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

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Showing 411 - 420 of 4933 results

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

Class (Stereo):
CHEMICAL (MIXED)

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

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Otenabant (CP-945,598) is Pfizer developed as a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, which exhibits 10,000-fold greater selectivity against human CB2 receptor, for treatment of obesity. In clinical trial III Pfizer decided to discontinue the development program based on changing regulatory perspectives on the risk/benefit profile of the CB1 class and likely new regulatory requirements for approval.
Status:
Investigational
Source:
INN:remetinostat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

METHYLPARABEN SUBEROHYDROXAMIC ACID PHENYL ESTER (more known as Remetinostat), a histone deacetylase (HDAC) inhibitor, was developed for the treatment of cutaneous T cell lymphoma (CTCL). This drug is participating in phase II clinical trial to evaluate the efficacy, safety, and tolerability to skin lesions in patients with early-stage cutaneous T-cell lymphoma. In May 2019 was announced the positive results from phase II trial of remetinostat in basal cell carcinoma (BCC) patients. Initial results suggest that remetinostat gel offers a potentially effective and well-tolerated, non-surgical intervention for the treatment of localized BCCs. The unique design of remetinostat enables topical application, making it active only in the skin. As soon as it reaches the blood stream, it is degraded, avoiding the side effects associated with other HDAC inhibitors. Besides, remetinostat was studied as the treatment of plaque psoriasis; however, this study was discontinued.
Status:
Investigational
Source:
INN:etazolate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Etazolate (EHT-0202) is a selective, positive GABAA receptor modulator has completed phase II clinical trials in patients with Alzheimer's disease. It is also a selective phosphodiesterase-4 inhibitor that is specific for cAMP. Etazolate showed anxiolytic and antidepressant activity and could be useful in managing post-traumatic stress disorder.
Status:
Investigational
Source:
INN:pararosaniline embonate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pararosaniline pamoate (CI 403-A) was developed as an orally active drug for the treatment of Schistosoma japonicum infection. The clinical trial has shown that capsules were safe and effective; in addition, this drug was well tolerated with a minimum of side effects, which were mostly mild and transient and did not require interruption of treatment. Besides, pararosaniline pamoate was an inhibitor of E.histolytica Hsp90 (EhHsp90) with promising activity against the parasite Pararosaniline pamoate, that causes amebiasis worldwide. Information about the current use of this drug is not available.
Pirinixic acid is a PPARα ligand that can affect atherogenesis by modulating hepatic lipid metabolism and by acting directly on vascular tissue. PPARα activation is generally assumed to be the primary means by which Pirinixic acid produces its biological effects. Nevertheless, there is increasing evidence to suggest that Pirinixic acid is also capable of affecting cellular processes directly. It is under experimental investigation for prevention of severe cardiac dysfunction, cardiomyopathy and heart failure as a result of lipid accumulation within cardiac myocytes. Treatment is primarily aimed at individuals with an adipose triglyceride lipase (ATGL) enzyme deficiency or mutation. For example, cardiac contractility was improved by treating ATGL(-/-) mice with the Pirinixic acid.
Status:
Investigational
Source:
INN:ioxabrolic acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ioxabrolic Acid is triiodobenzoic acid derivative and iodine-containing contrast media
Status:
Investigational
Source:
INN:iomorinic acid
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Iomorinic Acid is triiodobenzamide derivative patented by Lentia G.m.b.H. as a radiographic contrast medium for liver imaging.
Status:
Investigational
Source:
INN:clamidoxic acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Clamidoxic acid is a derivative of phenoxyacetic acid developed in the late 1950s by Smith and Nephew Research Ltd. Clamidoxic acid has been shown to have anti-inflammatory activity and low toxicity in animal tests. The compound was investigated in the clinical trials in patients suffering from rheumatoid arthritis and painful uncomplicated osteoarthritis of the hip, however, no further clinical development was reported.
Status:
Investigational
Source:
INN:traxoprodil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Traxoprodil (CP-101,606) is a potent, selective N-Methyl-D-aspartate (NMDA) receptor (NR2B subunit) antagonist under development by Pfizer for its potential as a neuroprotectant in head injury and neurodegenerative disease. It is in phase II trials in the US and in phase I in Japan for the potential treatment of head injury, such as, Depressive Disorder, Major and Parkinson's Disease. CP-101,606 does not protect against glutamate-induced neurotoxicity in cultured cerebellar neurons, up to a dose of 10 uM. These results are consistent with CP-101,606 being a potent NMDA antagonist, selective for the type of NMDA receptor associated with the hippocampus. Some further investigation revealed that CP-101,606 was associated with a dose-related dissociation and amnesia. These results support the hypothesis that glutamate antagonists may be useful antidyskinetic agents. However, future studies will have to determine if the benefits of dyskinesia suppression can be achieved without adverse cognitive effects.