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Category

Fluoroarenes

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eperezolid
Eperezolid is an oxazolidinone antibiotic.
orforglipron
Orforglipron, sold under the brand name Foundayo, is an oral, non-peptide, small-molecule GLP-1 receptor agonist developed as a weight loss drug by Eli Lilly and Company. It was discovered by Chugai Pharmaceutical Co., then was licensed to Lilly in 2018.
drinabant
Drinabant (INN; AVE-1625) is a drug that acts as a selective CB1 receptor antagonist, which was under investigation varyingly by Sanofi-Aventis as a treatment for obesity, schizophrenia, Alzheimer's disease, Parkinson's disease, and nicotine dependence. Though initially studied as a potential treatment for a variety of different medical conditions, Sanofi-Aventis eventually narrowed down the therapeutic indications of the compound to just appetite suppression. Drinabant reached phase IIb clinical trials for this purpose in the treatment of obesity but was shortly thereafter discontinued, likel
oteseconazole
Oteseconazole, a novel tetrazole containing orally bioavailable and selective inhibitor of fungal lanosterol 14α-demethylase (CYP51), has shown promising efficacy in the treatment of recurrent vulvovaginal candidiasis (RVVC).
telcagepant
Telcagepant (INN; development code MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co.
laropiprant
Laropiprant (INN) was a drug used in combination with nicotinic acid to reduce blood cholesterol (LDL and VLDL) that is no longer sold, due to increases in side-effects with no cardiovascular benefit. Laropiprant itself has no cholesterol lowering effect, but it reduces facial flushes induced by nicotinic acid.
tarenflurbil
Tarenflurbil, Flurizan or '''R-flurbiprofen''', is a single enantiomer of the racemate NSAID flurbiprofen. For several years, research and trials for the drug were conducted by Myriad Genetics, to investigate its potential as a treatment for Alzheimer's disease; that investigation concluded in June 2008 when the company announced it would discontinue development of the compound.
sotorasib
Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for various forms of cancer. Sotorasib is an inhibitor of the RAS GTPase family.
albaconazole
Albaconazole (development code UR-9825) is an experimental triazole antifungal. It has potential broad-spectrum activity. The drug blocks a number of CYP450 liver enzymes.
talazoparib
Talazoparib, sold under the brand name Talzenna, is an anti-cancer medication used for the treatment of breast cancer and prostate cancer. It is an orally available poly ADP ribose polymerase (PARP) inhibitor marketed by Pfizer for the treatment of advanced breast cancer with germline BRCA mutations. Talazoparib is similar to the first in class PARP inhibitor, olaparib.
cimicoxib
Cimicoxib (UR-8880 trade name Cimalgex) is a nonsteroidal anti-inflammatory drug (NSAID) used in veterinary medicine to treat dogs for pain and inflammation associated with osteoarthritis and for the management of pain and inflammation associated with surgery. It acts as a COX-2 inhibitor.
vestipitant
Vestipitant (INN) is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitus and insomnia.
ravuconazole
Ravuconazole (codenamed BMS-207147 and ER-30346) is a potent triazole antifungal, the development of which was discontinued in 2007. The drug has shown to have a similar spectrum of activity to voriconazole, with an increased half-life. However, ravuconazole has limited activity against species of Fusarium, Scedosporium, and Zygomycetes.
sarolaner
Sarolaner, sold under the brand name Simparica, is an ectoparasiticide veterinary medication for the treatment of flea and tick infestations in dogs. It is also used off-label to control sarcoptic mange and demodectic mange.
bictegravir
Bictegravir (INN; BIC, formerly known as GS-9883) is a second-generation integrase inhibitor (INSTI) class that was structurally derived from an earlier compound dolutegravir by scientists at Gilead Sciences. In vitro and clinical results were presented by Gilead in the summer of 2016. In 2016, bictegravir was in a Phase 3 trial as part of a single tablet regimen in combination with tenofovir alafenamide (TAF) and emtricitabine (FTC) for the treatment of HIV-1 infection.
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin hydrochloride
UH-301, also known as '(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin ((S)-5-FHDPAT'), is a drug and research chemical widely used in scientific studies. It acts as a selective serotonin 5-HT1A receptor silent antagonist. It is structurally related to 8-OH-DPAT. UH-301 was found to produce a head-twitch response in mice which is usually typical of 5-HT2A agonist drugs, and has subsequently been used to investigate how 5-HT1A receptor activity modulates 5-HT2A receptors downstream.
zoliflodacin
Zoliflodacin, sold under the brand name Nuzolvence, is an antibiotic used for the treatment of antibiotic-resistant Neisseria gonorrhoeae (gonorrhea). Zoliflodacin is being developed as part of a public-private partnership between Innoviva Specialty Therapeutics and the Global Antibiotic Research & Development Partnership (GARDP). Zoliflodacin is taken by mouth.
eravacycline
Eravacycline (TP-434, Xerava) is a synthetic halogenated tetracycline class antibiotic by Tetraphase Pharmaceuticals. It is closely related to tigecycline. It has a broad spectrum of activity including many multi-drug resistant strains of bacteria. Phase III studies in complicated intra-abdominal infections (cIAI) and complicated urinary tract infections (cUTI) were recently completed with mixed results. Eravacycline was granted fast track designation by the FDA and is currently available in USA.
cipargamin
Cipargamin (also known as KAE609 or NITD609) is a synthetic antimalarial compound belonging to the novel spiroindolone drug class. Developed by Novartis Institute for Tropical Diseases in Singapore, through a collaboration with the Genomics Institute of the Novartis Research Foundation (GNF), the Biomedical Primate Research Centre and the Swiss Tropical Institute, cipargamin represents a promising next-generation antimalarial drug currently undergoing Phase II clinical trials with a particular focus on safety evaluation. Cipargamin was awarded MMV Project of the Year 2009.
pradofloxacin
Pradofloxacin, sold under the brand name Veraflox among others, is a third-generation enhanced spectrum veterinary antibiotic of the fluoroquinolone class. It was developed by Elanco Animal Health GmbH and received approval from the European Commission in April 2011, for prescription-only use in veterinary medicine for the treatment of bacterial infections in dogs and cats.
pirtobrutinib
Pirtobrutinib, sold under the brand name Jaypirca, is an anti-cancer medication that is used to treat mantle cell lymphoma. It inhibits B cell lymphocyte proliferation and survival by binding and inhibiting Bruton's tyrosine kinase (BTK). It is taken by mouth.
nepicastat
Nepicastat (; developmental code names SYN117, RS-25560-197) is an inhibitor of dopamine β-hydroxylase (DBH), an enzyme that catalyzes the conversion of dopamine to norepinephrine.
efinaconazole
Efinaconazole, sold under the brand name Jublia and Clenafin among others, is a triazole antifungal compound discovered by Kaken Pharmaceutical, indicated for the treatment of onychomycosis, a fungal infection of the nail. Since it has low binding affinity with keratin, the main component of nails, it has superior nail-penetrating properties. It is approved for use in the United States, Canada, Japan and certain European countries as a 10% topical solution.
sutezolid
Sutezolid is an investigational new drug that is being evaluated for the treatment of extensively drug-resistant tuberculosis. It differs from linezolid by replacement of the morpholine oxygen with a sulfur atom. Like linezolid, sutezolid is a bacterial protein synthesis inhibitor. In preclinical studies, sutezolid demonstrated superior antituberculosis activity compared to linezolid.
manifaxine
Manifaxine (developmental code name GW-320,659) is a norepinephrine–dopamine reuptake inhibitor developed by GlaxoSmithKline through structural modification of radafaxine, an isomer of hydroxybupropion and one of the active metabolites of bupropion. Manifaxine was researched for treatment of attention deficit hyperactivity disorder (ADHD) and obesity and was found to be safe, reasonably effective, and well-tolerated for both applications. However, no results were reported following these initial trials and development was discontinued.
SB357134
SB-357134 is a drug which is used in scientific research. It acts as a potent, selective and orally active 5-HT6 receptor antagonist. SB-357134 and other 5-HT6 antagonists show nootropic effects in animal studies, and have been proposed as potential novel treatments for cognitive disorders such as schizophrenia and Alzheimer's disease.
ipragliflozin
Ipragliflozin (INN, trade names Suglat) is a pharmaceutical drug for treatment of type 2 diabetes. Ipragliflozin, jointly developed by Astellas Pharma and Kotobuki Pharmaceutical, was approved in Japan on January 17, 2014, and in Russia on May 22, 2019.
toceranib
Toceranib (INN), sold under the brand name Palladia, is a receptor tyrosine kinase inhibitor that is used in the treatment of canine mast cell tumor also called mastocytoma. It is the first medication developed specifically for the treatment of cancer in dogs. It is used as its phosphate salt, toceranib phosphate. It was developed by SUGEN as SU11654, a sister compound to sunitinib, which was later approved for human therapies. Toceranib is a tyrosine kinase inhibitor and works in two ways: by killing tumor cells and by cutting off the blood supply to the tumor.
deracoxib
Deracoxib (trade name Deramaxx) is a nonsteroidal anti-inflammatory drug (NSAID) of the coxib class, used in dogs to treat pain associated with osteoarthritis, or to prevent pain following orthopedic or dental surgery. It is available as beef-flavored tablets.
sorbinil
Sorbinil (INN) is an aldose reductase inhibitor being investigated for treatment of diabetic complications including neuropathy and retinopathy. Aldose reductase is an enzyme present in lens and brain that removes excess glucose by converting it to sorbitol. Sorbitol accumulation can lead to the development of cataracts in the lens and neuropathy in peripheral nerves. Sorbinil has been shown to inhibit aldose reductase in human brain and placenta and calf and rat lens. Sorbinil reduced sorbitol accumulation in rat lens and sciatic nerve of diabetic rats orally administered 0.25 mg/kg sorb
flufenoxuron
Flufenoxuron is an insecticide that belongs to the benzoylurea chitin synthesis inhibitor group, which also includes diflubenzuron, triflumuron, and lufenuron.
casopitant
Casopitant (), former tentative trade names Rezonic (U.S.) and Zunrisa (Europe), is an NK1 receptor antagonist which was undergoing research for the treatment of chemotherapy-induced nausea and vomiting. It was under development by GlaxoSmithKline. In July 2008, the company filed a marketing authorisation application with the European Medicines Agency. The application was withdrawn and development was discontinued in September 2009 because GlaxoSmithKline decided that further safety assessment was necessary. However, a 2022 review listed casopitant as under development as a potential novel ant
Robalzotan
Robalzotan (, ; developmental code names NAD-299, AZD-7371) is a selective antagonist at the serotonin 5-HT1A receptor which was under development for the treatment of major depressive disorder, anxiety disorders, gastrointestinal disorders, irritable bowel syndrome (IBS), and overactive bladder.
fosfluconazole
Fosfluconazole () is a water-soluble phosphate prodrug of fluconazole — a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.
Difludiazepam
Difludiazepam (Ro07-4065) is a benzodiazepine derivative which is the 2',6'-difluoro derivative of fludiazepam. It was invented in the 1970s but was never marketed, and has been used as a research tool to help determine the shape and function of the GABAA receptors, at which it has an IC50 of 4.1nM. Difludiazepam has subsequently been sold as a designer drug, and was first notified to the EMCDDA by Swedish authorities in 2017.
edivoxetine
Edivoxetine (INN; code name LY-2216684) is a drug which acts as a selective norepinephrine reuptake inhibitor and was under development by Eli Lilly for attention-deficit disorder (ADD) and as an antidepressant treatment. It was in phase III clinical trials in 2012 for major depressive disorder, but failed to get approval.
posizolid
Posizolid is an oxazolidinone antibiotic under investigation by AstraZeneca for the treatment of bacterial infections. At a concentration of 2 mg/L it inhibited 98% of all Gram-positive bacteria tested in vitro.
flosequinan
Flosequinan is a quinolone vasodilator that was discovered and developed by Boots UK and was sold for about a year under the trade name Manoplax. It had been approved in 1992 in the US and UK to treat people with heart failure who could not tolerate ACE inhibitors or digitalis.
L-838417
L-838,417 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. The compound was developed by Merck, Sharp and Dohme.
radezolid
Radezolid (INN, codenamed RX-1741) is a novel oxazolidinone antibiotic being developed by Melinta Therapeutics, Inc. for the treatment of bacterial acne.
Ro48-6791
Ro48-6791 is a drug, an imidazobenzodiazepine derivative developed by Hoffman-LaRoche in the 1990s.
entrectinib
Entrectinib, sold under the brand name Rozlytrek, is an anti-cancer medication used to treat ROS1-positive non-small cell lung cancer and NTRK fusion-positive solid tumors. It is a selective tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (TRK) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK).
fluorogesarol
Difluorodiphenyltrichloroethane (DFDT) is a chemical compound. Its composition is the same as that of the insecticide DDT, except that two of DDT's chlorine atoms are replaced by two fluorine atoms.
pentafluorophenol
Pentafluorophenol is the organofluorine compound (specifically a fluoroalcohol) with the formula . This is the perfluorinated analogue of phenol. It is a white solid that melts just above room temperature, and smells of phenol. With a pKa of 5.5, it is one of the most acidic phenols and can be easily deprotonated to pentafluorophenolate.
saflufenacil
Saflufenacil is the ISO common name for an organic compound of the pyrimidinedione chemical class used as an herbicide. It acts by inhibiting the enzyme protoporphyrinogen oxidase to control broadleaf weeds in crops including soybeans and corn.
2,5-dimethoxy-4-fluoroamphetamine
2,5-Dimethoxy-4-fluoroamphetamine (DOF) is a serotonin receptor modulator of the phenethylamine, amphetamine, and DOx families.
RWJ-51204
RWJ-51204 is an anxiolytic drug used in scientific research. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.
Ro60-0175
Ro60-0175, or Ro-600175, also known as '(S)-5-fluoro-6-chloro-α-methylisotryptamine ((S)-5-F-6-Cl-isoAMT'), is a serotonin 5-HT2 receptor agonist of the isotryptamine family developed by Hoffmann–La Roche, which has applications in scientific research. It is the enantiopure (S)- isomer of the 5-fluoro and 6-chloro derivative of α-methylisotryptamine (isoAMT).
acefluranol
Acefluranol (developmental code name BX-591), also known as 2,3-bis(3,4-diacetoxy-5-fluorophenyl)pentane, is a nonsteroidal antiestrogen of the stilbestrol group that was never marketed.
ranbezolid
Ranbezolid (RBx7644) is an oxazolidinone antibacterial. It competitively inhibits monoamine oxidase-A (MAO-A).
flucindole
Flucindole (, ; developmental code name WIN-35150) is an antipsychotic of the tetrahydrocarbazolamine family with a tricyclic cyclized tryptamine structure that was never marketed. It is the 6,8-difluoro derivative of ciclindole. The drug is about 5 to 10times more potent than ciclindole both in vitro and in vivo.
Ro48-8684
Ro48-8684 is a water-soluble benzodiazepine derivative developed by Hoffman-LaRoche in the 1990s, which was designed along with Ro48-6791 as an improved replacement for midazolam, but ultimately proved to have little advantages over the parent drug and has not been introduced into clinical practice.
5-fluoro-N,N-dimethyltryptamine
5-Fluoro-DMT, or 5-F-DMT, also known as '5-fluoro-N,N-dimethyltryptamine', is a psychedelic drug of the tryptamine family related to dimethyltryptamine (DMT) and to other psychedelic tryptamines like 5-chloro-DMT and 5-bromo-DMT.