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

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Showing 12061 - 12070 of 13362 results

Status:
Possibly Marketed Outside US
Source:
Heminevrin by Hoffman-La Roche
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Chlormethiazole has sedative, hypnotic, anticonvulsant and neuroprotective properties. This drug is approved in different counties under the different brand name (e.g., Heminevrin) and is used for the management of restlessness and agitation in the elderly, short-term treatment of severe insomnia in the elderly and treatment of alcohol withdrawal symptoms. Clomethiazole interacts with the picrotoxin/barbiturate site of the GABAA-receptor-chloride channel complex. Clomethiazole is pharmacologically distinct from both the benzodiazepines and the barbiturates. Given alone its effects on respiration are slight and the therapeutic index high.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aloglutamol is a salt of aluminum, gluconic acid, and tromethamine. Upon administration, the tromethamine interacts with hydrochloric acid and forms hydrochloride, while aluminum gluconate dihydroxide also binds to hydrochloric acid, forming aluminum chloride and free gluconic acid. Due to this chemical reaction, the pH of the stomach does not rise abruptly, so there is no rebound phenomenon. Aloglutamol is marketed worldwide under trade names Altris, Pyreses, Tasto, and Sabro. It is used for the treatment of hyperacidity, esophagitis, gastritis, peptic ulcer, and hiatal hernia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (EPIMERIC)

Clometocillin, one of the forms of penicillin, was active against pen-I or pen-R pneumococci and was used in children. The modern information about its application is not available.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Olmutinib is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor, used in the treatment of T790M mutation positive non-small cell lung cancer. Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen-activated protein kinase pathways which both promote cell survival and proliferation. By inhibiting EGFR activation, Olmutinib attenuates the activation of these tumor-promoting pathways. In the first phase I/II clinical study of Osimertinib, 800 mg/ day was chosen as the dose for subsequent studies, and the dose-limiting toxicity and maximum tolerated dose was not reached. Olmutinib received breakthrough therapy designation in the United States in December 2015 and was approved for use in Korea in May 2016.
Status:
Possibly Marketed Outside US
Source:
BESTATIN by Nippon Kayaku
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ubenimex is a dipeptide, which specificallyinhibits the activity of leukotriene A4 hydrolase, aminopeptidase B and leucine aminopeptidase of the cell membrane. The drug was isolated from Streptomyces oliooreticuli in 1976 in Nippon Kayaku, Japan and approved for the treatment of acute non-lymphocytic leukemia under the name Bestatin. In the USA the drug is currentlu in Phase II for the treatment of pulmonary arterial hypertension and lymphedema.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Tiazotic acid is an antioxidant. As tiazotic acid morpholinium salt it is marketed under the brand names Thiotriazoline, Tiokor among others in Russia, Ukraine, Uzbekistan as the treatment of ischemic heart diseases. It is proposed to be a hepatoprotective, wound-healing and antiviral agent. A comparative international multicenter randomized trial, assessed anti-anginal anti ischemic efficacy and safety of Trimetazidine (60 mg/d) and Thiotriazoline (600 mg/d) in symptomatic patients with chronic ischemic heart disease receiving the first line therapy. The study assessed the efficacy of the two drugs on total exercise duration, time to 1-mm ST segment depression, the number of angina attacks and nitroglycerin tablets consumed amount. Both drugs have demonstrated clinical efficacy equal for all primary and secondary endpoints. Thiotriazoline was also used for the he correction of hepatotoxicity during combined chemoradiotherapy for cancer patients.
Tiemonium (often used in a form of iodide or methylsulphate salt) is a muscarinic acetylcholine receptor antagonist, which is available in Asia (mainly Bangladesh) for the alleviation of muscle spasms of the intestine, biliary system, uterus and urinary bladder in gastrointestinal, biliary, urinary and gynecological diseases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Nitrovin (hydrochloride salt) is a discontinued food additive that was used in veterinarian practice to promote growth. Nitrovin was shown to inhibit Salmonella growth both in vitro and in vivo (in chickens).
Status:
Possibly Marketed Outside US
Source:
VASCULAT by Boehringer Ingelheim
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bamethan (butyl-sympatol or vasculat) is an adrenaline derivative developed by C. H. Boehringer Sohn. Bamethan shows a depressor action on peripheral blood vessels as a result of the peripheral vasodilating action caused by stimulation of adrenergic beta-receptor. Bamethan has been used abroad in the treatment of certain peripheral vascular and circulatory disturbances, such as vasospastic conditions, arteriosclerotic peripheral vascular disease, Raynaud's syndrome, occlusive vascular disease of the legs, the post-thrombotic syndrome, degenerative muscular disorders, and other conditions involving peripheral vascular insuffciency.
Status:
Possibly Marketed Outside US
Source:
SULINDAC by Alza
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(S)-Sulindac is the (S)-enantiomer of nonsteroidal anti-inflammatory drug (NSAID) Sulindac, that is marketed in the U.S. by Merck as Clinoril. Sulindac is a prodrug, derived from sulfinyl-indene, that is converted in vivo to an active sulfide compound by liver methionine sulfoxide reductases (Msr). The (Msr) family of enzymes includes two major classes, MsrA and MsrB, that specifically reduce the S- and R-epimers of Sulindac. Reduction of (S)-Sulindac to Sulindac Sulfide catalyzed by methionine sulfoxide reductase (Msr)-A. The oxidation of both epimers to sulindac sulfone is catalyzed primarily by the microsomal cytochrome P450 (P450) system. (S)-Sulindac increases the activity of the P450 system better than (R)-sulindac, but both epimers increase primarily the enzymes that oxidize (R)-sulindac. Both epimers can protect normal lung cells against oxidative damage and enhance the killing of lung cancer cells exposed to oxidative stress.

Showing 12061 - 12070 of 13362 results