Optimization of the β-Aminoester class of factor Xa inhibitors. part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant …

…, KD Brown, DJ Colussi, V Chu, CL Heran… - Bioorganic & medicinal …, 2002 - Elsevier
Further optimization of the β-aminoester class of factor Xa (fXa) inhibitors is described
culminating in the identification of 9c (FXV673), a potent and selective factor Xa inhibitor with …

A rabbit model for sublingual drug delivery: comparison with human pharmacokinetic studies of propranolol, verapamil and captopril

…, PA Moench, NR Mathias, PI Stetsko, CL Heran… - Journal of …, 2006 - Elsevier
A rabbit model for investigating sublingual drug absorption was established yielding results
consistent with clinical data reported in the literature. Using propranolol as a model …

Carbopol-mediated paracellular transport enhancement in Calu-3 cell layers

L Li, NR Mathias, CL Heran, P Moench, DA Wall… - Journal of …, 2006 - Elsevier
The interaction of Carbopol polymers with mucus producing Calu-3 human bronchial
epithelial cells was evaluated to test for potential paracellular transport enhancement. Using …

Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization

…, KD Brown, DJ Colussi, V Chu, CL Heran… - Journal of medicinal …, 1999 - ACS Publications
… mL) and treated with SO 2 Cl 2 (3.32 mL, 3.32 mmol, 1 M solution in CH 2 Cl 2 ) at 0 C. The
… followed by 100 mL of hot anhydrous CH 2 Cl 2 and was used without further purification (…

Identification and initial structure− activity relationships of a novel class of nonpeptide inhibitors of blood coagulation factor Xa

…, SA Bolton, K Brown, D Colussi, CL Heran… - Journal of medicinal …, 1998 - ACS Publications
The discovery and some of the basic structure−activity relationships of a series of novel
nonpeptide inhibitors of blood coagulation Factor Xa is described. These inhibitors are …

Effects of antithrombotic drugs in a rat model of aspirin-insensitive arterial thrombosis

…, TE Steinbacher, CL Heran… - Thrombosis and …, 1993 - thieme-connect.com
These studies describe experimental conditions where aspirin is less effective than other
antiplatelet and anticoagulant drugs in inhibiting acute arterial thrombosis. External electrolytic …

Low-molecular-weight heparin (fragmin) and thrombin active-site inhibitor (argatroban) compared in experimental arterial and venous thrombosis and bleeding time

WA Schumacher, CL Heran… - Journal of …, 1996 - journals.lww.com
The antithrombotic and bleeding effects of a low-molecular-weight heparin (LMWH, fragmin)
and a thrombin active-site inhibitor (argatroban) were determined in anesthetized rats. …

Superior activity of a thromboxane receptor antagonist as compared with aspirin in rat models of arterial and venous thrombosis

WA Schumacher, CL Heran… - Journal of …, 1993 - journals.lww.com
We determined the effects of aspirin and a novel thromboxane A2/prostaglandin endoperoxide
(TP)-receptor antagonist, BMS-180291, on thrombosis and bleeding times in skin and …

Effects of SQ 14,225, an orally active inhibitor of angiotensin-converting enzyme on blood pressure, heart rate and plasma renin activity of conscious normotensive …

DN Harris, CL Heran, HJ Goldenberg, JP High… - European Journal of …, 1978 - Elsevier
Oral administration of SQ 14,225 (0.03–3 mg/kg) to conscious normotensive dogs caused
inhibition of the pressor response to intravenously administered angiotensin I (AI), the duration …

[PDF][PDF] Comparison of thrombin active site and exosite inhibitors and heparin in experimental models of arterial and venous thrombosis and bleeding.

WA Schumacher, TE Steinbacher, CL Heran… - … of Pharmacology and …, 1993 - Citeseer
Different pharmacological approaches to thromn inhibition were compared for their effects on
thrombosis and bleeding time in anesthetized rats. Thrombosis was induced in the carotid …