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Results: 1 to 20 of 117

1.

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;58:136-52. doi: 10.1016/j.ejmech.2012.10.005. Epub 2012 Oct 16.

PMID:
23124211
[PubMed - indexed for MEDLINE]
2.

Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites.

Komoriya S, Haginoya N, Kobayashi S, Nagata T, Mochizuki A, Suzuki M, Yoshino T, Horino H, Nagahara T, Suzuki M, Isobe Y, Furugoori T.

Bioorg Med Chem. 2005 Jun 2;13(12):3927-54.

PMID:
15911309
[PubMed - indexed for MEDLINE]
3.

Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.

Zhang P, Bao L, Fan J, Jia ZJ, Sinha U, Wong PW, Park G, Hutchaleelaha A, Scarborough RM, Zhu BY.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2186-9. doi: 10.1016/j.bmcl.2009.02.114. Epub 2009 Mar 3.

PMID:
19297158
[PubMed - indexed for MEDLINE]
4.

Design, synthesis, and biological evaluation of peptidomimetic inhibitors of factor XIa as novel anticoagulants.

Lin J, Deng H, Jin L, Pandey P, Quinn J, Cantin S, Rynkiewicz MJ, Gorga JC, Bibbins F, Celatka CA, Nagafuji P, Bannister TD, Meyers HV, Babine RE, Hayward NJ, Weaver D, Benjamin H, Stassen F, Abdel-Meguid SS, Strickler JE.

J Med Chem. 2006 Dec 28;49(26):7781-91.

PMID:
17181160
[PubMed - indexed for MEDLINE]
5.

Design, synthesis, and structure-activity relationships of unsubstituted piperazinone-based transition state factor Xa inhibitors.

Huang W, Naughton MA, Yang H, Su T, Dam S, Wong PW, Arfsten A, Edwards S, Sinha U, Hollenbach S, Scarborough RM, Zhu BY.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):723-8.

PMID:
12639567
[PubMed - indexed for MEDLINE]
6.

Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.

Ishihara T, Seki N, Hirayama F, Orita M, Koshio H, Taniuchi Y, Sakai-Moritani Y, Iwatsuki Y, Kaku S, Kawasaki T, Matsumoto Y, Tsukamoto S.

Bioorg Med Chem. 2007 Jun 15;15(12):4175-92. Epub 2007 Mar 25.

PMID:
17416533
[PubMed - indexed for MEDLINE]
7.

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.

Zhang P, Bao L, Zuckett JF, Jia ZJ, Woolfrey J, Arfsten A, Edwards S, Sinha U, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):989-93.

PMID:
15013007
[PubMed - indexed for MEDLINE]
8.

Discovery and characterization of a potent and selective non-amidine inhibitor of human factor Xa.

Liang AM, Light DR, Kochanny M, Rumennik G, Trinh L, Lentz D, Post J, Morser J, Snider M.

Biochem Pharmacol. 2003 May 1;65(9):1407-18.

PMID:
12732352
[PubMed - indexed for MEDLINE]
9.

Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.

Shi Y, O'Connor SP, Sitkoff D, Zhang J, Shi M, Bisaha SN, Wang Y, Li C, Ruan Z, Lawrence RM, Klei HE, Kish K, Liu EC, Seiler SM, Schweizer L, Steinbacher TE, Schumacher WA, Robl JA, Macor JE, Atwal KS, Stein PD.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7516-21. doi: 10.1016/j.bmcl.2011.06.098. Epub 2011 Jun 28.

PMID:
22041058
[PubMed - indexed for MEDLINE]
10.

Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.

Ewing WR, Becker MR, Manetta VE, Davis RS, Pauls HW, Mason H, Choi-Sledeski YM, Green D, Cha D, Spada AP, Cheney DL, Mason JS, Maignan S, Guilloteau JP, Brown K, Colussi D, Bentley R, Bostwick J, Kasiewski CJ, Morgan SR, Leadley RJ, Dunwiddie CT, Perrone MH, Chu V.

J Med Chem. 1999 Sep 9;42(18):3557-71.

PMID:
10479288
[PubMed - indexed for MEDLINE]
11.

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.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):729-32.

PMID:
12639568
[PubMed - indexed for MEDLINE]
12.

Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors.

Maduskuie TP Jr, McNamara KJ, Ru Y, Knabb RM, Stouten PF.

J Med Chem. 1998 Jan 1;41(1):53-62.

PMID:
9438022
[PubMed - indexed for MEDLINE]
13.

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 Jr, Rossi KA, Jona J, Knabb RM, Luettgen JM, Wong PC, Bai SA, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5176-82. Epub 2006 Jul 25.

PMID:
16870435
[PubMed - indexed for MEDLINE]
14.

Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors.

Ye B, Arnaiz DO, Chou YL, Griedel BD, Karanjawala R, Lee W, Morrissey MM, Sacchi KL, Sakata ST, Shaw KJ, Wu SC, Zhao Z, Adler M, Cheeseman S, Dole WP, Ewing J, Fitch R, Lentz D, Liang A, Light D, Morser J, Post J, Rumennik G, Subramanyam B, Sullivan ME, Vergona R, Walters J, Wang YX, White KA, Whitlow M, Kochanny MJ.

J Med Chem. 2007 Jun 28;50(13):2967-80. Epub 2007 May 31.

PMID:
17536795
[PubMed - indexed for MEDLINE]
15.

Discovery of N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide (darexaban, YM150) as a potent and orally available factor Xa inhibitor.

Hirayama F, Koshio H, Ishihara T, Hachiya S, Sugasawa K, Koga Y, Seki N, Shiraki R, Shigenaga T, Iwatsuki Y, Moritani Y, Mori K, Kadokura T, Kawasaki T, Matsumoto Y, Sakamoto S, Tsukamoto S.

J Med Chem. 2011 Dec 8;54(23):8051-65. doi: 10.1021/jm200868m. Epub 2011 Nov 11.

PMID:
21995444
[PubMed - indexed for MEDLINE]
16.

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.

PMID:
15267248
[PubMed - indexed for MEDLINE]
17.

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.

PMID:
11170646
[PubMed - indexed for MEDLINE]
18.

Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors.

Chou YL, Davey DD, Eagen KA, Griedel BD, Karanjawala R, Phillips GB, Sacchi KL, Shaw KJ, Wu SC, Lentz D, Liang AM, Trinh L, Morrissey MM, Kochanny MJ.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):507-11.

PMID:
12565961
[PubMed - indexed for MEDLINE]
19.

Design, synthesis and biological activity of YM-60828 derivatives: potent and orally-bioavailable factor Xa inhibitors based on naphthoanilide and naphthalensulfonanilide templates.

Hirayama F, Koshio H, Ishihara T, Watanuki S, Hachiya S, Kaizawa H, Kuramochi T, Katayama N, Kurihara H, Taniuchi Y, Sato K, Sakai-Moritani Y, Kaku S, Kawasaki T, Matsumoto Y, Sakamoto S, Tsukamoto S.

Bioorg Med Chem. 2002 Aug;10(8):2597-610.

PMID:
12057649
[PubMed - indexed for MEDLINE]
20.

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.

Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Dunwiddie CT, Leadley RJ, Pauls HW.

Bioorg Med Chem Lett. 2002 Jun 17;12(12):1671-4.

PMID:
12039587
[PubMed - indexed for MEDLINE]

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