Derivados de Quinazolina e Quinolina

<p>Stability Hygroscopic, Unstable in Solution<br>Applications Tadalafil Ketolactam is a Tadalafil (T004500) impurity.<br></p>

<p>Impurity Felodipine EP Impurity C<br>Applications Nemadipine B (Felodipine EP Impurity C) is the diethyl ester analogue analogue of the calcium channel blocker Felodipine (F232375) with antihypertensive activity.<br>References Berntsson, P. et al.: J. Cardio. Pharmacol., 10, S60 (1987); Kwok, T.C. et al.: Nature, 441, 91 (2008);<br></p>

<p>Applications Dimetindene derivative, a histaminic H1 receptor antagonist.<br></p>

<p>Applications N-Despropyl-macitentan, is an active metabolite which is part of a family of endothelin receptor antagonist that allows for treatment of pulmonary arterial hypertension (PAH)<br>References Atsmon, J., et al.: Clin. Pharmacokinet., 525, 685 (2013); Sidharta, P.N., et al.: Clin. Drug Invest. (2014)<br></p>

<p>Applications A pesticide, like other BPUs it interferes with chitin synthesis.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Yamada, R., et al.: Biosci., Biotechnol., Biochem., 70, 54 (2006), Kryger, U., et al.: Vet. Parasitol., 143, 380 (2007), Arakawa, T., et al.: App. Entomol. Zool., 43, 167 (2008),<br></p>

<p>Stability Hygroscopic<br>Applications A metabolite of Mosapride (M731000).<br>References Chen, H., et al.: J. Pharm. Biomed. Anal., 40, 142 (2006), Pedraglio, S., et al.: J. Pharm. Biomed. Anal., 44, 665 (2007), Christopher, L., et al.: Drug Metab. Dispos., 36, 1341 (2008), Curran, M., et al.: Drugs, 68, 981 (2008),<br></p>

<p>Applications α2-Adrenergic agonist. Antihypertensive; analgesic for neuropathic pain.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Roach, A.G., et al.: J. Pharmacol. Exp. Ther., 227, 421 (1983), Glassman, A.H., et al.: Science, 226, 864 (1984), Abounassif, A.M., et al.: Anal. Profiles Drug Subs. Excip., 21, 109 (1992),<br></p>

<p>Applications 6-Hydroxy Chlorzoxazone-d2 is a labeled analogue of 6-Hydroxy Chlorzoxazone (H825120), A major metabolite of chlorzoxazone and formed by the actions of cytochrome P450IIE1.<br>References Twele, et al.: Arzneim.-Forsch., 32, 759 (1982); Peter, et al.: che. Res. Toxicol., 3, 566 (1990)<br></p>

<p>Applications Niclosamide Ethanolamine Salt is an ethanolamine salt of Niclosamide (N395500), which is used as an anthelmintic drug (Cestodes)<br>References Loftsson, T., et al.: J. Pharm. Sci., 85, 1017 (1996), Malik, N., et al.: Anti. Cancer Drugs, 10, 767 (1999), El-Sayed, M., et al.: Pharm. Res., 18, 23 (2001),<br></p>

<p>Applications Labelled (R)-Pramipexole enantiomer. A dopamine-D2-receptor agonist. Antiparkinsonian.<br>References Mierau, J., et al.: J. Med. Chem., 30, 494 (1987), Schilling, J.C., et al.: Clin. Pharmacol. Ther., 51, 541 (1992), Kieburtz, K., et al.: J. Am. Med. Assoc., 278, 125 (1997)<br></p>

<p>Impurity Nisoldipine<br>Applications Dehydronitrosonisoldipine is an impurity of Nisoldipine (N489125). Nisoldipine is a dihydropyridine calcium channel blocker and it is antihypertensive and antianginal.<br>References Kazda, S., et al.: Arzneimittel-Forsch., 30, 2144 (1980); Pasanisi, F., et al.: Eur. J. Clin. Pharmacol., 29, 21 (1985); Lam, J., et al.: J. Am. Col. Cardiol., 6, 447 (1985)<br></p>

<p>Applications An immune response modifier. It stimulates the production of interferon-a.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Megyeri, K., et al.: Mol. Cell Biol., 15, 2207, (1995), Witt, P.L., et al.: Cancer Res., 53, 5176 (1993), Edwards, L., et al.: Arch. Dermatol., 134, 25 (1998)<br></p>

<p>Applications 5’-[(Desloratidine)methyl] Rupatadine is an impurity of the antihistaminic drug Rupatadine (R701650).<br>References Wang, H. et al.: Yao. Fen. Zaz., 29, 791 (2009);<br></p>

<p>Applications Acetohydrazide is a metabolite of Isoniazid (I821450) an antibiotic for treatment of Mycobacterium tuberculosis, inhibits mycolic acid biosynthesis.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Metushi, I.G., et al.: Chem. Res. Toxciol., 25, 2567 (2012); Fukino, K., et al.: J. Toxicol. Sci., 33, 667 (2008);<br></p>

<p>Applications The active metabolite of Leflunomide, a potent disease-modifying antirheumatic drug used in the treatment of rheumatoid arthritis. LEF-M interferes with dendritic cell function.<br>References Kirsch, B.M., et al.: Arthritis Research and Therapy, 7, 3, R694, (2005)<br></p>

<p>Applications Deracoxib is a non-steroidal anti-inflammatory drug (NSAID) of the coxib class. Deracoxin is a selective cyclooxygenase-2 (COX-2) inhibitor used in the treatment of osteoarthritis in dogs. At low doses, adminsitartion of Deracoxin showed no factors associated with gastrointestinal tract perforation.<br>References Lascelles, B.D.X. et al.: J. Am. Vet. Med. Assoc., 227, 1112 (2005); Anderson, G.D. et al.: Inflam. Res., 58, 109 (2009); Brainard, B.M. et al.: Am. J. Vet. Res., 68, 251 (2007);<br></p>

<p>Applications Empagliflozin R/S-Furanose is a mixture of R and S isomers of Empagliflozin Furanose. Both are byproducts in the synthesis of Empagliflozin drug (E521510), which is potent and selective inhibitor of sodium glucose co-transporter-2 (SGLT-2).<br>References Thomas, L., et al.: Diabetes. Obesity. Metabol. 14, 94 (2012); Grempler, R., et al.: Diabetes. Obesity. Metabol., 14, 83 (2012); Wang, X., et al.: Org. Lett., 16, 4090 (2014);<br></p>

<p>Amiodarone (Cordarone) is an antiarrhythmic compound that induces pulmonary toxicity and inhibits ATP-sensitive potassium channels.</p>

<p>Applications A labelled metabolite of Olanzapine.<br>References Jacobsen, E., et al.: Acta Pharmacol. Toxacol., 11, 135 (1955), Chakrabarti, J.K., et al.: J. Med. Chem., 23, 878 (1980), Luo, H., et al.: J. Pharm. Sci., 11, 1079 (1992), Moore, N.A., et al.: Curr. Opin. Invest. Drugs, 2, 281 (1993),<br></p>

<p>Applications Aripiprazole Hydrate is an agonist at the dopamine autoreceptor and an antagonist at the postsynaptic D2 receptor (1,2,3,4). Aripiprazole is an antipsychotic and a potential drug candidate for treating psychoses such as schizophrenia.<br>References Pan, B., et al.: Psychopharmacology, PagesAhead of Print( 2019), Kim, J. Y., et al.: Anticancer Res., 38, 5101 (2018)<br></p>

<p>Applications 4-Amino-3,5-dichloropyridine is a metabolite of the selective phosphodiesterase 4 (PDE4) inhibitor, Roflumilast (R639700).<br>References Jeffrey, A.D. et al.: Drug Chem. Toxicol., 25, 93 (2002); Cassidy, K.C. et al.: J. Pharmac. Biomed. Anal., 22, 869 (2000);<br></p>

<p>Applications The active metabolite of the widely used non-steroidal antagonist Flutamide (F598850). Shown to be an antianhydrogen.<br>References Katchen, B., et al.: J. Clin. Endocrinol. Metab., 41, 373 (1975), Fau, D., et al.: J. Pharmacol. Exp. Ther., 269, 954 (1994), Anzenbacher, P., et al.: Drug Metab. Dispos., 30, 100 (2002), Norlin, M., et al.: J. Lipid Res., 43, 721 (2002),<br></p>

<p>Applications A cyclized labelled analog of orphenadrine and diphenhydramine; representative of a new class of centrally acting skeletal muscle relaxants, the benzoxazocines. Analgesic; antidepressant.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Bassett, et al.: Br. J. Pharmacol., 37, 69 (1969), Klohs, et al.: Arzneim.-Forsch., 22, 132 (1972), Hell, et al.: Drugs, 19, 249 (1980),<br></p>

<p>Stability Hygroscopic<br>Applications Labelled Rebamipide, which shows antiulcer activity in rats.<br>References Uchida, M., et al.: Chem. Pharm. Bull., 33, 3775 (1985), Yamasaki, K., et al.: Eur. J. Pharmacol., 142, 23 (1987),<br></p>

<p>Impurity Ranitidine EP Impurity J<br>Applications 1,1’-N-[Methylenebis(sulphanediylethylene)]bis(N’-methyl-2-nitroethene-1,1-diamine (Ranitidine EP Impurity J) is a Ranitidine (R120000) impurity.<br></p>

<p>Applications Quinoline is a starting material that may be transformed by bacteria and fungi to produce intermediates useful for the synthesis of drugs. Used in the synthesis of tertiary alcohol modulators of RORγ (1) which appears to have various biological functions. Also derivatives of quinoline have been seen to promote anticancer, antibacterial and antiviral activity, however quinoline itself is often seen as an environmental contaminant (2,3). Dyes and metabolites, Environmental Testing.Drinking water contaminant candidate list 3 (CCL 3) compound as per United States Environmental Protection Agency (EPA), environmental, and food contaminants.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References 1. Kummer, D. et al.: Bioorg. Med. Chem. Lett. 2017 Feb 21.2. Ramirez-Prada, J. et al.: Eur J Med Chem. 2017 Mar 16;131:237-254.3. Mestankova, H. et al.: Water Res. 2016 Apr 15;93:110-20<br></p>

<p>Applications Labelled Ephedrine derivative for controlling respiratory tract goblet cell hyperplasia in respiratory diseases including infection and bronchitis.<br>References Tan, Z., et al.: J. Therm. Anal., 45, 59 (1995), van Berkel, G., et al.: Anal. Chem., 76, 479 (2004), Di, Y., et al.: Chin. Phy., 17, 3276 (2008),<br></p>

<p>Applications 1,3-Dihydro-1-(1,2,3,6-tetrahydro-4-pyridinyl)-2H-benzimidazol-2-one is a reactant used in the synthesis of potential anti-parkinsonic agents.<br>References Vejdelek, Z. et al.: Coll. Czech. Chem. Comm., 49, 2649 (1984); Higashi, Y. et al. J. Liquid. Cheom. Rel. Tech., 31, 2762 (2008);<br></p>

<p>Applications n-Butyl Tadalafil is an analog of Tadalafil (T004500); a compound used for the treatment of erectile dysfunction (ED) by inhibiting the phosphodiesterase 5 enzyme (PDE-5).<br>References Carrier, S., et al.: Can. J. Urol., 10(1), 12 (2003); Doggrell, S.A., et al.: Expert Opin. Pharmacother., 6, 75 (2005); Forgue, S.T., et al.:Br. J. Clin. Pharmacol., 61, 280 (2005)<br></p>

<p>Applications A metabolite of Carbamazepine (C175840).<br>References Park, B., et al.: Biochem. Pharmacol., 36, 581 (1987), Yamazaki, H., et al.: Drug Metab. Dispos., 27, 1260 (1999), Dieckhaus, C., et al.: Chem. Res. Toxicol., 14, 958 (2001),<br></p>

<p>Applications A labelled metabolite of Erlotinib (E625000), an anti cancer agent.<br>References Rusch, V., et al.: Cancer Res., 53, 2379 (1993), Fontanini, G., et al.: Clin. Cancer Res., 4, 241 (1998), Comis, R., et al.: Oncologist, 10, 467 (2005), Ling, J., et al.: Drug Metab. Dispos., 34, 420 (2006),<br></p>

<p>Impurity Telmisartan EP Impurity E / Telmisartan Diacid<br>Applications An impurity of Telmisartan (T017000).<br>References Yu, W. et al.: Youji Huaxue, 26, 318 (2006);<br></p>

<p>Applications A metabolite of Eslicarbazepine acetate, (BIA 2-093), a novel central nervous system drug. A keto derivative of Carbamazepine. Used as an anticonvulsant. Neuroprotective &amp; Neuroresearch Product.<br>References Dam., M., et al.: Epilepsy Res., 3, 70 (1989); Beydoun, A., et al.: Expert Opin. Pharmacother., 3, 59 (2001);<br></p>

<p>Applications Regorafenib-d3 is the isotope labelled analog of Regorafenib (R143000); a compound that inhibits PDGFR tyrosine kinase with IC50=83nM and is useful for the treatment of inflammation. Also an anti-proliferative agent.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Leuner, C., et al.: Eur. J. Pharm. Biopharm., 50, 47 (2000)<br></p>

<p>Stability Hygroscopic<br>Applications Gabapentin is an Amino acid structurally related to γ-Aminobutyric Acid (GABA), designed to cross the blood brain barrier. Used as an anticonvulsant.<br>References Vollmer, K.-O. et al.: Arzneimittel-Forshc., 36, 830 (1986), Saletu, B., et al.: Int. J. Clin. Pharmacol. Ther. Toxicol., 24, 362 (1986)<br></p>

<p>Applications Labelled rac Rivastigmine. A brain selective acetylcholinesterase inhibitor. Nootropic.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Rosler, M., et al.: Brit. Med. J., 318, 633 (1999), Enz, A., et al.: Prog. Brain Res., 98, 431 (1993),<br></p>

<p>Impurity 2,4-Dimethyl Celecoxib Impurity<br>Applications 2-Methyl-Celecoxib is an analog of the anti-inflammatory drug Celecoxib (C251000). Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor.<br>References Simon, L.S., et al.: Arthritis Rheum., 41, 1591 (1998), Silverstein, F.E., et al.: J. Am. Med. Assoc., 284, 1247 (2000), Steinbach, G., et al.: N. Engl. J. Med., 342, 1946 (2000),<br></p>

<p>Applications Reagent used for the simultaneous preparation of amino alcohol solvating agents as well as preparation of orally available anticoagulants.<br>References Roehrig, S. et al: J. Med. Chem., 48, 5900 (2005); Bozkurt, S. et al: Tetra: Asymm., 22, 541 (2011);<br></p>

<p>Applications Antiallergic drug, used to treat bronchial asthma, allergic rhinitis and atopic dermatitis.<br>References Shiota, N., et al.: Brit. J. Pharmacol., 159, 626 (2010), Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010), Kawabata, Y., et al.: Eur. J. Pharm. Sci., 39, 256 (2010),<br></p>

<p>Applications Coronary vasodilator. Antianginal.<br>References Fujita, et al.: Jpn. J. Pharmacol., 17, 19 (1967), Harpey, C., et al.: Cardiovasc. Drug Rev., 6, 292 (1989),<br></p>

<p>Applications A metabolite of Naproxen.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Rettie, A., et al.: Chem. Res. Toxicol., 5, 54 (1992), Tracy, T., et al.: Biochem. Pharmacol., 52, 1305 (1996), Bonnabry, P., et al.: Eur. J. Clin. Pharmacol., 49, 305 (1996), Rao, S., et al.: J. Med. Chem., 43, 2789 (2000), Hutzler, J., et al.: Drug Metab. Dispos., 29, 1029 (2001),<br></p>

<p>Impurity Timolol EP Impurity D; Timolol BP Impurity D; Timolol USP Related Compound D<br>Applications 3-Hydroxy-4-morpholino-1,2,5-thiazole (Timolol EP Impurity D; Timolol BP Impurity D; Timolol USP Related Compound D) is an intermediate for the preparation of Timolol.<br>References Bodor, N., et al.: J. Med. Chem., 31, 100 (1988),<br></p>