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

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Showing 2521 - 2530 of 2619 results

Status:
Possibly Marketed Outside US
Source:
Canada:THALLIUM SULFATE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

THALLOUS OXIDE (Thallium (1) Oxide) has been used in the manufacturing of glass of a high coefficient of refraction for optical purposes (thallium flint glass) and for artificial gems. Thallium oxide is black in color and is the inorganic compound of Thallium and Oxygen. THALLOUS OXIDE compounds are typically insoluble in aqueous solutions (water) and extremely stable making them useful in ceramic structures as simple as producing clay bowls to advanced electronics (e.g. tablets) and in light weight structural components in aerospace and electrochemical applications such as fuel cells. THALLOUS OXIDE is toxic by ingestion. It has previously been used as rat poison and ant killer, but its use is prohibited since 1972.
Status:
Possibly Marketed Outside US
Source:
Japan:Giractide Acetate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Giractide is a polypeptide hormone corresponding to the first eighteen amino acid residues of corticotropin in which the 1-serine is replaced by glycine. Giractide acts through the stimulation of cell surface the adrenocorticotropic hormone (ACTH) receptors, which are primarily located on the adrenocortical cells. Giractide stimulates the cortex of the adrenal gland and boosts the synthesis of corticosteroids, mainly glucocorticoids but also sex steroids (androgens). Giractide has been studied in animal models to stimulate glucocorticoid production.
Status:
Possibly Marketed Outside US
Source:
Acetylmethadol by National Inst. for
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Methadyl Acetate is a narcotic analgesic with a long onset and duration of action. Methadyl Acetate is primarily a mu-type opioid receptor agonist and the drug decreases a patient's opioid use by preventing opioid withdrawal. Levacetylmethadol, the enantiomer of Methadyl Acetate, was approved in 1993 by the U.S. Food and Drug Administration for use in the treatment of opioid dependence. In 2001, levacetylmethadol was removed from the U.S. market due to reports of life-threatening ventricular rhythm disorders.
Status:
Possibly Marketed Outside US
Source:
Japan:Anecortave Acetate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Anecortave is a novel angiogenesis inhibitor used in the treatment of the exudative (wet) form of age-related macular degeneration. It will be marketed by Alcon as anecortave acetate (AA) for depot suspension under the trade name Retaane. In 2007 they received their letter of approval for Retaane’s indication to treat wet age-related macular degeneration (AMD), but final approval would require the completion of an additional clinical study. As a result, the Anecortave Acetate Risk-Reduction Trial (AART) was continued to be supported by Alcon. This study looked at the efficacy of Retaane to reduce the progression of the dry from of AMD to the wet-form. In 2008, Alcon Inc. announced they were terminating the development of anecortave acetate for the prevention of developing sight-threatening choroidal neovascularization secondary to age-related macular degeneration. In 2009, Alcon Inc. announced they would terminate the development of the drug for the reducing intraocular pressure associated with glaucoma. Currently, anecortave acetate is not on the market or being made for therapeutic use by Alcon Inc.[7] This could be due to the lack of efficacy of clinical trials with anecortave acetate or because of newer more efficacious products that are currently on the market. Anecortave acetate functions as an antiangiogenic agent, inhibiting blood vessel growth by decreasing extracellular protease expression and inhibiting endothelial cell migration. Its angiostatic activity does not seem to be mediated through any of the commonly known pharmacological receptors. RETAANE blocks signals from multiple growth factors because it acts downstream and independent of the initiating angiogenic stimuli and inhibits angiogenesis subsequent to the angiogenic stimulation. Recently was discovered, that phosphodiesterase 6-delta (PDE6D) was a molecular binding partner of AA and this provided insight into the role of this drug candidate in treating glaucoma.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Acetyldihydrocodeine, a narcotic opiate derivative that was used in Germany as an analgesic. This drug has never been marketed in the USA.
Status:
Possibly Marketed Outside US
Source:
Japan:Ambroxol Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine, which is itself a synthetic derivative of vasicine, the active principle extracted from the plant species Adhatoda vasica. Ambroxol is an expectorant exerting mucokinetic properties, mucociliary activity, stimulation of surfactant production, anti-inflammatory and antioxidative actions and the local anaesthetic effect. Ambroxol was discovered at and has been manufactured by Dr. Karl Thomae GmbH, a division of Boehringer Ingelheim. The ambroxol patent is expired and the drug is available as a generic product from many different companies. Ambroxol was originally developed by Boehringer Ingelheim as a OTC therapy for respiratory disorders related to excessive mucus. Ambroxol's indication is secretolytic therapy in acute and chronic bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport. Boehringer Ingelheim markets the product under various brand names such as Mucosolvan® and Lasolvan®. Ambroxol was identified and found to be a pH-dependent, mixed-type inhibitor of glucocerebrosidase (GCase). Its inhibitory activity was maximal at neutral pH, found in the endoplasmic reticulum, and undetectable at the acidic pH of lysosomes. The pH dependence of Ambroxol to bind and stabilize the enzyme was confirmed. Ambroxol increases both the lysosomal fraction and the enzymatic activity of several mutant GCase variants. This profile of Ambroxol would allow to bind and stabilize GCase in the endoplasmic reticulum (thus preventing its degradation within endoplasmic reticulum), but without affecting GCase in the lysosomes (thus allowing it to degrade glucosylceramide). Indeed, studies showed that Ambroxol treatment significantly increased N370S and F213I mutant GCase activity and protein levels in fibroblasts originally obtained from Gaucher patients. Gaucher's disease is caused by the deficiency of glucocerebrosidase; ambroxol is a chaperone that acts by binding to and stabilising glucocerebrosidase. Zywie (formerly ExSAR Corporation) and Belrose Pharma are developing ambroxol hydrochloride (BEL 0218) for the treatment of type III Gaucher's disease. .
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Quingestanol is a metabolite of the quingestanol acetate, oral contraceptive, which was studied for therapy of menopausal diabetic women. Quingestanol is also a prodrug of norethisterone, which is used in birth control.
Status:
Possibly Marketed Outside US
Source:
Japan:Halopredone Acetate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Halopredone (THS-201; (17,21-bis(acetyloxy)-2-bromo-6beta,9-difluoro-11beta-hydroxypregna-1,4-diene-3,20-dione; halopredone acetate; Topicon) is a highly topical corticosteroid. When it is used for intraarticular injections, the effects last longer than any other steroids which have been used, and it has less general effects. Halopredone acetate is used for arthritis and osteoarthritis (OA) patients. For RA patients, mean dose for a wrist is 12.5 mg and that for a knee is 25 mg. About 90% cases showed effectiveness and in about 45% cases the duration of effect is longer than 4 weeks. More than half cases of OA showed also improvements. It also possesses positive anti-inflammatory properties in dermatologic patients.

Showing 2521 - 2530 of 2619 results