Salts and Derivatives of Active Pharmaceutical Ingredients (API)

<p>Trandolaprilat is a prodrug of enalaprilat, which is an angiotensin-converting enzyme (ACE) inhibitor. Trandolaprilat binds to the active site of ACE and inhibits its activity, thereby causing a decrease in the formation of angiotensin II, a potent vasoconstrictor. Trandolaprilat has been shown to be effective in treating congestive heart failure and other cardiac disorders. Trandolaprilat has also been shown to have an effect on energy metabolism, as it inhibits the binding of ATPase to adenosine triphosphate (ATP). This inhibition leads to increased levels of ATP in cells and may be responsible for its cardioprotective effects.</p>

<p>Raloxifene N-oxide is a synthetic drug product that is used in the treatment of osteoporosis. It belongs to the family of selective estrogen receptor modulators (SERM). Raloxifene N-oxide has been shown to inhibit bone resorption and reduce the risk of vertebral fractures. It also has anti-estrogenic effects, which have been shown to be beneficial for prostate cancer patients who are receiving androgen deprivation therapy. Raloxifene N-oxide is an impurity in the synthesis of raloxifene, which is a drug product with CAS number 195454-31-0. The purity of this compound should be at least 99%.</p>

<p>Tanshinone IIA is an enantioselective hydroxamic acid that inhibits matrix metalloproteinase. It is a structural analogue of the hydroxamic acid Tanshinone I and has been shown to inhibit aggrecanase, which is an enzyme that hydrolyzes the glycosaminoglycan aggrecan. It also has anti-cancer effects due to its inhibition of cell proliferation in cancer cells. Tanshinone IIA can be used as a chiral synthon for polymerase chain reactions (PCR) because it contains a stereogenic centre in its structure.</p>

<p>N-Hydroxy riluzole N-b-D-glucuronide (NHRG) is a drug product that has been used as an analytical reference standard in metabolism studies. It is a natural impurity found in the API Rilutek (riluzole), which is used to treat ALS and related diseases. NHRG exhibits a retention time of 9.5 minutes on HPLC, and its purity should be at least 98%. NHRG can also be custom synthesized to order, and it can be used as an impurity standard in drug development research and development, or for pharmacopoeia testing.</p>

<p>Ethyl 3-aminopyrazole-4-carboxylate is an anticancer drug that inhibits the growth of cancer cells by inhibiting protein synthesis. It has been shown to inhibit the activity of dpp-iv and pde5, which are enzymes involved in cellular proliferation. Ethyl 3-aminopyrazole-4-carboxylate has also been shown to have antiinflammatory properties, which may be due to inhibition of prostaglandin synthesis. <br>Ethyl 3-aminopyrazole-4-carboxylate is a multinuclear compound that reacts with nitrogen atoms from the pyrazoles to form a stable molecule. Dimethylformamide is used as a solvent for this reaction. The synthesis of ethyl 3-aminopyrazole-4-carboxylate starts with acetylation, which converts the carboxylic acid group into an acetic acid group. The acetic acid group reacts with ammonia and hydrogen cyan</p>

<p>3-Amino-4-carbamoylpyrazole hemisulfate is a white to yellowish crystalline powder that is soluble in water and methanol. It is a condensation product of allopurinol and ethyl orthoformate with a molecular weight of 312.4. 3-Amino-4-carbamoylpyrazole hemisulfate can be used as an anti-inflammatory agent, but it has not been approved for medical use in the United States.</p>

<p>Cimetidine is a histamine-2 receptor antagonist that inhibits gastric acid secretion and reduces the activity of stomach enzymes. It is used to treat peptic ulcers, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. Cimetidine has been shown to inhibit the activity of drug-metabolizing enzymes such as cytochrome P450. Cimetidine also inhibits the transport protein P-glycoprotein (P-gp), which leads to increased concentrations of some drugs in the blood and tissues. This inhibition may lead to an increase in cardiac effects with certain drugs, such as x-ray diffraction data with taxol or h1 antagonists.</p>

<p>Apixaban impurity 2 is a drug product that is used as an impurity standard in the research and development of drugs. It is also used as a synthetic intermediate in the synthesis of other drugs. Apixaban impurity 2 has been shown to be pharmacologically active, with the ability to inhibit bacterial growth by binding to DNA-dependent RNA polymerase. This compound is not toxic to mammalian cells at high concentrations, but has been shown to have some effects on the central nervous system, including depression of spontaneous motor activity and decrease in locomotor activity. Apixaban Impurity 2 is soluble in acetone and chloroform, but insoluble in water. The molecular weight of this compound is not known, but it can be determined using HPLC. Apixaban Impurity 2 has CAS number 2187409-01-2 and its molecular formula is C21H22N2O4S.</p>

<p>Diclofenac impurity B is a regulatory impurity in the drug Diclofenac, which is a nonsteroidal anti-inflammatory drug. Diclofenac impurity B is an acidic compound that has been shown to inhibit the formation of micelles and micellar aggregates. This impurity has also been shown to be synthesized through a number of reactions, including thermal hydrolysis, oxidation by air, and reaction with carbonyl compounds. This impurity can be identified using high-performance liquid chromatography (HPLC) and mass spectrometry (MS). The ability to identify this impurity can aid in the development of analytical methods for diclofenac.</p>

<p>2-Hydroxy-2,2-bis(2-thienyl) acetic acid is a long-acting bronchodilator that can be administered by inhalation. It has been used in the clinical development of medicines for the treatment of asthma and chronic obstructive pulmonary disease. 2-Hydroxy-2,2-bis(2-thienyl) acetic acid is chemically related to pyridinium compounds. It is a potent inhibitor of muscarinic receptors and has an anticholinergic profile similar to atropine. The safety profile of this drug seems to be favourable in humans with no major side effects reported so far.</p>

<p>Apixaban Impurity 3 is a reactant in medicines. It reacts with an amide to form the target compound, apixaban. Apixaban is a drug used to prevent stroke and blood clots in patients who have atrial fibrillation.</p>

<p>2-Ethoxy-4-[2-[[(1R)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid ethyl ester is a drug product that has been custom synthesized for use in research and development. This chemical has analytical properties, which can be used to study the metabolism of this compound. It is also used as a pharmacopoeia impurity standard and an API impurity. 2-Ethoxy-4-[2-[[(1R)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid ethyl ester is metabolized in vivo to form metabolites with different spectra of activity. These metabolites are used as analytical standards for HPLC analysis.</p>

Allopurinol impurity C is a product of the reaction between allopurinol and n-butyl alcohol, which occurs in the presence of sodium hydroxide solution and dimethylformamide. The reaction condition is heated to reflux for 12 hours, after which the mixture is filtered and concentrated under reduced pressure. The resultant crude product is purified by column chromatography with ethyl acetate and then recrystallized from methanol. The synthesis scheme can be found in Figure 1.

<p>5-chloro-N-[[(5R)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-5-oxazolidinyl]methyl]-2-thiophenecarboxamide (CTP) is a potent inhibitor of the cytochrome P450 enzyme CYP3A4. CTP has been shown to inhibit the metabolism of midazolam, an important drug for general anesthesia and sedation, in a study investigating the interaction between CYP3A4 inhibitors and midazolam. Ketoconazole, another inhibitor of CYP3A4, inhibited the metabolism of midazolam in vitro as well. In addition, CTP was shown to be a substrate for CYP2D6 and CYP1A2 in vitro.</p>

<p>Intermediate for tiotropium bromide synthesis</p>

<p>Ceftazidime impurity G is a heterocycle that has been found to be a potential flavonoid. It has antiviral and protease inhibitory properties, which may be due to its ability to bind to the serine protease. It also has anti-inflammatory properties, which may be due to its inhibition of tyrosine kinase activity. Ceftazidime impurity G can be used as a pharmaceutical preparation for cardiovascular diseases, cancer, hepatitis, and other diseases.</p>

<p>Travoprost (Fluprostenol isopropyl ester) is used to treat glaucoma and ocular hypertension,is a potent and selective FP prostaglandin receptor agonist.</p>

<p>Applications (E)-ethyl 4-(8-chloro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(6H)-ylidene)-3,4-dihydropyridine-1(2H)-carboxylate is an impurity of loratadine (L469575), which is a nonsedating-type histamine H1-receptor.<br>References Bruttmann, G., et al.: J. Allergy Clin. Immunol., 83, 411 (1989), Haria, M., et al.: Drugs, 48, 617 (1994)<br></p>

<p>Applications (3aR,4R,5R,6aS)-4-Formyl-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate is an intermediate in the synthesis of Prostaglandin E2 (P838610), the most common and biologically potent of mammalian prostaglandins.<br>References Radeuchel, B., et al.: Tetrahedron. Lett., 633, 9 (1975);<br></p>

<p>Applications Diclofenac Potassium Salt is a nonsteroidal anti-inflammatory compound an decycloxygenase (COX) inhibitor.<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 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>

<p>Applications 8-Epitacrolimus is a new l-pipecolic acid macrolide lactone, an important immunosuppressive drug that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. 8-Epitacrolimus is also an Epimer of Tacrolimus (F370000).<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 Skytte, D.M., et al.: J. Nat. Prod.,73, 776 (2010); Rokaw, M.D., et al.: Am. J. Physiol., 271, C194 (1996); Knoll, G.A., and Bell, R.C.: Brit. Med. J., 318, 1104 (1999);<br></p>

<p>Applications A labelled metabolite of Misoprostol. Cytoprotective PGE1 analog that prevents NSAID-induced gastric ulceration.<br>References Graham, Y., et al.: Lancet, 2, 1277 (1988), 11) Garris, R., et al.: Clin. Pharmacol., 8, 627 (1989), Karim, A., et al.: J. Clin. Pharmacol., 29, 439 (1989),<br></p>

<p>Applications Latanoprost Enol is an impurity of Latanoprost (L177280), a prostaglandin analogue used to treat glaucoma and other degenerative diseases of the eye.<br>References Resul, B., et al.: J. Med. Chem., 36, 2242 (1993);<br></p>

<p>FSC231 is a PICK1 inhibitor with analgesic activity, activating GSK-3β and ERK1/2.</p>