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

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Showing 151 - 160 of 1136 results

AZD8055 is a new ATP-competitive mTOR kinase inhibitor that was developed to overcome the limitations of the first generation of allosteric mTORC1 inhibitors (rapamycin and its analogs) as anticancer agents. AZD8055 potently and selectively inhibits mTOR by directly targeting its catalytic site, which results in the blockade of the activity of both mTORC1 and mTORC2 complexes. It displays antitumoral activity by inhibiting proliferation and/or inducing cell death in various cancer cell models, including ovarian clear cell carcinoma.
Status:
Investigational
Source:
INN:pomaglumetad methionil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

LY404039 [(-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid] is an agonist of orthosteric metabotropic glutamate receptor (mGluR)2/3. In addition, it acts as an agonist at dopamine D2 receptors. LY404039 demonstrated broad antipsychotic and anxiolytic efficacy across multiple animal models. LY-2140023 is a methionine amide prodrug of LY-404039 being developed by Eli Lilly & Co for the potential oral treatment of schizophrenia.
Status:
Investigational
Source:
NCT00103246: Phase 1 Interventional Completed Lymphoma
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Balicatib is a potent cathepsine K inhibitor that was developed for the treatment of knee osteoarthritis. The development of Balicatib was terminated in phase II due to the occurrence of skin rashes and rarer incidences of morphea-like skin changes.
Orvepitant is a novel generation brain penetrant, selective and potent, small molecule NK-1 receptor antagonist. Orvepitant’s (GW823296) mode of action and developability characteristics made it a suitable development candidate for the treatment of common anxiety disorders, posttraumatic stress disorder and major depressive disorder. It’s in phase II clinical trials as an effective inhibitor of itch-associated response.
Status:
Investigational
Source:
NCT02764385: Not Applicable Interventional Completed Smoking
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (ACHIRAL)


Clonitazene is a synthetic opioid analgesic, structurally related to etonitazene. In the USA clonitazene is a schedule I narcotic controlled substance.
Status:
Investigational
Source:
INN:piclozotan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Piclozotan (SUN N4057) is a 1,4-benzoxazepine derivative that exhibits sub-nanomolar affinity at serotonin 1A receptor with good selectivity over dopamine D2 and α1-adrenoceptors. Piclozotan reduced levodopa-induced forelimb hyperkinesia by 55% and 69%, respectively, at 1h relative to the control. Piclozotan significantly lengthened the duration of rotational behavior by 26% versus the control and attenuated the increase in striatal levodopa-derived extracellular dopamine levels. Piclozotan, a serotonin 1A agonist, can improve motor complications in patients with advanced Parkinson's disease. Piclozotan has been shown to be neuroprotective against ischemic neuronal damage in animal models. Piclozotan had been in phase II for the treatment of stroke. However, this research has been discontinued.
Status:
Investigational
Source:
NCT03194620: Not Applicable Interventional Completed Healthy
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

(-)-Epigallocatechin is a polyphenol, which occurs naturally in various plants, including green tea leaves. The compound was shown to have anti-cancer activity in vitro, with breast cancer, lung cancer, and colon cancer cells. The commercial preparation of Polyphenon E contains about 3% (-)-epigallocatechin as an impurity.
Status:
Investigational
Source:
INN:dichloroxylenol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dichloroxylenol is a bactericide, preservative and deodorant. It is often used in the preparation of antiseptic and deodorant lotions and bath preparations. Dichloroxylenol also showed slightly greater activity against S. aureus Oxoid 701/1 Lot 610254 than against Escherichia coli and Salmonella typhi, indicating a probable role for cell wall in the susceptibility of bacteria to dichloroxylenol. The efficacy of either povidone-iodine (Betadine) or dichloroxylenol (Septocid) intrauterine infusions on the treatment of endometritis and/or cervicitis in cows was examined. The recovery and conception rates obtained after Betadine treatment were better than those obtained after Septocid. Moreover, healthy cows and those inseminated before post-partum day 180, having no more than 4-7 previous services, responded well to either Betadine or Septocid treatment.