelli, C.A.6
Luengo, J.I.7
Newlander, K.A.8
Parrish, C.A.9
Ridgers, L.H.10
Sarpong, M.A.11
-
128
-
-
70350176755
-
A phase I dose-escalation study of the safety, pharmacokinetics (PK) and pharmacodynamics of XL765, a PI3K/TORC1/TORC2 inhibitor administered orally to patients with advanced solid tumors
-
Abs
-
LoRusso P, Markman B, Tabernero J, Shazer R, Nguyen L, Heath E, Patnaik A, Papadopoulos K: A phase I dose-escalation study of the safety, pharmacokinetics (PK) and pharmacodynamics of XL765, a PI3K/TORC1/TORC2 inhibitor administered orally to patients with advanced solid tumors. J Clin Oncol (2009)27(15S):Abs 3502.
-
(2009)
J. Clin. Oncol.
, vol.27
, Issue.15
, pp. 3502
-
-
LoRusso, P.1
Markman, B.2
Tabernero, J.3
Shazer, R.4
Nguyen, L.5
Heath, E.6
Patnaik, A.7
Papadopoulos, K.8
-
129
-
-
56449087509
-
Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability
-
Xue Q, Hopkins B, Perruzzi C, Udayakumar D, Sherris D, Benjamin LE: Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability. Cancer Res (2008)68(22):9551-9557.
-
(2008)
Cancer Res.
, vol.68
, Issue.22
, pp. 9551-9557
-
-
Xue, Q.1
Hopkins, B.2
Perruzzi, C.3
Udayakumar, D.4
Sherris, D.5
Benjamin, L.E.6
-
130
-
-
68549087108
-
NV-128, a novel isoflavone derivative, induces caspase-independent cell death through the Akt/mammalian target of rapamycin pathway
-
Alvero AB, Montagna MK, Chen R, Kim KH, Kyungjin K, Visintin I, Fu HH, Brown D, Mor G: NV-128, a novel isoflavone derivative, induces
-
(2009)
Cancer
, vol.115
, Issue.14
, pp. 3204-3216
-
-
Alvero, A.B.1
Montagna, M.K.2
Chen, R.3
Kim, K.H.4
Kyungjin, K.5
Visintin, I.6
Fu, H.H.7
Brown, D.8
Mor, G.9
-
131
-
-
67651171652
-
Honokiol-mediated inhibition of PI3K/mTOR pathway: A potential strategy to overcome immunoresistance in glioma, breast, and prostate carcinoma without impacting T cell function
-
Crane C, Panner A, Pieper RO, Arbiser J, Parsa AT: Honokiol-mediated inhibition of PI3K/mTOR pathway: A potential strategy to overcome immunoresistance in glioma, breast, and prostate carcinoma without impacting T cell function. J Immunother (2009)32(6):585-592.
-
(2009)
J. Immunother.
, vol.32
, Issue.6
, pp. 585-592
-
-
Crane, C.1
Panner, A.2
Pieper, R.O.3
Arbiser, J.4
Parsa, A.T.5
-
132
-
-
70349616273
-
Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling
-
Balgi AD, Fonseca BD, Donohue E, Tsang TC, Lajoie P, Proud CG, Nabi IR, Roberge M: Screen for chemical modulators of autophagy reveals novel therapeutic inhibitors of mTORC1 signaling. PLos One (2009)4(9):e7124.
-
(2009)
PLos One
, vol.4
, Issue.9
-
-
Balgi, A.D.1
Fonseca, B.D.2
Donohue, E.3
Tsang, T.C.4
Lajoie, P.5
Proud, C.G.6
Nabi, I.R.7
Roberge, M.8
|