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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Tilapertin (also known as AMG 747) is a piperazineacetic acid derivative patented by Amgen Inc as glycine transporter-1 inhibitor useful for the treatment of negative symptoms of schizophrenia. Oral administration of AMG 747 dose-dependently increases cerebrospinal fluid(CSF) glycine concentration in rats. In humans, Tilapertin has linear pharmacokinetics, prolonged half-life, and acceptable safety and tolerability at multiple doses up to 60 mg daily dosing. Unfortunately, in clinical trials, Tilapertin failed to demonstrate superior efficacy compare antipsychotic therapy in clinically stable people with schizophrenia.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
IRDABISANT is a histamine H3 receptor inverse agonist with potential therapeutic utility in cognition enhancement.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
ARMGO and Servier are developing an anti-arrhythmia drug aladorian (ARM036) for the treatment of heart failure, arrhythmia and ventricular tachycardia. Aladorian was the first in-house discovered, novel, small molecule NCE (Rycal®) from ARMGO’s library that was advanced into clinical studies. ARM036 completed multiple Phase IIa clinical studies in chronic heart failure patients, demonstrating positive activity and safety in patients, and validating ARMGO’s approach for drug discovery and candidate selection on the RyR target.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Tezampanel, also known as LY 293558 and NGX-424, is a drug originally developed by Eli Lilly, which is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family. Tezampanel was in phase II clinical trial for treatment migraine, but this study was discontinued. Also this drug has several others potential pharmacological actions, one of them is anxiety disorders
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Talabostat is a prolineboronate ester derivative patented by Boehringer Ingelheim Pharmaceuticals, Inc. as an antineoplastic agent. Talabostat inhibits dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity. Talabostat has been shown to cause caspase-1 activation and IL-1β induction in macrophages, which in turn causes upregulation of the cytokines and chemokines that characterize the responses to talabostat, both in vitro and in tumor-bearing mice. Talabostat may also stimulate the production of colony stimulating factors, such as granulocyte colony stimulating factor (G-CSF), resulting in the stimulation of hematopoiesis. In clinical trials, the combination of talabostat and cisplatin was well tolerated compared to historical data using cisplatin alone. The most frequent adverse events were nausea, vomiting, fatigue, anemia, edema, and constipation. Unfortunately was no evidence that Talabostat enhanced the clinical activity of other anticancer drugs and further development was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (UNKNOWN)
Cofisatin is a synthetic derivative of a dehydrocholic acid and isatine, invented by French Societe D'etudes et Applications Chimiques in the 1950s. The compound is claimed to promote intestinal peristaltic without causing irritation.
Status:
Investigational
Source:
INN:taspoglutide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Taspoglutide is a glucagon-like peptide-1 agonist was studied in phase III clinical trials for the treatment patients with type 2 diabetes. However, in September 2010 Roche halted Phase III clinical trials due to gastrointestinal intolerability and serious hypersensitivity reactions experienced by some trial participants.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lofentanil is a pure mu-opioid receptor agonist derived from fentanyl. It is the most potent opioid to be administered to humans, about 500-1000 times more potent than morphine. Lofentanil provides a higher affinity quotient with longer dissociation times for the mu-receptors than fentanyl. The clinical study of the compound is difficult because there is a very individual sensibility. The appropriate doses are not easy to evaluate. Reversal of the loventanil depression needs very high and repeated naloxone dose. Practical use of lofentanil is limited. Lofentanil side effects are: nausea, vomiting and sedation.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
ISOMETAMIDIUM (as a chloride salt) is widely used in tropical countries as an antiprotozoal agent to control animal trypanosomiasis. It is used principally in cattle but also in sheep, goats, buffalos, donkeys, horses, camels and dogs.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)