Detail of "147511-69-1"

Reference

Celullar cholesterol absorption modifiers

All Rights Reserved. Celullar cholesterol absorption modifiers. Gardiner, Elisabeth M.; Duron, Wergio G.; Massari, Mark E.; Severance, Daniel L.; Semple, Joseph E.; Smith, Nicholas D. ( Kalypsys, Inc., USA). PCT Int. Appl. WO 2007008529 A2 18 Jan 2007, 76pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: A61K. 147511-69-1 and 312946-11-5 are also in the experiment. APPLICATION: WO 2006-US26197 6 Jul 2006. PRIORITY: US 2005-697687P 8 Jul 2005; US 2005-727652P 17 Oct 2005; US 2006-781972P 13 Mar 2006. DOCUMENT TYPE: Patent CA Section: 1 (Pharmacology) The present invention relates to compds. and methods useful as inhibitors of cholesterol absorption for the treatment or prevention of cholesterol-related diseases, such as atherosclerosis (Markush structures given). Fifty two novel arom. diaza derivs. that prevent cholesterol absorption by inhibitionof NPC1L1 was prepd. and their antihypercholesterolemic activity is shown. .

Analysis of the global RNA expression profiles of skeletal muscle cells treated with statins

All Rights Reserved. Analysis of the global RNA expression profiles of skeletal muscle cells treated with statins. Morikawa, Shigeru; Murakami, Takeshi; Yamazaki, Hiroyuki; Izumi, Akashi; Saito, Yasushi; Hamakubo, Takao; Kodama, Tatsuhiko ( Laboratory for Systems Biology and Medicine, RCAST, The University of Tokyo, Tokyo, Japan). Journal of Atherosclerosis and Thrombosis, 12(3), 121-131 (English) 2005 Japan Atherosclerosis Society. CODEN: JATHEH. ISSN: 1340-3478. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 3 The 3-hydroxy-3-methylglutaryl CoA reductase inhibitors (statins) are the most effective drugs for hypercholesteloremia. However, a significant side effect of statin treatment is rhabdomyolysis. In order to study the effect of statins in skeletal muscle cells, we used a DNA microarray anal. to investigate the changes in gene expression profiles brought about by statins in two skeletal muscle cell lines, namely, differentiated rat L6 myotubes and a human skeletal muscle cell line (hSkMC). In both cell lines, the statins (atorvastatin, cerivastatin and pitavastatin) induced the expression of four genes, which relate to cholesterol metab., namely, HMG-CoA synthase 1, HMG-CoA reductase, farnesyl diphosphate synthase and isopentenyl-diphosphate delta isomerase. Statin inhibited the synthesis of cholesterol at least five times more effectively in hSkMCs than in the hepatocytes. In addn., unlike in osteoblasts or coronary artery smooth muscle cells, statins upregulated the mRNA expression of cholesterol-assocd.In this experiment, several chemicals are used like 147511-69-1 and 145599-86-6 enzymes in hSkMCs. These results provide basic information on skeletal muscle cells treated with statins and indicate that the cells are sensitive to the inhibition of HMG-CoA reductase, which may be related to the pathogenesis of muscle damage in statin therapy. .