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

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Showing 8141 - 8150 of 8504 results

Status:
Possibly Marketed Outside US
Source:
INAVIR by Daiichi Sankyo
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Laninamivir ocatanoate is a prodrug of Laninamivir (R-125489), a new neuraminidase (NA) inhibitor, was discovered, and in this study, its NA inhibitory activities against various influenza viruses including oseltamivir-resistant viruses are reported. Laninamivir octanoate has been approved for use in Japanese clinics for the treatment and prevention of influenza in both adults and children. The inhaled laninamivir octanoate is converted into its active form, laninamivir, in the lungs where a high concentration persists for a long period of time.
Azapropazone is a non-steroidal anti-inflammatory drug. It is indicated for use in the treatment of rheumatoid arthritis, osteo-arthritis and gout. Gastro-intestinal disturbances, allergic skin rashes and photosensitivity, headache, vertigo, oedema and kidney impairment may occur. Gastro-intestinal bleeding and angioedema have been reported. Pre-treatment with this drug failed to modify plasma concentrations of phenobarbitone. Brain levels of imipramine or desmethyl imipramine were unaffected 60 minutes after oral administration of imipramine.
Todralazine is a hydralazinophthalazine-derived drug currently used in the treatment of arterial hypertension. As vasodilator, it might be used in combination with isosorbide dinitrate. Side effects and drug toxicity were uncommon in such vasodilator therapy.
Ethamsylate (2,5-dihydroxy-benzene-sulfonate diethylammonium salt) is a synthetic hemostatic drug indicated in cases of capillary bleeding. Ethamsylate acts on the first step of hemostasis by improving platelet adhesiveness and restoring capillary resistance. In addition it inhibits prostaglandin biosynthesis. Well-controlled clinical trials clearly showed the therapeutic efficacy of ethamsylate in dysfunctional uterine bleeding, with the magnitude of blood-loss reduction being directly proportional to the severity of the menorrhagia. Other well-controlled clinical trials showed therapeutic efficacy of ethamsylate in periventricular hemorrhage in very low birth weight babies and surgical or postsurgical capillary bleeding.
Status:
Possibly Marketed Outside US
Source:
Japan:Penaprazole Sodium Hydrate
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Nepaprazole is a proton pump inhibitor of substituted 2-(2-pyridinylmethylsulfinyl)-1H-benzimidazole class evaluated as useful drug for the clinical treatment of peptic ulcer diseases. The effects of the TY-11345 (nepaprazole sodium salt) on gastric mucosal proton pump (H+/K(+)-ATPase) activity, gastric acid secretion and gastro-duodenal lesions were investigated in experimental animals. TY-11345 potently inhibited H+/K(+)-ATPase activity in isolated rabbit gastric mucosal microsomes and the inhibitory effect was enhanced under weak acid conditions. In Ghosh & Schild rats, intravenous injection of TY-11345 significantly inhibited gastric acid secretion stimulated by tetragastrin; the effect of TY-11345 was twice as potent as that of omeprazole. In pylorus ligated rats, TY-11345 inhibited basal gastric acid secretion by both the intraduodenal and oral routes with 9 and 5 times more greater potency than those of omeprazole, respectively. The antisecretory effect of TY-11345 persisted for more than 24 h in pylorus ligated rats. In experimental ulcer models, TY-11345 prevented the formation of water-immersion stress, ethanol or indomethacin-induced gastric lesions and mepirizole-induced duodenal lesions in rats. The antiulcer effects of TY-11345 were 3 to 15 times more potent than those of omeprazole. These results suggested that TY-11345 had potent antisecretory and antiulcer effects which are exerted by suppression of H+/K(+)-ATPase activity in gastric parietal cells. Nepaprazole sodium had been studied in phase II clinical trials for treatment of gastric ulser but this research has been discontinued.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefminox Sodium
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefminox is a broad-spectrum, bactericidal cephalosporin antibiotic. It is especially effective against Gram-negative and anaerobic bacteria. It is indicated in treatment of the following infections caused by sensitive bacteria: 1. Respiratory infections: Amygdalitis, circumtonsillar abscess, bronchitis, bronchiolitis, bronchiectasis (in fection), secondary infections of chronic respiratory diseases, pneumonia, and pulmonary suppuration; 2. Infection in urinary system: Nephropyelitis, cystitis; 3. Infections in abdominal cavity: Cholecystitis' angiocholitis'peritonitis; 4. Infections in pelvic cavity: Pelvic peritonitis, adnexitis, intrauterine infection, inflammation in pelvic dead space, and parametritis; 5. Septicaemia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfamonomethoxine is a long-acting sulfonamide antibiotic. It is active against Streptococcus spp. (Including Streptococcus pneumoniae, Enterococcus spp.), Staphylococcus spp., Escherichia coli, Shigella spp., some strains of Proteus spp., Neisseria gonorrhoeae, Neisseria meningitides. Sulfamonomethoxine also active against Chlamydia spp., Toxoplasma gondii, Plasmodium. Rapidly absorbed from the gastrointestinal tract, it penetrates the BBB. The relatively low toxicity. Sulfamonomethoxine is a competitive inhibitor of dihydropteroate synthetase used to block the synthesis of folic acid. By preventing the production of folate in bacteria, the sulfonamide antibiotics ultimately suppress bacterial DNA replication.
Status:
Possibly Marketed Outside US
Source:
Farom by Asubio Pharma
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Faropenem is a unique antimicrobial penem being developed for oral administration. It markets it in two forms: faropenem sodium and faropenem medoxomil. The high binding affinities of faropenem to penicillin-binding proteins from gram-negative and gram-positive bacteria are mirrored by its pronounced and concentration-dependent bactericidal effect. It is usually used to treat a wide range of infections such as skin, respiratory and otorhinologic infections. The most commonly reported adverse reactions include diarrhea, abdominal pain, loose stool, rash and nausea. The FDA refused to approve faropenem – the applicant have to conduct new studies and clinical trials to prove the drug treats community-acquired pneumonia, bacterial sinusitis, chronic bronchitis, and skin infections.
Status:
Possibly Marketed Outside US
Source:
Starasid by Nippon Kayaku|Yamasa
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cytarabine ocfosfate (commercial name: Starasid) is a prodrug having stearyl group attached to phosphoric acid at 5' position of arabinose moiety of cytosine arabinoside (Ara-C). This drug is given orally. The mode of action is in the inhibition of DNA synthesis after conversion to Ara-CTP as in Ara-C. The drug is metabolized in the liver, producing the intermediate metabolite, C-C3PCA which is converted to Ara-C gradually. This property results in the maintenance of relatively long time the blood Ara-C levels. This was proved to be active clinically against acute leukemia and MDS.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefmatilen Hydrochloride Hydrate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefmatilen (codenamed S-1090) is an orally-active cephalosporin antibiotic, that shows high activity against a variety of Gram-positive and Gram-negative bacteria, including Streptococcus pyogenes and Neisseria gonorrhoeae.

Showing 8141 - 8150 of 8504 results