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

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Showing 2471 - 2480 of 3565 results

Status:
Possibly Marketed Outside US
Source:
Bunaprolast by ZYF Pharm Chemical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Bunaprolast has been described as the most potent antioxidant inhibitor of endothelial activation of NF-kB and gene expression of E-selectin and vascular cell adhesion molecule-1. Bunaprolast is a potent inhibitor of leukotriene B4 production in human whole blood and undergoes deacetylation to an initial metabolite with similar pharmacological potency. The in vivo demonstration of inhibition of pulmonary bronchoconstriction by this compound, in a model known to be leukotriene sensitive, coupled with its potent in vitro inhibition of 5-lipoxygenase enzymes, suggests bunaprolast may be of use in 5-lypoxygenase-mediated models of asthma.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Flumedroxone is a progestative agent. It is a pregnane derivative substituted at C-6 by a trifluoromethyl group. It was tested whether flumedroxone had prophylactic value in migraine. No benefit was found in males, or in females with no history of menstrual exacerbation of migraine. In women whose migraine was worse around the time of menstruation flumedroxone resulted in statistically fewer headaches of less severity. With the dose used in this trial side-effects were frequent, the commonest being polymenorrhagia, which occurred in half the women of reproductive age.
Status:
Possibly Marketed Outside US
Source:
NCT01321034: Phase 4 Interventional Completed Hypercholesterolemia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Laropiprant is a drug, which was used in combination with nicotinic acid (also known as niacin) and was known under tradename: tredaptive. Tredaptive was indicated as adjunctive therapy to diet for use in patients with primary hypercholesterolaemia (heterozygous familial and non-familial) or mixed dyslipidaemia. The marketing authorisation for Tredaptive has been withdrawn at the request of the marketing-authorisation holder due to increases in side effects with no cardiovascular benefit. Laropiprant is a selective antagonist of the prostaglandin D(2) (PGD(2)) receptor subtype 1 (DP1). It also has the affinity to interact with thromboxane A2 receptor (TP), although it is approximately 190-fold less potent when compared to DP1. Activation of TP has been shown to induce platelet aggregation in vitro, whereas activation of human platelet DP1 inhibits platelet aggregation. These in vitro data indicate that laropiprant may alter platelet function either by enhancement of platelet reactivity through DP1 antagonism or by inhibition of platelet aggregation through TP antagonism. Also were clinical trials phase II for the laropiprant alone, there were shown, that drug did not demonstrate efficacy in asthmatic patients or patients with allergic rhinitis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Anagestone acetate is a progestin medication, used in the 1960s in combination with the estrogen mestranol as a combined birth control pill. Toxicological study of chronic administration in dogs and monkeys showed the increased risk of developing malignant tumors in the mammary glands and a dose-dependent, nonprogressive decrease in hemoglobin and hematocrits. The drug was voluntarily withdrawn from the market in 1969.
Status:
Possibly Marketed Outside US
Source:
RECORDIL by Recordati
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Efloxate is a coronary vasodilator developed in 1959 in Italy by Recordati and used for the treatment of angina pectoris. The drug is no longer marketed.
Status:
Possibly Marketed Outside US
Source:
NCT02307396: Phase 4 Interventional Completed Schizophrenia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Zuclopenthixol is indicated the management of the manifestations of schizophrenia and other mental illnesses with disturbances in thinking, emotional reactions and behaviour. It is also used to treat the manic phase of manic depressive illness. Zuclopenthixol, a thioxanthene derivative, has high affinity for both dopamine D1 receptors and dopamine D2 receptors. Zuclopenthixol also has high affinity for α1-adrenergic and 5-HT2 receptors. Zuclopenthixol (CLOPIXOL®) is avavilable in the form of tablets and solution for intramuscular injections.
Elliptinium is an antineoplastic agent, which was used in the treatment of metastatic breast cancer in France under the name Celiptium. The drug is known to intercalate into DNA and inhibit topoisomerase II. Several studies have demonstrated that this molecule can be oxidized, yielding a reactive electrophilic form, which is able to bind covalently to a nucleophilic biological molecule.
Status:
Possibly Marketed Outside US
Source:
Canada:BERYLLIUM METALLICUM
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Beryllium is a chemical element in the periodic table that has the symbol Be and atomic number 4. A toxic bivalent element, beryllium is a steel grey, strong, light-weight yet brittle, alkaline earth metal. Beryllium is an ubiquitous element in the environment, and it has many commercial applications. Beryllium is used in alloys with copper or nickel to make gyroscopes, springs, electrical contacts, spot-welding electrodes and non-sparking tools. Mixing beryllium with these metals increases their electrical and thermal conductivity. Other beryllium alloys are used as structural materials for high-speed aircraft, missiles, spacecraft and communication satellites. Beryllium is relatively transparent to X-rays so ultra-thin beryllium foil is finding use in X-ray lithography. Beryllium is also used in nuclear reactors as a reflector or moderator of neutrons. Beryllium and its compounds are toxic and carcinogenic. If beryllium dust or fumes are inhaled, it can lead to an incurable inflammation of the lungs called berylliosis. Because it is strong, stable, can handle elevated levels of heat resistance and is highly transparent to x-rays, beryllium, in thin foil form, has long been critical to the operation of medical and scientific x-ray equipment. Beryllium foil provides the window through which tissue-penetrating x-rays are focused, while maintaining the vacuum inside the x-ray tube generator. Beryllium foil remains indispensible for high-resolution medical radiography, including CT scanning and mammography. Beryllium in newer generation mammography equipment enables a lower radiation dose scan with significantly finer tumor resolution, enabling breast cancer detection at its early, most treatable stages. Beryllium is also used in components of the analytical equipment used to analyze blood for HIV and other diseases, offering the precision and reliability that doctors and patients demand.
Status:
Possibly Marketed Outside US
Source:
NCT02682524: Phase 4 Interventional Completed Osteoarthritis of Knee
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. The dose is 100 mg twice daily, and should not be given to people with porphyria or breastfeeding mothers and is not recommended for children. Aceclofenac is a cytokine inhibitor. Aceclofenac works by blocking the action of a substance in the body called cyclo-oxygenase. Cyclo-oxygenase is involved in the production of prostaglandins (chemicals in the body which cause pain, swelling and inflammation). Aceclofenac is the glycolic acid ester of diclofenac. The incidence of gastric ulcerogenicity of aceclofenac has been reported to be significantly lower than that of other frequently prescribed NSAIDs: for instance, 2-fold less than naproxen, 4-fold less than diclofenac, and 7-fold less than indomethacin. Aceclofenac is metabolized in human hepatocytes and human microsomes to form [2-(2',6'-dichloro-4'-hydroxy- phenylamino)phenyl] acetoxyacetic acid as the major metabolite, which is then further conjugated.
Status:
Possibly Marketed Outside US
Source:
NCT03077555: Phase 4 Interventional Completed Ovulation Inhibition
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nomegestrol acetate (NOMAC) is a 19-norprogesterone derivative with high biological activity at the progesterone receptor, a weak anti-androgenic effect, but with no binding to estrogen, glucocorticoid or mineralocorticoid receptors. Nomegestrol has been developed by the Monaco-based company Théramex SAM (a Teva subsidiary). Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy in combination with estradiol for the relief of menopausal symptoms; it has been approved in Europe as monotherapy for the treatment of the menopausal syndrome, uterine diseases and menorrhagia, and in combination with an estrogen for the treatment of menopausal symptoms. Nomegestrol acetate in combination with estradiol is used as an oral contraceptive.

Showing 2471 - 2480 of 3565 results