Patent SG-11201408711P-A (SG)
Title: Novel rebamipide prodrug, method for producing same, and usage thereof
Inventor: CHO EUI-HWAN
IPC: C07D413/12
Filed: 2013-06-26
Abstract: (43) ^n^7B Q 2014 \lll3^ (03.01.2014) W1POIPCT (10) ^1^7111*1 Jl WO 2014/003424 A1 (51) ^1^^: C07D 215/227 ( 2006.01) C07D 413/12 (2006.01) A61K31/4704 (2006.01) A61P1/04 (2006.01) PCT/KR2013/005 622 2013 6 € 26 H (26.06.2013) (2i) (22) (25) (26) iMISH: (30) 10-2012-0068394 2012 ^ 6 € 26 H (26.06.2012) KR (71) (SAM JIN PHARMA­ CEUTICAL CO., LTD.) [KR/KR]; 121-836 *i-irA] v}g_ 338-8, Seoul (KR). ( ^ ) <^| <>1 ^ i (ASTECH. CO., LTD.) [KR/KR]; 441-813 ^ 7] £ A] ^A^ 958 ^TEM^HIe] 508 J:, Gyeonggi- do (KR). (72) 2^]^: (CHO, Eui-Hwan); 140-030 '•\"] vHrV^-l 430 <S^l?!: dM l WH. 7 0 0 110T? 701 J:, Seoul (KR). (CHOI, Sung Ju); 137-060 *| -£-4 : rVl A 1 ¥%S-21^ 29-6 502 J:, Seoul (KR). (LEE, Sung Woo); 150-918 *i 1^1 ^S|^S3?1 10 201-2904, Seoul (KR). -^1^# (SHIN, Hee Jong); 420- 761 ^7]£ Jf^A] ^T:]^ =f 2^ 1404 ^ 101 J:, Gyeonggi-do (KR). ^ (KWON, Ho Seok); 441-741 ^-fiA] ^A}^- ^A}=- tfA>o]-3|-E 401 v> 702 SV , Gyeonggi-do (KR). <=>1 A \"S\" (LEE, Jae Woong); 443-780 ^7]£ ^A] a\" iir%! °1-5|-H. 232 1504 3L, Gyeonggi-do (KR). H (JOO, Jeong Ho); 427-708 7] £ A] S«J=S 110, 620 -o- 401 SV, Gyeonggi-do (KR). ^3 (KIM, Hyun Tae); 443-712 ^ 7] £ =r€ A 1 ^ ^^ cfl HJ 2 ^ ^ 1 101 607 J:, Gyeonggi-do (KR). ^-T\" fl (SONG, Woo-Heon); 441-390 ^7]£ =r-fiA] ^A^ T^T9.°1\"1 0 J^3. 1 A ~E\ 301 903 3L, Gyeonggi-do (KR). (YOON, Jong Bae); 440-735 ^ 7] £ -?-[ A 1 ^S20^^ 25 SK^SK^KS 625-1203, Gyeonggi-do (KR). ^71*} (PARK, Ki Seok); 429-240 ^7]£ Al^Al A]«:q]S- 268 ^ 75 H !! 1 1401-404, Gyeonggi-do (KR). (PARK, Ho Joon); 442-752 ^ 7] £ =r-fiA] -f 2 -f T?Pr ^ 1 #*1 101 ^ 306 J:, Gyeonggi-do (KR). (NAM, Ho Tae); 441-440 ^7]£ =r-fiA] ^A^ 54 502 3L, Gyeonggi-do (KR). (74) tflel®!: 1JJ-XI3: (PARK, Ji Ho); 135-915 *1-8^1 ^Yh'- ^ ^ 677-18 2:°] 3 f\ Seoul (KR). (81) *13^ (l^ 2 ! iA] 7} ?V,7}^-?!: 5L& ^ e] S] iL J:# ^ ): 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, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, [[}§ ^ (54) Title: NOVEL REBAMIPIDE PRODRUG, METHOD FOR PRODUCING SAME, AND USAGE THEREOF = (54)1-^31 ^ : AJ^ E]|U[D|H|H 2^*11 SI =L J||5yB4 •t CJ •t m o o o CJ o & BB • prodrug 9 3 HI • Rebamipide SS^jHI cc 7min 10min AA AA AA ... min BB prodrug ... area ratio CC ... Rebamipide area ratio (57) Abstract: The present invention relates to a novel rebamipide prodrug, method a for producing same, and usage thereof, and more specifically to a novel rebamipide prodrug, method a for producing same, and a pharmaceutical composition containing same as an active ingredient. The novel rebamipide prodrug according to the present invention has an absorption rate in the body approx - imately 25 times the absorption rate of rebamipide, and thus can be effectively used, in place of rebamipide, in preventing or treating gastric ulcer, acute and chronic gastritis, dry eye syndrome, cancer, degenerative joint disease, rheumatoid arthritis or obesity. (57) si; 3]H. ^1^1, °11- Hj-ia ^ o]S ^SAi,^ ^ o] A]^ H°il «lsfl ^ 25 tiflSAi, 5114^1^ — !• ^ \"ST 1 H SI V]v)-Sr tri^ A}-^ ^ t -e-SL^^-5- WO 2014/003424 AI III llll IIII III III Hill III III III Hill II 111 lllll 111 llll mill llll 111 llll 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) *1^ Of &A]7} tV, 7}^ JSL-s- fSr°l « ifl e] $] iL J:# ^ ); ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), -rr A 1 °> (AM, AZ, BY, KG, KZ, RU, TJ, TM), -rr't! (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). — Ai 4 *N1 (£?]= *11 21 2(3))