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Showing 141 - 150 of 2667 results

Status:
Investigational
Source:
INN:vincofos
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Vincofos is a broad-spectrum canine anthelmintic. All or nearly all of the ascarids, hookworms, whipworms, and the tapeworm, Taenia pisiformis, were expelled following therapy with vincofos. The tapeworm, Dipylidium caninum, was also effectively removed by the vincofos treatment, but it appeared that a slightly greater dosage would be required to obtain maximum anthelmintic effect.
Status:
Investigational
Source:
INN:megalomicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Megalomicin is a Micromonospora-produced macrolide antibiotic complex. Megalomicin A component was studied most extensively. It inhibited the ATP-dependent acidification of lysosomes and intra-Golgi transport in vitro. Megalomicin induces a powerful inhibitory effect on HIV-1 replication at nontoxic concentrations by preventing the processing of HIV-1 gp160 envelope protein and the subsequent formation of infectious viral particles.
Status:
Investigational
Source:
INN:sodium picofosfate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Picofosforic acid is the laxative.
Status:
Investigational
Source:
INN:norcodeine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Norcodeine is the N-demethylated derivative of codeine. It has relatively little opioid activity in its own right, but is formed as a metabolite of codeine following ingestion. Codeine and its other major metabolites codeine-6-glucuronide and norcodeine have weak affinity to opioid μ-receptors.
Ganetespib (formerly called STA-9090) is a novel, injectable resorcinolic triazolone small molecule inhibitor of Hsp90, developed by Synta Pharmaceuticals. Ganetespib inhibits the growth of many tumor types in vitro and in vivo including AML, ALL, CML, NHL, neuroblastoma, Ewing sarcoma, rhabdoid cancer, rhabdomyosarcoma, melanoma, and carcinomas of the breast, lung, prostate, bladder and colon7-10,14-27. Ganetespib has being studied in multiple adult oncology indications. The 50% inhibitory concentrations (IC50) for Ganetespib against malignant mast cell lines are 10-50 times lower than that for 17-AAG, indicating that triazolone class of HSP90 inhibitors likely exhibits greater potency than geldanamycin based inhibitors. Ganetespib inhibits MG63 cell lines with IC50 of 43 nM. Ganetespib binds to the ATP-binding domain at the N-terminus of Hsp90 and serves as a potent Hsp90 inhibitor by causing degradation of multiple oncogenic Hsp90 client proteins including HER2/neu, mutated EGFR, Akt, c-Kit, IGF-1R, PDGFRα, Jak1, Jak2, STAT3, STAT5, HIF-1α, CDC2 and c-Met as well as Wilms' tumor 1. Ganetespib, at low nanomolar concentrations, potently arrests cell proliferation and induces apoptosis in a wide variety of human cancer cell lines, including many receptor tyrosine kinase inhibitor- and tanespimycin-resistant cell lines. Ganetespib exhibits potent cytotoxicity in a range of solid and hematologic tumor cell lines, including those that express mutated kinases that confer resistance to small-molecule tyrosine kinase inhibitors. Ganetespib has been studied in 5 completed Synta-sponsored clinical trials (Studies 9090-02, 9090-03, 9090-04, 9090-05, and 9090-07) and 3 completed Synta-sponsored studies in normal healthy volunteers (9090-12, 9090-13, and 9090-15). Ganetespib is currently being studied in 6 Synta-sponsored clinical trials. Studies include: one Phase 1 study, three Phase 2 studies, one Phase 2b study, and one Phase 3 study. Ganetespib is also being studied in 24 Investigator Sponsored Trials (ISTs)
Status:
Investigational
Source:
INN:ristianol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ristianol (Ristianol phosphate) is a bioactive chemical that is registered as an anti-inflammatory agent and immunoregulator (in Europe), but no further information is available.
Status:
Investigational
Source:
INN:fosfosal
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fosfosal (2-phosphonoxybenzoic acid) is a O-phosphorylated derivative of salicylic acid used in analgesic and anti-inflammatory therapy. Fosfosal showed analgesic effect in the acetic acid-induced writhing and in the hot plate tests in mice, and showed antiinflammatory effect in the xylene induced mice ears swelling and in acetic acid induced increased vascular permeability tests in mice. Both the effects had no significant differences between fosfosal and aspirin, but the former had less stomach irritation.
Status:
Investigational
Source:
NCT00504790: Phase 1 Interventional Completed Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


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.
Dexfosfoserine (Phosphoserine, L-Serine-O-Phosphate, O-Phosphoserine), the most abundant phosphoamino acid in the eukaryotic phosphoproteome, is not encoded in the genetic code but synthesized posttranslationally. Dexfosfoserine is an agonist of the group III metabotropic glutamate receptors. This endogenous compound inhibits neural stem cells proliferation and promotes survival of nascent neurons thus it has potential therapeutic value in addition to its basic utility as a probe for dissecting molecular mechanisms underlying neurogenesis.
Status:
Investigational
Source:
INN:satavaptan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Sanofi-Synthélabo has developed satavaptan (previously known as SR121463) as a non-peptidic vasopressin V2 receptor antagonist for the potential treatment for cardiovascular indications such as congestive heart failure (CHF) and hypertension. The drug reached phase II for these indications before the studies were discontinued. Satavaptan was also studied for the potential treatment of glaucoma. In addition, this drug was involved in phase III clinical trials in patients with ascites due to cirrhosis of the liver and in in patients with dilutional hyponatremia. However, the further development of the satavaptan was discontinued in 2009.