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Showing 221 - 230 of 2579 results

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.
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.
Status:
Investigational
Source:
INN:flosatidil
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
Status:
Investigational
Source:
INN:ketocainol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

KETOCAINOL is an antiarrhythmic agent, anaesthetic.
Status:
Investigational
Source:
INN:tinofedrine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tinofedrine is a dithienylamine derivative patented by Deutsche Gold- und Silber-Scheideanstalt vorm. Roessler for improvement of cerebral and peripheral blood flow. In anesthetized dogs, Tinofedrine causes a remarkable increase of cardiac output by positive inotropic and chronotropic stimulation of the heart and simultaneous reduction of peripheral vascular resistance. In comparison with typical beta-agonists Tinofedrine at isotropically equieffective doses, has a much weaker effect on the heart rate. In coronary circulation, Tinofedrine causes vasodilation so that in a therapeutic dose range increased workload is equalized by sufficient myocardial supply.
Status:
Investigational
Source:
INN:edonentan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Edonentan (BMS 207940) is a highly selective biphenylsulfonamide endothelin A receptor antagonist. (11)C- and (18)F-labeled analogs of edonentan were evaluated of novel PET radioligands for imaging the endothelin-A receptor. Edonentan was in clinical trials for the treatment of heart failure however its development has been discontinued.
Status:
Investigational
Source:
INN:nifenalol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Nifenalol is the beta-receptor antagonist. It has optical isomers. The racemic mixture and the levo-isomer are active in antagonizing beta-receptors, but the dextro-isomer is inactive. The levo-isomer seems to be about twice as active in blocking beta-receptors as the racemate. Nifenalol is virtually devoid of local anesthetic properties in contrast to procaine, propranolol, and butidrine. Nifenalol exacerbated the fighting behavior in male mice by foot-shock. Nifenalol has been studied in patients with coronary artery disease. It afforded the coronary patient good protection against angina and ischemic changes in the EKG. It was further noted that nifenalol had no antiarrhythmic action and that it was devoid of evident side effects. Nifenalol possessed weak action against tremorine and oxotremorine induced tremor.