U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 1851 - 1860 of 132111 results

Status:
Investigational
Source:
INN:flurocitabine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flurocitabine is an anti-metabolite that was developed by Hoffmann-La Roche for the treatment of cancer. The drug is metabolized to 2 biologically active substances, AFC (1-beta-D-arabinofuranosyl-5-fluorocytosine) and AFU (arabinofuranosyl-5-fluorouracil). Flurocitabine was tested against stomach cancer, pancreatic cancer, small cell lung cancer and AML, however, the development was terminated in the early phases.
Status:
Investigational
Source:
INN:fluprofen
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Fluprofen was invented as an analgesic and anti-inflammatory agent. However, information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:emlenoflast [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:pipequaline [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pipequaline (PK-8165, 2-phenyl-4[2-(4-piperidinyl) ethyl]quinoline) is a benzodiazepine receptor partial agonist.
Status:
Investigational
Source:
INN:perflisobutane [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Perflisobutane is an anesthetic agent.
Gomisin A (BESIGOMSIN/GA) one of the major dibenzocyclooctadiene lignans isolated from Schisandra chinensis Baill, has proved to possess a variety of pharmacological effects. It has been found to promote hepatocyte growth factor, limit lipid peroxidation, and inhibit apoptosis in acute hepatic injury animal models. Besigomsine also acts as an anti-inflammatory by preventing the release of arachidonic acid in macrophages in vitro. Laboratory evidence suggests that Besigomsine may have anticarcinogenic effects. Chronic administration of Gomisin A had an antihypertensive effect in AngII-induced hypertensive mice. Gomisin A may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. Also it induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway.
Status:
Investigational
Source:
INN:evobrutinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Evobrutinib is a highly selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK). It potently inhibits BCR- and Fc receptor-mediated signaling and, thus, subsequent activation and function of B cells and innate immune cells such as monocytes and basophils. Evobrutinib demonstrated effectivity in autoimmune disease preclinical models. Evobrutinib is being developed by Merck Serono for the treatment of various autoimmune disorders.
Status:
Investigational
Source:
INN:emricasan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Emricasan (IDN- 6556 or PF-03491390) (3-[2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid) is a pan-caspase inhibitor. Testing in vitro enzyme assays demonstrated that emricasan efficiently inhibits all human caspases at low nanomolar concentrations. Preclinically, emricasan was effective in inhibiting apoptosis of sinusoidal endothelial cells. Emricasan has marked efficacy in models of liver disease after oral administration and thus, is an excellent candidate for the treatment of liver diseases characterized by excessive apoptosis. This drug is a first-in-class anti-apoptotic caspase inhibitor with demonstrated preliminary efficacy in liver-impaired patients in humans.
Status:
Investigational
Source:
INN:deutivacaftor [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

CTP-656 is a deuterium-modified form of ivacaftor, an FDA-approved drug for the treatment of cystic fibrosis. CTP-656 is jointly developed by Concert Pharmaceuticals and Vertex Pharmaceuticals, and is believed to have higher metabolic stability, lower toxic byproducts and increased half-life compared to the original. CTP-656 acts as a potentiator of is a cystic fibrosis transmembrane conductance regulator (CFTR) protein. CTP-656 is investigated in phase 2 clinical trials for the treatment of cystic fibrosis.
Status:
Investigational
Source:
INN:netobimin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Netobimin is a carbamate compound which is used as an anthelmintic drug in veterinarymedicine. Netobimin-containing products are available as liquid suspensions which are intendedfor oral administration. Products are available for sheep and cattle. An oral dose of 7.5 mg/kg bw is recommended for the treatment of gastrointestinal infestations of roundworms and tapeworms;and 20 mg/kg bw is recommended for type II ostertagiasis and adult flukes. In order to be pharmacologically active, netobimin needs to be converted to the broad spectrumanthelmintic drug albendazole, by the splitting off of a side-chain and the formation of abenzimidazole group. This occurs naturally in the ruminant gut.

Showing 1851 - 1860 of 132111 results