Detail of "190448-57-8"

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A LC-MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1

A LC-MS/MS method to quantify the novel cholesterol lowering drug ezetimibe in human serum, urine and feces in healthy subjects genotyped for SLCO1B1.Some chemicals with cas registry numbers like 190448-57-8 and 163222-33-1 are also used. Oswald, Stefan; Scheuch, Eberhard; Cascorbi, Ingolf; Siegmund, Werner (Department of Clinical Pharmacology of the Peter Holtz Research Center of Pharmacology and Experimental Therapeutics, University of Greifswald, Greifswald D-17487, Germany). Journal of Chromatography, B: Analytical Technologies in the Biomedical and Life Sciences, 830(1), 143-150 (English) 2006 Elsevier B.V. CODEN: JCBAAI. ISSN: 1570-0232. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Ezetimibe (Ezetrol) is a novel cholesterol lowering drug which disposition is not fully understood in man. The authors developed a selective and high-sensitive assay to measure serum concn.-time profiles, renal and fecal elimination of ezetimibe in pharmacokinetic studies. Ezetimibe glucuronide, the major metabolite of ezetimibe was detd. by enzymic degrdn. to the parent compd. Ezetimibe was measured after extn. with Me tert-Bu ether using 4-hydroxychalcone as internal std. and liq. chromatog. coupled via an APCI interface with tandem mass spectrometry (LC-MS/MS) for detection. The chromatog. (column XTerra MS, C18, 2.1 mm ′ 100 mm, particle size 3.5 mm) was done isocratically with acetonitrile/water (60/40, vol./vol.; flow rate 200 ml/min). The MS/MS anal. was performed in the neg. ion mode (m/z transition: ezetimibe 408-271, internal std. 223-117). The validation ranges for ezetimibe and total ezetimibe were as follows: serum 0.0001-0.015 mg/mL and 0.001-0.2 mg/mL; urine and fecal homogenate 0.025-10 mg/mL and 0.1-20 mg/mL, resp. The assay was successfully applied to measure ezetimibe disposition in two subjects genotyped for the hepatic uptake transporter SLCO1B1. .

Preparation of glycoside-substituted 2-azetidinones useful as hypocholesterolemic agents

Preparation of glycoside-substituted 2-azetidinones useful as hypocholesterolemic agents. Yumibe, Nathan P.; Alton, Kevin B.; Van Heek, Margaret; Davis, Harry R.; Vaccaro, Wayne D. (Schering Corporation, USA). PCT Int. Appl.Some commonly used reagents like 190448-57-8 is used in this experiment. WO 9716455 A1 9 May 1997, 47 pp. DESIGNATED STATES: W: AL, AM, AU, AZ, BA, BB, BG, BR, BY, CA, CN, CZ, EE, GE, HU, IL, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TJ, TM, TR, TT, UA, UZ, VN, AM, AZ, BY, KG, KZ, MD, RU, TJ, TM; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07H003-04. ICS: C07H017-02; A61K031-70. APPLICATION: WO 1996-US16823 29 Oct 1996. PRIORITY: US 1995-8185 31 Oct 1995; US 1995-570847 12 Dec 1995. DOCUMENT TYPE: Patent CA Section: 33 (Carbohydrates) Section cross-reference(s): 15, 63 Hypocholesterolemic glycoside-substituted 2-azetidinones I (R = alkyl, ether, keto, alkylamine, ; R1, R2 = aryl; R3 = H, glycosyloxy; G = glycosyl) are prepd. as sugar-substituted 2-azetidinone cholesterol-lowering agent and a cholesterol bio-prepn. inhibitor for the treatment and prevention of atherosclerosis. 190448-57-8 which is the cas registry number of one of substances is just one of reagents here. Thus, 1-O-[4-[trans-(3R,4S)-1-(4-fluorophenyl)-2-oxo-3-[3-[(S)-hydroxy-4-iodo phenyl]propyl]-4-azetidinyl]phenyl]-b-D-glucuronic acid was prepd. and show a 50-98 % redn. in hepatic cholesterol esters. ..