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Restrict the search for
vitamin a
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Status:
Investigational
Source:
NCT03447951: Phase 2 Interventional Recruiting Hepatocellular Carcinoma
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
p-Toluene sulfonamide was used to prepare the precursor required for synthesis of ethyl 6-phenyl-1-tosyl-1,2,5,6-tetrahydropyridine-3-carboxylate. It acts as a derivative of ammonia activated to alkylation by alkyl halides is exemplified by the synthesis of N-tosyl-2,3-dihydroisoindole from o-xylylene dibromide. It is a precursor of N-tosyl imines. Hybrid compounds of tacrine and p-toluenesulfonamide are effective inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with the preferential inhibition of BChE. p-Toluenesulfonamide has been employed as nucleophile during tetrabutylammonium fluoride (TBAF) catalyzed vinyl aziridine opening reaction and as a reagent during selective aziridination of olefins catalyzed by dirhodium (II) caprolactamate.
Status:
Investigational
Source:
NCT00400283: Phase 1 Interventional Completed Diabetes
(2001)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tifenazoxide is a thiadiazine derivative patented by Novo Nordisk A/S as the opener of the KATP-regulated potassium channels useful in the treatment of the endocrine system diseases. Tifenazoxide is a selective opener of the beta-cell type (SUR1 / Kir6.2) KATP channel that characterized as competitive inhibitors of glibenclamide binding to membranes of HEK293 cells expressing human SUR1/Kir6.2and as potent inhibitors of insulin release in isolated rat islets. In clinical trials, Tifenazoxide administration leads to a decrease in insulin concentrations 1 h post-dose. This was accompanied by an increase in glucose and growth hormone concentrations (NS), but not of glucagon. During the OGTT a dose-dependent reduction in the 2 h glucose value was observed.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Nicodicodine is a cough suppressant and analgesic. It was first synthesized in 1904. It is a Schedule III drug. Nicodicodine is metabolised in the liver to dihydromorphine. Since the final active metabolite is the slightly stronger opiate than morphine, nicodicodine can be expected to be more potent and longer acting than nicocodeine.
Status:
Investigational
Source:
NCT01692197: Phase 2 Interventional Completed Leukemia
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Indisulam (also known as E7070) is a sulfonamide derivative patented by Japanese pharmaceutical company Eisai Co. as antitumor agent. Indisulam inhibits cyclin-dependent kinases (CDK), which regulate cell cycle progression and are usually over-expressed in cancerous cells. Inhibition of CDK results in G1/S phase arrest of the cell cycle, and may lead to induction of apoptosis and inhibition of tumor cell proliferation. Preclinical and clinical studies have established the synergy of indisulam with nucleoside analogs as well as topoisomerase inhibitors. These combinations were tolerated with acceptable toxicities, including diarrhea, vomiting, and myelosuppression. In Phase II clinical trials Combination of indisulam with DNA‐damaging agent (idarubicin) and nucleoside analog (cytarabine) in patients with relapsed and refractory AML is effective and largely well tolerated.
Status:
Investigational
Source:
NCT00005093: Phase 3 Interventional Completed Lung Cancer
(1999)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
A second generation of HDACs, synthetic benzamide-containing HDACs such as Tacedinaline (CI-994), have reached phase I and II clinical trials. It has been investigated for its applications to the treatment of cancers such as Breast cancer and Colorectal cancer. Tacedinaline has been in phase III clinical trials by Pfizer for the treatment of advanced non-small cell lung cancer and pancreatic cancer combined with gemcitabine. However, this research has been discontinued. Mechanism of Action: Angiogenesis inhibitors; Histone deacetylase inhibitors. Pharmacokinetics showed that CI-994 absorption and disposition were unaffected by carboplatin and paclitaxel coadministration.
Status:
Investigational
Source:
NCT00640523: Phase 2 Interventional Completed Chronic Lymphocytic Leukemia (CLL)
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Forodesine hydrochloride is the salt of the synthetic high-affinity transition-state analog forodesine (BCX-1777, immucillin-H), a substrate designed to mimic the properties or the geometry of the transition state of reaction. It is an anticancer drug that has been developed for the treatment of different hematologic malignancies. In December 2006, orphan designation (EU/3/06/421) was granted by the European Commission to Napp Pharmaceuticals Research Limited, United Kingdom, for forodesine hydrochloride for the treatment of acute lymphoblastic leukemia. Forodesine hydrochloride has been evaluated in Phase I/Phase II clinical trials for several cancer types including chronic lymphocytic leukemia (CLL), B-Cell acute lymphoblastic leukemia and refractory cutaneous T-cell lymphoma (CTCL). Forodesine is a potent purine nucleoside phosphorylase (PNP) inhibitor that acts by elevating plasma 2'-deoxyguanosine (dGuo) and intracellular deoxyguanosine triphosphate, which in turn affects deoxynucleotide-triphosphate pools and induces cell death by apoptosis. Forodesine in the presence of dGuo inhibited the proliferation of CEM-SS (T-acute lymphoblastic leukemia) cells with an IC50 of 0.015 uM. This inhibition by forodesine and dGuo was accompanied by a 154-fold and 8-fold elevation of endogenous dGuo triphosphate (dGTP) and deoxyadenosine triphosphate (dATP) pools, respectively. Cytotoxic activity of forodesine in the presence of dGuo was selective to T lymphocytes. It is a 10- to 100-fold more potent inhibitor of human lymphocyte proliferation than other known PNP inhibitors such as PD141955 and BCX-34.8
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Atiprosin (AY-28,228), an octahydro-pyrazino-pyrido-indole drug, possesses the alpha-adrenoceptor antagonist activity and exerts antihypertensive effects. Atiprosin has never been marketed
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ataprost (also known as ONO-41483; OP-41483), an epoprostenol agonist, participated in phase II clinical trials in Japan for the treatment patients with heart failure and myocardial ischemia. However, these trials were discontinued.
Status:
Investigational
Source:
NCT01100684: Phase 3 Interventional Completed Diarrhea Predominant Irritable Bowel Syndrome
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Asimadoline is an orally active, highly selective kappa-opioid receptor agonist with approximately 500-fold greater affinity for human kappa-, as compared with either delta- or mu-opioid receptors. Due to its high selectivity for the kappa-opioid receptor, asimadoline does not produce mu-opioid like side effects. It is investigated for use/treatment in irritable bowel syndrome, pruritus, postoperative ileus. A drug interaction study investigating the coadministration of asimadoline with ketoconazole was performed in healthy volunteers - a two to three-fold increase in AUC and Cmax of asimadoline was observed with concomitant administration of ketoconazole. The most common adverse events are diarrhea, nausea, sinusitis, headache and fatigue.
Class (Stereo):
CHEMICAL (ACHIRAL)
Acetryptine is an antihypertensive agent. Acetryptine was found to bind 5-HT1A and 5-HT1D receptors with high affinity. It may also act as a monoamine oxidase inhibitor (MAOI), specifically, as an inhibitor of MAO-A.
