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

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Showing 6261 - 6270 of 12702 results

Status:
Possibly Marketed Outside US
Source:
Japan:Iocarmic Acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Iocarmic acid is a molecule used in seventies as a contrast media for myelography. Iocarmate meglumine (Dimer-X), a water-soluble salt of iocarmic acid was reported to be safe and best tolerated by central nervous system compared to metrizamide in a double-blind test in patients with symptoms of lumbar and sacral root involvement. In the experimental and clinical studies of Dimer-X used for ventriculography the apparent superiority of Dimer-X over Conray 60 and Angiografin as far as side effects were concerned was demonstrated, but there were no particular differences in the intensities of the ventriculograms obtained. Morphological studies of the ventricles and histological examinations of the ventricular walls 1 month after injections of Dimer-X into the ventricles of dogs showed no abnormalities. In the clinical studies, ventriculography Dimer-X, performed on patients with diseases of the central nervous system, produced ventriculograms of good diagnostic value with no side effects, such as convulsions, apart from mild headache or vomiting in 4 instances. Ventriculography with Dimer-X was carried in 15 infants with myelomeningocele and progressive hydrocephalus. However, as was shown in a number of studies iocarmate produced moderate to severe arachnoiditis from myelography in primates. Early meningitis side effects following lumbar radiculography with iocarmate meglumine were demonstrated.
Status:
Possibly Marketed Outside US
Source:
Japan:1-Naphthylacetic Acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



1-Naphthyl acetate may be used in a rapid staining method for identification of macrophages. And it was used as a susbtrate for different type of esterases, e.g. butyrylcholinesterase, α-naphthyl acetate esterase for determination of their properties towards to insecticide resistance.
Piribedil is an antiparkinsonian agent which acts as D2 and D3 receptor agonist. In European countries and worldwide it is used as a monotherapy or in combination with dopatherapy for treatment of Parkinson's disease, cognitive impairment and obliterating arteriopathy.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Niridazole is used (but not officially recommended) for the treatment of schistosomiasis, dracunculiasis and tungiasis. The mode of action of niridazole is not fully understood. The major action of niridazole seems to be on the glycogen metabolism of the helminths. The drug also case structural damage to the reproductive system of female schistosomes. Another possible mechanism of action of niridazole involves the inhibition of DNA synthesis in schistosomes. It is metabolized in the liver. The most serious side effects were those connected with the nervous area (convulsion, hallucination, etc.).
Status:
Possibly Marketed Outside US
Source:
UK NHS:Sultiame
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Sulthiame is a potent inhibitor of carbonic anhydrase II, VII, IX, and XII. Sulthiame is an antiepileptic drug that is used widely in some European countries and in Israel. Sometimes it is used as an additional (add-on) antiepileptic medicine in non responders, alongside an existing antiepileptic medicine.
Status:
Possibly Marketed Outside US
Source:
Japan:Benzbromarone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Benzbromarone (INN) is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used in the treatment of gout, especially when the first line treatment, allopurinol, fails or produces intolerable adverse effects. It is structurally related to the antiarrhythmic amiodarone. Benzbromarone was introduced in the 1970s and was viewed as having few associated serious adverse reactions. It was registered in about 20 countries throughout Asia, South America and Europe. In 2003, the drug was withdrawn by Sanofi-Synthélabo, after reports of serious hepatotoxicity, although it is still marketed in several countries by other drug companies. The withdrawal has greatly limited its availability around the world and increased difficulty in accessing it in other countries where it has never been available. Standard dosages of benzbromarone (100 mg/day) tend to produce greater hypouricaemic effects than standard doses of allopourinol (300 mg/day) or probenecid (1000 mg/day). Adverse effects associated with benzbromarone are relatively infrequent but potentially severe. Four cases of benzbromarone-induced hepatotoxicity were identified from primary literature, and eleven cases have been reported by Sanofi-Synthélabo but details are not available in the public domain. Only one of the four publicly published cases demonstrated a clear relationship between the drug and liver injury as demonstrated by rechallenge. The other three cases lacked incontrovertible evidence to support a diagnosis of benzbromarone-induced hepatotoxicity. If all the reported cases are assumed to be due to benzbromarone, the estimated risk of hepatotoxicity in Europe was approximately 1 in 17 000 patients but may be higher in Japan. Benzbromarone is a very potent inhibitor of CYP2C9. The mechanism of benzbromarone hepatotoxicity is believed to be due to its hepatic metabolism by CYP2C9 and possible effects of the parent compound or its metabolites on mitochondrial function. Benzbromarone is a benzofuran and shares structural similarities with benzarone and amiodarone, all three of which affect mitochondrial function.
Status:
Possibly Marketed Outside US
Source:
Dorixina by Schering
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clonixin is a nonsteroidal agent. It is an anilino-nicotinic acid derivative. It is a drug of anti-inflammatory antipyretic and analgesic activity that produces minor digestive side-effects. At high concentrations, clonixin inhibited PGE2 formed by COX-2 and partly by COX-1 activity. The drug is indicated for the relief of headaches, muscle aches, joint, dental, ear, dysmenorrhea, post-traumatic, post-surgical, gynecological. Adverse effects are occasionally nausea, dizziness, and somnolence, were mild and transient. On rare occasions, and administering high doses, it is possible the appearance of dry mouth or constipation. Concomitant use of anticholinergic drugs to be avoided by the possibility that they enhance their effects atropine.
Status:
Possibly Marketed Outside US
Source:
Japan:Epitiostanol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Epitiostanol is androgenic antiestrogen developed for the treatment of breast cancer. The drug inhibits estrogen receptor and activates androgen receptor and was shown to be active in vitro on MCF-7, U-2 and U-3 cells. The current marketing status of Epitiostanol is unknown and is supposed to be "discontimued".
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Adrafinil (CRL 40028) was synthesized by Louis Lafon Laboratories. The proprietary name of adrafinil is Olmifon®; its chemical name is (diphenylmethyl )sulfinyl-2-acetohydroxamic acid. Adrafinil is metabolized to modafinil. Adrafinil and modafinil both serve as α1-adrenergic–receptor agonists. The evidence in support of this hypothesis, however, is weak, and other mechanisms of action are probable. Adrafinil may modify the intracerebral release of amino acids (both GABA and glutamate) and adrafinil may increase cerebral metabolism. Olmifon ® tablets, 300 mg (adrafinil) were indicated for the treatment of disorders of vigilance, attention, and ideo-motor slowing in the elderly. It has been marketed in France since September 19, 1985. Cephalon announced their intent to stop marketing the drug, and has discontinued production and marketing of Olmifon in September 2011. Adrafinil is marketing as nootropic supplement to improve cognitive functions.
Bendazac, (1-benzyl-1H-indazol-3-yl-oxy)-acetic acid, is structurally related to indomethacin. Its lysine salt has been reported to be absorbed better than the parent compound. It is applied topically as bendazac lysine 0.5% (wt/vol) aqueous solution for delaying the progression of cataract. Topical application of bendazac is associated with transient burning sensation. It reduces the secretion of the skin ulcer surface, promotes skin formation and accelerates tissue repair.

Showing 6261 - 6270 of 12702 results