Salts and Derivatives of Active Pharmaceutical Ingredients (API)

<p>Stability Hygroscopic<br>Applications 4a-Hydroxy Ivermectin is an impurity of Ivermectin (I940800), an antiparasitic drug that is active against a wide variety of nematode and arthropod parasites and is used to treat scabies and lice in humans. An invitro inhibitor of SARS-CoV-2/ Covid-19.<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 Campbell, W., et al.: Science, 221, 823 (1983); Glaziou, P., et al.: Trop. Med. Parasitol., 45, 253 (1994); Meinking, T., et al.: New Engl. J. Med., 333, 26 (1995); Caly, L., et al.: Antivir. Res., 178<br></p>

<p>Applications S(+)-N-(2-(2-Thienyl)ethyl)-2-chlorophenyl Glycine Methyl Ester Hydrochloride is an impurity from Clopidogrel (C587250) which acts as an anti-platelet agent.<br>References Zhu, Y. et al.: ACS. Med. Chem. Lett., 4, 349 (2013); Feuerstein, G., et al.: Exp. Opin. Invest. Drugs, 4, 425 (1995)<br></p>

<p>Applications Ethyl 6-​(4-​Aminophenyl)​-​1-​(4-methoxyphenyl)​-​7-​oxo-​4,​5,​6,​7-​tetrahydro-​1H-​pyrazolo[3,​4-​c]​pyridine-​3-​carboxylate is an impurity of Apixaban (A726700), A potent, direct, selective, and orally active inhibitor of coagulation factor Xa. It is a potential new oral coagulant that may be useful prevention of venous thromboembolism in total hip, knee replacement orthopedic surgery and stroke in treatment of patient with venous thromboembolic disorder or with atrial fibrillation.<br>References Nevuluri, N. et al.: Monat. fuer Chem., 148, 1477 (2017);<br></p>

<p>Stability Hygroscopic<br>Applications 2-[[(3aS,4R,6S,6aa)-4-[7-[[(1R,2S)-2-(3,4-Difluorophenyl)cyclopropyl]amino]-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-2,2-dimethyl-tetrahydro-3aH-cyclopenta[d][1,3]dioxol-6-yl]oxy]ethanol is an intermediate in the synthesis of Ticagrelor (T437700) which is an anticoagulant.<br>References Qiao, D., et al.: Preparation of anticoagulant Ticagrelor, China Patent 104592237, May 6, 2015;<br></p>

<p>Applications Deferasirox Methyl Ester is a derivative of Deferasirox (D228650); an orally active tridentate iron chelator.<br>References Hershko, C., et al.: Blood, 97, 1115 (2001); Galanello, R., et al.: J. Clin. Pharmacol., 43, 565 (2003); Nick, H., et al.: Curr. Med. Chem., 10, 1065 (2003)<br></p>

<p>Applications Levosimendan Cyanoacetamide Hydrazone Impurity is an impurity of Levosimendan (L378000) which is a bioactive enantiomer of racemate, Simendan. It is a positive inotropic agent with vasodilating activity and also cardiotonic.<br>References Sandell, E.-P., et al.: J. Cardiovasc. Pharmacol., 26, S57 (1995); Pagel, P.S., et al.: Cardiovasc. Drug Rev., 14, 286 (1996)<br></p>

<p>Impurity Leflunomide EP Impurity H<br>Stability Hygroscopic<br>Applications 2-Cyano-N-[4-(trifluoromethyl)phenyl]acetamide (Leflunomide EP Impurity H) is used to prepare aminothiophene carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers. It is also used to synthesize (1,2,3-triazol-4-yl)benzenamines as inhibitors against VEGF receptors 1 and 2.<br>References Nikolakopoulos, G., et al.: Bioorg. Med. Chem., 14, 2358 (2006); Kiselyov, A., et al.: Bioorg. Med. Chem. Lett., 19, 1344 (2009)<br></p>

<p>Applications N-Mesyldronedarone is an impurity of Dronedarone (D679445, HCl); a drug used for the treatment of atrial fibrillation and atrial flutter in patients who have suffered cardiac arrhythmias.<br>References Singh, B., et al.: J. Cardiovas. Pharmacol., 52, 300 (2008); Hoy, S., et al.: Drugs, 69, 1647 (2009); Hohnloser, S., et al.: New Eng. J. Med., 360, 668 (2009); Mahender, M., et al.: Org. Process Res. Dev., 18, 157 (2014)<br></p>

<p>Applications (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine is an intermediate in the preparation of orally active reversible P2Y12 receptor antagonists such as Ticagrelor (T437700)for the prevention of thrombosis.<br>References Springthorpe, B. et al.: Bioorg. Med. Chem. Lett., 17, 6013 (2007);<br></p>

<p>Impurity Apixaban<br>Applications Analytical standard impurity of drug.<br></p>

<p>Impurity Leflunomide EP Impurity E<br>Applications 5-Desmethyl-3-methyl Leflunomide (Leflunomide EP Impurity E) is the 3-methyl-isomer of Leflunomide (L322750), as a poisonous impurity.<br></p>

<p>Applications Diclofenac-13C6 is a labelled analogue of Diclofenac Acid (D436465), which is a nonsteroidal anti-inflammatory compound and decycloxygenase (COX) inhibitor. Diclofenac-13C6 is also an intermediate in synthesizing Diclofenac-13C6 Sodium Salt (D436453), which is a labelled analogue of Diclofenac Sodium Salt (D436450).<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 Yagi, K., et. al.: Biol. Pharm. Bull., 37, 1234 (2014); Kenny, J. R., et al.: J. Med. Chem., 47, 2816 (2004); Sasaki, A., et al.: J. Pharmacol. Sci., 108, 266 (2008); Dalvie, D., et al.: Chem. Res. Toxicol., 22, 357 (2009); Kenny, J. R., et al.: J. Med. Chem., 47, 2816 (2004), Sasaki, A., et al.: J. Pharmacol. Sci., 108, 266 (2008); Dalvie, D., et al.: Chem. Res. Toxicol., 22, 357 (2009)<br></p>