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

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Showing 6241 - 6250 of 167129 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Proxifezone is a mixture of phenylbutazone and d-propoxyphene patented by Societe d'Etudes de Recherches et d'Applications Scientifiques et Medicales E.R.A.S.M.E. as an anti-inflammation pharmaceutical composition with potent analgesic activity. Anti-inflammatory effects of Proxifezone associated with Phenylbutazone, that acts as a nonsteroidal anti-inflammatory drug (NSAID). D-propoxyphene acts as an opioid analgesic, that provides strong pain relief.
Status:
Investigational
Source:
INN:fenleuton [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

FENLEUTON is a potent, reversible and selective inhibitor of 5-lipoxygenase with IC50 values ranging from 80 to 1100 nM. It was studied for potential use in veterinary medicine to treat chronic obstructive pulmonary disease in horses.
Status:
Investigational
Source:
USAN:CARBON MONOXIDE C 11 [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Carbon Monoxide C-11 is a colorless, odorless, and tasteless flammable radiolabeled gas patented by Glaxo Group Limited as imaging agent
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.
Status:
Investigational
Source:
INN:lubazodone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Lubazodone (YM 992) or (S)-2-[[(7-fluoro-4-indanyl)oxy]methyl]morpholine monohydrochloride, exhibited the biochemical profile of a selective serotonin (5-HT) reuptake inhibitor (SSRI) with 5-HT2A receptor antagonistic activity. It has been studied in the treatment of depression.
Status:
Investigational
Source:
INN:trimeperidine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Trimeperidine (promedol) is the earliest and mostly studied opioid analgesic. Trimeperidine stimulates opioid receptors in the central nervous system. Compared with morphine, it has a weaker and shorter analgesic effect, less affects the respiratory, vomiting and vagal centers, does not cause smooth muscle spasm (except for the myometrium), and has a moderate antispasmodic and hypnotic effect. It is used to treat severe pain syndrome, acute left ventricular failure, pulmonary edema, cardiogenic shock, preparation for surgery, childbirth, high fever, post-transfusion complications, poisoning with atropine, barbiturates, barium, gasoline, boric acid, strong acids, carbon monoxide, turpentine, formalin, formalin. It has several side effects. Administration of this substance is associated with the development of life-threatening conditions accompanied by the suppression of respiration center. Analgesic trimeperidine (promedol) was included into the health care kits by various Ministries of the Russian Federation at different times.
Status:
Investigational
Source:
INN:picumeterol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.
Status:
Investigational
Source:
INN:climiqualine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Climiqualine is a compound developed by Hoersht AG and claimed to possess hypolipemic and hypoglycemic activities in rats and rabbits.
Status:
Investigational
Source:
NCT00372957: Phase 2 Interventional Completed Diabetes Mellitus, Type 2
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Denagliptin is a dipeptidyl peptidase IV (DPP-IV) and and tripeptidyl-peptidase inhibitor, which entered phase III clinical trials in 2006 for the treatment of type 2 diabetes mellitus at GlaxoSmithKline. Development of this compound was put on hold due to unfavorable preliminary data from preclinical long-term toxicity trials. Stress testing or forced degradation studies of denagliptin revealed that drug was stable in the solid-state, but degraded in solution, in blends with all excipients, and in capsules predominantly by cyclization to (3S,7S,8aS) amidine, which epimerized to (3S,7S,8aR) amidine.
Status:
Investigational
Source:
NCT00427856: Phase 2 Interventional Completed Lymphoma, Follicular
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Obatoclax (GX15-070) is a novel BH3 mimetic pan Bcl- 2 inhibitor. The clinically studied formulation is as obatoclax mesylate (Box 1), a salt. It is only under study as an intravenous preparation. It functions to block BH3-mediated binding of Bcl-2, Bcl-XL, Mcl-1 and A1 to Bax and Bak. Bax and Bak thus are unopposed and able to dimerize to allow initiation of intrinsic apoptosis. Preclinically, obatoclax has been shown to reverse inhibition of Bax or Bak by Bcl-2, Bcl-XL, Bcl-w and Mcl-1. Obatoclax was discovered by Gemin X, which was acquired by Cephalon, which has since been acquired by Teva Pharmaceuticals. Obatoclax had been in phase III clinical trials by Gemin X Biotechnologies (subsidiary of Teva) for the treatment of non-small lung cancer (NSCLC). The compound received orphan drug designation in the U.S. in 2004 for the treatment of chronic lymphocytic leukemia (CLL). However, Teva discontinued the development of obatoclax in 2013.

Showing 6241 - 6250 of 167129 results