Dérivés des Purines et Pyrimidines

<p>M02443 - (R)-Roscovitine</p>

<p>Impurity Rizatriptan EP Impurity I<br>Applications N10-Monodesmethyl Rizatriptan (Rizatriptan EP Impurity I) is a metabolite of Rizatriptan.<br>References Dechant, K., et al.: Drugs, 43, 776 (1992), Castro, J., et al.: Bioorg. Med. Chem. Lett., 3, 993 (1993), Lee, Y., et al.: Biopharm. Drug Dispos., 19, 577 (1998), Chen, J., et al.: J. Pharm. Biomed. Anal., 35, 639 (2004),<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 Dopamine depleting agent. An antidyskinetic; antipsychotic.<br>References Schwartz, et al.: Biochem. Pharmacol., 15, 645 (1966), Janovic, J., et al.: Ann. Neurol., 11, 41 (1982), Janovic, J., et al.: Neurology, 38, 391 (1988),<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>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>

<p>Stability Very Hygroscopic<br>Applications A labelled metabolite of Temozolomide.<br>References Jaeken, J., et al.: Lancet, 2, 1058 (1984), Baggott, J., et al.: Biochem. J., 236, 193 (1986), Baggott, J., et al.: Arch. Dermatol., 135, 813 (1999),<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 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 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>Stability Very Very Moisture sensitive<br>Applications Chloroformic Acid Chloromethyl Ester is used as a reagent in the synthesis of carbamates and carbonates.<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 Safadi, M. et al.: Pharm. Res. 10, 1350 (1993); Loren, J.C. et al.: Synlett, 18, 2847 (2005);<br></p>

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

<p>Applications [[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]monophenylester 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>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 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>Stability Hygroscopic<br>Applications Methotrexate intermediate.<br>References Feng, Y., et al.: J. Med. Chem., 49, 770 (2006),<br></p>

<p>Stability Hygroscopic, Temperature Sensitive<br>Applications 4-[2-(4-Chlorobutylidene)hydrazinyl]-N-methylbenzenemethanesulfonamide is an intermediate in the synthesis of 3-(2-Aminoethyl)-N-methyl-1H-indole-5-methanesulfonamide (Didesmethyl Sumatriptan) (Sumatriptan EP Impurity E) (A609165), which is an antimigraine agent. A Sumatriptan intermediate.<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></p>

<p>Stability Photosensitive<br>Applications It is used for the treatment of pancreatic cancer and acute myelogenous leukaemia (AML).<br></p>

<p>Applications 1,11b-Dedihydrotetrabenazine is a product of photolytic degradation of Tetrabenazine (T284000) which is a dopamine depleting agent.<br>References Bourezg, Z., et al.: J. Pharmaceut. Biomed., 91, 138 (2014); Schwartz, et al.: Biochem. Pharmacol., 15, 645 (1966); Janovic, J., et al.: Ann. Neurol., 11, 41 (1982); Janovic, J., et al.: Neurology, 38, 391 (1988);<br></p>

<p>Applications 2-Hydroxy-N-(pyridin-4-yl)butanamide is a useful synthetic intermediate.<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 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>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 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 (+)-9-deMe-DTBZ is a desmethyl derivative of Tetrabenzine (T284000), a dopamine depleting agent. An antidyskinetic; antipsychotic.<br>References Schwartz, et al.: Biochem. Pharmacol., 15, 645 (1966), Janovic, J., et al.: Ann. Neurol., 11, 41 (1982), Janovic, J., et al.: Neurology, 38, 391 (1988),<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 Methotrexate-d3 Pentaglutamate is the isotope labelled analog of Methotrexate Pentaglutamate (M260735); a metabolite of Methotrexate (M260675) which is 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 This compound is an isomer of compound (E925685) used in the synthesis of neuraminidase inhibitors.<br>References Jarinrat K. et al.: Bioorg. Med. Chem. Lett., 20, 2152 (2012);<br></p>

<p>Applications A metabolite of Tetrabenazine in vivo, which is likely the active pharmacological agent. The cis isomer of Dihydrotetrabenazine is used for the treatment of hyperkinetic movement disorders.<br>References Kilbourn, M., et al.: Eur. J. Pharmacol., 278, 249 (1995), Perera, R., et al.: J. Med. Chem., 46, 2599 (2003), Mager, D., et al.: J. Pharm. Sci., 94, 2475 (2005), Zheng, G., et al.: Bioorg. Med. Chem., 16, 5018 (2006),<br></p>

<p>Stability Hygroscopic<br>Applications Tenofovir (T018500) impurity.<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>Applications A metabolite of Febuxostat (F229000), a novel nonpurine selective inhibitor of Xanthin Oxidase.<br>References Grabowski, B., et al.: J. Clin. Pharmacol., 51, 189 (2011); 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>Stability Hygroscopic<br>Applications rac-Clopidogrel Carboxylic Acid Hydrochloride is a salt metabolite of rac-Clopidogrel.<br></p>

<p>Applications Labelled Hydroxyurea. An anti-neoplastic - inhibits ribonucleoside reductase and DNA replication. A potential therapy for sickle cell anemia which involves the nitrosylation of sickle cell hemoglobin. Horseradish peroxidase catalyzes nitric oxide formation from hydroxyurea in the presence of hydrogen peroxide.<br>References Ratcliffe, W., et al.: Lancet, 339, 164 (1992), Roodman, G., et al.: Cancer, 80, 1557 (1997), Horwitz, M., et al.: J. Clin. Endocrinol. Metab., 2003, 88, 1603 (2003),<br></p>

<p>Applications The 5-aminopentyl amide derivative of the folic acid antagonist Methotrexate (M260675) used in the study of membrane-associated folate transporters from L1210 cells.<br>References Fan, J. et al.: J. Biol. Chem., 266, 14862 (1991);<br></p>

<p>Applications Labelled Urea. Physiological regulator of nitrogen excretion in mammals; synthesized in the liver as an end-product of protein catabolism and excreted in urine. Also occurs normally in skin. Emollient; diuretic.<br>References Demetriou, A., et al.: Science, 233, 1190 (1986), Aebischer, P., et al.: Nat. Med., 2, 696 (1996), Prakash, S., et al.: Biotechnol. Bioeng., 46, 621 (1995),<br></p>

<p>Applications Febuxostat 67M-2 is a derivative compound of Febuxostat 67M-1 (F229005) which is an inhibitor of xanthine oxidase. It reduces uric acid production in the body and also used to reduce the risk of gout or kidney stone formation.<br>References Du, J., et al.: Handbook of Metabolic Pathways of Xenobiotics, 4, 1395 (2014)<br></p>

<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 Valbenzine is a highly selective vesicular monoamine transporter 2 inhibitor. It is used in the treatment of tardive dykinesia.<br>References O'Brien, C. et al.: Movement Dis., 30, 1681 (2015);<br></p>

<p>Stability Light Sensitive, Temperature Sensitive<br>Applications 1-Methyl-1,4-dihydronicotinamide (cas# 17750-23-1) is a compound useful in organic synthesis.<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>Impurity Zolmitriptan USP Related Compound F<br>Stability Hygroscopic<br>Applications (N,N-Dimethyl-1-butanamine) Zolmitriptan Dimer (Zolmitriptan USP Related Compound F) is an impurity from the synthesis of Zolmitriptan (Z639000). Zolmitriptan is a Serotonin 5HTID-receptor agonist.<br>References Glen, R.C., et al.: J. Med. Chem., 38, 3566 (1995), Seaber, E., et al.: Brit. J. Clin. Pharmacol., 41, 141 (1996), Tepper, S.J., et al.: Curr. Med. Res. Opin., 15, 254 (1999)<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>Stability Very Hygroscopic<br>Applications Tenofovir (T018500) impurity.<br></p>