메뉴 건너뛰기




Volumn 7, Issue 4, 2004, Pages 460-469

The race to an orally active Factor Xa inhibitor: Recent advances

Author keywords

Anticoagulant; Antithrombotic; Factor Xa; Thrombosis

Indexed keywords

1 [3 (AMINOMETHYL)PHENYL] N [3 FLUORO 2' (METHYLSULFONYL)[1,1' BIPHENYL] 4 YL] 3 (TRIFLUOROMETHYL) 1H PYRAZOLE 5 CARBOXAMIDE; ACETYLSALICYLIC ACID; ANTICOAGULANT AGENT; ANTITHROMBOCYTIC AGENT; BENZAMIDINE; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; CLOPIDOGREL; ENOXAPARIN; LOW MOLECULAR WEIGHT HEPARIN; PROTHROMBIN; PYRAZOLE DERIVATIVE; RAZAXABAN; SN 429; SULFONAMIDE; THROMBIN; UNCLASSIFIED DRUG; ANTITHROMBIN III;

EID: 4644221541     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (58)

References (66)
  • 1
    • 0037437117 scopus 로고    scopus 로고
    • Management of venous thromboembolism. Past, present and future
    • Hyers TM: Management of venous thromboembolism. Past, present and future. Arch Intern Med (2003) 163(7):759-768.
    • (2003) Arch Intern Med , vol.163 , Issue.7 , pp. 759-768
    • Hyers, T.M.1
  • 2
    • 0030858230 scopus 로고    scopus 로고
    • Low-molecular-weight heparins
    • Weitz JI: Low-molecular-weight heparins. New Engl J Med (1997) 337(10):688-698.
    • (1997) New Engl J Med , vol.337 , Issue.10 , pp. 688-698
    • Weitz, J.I.1
  • 3
    • 0034917336 scopus 로고    scopus 로고
    • Low-molecular-weight heparins in the treatment of acute coronary syndromes
    • Turpie AG, Antman EM: Low-molecular-weight heparins in the treatment of acute coronary syndromes. Arch Intern Med (2001) 161(12):1484-1490.
    • (2001) Arch Intern Med , vol.161 , Issue.12 , pp. 1484-1490
    • Turpie, A.G.1    Antman, E.M.2
  • 4
    • 0037239007 scopus 로고    scopus 로고
    • Evaluation of the pharmacological properties and clinical results of the synthetic pentasaccharide (fondaparinux)
    • Samama MM, Gerotziafas GT: Evaluation of the pharmacological properties and clinical results of the synthetic pentasaccharide (fondaparinux). Thromb Res (2003) 109(1):1-11.
    • (2003) Thromb Res , vol.109 , Issue.1 , pp. 1-11
    • Samama, M.M.1    Gerotziafas, G.T.2
  • 6
    • 0037797327 scopus 로고    scopus 로고
    • New antithrombotic drugs on the horizon
    • Ruef J, Katus HA: New antithrombotic drugs on the horizon. Expert Opin Investig Drugs (2003) 12(5):781-797.
    • (2003) Expert Opin Investig Drugs , vol.12 , Issue.5 , pp. 781-797
    • Ruef, J.1    Katus, H.A.2
  • 7
    • 0035383645 scopus 로고    scopus 로고
    • Coagulation Factor Xa inhibition: Biological background and rationale
    • Leadley RJ Jr: Coagulation Factor Xa inhibition: Biological background and rationale. Curr Top Med Chem (2001) 1(2):151-159.
    • (2001) Curr Top Med Chem , vol.1 , Issue.2 , pp. 151-159
    • Leadley Jr., R.J.1
  • 8
    • 0344629348 scopus 로고    scopus 로고
    • Synthetic inhibitors of thrombin and Factor Xa: From bench to bedside
    • Hauptmann J, Stürzebecher J: Synthetic inhibitors of thrombin and Factor Xa: From bench to bedside. Thromb Res (1999) 93(5):203-241.
    • (1999) Thromb Res , vol.93 , Issue.5 , pp. 203-241
    • Hauptmann, J.1    Stürzebecher, J.2
  • 11
    • 0036588776 scopus 로고    scopus 로고
    • Synthetic direct and indirect Factor Xa inhibitors
    • Samama MM: Synthetic direct and indirect Factor Xa inhibitors. Thromb Res (2002) 106(3):V267-V273.
    • (2002) Thromb Res , vol.106 , Issue.3
    • Samama, M.M.1
  • 12
    • 0036180835 scopus 로고    scopus 로고
    • Factor Xa - A promising target for drug development
    • Kaiser B: Factor Xa - A promising target for drug development. Cell Mol Life Sci (2002) 59(2):189-192.
    • (2002) Cell Mol Life Sci , vol.59 , Issue.2 , pp. 189-192
    • Kaiser, B.1
  • 13
    • 0038012642 scopus 로고    scopus 로고
    • Selective Factor Xa inhibition improves efficacy of venous thromboembolism prophylaxis in orthopedic surgery
    • Comp PC: Selective Factor Xa inhibition improves efficacy of venous thromboembolism prophylaxis in orthopedic surgery. Pharmacotherapy (2003) 23(6):772-787.
    • (2003) Pharmacotherapy , vol.23 , Issue.6 , pp. 772-787
    • Comp, P.C.1
  • 15
    • 0036847576 scopus 로고    scopus 로고
    • Antithrombotic effects of DX-9065a, a direct Factor Xa inhibitor: A comparative study in humans versus low-molecular-weight heparin
    • Shimbo D, Osende J, Chen J, Robbins J, Shimoto Y, Kunitada S, Fuster V, Badimon JJ: Antithrombotic effects of DX-9065a, a direct Factor Xa inhibitor: A comparative study in humans versus low-molecular-weight heparin. Thromb Haemost (2002) 88(5):733-738.
    • (2002) Thromb Haemost , vol.88 , Issue.5 , pp. 733-738
    • Shimbo, D.1    Osende, J.2    Chen, J.3    Robbins, J.4    Shimoto, Y.5    Kunitada, S.6    Fuster, V.7    Badimon, J.J.8
  • 16
    • 0035865785 scopus 로고    scopus 로고
    • The discovery of 1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2′- (methylsulfonyl)-[(1,1-biphenyl)]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5- carboxamide (DPC423), a highly potent, selective and orally bioavailable inhibitor of blood coagulation Factor Xa
    • Pinto DJ, Orwat MJ, Wang S, Fevig JM, Quan ML, Amparo E, Cacciola J, Rossi KA, Alexander RS, Smallwood AM, Luettgen JM et al: The discovery of 1-[3-(aminomethyl)phenyl]-N-[3-fluoro-2′-(methylsulfonyl)-[(1,1-biphenyl)] -4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective and orally bioavailable inhibitor of blood coagulation Factor Xa. J Med Chem (2001) 44(4):566-578. Review discussing the SAR leading to the discovery of DMP-423, a potent and selective fXa inhibitor with good oral bioavailability and antithrombotic efficacy.
    • (2001) J Med Chem , vol.44 , Issue.4 , pp. 566-578
    • Pinto, D.J.1    Orwat, M.J.2    Wang, S.3    Fevig, J.M.4    Quan, M.L.5    Amparo, E.6    Cacciola, J.7    Rossi, K.A.8    Alexander, R.S.9    Smallwood, A.M.10    Luettgen, J.M.11
  • 17
  • 18
    • 0036387145 scopus 로고    scopus 로고
    • Nonpeptide Factor Xa inhibitors: DPC423, a highly potent and orally bioavailable pyrazole antithrombotic agent
    • Wong PC, Pinto DJ, Knabb RM: Nonpeptide Factor Xa inhibitors: DPC423, a highly potent and orally bioavailable pyrazole antithrombotic agent. Cardiovascular Drug Rev (2002) 20(2):137-152. Summary of the in vitro and in vivo pharmacology of DMP-423.
    • (2002) Cardiovascular Drug Rev , vol.20 , Issue.2 , pp. 137-152
    • Wong, P.C.1    Pinto, D.J.2    Knabb, R.M.3
  • 19
    • 10744229522 scopus 로고    scopus 로고
    • Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N-[3-fluoro- 2′-(aminosulfonyl)-[(1,1′-biphenyl)]-4-yl]-1H-pyrazole-5- carboxyamide (DPC602), a potent, selective, and orally bioavailable Factor Xa inhibitor
    • Pruitt JR, Pinto DJ, Galemmo RA Jr, Alexander RS, Rossi KA, Wells BL, Drummond S, Bostrom LL, Burdick D, Bruckner R, Chen H et al: Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N-[3-fluoro-2′-(aminosulfonyl) -[(1,1′-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable Factor Xa inhibitor. J Med Chem (2003) 46(25):5298-5315.
    • (2003) J Med Chem , vol.46 , Issue.25 , pp. 5298-5315
    • Pruitt, J.R.1    Pinto, D.J.2    Galemmo Jr., R.A.3    Alexander, R.S.4    Rossi, K.A.5    Wells, B.L.6    Drummond, S.7    Bostrom, L.L.8    Burdick, D.9    Bruckner, R.10    Chen, H.11
  • 20
    • 10744220641 scopus 로고    scopus 로고
    • Structure-based design of novel guanidine/benzamidine mimics: Potent and orally bioavailable Factor Xa inhibitors as novel anticoagulants
    • Lam PY, Clark CG, Li R, Pinto DJ, Orwat MJ, Galemmo RA, Fevig JM, Teteha CA, Alexander RS, Smallwood AM, Rossi KA et al: Structure-based design of novel guanidine/benzamidine mimics: Potent and orally bioavailable Factor Xa inhibitors as novel anticoagulants. J Med Chem (2003) 46(21):4405-4418. A good example of rational design resulting in the discovery of novel benzamidine mimics.
    • (2003) J Med Chem , vol.46 , Issue.21 , pp. 4405-4418
    • Lam, P.Y.1    Clark, C.G.2    Li, R.3    Pinto, D.J.4    Orwat, M.J.5    Galemmo, R.A.6    Fevig, J.M.7    Teteha, C.A.8    Alexander, R.S.9    Smallwood, A.M.10    Rossi, K.A.11
  • 22
    • 33748642125 scopus 로고    scopus 로고
    • Discovery of 1-(3′-aminobenzisoxazol-5′-yl)-3- trifluoromethyl-N-[2-fluoro-4-[(2′-dimethylaminornethyl)imidazol-1-yl] phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent and selective, orally bioavailable Factor Xa inhibitor
    • in press
    • Quan ML, Lam PY, Han Q, Pinto DJ, He M, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS et al: Discovery of 1-(3′-aminobenzisoxazol- 5′-yl)-3-trifluoromethyl-N-[2-fluoro-4-[(2′-dimethylaminornethyl) imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent and selective, orally bioavailable Factor Xa inhibitor. J Med Chem (2004): in press. Successful lead optimization leading to the identification of razaxaban.
    • (2004) J Med Chem
    • Quan, M.L.1    Lam, P.Y.2    Han, Q.3    Pinto, D.J.4    He, M.5    Li, R.6    Ellis, C.D.7    Clark, C.G.8    Teleha, C.A.9    Sun, J.H.10    Alexander, R.S.11
  • 24
    • 0037124198 scopus 로고    scopus 로고
    • Design, synthesis and biological activity of novel non-amidine Factor Xa inhibitors. Part 1: P1 structure-activity relationships of the substituted 1-(2-naphthyl)-1H-pyrazolo-5-carboxylamides
    • Jia ZJ, Wu Y, Huang W, Goldman E, Zhang P, Woolfrey J, Wong P, Huang B, Sinha U, Reed A, Scarborough RM et al: Design, synthesis and biological activity of novel non-amidine Factor Xa inhibitors. Part 1: P1 structure-activity relationships of the substituted 1-(2-naphthyl)-1H-pyrazolo-5-carboxylamides. Bioorg Med Chem Lett (2002) 12(12):1651-1655.
    • (2002) Bioorg Med Chem Lett , vol.12 , Issue.12 , pp. 1651-1655
    • Jia, Z.J.1    Wu, Y.2    Huang, W.3    Goldman, E.4    Zhang, P.5    Woolfrey, J.6    Wong, P.7    Huang, B.8    Sinha, U.9    Reed, A.10    Scarborough, R.M.11
  • 28
    • 33748647921 scopus 로고    scopus 로고
    • Design, synthesis, and biological activity of novel non-amidine Factor Xa inhibitors, 4: Optimization of hydrophilic substituents for potency and oral availability
    • San Diego, CA, USA MEDI 128
    • Ye B, Cheeseman S, Chou YL, Ewing J, Fitch R, Griedel BD, Karanjawala R, Lee W, Lentz D, Liang A, Morrissey MM et al: Design, synthesis, and biological activity of novel non-amidine Factor Xa inhibitors, 4: Optimization of hydrophilic substituents for potency and oral availability. 221st ACS Meeting, San Diego, CA, USA (2001):MEDI 128.
    • (2001) 221st ACS Meeting
    • Ye, B.1    Cheeseman, S.2    Chou, Y.L.3    Ewing, J.4    Fitch, R.5    Griedel, B.D.6    Karanjawala, R.7    Lee, W.8    Lentz, D.9    Liang, A.10    Morrissey, M.M.11
  • 34
    • 0037468474 scopus 로고    scopus 로고
    • Discovery of an orally efficacious inhibitor of coagulation Factor Xa which incorporates a neutral P1 ligand
    • Choi-Sledeski YM, Keamey R, Poli G, Pauls H, Gardner C, Gong Y, Becker M, Davis R, Spada A, Liang G, Chu V et al: Discovery of an orally efficacious inhibitor of coagulation Factor Xa which incorporates a neutral P1 ligand. J Med Chem (2003) 46(5):681-684. SAR study leading to the identification of RPR-209685, which displayed a reversal of the canonical fXa binding orientation with a neutral group in the P1 pocket and a basic group in the P4 pocket.
    • (2003) J Med Chem , vol.46 , Issue.5 , pp. 681-684
    • Choi-Sledeski, Y.M.1    Keamey, R.2    Poli, G.3    Pauls, H.4    Gardner, C.5    Gong, Y.6    Becker, M.7    Davis, R.8    Spada, A.9    Liang, G.10    Chu, V.11
  • 35
    • 0037468471 scopus 로고    scopus 로고
    • Molecular structures of human Factor Xa complexed with ketopiperazine inhibitors: Preference for a neutral group in the S1 pocket
    • Maignan S, Guilloteau JP, Choi-Sledeski YM, Becker MR, Ewing WR, Pauls HW, Spada AP, Mikol V: Molecular structures of human Factor Xa complexed with ketopiperazine inhibitors: Preference for a neutral group in the S1 pocket. J Med Chem (2003) 46(5):685-690. Additional examples of fXa-inhibitor crystal complexes with neutral P1 groups.
    • (2003) J Med Chem , vol.46 , Issue.5 , pp. 685-690
    • Maignan, S.1    Guilloteau, J.P.2    Choi-Sledeski, Y.M.3    Becker, M.R.4    Ewing, W.R.5    Pauls, H.W.6    Spada, A.P.7    Mikol, V.8
  • 38
    • 0037292995 scopus 로고    scopus 로고
    • Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state Factor Xa inhibitors
    • Su T, Yang H, Volkots D, Woolfrey J, Dam S, Wong P, Sinha U, Scarborough RM, Zhu BY: Design, synthesis, and structure-activity relationships of substituted piperazinone-based transition state Factor Xa inhibitors. Bioorg Med Chem Lett (2003) 13(4):729-732.
    • (2003) Bioorg Med Chem Lett , vol.13 , Issue.4 , pp. 729-732
    • Su, T.1    Yang, H.2    Volkots, D.3    Woolfrey, J.4    Dam, S.5    Wong, P.6    Sinha, U.7    Scarborough, R.M.8    Zhu, B.Y.9
  • 39
    • 11144357441 scopus 로고    scopus 로고
    • N,N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent Factor Xa inhibitors
    • Zhaozhong JJ, Su T, Zuckett JF, Wu Y, Goldman EA, Li W, Zhang P, Clizbe LA, Song Y, Bauer SM, Huang W et al: N,N-Dialkylated 4-(4- arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo- piperazin-1-ylmethyl)-benzamidines as potent Factor Xa inhibitors. Bioorg Med Chem Lett (2004) 14(9):2073-2078.
    • (2004) Bioorg Med Chem Lett , vol.14 , Issue.9 , pp. 2073-2078
    • Zhaozhong, J.J.1    Su, T.2    Zuckett, J.F.3    Wu, Y.4    Goldman, E.A.5    Li, W.6    Zhang, P.7    Clizbe, L.A.8    Song, Y.9    Bauer, S.M.10    Huang, W.11
  • 44
    • 0141768350 scopus 로고    scopus 로고
    • A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic Factor Xa inhibitors
    • Mederski WW, Germann M: A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic Factor Xa inhibitors. Bioorg Med Chem Lett (2003) 13(21):3715-3718.
    • (2003) Bioorg Med Chem Lett , vol.13 , Issue.21 , pp. 3715-3718
    • Mederski, W.W.1    Germann, M.2
  • 45
    • 0038416714 scopus 로고    scopus 로고
    • Rational design, synthesis and structure-activity relationships of novel Factor Xa inhibitors: (2-Substituted-4-amidinophenyl)pyruvic and propionic acids
    • Sagi K, Nakagawa T, Yamanashi M, Makino S, Takahashi M, Takayanagi M, Takenaka K, Suzuki N, Oono S, Kataoka N, Ishikawa K et al: Rational design, synthesis and structure-activity relationships of novel Factor Xa inhibitors: (2-Substituted-4-amidinophenyl)pyruvic and propionic acids. J Med Chem (2003) 46(10):1845-1857.
    • (2003) J Med Chem , vol.46 , Issue.10 , pp. 1845-1857
    • Sagi, K.1    Nakagawa, T.2    Yamanashi, M.3    Makino, S.4    Takahashi, M.5    Takayanagi, M.6    Takenaka, K.7    Suzuki, N.8    Oono, S.9    Kataoka, N.10    Ishikawa, K.11
  • 47
    • 0030097984 scopus 로고    scopus 로고
    • DX-9065a, a novel, synthetic, selective and orally active inhibitor of Factor Xa: In vitro and in vivo studies
    • Herbert JM, Bernat A, Dol F, Herault JP, Crepon B, Lormeau JC: DX-9065a, a novel, synthetic, selective and orally active inhibitor of Factor Xa: In vitro and in vivo studies. J Pharmacol Exp Ther (1996) 276(3):1030-1038.
    • (1996) J Pharmacol Exp Ther , vol.276 , Issue.3 , pp. 1030-1038
    • Herbert, J.M.1    Bernat, A.2    Dol, F.3    Herault, J.P.4    Crepon, B.5    Lormeau, J.C.6
  • 48
    • 1842737110 scopus 로고    scopus 로고
    • Design, synthesis and biological activity of amindinobicyclic compounds (derivatives of DX-9065a) as Factor Xa inhibitors: SAR study of S1 and aryl binding sites
    • Komoriya S, Kanaya N, Nagahara T, Yokoyama A, Inamura K, Yokoyama Y, Katakura S, Hara T: Design, synthesis and biological activity of amindinobicyclic compounds (derivatives of DX-9065a) as Factor Xa inhibitors: SAR study of S1 and aryl binding sites. Bioorg Med Chem (2004) 12(9):2099-2114. Identification of a 6-amidino-1-ethylindole analog of DX-9065a with improved fXa potency and oral bioavailability in rats.
    • (2004) Bioorg Med Chem , vol.12 , Issue.9 , pp. 2099-2114
    • Komoriya, S.1    Kanaya, N.2    Nagahara, T.3    Yokoyama, A.4    Inamura, K.5    Yokoyama, Y.6    Katakura, S.7    Hara, T.8
  • 50
    • 0037310402 scopus 로고    scopus 로고
    • Antithrombotic effects of YM466, a synthesized direct inhibitor of Factor Xa, in an arterio-venous shunt thrombosis model in squirrel monkeys
    • Iwatsuki Y, Kaku S, Moritani Y, Taniuchi Y, Hirayama F, Koshio H, Matsumoto Y, Mano Y, Kawasaki T: Antithrombotic effects of YM466, a synthesized direct inhibitor of Factor Xa, in an arterio-venous shunt thrombosis model in squirrel monkeys. Drug Dev Res (2003) 58(2):190-195.
    • (2003) Drug Dev Res , vol.58 , Issue.2 , pp. 190-195
    • Iwatsuki, Y.1    Kaku, S.2    Moritani, Y.3    Taniuchi, Y.4    Hirayama, F.5    Koshio, H.6    Matsumoto, Y.7    Mano, Y.8    Kawasaki, T.9
  • 51
    • 11144353708 scopus 로고    scopus 로고
    • Synthesis and biological activity of novel 1,4-diazepine derivatives as Factor Xa inhibitor with potent anticoagulant and antithrombotic activity
    • Koshio H, Hirayama F, Ishihara T, Taniuchi Y, Sato K, Sakai-Moritani Y, Kaku S, Kawasaki T, Matsumoto Y, Sakamoto S, Tsukamoto S: Synthesis and biological activity of novel 1,4-diazepine derivatives as Factor Xa inhibitor with potent anticoagulant and antithrombotic activity. Bioorg Med Chem (2004) 12(9):2179-2191. Optimization of the P4 moiety in YM-60828 provided YM-96765, which demonstrated antithrombotic efficacy in animal models and good oral bioavailability in cynomolgus monkeys.
    • (2004) Bioorg Med Chem , vol.12 , Issue.9 , pp. 2179-2191
    • Koshio, H.1    Hirayama, F.2    Ishihara, T.3    Taniuchi, Y.4    Sato, K.5    Sakai-Moritani, Y.6    Kaku, S.7    Kawasaki, T.8    Matsumoto, Y.9    Sakamoto, S.10    Tsukamoto, S.11
  • 52
    • 0037295132 scopus 로고    scopus 로고
    • Design, synthesis and biological activity of YM-60828 derivatives. Part 2: Potent and orally bioavailable Factor Xa inhibitors based on benzothiadiazine-4-one template
    • Hirayama F, Koshio H, Katayama N, Ishihara T, Kaizawa H, Taniuchi Y, Sato K, Sakai-Moritani Y, Kaku S, Kurihara H, Kawasaki T et al: Design, synthesis and biological activity of YM-60828 derivatives. Part 2: Potent and orally bioavailable Factor Xa inhibitors based on benzothiadiazine-4-one template. Bioorg Med Chem (2003) 11(3):367-381. Identification of YM-169920 with improved potency and trypsin selectivity compared to YM-60828, and oral bioavailability in both mice and squirrel monkeys.
    • (2003) Bioorg Med Chem , vol.11 , Issue.3 , pp. 367-381
    • Hirayama, F.1    Koshio, H.2    Katayama, N.3    Ishihara, T.4    Kaizawa, H.5    Taniuchi, Y.6    Sato, K.7    Sakai-Moritani, Y.8    Kaku, S.9    Kurihara, H.10    Kawasaki, T.11
  • 57
    • 0036038490 scopus 로고    scopus 로고
    • Reduction of N-hydroxylated compounds: Amidoximes (N-hydroxyamidines) as pro-drugs of amidines
    • Clement B: Reduction of N-hydroxylated compounds: Amidoximes (N-hydroxyamidines) as pro-drugs of amidines. Drug Metab Rev (2002) 34(3):565-579.
    • (2002) Drug Metab Rev , vol.34 , Issue.3 , pp. 565-579
    • Clement, B.1
  • 59
    • 33748654160 scopus 로고    scopus 로고
    • Medicinal Chemistry - 12th RSC-SCI Symposium (Part I), Enzyme inhibitors, Cambridge, UK
    • Thomson Scientific, London, UK
    • Norman P: Medicinal Chemistry - 12th RSC-SCI Symposium (Part I), Enzyme inhibitors, Cambridge, UK. IDdb3 Meeting Report, Thomson Scientific, London, UK (2003).
    • (2003) IDdb3 Meeting Report
    • Norman, P.1
  • 60
    • 24944439340 scopus 로고    scopus 로고
    • Single dose escalation study investigating the pharmacodynamics, safety and pharmacokinetics of BAY59-7939 an oral direct Factor Xa inhibitor in healthy male subjects
    • Abs 3010
    • Kubitza D, Becka M, Wensing G, Voith B, Zuehlsdorf M: Single dose escalation study investigating the pharmacodynamics, safety and pharmacokinetics of BAY59-7939 an oral direct Factor Xa inhibitor in healthy male subjects. Blood (2003) 102(11):Abs 3010.
    • (2003) Blood , vol.102 , Issue.11
    • Kubitza, D.1    Becka, M.2    Wensing, G.3    Voith, B.4    Zuehlsdorf, M.5
  • 62
    • 24944439340 scopus 로고    scopus 로고
    • Multiple dose escalation study investigating the pharmacodynamics, safety, and pharmacokinetics of BAY59-7939, an oral, direct Factor Xa inhibitor in healthy male subjects
    • Abs 3004
    • Kubitza D, Becka M, Wensing G, Voith B, Zuehlsdorf M: Multiple dose escalation study investigating the pharmacodynamics, safety, and pharmacokinetics of BAY59-7939, an oral, direct Factor Xa inhibitor in healthy male subjects. Blood (2003) 102(11):Abs 3004.
    • (2003) Blood , vol.102 , Issue.11
    • Kubitza, D.1    Becka, M.2    Wensing, G.3    Voith, B.4    Zuehlsdorf, M.5
  • 64
    • 10644226422 scopus 로고    scopus 로고
    • Pharmacokinetic and pharmacodynamic characteristics in healthy volunteers of razaxaban, an orally-active, potent, selective inhibitor of Factor Xa
    • Swaminathan A, Frost C, Bai S, Knabb R, Komhauser D, Mosqueda-Garcia R: Pharmacokinetic and pharmacodynamic characteristics in healthy volunteers of razaxaban, an orally-active, potent, selective inhibitor of Factor Xa. Clin Pharmacol Ther (2004) 75(2):P6.
    • (2004) Clin Pharmacol Ther , vol.75 , Issue.2
    • Swaminathan, A.1    Frost, C.2    Bai, S.3    Knabb, R.4    Komhauser, D.5    Mosqueda-Garcia, R.6
  • 66
    • 11244325810 scopus 로고    scopus 로고
    • A phase II randomized, double-blind, five-arm, parallel-group, dose-response study of a new oral directly-acting Factor Xa inhibitor, razaxaban, for the prevention of deep vein thrombosis in knee replacement surgery - On behalf of the razaxaban investigators
    • Lassen, MR, Davidson BL, Gallus A, Pineo G, Ansell J, Deitchman D: A phase II randomized, double-blind, five-arm, parallel-group, dose-response study of a new oral directly-acting Factor Xa inhibitor, razaxaban, for the prevention of deep vein thrombosis in knee replacement surgery - On behalf of the razaxaban investigators. Blood (2003) 102(11):Abs 41.
    • (2003) Blood , vol.102 , Issue.11 , pp. 41
    • Lassen, M.R.1    Davidson, B.L.2    Gallus, A.3    Pineo, G.4    Ansell, J.5    Deitchman, D.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.