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

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Showing 41 - 50 of 9165 results

Status:
Investigational
Source:
INN:azaspirium chloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Azaspirium was studied as a spasmolytic and antihypertensive agent.
Status:
Investigational
Source:
NCT01147029: Phase 1 Interventional Terminated Unspecified Adult Solid Tumor, Protocol Specific
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Glutathione arsenoxide (GSAO) is a peptide trivalent arsenical that has potential anti-angiogenic capability, suggesting that it could be used for treatment in cancers where tumor metastasis relies on new blood vessel formation (angiogenesis). Endothelial cell proliferation drives new blood vessel formation. GSAO treatment causes a concentration-dependent increase in superoxide levels, ATP depletion, mitochondrial depolarization, and apoptosis in proliferating, but not endothelial cells. GSAO is able to block blood flow to solid tumors in mice, thereby inhibiting tumor growth in mice with no apparent toxicity at efficacious doses. Initial experiments have implicated GSAO in perturbing mitochondrial function. Other molecular effects of GSAO in human cells, for example on the phosphorylation of proteins, are still largely unknown. A phase I clinical trial has been terminated.
Status:
Investigational
Source:
INN:MOXIRAPRINE [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Moxiraprine (also known as CM-30366) is aminopyridazine derivative with antidepressant activity. In preclinical studies Moxiraprine induced stereotyped behaviour and antagonized haloperidol-induced catalepsy in rats, after parenteral and oral administration. In 6-hydroxy dopamine (6-OHDA)-lesioned mice, Moxiraprine induced contralateral rotations and, when injected before 6-OHDA, protected mice against its neurotoxicity. Moxiraprine also provoked contralateral rotations when injected directly into the mouse right striatum. After parenteral injection, Moxiraprine slightly increased motility in mice, at least at low doses. The stereotypies and rotations (after intrastriatal injection) induced by Moxiraprine were antagonized by haloperidol, alpha-methyl-p-tyrosine and reserpine. The effects of Moxiraprine were compared to those of direct and indirect dopamine-like drugs. Bromocriptine induced a behavioural profile, which in most aspects, was qualitatively and quantitatively similar to that of Moxiraprine. Apomorphine was found slightly more potent than Moxiraprine, but in contrast to the latter, apomorphine-induced stereotypies were insensitive to alpha-methyl-p-tyrosine or reserpine. (+)-Amphetamine and nomifensine were less potent than Moxiraprine, and unlike Moxiraprine, induced ipsilateral rotations in 6-OHDA-lesioned mice.
Status:
Investigational
Source:
Pediatr Blood Cancer. Dec 2009;53(7):1271-6.: Phase 2 Human clinical trial Completed Histiocytosis, Langerhans-Cell
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04066244: Phase 2 Interventional Recruiting Amyotrophic Lateral Sclerosis
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



BLZ 945, an orally active antagonist of the colony-stimulating factor1 receptor (CSF1R), is being developed by Novartis and Celgene Corporation for the treatment of advanced solid tumors and tumor-induced osteolytic lesions in bone and skeletal-related events. Phase I/II development for solid tumors is underway in the US, Italy, Spain, and Singapore. Preclinical trials were ongoing for tumor-induced osteolysis in Europe and the US. However, no recent reports of development had been identified for this indication.
Status:
Investigational
Source:
NCT00415038: Phase 2 Interventional Completed Essential Hypertension
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Rostafuroxin (PST 2238) is a digitoxygenin derivative, which selectively displaces ouabain from the Na ,K -ATPase receptor. PST 2238, at concentrations up to 10−4 M, did not show any significant interaction with a- and b-adrenergic, D1, D2, D3, 5-HT1, 5-HT2, H1, H2, M1, M2, A1, A2, Ca2 , Na , or K channel–associated receptors, AT1, AT2, ETa, ETb, GABA, thromboxane, vasopressin, angiotensin II, or the steorid-hormone receptors (androgen, progestogen, estrogen and mineralocorticoid), confirming that PST 2238 is specific for Na ,K -ATPase. Rostafuroxin has been developed in an attempt to unravel the contribution of mutated adducin and endogenous ouabain in the pathogenesis of hypertension. The compound lowered blood pressure in Milan hypertensive rats and humans. Rostafuroxine had been in phase II clinical trials for the treatment of hypertension. Following adverse events in Rostafuroxin group were described: dizziness, headache, upper respiratory tract infections, high blood pressure.
Status:
Investigational
Source:
INN:PRAMICONAZOLE [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pramiconazole is a novel azole with potent antifungal activity against yeasts, dermatophytes and many other fungal species. It is a new addition to the family of triazole antifungal agents that act by inhibiting fungal cell membrane ergosterol synthesis, thereby leading to increased cell permeability and destruction. In preclinical studies, pramiconazole exhibited similar or superior antifungal activity to ketoconazole and itraconazole, and selectively inhibited ergosterol synthesis with a broad spectrum activity. Pramiconazole was absorbed rapidly and had a long half-life, allowing for once-daily dosing. In phase I and II clinical trials, pramiconazole reduced the growth of Candida albicans, Malassezia globosa, Microsporum canis, Trichophyton mentagrophytes and Trichophyton rubrum, and was generally well tolerated. Pramiconazole is a well-tolerated and effective treatment for pityriasis versicolor.
Status:
Investigational
Source:
INN:ciclopramine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ciclopramine is a tetracyclic antidepressant patented by the pharmaceutical company “Chemische Fabrik Promonta G.m.b.H.” for central nervous system disorders treatment.
Status:
Investigational
Source:
NCT01631383: Phase 1 Interventional Completed Cocaine Use
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tetrahydropalmatine is a tetrahydroprotoberberine isoquinoline alkaloid that is a primary active constituent of herbal preparations containing plant species of the genera Stephania and Corydalis. The levo isomer of THP (L-THP) appears to contribute to many of the therapeutic effects of these preparations. The pharmacological profile of L-THP, which includes antagonism of dopamine D1 and D2 receptors and actions at dopamine D3, suggests that it may have utility for treating addiction. Clinical trials where L-THP was used for the treatment of cocaine and heroin addiction have promising results. The clinical trial is planned for the treatment of schizophrenia. L-Tetrahydropalmatine is recorded in the Chinese pharmacopoeia.
Status:
Investigational
Source:
INN:NIRAXOSTAT [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Y-700 (Niraxostat or 1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid) is an inhibitor of xanthine oxidoreductase. Y-700 demonstrated high oral bioavailability being predominantly eliminated via the liver. It potently reduces serum uric acid levels. Y-700 was in clinical trials for the treatment of gout.