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Karasik, A.1
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Davies, M.J.4
Stein, P.P.5
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4
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61349143225
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For lead DPP-4 references, see:
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For lead DPP-4 references, see:. Havale S.H., and Pal M. Bioorg. Med. Chem. 17 (2009) 1783
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Havale, S.H.1
Pal, M.2
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11
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0141461415
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During M.J., Cao L., Zuzga D.S., Francis J.S., Fitzsimons H.L., Jiao X., Bland R.J., Klugmann M., Banks W.A., Drucker D.J., and Haile C.N. Nat. Med. 9 (2003) 1173
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During, M.J.1
Cao, L.2
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Francis, J.S.4
Fitzsimons, H.L.5
Jiao, X.6
Bland, R.J.7
Klugmann, M.8
Banks, W.A.9
Drucker, D.J.10
Haile, C.N.11
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12
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34249280590
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Biftu T., Scapin G., Singh S., Feng D., Becker J.W., Eiermann G., He H., Lyons K., Patel S., Petrov A., Sinha-Roy R., Zhang B., Wu J., Zhang X., Doss G.A., Thornberry N.A., and Weber A.E. Bioorg. Med. Chem. Lett. 17 (2007) 3384
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Bioorg. Med. Chem. Lett.
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Biftu, T.1
Scapin, G.2
Singh, S.3
Feng, D.4
Becker, J.W.5
Eiermann, G.6
He, H.7
Lyons, K.8
Patel, S.9
Petrov, A.10
Sinha-Roy, R.11
Zhang, B.12
Wu, J.13
Zhang, X.14
Doss, G.A.15
Thornberry, N.A.16
Weber, A.E.17
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13
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34250346390
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Gao Y.-D., Feng D., Sheridan R.P., Scapin G., Patel S.B., Wu J.K., Shang J., Sinha-Roy R., Thornberry N.A., Weber A.E., and Biftu T. Bioorg. Med. Chem. Lett. 17 (2007) 3877
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Gao, Y.-D.1
Feng, D.2
Sheridan, R.P.3
Scapin, G.4
Patel, S.B.5
Wu, J.K.6
Shang, J.7
Sinha-Roy, R.8
Thornberry, N.A.9
Weber, A.E.10
Biftu, T.11
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14
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34447309570
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Cox J.M., Harper B., Mastracchio A., Leiting B., Sinha Roy R., Patel R.A., Wu J.K., Lyons K.A., He H., Xu S., Zhu B., Thornberry N.A., Weber A.E., and Edmondson S.D. Bioorg. Med. Chem. Lett. 17 (2007) 4579
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Cox, J.M.1
Harper, B.2
Mastracchio, A.3
Leiting, B.4
Sinha Roy, R.5
Patel, R.A.6
Wu, J.K.7
Lyons, K.A.8
He, H.9
Xu, S.10
Zhu, B.11
Thornberry, N.A.12
Weber, A.E.13
Edmondson, S.D.14
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15
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67649948462
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1H NMR and LC-MS. Detailed procedures and spectral data for selected compounds are described in the following patents: Cox, J. M.; Edmondson, S. D.; Mastracchio, A. Fused Aminopiperidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes WO 2006/058064, filed Nov. 22, 2005.
-
1H NMR and LC-MS. Detailed procedures and spectral data for selected compounds are described in the following patents: Cox, J. M.; Edmondson, S. D.; Mastracchio, A. Fused Aminopiperidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes WO 2006/058064, filed Nov. 22, 2005.
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16
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67649951287
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Cox, J. M.; Edmondson, S. D.; Mastracchio, A. Fused Aminopiperidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes WO 2007/024993, filed Aug. 22, 2006; Biftu, T.; Cox, J. M.; Edmondson, S. D.; Mastracchio, A. Fused Aminopiperidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes WO 2007/070434, filed Dec. 8, 2006.
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Cox, J. M.; Edmondson, S. D.; Mastracchio, A. Fused Aminopiperidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes WO 2007/024993, filed Aug. 22, 2006; Biftu, T.; Cox, J. M.; Edmondson, S. D.; Mastracchio, A. Fused Aminopiperidines as Dipeptidyl Peptidase-IV Inhibitors for the Treatment or Prevention of Diabetes WO 2007/070434, filed Dec. 8, 2006.
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18
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0037964447
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50 determinations for DPP-4 and QPP were carried out as described in
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50 determinations for DPP-4 and QPP were carried out as described in. Leiting B., Pryor K.D., Wu J.K., Marsilio F., Patel R.A., Craik C.S., Ellman J.A., Cummings R.T., and Thornberry N.A. Biochem. J. 371 (2003) 525
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Biochem. J.
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Leiting, B.1
Pryor, K.D.2
Wu, J.K.3
Marsilio, F.4
Patel, R.A.5
Craik, C.S.6
Ellman, J.A.7
Cummings, R.T.8
Thornberry, N.A.9
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19
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67649963932
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note
-
50's are an average of n ≥ 4, with standard deviations less than 60% of the average.
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-
-
-
20
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25844459084
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For a discussion of the relevance of selectivity over DPP-8 and DPP-9, see
-
For a discussion of the relevance of selectivity over DPP-8 and DPP-9, see. Lankas G.R., Leiting B., Sinha Roy R., Eiermann G.J., Beconi M.G., Biftu T., Chan C.-C., Edmondson S., Feeney W.P., He H., Ippolito D.E., Kim D., Lyons K.A., Ok H.O., Patel R.A., Petrov A.N., Pryor K.A., Qian X., Reigle L., Woods A., Wu J.K., Zaller D., Zhang X., Zhu L., Weber A.E., and Thornberry N.A. Diabetes 54 (2005) 2988
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(2005)
Diabetes
, vol.54
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Lankas, G.R.1
Leiting, B.2
Sinha Roy, R.3
Eiermann, G.J.4
Beconi, M.G.5
Biftu, T.6
Chan, C.-C.7
Edmondson, S.8
Feeney, W.P.9
He, H.10
Ippolito, D.E.11
Kim, D.12
Lyons, K.A.13
Ok, H.O.14
Patel, R.A.15
Petrov, A.N.16
Pryor, K.A.17
Qian, X.18
Reigle, L.19
Woods, A.20
Wu, J.K.21
Zaller, D.22
Zhang, X.23
Zhu, L.24
Weber, A.E.25
Thornberry, N.A.26
more..
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21
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67649936005
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note
-
The atomic coordinates for the X-ray structures of DPP-4 in complex with 25 and 34 have been deposited into the RCSB protein data bank under RCSB ID codes RCSB052890 and RCSB052891, and under PDB ID codes 3HAB and 3HAC, respectively.
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-
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22
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4544315126
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50 determinations for hERG was carried out as described in
-
50 determinations for hERG was carried out as described in. Friesen R.W., Ducharme Y., Ball R.G., Blouin M., Boulet L., Cote B., Frenette R., Girard M., Guay D., Huang Z., Jones T.R., Laliberte F., Lynch J.J., Mancini J., Martins E., Masson P., Muise E., Pon D.J., Siegel P.K.S., Styhler A., Tsou N.N., Turner M.J., Young R.N., and Girard Y. J. Med. Chem. 46 (2003) 2017
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J. Med. Chem.
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, pp. 2017
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Friesen, R.W.1
Ducharme, Y.2
Ball, R.G.3
Blouin, M.4
Boulet, L.5
Cote, B.6
Frenette, R.7
Girard, M.8
Guay, D.9
Huang, Z.10
Jones, T.R.11
Laliberte, F.12
Lynch, J.J.13
Mancini, J.14
Martins, E.15
Masson, P.16
Muise, E.17
Pon, D.J.18
Siegel, P.K.S.19
Styhler, A.20
Tsou, N.N.21
Turner, M.J.22
Young, R.N.23
Girard, Y.24
more..
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23
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33745151060
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Edmondson S.D., Mastracchio A., Mathvink R.J., He J., Harper B., Park J.-J., Beconi M., Di Salvo J., Eiermann G.J., He H., Leiting B., Leone J.F., Levorse D.A., Lyons K., Patel R.A., Patel S.B., Petrov A., Scapin G., Shang J., Sinha Roy R., Smith A., Wu J.K., Xu S., Zhu B., Thornberry N.A., and Weber A.E. J. Med. Chem. 49 (2006) 3614
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(2006)
J. Med. Chem.
, vol.49
, pp. 3614
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Edmondson, S.D.1
Mastracchio, A.2
Mathvink, R.J.3
He, J.4
Harper, B.5
Park, J.-J.6
Beconi, M.7
Di Salvo, J.8
Eiermann, G.J.9
He, H.10
Leiting, B.11
Leone, J.F.12
Levorse, D.A.13
Lyons, K.14
Patel, R.A.15
Patel, S.B.16
Petrov, A.17
Scapin, G.18
Shang, J.19
Sinha Roy, R.20
Smith, A.21
Wu, J.K.22
Xu, S.23
Zhu, B.24
Thornberry, N.A.25
Weber, A.E.26
more..
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24
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0023089725
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50 determinations for rabbit calcium channel were carried out as described in
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50 determinations for rabbit calcium channel were carried out as described in. Shoemaker H., Hicks P., and Langer S. J. Cardiovasc. Pharm. 9 (1987) 173
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(1987)
J. Cardiovasc. Pharm.
, vol.9
, pp. 173
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Shoemaker, H.1
Hicks, P.2
Langer, S.3
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26
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0034612348
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Marquet D., Baggio L., Kobayashi T., Bernard A.-M., Pierres M., Nielsen M., Ribel U., Watanabe T., Drucker D.J., and Wagtmann N.P. Proc. Natl. Acad. Sci. U.S.A. 97 (2000) 6874
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(2000)
Proc. Natl. Acad. Sci. U.S.A.
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Marquet, D.1
Baggio, L.2
Kobayashi, T.3
Bernard, A.-M.4
Pierres, M.5
Nielsen, M.6
Ribel, U.7
Watanabe, T.8
Drucker, D.J.9
Wagtmann, N.P.10
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