-
1
-
-
0021363316
-
-
J.R.S. Arch, A.T. Ainsworth, M.A. Cawthorne, C. Wilson, and S. Wilson Nature 309 1984 163
-
(1984)
Nature
, vol.309
, pp. 163
-
-
Arch, J.R.S.1
Ainsworth, A.T.2
Cawthorne, M.A.3
Wilson, C.4
Wilson, S.5
-
4
-
-
0024470363
-
-
L.J. Emorine, S. Marullo, M.-M. Briend-Sutren, G. Patey, K. Tate, C. Delavier-Klutchko, and A.D. Strosberg Science 245 1989 1118
-
(1989)
Science
, vol.245
, pp. 1118
-
-
Emorine, L.J.1
Marullo, S.2
Briend-Sutren, M.-M.3
Patey, G.4
Tate, K.5
Delavier-Klutchko, C.6
Strosberg, A.D.7
-
8
-
-
0344490248
-
-
S. Rathi, S. Kazerounian, K. Banwait, S. Schulz, S.A. Waldman, and S.J. Ratten J. Pharmacol. Exp. Ther. 305 2003 615
-
(2003)
J. Pharmacol. Exp. Ther.
, vol.305
, pp. 615
-
-
Rathi, S.1
Kazerounian, S.2
Banwait, K.3
Schulz, S.4
Waldman, S.A.5
Ratten, S.J.6
-
9
-
-
0032588710
-
-
M. Takeda, K. Obara, T. Mizusawa, Y. Tomita, K. Aria, T. Tsutsui, A. Hatano, K. Takahashi, and S. Nomura J. Pharmacol. Exp. Ther. 288 1999 1367
-
(1999)
J. Pharmacol. Exp. Ther.
, vol.288
, pp. 1367
-
-
Takeda, M.1
Obara, K.2
Mizusawa, T.3
Tomita, Y.4
Aria, K.5
Tsutsui, T.6
Hatano, A.7
Takahashi, K.8
Nomura, S.9
-
12
-
-
84930538142
-
-
P. Tyagi, V. Tyagi, N. Yoshimura, M. Chancellor, and O. Yamaguchi Drugs Future 34 2009 635
-
(2009)
Drugs Future
, vol.34
, pp. 635
-
-
Tyagi, P.1
Tyagi, V.2
Yoshimura, N.3
Chancellor, M.4
Yamaguchi, O.5
-
13
-
-
34547900257
-
-
J.A. Lafontaine, R.F. Day, J. Dibrino, J.R. Hadcock, D.M. Hargrove, M. Linhares, K.A. Martin, T.S. Maurer, N.A. Nardone, D.A. Tess, and P. DaSilva-Jardin Bioorg. Med. Chem. Lett. 17 2007 5245
-
(2007)
Bioorg. Med. Chem. Lett.
, vol.17
, pp. 5245
-
-
Lafontaine, J.A.1
Day, R.F.2
Dibrino, J.3
Hadcock, J.R.4
Hargrove, D.M.5
Linhares, M.6
Martin, K.A.7
Maurer, T.S.8
Nardone, N.A.9
Tess, D.A.10
Dasilva-Jardin, P.11
-
14
-
-
34548840602
-
-
A. Hicks, G.P. McCafferty, E. Riedel, N. Aiyar, M. Pullen, C. Evans, T.D. Luce, R.W. Coatney, G.C. Rivera, T.D. Westfall, and J.P. Hieble J. Pharmacol. Exp. Ther. 323 2007 202
-
(2007)
J. Pharmacol. Exp. Ther.
, vol.323
, pp. 202
-
-
Hicks, A.1
McCafferty, G.P.2
Riedel, E.3
Aiyar, N.4
Pullen, M.5
Evans, C.6
Luce, T.D.7
Coatney, R.W.8
Rivera, G.C.9
Westfall, T.D.10
Hieble, J.P.11
-
15
-
-
79952361655
-
-
U.S. Patent 6,346,532 2002
-
Maruyama, T.; Suzuki, T.; Onda, K.; Hayakawa, M.; Moritomo, H.; Kimizuka, T.; Matsui, T. U.S. Patent 6,346,532, 2002; Chem. Abstr. 1998, 129, 19801.
-
(1998)
Chem. Abstr.
, vol.129
, pp. 19801
-
-
Maruyama, T.1
Suzuki, T.2
Onda, K.3
Hayakawa, M.4
Moritomo, H.5
Kimizuka, T.6
Matsui, T.7
-
16
-
-
0036783754
-
-
T.M. Larsen, S. Toubro, M.A. van Baak, K.M. Gottesdiener, P. Larson, and W.H.M. Saris Am. J. Clin. Nutr. 76 2002 780
-
(2002)
Am. J. Clin. Nutr.
, vol.76
, pp. 780
-
-
Larsen, T.M.1
Toubro, S.2
Van Baak, M.A.3
Gottesdiener, K.M.4
Larson, P.5
Saris, W.H.M.6
-
17
-
-
0034687253
-
-
R.J. Mathvink, S.J. Tolman, D. Chitty, M.R. Candelore, M.A. Cascieri, L.F. Colwell, L. Deng, W.P. Feeney, M.J. Forrest, G.J. Hom, E.D. MacIntyre, R.R. Miller, R.A. Stearns, L. Tota, M.J. Wyvratt, M.H. Fisher, and A.E. Weber J. Med. Chem. 43 2000 3832
-
(2000)
J. Med. Chem.
, vol.43
, pp. 3832
-
-
Mathvink, R.J.1
Tolman, S.J.2
Chitty, D.3
Candelore, M.R.4
Cascieri, M.A.5
Colwell, L.F.6
Deng, L.7
Feeney, W.P.8
Forrest, M.J.9
Hom, G.J.10
MacIntyre, E.D.11
Miller, R.R.12
Stearns, R.A.13
Tota, L.14
Wyvratt, M.J.15
Fisher, M.H.16
Weber, A.E.17
-
18
-
-
0026675653
-
-
J.D. Bloom, M.D. Dutia, B.D. Johnson, A. Wissner, M.G. Burns, E.E. Largis, J.A. Dolan, and T.H. Claus J. Med. Chem. 35 1992 3081
-
(1992)
J. Med. Chem.
, vol.35
, pp. 3081
-
-
Bloom, J.D.1
Dutia, M.D.2
Johnson, B.D.3
Wissner, A.4
Burns, M.G.5
Largis, E.E.6
Dolan, J.A.7
Claus, T.H.8
-
19
-
-
0035656144
-
-
N. Tanaka, T. Tamai, H. Mukaiyama, A. Hirabayashi, H. Muranaka, T. Ishikawa, S. Akahane, and M. Akahane Bioorg. Med. Chem. 9 2001 3265
-
(2001)
Bioorg. Med. Chem.
, vol.9
, pp. 3265
-
-
Tanaka, N.1
Tamai, T.2
Mukaiyama, H.3
Hirabayashi, A.4
Muranaka, H.5
Ishikawa, T.6
Akahane, S.7
Akahane, M.8
-
20
-
-
0034605254
-
-
R.J. Mathvink, S.J. Tolman, D. Chitty, M.R. Candelore, M.A. Cascieri, L.F. Colwell, L. Deng, W.P. Feeney, M.J. Forrest, G.J. Hom, E.D. MacIntyre, L. Tota, M.J. Wyvratt, M.H. Fisher, and A.E. Weber Bioorg. Med. Chem. Lett. 10 2000 1971
-
(2000)
Bioorg. Med. Chem. Lett.
, vol.10
, pp. 1971
-
-
Mathvink, R.J.1
Tolman, S.J.2
Chitty, D.3
Candelore, M.R.4
Cascieri, M.A.5
Colwell, L.F.6
Deng, L.7
Feeney, W.P.8
Forrest, M.J.9
Hom, G.J.10
MacIntyre, E.D.11
Tota, L.12
Wyvratt, M.J.13
Fisher, M.H.14
Weber, A.E.15
-
21
-
-
0035987890
-
-
R.A. Stearns, R.R. Miller, W. Tang, G.Y. Kwei, F.S. Tang, R.J. Mathvink, E.M. Naylor, D. Chitty, V.J. Colandrea, A.E. Weber, A.E. Colletti, J.R. Struss, C.A. Keohane, W.P. Feeney, S.A. Iliff, and S.-H.L. Chiu Drug Metab. Dispos. 30 2002 771
-
(2002)
Drug Metab. Dispos.
, vol.30
, pp. 771
-
-
Stearns, R.A.1
Miller, R.R.2
Tang, W.3
Kwei, G.Y.4
Tang, F.S.5
Mathvink, R.J.6
Naylor, E.M.7
Chitty, D.8
Colandrea, V.J.9
Weber, A.E.10
Colletti, A.E.11
Struss, J.R.12
Keohane, C.A.13
Feeney, W.P.14
Iliff, S.A.15
Chiu, S.-H.L.16
-
22
-
-
0035987888
-
-
W. Tang, R.A. Stearns, R.R. Miller, J.S. Ngui, R.J. Mathvink, A.E. Weber, G.Y. Kwei, J.R. Strauss, C.A. Keohane, G.A. Doss, S.-H.L. Chiu, and T. Baillie Drug Metab. Depos. 30 2002 778
-
(2002)
Drug Metab. Depos.
, vol.30
, pp. 778
-
-
Tang, W.1
Stearns, R.A.2
Miller, R.R.3
Ngui, J.S.4
Mathvink, R.J.5
Weber, A.E.6
Kwei, G.Y.7
Strauss, J.R.8
Keohane, C.A.9
Doss, G.A.10
Chiu, S.-H.L.11
Baillie, T.12
-
23
-
-
79952360328
-
-
For the purpose of easier synthetic manipulation, the phenyl analog of L-796,568 was chosen for comparison since it has similar in vitro potency and metabolic properties as L-796,568
-
For the purpose of easier synthetic manipulation, the phenyl analog of L-796,568 was chosen for comparison since it has similar in vitro potency and metabolic properties as L-796,568.
-
-
-
-
28
-
-
79952364497
-
-
Zhan Catalyst I is available from Zannan Pharma LTD, catalog number RC-301. Patents CN1907992A, US 2007/0043180 A1, PCT WO 2007/003135 A1
-
Zhan Catalyst I is available from Zannan Pharma LTD, catalog number RC-301. Patents CN1907992A, US 2007/0043180 A1, PCT WO 2007/003135 A1.
-
-
-
-
29
-
-
79952364083
-
-
10
-
10
-
-
-
-
30
-
-
79952360625
-
-
The major isomer eluted first at retention time of 4.11 min, while the second isomer eluted at 4.56 min.
-
The major isomer eluted first at retention time of 4.11 min, while the second isomer eluted at 4.56 min.
-
-
-
-
31
-
-
79952361334
-
-
The stereochemistry of the two pyrrolidine chiral centers was determined to be cis based on 2D NOE NMR data (see Supplementary data)
-
The stereochemistry of the two pyrrolidine chiral centers was determined to be cis based on 2D NOE NMR data (see Supplementary data).
-
-
-
-
32
-
-
79952362676
-
-
Selectivity was assessed by SFC analytical analysis and the effort to improve selectivity was studied via trial and error of changes in the reaction conditions. Original less selective conditions: Dilution 0.02 M and stoichiometric amount (by weight) of the catalyst (resulted in 3:1 mixture of cis/trans)
-
Selectivity was assessed by SFC analytical analysis and the effort to improve selectivity was studied via trial and error of changes in the reaction conditions. Original less selective conditions: Dilution 0.02 M and stoichiometric amount (by weight) of the catalyst (resulted in 3:1 mixture of cis/trans).
-
-
-
-
33
-
-
77549086075
-
-
S.D. Goble, L. Wang, K.L. Howell, A. Bansal, R. Berger, L. Brocknier, J. DiSalvo, S. Feighner, B. Harber, J. He, A. Hurley, D. Hreniuk, E. Parmee, M. Robbins, G. Salituro, A. Sanfiz, E. Streckfuss, E. Watkins, A. Weber, M. Struthers, and S.D. Edmondson Bioorg. Med. Chem. Lett. 20 2010 1895
-
(2010)
Bioorg. Med. Chem. Lett.
, vol.20
, pp. 1895
-
-
Goble, S.D.1
Wang, L.2
Howell, K.L.3
Bansal, A.4
Berger, R.5
Brocknier, L.6
Disalvo, J.7
Feighner, S.8
Harber, B.9
He, J.10
Hurley, A.11
Hreniuk, D.12
Parmee, E.13
Robbins, M.14
Salituro, G.15
Sanfiz, A.16
Streckfuss, E.17
Watkins, E.18
Weber, A.19
Struthers, M.20
Edmondson, S.D.21
more..
-
34
-
-
4043083603
-
-
J.P. Felix, B.S. Williams, B.T. Priest, R.M. Brochu, I.E. Dick, V.A. Warren, L. Yan, R.S. Slaughter, G.J. Kaczorowski, M.M. Smith, and M. Garcia Assay Drug Dev. Technol. 2 2004 260
-
(2004)
Assay Drug Dev. Technol.
, vol.2
, pp. 260
-
-
Felix, J.P.1
Williams, B.S.2
Priest, B.T.3
Brochu, R.M.4
Dick, I.E.5
Warren, V.A.6
Yan, L.7
Slaughter, R.S.8
Kaczorowski, G.J.9
Smith, M.M.10
Garcia, M.11
-
35
-
-
0030048695
-
-
J.E. Ridings, M.D. Barratt, R. Cary, C.G. Earnshaw, C.E. Eggington, M.K. Ellis, P.N. Judson, J.J. Langowski, C.A. Marchant, M.P. Payne, W.P. Watson, and T.D. Yih Toxicology 106 1996 267
-
(1996)
Toxicology
, vol.106
, pp. 267
-
-
Ridings, J.E.1
Barratt, M.D.2
Cary, R.3
Earnshaw, C.G.4
Eggington, C.E.5
Ellis, M.K.6
Judson, P.N.7
Langowski, J.J.8
Marchant, C.A.9
Payne, M.P.10
Watson, W.P.11
Yih, T.D.12
-
36
-
-
0036319482
-
-
N.F. Cariello, J.D. Wilson, B.H. Britt, D.J. Wedd, B. Burlinson, and V. Gombar Mutagenesis 17 2002 321
-
(2002)
Mutagenesis
, vol.17
, pp. 321
-
-
Cariello, N.F.1
Wilson, J.D.2
Britt, B.H.3
Wedd, D.J.4
Burlinson, B.5
Gombar, V.6
|