Reference

Preparation of N-cyclic benzenesulfonamido compounds as inhibitors of gamma-secretase

Preparation of N-cyclic benzenesulfonamido compounds as inhibitors of gamma-secretase. Neitzel, Martin L.; Marugg, Jennifer L. (Elan Pharmaceuticals, Inc., USA). PCT Int. Appl. WO 2005113542 A2 1 Dec 2005, 71 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, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, 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, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2.Several substances like 338454-52-7 may be metioned in this study. CLASS: ICM: C07D401-04. ICS: C07D209-42; C07D277-06; C07D491-10; C07D215-58; C07D241-50; C07D263-56; A61K031-4406; A61P025-28; C07D405-06; C07D235-02; C07D217-22; C07D273-00; C07D243-14; C07D471-04. APPLICATION: WO 2005-US17985 20 May 2005. PRIORITY: US 2004-572862P 20 May 2004. DOCUMENT TYPE: Patent CA Section: 25 (Benzene, Its Derivatives, and Condensed Benzenoid Compounds) Section cross-reference(s): 1, 63 Benzenesulfonamides of formula I [A = N-bonded (substituted) nitrogen-contg. There are some commonly used reagents like 338454-52-7 in this article. ring; R1-R5 = H, OH, NH2, halo, alkoxy, etc.] are prepd. as g-secretase inhibitors for use in treating or preventing cognitive disorders, such as Alzheimer's disease. Thus, II was prepd., and had IC50 value in the range of 100-1000 nM in Notch signaling assay. ..

Determination of low molecular weight aliphatic primary amines in urine as their benzenesulfonyl derivatives by gas chromatography with flame photometric detection

Determination of low molecular weight aliphatic primary amines in urine as their benzenesulfonyl derivatives by gas chromatography with flame photometric detection. Kataoka, Hiroyuki; Ohrui, Satoshi; Miyamoto, Yoshiaki; Makita, Masami (Fac. Pharm. Sci., Okayama Univ., Tsushima 700, Japan). Biomed. Chromatogr., 6(5), 251-4 (English) 1992. CODEN: BICHE2. ISSN: 0269-3879. DOCUMENT TYPE: Journal CA Section: 9 (Biochemical Methods) Section cross-reference(s): 13 A selective and sensitive method for the detn. of low mol. wt. aliph. primary amines in urine is described. These amines were converted into their benzenesulfonyl derivs. by a modified Hinsberg procedure, and measured by gas chromatog. with flame photometric detection (FPD-GC) using a DB-1 capillary column. The derivs. were very stable and provided excellent FPD responses. By FPD-GC, linear calibration curves were obtained in the range 10-200 ng of methylamine, ethylamine, n-propylamine, isobutylamine and n-butylamine using tert-butylamine as an internal std., and the detection limits of these amines were ca. 6-25 pg as the injection amt. Benzenesulfonamide derived from ammonia was converted into its N-dimethylaminomethylene deriv. which has a longer retention time, and sepd. from benzenesulfonyl derivs. of low mol. wt. primary amines on the chromatogram. The recoveries of aliph. primary amines added to urine samples were 91-107% and the relative std. deviations were 0.2-4.5%. Anal. results of aliph. primary amine contents in urine samples of normal subjects are presented.