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

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Showing 12471 - 12480 of 12523 results

Status:
Possibly Marketed Outside US
Source:
VIVACE by Takeda Chemical Industries
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Delapril is a lipophilic nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor, which has been shown to exert potent ACE inhibitory activity and is marketed as an antihypertensive drug. Delapril has been shown to exist in solution as a mixture of s-cis and s-trans conformational isomers, as a result of restricted rotation about the amide bond.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Azalanstat is a synthetic imidazole. It has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. In hamsters it lowered serum cholesterol in a dose-dependent manner. Azalanstat preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1. Azalanstat inhibited hepatic microsomal hydroxymethylglutaryl-CoA (HMG-CoA) reductase activity in hamsters in a dose-dependent manner and this was highly correlated with serum cholesterol lowering. In vitro studies with HepG2 cells indicated that this modulation of reductase activity was indirect, occurring at a post-transcriptional step. Azalanstat has been in preclinical phase for the treatment of hyperlipidaemia but this research has been discontinued.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Fenticonazole is an imidazole derivative with a broad spectrum of antimycotic activity. It is used as a nitrate salt under different trade names (Lomexin, Gynoxin, Fentizol, etc) for the treatment of vaginal candidiasis. Fenticonazole inhibits the synthesis of ergosterol, an important step in the formation of the wall of fungi and blocks the oxidizing enzymes with the corresponding accumulation of peroxides and necrosis of the fungal cell. In vitro studies have shown a broad fungistatic and fungicidal activity. Like other azole agents, the spectrum of action of Fenticonazole also extends to some gram-positive bacteria such as Staphylococcus aureus. In vivo studies have also shown activity against Trichomonas Vaginalis.
Status:
Possibly Marketed Outside US
Source:
NCT02939495: Phase 4 Interventional Completed Premature Ejaculation
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dapoxetine hydrochloride is a selective serotonin reuptake inhibitor (SSRIs). In addition, dapoxetine inhibits voltage-dependent K+ (Kv) channels in a dose-, time-, use-, and state (open)-dependent manner, independent of serotonin reuptake inhibition. Dapoxetine is indicated for the treatment of premature ejaculation (PE) in men 18 to 64 years of age, who have all of the following: persistent or recurrent ejaculation with minimal sexual stimulation before, on, or shortly after penetration and before the patient wishes; and marked personal distress or interpersonal difficulty as a consequence of PE; and poor control over ejaculation. The mechanism of action of dapoxetine in premature ejaculation is presumed to be linked to the inhibition of neuronal reuptake of serotonin and the subsequent potentiation of the neurotransmitter's action at pre- and post-synaptic receptors. The most common effects when taking dapoxetine are nausea, dizziness, dry mouth, headache, diarrhea, and insomnia.
Status:
Possibly Marketed Outside US
Source:
Neo-Percamin S by Teikoku Kagaku Sangyo
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


2-Diethylaminoethyl 4-Butylaminobenzoate (farmocaine, T-caine) is an ester-type local anesthetic drug. Like all ester-type local anesthetic drugs farmocaine is very unstable in the body, and in humans they are rapidly hydrolyzed in the plasma. No direct correlation between the saponification and biological activity of farmocaine and similar local anesthetic esters was found. T-Caine has been used as a spray anesthetization of the throat and as a component of Neoarsen black, Neo-percamin S, topical Neozalocain(R) pasta (benzocaine and farmocaine, Neo Dental Chemical Products, Osaka, Japan) and as a calvital powder in dentistry.
Gabexate is a synthetic protease inhibitor, was shown to be effective in treating patients with sepsis-associated disseminated intravascular coagulation in which tumor necrosis factor-alpha (TNF-alpha) plays a critical role. Gabexate mesylate is a drug marketed only in Italy and Japan and it is considered an essential drug in the treatment of acute pancreatitis. Gabexate is marketed under the brand name REMINARON among others in Japan. It relieves inflammatory symptoms in the pancreas by inhibiting various enzymes. It also improves organ disorders and bleeding tendency caused by blood clots in blood vessels by inhibiting blood coagulation. It is usually used to treat acute pancreatitis with deviation of proteolytic enzymes (such as trypsin, kallikrein and plasmin), acute exacerbation of chronic recurrent pancreatitis, acute pancreatitis after surgery and disseminated intravascular coagulation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Acecainide (N-acetylprocainamide), the N-acetylated metabolite of procainamide, is a Class III antiarrhythmic agent. Acecainide exerts cardiac anticholinergic effect. It elicits smooth muscle relaxation mainly through the activation of plasma membrane K+ channels. Acecainide markedly reduced premature ventricular beats and prevented induction of ventricular tachycardia. Acecainide appears to offer advantages over procainamide, particularly with respect to the reduced formation of antinuclear antibodies. Acecainide development has been discontinued.
Status:
Possibly Marketed Outside US
Source:
PIPORTIL L4 by Puech, A.J.|Chermat, R.|Malatray, J.|Simon, P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pipotiazine (Piportil), also known as Pipothiazine, is a typical antipsychotic of the phenothiazine class used in the United Kingdom and other countries for the treatment of schizophrenia. Its properties are similar to those of chlorpromazine. Piportil® L4 (pipotiazine palmitate) is the palmitic ester of pipotiazine, a piperidine phenothiazine with antipsychotic properties and weak sedative activity. The esterification of pipotiazine is responsible for its prolonged duration of action. The onset of action appears usually within the first 2 to 3 days after injection and the effects of the drug on psychotic symptoms are significant within one week. Improvement in symptomatology lasts from 3 to 6 weeks, but adequate control may frequently be maintained with one injection every 4 weeks. However, in view of the variations in individual response, careful supervision is required throughout treatment. Piportil L4 has actions similar to those of other phenothiazines. Among the different phenothiazine derivatives, Piportil L4 appears to be less sedating and to have a weak propensity for causing hypotension or potentiating the effects of CNS depressants and anesthetics. However, it produces a high incidence of extrapyramidal reactions.
Status:
Possibly Marketed Outside US
Source:
TRIMOL by Fujisawa Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Piroheptine is an antagonist of muscarinic acetylcholine receptors. The drug was used for the treatment of Parkinson's disease, however, it is no longer marketed.
Status:
Possibly Marketed Outside US
Source:
Japan:Proxazole Citrate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Proxazole Citrate is a spasmolytic papaverine-like agent used for functional gastrointestinal disorders in veterinary and acute renal insufficiency. In animal models, Proxazole has antitussive, antispasmodic, analgesic, anti-inflammatory, and antipyretic activities. Proxazole has veterinary uses against gastritis, infective and non-infective gastro-enteritis, urethritis, cystitis and spastic states with an inflammatory component of the smooth muscles of the digestive and genito-urinary systems. Proxazole is excreted both in feces and urine mainly as inactive metabolites.

Showing 12471 - 12480 of 12523 results