Reference

Use of the surgical wound infection model to determine the efficacious dosing regimen of retapamulin, a novel topical antibiotic

All Rights Reserved. Use of the surgical wound infection model to determine the efficacious dosing regimen of retapamulin, a novel topical antibiotic. Rittenhouse, Stephen; Singley, Christine; Hoover, Jennifer; Page, Roni; Payne, David (Department of Microbiology, MMPD CEDD, GlaxoSmithKline Pharmaceuticals, Upper Providence, PA, USA). Antimicrobial Agents and Chemotherapy, 50(11), 3886-3888 (English) 2006 American Society for Microbiology. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effect of topically applied retapamulin ointment was evaluated using various dosing regimens in the Staphylococcus aureus and Streptococcus pyogenes wound infection model. Retapamulin (1%, wt/wt) was efficacious using twice-daily (b.i. 224452-66-8 which is the cas registry number is also used here.d.) applications for 4 or 5 days. These data underpinned the decision to evaluate 1% retapamulin b.i.d. in clin. trials. .

Process for preparation of mutilin derivatives and their salts as antibacterial agents

Process for preparation of mutilin derivatives and their salts as antibacterial agents. Breen, Gary Francis; Forth, Michael Anthony; Kopelman, Susan Shumei Hu; Muller, Francis Xavier; Sanderson, Francis Dominic (Glaxo Group Limited, UK). PCT Int. Appl. WO 2005023257 A1 17 Mar 2005, 66 pp. 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, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: A61K031-439. ICS: C07D453-02. APPLICATION: WO 2004-US28159 30 Aug 2004. PRIORITY: US 2003-PV499781 3 Sep 2003. DOCUMENT TYPE: Patent CA Section: 30 (Terpenes and Terpenoids) Section cross-reference(s): 1, 63 A process for prepn. of mutilin derivs. (m = 0, 1, 2; R1 = vinyl, Et; R2 = optionally substituted non-arom. monocyclic of bicyclic group contg. one or two basic nitrogen atoms and attached through a ring carbon atom; R3 = H, OH) and their pharmaceutically acceptable salts via substitution reactions of pleuromutilin derivs. with thiols. Mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.1]oct-3-ylsulfanyl)acetate was prepd. and its salts or solvates were used as pharmaceutical compns. or formulations for topical administration used in medical therapy, particularly antibacterial therapy. Thus, mutilin 14-(exo-8-methyl-8-azabicyclo[3.2.l]oct-3-ylsulfanyl)acetate was prepd.Several substances are used for example 224452-66-8 which is its cas registry number. by reaction of pleuromutilin-22-mesylate with 3-tropinethiol. The intermediates and purifn. were described in detail. .