U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 181 - 190 of 2551 results

Status:
Investigational
Source:
INN:lamtidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

LAMTIDINE is an irreversible and specific gastric histamine H2-receptor antagonist.
Status:
Investigational
Source:
INN:becliconazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Becliconazole (or 1-CBCMI) is an antimycotic agent. Information about the nowadays application of this drug is not available
Status:
Investigational
Source:
INN:tiplasinin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Tiplasinin (PAI-039) is an orally efficacious and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor. Tiplasinin bound specifically to the active conformation of PAI-1 and exhibited reversible inactivation of PAI-1 in vitro. Tiplaxtinin exhibited in vivo oral efficacy in two different models of acute arterial thrombosis. The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to Phase-I clinical trial for Thrombosis, which was later discontinued.
Status:
Investigational
Source:
INN:cliropamine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Cliropamine (D 16427) is a positive inotropic compound.
Status:
Investigational
Source:
INN:cetaben [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Cetaben has been identified as an anti-atherosclerotic hypolipidaemic substance. Cetaben is a unique, PPARα-independent peroxisome proliferator with hypolipidemic activity that inhibits cholesterol synthesis in the human hepatoma Hep-G2 cells resulting in reversible changes in Golgi morphology. Cetaben represents an exceptional type of peroxisome proliferator, specifically affecting peroxisomes, without having a negative influence on the processes of peroxisome biogenesis. Cetaben raised only the peroxisomal enzymes, acyl-CoA oxidase, glycerone-phosphate acyltransferase, D-amino-acid oxidase, catalase, and urate oxidase. Cetaben sodium has being shown to be an antiatherosclerotic agent.
Status:
Investigational
Source:
INN:sufugolix [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sufugolix (TAK-013 or 5-(N-benzyl-N-methylaminomethyl)-1-(2,6-difluorobenzyl)-6-[4-(3-methoxyureido)phenyl]-3-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione) is a highly potent and orally active non-peptide antagonist of luteinizing hormone-releasing hormone (LHRH) receptor. Sufugolix by oral administration suppresses a pituitary-ovarian axis continuously and reversibly in cynomolgus monkeys. Takeda studied Sufugolix in the trials for the treatment of endometriosis and uterine leiomyoma however development was discontinued.
Status:
Investigational
Source:
INN:trizoxime [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Trizoxime is an antidepressant.
Status:
Investigational
Source:
NCT00106808: Phase 3 Interventional Completed Type 2 Diabetes Mellitus
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Muraglitazar previously known as BMS-298585 has been identified as a non-thiazolidinedione dual agonist of peroxisome proliferator-activated receptor alpha/gamma. Muraglitazar is currently in clinical trial phase III development for the treatment of type 2 diabetes and dyslipidemia.
Status:
Investigational
Source:
INN:pirodavir
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pirodavir (R77975) (ethyl 4-[2-(1-[6-methyl-3-pyridazinyl]-4-piperidinyl)ethoxy]benzoate) and its predecessor (R61837) belong to a series of pyridazine analogues developed by the Janssen Research Foundation. Compared to R61837, pirodavir was 500-fold more potent as an antiviral in vitro, inhibiting 80% of 100 rhinovirus serotypes tested at concentration of 0.064 mg/mL or less. Pirodavir acts at an early stage of the viral replication cycle (up to 40 min after infection) and reduces the yield of selected rhinoviruses 1,000- to 100,000-fold in a single round of replication. The mode of action appears to be serotype specific, since pirodavir was able to inhibit the adsorption of human rhinovirus 9 but not that of human rhinovirus 1A. Pirodavir is a novel capsid-binding antipicornavirus agent with potent in vitro activity against both group A and group B rhinovirus serotypes.
Status:
Investigational
Source:
INN:tienoxolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tienoxolol is a benzoic acid derivative patented by Centre d'Activite et de Recherche Pharmaceutique Industrielle Biologique et Medicale as β-sympatholytic and diuretic. Tienoxolol acts as a beta-adrenergic receptor antagonist shows potent diuretic and natriuretic activity and, besides that anti-hypertension activity in preclinical models. In clinical trials, Tienoxolol significantly and dose-dependently reduced exercise-induced tachycardia. This effect started 1 h after drug administration, peaked between 4 h and 6 h and lasted at least 12 h.