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Restrict the search for
vitamin a
to a specific field?
Status:
Investigational
Source:
JAN:CILOSTAMIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Cilostamide (also known as OPC 3689) is a selective inhibitor of type III phosphodiesterases: PDE3A and PDE3B, which inhibits thrombin-induced platelet aggregation. Elevating intracellular cAMP has been shown to inhibit platelet function. cAMP interferes with platelet-activating signals, which leads to aggregation inhibition, but the precise mechanism is unclear. It is known, that inhibition of Akt phosphorylation leads to inhibition of phosphorylation of glycogen synthase kinase 3-beta (GSK-3beta), which is an effector of Akt. However, cAMP-elevating agents’ stimulated GSK-3beta phosphorylation at Ser9. The cAMP-elevating agent cilostamide did not directly affect the enzyme activity of PI3-kinase, and thus it has two effects on PI3K signaling: inhibition of Akt phosphorylation independent of PKA. And stimulation of GSK-3beta phosphorylation dependent on PKA.
Status:
Investigational
Source:
INN:ciheptolane [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Ciheptolane is spirodibenzocycloalkanedioxalane derivative with analgesic, sedative, antihistaminic, antiserotonic, antiinflammatory, anticonvulsant, and antidepressant activity.
Status:
Investigational
Source:
NCT01428453: Phase 2 Interventional Completed Alzheimer's Disease
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Rilapladib (SB659032) is a potent and selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Inhibition of Lp-PLA2 can reduce peripheral measures of inflammation. Rilapladib has been evaluated for treatment in Alzheimer’s disease and atherosclerosis. Initial results from clinical trials in Alzheimer patients suggests that oral administration of rilapladib may slow down the progression of Alzheimer’s disease. Initial evidence has also been found that inhibition of Lp-PLA2 may attenuate intimal macrophage accumulation and consequently stabilize atherosclerotic plaque.
Status:
Investigational
Source:
INN:bentamapimod [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Bentamapimod (AS602801) a newly developed, orally-active, ATP competitive inhibitor of JNK, which is in phase IIa clinical trials for the treatment of endometriosis. Bentamapimod showed selective cytotoxic activity against serum-cultured cancer cells and cancer stem cells in vitro. It blocks T-cell proliferation and induces apoptosis. Bentamapimod was discovered by Merck Serono. Then PregLem (a member of the Richter Group) acquired worldwide rights in 2010.
Status:
Investigational
Source:
NCT00116376: Phase 1/Phase 2 Interventional Completed Glioblastoma Multiforme
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
AEE-788 is an orally available anticancer agent that was being developed by Novartis. AEE-788 is a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. At the enzyme level, AEE-788 inhibited EGFR and VEGF receptor tyrosine kinases in the nm range (IC(50)s: EGFR 2 nm, ErbB2 6 nm, KDR 77 nm, and Flt-1 59 nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited (IC(50)s: 11 and 220 nm, respectively). AEE-788 demonstrated antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibited the proliferation of epidermal growth factor- and VEGF-stimulated human umbilical vein endothelial cells. These properties, combined with a favorable pharmacokinetic profile, were associated with a potent antitumor activity in a number of animal models of cancer, including tumors that overexpress EGFR and or ErbB2. Oral administration of AEE-788 to tumor-bearing mice resulted in high and persistent compound levels in tumor tissue. Moreover, AEE-788 efficiently inhibited growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h, a phenomenon correlating with the antitumor efficacy of intermittent treatment schedules. AEE-788 has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters. AEE-788 had been in phase Ⅱ clinical trials by Novartis for the treatment of glioblastoma multiforme. However, this research has been discontinued.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tiametonium (also known as Thiamethon) is a lanthionamine derivative with ganglionic blocking activity. In preclinical models, Thiamethon prevents nicotine-induced convulsions in mice.
Status:
Investigational
Source:
NCT00502710: Phase 2 Interventional Completed Diabetes Mellitus Type 2
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Carmegliptin is a potent, long-acting, selective, orally bioavailable, pyrrolidinone-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. ). DPP-IV is a proline-specific serine protease enzyme that is known to rapidly inactivate two incretin hormones released during food ingestion, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Incretins are essential for regulating both fasting and postprandial plasma glucose by stimulating insulin secretion, supporting β-cell mass, and inhibiting glucagon production by the α-cells to reduce glucose production by the liver. By selectively inhibiting DPP-IV, carmegliptin prolongs the activity of circulating GLP-1 and GIP and improves their potential to prolong the antidiabetic actions. Carmegliptin is indicated for use as monotherapy or in combination with other oral antihyperglycemic agents for the treatment of Type 2 diabetes.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Metrenperone, a 5-hydroxytryptamine blocker, is used in veterinary as an antimyopathic agent. Experiments on rabbits have shown that the drug had positive effects on collagen turnover, remodeling, and organization during acute inflammation and fibroplasia.
Status:
Investigational
Source:
INN:broxitalamic acid [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Broxitalamic acid is tribromobenzoic acid derivative used as x-ray contrast medium
Status:
Investigational
Source:
INN:phenadoxone [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Phenadoxone hydrochloride is one of some forty amino-ketones and amino-esters related to amidone. The compound is a very potent analgesic for the rat; by the subcutaneous route it is more active than either morphine or amidone. In spite of this its acute toxicity to mice is lower than that of amidone and its therapeutic index is therefore correspondingly higher, giving a wider margin of safety. Side effects in dogs, such as narcosis, sedation, and general depression, were much less with phenadoxone than with amidone or morphine. Nausea and vomiting did not occur after phenadoxone in non-tolerant dogs. Clinical results show that for relieving certain types of pain in human subjects it is a potent analgesic that compares favorably with morphine and amidone. At therapeutic dose levels undesirable pharmacological effects, such as cardiac depression and vasomotor disturbance, are absent, and it is only at extremely high dose levels that untoward effects occur. However, the drug has a strong respiratory depressant action when given in high doses; it should be used with special caution if injected intravenously.
