piperidines and Cerebral-Arterial-Diseases

piperidines has been researched along with Cerebral-Arterial-Diseases* in 2 studies

Other Studies

2 other study(ies) available for piperidines and Cerebral-Arterial-Diseases

Article	Year
Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring. Journal of medicinal chemistry, 2005, May-19, Volume: 48, Issue:10 A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkeys, showed a dose-dependent antithrombotic effect at 0.1, 0.3, and 1 mg kg(-1) h(-1) in a rat model of venous thrombosis, and significantly reduced the size of brain infarction in a middle cerebral artery occlusion model at a dose of 0.1 mg kg(-1) h(-1). These results suggest that compound 2 (JTV-803) is likely to be useful as both a venous and arterial antithrombotic agent. Topics: Administration, Oral; Animals; Arterial Occlusive Diseases; Brain Infarction; Cerebral Arterial Diseases; Factor Xa; Factor Xa Inhibitors; Fibrinolytic Agents; Humans; Injections, Intravenous; Isoquinolines; Macaca fascicularis; Middle Cerebral Artery; Models, Molecular; Piperidines; Pyridines; Rats; Structure-Activity Relationship; Tetrahydroisoquinolines; Venous Thrombosis	2005
[Role of gamma cineangiography in the evaluation of chronic cerebral arteriopathies]. La semaine des hopitaux : organe fonde par l'Association d'enseignement medical des hopitaux de Paris, 1983, Nov-03, Volume: 59, Issue:40 Gamma scintigraphy plays an important role in the topographic diagnosis of focalized cerebrovascular insufficiency. Furthermore, sequential imaging allows a comparative study of arterial distribution while studying the "transit time" of the radioactive tracer. In this work, the authors attempted to quantify transit time in patients with chronic cerebrovascular insufficiency while comparing the radioactivity in the hemispheres with that of the various arterial territories. The study of the arca and slope of the various arterial territories. The study of the area and slope of the tracer profile indirectly gives information about the cerebro-correlation between cerebrovascular resistance and the clinical state, there was, however, an interesting relation during vasodilator treatment (ifenprodil tartrate) in which promising clinical results were preceded by an increase in the arterial inflow component of the radioactivity curve. Topics: Adult; Aged; Cerebral Arterial Diseases; Chronic Disease; Female; Gamma Rays; Humans; Male; Middle Aged; Piperidines; Radionuclide Imaging; Technetium; Vasodilator Agents	1983

Article

Year

Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.

Journal of medicinal chemistry, 2005, May-19, Volume: 48, Issue:10

A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 exhibited potent inhibitory activity against factor Xa (FXa) and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkeys, showed a dose-dependent antithrombotic effect at 0.1, 0.3, and 1 mg kg(-1) h(-1) in a rat model of venous thrombosis, and significantly reduced the size of brain infarction in a middle cerebral artery occlusion model at a dose of 0.1 mg kg(-1) h(-1). These results suggest that compound 2 (JTV-803) is likely to be useful as both a venous and arterial antithrombotic agent.

Topics: Administration, Oral; Animals; Arterial Occlusive Diseases; Brain Infarction; Cerebral Arterial Diseases; Factor Xa; Factor Xa Inhibitors; Fibrinolytic Agents; Humans; Injections, Intravenous; Isoquinolines; Macaca fascicularis; Middle Cerebral Artery; Models, Molecular; Piperidines; Pyridines; Rats; Structure-Activity Relationship; Tetrahydroisoquinolines; Venous Thrombosis

2005

[Role of gamma cineangiography in the evaluation of chronic cerebral arteriopathies].

La semaine des hopitaux : organe fonde par l'Association d'enseignement medical des hopitaux de Paris, 1983, Nov-03, Volume: 59, Issue:40

Gamma scintigraphy plays an important role in the topographic diagnosis of focalized cerebrovascular insufficiency. Furthermore, sequential imaging allows a comparative study of arterial distribution while studying the "transit time" of the radioactive tracer. In this work, the authors attempted to quantify transit time in patients with chronic cerebrovascular insufficiency while comparing the radioactivity in the hemispheres with that of the various arterial territories. The study of the arca and slope of the various arterial territories. The study of the area and slope of the tracer profile indirectly gives information about the cerebro-correlation between cerebrovascular resistance and the clinical state, there was, however, an interesting relation during vasodilator treatment (ifenprodil tartrate) in which promising clinical results were preceded by an increase in the arterial inflow component of the radioactivity curve.

Topics: Adult; Aged; Cerebral Arterial Diseases; Chronic Disease; Female; Gamma Rays; Humans; Male; Middle Aged; Piperidines; Radionuclide Imaging; Technetium; Vasodilator Agents

1983