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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 1161 - 1170 of 13240 results

Status:
Investigational
Source:
INN:fronepidil
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

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

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT00244322: Phase 2 Interventional Completed Alzheimer's Disease
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Semagacestat (LY-450139) was a gamma secretase inhibitor being developed as a treatment for Alzheimer's disease by Eli Lilly. It was hoped that the drug would help to delay the onset of severe Alzheimer's disease, and thereby help preserve cognitive and executive functioning and in turn improve patient quality of life. Semagacestat (LY-450139) is designed to inhibit gamma secretase, an enzyme that is involved in the cleavage of APP to beta-amyloid. By decreasing production of beta-amyloid, it is hoped that gamma secretase inhibitors will exert a disease-modifying effect in Alzheimer's disease and thus slow or halt the destruction of nerve cells – the final stage in the amyloid cascade hypothesis. In March 2008 semagacestat (LY-450139) advanced to Phase III development, where it was evaluated in the IDENTITY (Interrupting Alzheimer's Dementia by EvaluatiNg Treatment of AmyloId PaThologY) trial, the first Phase III trial for this new anti-dementia drug. In August 2010, Eli Lilly announced its decision to halt the development of Semagacestat. The decision was taken after analysing the preliminary results of the second Phase III clinical trial of the drug, which indicated that semagacestat failed to slow disease progression. The drug, in fact, worsened cognition and the ability to perform day-to-day activities.
Status:
Investigational
Source:
NCT00503360: Phase 1 Interventional Completed Ocular Hypertension
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00285025: Phase 2 Interventional Completed Alzheimer Disease
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Paliroden is an orally active drug that activates the synthesis of endogenous neurotrophins or nerve growth factors. Paliroden was investigated in phase II clinical trial in patients with Alzheimer's disease and to evaluate its effect on 18F-Dopa PET imaging in patients with Parkinson's disease. The further development of paliroden was discontinued due to its insufficient efficacy.
Status:
Investigational
Source:
INN:felipyrine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Felipyrine is a 1-aryl-2-pyrrolidinone derivative exerting anti-inflammatory activity.
Status:
Investigational
Source:
INN:bentamapimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



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)



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:
Investigational
Source:
INN:cortisuzol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cortisuzol is a glucocorticoid corticosteroid, discovered by the French company Roussel Uclaf, and claimed to have anti-inflammatory activity in a number of clinical case reports.
Status:
Investigational
Source:
INN:oxazidione [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

OXAZIDIONE was developed as an anticoagulant that could prevent the formation of clots in thromboembolic disease. However, this drug has never been marketed.

Showing 1161 - 1170 of 13240 results