Salts and Derivatives of Active Pharmaceutical Ingredients (API)

Applications (7α,17α)- 9,17-Dihydroxy-3-oxo-pregn-4-ene-7,21-dicarboxylic Acid Di-γ-lactone is an eplerenone (E588775) impurity. Eplerenone is a selective aldosterone receptor antagonist (SARA), structurally similar to Spiranolactone. Eplerenone is used alone or in combination with other medications to treat high blood pressure. Eplerenone is in a class of medications called mineralocorticoid receptor antagonists. It works by blocking the action of aldosterone, a natural substance in the body that raises blood pressure. References de Gasparo, M., et al.: J. Pharmacol. Exp. Ther., 240, 650 (1987), Delyani, J.A., et al.: Cardiovasc. Drug Rev., 19, 185 (2001), Burgess, E., et al.: Expert. Opin. Pharmacother., 5, 2573 (2004), Ravis, W.R., et al.: J. Clin. Pharmacol., 45, 810 (2005),

Applications A metabolite of Clomipramine. References McTavish, D., et al.: Drugs, 39, 136 (1990), Chauret, N., et al.: Drug Metab. Dispos., 25, 1130 (1997), Gex-Fabry, M., et al.: Ther. Drug Monit., 22, 701 (2000), Herrera, D., et al.: J. Clin. Pharmacol., 40, 1488 (2000),

Stability Very Hygroscopic Applications Ibandronate sodium (I120001) impurity. References Dunn, C., et al.: Drugs, 2001, 61, 685 (2001), Szabo, C., et al.: J. Med. Chem., 45, 2185 (2002),

Stability Hygroscopic Applications 11-(4-Ethyl-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine is an impurity of Quetiapine hemifumarate (Q510000), a dibenzothiazepine antipsychotic medication used in the treatment of schizophrenia. References Kumar, K., et al.: Org. Chem.: An Indian Journal, 8, 164 (2012); Raju, I., et al.: Chromatographia, 70, 545 (2009)

Applications β-Hydroxyl Phentermine is derived from 2-Nitropropane (N519600), which is an oxidative stress-inducing agent and also a carcinogen. It is used in the induction of DNA polymerase β-dependent base excision repair in response to oxidative stress in the liver. References Cabelof, D.C., et al.: Carcinogenesis,23, 1419 (2002); Kreis, P., et al.: Carcinogenesis, 21, 295 (2000)

Imides and their derivatives (excluding sacharin), salt thereof

Compounds containing an unfused pyrazole ring, whether or not hydrogenated, in the structure, nesoi

Impurity Timolol EP Impurity H Applications 2-(3-(tert-Butylamino)-2-hydroxypropyl)-4-morpholino-1,2,5-thiadiazol-3(2H)-one is a impurity of Timolol (T443710), an antihypertensive; antiarrhythmic (class II); antianginal; antiglaucoma agent. References Lacroix, P.M., et. al.: Chirality, 6, 484 (1994); Wasson, et al.: J. Med. Chem., 15, 651 (1972); Franciosa, et al.: Clin. Pharmacol. Ther., 13, 138 (1972); Heel, R.C., et al.: Drugs, 17, 38 (1979); Rofman, B.A., et al.: Hypertension, 2, 643 (1980); Mazzo, D.J., et al.: Anal. Profiles Drug Subs., 16, 641 (1987)

Ketone-alcohols and ketone-aldehydes, nesoi

Applications Tigecycline (open C-ring D-ring) quinone Trifluoroacetic Acid Salt is a salt of Tigecycline (open C-ring D-ring) quinone, an impurity of Tigecycline (T440015). Tigecycline (open C-ring D-ring) quinone is one of the very few glycylcycline antimicrobials that exhibit activity against Gram-negative bacteria and also one of the few that also circumvent around the major resistance mechanisms of tetracycline. References Grosse, E., et al.: Clin. Infect. Dis. (Supplement 5), 41, S341 (2005); Livermore, D.: J. Antimicrob. Chemoth., 56, 611 (2005); Stein, G. & Craig, W.: Clin. Infect. Dis., 43, 518 (2006)

Applications 4-Hydroxybenzhydrazide works as an indicator in the determination of carbohydrates. Tissue (liver) bounded 4-Hydroxybenzhydrazide, the acid-hydrolyzable side chain of Nifuroxazide (N458500) can be used as a marker to monitor it’s residue in chicken. References Lever, M., et al.: Anal. Biochem., 139, 205 (1984); Rocco, M., et al.: Anal. Biochem., 377, 251 (2008); Gao, F., et al.: J. Sci. Food Agr., 93, 2172 (2013)