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20144374942
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Quan M.L., Lam P.Y., Han Q., Pinto D.J.P., He M.Y., Li R., Ellis C.D., Clark C.G., Teleha C.A., Sun J.H., Alexander R.S., Bai S., Luettgen J.M., Knabb R.M., Wong P.C., and Wexler R.R. J. Med. Chem. 48 (2005) 1729
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41149172888
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38149086061
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Varnes J.G., Wacker D.A., Pinto D.J.P., Orwat M.J., Theroff J.P., Wells B., Galemo Jr. R.A., Luettgen J.M., Knabb R.M., Bai S., He K., Lam P.Y.S., and Wexler R.R. Bioorg. Med. Chem. Lett. 18 (2008) 749
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35649028680
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Varnes J.G., Wacker D.A., Jacobson I.C., Quan M.L., Ellis C.D., Rossi K.A., He M.Y., Luettgen J.M., Knabb R.M., Bai S., He K., Lam P.Y.S., and Wexler R.R. Bioorg. Med. Chem. Lett. 17 (2007) 6481
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He, K.11
Lam, P.Y.S.12
Wexler, R.R.13
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16
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33745123026
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Pinto D.J.P., Orwat M.J., Quan M.L., Han Q., Galemmo Jr. R.A., Amparo E., Wells B., Ellis C., He M.Y., Alexander R.S., Rossi K.A., Smallwood A., Wong P.C., Luettgen J.M., Rendina A.R., Knabb R.M., Mersinger L., Kettner C., Bai S., He K., Wexler R.R., and Lam P.Y.S. Bioorg. Med. Chem. Lett. 16 (2006) 4141
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Wells, B.7
Ellis, C.8
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Wong, P.C.13
Luettgen, J.M.14
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Knabb, R.M.16
Mersinger, L.17
Kettner, C.18
Bai, S.19
He, K.20
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Lam, P.Y.S.22
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17
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33745154028
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Fevig J.M., Cacciola J., Buriak Jr. J., Rossi K.A., Knabb R.M., Luettgen J.M., Wong P.C., Wexler R.R., and Lam P.Y.S. Bioorg. Med. Chem. Lett. 16 (2006) 3755
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Wong, P.C.7
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Lam, P.Y.S.9
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18
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33748788587
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Pinto D.J.P., Galemmo Jr. R.A., Quan M.L., Orwat M.J., Clark C., Li R., Wells B., Woerner F., alexander R.S., Rossi K.A., Smallwood A., Wong P.C., Luettgen J.M., Rendina A.R., Knabb R.M., He K., Wexler R.R., and Lam P.Y.S. Bioorg. Med. Chem. Lett. 16 (2006) 5584
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Knabb, R.M.15
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Lam, P.Y.S.18
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19
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35848929515
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Pinto D.J.P., Orwat M.J., Koch S., Rossi K.A., Alexander R.S., Smallwood A., Wong P.C., Rendina A.R., Luettgen J.M., Knabb R.M., He K., Xin B., Wexler R.R., and Lam P.Y.S. J. Med. Chem. 50 (2007) 5339
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Wexler, R.R.13
Lam, P.Y.S.14
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20
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0037468474
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Other groups have reported independently on factor Xa inhibitors with lactam cores which incorporate sulfonamide linked P1 groups, for example:
-
Other groups have reported independently on factor Xa inhibitors with lactam cores which incorporate sulfonamide linked P1 groups, for example:. Choi-Sledeski Y.M., Kearney R., Poli G., Pauls H., Gardner C., Gong Y., Becker M., Davis R., Spada A., Liang G., Chu V., Brown K., Collussi D., Leadley Jr. R., Rebello S., Moxey P., Morgan S., Bentley R., Kasiewski C., Maignan S., Guilloteau J.P., and Mikol V. J. Med. Chem. 46 (2003) 681
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Maignan, S.20
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Mikol, V.22
more..
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21
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0037293060
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Huang W., Naughton M.A., Yang H., Su T., Dam S., Wong P.W., Artsten A., Edwards S., Sinha U., Hollenbach S., Scarborough R.M., and Zhu B.Y. Bioog. Med. Chem. Lett. 13 (2003) 723
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41149087992
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Young R.J., Borthwick A.D., Brown D., Burns-Kurtis C.L., Campbell M., Chan C., Charbaut M., Chung C., Convery M.A., Kelly H.A., King N.P., Kleanthous S., Mason A.M., Pateman A.J., Patikis A.N., Pinto I.L., Pollard D.R., Senger S., Shah G.P., Toomey J.R., Watson N.S., and Weston H.E. Bioorg. Med. Chem. Lett. 23 (2008)
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Mason, A.M.13
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Senger, S.18
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Weston, H.E.22
more..
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23
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41149090958
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Young R.J., Borthwick A.D., Brown D., Burns-Kurtis C.L., Campbell M., Chan C., Charbaut M., Convery M.A., Diallo H., Hortense E., Irving W.R., Kelly H.A., King N.P., Kleanthous S., Mason A.M., Pateman A.J., Patikis A.N., Pinto I.L., Pollard D.R., Senger S., Shah G.P., Toomey J.R., Watson N.S., Weston H.E., and Zhou P. Bioorg. Med. Chem. Lett. 28 (2008)
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Kleanthous, S.14
Mason, A.M.15
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Senger, S.20
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Toomey, J.R.22
Watson, N.S.23
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more..
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24
-
-
41149124206
-
-
note
-
All of the compounds in Tables 1-5 gave satisfactory spectral and analytical data. Compounds 19-20, 29-30, 34-36, 38-41, 43-44, 46, 48 and 50 were isolated as TFA salts.
-
-
-
-
27
-
-
41149121872
-
-
note
-
Prothrombin time assay was carried as described in Refs. 3 and 4.
-
-
-
-
28
-
-
41149083771
-
-
note
-
i to in vitro anticoagulant activity see Ref. 4.
-
-
-
-
29
-
-
41149162418
-
-
D.J.P. Pinto, unpublished results.
-
D.J.P. Pinto, unpublished results.
-
-
-
-
30
-
-
41149117741
-
-
Single enantiomers of 48 were separated by chiral HPLC.
-
Single enantiomers of 48 were separated by chiral HPLC.
-
-
-
-
31
-
-
41149166925
-
-
note
-
Caco-2 and dog PK parameters were measured as described in Refs. 3 and 4.
-
-
-
-
32
-
-
34147118050
-
-
Experimental details for mechanism studies are described in a manuscript in preparation on apixaban and in
-
Experimental details for mechanism studies are described in a manuscript in preparation on apixaban and in. Luettgen J.M., Bozarth T.A., Bozarth J.M., Barbera F.A., Lam P.Y.L., Quan M.L., Pinto D.J., Wexler R.R., Rendina A.R., and Knabb R.M. Blood 108 (2006) A4130
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Knabb, R.M.10
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33
-
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41149117272
-
-
note
-
S2765 (N-α-benzoyloxycarbonyl-d-arg-l-gly-l-arg-p-nitro aniline).
-
-
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35
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0033588944
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Brown, K.D.11
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Leadley, R.J.13
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36
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10744229522
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Pruitt J.R., Pinto D.J., Galemmo Jr. R.A., Alexander R.S., Rossi K.A., Wells B.L., Drummond S., Bostrom L.L., Burdick D., Bruckner R., Chen H., Smallwood A., Wong P.C., Wright M.R., Bai S., Luettgen J.M., Knabb R.M., Lam P.Y.S., and Wexler R.R. J. Med. Chem. 46 (2003) 5298
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Lam, P.Y.S.18
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