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Restrict the search for
l-glutamine
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Class (Stereo):
CHEMICAL (ACHIRAL)
Pyridarone is a 2-Pyridylbenzofuran derivative patented by Societe Belge de l'Azote et des Produits Chimiques du Marly S.A. as anxiolytic useful for the treatment of fear in emotions of psychogenic origin.
Class (Stereo):
CHEMICAL (RACEMIC)
Serfibrate, a clofibrate derivative, is a peroxisome proliferator activated receptor-α (PPAR-α) agonist. It is a hypolipidemic agent.
Status:
Investigational
Source:
NCT02204397: Phase 2 Interventional Completed Type 1 Diabetes Mellitus
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT00413686: Phase 1 Interventional Completed Solid Tumors
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
AstraZeneca was developing AZD-7762 for the treatment of solid tumours. AZD-7762 is a potent inhibitor of Chk1 that binds in the ATP binding pocket (IC50 of 5nM; Ki of 3.6nM). AZD-7762 has activity on a range of other kinases {examples with a < 5 fold selectivity included Rous sarcoma oncogene cellular homolog (SRC) family members (e.g., Fgr, Fyn, lymphocyte-specific protein-tyrosine kinase [Lck], and Lyn, but not SRC), Flt1/3, colony stimulating factor receptor (CSF1R), RET, Abelson tyrosine kinase (Abl), and checkpoint kinase 2 (Chk2)}. It is not known if these in vitro kinase inhibitions translate into an effect in vivo. In combination with DNA-damaging agents (gemcitabine, topotecan, doxorubicin, and cisplatin), AZD-7762 inhibits tumour cell growth in vitro with a mode of action that correlates with Chk1 inhibition and abrogation of the Gap 2 (G2) and S phase checkpoints. Rightward shifts in 50% growth inhibition (GI50) values over DNA-damaging agents alone ranged from 5- to 20-fold with gemcitabine demonstrating the largest shifts followed by topotecan. In combination with radiation, AZD-7762 enhances tumour cell growth inhibition and death with survival enhancement ratios ranging from 1.7 to 1.9. Triple combinations with AZD-7762, gemcitabine, and radiation yield the largest survival enhancement ratios. AZD-7762 had been in phase I clinical trials by AstraZeneca for the treatment of solid tumors. However, this study was terminated for the safety reason in 2011.
Class (Stereo):
CHEMICAL (ACHIRAL)
Etabenzarone is an anti-inflammatory and anticoagulant agent.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Ragaglitazar (DRF 2725, NNC 61-0029) is phenoxazine analog of phenyl propanoic acid having dual (PPARα and PPARγ) agonist property intended to restore insulin sensitivity and correct diabetic dyslipidemia. PPAR-α is highly expressed in liver and muscle and upon activation leads to decreases in plasma triglycerides and increases in HDL cholesterol levels. PPAR-γ activation leads to enhancement of glucose uptake in skeletal muscles and adipose tissue. Ragaglitazar provided the glycemic control that was comparable with that of pioglitazone and, compared with placebo, provided a significant improvement in the lipid profile.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Nemorubicin, a doxorubicin derivative, is a DNA-intercalator, topoisomerase and RNA synthesis inhibitor that was undergoing development with Nerviano Medical Sciences (Nerviano MS; formerly Pharmacia Italia) for the treatment of solid tumours, specifically, the loco-regional treatment of primary liver tumours (hepatocellular carcinoma). The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway, where current therapies fail.
Nemorubicin is biotransformed in the liver into cytotoxic metabolites that may further contribute to render this drug highly active against primary liver tumors or liver metastases. Clinical trials were conducted in Europe, US and China with Nemorubicin given at different dose-schedules and by different routes of administration: as single agent by systemic IV route, oral route and by intra-hepatic artery (IHA) infusion alone or in combination with cisplatin.
Status:
Investigational
Source:
NCT00044421: Phase 3 Interventional Completed Diabetic Neuropathies
(2002)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Ruboxistaurin is an orally bioavailable, selective, potent inhibitor of protein kinase C β developed for treating diabetic retinopathy. In vitro and in vivo non-clinical models have demonstrated that Ruboxistaurin decreases PKC β activity and ameliorates many of the effects of PKC β on pathologic processes in the retina. Ruboxistaurin prevents the slowing of retinal blood flow that is observed by fluorescein video angiography in the eyes of diabetic rats. It is also reported to cause regression of retinal neovascularization produced by laser-induced major branch vein occlusions in a porcine model. Ruboxistaurin positively affected the diabetes-induced retinal blood flow abnormalities in a Phase Ib study in diabetic patients. Ruboxistaurin is in phase III clinical trials for the treatment of diabetic nephropathy and diabetic macular edema. Eli Lilly had submitted Ruboxistaurin for approval in the US and the EU; however, the company subsequently discontinued development as it was unable to demonstrate sufficient efficacy
Status:
Investigational
Source:
NCT00233909: Phase 1/Phase 2 Interventional Completed Leukemia, Myeloid
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Zosuquidar (LY-335979) is an experimental antineoplastic drug. It is is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Zosuqidar was initially characterized by Syntex Corporation, which was acquired by Roche in 1990. Roche licensed the drug to Eli Lilly in 1997. It was granted orphan drug status by the FDA in 2006 for AML. Zosuquidar Trihydrochloride had been in phase III clinical trials by Kanisa Pharmaceuticals for the treatment of acute myeloid leukaemia. However, this research has been discontinued.
Status:
Investigational
Source:
Peptides. Oct 2012;37(2):194-9.: Not Applicable Veterinary clinical trial Completed N/A
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bombesin (BN), a neuropeptide that originally was purified from the skin of the European frog (Bombina bombina). It has many biological effects including hormone release, stimulation of pancreatic enzyme secretion, gallbladder contraction and bronchoconstriction. Bombesin is a highly specific marker of neuroendocrine differentiation and thus a valuable tumor marker. It activates three different G-protein-coupled receptors known as BBR1, -2, and -3.
