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Restrict the search for
icosapent ethyl
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Indolapril (CI-907) is a new orally active prodrug of nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor, developed by Warner-Lambert/Parke-Davis Pharmaceutical Research for treating hypertension. Indolapril is epimer of trandolapril, well-known ACE inhibitor currently in the market for hypertension treatment. Indolapril (Monoester form) and it’s active component (diacid form) produced concentration related ACE inhibition in guinea-pig serum (IC50 for monoester -- 0.1 mkM and for diacid -- 2.6 nM). In isolated rabbit aortic rings and in rat and dog autonomic studies, Indolapril is highly specific in suppressing the contractile or pressor responses to angiotensin I. In two-kidney, one-clip Goldblatt hypertensive rats, single daily doses (0.03-30 mg/kg p.o.) produced dose-dependent decreases in blood pressure; 3 mg/kg lowered blood pressure to normotensive levels. In the spontaneously hypertensive rat, subacute administration of Indolapril produced the same decrease in blood pressure as that obtained in the renal hypertensive rat. In diuretic-pretreated renal hypertensive dogs, 10 mg/kg normalized blood pressure. For equivalent drops in blood pressure, heart rate increases were less in Indolapril than in enalapril-treated renal hypertensive dogs. No side effects were observed with CI-907 in any of the conscious animals. The antihypertensive response to Indolapril (0.03-1.0 mg/kg p.o.) was found to correlate with inhibition of vascular tissue ACE, but not plasma or brain ACE in two-kidney, one-clip renal hypertensive rats.
Class (Stereo):
CHEMICAL (ABSOLUTE)
FERTIRELIN is an analog of luteinizing hormone releasing factor. The drug has been used since 1981 in Japan to treat various types of reproductive failure in cattle.
Status:
Investigational
Source:
NCT04581629: Phase 2 Interventional Completed Autosomal Dominant Hypocalcemia (ADH)
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Encaleret (JTT-305 or MK-5442) is a potent oral short-acting calcium-sensing receptor (CaSR) antagonist and transiently stimulates endogenous parathyroid hormone (PTH) secretion.
CaSR antagonists stimulate endogenous PTH secretion through CaSR on the surface of parathyroid cells and thereby may be anabolic agents for osteoporosis. Japan Tobacco and Merck were developing encaleret for the treatment of osteoporosis however development has been discontinued.
Status:
Investigational
Source:
NCT00741910: Phase 2 Interventional Completed Crohn's Disease
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.
Class (Stereo):
CHEMICAL (ACHIRAL)
Lupitidine (SKF 93479) is a histamine H2 receptor antagonist. Lupitidine is a potent inhibitor of gastric acid secretion with a long duration of action. It lacks an antiandrogenic effect. It enhances pituitary thyroid stimulating hormone drive by increasing thyroid hormone clearance. It exerts an antinociceptive effect in rodents.
Status:
Investigational
Source:
JAN:SEMOTIADIL FUMARATE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Semotiadil (also known as sesamodil or SD 3211) is a (+)-(R)-stereoisomer, the corresponding (−)-(S)-stereoisomer is called levosemotiadil. Semotiadil, a benzothiazine derivative was developed as a novel Ca2+ channel blocker with antiplatelet activity. Experiments on rodents have revealed that the drug had an advantage in the treatment of angina with regard to long-lasting action and selectivity for coronary artery and myocardium. In addition, semotiadil improved survival of rats with monocrotaline-induced pulmonary hypertension: comparison with diltiazem. Semotiadil was studied in phase II clinical trials for the treatment of angina pectoris and hypertension in Europe, and in Japan for the treatment of arrhythmias. However, the further development of semotiadil has now been discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Enpiprazole is a heterocyclic three-ringed pyrazolylalkyl piperazine derivative. Enpiprazole has a cataleptic action very similar to that of neuroleptics, and its effect on muscle relaxation is comparable with that of diazepam. Enpiprazole exerts anxiolytic properties in animals.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Thiazesim (also known as ) is a benzothiazepine derivative patented by Olin Mathieson Chemical Corp. as an oral anti-depressant and tranquilizer useful in the treatment of Parkinsonism. Thiazesim is chemically related to the tranquilizing drugs chlordiazepoxide and diazepam but possesses a unique action on the limbic system, namely a selective depression of the lateral amygdaloid nucleus in experimental animals. Thiazesim shows potent anti-depressant activity in clinical trials.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Suxethonium is a depolarising muscle relaxant, with low incidence of postoperative muscle pain.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Pimetine has been reported to be an antiatherogenic agent of particular interest since its activities are unrelated to blood cholesterol levels. Pimetine hydrochloride (IN 379) alters the production and utilization of acid mucopolysaeeharides and may block the formation of atherosclerotic plaque. The initial clinical evaluation of pimetine in neuropsychiatric disorders was performed in hospitalized patients with the diagnosis of "chronic brain syndrome". Behavioral effects of pimetine were increased alertness, interest and sociability with improvement in organization of thought processes. In patients suffering from chronic organic diseases, pimetine was reported to produce a feeling of "more energy", a general feeling of "well being" and mild insomnia was reported as a non-limiting side effect. Pimetine was found to be a less active stimulant than amphetamine.
