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Journal Abstract Search

169 related items for PubMed ID: 16730984

  • 1. 1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
    Pinto DJ, Orwat MJ, Quan ML, Han Q, Galemmo RA, Amparo E, Wells B, Ellis C, He MY, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, Mersinger L, Kettner C, Bai S, He K, Wexler RR, Lam PY.
    Bioorg Med Chem Lett; 2006 Aug 01; 16(15):4141-7. PubMed ID: 16730984
    [Abstract] [Full Text] [Related]

  • 2. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
    Pinto DJ, Orwat MJ, Koch S, Rossi KA, Alexander RS, Smallwood A, Wong PC, Rendina AR, Luettgen JM, Knabb RM, He K, Xin B, Wexler RR, Lam PY.
    J Med Chem; 2007 Nov 01; 50(22):5339-56. PubMed ID: 17914785
    [Abstract] [Full Text] [Related]

  • 3. Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
    Quan ML, Lam PY, Han Q, Pinto DJ, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS, Bai S, Luettgen JM, Knabb RM, Wong PC, Wexler RR.
    J Med Chem; 2005 Mar 24; 48(6):1729-44. PubMed ID: 15771420
    [Abstract] [Full Text] [Related]

  • 4. 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(1).
    Pruitt JR, Pinto DJ, Galemmo RA, Alexander RS, Rossi KA, Wells BL, Drummond S, Bostrom LL, Burdick D, Bruckner R, Chen H, Smallwood A, Wong PC, Wright MR, Bai S, Luettgen JM, Knabb RM, Lam PY, Wexler RR.
    J Med Chem; 2003 Dec 04; 46(25):5298-315. PubMed ID: 14640539
    [Abstract] [Full Text] [Related]

  • 5. Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
    Qiao JX, King SR, He K, Wong PC, Rendina AR, Luettgen JM, Xin B, Knabb RM, Wexler RR, Lam PY.
    Bioorg Med Chem Lett; 2009 Jan 15; 19(2):462-8. PubMed ID: 19046881
    [Abstract] [Full Text] [Related]

  • 6. Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.
    Varnes JG, Wacker DA, Pinto DJ, Orwat MJ, Theroff JP, Wells B, Galemo RA, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR.
    Bioorg Med Chem Lett; 2008 Jan 15; 18(2):749-54. PubMed ID: 18054227
    [Abstract] [Full Text] [Related]

  • 7. Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
    Quan ML, Han Q, Fevig JM, Lam PY, Bai S, Knabb RM, Luettgen JM, Wong PC, Wexler RR.
    Bioorg Med Chem Lett; 2006 Apr 01; 16(7):1795-8. PubMed ID: 16434195
    [Abstract] [Full Text] [Related]

  • 8.
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    [No Abstract] [Full Text] [Related]

  • 9. Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa.
    Li YL, Fevig JM, Cacciola J, Buriak J, Rossi KA, Jona J, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY.
    Bioorg Med Chem Lett; 2006 Oct 01; 16(19):5176-82. PubMed ID: 16870435
    [Abstract] [Full Text] [Related]

  • 10. Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
    Fevig JM, Cacciola J, Buriak J, Rossi KA, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY.
    Bioorg Med Chem Lett; 2006 Jul 15; 16(14):3755-60. PubMed ID: 16682200
    [Abstract] [Full Text] [Related]

  • 11. Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
    Nazaré M, Essrich M, Will DW, Matter H, Ritter K, Urmann M, Bauer A, Schreuder H, Czech J, Lorenz M, Laux V, Wehner V.
    Bioorg Med Chem Lett; 2004 Aug 16; 14(16):4197-201. PubMed ID: 15261269
    [Abstract] [Full Text] [Related]

  • 12. 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, Liang L, Aungst BJ, Wright MR, Knabb RM, Wong PC, Wexler RR, Lam PY.
    J Med Chem; 2001 Feb 15; 44(4):566-78. PubMed ID: 11170646
    [Abstract] [Full Text] [Related]

  • 13. Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa.
    Phillips GB, Buckman BO, Davey DD, Eagen KA, Guilford WJ, Hinchman J, Ho E, Koovakkat S, Liang A, Light DR, Mohan R, Ng HP, Post JM, Shaw KJ, Smith D, Subramanyam B, Sullivan ME, Trinh L, Vergona R, Walters J, White K, Whitlow M, Wu S, Xu W, Morrissey MM.
    J Med Chem; 1998 Sep 10; 41(19):3557-62. PubMed ID: 9733480
    [No Abstract] [Full Text] [Related]

  • 14. Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.
    Shi Y, Sitkoff D, Zhang J, Han W, Hu Z, Stein PD, Wang Y, Kennedy LJ, O'Connor SP, Ahmad S, Liu EC, Seiler SM, Lam PY, Robl JA, Macor JE, Atwal KS, Zahler R.
    Bioorg Med Chem Lett; 2007 Nov 01; 17(21):5952-8. PubMed ID: 17855089
    [Abstract] [Full Text] [Related]

  • 15. Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
    Corte JR, Fang T, Pinto DJ, Han W, Hu Z, Jiang XJ, Li YL, Gauuan JF, Hadden M, Orton D, Rendina AR, Luettgen JM, Wong PC, He K, Morin PE, Chang CH, Cheney DL, Knabb RM, Wexler RR, Lam PY.
    Bioorg Med Chem Lett; 2008 May 01; 18(9):2845-9. PubMed ID: 18424044
    [Abstract] [Full Text] [Related]

  • 16. Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.
    Qiao JX, Cheng X, Smallheer JM, Galemmo RA, Drummond S, Pinto DJ, Cheney DL, He K, Wong PC, Luettgen JM, Knabb RM, Wexler RR, Lam PY.
    Bioorg Med Chem Lett; 2007 Mar 01; 17(5):1432-7. PubMed ID: 17174550
    [Abstract] [Full Text] [Related]

  • 17. Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.
    Orwat MJ, Qiao JX, He K, Rendina AR, Luettgen JM, Rossi KA, Xin B, Knabb RM, Wexler RR, Lam PY, Pinto DJ.
    Bioorg Med Chem Lett; 2014 Aug 01; 24(15):3341-5. PubMed ID: 24951330
    [Abstract] [Full Text] [Related]

  • 18. Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa.
    Willardsen JA, Dudley DA, Cody WL, Chi L, McClanahan TB, Mertz TE, Potoczak RE, Narasimhan LS, Holland DR, Rapundalo ST, Edmunds JJ.
    J Med Chem; 2004 Jul 29; 47(16):4089-99. PubMed ID: 15267248
    [Abstract] [Full Text] [Related]

  • 19. Phenyltriazolinones as potent factor Xa inhibitors.
    Quan ML, Pinto DJ, Rossi KA, Sheriff S, Alexander RS, Amparo E, Kish K, Knabb RM, Luettgen JM, Morin P, Smallwood A, Woerner FJ, Wexler RR.
    Bioorg Med Chem Lett; 2010 Feb 15; 20(4):1373-7. PubMed ID: 20100660
    [Abstract] [Full Text] [Related]

  • 20. Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element.
    Pandya V, Jain M, Chakrabarti G, Soni H, Parmar B, Chaugule B, Patel J, Jarag T, Joshi J, Joshi N, Rath A, Unadkat V, Sharma B, Ajani H, Kumar J, Sairam KV, Patel H, Patel P.
    Eur J Med Chem; 2012 Dec 15; 58():136-52. PubMed ID: 23124211
    [Abstract] [Full Text] [Related]

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