Patent SG-11201408359P-A (SG)
Title: Novel indanesulfamide derivative
Inventor: KAZUTA YUJI
IPC: A61K31/277
Filed: 2013-06-17
Abstract: (i2) mwu ft iz s-5 iv x m £ titz s issaj n d9) mm IHMMi _ (43) 2013 ^ 12 ^ 27 0(27.12.2013) WIPO I PCT (10) WO 2013/191144 A1 (51) C07C 307/08 (2006.01) A61K31/18 (2006.01) (21) (22) (25) g&fflgia)] =E. DP . A61K 31/277 (2006.01) A61P 25/08 (2006.01) PCT/JP2013/066623 2013 ^ 6 ^ 17 0(17.06.2013) 0*lg (26) @U8&M©Wi§: (30) fiBfcftf '— 1 61/662626 2012^6^ 21 0(21.06.2012) US 61/709737 2012 ^ 10 ^ 4 0(04.10.2012) US 61/751331 2013 ^1^110(11.01.2013) US (71) ttiHA: X—!f>r • T-)l • • T> K 7 -r- s • > h tt_(EISAI R&DJVIANAGE- MENT CO., LTD.) [JP/JP]; T 1128088 ICijliRXjS. E Al^JII E3T g 6 H 1 0-^- Tokyo (JP). (72) fj(H £f \"(KAZUTA Yu ji); T3002635 ^ limm^^5Tg 1 #±fe3 Ibaraki (JP). ;Jl ill *r (WATANABE Toru); T 3002635 18|0 < lirfT^ ^5TI1S»3 X-- PJT fa Ibaraki (JP). 5BJ ^ — (SORIMACHI Keii- chi); T 3002635 l#fO< I £rfT|£ ?•£-£• 5 T g 1 # Ibaraki (JP). StU oV-fc^SAITO Minako); T 3002635 »o< iimm^^5Tg 1 Site 3 X—yvtt Ibaraki (JP). H\"(KITA Yoichi); T 3002635 lifO < l£~ rfTKft-n 5 Tg 1#Jft3 X— +f J ttSC^a®[S®W5ERlT A Ibaraki (JP). EEI 4^ ?IJ & (TANAKA Toshiaki); T 1128088 ^5liRS;5l|E/h5JI| 4Tg 6# 1 0 X — +P >f 3; £ a fa Tofyo (JP). M UJ Si (HIGASHIYAMA Hiroyuki); T 3002635 IS§0< 5Tg 1 #±fe3 x—yvtta^a Ibaraki (JP). ft H $££.(HANADA Takahisa); T 3002635 5 T g 1 #±t3 x— Ibaraki (JP). £(TERAMOTO Tetsuyuki); T 3002635 ISIO < 5 T g 1 #±fe 3 X— Ibaraki (JP). /J\£f ftS&(KOSASA Takashi); T 3002635 lilO < li fI^5Tg1ftt3 X—!f>rtt3C^a®[ ;J$EJF R)T fa Ibaraki (JP). 5 J11 (ISHIKAWA Yukio); T 3002635 li|0< lirtT MJin 5 T g imm^i (54) Title: NOVEL INDANESULFAMIDE DERIVATIVE (54) : §T£H >£* >X)\sZ> y £ Rl§2»ft AA Vehicle (%) lOmg/kgp.o. 20mg/kgp.o. 50mg/kgp.o. (%) •t •t 0\ i-H cn i-H o CJ o & p<0.01 AA Compound of example 1 p<0.001 p<0.0001 (57) Abstract: A novel indanesulfamide com­ pound, such as N-[(lS)-2,2,5,7-tetrafluoro-2,3- dihydro-lH-inden-l-yl]- sulfamide, N-[(1S)- 2,2,4,7-tetrafluoro-2,3-dihydro- 1H- inden-1- yl]sulfamide and (+)-N-(2,2,4,6,7- pentafluoro- 2,3-dihydro-lH-inden-l-yl)sulfamide, or a pharmaceutically acceptable salt thereof has an effect of improving the severity (score) of an at­ tack in a mouse kindling model and therefore can be expected to serve as a therapeutic agent for epilepsy. (57)®$: N- [ ( 1 S) -2, 2, 5, 7 -7- h^7;U^-P-2, 3—V t RP - 1 H -4 >x>- 1 )\A XJl/77? h\ N - [ ( 1 S) - 2, 2, 4, 7-f h77JI/tO-2, 3 — y t K • — 1 H - - >T W > 1 -'f ;u ] X )l Z> 7 £ h\ ( +) - - N (2, 2, 4, 6, • — 2 , 3-5/th'O-IH-Of 5 K£<!fa>$fr X + > K U X/^Ef^Ucfcl^TfgfFS SJS (x=ir) §f= ft, o WO 2013/191144 AlllllllH Ibaraki (JP). (74) ft II A. 5?fit, ^(HASIX.AWA Yoshiki etal.); T 1000005 E ACDfa ~ T @ 1 MY PLAZA Tokyo (JP). (8i) ti^@(^a>&i^PBy, AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) (^am^su > ±T(Dmm(Dfcm% 11^ nlfb): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), J- — 7 V T (AM, AZ, BY, KG, KZ, RU, TJ, TM), 3 — • V / ^ (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). - (&&£ 21 &(3))