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Restrict the search for
m nalidixic acid
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Class (Stereo):
CHEMICAL (UNKNOWN)
Libecillide is a specific monovalent penicilloyl hapten inhibitor of allergic reactions to penicillin. A depression of skin hypersensitivity to PPL and/or penicillin and penicillin derivatives sometimes persisting for weeks and months was obvious in numerous allergic patients submitted to combined libecillide-penicillin treatment. A depressing effect on antipenicillin antibody titers detected by passive hemaglutination was also manifest in some patients. The overall tolerance of libecillide in allergic patients has been very good. Nevertheless, the major obstacle to a wider general use of libecillide at the present time appears to be the occurrence of positive skin reactions to that compound in approximately 5 percent of patients allergic to penicillin.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
LADOSTIGIL, a rasagiline derivative, is a reversible acetylcholinesterase and butyrylcholinesterase inhibitor with neuroprotective properties. It also acts as an irreversible brain monoamine oxidases inhibitor. It is under development for the treatment of neurodegenerative disorders like dementia and Alzheimer's disease.
Status:
Investigational
Source:
INN:bimosiamose [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bimosiamose, discovered by Encysive Pharmaceutical and presently being developed by Revotar Biopharmaceuticals, is an 863 g/mol molecular weight dimer with minimal carbohydrate content and is, to date, the leading selectin inhibitor in clinical development. It was developed as anti-inflammatory drug fir the treatment of acute chronic inflammatory disorders including COPD. This compound has shown promise in a phase IIa 'proof of concept' trial in patients with asthma, reducing airway recruitment of eosinophils after intravenous administration. In acute lung injury, neutrophils (a type of white blood cells, thus belonging to the group of cells of the body’s defence system-the immune system) are drawn to the small lung bloodvessels and migrate into the air sacs (alveoli). There they release substances, which cause the inflammation leading to further destruction of the lung tissue. Bimosiamose disodium is expected to hinder the migration of these neutrophils into the alveoli.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Efipladib is an inhibitor of cytosolic phospholipase A2 alpha both in vitro and in vivo. It is able to relieve inflammatory pain in animal model. Additionally, efipladib exerts antitumor potential. Efipladib was in clinical trials for the treatment of asthma and arthritis however its development has been discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Fosquidone (also known as GR63178A), a pentacyclic pyrroloquinone that was developed as an anticancer agent. Fosquidone participated in phase II clinical trial for the treatment of patients with colorectal, renal and non-small cell lung cancer. However, the drug didn’t show significant antitumor activity. The further development of this drug was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Fospirate is an organophosphorus insecticide used in veterinary as an anthelmintic agent.
Class (Stereo):
CHEMICAL (RACEMIC)
Fluprofen was invented as an analgesic and anti-inflammatory agent. However, information about the current use of this drug is not available.
Status:
Investigational
Source:
INN:evobrutinib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Evobrutinib is a highly selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK). It potently inhibits BCR- and Fc receptor-mediated signaling and, thus, subsequent activation and function of B cells and innate immune cells such as monocytes and basophils. Evobrutinib demonstrated effectivity in autoimmune disease preclinical models. Evobrutinib is being developed by Merck Serono for the treatment of various autoimmune disorders.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Emricasan (IDN- 6556 or PF-03491390) (3-[2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid) is a pan-caspase inhibitor. Testing in vitro enzyme assays demonstrated that emricasan efficiently inhibits all human caspases at low nanomolar concentrations. Preclinically, emricasan was effective in inhibiting apoptosis of sinusoidal endothelial cells. Emricasan has marked efficacy in models of liver disease after oral administration and thus, is an excellent candidate for the treatment of liver diseases characterized by excessive apoptosis. This drug is a first-in-class anti-apoptotic caspase inhibitor with demonstrated preliminary efficacy in liver-impaired patients in humans.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Netobimin is a carbamate compound which is used as an anthelmintic drug in veterinarymedicine. Netobimin-containing products are available as liquid suspensions which are intendedfor oral administration. Products are available for sheep and cattle. An oral dose of 7.5 mg/kg bw is recommended for the treatment of gastrointestinal infestations of roundworms and tapeworms;and 20 mg/kg bw is recommended for type II ostertagiasis and adult flukes. In order to be pharmacologically active, netobimin needs to be converted to the broad spectrumanthelmintic drug albendazole, by the splitting off of a side-chain and the formation of abenzimidazole group. This occurs naturally in the ruminant gut.
