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Items: 16

1.

Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.

Lu T, Markotan T, Ballentine SK, Giardino EC, Spurlino J, Crysler CS, Brown K, Maryanoff BE, Tomczuk BE, Damiano BP, Shukla U, End D, Andrade-Gordon P, Bone RF, Player MR.

J Med Chem. 2010 Feb 25;53(4):1843-56. doi: 10.1021/jm901802n. Erratum in: J Med Chem. 2010 Apr 22;53(8):3422. Crysler, Carl S [added].

PMID:
20102150
2.

Torcetrapib produces endothelial dysfunction independent of cholesteryl ester transfer protein inhibition.

Connelly MA, Parry TJ, Giardino EC, Huang Z, Cheung WM, Chen C, Cools F, Van der Linde H, Gallacher DJ, Kuo GH, Sarich TC, Demarest KT, Damiano BP.

J Cardiovasc Pharmacol. 2010 May;55(5):459-68. doi: 10.1097/FJC.0b013e3181cf03cb.

PMID:
20051879
3.

Cooperative antithrombotic effect from the simultaneous inhibition of thrombin and factor Xa.

Giardino EC, Haertlein BJ, de Garavilla L, Costanzo MJ, Damiano BP, Andrade-Gordon P, Maryanoff BE.

Blood Coagul Fibrinolysis. 2010 Mar;21(2):128-34. doi: 10.1097/MBC.0b013e3283358100.

PMID:
20010091
4.

Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.

Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR.

Bioorg Med Chem Lett. 2008 May 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8.

PMID:
18420408
5.

7-fluoroindazoles as potent and selective inhibitors of factor Xa.

Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR.

J Med Chem. 2008 Jan 24;51(2):282-97. Epub 2007 Dec 27.

PMID:
18159923
6.

Exploration of potential prodrugs of RWJ-445167, an oxyguanidine-based dual inhibitor of thrombin and factor Xa.

Maryanoff BE, McComsey DF, Costanzo MJ, Yabut SC, Lu T, Player MR, Giardino EC, Damiano BP.

Chem Biol Drug Des. 2006 Jul;68(1):29-36.

PMID:
16923023
7.

In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.

Costanzo MJ, Almond HR Jr, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE.

J Med Chem. 2005 Mar 24;48(6):1984-2008. Erratum in: J Med Chem. 2007 Nov 15;50(23):5868.

PMID:
15771442
8.

A novel, potent dual inhibitor of the leukocyte proteases cathepsin G and chymase: molecular mechanisms and anti-inflammatory activity in vivo.

de Garavilla L, Greco MN, Sukumar N, Chen ZW, Pineda AO, Mathews FS, Di Cera E, Giardino EC, Wells GI, Haertlein BJ, Kauffman JA, Corcoran TW, Derian CK, Eckardt AJ, Damiano BP, Andrade-Gordon P, Maryanoff BE.

J Biol Chem. 2005 May 6;280(18):18001-7. Epub 2005 Feb 28.

9.

Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.

Lu T, Markotan T, Coppo F, Tomczuk B, Crysler C, Eisennagel S, Spurlino J, Gremminger L, Soll RM, Giardino EC, Bone R.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3727-31.

PMID:
15203151
10.

Administration of a potent antagonist of protease-activated receptor-1 (PAR-1) attenuates vascular restenosis following balloon angioplasty in rats.

Andrade-Gordon P, Derian CK, Maryanoff BE, Zhang HC, Addo MF, Cheung Wm, Damiano BP, D'Andrea MR, Darrow AL, de Garavilla L, Eckardt AJ, Giardino EC, Haertlein BJ, McComsey DF.

J Pharmacol Exp Ther. 2001 Jul;298(1):34-42.

PMID:
11408522
11.

Antithrombotic properties of RWJ-50353, a potent and novel thrombin inhibitor.

Giardino EC, Costanzo MJ, Kauffman JA, Li QS, Maryanoff BE, Andrade-Gordon P.

Thromb Res. 2000 Apr 1;98(1):83-93.

PMID:
10706936
12.

Cardiovascular profile of RWJ 29009, a new potassium channel activator, in anesthetized and conscious dogs.

Damiano BP, Giardino EC, Haertlein BJ, Stump GL, Mitchell JA, Falotico R.

J Cardiovasc Pharmacol. 1994 Feb;23(2):300-10.

PMID:
7511761
13.

RWJ 26629, a new potassium channel opener and vascular smooth muscle relaxant: a potential antihypertensive and antianginal agent.

Katz LB, Giardino EC, Salata JJ, Moore JB Jr, Falotico R.

J Pharmacol Exp Ther. 1993 Nov;267(2):648-56.

PMID:
8246137
14.

Renal vasodilators. The role of the 4-substituent in isoquinolin-3-ol cardiovascular agents: 4-ureido derivatives of isoquinolin-3-ol with selective renal vasodilator properties.

Kanojia RM, Lever OW Jr, Press JB, Williams L, Werblood HM, Giardino EC, Falotico R, Tobia AJ.

J Med Chem. 1989 May;32(5):990-7.

PMID:
2709385
15.

Renal vasodilator responses to captopril in dogs pretreated with indomethacin.

Tobia AJ, Giardino EC.

Proc Soc Exp Biol Med. 1981 Jun;167(2):242-7. No abstract available.

PMID:
7232430
16.

Levo-bunolol and propranolol: further evaluation of oral beta-blocking activity in conscious dogs.

Commarato MA, Giardino EC, Kopia GA, Kaplan HR.

Arch Int Pharmacodyn Ther. 1977 Apr;226(2):205-13.

PMID:
327960

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