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Restrict the search for
m ulipristal acetate
to a specific field?
Status:
Investigational
Source:
NCT00623363: Phase 2 Interventional Completed Parkinson's Disease
(2007)
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:
Class (Stereo):
CHEMICAL (ACHIRAL)
Hydroxypethidine, an opioid analgesic is an opioid receptor agonist. Hydroxypethidine is under the control of narcotic drugs according to US Single Convention 1961.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Estrofurate (AY-11483) is an impeded estrogen. it prevents ovulation and implantation.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Acetorphine is a synthetic narcotic analgesic. Acetorphine was reported to have uses in veterinary medicine with pronounced advantages in the immobilization of the giraffe in which toxic effects were reduced as compared to the effects of etorphine. In July 1966, the Director-General of the World Health Organization informed the Secretary-General that WHO had arrived at the conclusion that etorphine and acetorphine should be included in Schedule I of the Convention, since they could give rise to similar abuse, and produce similar ill effects as the substances already listed therein. Acetorphine is a Schedule I controlled substance in the United States.
Status:
Investigational
Source:
NCT01128335: Phase 2 Interventional Completed Liver Transplantation
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Sotrastaurin, an orally-active, first-in-class immunomodulator, is under development by Novartis for the treatment of uveal melanoma and diffuse-large B-cell lymphoma. Sotrastaurin is a low molecular mass synthetic compound
that potently inhibits the PKC α, β and the θ isoforms
resulting in selective NF-κB inactivation. Sotrastaurin is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM in a cell-free assay. Inhibition of PKC beta in B-cells results in prevention of NF-kB-mediated signaling and down regulation of NF-kB target genes. This may eventually lead to an induction of G1 cell cycle arrest and tumor cell apoptosis in susceptible tumor cells. This agent may act synergistically with other chemotherapeutic agents. PKC, a family of serine/threonine protein kinases overexpressed in certain types of cancer cells, is involved in cell differentiation, mitogenesis, inflammation, and the activation and survival of lymphocytes. Sotrastaurin is currently in phase II trials by Novartis for the treatment of large B-cell lymphoma and uveal melanoma. Sotrastaurin was in Phase II of clinical development for the prevention of acute rejection after solid organ transplantation and psoriasis, but this reseach had being discontinued.
Status:
Investigational
Source:
NCT00504790: Phase 1 Interventional Completed Cancer
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
GSK-923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E), and the third novel drug candidate to arise from Cytokinetics' broad strategic alliance with GlaxoSmithKline (GSK). GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors. GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. GSK-923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of CENP-E to microtubules is insufficient to satisfy the mitotic checkpoint. Consistent with genetic studies in mice suggesting that decreased CENP-E function can have a tumor-suppressive effect, inhibition of CENP-E induced tumor cell apoptosis and tumor regression.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Froxiprost (ONO-995), a synthetic analog of dinoprost, is a prostanoid receptor agonist. Froxiprost is active in contracting the uterine smooth muscle and is used as a pharmacological tool.
Status:
Investigational
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:
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:
NCT00427856: Phase 2 Interventional Completed Lymphoma, Follicular
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
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.
