Sulfonamides and Derivatives

Applications Indomethacin terpenoids' esters were synthesized and assessed both in vitro and in vivo as indomethacin dermal prodrugs.
References Bonina,, Francesco. , et al.: European Journal of Pharmaceutical Sciences, 14, 123 (2001),

Applications An active labelled metabolite of Glimepiride (G410150).
References Groop, L., et al.: Diabetes Care, 15, 737 (1992), Muller, G., et al.: Diabetes, 42, 1852 (1993), Kramer, W., et al.: Biochem. Biophys. Acta, 119, 278 (1994),

Applications 3-[(4-Aminophenyl)sulfonyl]benzenamine is an impurity of Dapsone (D193250), an antibacterial used in the treatment of dermatitis herpetiformis.
References Francis, J., et al.: Br. J. Pharmacol., 5, 565 (1950); Uetrecht, J., et al.: Clin. Dermatol., 7, 111 (1989); Reszka, K., et al.: Chem. Res. Toxicol., 22, 1137 (2009); Santos, J., et al.: Bioorg. Med. Chem., 17, 3795 (2009);Varma, M., et al.: J. Med. Chem., 52, 4844 (2009)

Applications A deuterated metabolite of the drug Sulfathiazole.

Applications 3-Azabicyclo[3.3.0]octane Hydrochloride is a reactant in the preparation of substituted pyrimidines derivatives as novel hedgehog signaling pathway inhibitors.
References Xin, M. et al.: Med. Chem. Res., 23, 3784 (2014); Xin, M. et al.: Bioorg. Med. Chem. Lett., 24, 983 (2014);

Impurity Etodolac EP Impurity D
Applications 8-Isopropyl Etodolac (Etodolac EP Impurity D) is an impurity in the synthesis of Etodolac (E933100), may have use in the treatment of myeloma. COX-1/COX-2/β-catenin inhibitors, or anti-inflammatory agent.
References Humber, L.G., et al.: Med. Res. Rev., 7, 1 (1987); Balfour, J.A, et al.: Drugs, 42, 274 (1991); Kato, et al.: J. Pharm. Pharmacol., 53 1679 (2001);

Applications A major labelled metabolite of Sulfadiazine.
References Woolley, J., et al.: Drug Metab. Dispos., 7, 94 (1979), Nielsen, P., et al.: Biochem. Pharmacol., 35, 2509 (1986), Anari, M., et al.: Anal. Chem., 76, 823 (2004), Edlund, P., et al.: J. Pharm. Biomed. Anal., 34, 1079 (2004),

Applications (4R,6S)-4H-Thieno[2,3-b]thiopyran-4-ol, 5,6-dihydro-6-methyl-,7,7-dioxide is an analog of topically-active carbonic anhydrase inhibitor MK-507 also commonly known as Dorzolamide (D535100).
References Blacklock, T., et al.: J. Org. Chem., 58, 1672 (1993); Tempkin, O., et al.: Tetrahedron: Asym., 7, 2721 (1996)

Applications Glimepiride-d4 (phenylethyl-a,a,b,b-d4) (cis/trans) is a useful isotopically labeled compound of Glimepiride (G410150)

Applications Ibuprofen Alcohol (Ibuprofen EP Impurity P) is an impurity of Ibuprofen (I140000). Ibuprofen impurity P as per EP.
References Haikala, V., et al.: J. Pharm. Sci., 80, 456 (1991), Zhao, J., et al.: Anal. Chem., 72, 302 (2000), Kucera, R., et al.: J. Pharm. Biomed. Anal., 38, 609 (2005),

Impurity Etodolac EP Impurity A
Applications 8-Desethyl Etodolac (Etodolac EP Impurity A) is an impurity of Etodolac (E933100) which was examined for mutagenicity in reverse mutation tests on bacteria. Etodolac impurity A.
References Franke, L., et al.: J. Med. Chem., 48, 6997 (2005), Fox, T., et al.: Curr. Top Med. Chem., 6, 1579 (2006),

Applications Indometacin 1-Glycerin Ester was synthesized and evaluated for anti-flammatory activity in the rate paw carrageenin edema essay.
References Paris, Gerard. , et al.: J. Med. Chem, 23, 9 (1980)

Applications (S)-4-Hydroxy-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide 1,1-Dioxide has been used as a reactant for the preparation of Brinzolamide (AL-4862) [B677600], a topical carbonic anhydrase inhibitor.
References Conrow, R.E., et. al.: Org. Process Res. Dev., 3, 114 (1999)

Stability Hygroscopic
Applications A labelled metabolite of Tolbutamide. Formed by the cytochrome CYP2CIIC8 and IIC9 subfamily of P450 enzymes.
References Relling, etl al.: J. Pharmacol. Exp. Ther., 252, 442 (1990), Parent, et al.: J. Pharmacol. Exp. Ther., 261, 780 (1992), Ho, et al.: Life Sci., 52, 21 (1993),

Applications 4-​Nitro-​2-​phenoxyphenol is a impurity of Nimesulide (N477500), antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-alpha production. Also used in the preparation of benzoxirenes and the synthesis of trioxonins.
References Pairet, M., et al.: Inflamm. Res., 47, S93 (1998), Fukutake, M., et al.: Carcinogenesis, 19, 1939 (1998), Okajima., E., et al.: Cancer Res., 58, 3028 (1998), Azab, A., et al.: Life Sci., 63, 323 (1998)

Applications The major labelled metabolite of Indomethacin.
References Lewis, R., et al.: J. Clin. Invest., 53, 1607 (1974), Alvan, G., et al.: Clin. Pharmacol. Ther., 18, 364 (1975), Mungall, D., et al.: J. Pharm. Sci., 73, 1000 (1984), Baldwin, S., et al.: Xenobiotica, 25, 261 (1995),

Impurity Ibuprofen EP Impurity G
Applications Ibuprofen Dimer (Ibuprofen EP Impurity G) is a dimer impurity of Ibuprofen (I140000).

Applications Phenacetin-d3 is the labeled analogue of Phenacetin (P294580), an analgesic, antipyretic; component of APC tablets, analgesic mixture also containing aspirin and caffeine. Phenacetin is reasonably anticipated to be a human carcinogen; analgesic mixtures containing Phenacetin are listed as known human carcinogens.
References Boyd, et al.: Toxicol. Appl. Pharmacol., 1, 240 (1959); Dubach, C.U., et al.: N. Engl. J. Med., 308, 357 (1983)