Triazolopyridine
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Triazolopyridine
Triazolopyridines are a class of heterocyclic chemical compounds with a triazole ring fused to a pyridine ring. There are multiple isomers which differ by the location of the nitrogen atoms and the nature of the ring fusion. The term ''triazolopyridine'' can also refer to a class of antidepressant drugs whose chemical structure includes a trazolopyridine-derived ring system. One example is trazodone. Other pharmaceutical drugs that contain a triazolopyridine ring system include filgotinib, tucatinib, and enarodustat. In addition, the reagents used in organic chemistry HATU, HOAt, and PyAOP are triazolopyridine derivatives The derivative of a function is the rate of change of the function's output relative to its input value. Derivative may also refer to: In mathematics and economics * Brzozowski derivative in the theory of formal languages * Formal derivative, an .... References {{heterocyclic-stub ...
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Triazolopyridine Isomers
Triazolopyridines are a class of heterocyclic chemical compounds with a triazole ring fused to a pyridine ring. There are multiple isomers which differ by the location of the nitrogen atoms and the nature of the ring fusion. The term ''triazolopyridine'' can also refer to a class of antidepressant drugs whose chemical structure includes a trazolopyridine-derived ring system. One example is trazodone. Other pharmaceutical drugs that contain a triazolopyridine ring system include filgotinib, tucatinib, and enarodustat. In addition, the reagents used in organic chemistry HATU, HOAt, and PyAOP are triazolopyridine derivatives The derivative of a function is the rate of change of the function's output relative to its input value. Derivative may also refer to: In mathematics and economics * Brzozowski derivative in the theory of formal languages * Formal derivative, an .... References {{heterocyclic-stub ...
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Trazodone
Trazodone, sold under many brand names, is an antidepressant medication. It is used to treat major depressive disorder, anxiety disorders, and difficulties with sleep. The medication is taken orally. Common side-effects include dry mouth, feeling faint, vomiting, and headache. More serious side effects may include suicide, mania, irregular heart rate, and pathologically prolonged erections. It is unclear if use during pregnancy or breastfeeding is safe. It is a phenylpiperazine compound of the serotonin antagonist and reuptake inhibitor (SARI) class. Trazodone also has sedating effects. Trazodone was approved for medical use in the United States in 1981. It is available as a generic medication. In 2020, it was the 21st most commonly prescribed medication in the United States, with more than 26million prescriptions. Medical uses Depression The primary use of trazodone is the treatment of unipolar major depression with or without anxiety. Data from open and double-blind ...
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Heterocyclic
A heterocyclic compound or ring structure is a cyclic compound that has atoms of at least two different elements as members of its ring(s). Heterocyclic chemistry is the branch of organic chemistry dealing with the synthesis, properties, and applications of these heterocycles. Examples of heterocyclic compounds include all of the nucleic acids, the majority of drugs, most biomass (cellulose and related materials), and many natural and synthetic dyes. More than half of known compounds are heterocycles. 59% of US FDA-approved drugs contain nitrogen heterocycles. Classification The study of heterocyclic chemistry focuses especially on unsaturated derivatives, and the preponderance of work and applications involves unstrained 5- and 6-membered rings. Included are pyridine, thiophene, pyrrole, and furan. Another large class of heterocycles refers to those fused to benzene rings. For example, the fused benzene derivatives of pyridine, thiophene, pyrrole, and furan are quinol ...
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Triazole
A triazole is a heterocyclic compound featuring a five-membered ring of two carbon atoms and three nitrogen atoms with molecular formula C2H3N3. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. However, triazoles are also useful in bioorthogonal chemistry, because the large number of nitrogen atoms causes triazoles to react similar to azides. Lastly, the many free lone pairs in triazoles make them useful as coordination compounds, although not typically as haptic ligands. Isomerism There are four triazole isomers, which are conventionally divided into two pairs of tautomers. In the 1,2,3-triazoles, the three nitrogen atoms are adjacent; in the 1,2,4-triazoles, an interstitial carbon separates out one nitrogen atom. Each category has two tautomers that differ by which nitrogen has a hydrogen bonded ...
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Pyridine
Pyridine is a basic heterocyclic organic compound with the chemical formula . It is structurally related to benzene, with one methine group replaced by a nitrogen atom. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell. Pyridine is colorless, but older or impure samples can appear yellow, due to the formation of extended, unsaturated polymeric chains, which show significant electrical conductivity. The pyridine ring occurs in many important compounds, including agrochemicals, pharmaceuticals, and vitamins. Historically, pyridine was produced from coal tar. As of 2016, it is synthesized on the scale of about 20,000 tons per year worldwide. Properties Physical properties The molecular electric dipole moment is 2.2 debyes. Pyridine is diamagnetic and has a diamagnetic susceptibility of −48.7 × 10−6 cm3·mol−1. The standard enthalpy of formation is 100.2 kJ·mol−1 in the liquid phase ...
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Isomer
In chemistry, isomers are molecules or polyatomic ions with identical molecular formulae – that is, same number of atoms of each element – but distinct arrangements of atoms in space. Isomerism is existence or possibility of isomers. Isomers do not necessarily share similar chemical or physical properties. Two main forms of isomerism are structural or constitutional isomerism, in which ''bonds'' between the atoms differ; and stereoisomerism or spatial isomerism, in which the bonds are the same but the ''relative positions'' of the atoms differ. Isomeric relationships form a hierarchy. Two chemicals might be the same constitutional isomer, but upon deeper analysis be stereoisomers of each other. Two molecules that are the same stereoisomer as each other might be in different conformational forms or be different isotopologues. The depth of analysis depends on the field of study or the chemical and physical properties of interest. The English word "isomer" () is a back-for ...
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Filgotinib
Filgotinib, sold under the brand name Jyseleca, is a medication used for the treatment of rheumatoid arthritis (RA). It was developed by the Belgium, Belgian-Netherlands, Dutch biotech company Galapagos NV. The most common side effects include nausea (feeling sick), upper respiratory tract infection (nose and throat infection), urinary tract infection and dizziness. Filgotinib was approved for medical use in both the European Union and Japan in September 2020. Medical uses Filgotinib is Indication (medicine), indicated for the treatment of moderate to severe active rheumatoid arthritis in adults who have responded inadequately to, or who are intolerant to one or more disease‑modifying anti‑rheumatic drugs (DMARDs). Filgotinib may be used as monotherapy or in combination with methotrexate (MTX). Mechanism of action Filgotinib is a Janus kinase inhibitor with selectivity for subtype JAK1 of this enzyme. It is considered a promising agent as it inhibits JAK1 selectively, simi ...
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Tucatinib
Tucatinib, sold under the brand name Tukysa, is an anticancer medication used for the treatment of HER2-positive breast cancer. It is a small molecule inhibitor of HER2. It was developed by Array BioPharma and licensed to Cascadian Therapeutics (formerly Oncothyreon, subsequently part of Seattle Genetics). Common side effects include diarrhea, palmar-plantar erythrodysesthesia (burning or tingling discomfort in the hands and feet), nausea, fatigue, hepatotoxicity (liver damage), vomiting, stomatitis (inflammation of the mouth and lips), decreased appetite, abdominal pain, headache, anemia and rash. Tucatinib may cause harm to a developing fetus or baby. Tucatinib was approved for medical use in the United States in April 2020, in Australia in August 2020, and in the European Union in February 2021. Medical uses Tucatinib is a kinase inhibitor indicated in combination with trastuzumab and capecitabine for the treatment of adults with advanced unresectable or metastatic HER ...
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Enarodustat
Enarodustat (development code JTZ-951; brand name Enaroy) is a drug used for the treatment of anemia, especially when associated with chronic kidney disease (CKD). Enarodustat functions as a inhibitor of hypoxia inducible factor-proly hydroxylase (HIF-PH). The drug was approved in September 2020 in Japan for anemia associated with CKD and is currently in clinical development Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regu ... in the United States and South Korea. The drug is being developed by Japan Tobacco and JW Pharmaceutical. References Drugs acting on the blood and blood forming organs Alpha-Amino acids Triazolopyridines Secondary amino acids {{blood-drug-stub ...
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Reagent
In chemistry, a reagent ( ) or analytical reagent is a substance or compound added to a system to cause a chemical reaction, or test if one occurs. The terms ''reactant'' and ''reagent'' are often used interchangeably, but reactant specifies a substance ''consumed'' in the course of a chemical reaction. ''Solvents'', though involved in the reaction mechanism, are usually not called reactants. Similarly, ''catalysts'' are not consumed by the reaction, so they are not reactants. In biochemistry, especially in connection with enzyme-catalyzed reactions, the reactants are commonly called substrates. Definitions Organic chemistry In organic chemistry, the term "reagent" denotes a chemical ingredient (a compound or mixture, typically of inorganic or small organic molecules) introduced to cause the desired transformation of an organic substance. Examples include the Collins reagent, Fenton's reagent, and Grignard reagents. Analytical chemistry In analytical chemistry, a reagent ...
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HATU
HATU (1- is(dimethylamino)methylene1H-1,2,3-triazolo ,5-byridinium 3-oxide hexafluorophosphate, Hexafluorophosphate Azabenzotriazole Tetramethyl Uronium) is a reagent used in peptide coupling chemistry to generate an active ester from a carboxylic acid. HATU is used along with Hünig's base (''N,N''-diisopropylethylamine, DIPEA), or triethylamine to form amide bonds. Typically DMF is used as solvent, although other polar aprotic solvents can also be used. History HATU was first reported by Louis A. Carpino in 1993 as an efficient means of preparing active esters derived from 1-hydroxy-7-azabenzotriazole (HOAt). HATU can exist as either the uronium salt (''O-''form) or the less reactive iminium salt (''N''-form). HATU was initially reported as the O-form using the original preparation reported by Carpino; however, X-ray crystallographic and NMR studies revealed the true structure of HATU to be the less reactive guanidinium isomer. It is, however, possible to obtain the uronium i ...
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HOAt
1-Hydroxy-7-azabenzotriazole (HOAt) is a triazole used as a peptide coupling reagent In organic chemistry, peptide synthesis is the production of peptides, compounds where multiple amino acids are linked via amide bonds, also known as peptide bonds. Peptides are chemically synthesized by the condensation reaction of the carboxyl .... It suppresses the racemization. HOAt has a melting point between 213 and 216 degrees Celsius. As a liquid, it is transparent and without any color. References Peptide coupling reagents Triazolopyridines Reagents for biochemistry Hydroxylamines {{heterocyclic-stub ...
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