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Restrict the search for
phenyl aminosalicylate
to a specific field?
Status:
Investigational
Source:
USAN:ORBOFIBAN ACETATE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT01218477: Phase 1/Phase 2 Interventional Completed Leukemia
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
BMS-833923 was discovered by Exelixis and was out-licensed to Bristol-Myers Squibb. BMS-833923 is an orally bioavailable Smoothened antagonist. BMS-833923 reduces hedgehog pathway activity, decreases cell proliferation and induces apoptosis via the intrinsic pathway in esophageal adenocarcinoma (EAC) cell lines. BMS-833923 dose-dependently affects canonical and prostate hedgehog signature gene transcription in vitro. BMS-833923 is in phase II clinical trials for the treatment of chronic myeloid leukaemia.
Status:
Investigational
Source:
NCT00741910: Phase 2 Interventional Completed Crohn's Disease
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.
Status:
Investigational
Source:
NCT02784444: Phase 2 Interventional Completed Non-alcoholic Fatty Liver Disease
(2016)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
MSDC 0602, a first-in-class oral, once-daily, insulin sensitiser that acts by stimulating mitochondrial proteins, is being developed by Metabolic Solutions and Cirius Therapeutics for treatment Type 2 diabetes mellitus and Non-alcoholic steatohepatitis. MSDC-0602 prevented and reversed liver fibrosis and suppressed expression of markers of stellate cell activation in livers of mice fed a diet rich in trans-fatty acids, fructose, and cholesterol. Moreover, mice with liver-specific deletion of MPC2 were protected from development of NASH on this diet. MSDC-0602 directly reduced hepatic stellate cell activation in vitro, and MSDC-0602 treatment or hepatocyte MPC2 deletion also limited stellate cell activation indirectly by affecting secretion of exosomes from hepatocytes. Cirius Therapeutics plans the phase III trial for Type 2 diabetes mellitus and Non-alcoholic steatohepatitis in September 2019
Class (Stereo):
CHEMICAL (RACEMIC)
Trimeperidine (promedol) is the earliest and mostly studied opioid analgesic. Trimeperidine stimulates opioid receptors in the central nervous system. Compared with morphine, it has a weaker and shorter analgesic effect, less affects the respiratory, vomiting and vagal centers, does not cause smooth muscle spasm (except for the myometrium), and has a moderate antispasmodic and hypnotic effect. It is used to treat severe pain syndrome, acute left ventricular failure, pulmonary edema, cardiogenic shock, preparation for surgery, childbirth, high fever, post-transfusion complications, poisoning with atropine, barbiturates, barium, gasoline, boric acid, strong acids, carbon monoxide, turpentine, formalin, formalin. It has several side effects. Administration of this substance is associated with the development of life-threatening conditions accompanied by the suppression of respiration center. Analgesic trimeperidine (promedol) was included into the health care kits by various Ministries of the Russian Federation at different times.
Status:
Investigational
Source:
NCT00336713: Phase 3 Interventional Completed Depressive Disorder
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sanofi aventis developed saredutant (also known as SR 48968C) as a tachykinin neurokinin-2 (NK2) receptor antagonist for the treatment of depressive disorders and generalized anxiety disorder. This drug participated in phase III clinical trials in patients with a generalized anxiety disorder and as Combination Treatment for major depressive disorder, however, the drug failed to meet efficacy endpoints. It is known that NK-2 receptor mediates airway obstruction that is why saredutant was studied as a potential treatment of asthma. However, all studies of the drug were discontinued.
Status:
Investigational
Source:
NCT00232258: Phase 2 Interventional Completed Ulcerative Colitis
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Nolpitantium (SR-140333) is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extravasation in rats. Nolpitantium was found to be effective in the modulation of the inflammatory response and airway remodeling in mice. Nolpitantium is reported to cause antagonism of the SP-induced relaxations of human isolated intralobar pulmonary arterial rings. Nolpitantium also blocked the activation of rat thalamic neurons after nociceptive stimulation. Nolpitantium has been shown to reduce the severity of inflammation in trinitrobenzene sulfonic acid-induced colitis in the rat colon. Nolpitantium inhibited mustard oil-induced plasma protein extravasations in the dorsal skin of the rat hind paw. Nolpitantium had been in some phase II clinical trials but further studies were discontinued.
Status:
Investigational
Source:
NCT01211470: Phase 2 Interventional Completed Acute Bacterial Skin and Skin-structure Infection(ABSSSI) Due to Staphylococcus Aureus (MSSA)
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Brilacidin (formerly PMX-30063) is a polymer-based antibiotic and an investigational new drug, that was studied in human clinical trials, and represents a new class of antibiotics called host defense protein mimetics. Brilacidin is an antibiotic that works by disrupting bacterial cell membranes, mimicking defensins that play a role in innate immunity. Brilacidin has shown great efficacy in phase II clinical trials against acute Staphylococcus aureus skin and skin structure infections, comparable to that of the lipopeptidic drug daptomycin, which is currently used clinically to treat drug-resistant staph infections. Brilacidin also has potent broad-spectrum activity in vitro against several other Gram-positive and Gram-negative pathogenic bacteria, including several multidrug-resistant strains.
Status:
Investigational
Source:
NCT00606749: Phase 2 Interventional Completed Pemphigus Vulgaris
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
ITX-5061, an arylketoamide derivative, is a scavenger receptor B1 antagonist and a potent hepatitis C virus (HCV) entry inhibitor. It entered phase I clinical trial in liver transplant recipients with HCV but the trial was terminated.
Status:
Investigational
Source:
NCT01221298: Phase 2 Interventional Completed Hepatitis C
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
