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

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Showing 5601 - 5610 of 12702 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Zorubicin is a benzoylhydrazone derivative of the anthracycline antineoplastic antibiotic daunorubicin, but it introduces lower cardiomyopathy and bone marrow toxicity. Zorubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair as well as RNA and protein synthesis. The cytotoxic effect results from intercalation between DNA pairs. To minimize toxicity, individualized dose regimens are given preferentially over prolonged periods of time by carefully inspecting i.v. administration to prevent extravasation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dexetimide is a potent central and peripheral anticholinergic agent. It has a high affinity for all subtypes of muscarinic receptor and a long duration action. It forms very stable complex with mAChR. Dexetimide was used for many years in Europe for the treatment of extrapyramidal disorders. Neuroleptic-induced parkinsonian symptoms are effectively controlled by dexetimide. It is a safe, potent, and long-acting antiparkinsonian agent.
Status:
Possibly Marketed Outside US
Source:
Japan:Arundic Acid
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



ARUNDIC ACID (ONO-2506) is an enantiomeric, three carbon atom homolog of valproic acid under development by ONO Pharmaceutical for the potential treatment of stroke, as well as Amyotrophic Lateral Sclerosis and Parkinson's disease. The injectable formulation (Proglia) is finished phase III trials for acute-phase cerebral infarction, and the oral formulation (Cereact) is finished phase II trials in the UK for Alzheimer's disease (AD) and Parkinson's disease (PD). ARUNDIC ACID restores normal astrocyte functions after brain damage by preventing reactive astrocytosis, by activating astrocytic GABAA receptors and suppressing GABA transferase. ARUNDIC ACID inhibits S-100β synthesis in activated cultured astrocytes. This agent has additional antiglutamate and antiinflammatory COX-2 inhibitor properties
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Propatylnitrate (or propatyl nitrate), a coronary vasodilator that has been studied for the relief of acute attacks of angina pectoris. However, was revealed that this drug didn’t abolish or diminish the frequency of attacks of angina pectoris.
Status:
Possibly Marketed Outside US
Source:
ABADOL by Traumann, V.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Aminothiazole is a heterocyclic amine, commonly used as a starting point for synthesis of many compounds. In 1940s aminothiazole was used for the treatment of thyrotoxicosis. It has a direct action on the thyroid and acts by inhibiting T4 synthesis and accelerating its deiodination. Aminothiazole is an inhibitor of inducible NO synthetase (IC50 18 uM).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Fendiline or Sensit (N-(3,3-diphenylpropyl)-(1-phenylethyl)-amine), is a diphenylalkylamine blocker of L-type calcium channels. Fendiline is an anti-anginal agent for the treatment of coronary heart disease. Pharmaco-dynamically, it exerts the typical calcium as well as calmodulin antagonistic actions: inhibition of the transmembrane calcium current, smooth muscle relaxation, negative inotropism, cardioprotection, inhibition of calmodulin-activated myosin light-chain kinase and phosphodiesterase. Pharmacokinetics reveal slow onset of action and a long half-life. The anti-anginal and anti-ischaemic efficacy of fendiline has been proven in several placebo-controlled, double-blind trials. Fendiline is an FDA-approved, albeit now clinically obsolete. Additionally, fendiline is a specific inhibitor of K-Ras plasma membrane localization that also inhibits K-Ras signal output and blocks the proliferation of K-Ras-transformed tumor cells.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Fazadinium (used as a bromide salt) is a muscle relaxant, which was applied in anesthesia under the name Fazadon. The current marketing status is unknown and the drug is supposed to be discontinued.
Status:
Possibly Marketed Outside US
Source:
Japan:Timiperone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Timiperone is a neuroleptic agent that was developed in Japan. Timiperone has a potent antipsychotic activity, which is comparable to other butyrophenones such as haloperidol (HAL). Timiperone has a five-eight-times higher affinity to dopamine receptors and a 15-times higher affinity to serotonin receptors than those of HAL. Clinical trials have suggested that TIM has a specific action against negative symptoms such as lack of initiative or blunted affect as well as positive symptoms such as delusions and hallucinations in schizophrenics.
Masitinib is a new orally administered tyrosine kinase inhibitor that targets mast cells and macrophages, important cells for immunity, through inhibiting a limited number of kinases. Based on its unique mechanism of action, masitinib can be developed in a large number of conditions in oncology, in inflammatory diseases, and in certain diseases of the central nervous system. In oncology due to its immunotherapy effect, masitinib can have an effect on survival, alone or in combination with chemotherapy. Through its activity on mast cells and consequently the inhibition of the activation of the inflammatory process, masitinib can have an effect on the symptoms associated with some inflammatory and central nervous system diseases and the degeneration of these diseases. AB Science is developing masitinib in multiple sclerosis and alzheimer's disease. Masitinib targets kinases, including c-Kit, PDGFR, and Lyn. It is used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet.
Status:
Possibly Marketed Outside US
Source:
Japan:Vapiprost Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Vapiprost is a potent dicyclopentadiene thromboxane receptor antagonist that was being developed by Glaxo Wellcome in Japan. Vapiprost has been shown to be a potent and specific thromboxane (Tx)A2 receptor blocking drug in vitro using platelets and both vascular and airways smooth muscle preparations from different species. The drug is active in various experimental models of thrombosis. The potential clinical applications for a thromboxane receptor blocking drug include the treatment of thrombotic events and occlusive vascular disease. Phase III trials were underway in Japan for the treatment of deep vein thrombosis, which later were discontinued.

Showing 5601 - 5610 of 12702 results