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

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Showing 991 - 1000 of 10251 results

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

Class (Stereo):
CHEMICAL (UNKNOWN)

Canbisol is dihydroxyhexahydrodibenzo(b,d)pyran derivative patented by pharmaceutical company Eli Lilly and Co. as antihypertensive agent. At the dosages studied, Canbisol reduced food consumption by rats.
Status:
Investigational
Source:
INN:pemedolac
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dexpemedolac is long-acting non-narcotic analgesic. Dexpemedolac exhibited potent analgesic effects against chemically induced pain in rats and mice and against inflammatory pain in rats. Dexpemedolac differed from standard nonsteroidal anti-inflammatory drugs (NSAIDs) in that the doses, which produced analgesia were much lower than those required for either anti-inflammatory or gastric irritant effects. The common to the NCAIDs class actions are antipyresis and inhibitory effects on platelet aggregation. In yeast-induced hyperthermic rats, dexpemedolac exhibited antipyretic actions, whereas the drug did not affect body temperature in normothermic animals. Aggregation of human platelets was inhibited by high concentrations of dexpemedolac.
Status:
Investigational
Source:
INN:parapropamol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

There is no much information related to the pharmacological and/or biological properties of parapropamol. However, the analgesic properties of this compound had been studied in dentistry.
Status:
Investigational
Source:
INN:quilostigmine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Quilostigmine (also known as NXX-066) is an isoquinolinecarboxylate patented by Hoechst-Roussel Pharmaceuticals Inc as a memory enhancer. Quilostigmine acts as acetylcholinesterase inhibitor and studies as a potential drug for treating Alzheimer’s disease. Quilostigmine is well absorbed from the gastrointestinal tract, but the oral bioavailability poor to moderate in rats and dogs because of pre-systemic metabolism. In preclinical studies has demonstrated activity in animal models of memory function. In clinical trials, Quilostigmine was well tolerated in healthy subjects up to a single dose of 64 mg and multiple doses of 60 mg QD for seven days
Status:
Investigational
Source:
INN:properidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Properidine is an isopropyl analog of pethidine that acts as opioid analgesic.
Status:
Investigational
Source:
NCT00304525: Phase 1/Phase 2 Interventional Completed Metastatic Melanoma
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


CHIR-265 (RAF265) is a potent selective orally active small molecule Raf-kinase inhibitor with anti‐angiogenic activity through inhibition of vascular endothelial growth factor type 2 (VEGFR‐2) in preclinical models. CHIR-265 effectively block phosphorylation of Raf's downstream substrates MEK and ERK in cells and also kill melanoma and colorectal cancer cell lines harboring B-Raf mutations independent of PTEN mutation status. Raf kinase inhibition by CHIR-265 in mutant B-Raf melanoma cell lines causes cell cycle arrest and induces apoptosis, mimicking the effect of Raf RNAi in these cells. CHIR-265 also potently inhibits the phosphorylation of VEGFR2 and proliferation of VEGF-stimulated hMVEC.
Status:
Investigational
Source:
INN:phenampromide [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Phenampromide is an opioid analgesic, which is considered to be structurally similar to isomethadone. Phenampromide belongs to the ampromide family of drugs, which also include propiram and diampromide. According to the literature, (R)-phenampromide has greater analgesic potency than its (S)-enantiomer. Synthetic narcotic analgesic phenampromide is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.
Status:
Investigational
Source:
NCT00332202: Phase 3 Interventional Completed Non Hodgkin Lymphoma
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Enzastaurin is a serine/threonine kinase inhibitor that showed antiangiogenic, antiproliferative, and proapoptotic properties in vitro and antitumor activity in vivo in a xenograft Waldenström macroglobulinemia (WM) model. Enzastaurin (LY317615) is a potent PKCβ selective inhibitor. Enzastaurin suppresses angiogenesis and was advanced for clinical development based upon this antiangiogenic activity. Enzastaurin suppresses tumor growth through multiple mechanisms: direct suppression of tumor cell proliferation and the induction of tumor cell death coupled to the indirect effect of suppressing tumor-induced angiogenesis. Enzastaurin is an orally administered drug that was intended for the treatment of solid and haematological cancers. Enzastaurin had shown encouraging preclinical results for the prevention of angiogenesis, inhibition of proliferation and induction of apoptosis as well as showing limited cytotoxicity within phase I clinical trials. However, during its assessment in phase II and III clinical trials the efficacy of enzastaurin was poor both in combination with other drugs and as a single agent. Eli Lilly discontinued development of enzastaurin after top-line data from the double-blind, international Phase III PRELUDE trial in 758 DLBCL patients showed that enzastaurin missed the primary endpoint of improving DFS vs. placebo.
Status:
Investigational
Source:
INN:metoxepin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Metoxepin was developed as an antiemetic, neuroleptic and antihistamine agent. This drug has never been marketed.
Status:
Investigational
Source:
INN:mezepine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Mezepine is an antidepressive agent, that has never been marketed.