Derivati delle Purine e Pirimidine

<p>Impurity Proguanil USP Related Compound E (1-(4-chlorophenyl)-3-cyanoguanidine)<br>Applications Halo-aryl substituted guanidine derivative used in the preparation of antimalarial agents. Proguanil USP Related Compound E (1-(4-chlorophenyl)-3-cyanoguanidine).<br>References Warner, V. et al.: J. Pharmac. Sci., 66, 418 (1977); Das, A. et al.: Ind. Drugs, 20, 19 (1980);<br></p>

<p>Applications Ethyl 2-(4-Butoxy-3-cyanophenyl)-4-methylthiazole-5-carboxylate, is an impurity in the synthesis of Febuxostat n-Butyl Isomer (F229035).<br></p>

<p>Stability Hygroscopic<br>Applications Methotrexate Hexaglutamate is a metabolite of Methotrexate (M260675); a folic acid antagonist, antineoplastic, and antirheumatic.<br>References Freeman, M.V., J. Pharmacol. Exp. Ther., 122, 154 (1958); Weinblass, M.E., et al.: N. Engl. J. Med., 312, 818 (1985)<br></p>

<p>Applications Degradation product of Sumatriptan Succinate (S810000).<br>References Xu, X. et al.: J. Pharmaceut. Biomed. 367, 26 (2001)<br></p>

<p>Applications Benzofuran-6-carboxylic Acid is a reagent in the development of potent LFA-1/ICAM antagonist SAR 118 as an opthalmic solution for treating dry eyes. Preparation of piperidinylpyrimidine derivatives as inhibitors of HIV-1 LTR activation.<br>References Zhong, M., et al.: ACS Med. Chem., 3, 203 (2012); Fujiwara, N., et al.: Bioorg. Med. Chem., 16, 9804 (2008)<br></p>

<p>Applications An impurity of Tenofovir (T018500(P)). Tenofovir is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor. It is used as an anti-HIV agent. Antiviral.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997); Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007);<br></p>

<p>Applications A nicotinic acid derivative for prevention and treatment of cancer by activating RUNX3 gene.<br>References Ludwig, et al.: Cancer Res., 50, 2470 (1990), Gupta., et al.: Biomed. Environ. Sci., 13,122 (2000), Cai., et al.: J. Med. Chem., 46, 2474 (2003),<br></p>

<p>Impurity Naratriptan Impurity F<br>Stability Hygroscopic<br>Applications 4-[1,5-Bis-(2-methylsulfamoylethyl)-1H-indol-3-yl]-1-methylpyridinium Chloride is an impurity of Naratriptan (N378730).<br></p>

<p>Applications Caffeine-D10 is the labeled compound of Caffeine(C080100). Caffeine (Pentoxifylline EP Impurity F) is a bitter, white crystalline xanthine alkaloid that acts as a stimulant drug and a reversible acetylcholinesterase inhibitor (1,2,3). Caffeine is found in varying quantities in the seeds, leaves, and fruit of some plants, where it acts as a natural pesticide that paralyzes and kills certain insects feeding on the plants. In humans, caffeine acts as a central nervous system stimulant, temporarily warding off drowsiness and restoring alertness. Caffeine is a cardiac and respiratory stimulant; diuretic. Caffeine is toxic at sufficiently high doses. Caffeine is a non-competitive inhibitor of acetylcholinesterase (3).<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 Zubair, U.M., et al.: Anal. Profiles Drug Subs., 15, 71 (1986); Cherrah, Y., et al.: Biochem. Pharmacol., 37, 1311 (1988);<br></p>

<p>Applications 2-Chloro-6-amino-9-(2’,3’,5’-tri-O-acetyl-β-D-ribofuranosyl)purine (cas# 79999-39-6) is a compound useful in organic synthesis.<br></p>

<p>Applications Tenofovir is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor. It is used as an anti-HIV agent. Antiviral. Tenofovir (T018500) impurity.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997); Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol.,  46, 265 (2006), Seminari, E., et al.:  J. Antimicrob. Chemother., 60, 831 (2007);<br></p>

<p>Applications D-Alanine Isopropyl Ester Hydrochloride is a chiral reagent used in the synthesis of nucleotide prodrugs such as (PSI-7977) for the treatment of hepatitis C. Also used in the preparation of synthetic sweeteners.<br>References Sofia, M. et al.: J. Med. Chem., 53, 7202 (2010); Mazur, R. et al.: J. Med. Chem., 16, 1284 (1973);<br></p>

<p>Stability Hygroscopic<br>Applications Pemetrexed L-Glutamic acid is an impurity of Pemetrexed (P219500). Pemetrexed impurity D.<br></p>

<p>Applications (S)-9-[2-(Hydroxypropyl] Adenine is an inhibitor of adenosine deaminase. (S)-9-[2-(Hydroxypropyl] Adenine is used in the preparation of antiviral acyclic nucleoside thiophosphonates such as (S)-Tenofovir Disoproxil Fumarate (T018506).<br>References Roux, L. et al.: Eur. J. Med. Chem., 63, 869 (2013); Schaeffer, H. et al.: J. Med. Chem., 15, 456 (1972); Schaeffer, H. &amp; Vince, R.: J. Med. Chem., 10, 689 (1967)<br></p>

<p>Applications 4-Hydroxy-1,3-benzenedicarbonitrile is used in the preparation of febuxostat (F229000), a non-purine xanthine oxidase inhibitor used as a treatment for hyperuricaemia and chronic gout.<br>References Smith, C.J., et al.: Bioorg. Med. Chem. Lett., 20, 346 (2010); Cramp. S., et al.: BIoorg. Med. Chem. Lett., 20, 2516 (2010); Sato, T., et al.: Bioorg. Med. Chem. Lett., 19, 184 (2009);<br></p>

<p>Applications 8-13C-Uric Acid is the labeled analogue of Uric Acid (U829200), a heterocyclcic compound that is created when purine nucleotides are broken down of by the human body. High blood concetration of Uric Acid is known as hyperuricemia and is often associated with a wide range of disorders and medical conditions such as gout, diabetes and metabolic syndrome. Uric acid may be a marker of oxidative stress and may have a potential therapeutic role as an antioxidant.<br>References Heinig, M. et al.: Cle. Clin. J. Med., 73, 1059 (2006); Glantzounis, G.K. et al.: Curr. Pharmac. Des., 11, 4145 (2005); Dehghan, A. et al.: Diab. Care, 31, 361 (2008); Nakagawa, T. et al.: Am. J. Physiol. Renal Physiol., 290, F625 (2006)<br></p>

<p>Applications 2-Pyrimidinemethanamine (cas# 75985-45-4) is a useful research chemical.<br></p>

<p>Applications Caffeine citrate (Cafcit) is a citrate salt of Caffeine, sometimes used in medical treatment, including short-term treatment of apnea of prematurity (lack of breathing in premature infants). Caffeine citrate functions in much the same capacity as does caffeine, but takes effect more quickly; its speed of dissociation is faster than that of Caffeine. Caffeine citrate is typically only used to treat severe migraines.<br>References Zubair, U.M., et al.: Anal. Profiles Drug Subs., 15, 71 (1986); Cherrah, Y., et al.: Biochem. Pharmacol., 37, 1311 (1988); Grillon, C., et al.: Clin. Neurophysiol., 114, 1557 (2003); Duangdao, D., et al.: Behav. Brain Res., 205, 1 (2009);<br></p>

<p>Applications Sumatriptan Impurity 1, is an impurity of Sumatriptan (S810000), which is a serotonin 5HT1-receptor agonist, used for the treatment of migraine headaches.<br>References Humphrey, P.P.A., et al.: Brit. J. Pharmacol., 94, 1123 (1988), Doenicke, A., et al.: Lancet 1, 1309 (1988),<br></p>

<p>Applications: Labelled Almotriptan (A575200). Almotriptan is a serotonin 5HT1B /1D-receptor agonist used for treatment of migraine.<br>References Fleishaker, J.C., et al.: Clin. Pharmacol. Ther., 67, 498 (2000), Kamali, F., et al.: Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs, 2, 197 (2000), Dodick, D.W., et al.: Expert Opin.Pharmacother., 4, 1157 (2003)<br></p>

<p>Applications Pemetrexed Disodium Heptahydrate is an chemotherapy drug for the treatment of pleural mesothelioma and non-small cell lung cancer. Pemetrexed Disodium Heptahydrate exhibit inhibitory activities towards thymidylate synthase as well as other folate dependent enzymes.<br>References Vogelzang, N.J., et al.: J. Clin. Oncol., 21,2636 (2003); Paz-Ares, L., et al.: Lancet. Oncol., 13, 247 (2012);<br></p>

<p>Applications Thiamine (T344185) impurity.<br></p>

<p>Applications 3-Descyano Febuxostat Ethyl Ester is an impurity of Febuxostat (F229000), a xanthine oxidase/xanthine dehydrogenase inhibitor. Used for treatment of hyperuricemia and chronic gout. 40-120 mg/day febuxostat was proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.<br>References Vallu, V., et. al.: Anal. Chem. Indian J., 14, 339 (2014); Osada, Y., et al.: Eur. J. Pharmacol., 241, 183 (1993); Okamoto, K., et al.: J. Biol. Chem., 278, 1848 (2003); Mayer, M.D., et al.: Am. J. Therap., 12, 22 (2005); Tomlinson, B., et al.: Curr. Opin. Invest. Drugs, 6, 1168 (2005)<br></p>

<p>Impurity Sumatriptan EP Impurity D<br>Stability Hygroscopic, Unstable in DMSO<br>Applications Sumatriptan N-Oxide (Sumatriptan EP Impurity D) is the degradation product of the antimigraine drug Sumatriptan (S810000).<br>References Xu, X. et al.: J. Pharmac. Biomed. Anal., 26, 367 (2001); Cheng, K.N. et al.: J. Pharmac. Biomed. Anal., 17, 399 (1998);<br></p>

<p>Applications rac-Clopidogrel Hydrogen Sulfate is used in the synthesis of Clopidogrel derivatives as platelet aggregation inhibitors.<br>References Chen, J., et. al.: Hecheng Huaxue, 18, 586 (2010); Defreyn, G. et al.: Thromb. Haemo., 65, 186 (1991);<br></p>

<p>Applications Diethyl p-Toluenesulfonyloxymethylphosphonate is an antiviral agent and a Tenofovir (T018500) intermediate. Tenofovir is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor used as an anti-HIV agent.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997), Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007),<br></p>

<p>Applications 5-Carboxy-2'-deoxyuridine, is a derivative of Trifluridine, an anti-herpesvirus antiviral drug, used primarily on the eye.<br>References Kuster, P., et al.: CLAO J. 24(2), 122 (1998); O’Brien, W., Invest. Opthalmol. Vis. Sci., 32 (9), 2455 (1991);<br></p>

<p>Applications Barbituric Acid (B118650) derivative with anti-convulsive properties. Controlled Substance.<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 Carissime, M. et al.: Farmac. Edi. Sci., 17, 390 (1962); Harvey, D.J. et al.: Drug. Metab. Disp., 5, 527 (1977);<br></p>

<p>Stability Hygroscopic<br>Applications rac-Clopidogrel Carboxylic Acid Hydrochloride is a salt metabolite of rac-Clopidogrel.<br></p>

<p>Stability Hygroscopic<br>Applications Tenofovir (T018500) impurity.<br></p>

<p>Applications 1-Bromoethyl Acetate is a 1-haloalkyl ester that is used in the modification of antibiotics.<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 Zakrzewski, J. et al.: Pol. J. Chem. Technol., 8, 83 (2006); Kamachi, H. et al.: J. Antibiot., 41, 1602 (1988);<br></p>

<p>Stability Hygroscopic<br>Applications One of the unknown impurities generated during the accelerated stability storage of Clopidogrel bisulfate tablets. Clopidogrel impurity.<br>References Gomez, Y., et al.: J. Pharm. Biomed. Anal., 34, 341 (2004), Ksycinska, H., et al.: J. Pharm. Biomed. Anal., 41, 533 (2006),<br></p>

<p>Stability Very Hygroscopic<br>Applications Tenofovir Dimer is a dimer of Tenofovir (T018500). Tenofovir is a reverse transcriptase inhibitor. Used as an anti-HIV agent.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997), Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007),<br></p>

<p>Applications Fungal tyrosinases and their capability to oxidize peptide-bound tyrosine residues is important in a view of applicability of tyrosinases.<br>References Bowness, J., et al.: Biochem. J., 53, 620 (1953), Cuff, M., et al.: J. Mol. Biol., 278, 855 (1998), Kubo, I., et al.: Bioorg. Med. Chem., 12, 5349 (2004),<br></p>