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

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Showing 991 - 1000 of 18894 results

Status:
Investigational
Source:
JAN:DIPHENYLPIPERIDINOBUTANOL HYDROCHLORIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Aspaminol (1,1 diphenyl-3-piperidinobutanol hydrochloride) is a nonspecific smooth muscle relaxant. It inhibits calcium uptake. The relaxation of smooth muscle induced by aspaminol may be due to a combining of aspaminol with calcium ions at the binding sites on the surface of smooth muscle, thus decreasing the supply of calcium ions to the contractile element.
Status:
Investigational
Source:
NCT01730768: Phase 2 Interventional Completed Schizophrenia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT03193853: Phase 2 Interventional Completed Triple Negative Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Serabelisib (INK1117 and TAK-117) is an orally bioavailable, PI3K p110α- isoform-specific inhibitor with an in vitro IC50 of 15 nM, highly selective against other isoforms (p110β, p110γ, and p110δ) and mTOR (no significant inhibitions at 1 μM concentration). It displayed significant efficacy in several PI3Kα mutant-specific preclinical mouse xenograft tumor models, and blocked signaling to Akt and inhibited the growth of cancer cells harboring wild-type or mutated p110α. Preclinical studies showed TAK-117 to have the low potential for disrupting glucose metabolism or for causing cardiac adverse events; in rats and monkeys, doses up to 50 mg/kg/day were well tolerated. Serabelisib is currently under clinical evaluation.
Status:
Investigational
Source:
JAN:DL-METHYLEPHEDRINE SACCHARINATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT00588185: Not Applicable Interventional Recruiting Prostate Cancer
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:endrisone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Endrysone is a glucocorticoid with anti-inflammatory and antiallergic properties. It is used topically for skin conditions as an ophthalmic anti-inflammatory agent.
Status:
Investigational
Source:
INN:tipredane
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tipredane is one of the compounds of a new series of sulfur-containing steroids synthesized at The Squibb Institute for Medical Research and is being developed for topical treatment of human dermatoses. Tipredane is structurally unique in that the classical l7-beta two-carbon side chain and the 17-alpha hydrogen of the steroid have been replaced by two alkylthio substituents. Tipredane has been shown to possess moderate to potent anti-inflammatory activity in various animal models, and to exhibit favorable separation of local anti-inflammatory activity from adverse systemic effects in both animals and humans. After oral administration, [3H]tipredane was rapidly absorbed, metabolized, and excreted into urine and feces. Metabolism of tipredane was rapid and complex, with significant species differences, although the disposition in rhesus and cynomolgus monkeys seemed to be similar to humans. Tipredane had been investigated as the therapeutic agent for the treatment of allergic rhinitis, asthma and skin disorders. However, this development was discontinued.
Status:
Investigational
Source:
NCT02260661: Phase 1 Interventional Completed Advanced Solid Malignancies
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AZD-8835 is a potent inhibitor of PI3Kα and PI3Kδ with selectivity versus PI3Kβ, PI3Kγ, and other kinases that preferentially inhibited growth in cells with mutant PIK3CA status, such as in estrogen receptor-positive (ER(+)) breast cancer cell lines BT474, MCF7, and T47D (sub-umol/L GI50s). Consistent with this, AZD-8835 demonstrated antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously. AZD-8835 is a selective, oral inhibitor of PI3K isoforms α and δ with the following activity in enzymatic assays: PI3K α – IC50 = 6nM (equipotent vs wt and E545K / H1047R mutants); PI3K δ – IC50 = 6nM; PI3K γ – IC50 = 90nM; PI3K β – IC50 = 431nM. Inhibition of signalling in cells (pAKT endpoint): PI3K α – IC50 = 57nM; PI3K δ – IC50 = 49nM; PI3K β – IC50 = 3.6uM; PI3K γ - IC50 = 532nM. AZD-8835 is in phase I clinical studies by AstraZeneca for the treatment of advanced solid tumors and ER+ and HER-2 negative breast cancer.
Status:
Investigational
Source:
NCT00784875: Phase 2 Interventional Completed Primary Insomnia
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:dimesone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dimesone is a synthetic glucocorticoid with anti-inflammatory and anti-allergic activity.