Carboxamides

Eliglustat, sold under the brand name Cerdelga, is a medication used for the treatment of Gaucher's disease. It was discovered at the University of Michigan, developed by Genzyme Corp, and was approved by the FDA in August 2014. Commonly used as the tartrate salt, the compound is believed to work by inhibition of glucosylceramide synthase. According to an article in Journal of the American Medical Association the oral substrate reduction therapy resulted in "significant improvements in spleen volume, hemoglobin level, liver volume, and platelet count" in untreated adults with Gaucher disease T

Tranilast (INN, brand name Rizaben) is an antiallergic drug. It was developed by Kissei Pharmaceuticals and was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in the 1980s.

Clofibride is a fibrate. Clofibride is a derivative of clofibrate. In the body it is converted into 4-chlorophenoxyisobutyric acid (clofibric acid), which is the true hypolipidemic agent. So clofibride, just like clofibrate is a prodrug of clofibric acid.

Boscalid is a broad spectrum fungicide used in agriculture to protect crops from fungal diseases. It was first marketed by BASF in 2002 using their brand name Endura. The compound is an biphenyl amide derived inhibitor of succinate dehydrogenase.

Asciminib, sold under the brand name Scemblix, is a medication used to treat Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML). Asciminib is a protein kinase inhibitor.

Saripidem is a sedative and anxiolytic drug in the imidazopyridine family, which is related to the better known drugs zolpidem and alpidem.

Mirfentanil is a fentanyl derivative with strong selectivity for the μ opioid receptor. At lower doses, it antagonizes the analgesic effects of alfentanil and substitutes for naloxone in morphine-treated monkeys; however, it also reverses naloxone-precipitated withdrawal in pigeons trained to discriminate morphine from naloxone.

Eclanamine (U-48,753) is a drug which was patented as an antidepressant, but was never marketed. It acts by inhibiting the reuptake of serotonin and norepinephrine.

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.

Ageliferin is a chemical compound produced by some sponges. It was first isolated from Caribbean and then Okinawan marine sponges in the genus Agelas. It often co-exists with the related compound sceptrin and other similar compounds. It has antibacterial properties and can cause biofilms to dissolve. Total syntheses have been independently accomplished by the research groups of Phil S. Baran at the Scripps Research Institute, Chuo Chen at UT Southwestern Medical Center, Patrick Harran at UCLA, and Daisuke Urabe at Toyama Prefectural University.

Bunaftine (or bunaphtine) is an antiarrhythmic agent. It is classified in class III.

chemical compound

SB-431542 is a drug candidate developed by GlaxoSmithKline (GSK) as an inhibitor of the activin receptor-like kinase (ALK) receptors, ALK5, ALK4 and ALK7. However, it is not an inhibitor of anaplastic lymphoma kinase (which are commonly known as ALK inhibitors).

chemical compound

JTV-519 (K201) is a 1,4-benzothiazepine derivative that interacts with many cellular targets. It has many structural similarities to diltiazem, a Ca2+ channel blocker used for treatment of hypertension, angina pectoris and some types of arrhythmias. JTV-519 acts in the sarcoplasmic reticulum (SR) of cardiac myocytes by binding to and stabilizing the ryanodine receptor (RyR2) in its closed state. It can be used in the treatment of cardiac arrhythmias, heart failure, catecholaminergic polymorphic ventricular tachycardia (CPVT) and store overload-induced Ca2+ release (SOICR). Currently, this drug

Tenonitrozole is an antiprotozoal agent. ==References==

BOL-148, also known as 2-bromo-LSD or as bromolysergide, is a non-hallucinogenic serotonin receptor modulator of the lysergamide family related to the psychedelic drug lysergic acid diethylamide (LSD). It is specifically the 2-bromo derivative of LSD.

Talnetant (SB-223,412) is a neurokinin 3 receptor antagonist developed by GlaxoSmithKline, which is being researched for several functions (primarily treatment of irritable bowel syndrome, despite a 2007 study finding no statistically significant improvement in rectal hypersensitivity over placebo). Its use as a potential antipsychotic drug for the treatment of schizophrenia has also been discontinued.

'''N-Oxalylglycine''' is the organic compound with the formula HO2CC(O)NHCH2CO2H. This colourless solid is used as an inhibitor of α-ketoglutarate-dependent enzymes. It is isosteric with α-Ketoglutaric acid. Such enzymes are pervasive and, for example, are required for the synthesis of 4-hydroxyproline.

CP-532,903 is a selective adenosine A3 subtype receptor agonist. It has antiinflammatory effects and has been shown to reduce superoxide generation in damaged tissues, and protects against tissue damage following myocardial ischemia, mediated via an interaction with ATP-sensitive potassium channels.

Abitesartan (INN) is an Angiotensin II receptor antagonist.

class of chemical compounds

Monatepil is a calcium channel blocker and α1-adrenergic receptor antagonist used as an antihypertensive.

chemical compound

Repinotan (BAYx3702), an aminomethylchroman derivative, is a selective 5-HT1A receptor full agonist with high potency and efficacy. It has neuroprotective effects in animal studies, and was trialed in humans for reducing brain injury following head trauma. It was subsequently trialed up to phase II for treatment of stroke, but while side effects were mild and consisted mainly of nausea, repinotan failed to demonstrate sufficient efficacy to justify further clinical trials. However, repinotan continues to be investigated for other applications, and was found to be effective at counteracting the

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.

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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.

Prethcamide, sold under the brand name Micoren, is a respiratory stimulant composed of two related drugs, cropropamide and crotethamide. It was developed by Ciba-Geigy.

Cinepazide or cinepazide maleate (Kelinao or Anjieli in China) is a vasodilator used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases. It appears to work by potentiating A2 adenosine receptors.

Phenylacetylglutamine is a product formed by the conjugation of phenylacetate and glutamine. It is a common metabolite that occurs naturally in human urine.

Tenidap was a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate that was under development by Pfizer as a promising potential treatment for rheumatoid arthritis, but Pfizer halted development after marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage.

Lapaquistat (TAK-475) is a cholesterol-lowering drug candidate that was abandoned before being marketed.

Semagacestat (LY-450139) was a candidate drug for a causal therapy against Alzheimer's disease. It was originally developed by Eli Lilly and Elan, and clinical trials were conducted by Eli Lilly. Phase III trials included over 3000 patients, but in August 2010, a disappointing interim analysis, in which semagacestat performed worse than the placebo, led to the trials being stopped.

JNJ-7777120 was a drug being developed by Johnson & Johnson Pharmaceutical Research & Development which acts as a potent and selective antagonist at the histamine H4 receptor. It has anti-inflammatory effects, and has been demonstrated to be superior to traditional (H1) antihistamines in the treatment of pruritus (itching). The drug was abandoned because of its short in vivo half-life and hypoadrenocorticism toxicity in rats and dogs, that prevented advancing it into clinical studies.

Rocaglamide is a natural product which belongs to a class of molecules called flavaglines. This compound was isolated in 1982 by Ming-Lu King (金明儒) and colleagues based on its antileukemic activity. The name of Rocaglamide is named from two parts: Roc- and aglamide. Roc- means Republic of China (中華民國), where this product was first isolated; aglamide indicates this product is isolated from Large-leaved Aglaia (Scientific name: Aglaia rimosa

A-836,339 is a drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist. It is selective for CB2, with Ki values of 0.64 nM at CB2 vs 270 nM at the psychoactive CB1 receptor, but while it exhibits selective analgesic, anti-inflammatory and anti-hyperalgesic effects at low doses, its high efficacy at both targets results in typical cannabis-like effects appearing at higher doses, despite its low binding affinity for CB1. In 2012 A-836,339 was detected via X-ray crystallography in a "dubious product" sold in Japan, though the product was described a

Hydracarbazine is a pyridazine that has found use as an antihypertensive agent.

Bupicomide is a chemical compound created and manufactured by Lanospharma Laboratories Company, Ltd. It is used experimentally as a beta blocker and clinically as a strong vasodilator with the noted side effects of reduced systolic, diastolic and mean arterial pressure.

Rifalazil (also known as KRM-1648 and AMI-1648) is an antibiotic substance that kills bacterial cells by blocking off the β-subunit in RNA polymerase. Rifalazil is used as a treatment for many different diseases. The most common are Chlamydia infection, Clostridioides difficile associated diarrhea (CDAD), and tuberculosis (TB). Using rifalazil and the effects that coincide with taking rifalazil for treating a bacterial disease vary from person to person, as does any drug put into the human body. Food interactions and genetic variation are a few causes for the variation in side effects from the

chemical compound

chemical compound

Mizoribine (INN; MZB; trade name Bredinin) is an immunosuppressive drug. The compound was first observed in Tokyo, Japan, in 1971. It was first isolated from the fungus Penicillium brefeldianum. Mizoribine is an imidazole nucleoside that has been used in renal transplantation, and in steroid-resistant nephrotic syndrome, IgA nephropathy, lupus, as well as for adults with rheumatoid arthritis, lupus nephritis and other rheumatic diseases. MZB exerts its activity through selective inhibition of inosine monophosphate dehydrogenase and guanosine monophosphate synthetase, resulting in the complete

Orteronel (TAK-700) is a nonsteroidal CYP17A1 inhibitor that was being developed for the treatment of cancer by Takeda Pharmaceutical Company in conjunction with Millennium Pharmaceuticals. It completed two phase III clinical trials for metastatic, hormone-refractory prostate cancer but failed to extend overall survival rates, and development was voluntarily terminated as a result.

Adatanserin (WY-50,324, SEB-324) is a mixed 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2C receptor antagonist. It was under development by Wyeth as an antidepressant but was ultimately not pursued.

Cresomycin is an experimental antibiotic. It binds to the bacterial ribosome in both Gram-negative and Gram-positive bacteria, and it has been found to be effective against multi-drug-resistant stains of Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. It belongs to the bridged macrobicyclic oxepanoprolinamide antibiotics, which have similarities with lincosamides antibiotics.

ICI-190,622 is an anxiolytic drug used in scientific research. It is a pyrazolopyridine derivative, related to other anxiolytic compounds such as tracazolate, and more distantly to zaleplon. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.

JTE-907 is a drug used in scientific research that acts as a selective CB2 inverse agonist. It has anti-inflammatory effects in animal studies, thought to be mediated by an interaction between the CB2 receptor and IgE.

Prochloraz, brand name Sportak, is an imidazole fungicide that was introduced in 1978 and is widely used in Europe, Australia, Asia, and South America within gardening and agriculture to control the growth of fungi. It is not registered for use in the United States.

BP-897 is a drug used in scientific research which acts as a potent selective dopamine D3 receptor partial agonist with an in vitro intrinsic activity of ~0.6 and ~70x greater affinity for D3 over D2 receptors and is suspected to have partial agonist or antagonist activity in vivo. It has mainly been used in the study of treatments for cocaine addiction. A study comparing BP-897 with the potent, antagonistic, and highly D3 selective SB-277,011-A found, "SB 277011-A (1–10 mg/kg) was able to block cue-induced reinstatement of nicotine-seeking, indicating that DRD3 selective antagonism may be an

Glycidamide is an organic compound with the formula H2NC(O)C2H3O. It is a colorless oil. Structurally, it contains adjacent amides and epoxide functional groups. It is a bioactive, potentially toxic or even carcinogenic metabolite of acrylonitrile and acrylamide. It is a chiral molecule.

Linomide (Roquinimex) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity. It also inhibits angiogenesis and reduces the secretion of TNF alpha.

Coronatine (COR) is a toxin produced by the bacterium Pseudomonas syringae. It is involved in causing stomata to re-open after they close in response to pathogen-associated molecular patterns, as well as interfering with the responses mediated by salicylic acid after the infection has begun. It consists of coronafacic acid (CFA), which is an analog of methyl jasmonic acid (MeJA), and coronamic acid (CMA), joined by an amide bond between the acid group of CFA and the amino group of CMA.

Ritlecitinib, sold under the brand name Litfulo, is a medication used for the treatment of severe alopecia areata (hair loss). Ritlecitinib is a kinase inhibitor which inhibits Janus kinase 3 and tyrosine kinase.

Pivagabine (INN; brand name Tonerg), also known as '''N-pivaloyl-γ-aminobutyric acid or N-pivaloyl-GABA''', is an antidepressant and anxiolytic drug which was introduced in Italy in 1997 for the treatment of depressive and maladaptive syndromes. But it was discontinued in Italy (according to Martindale). Originally believed to function as a prodrug to GABA, pivagabine is now believed to act somehow via modulation of corticotropin-releasing factor (CRF).

JDTic is a selective, long-acting ("inactivating") antagonist of the κ-opioid receptor (KOR). JDTic is a 4-phenylpiperidine derivative, distantly related structurally to analgesics such as pethidine and ketobemidone, and more closely to the MOR antagonist alvimopan. In addition, it is structurally distinct from other KOR antagonists such as norbinaltorphimine. JDTic has been used to create crystal structures of KOR [ ].

Luminespib (INN, previously known as NVP-AUY922) is an experimental drug candidate for the treatment of cancer. It was discovered through a collaboration between The Institute of Cancer Research and the pharmaceutical company Vernalis and licensed to Novartis. From 2011 to 2014 it was in Phase II clinical trials. Chemically it is a resorcinylic isoxazole amide

Tiazofurin is a drug which acts as an inhibitor of the enzyme IMP dehydrogenase. Tiazofurin and its analogues were under investigation for potential use in the treatment of cancer, though side effects such as pleuropericarditis and a flu-like syndrome precluded further development. They also show antiviral effects and may be reevaluated as potential options in the treatment of newly emerging viral diseases. ==Synthesis== [[File:Tiazofurin synthesis.svg|thumb|center|500px|ChemDrug Synthesis:]] The treatment of 1-O-Acetyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranose [6974-32-9] (1) with trimethylsily

Pyrrolidonyl-β-naphthylamide (PYR) is a molecule used in microbiology to detect the presence of pyrrolidonyl peptidase. In the presence of bacteria with pyrrolidonyl peptidase, it is broken down to pyroglutamic acid and 2-naphthylamine. To detect this process, p-dimethylaminocinnamaldehyde is added and a change to a pink color can then be detected.

chemical compound