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

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Showing 1131 - 1140 of 10251 results

Status:
Investigational
Source:
NCT04716335: Early Phase 1 Interventional Completed Emotions
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Harmine (aka telepathine) is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It is a naturally occurring metabolite in a number of plants, notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi. Harmine is a reversible inhibitor of monoamine oxidase A (MAO-A), but not MAO-B. Harmine has been found to have potential anti-cancer and neuroprotective properties, and also promotes differentiation of osteoblasts and chondrocytes while inhibiting osteoclastogenesis. Harmine has also been used as a C-11 labeled probe in positron emission tomography.
Status:
Investigational
Source:
NCT02322086: Phase 2 Interventional Completed Psoriasis
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Rose Bengal lactone is a polyhalogenated derivative of Fluorescein. Rose Bengal lactone is a dye compound described to produce cell membrane damage. Rose Bengal lactone and other Fluorescein derivatives are also described to modulate the function of ATP-sensitive K+ channels. Rose bengal lactone reacts readily with bases so treatment with triethylamine immediately yields the Rose Bengal salt.
Status:
Investigational
Source:
INN:cartazolate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cartazolate (also known as SQ-65,396) is GABAA receptor positive allosteric modulator with potent anxiolytic activity proven in clinical trials. Cartazolate is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor.
Status:
Investigational
Source:
INN:diftalone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Diftalone is a symmetrical tetracyclic compound with anti-inflammatory and antipyretic activities. The anti-inflammatory potency of diftalone is greater than that of aspirin, approximately equal to that of phenylbutazone, but lower than that of indomethacin. Diftalone exhibited limited but statistically significant antipyretic activities. It less potent than aspirin or phenylbutazone. Diftalone seems to be an effective and safe anti-inflammatory agent in the treatment of rheumatoid arthritis. It demonstrated the same activity as indomethacin and phenylbutazone. However, because of hepatotoxicity and carcinogenicity (hepatoma) in preclinical studies and hemotoxicity and gastrointestinal adverse effects in humans, diftalone was withdrawn by its manufacturer.
Status:
Investigational
Source:
NCT00063687: Phase 2/Phase 3 Interventional Completed Congestive Heart Failure
(2003)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Oxypurinol is an active metabolite of allopurinol and is an inhibitor of xanthine oxidase. Cardiome Pharma developed oxipurinol for the treatment of allopurinol-intolerant hyperuricemia (gout) and for the treatment of congestive heart failure. It is known, that inhibition of xanthine oxidase can improve myocardial work efficiency by sensitizing cardiac muscle cells to calcium ions, which are a key determinant of cardiac muscle function. However, all these studied were discontinued.
Status:
Investigational
Source:
INN:berythromycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Berythromycin or erythromycin B (also known as 12-deoxyerythromycin A), an acid-stable co-metabolite of the antibiotic erythromycin A, exhibits broad-spectrum antibiotic activity. The antibacterial activity of erythromycin B is similar to that of erythromycin A, but after acid-treatment, resembling exposure to the stomach, erythromycin B substantially retains antibacterial activity, whereas erythromycin A does not. Erythromycin B played an integral part of the structure activity relationship studies of semi-synthetic erythromycins.
Status:
Investigational
Source:
NCT00273884: Phase 2 Interventional Completed Acute Myeloid Leukemia
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Amonafide L-malate (AS1413, Xanafide) is a DNA intercalator and topoisomerase II inhibitor that induces apoptosis by disrupting chromatin organisation independently of ATP. This is different from classical topoisomerase II inhibitors which induce apoptosis by causing extensive DNA damage. Amonafide L-malate is also able to evade P-glycoprotein and related transporters that contribute to multi-drug resistance. AS1413 had orphan drug status in both the U.S. and the E.U. for the treatment of AML and also received Fast Track status from the U.S. FDA for the treatment of secondary AML. Amonafide L-malate was originated by Xanthus Pharmaceuticals. It was added to Antisoma's pipeline through the acquisition of Xanthus Pharmaceuticals, Inc. in June 2008. Antisoma discontinued development of Amonafide L-malate after data from the open-label, international Phase III ACCEDE trial in over 420 patients showed that 600 mg/m 2 IV amonafide for 5 days plus cytarabine missed the primary endpoint of significantly improving initial remission rate, defined as the proportion of patients who achieve CR or CRi, vs. daunorubicin plus cytarabine.
Status:
Investigational
Source:
INN:cortodoxone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



11-Deoxycortisol (also known as cortodoxone) is the predominant deoxycorticosteroid and is the immediate precursor of cortisol, which is formed by the enzymatic action of 11beta-hydrozylase (P450). Deficiency of this enzyme causes congenital adrenal hyperplasia, which is characterized by hypertension. 11-deoxycortisol is measured as part of the Metyrapone Test. Metyrapone blocks the formation of cortisol, resulting in increased secretion of Adrenocorticotropic hormone (ACTH) and 11-deoxycortisol in normal individuals.
Status:
Investigational
Source:
USAN:Aminophenazone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Ampyrone (4-Aminoantipyrine or AAP) is a metabolite of aminophenazone and is an aromatic substance with analgesic, antipyretic and anti-inflammatory properties. When combined with the antineoplastic agents, ampyrone decreased their genotoxic, mutagenic, apoptotic, and phagocytic effects. However, ampyrone usually produces side effects, such as the risk of agranulocytosis. Although ampyrone is scarcely ever administered as an analgesic because of the potential side effects, as a raw material, it is mostly used to produce ampyrone derivatives, which have better biological activities. In addition, it is used as a reagent for biochemical reactions producing peroxides or phenols and can also be used to detect phenols in the environment. Exposure to ampyrone could induce changes in the enzyme catalase structure and function.

Showing 1131 - 1140 of 10251 results