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

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Showing 10061 - 10070 of 10251 results

Status:
Possibly Marketed Outside US
Source:
PARKINSAN by Byk-Gulden Lomberg Chemische Fabrik
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Budipine is an antiparkinsonian drug, which was developed by Byk Gulden (now Takeda) for the treatment of Parkinson's disease. The drug has multiple mechanisms of action: it was found to interfere with dopamine biosynthesis, mainly by inhibiting MAO-B enzyme and stimulating aromatic L-amino acid decarboxylase. Also the drug inhibits the dopamine re-uptake and has weak affinity to NMDA and muscarinic receptors. Budipine passes the blood-brain barrier, is metabolized by hydroxylation, and is excreted by both in urine and feces within 24 h.
Status:
Possibly Marketed Outside US
Source:
Japan:Exatecan Mesilate Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Exatecan (DX-8951f), a new hexacyclic camptothecin analogue, is a second-generation topoisomerase inhibitor that prevents rapidly dividing cells from replicating by interrupting DNA transcription, ultimately leading to cell death. Preclinical studies showed exatecan to have broad-spectrum antitumor efficacy. Exatecan is in phase III clinical trials for the treatment of pancreas cancer. However, there is no recent report of this research. The compound was co-developed by Daiichi Pharmaceutical (now Daiichi Sankyo) and Yakult Honsha.
Status:
Possibly Marketed Outside US
Source:
BIFEMELANE by Mitsubishi Chemical
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Bifemelane is a psychotropic drug, was found to inhibit monoamine oxidase (MAO). It inhibited type A MAO (MAO-A) competitively and type B (MAO-B) noncompetitively and it was a more potent inhibitor of MAO-A than of MAO-B. Bifemelane is an antidepressant and cerebral activator that is used in Japan for the treatment of cerebral infarction patients with depressive symptoms, and in the treatment of senile dementia as well. It also appears to be useful in the treatment of glaucoma.
Status:
Possibly Marketed Outside US
Source:
UK NHS:Propamidine isetionate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Propamidine, an aromatic diamidine compound, is widely used as an antimicrobial agent. Propamidine isethionate, the salt of propamidine with isethionic acid, is used in the treatment of Acanthamoeba infection. Diseases caused by Acanthamoeba include keratitis and granulomatous amoebic encephalitis.
Status:
Possibly Marketed Outside US
Source:
NCT03431649: Phase 4 Interventional Completed Pediatric Pulmonary Hypertension
(2017)
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)



Beraprost is a stable, orally active prostacyclin analogue. Beraprost acts by binding to prostacyclin membrane receptors ultimately inhibiting the release of Ca2+ from intracellular storage sites. This reduction in the influx of Ca2+ has been postulated to cause relaxation of the smooth muscle cells and vasodilation. Beraprost is indicated for the treatment of pulmonary hypertension and improvement of ulcers, pain & feeling of coldness associated with chronic arterial occlusion. In addition beraprost displays thyroid hormone receptor antagonistic properties.
Status:
Possibly Marketed Outside US
Source:
Gastopsin by Nippon Kayaku
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tetragastrin is a C-terminal tetrapeptide (Trp–Met–Asp–Phe–NH2) of gastrin. It is the smallest peptide fragment of gastrin which has the same physiological and pharmacological activity as gastrin. It is used to test the secretion of digestive juice. It causes severe anxiety symptoms when administered to humans and is commonly used in scientific research to induce panic attacks for the purpose of testing new anxiolytic drugs. Tetragastrin is a selective cholecystokinin B (CCKB) receptor agonist. Tetragastrin is used as a gastric stimulant at a dose of 4 ug/kg, it was marketed in Japan under the brand name Gastopsin.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefodizime is a third-generation cephalosporin with a broad spectrum of antibacterial activity. Administered intravenously or intramuscularly 1 to 4 g of cefodizime daily for an average of 7 to 10 days produces a clinical cure in 80 to 100% of patients (adults, elderly or children) with upper or lower respiratory tract infections or urinary tract infections. In comparative trials cefodizime was as effective as other third generation cephalosporins. A single dose of cefodizime (1 or 2 g) is also useful in treating lower urinary tract infections. Urogenital gonorrhoea, whether caused by beta-lactamase producing or non-beta-lactamase producing Neisseria gonorrhoeae, is very effectively treated by single dose therapy with intramuscular cefodizime. Preliminary data from a small number of patients indicates that cefodizime may also be useful in the treatment of otitis media, sinusitis and gynaecological infections, and for the prophylaxis or treatment of surgical infections. The clinical efficacy of cefodizime compared to other third generation cephalosporins is superior to that predicted from in vitro results. This superior activity of cefodizime may be related to the relatively long elimination half-life of the drug or its ability to modify some functions of the immune system--a potentially important finding awaiting further investigation. Cefodizime is well tolerated and has a tolerability profile similar to other members of its class with systemic adverse events being primarily gastrointestinal or dermatological. Cefodizime may be more convenient to administer than some other agents of its class as it may be given once or twice daily. While there are no trials comparing cefodizime to other third generation cephalosporins in immunosuppressed populations, preliminary information indicates cefodizime may be useful in this group. Cefodizime targets penicillin-binding proteins (PBPs) 1A/B, 2, and 3 resulting in the eventual death of the bacterial cell. In vivo experimental models of infection showed that bacterial clearance by this drug is at least as effective compared with other 3rd generation cephalosporins. It has a similar adverse effect profile to other 3rd generation cephalosporins which is mainly being limited to gastrointestinal or dermatological side effects. It is not currently approved by the FDA for use in the United States.
Status:
Possibly Marketed Outside US
Source:
NCT00190697: Phase 4 Interventional Completed Breast Cancer
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Arzoxifene (LY353381) is a synthetic, nonsteroidal ligand termed selective estrogen receptor modulator. Arzoxifene has antiestrogenic effects on the breast and endometrium, but pro-estrogenic effects on bone and lipids. Arzoxifene has been studied in the treatment of various hormone-responsive neoplasms. Its development has been discontinued.
Status:
Possibly Marketed Outside US
Source:
Japan:Lazabemide Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lazabemide is a reversible and selective inhibitor of monoamine oxidase B (MAO-B) that was under clinical development against Parkinson's disease, Alzheimer's disease and as an aid to smoking cessation. The development of the drug was discontinued due to liver toxicity.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Tilorone (trade names Amixin, Lavomax and others) is the first recognized synthetic, small molecular weight compound that is an orally active interferon inducer. Tilorone induces the formation of interferons (alpha, beta, gamma) by intestinal epithelial cells, hepatocytes, T-lymphocytes, and granulocytes. After ingestion, the maximum production of interferon is determined in the sequence of the intestine - liver - blood after 4-24 hours. Activates the stem cells of the bone marrow, stimulates humoral immunity, increases the production of IgM, IgA, IgG, affects the antibody formation, reduces the degree of immunosuppression, restores the ratio of T-helperers / T-suppressors. The mechanism of antiviral action is associated with the inhibition of translation of virus-specific proteins in infected cells, thereby suppressing the replication of the virus. Effective against influenza viruses and viruses that cause ARVI, hepato- and herpesviruses, incl. CMV and others. The mechanism of antiviral action is associated with the inhibition of translation of virus-specific proteins in infected cells, thereby suppressing the replication of the virus.

Showing 10061 - 10070 of 10251 results