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Restrict the search for
m nalidixic acid
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Fostriecin, an antitumor antibiotic produced by Streptomyces pulveraceus, is a strong inhibitor of serine/threonine protein phosphatases type 2A and type 4, and inhibits the catalytic activity of partially purified Topo II (type II topoisomerase) in a non-competitive manner.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Avoralstat, a small molecule inhibitor of plasma kallikrein, participated in clinical trials phase III to prevent hereditary angioedema, but these studied were discontinued due to insufficient efficacy study. Recently published article has described that avoralstat could improve the quality of life in C1‐INH‐HAE patients. Hereditary angioedema (HAE) with C1 inhibitor deficiency (C1‐INH‐HAE) is an autosomal dominant disorder characterized by recurrent episodes of swelling of the skin, pharynx, gastrointestinal tract, genitals, and is due primarily to mutations in the SERPING1 gene that results in insufficient production of the natural plasma kallikrein inhibitor, C1 inhibitor (C1‐INH).
Status:
Investigational
Source:
USAN:IPROFENIN [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
IPROFENIN is an iminodiacetic acid derivative. Its 99mTc radiolabelled form was used in cholescintigraphy and hepatobiliary scintigraphy to diagnose problems of the liver, gallbladder and bile ducts.
Status:
Investigational
Source:
INN:lesogaberan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lesogaberan is a peripherally restricted high-affinity GABAB-R-specific agonist, originally developed for the treatment of gastroesophageal reflux disease (GERD) that appears to be safe for human use. The toxicity profile shows no indication of hepatic effect. Lesogaberan has been shown to induce decreased body weight and decreased food consumption. A dose-dependent diuretic effect was also noted in rats. Treatment with lesogaberan significantly enhanced replication of human islet cells in vitro, which was abrogated by a GABAB-R antagonist. Lesogaberan may be a promising drug candidate for clinical studies of diabetes intervention and islet transplantation. Disappointingly, in phase IIb study it was shown that lesogaberan is only marginally superior to placebo in gastroesophageal reflux disease (GERD) patients who are partially responsive to proton pump inhibitor (PPI) therapy.
Class (Stereo):
CHEMICAL (UNKNOWN)
Cronidipine (LF 2.0254) is a calcium channel blocker. LF 2.0254 inhibited in a time-dependent fashion K(+)- and Ca2(+)-induced contractions of rabbit aorta with respective IC50 of 2.7 nM and 1.7 nM. Cronidipine had a long-lasting antihypertensive action in spontaneously hypertensive rats and was able to decrease blood pressure and increase heart rate and plasma renin activity in hypertensive dogs.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Propoxate (R7464) is a potent anesthetic agent in cold-blooded vertebrates, which has never been marked and has never been used on humans.
Status:
Investigational
Source:
INN:fluzinamide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Fluzinamide (AHR-8559), an anticonvulsant agent that was studied in patients with refractory partial seizures. However, information about the further development of this drug is not available.
Status:
Investigational
Source:
JAN:CAROTEGRAST METHYL [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Carotegrast is phenylalanine derivative patented by pharmaceutical company Ajinomoto Co. for the treatment or prevention of inflammatory disease states related to the α4 integrin-dependent adhesion process. In preclinical studies, Carotegrast shows pharmacological activity in rheumatoid arthritis and inflammatory bowel disease.
Status:
Investigational
Source:
JAN:MOTESANIB PHOSPHATE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Motesanib (AMG 706), a novel nicotinamide, was identified as a potent, orally bioavailable inhibitor of the VEGFR1/Flt1, VEGFR2/kinase domain receptor/Flk-1, VEGFR3/Flt4 and Kit receptors. Motesanib was expected to reduce vascular permeability and blood flow in human tumours. A phase III trial of motesanib in combination with paclitaxel and carboplatin in non-squamous NSCLC has been terminated by Takeda and subsequently the development was discontinued. Motesanib has also been investigated up to phase II in breast, thyroid, colorectal and gastrointestinal stromal tumours. However, development has been discontinued in these indications.
Status:
Investigational
Source:
NCT00103246: Phase 1 Interventional Completed Lymphoma
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
