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publicationDate 2018-12-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber SG-11201809132R-A
titleOfInvention Novel compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same
abstract INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 11111111111111111111111111111111111111111111111111111111111111111111111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/212534 Al 22 November 2018 (22.11.2018) WIPO I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every CO7D 471/04 (2006.01) A61K 31/506 (2006.01) kind of national protection available): AE, AG, AL, AM, A61K 31/437 (2006.01) CO7D 471/10 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, (21) International Application Number: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, PCT/KR2018/005516 DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, (22) International Filing Date: KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, 15 May 2018 (15.05.2018) MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (25) Filing Language: English SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, (26) Publication Language: English TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 10-2017-0060940 17 May 2017 (17.05.2017) KR kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (71) Applicant: LEGOCHEM BIOSCIENCES, INC. UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, [KR/KR]; (Munpyeongdong) 8-26, Munpyeongseo-ro, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, Daedeok-gu, Daejeon 34302 (KR). EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, _ (72) Inventors: LEE, Dae Yon; (Munpyeongdong) MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, (KR). CHAE, Sang Eun; (Munpyeongdong) 8-26, KM, ML, MR, NE, SN, TD, TG). _ Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 (KR). JUNG, Eun Mi; (Munpyeongdong) 8-26, Munpyeongseo- Published: = ro, Daedeok-gu, Daejeon 34302 (KR). YANG, Eun Hye; — with international search report (Art. 21(3)) (Munpyeongdong) 8-26, Munpyeongseo-ro, Daedeok-gu, = — Daejeon 34302 (KR). CHOI, Yoon Jeong; (Munpyeong- — _ Bong) 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 (KR). CHUNG, Chul-Woong; (Munpyeong- dong) 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon = _ 34302 (KR). SHIN, Ju Hyun; (Munpyeongdong) 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 (KR). — KIM, Yun Ki; (Munpyeongdong) 8-26, Munpyeongseo- ro, Daedeok-gu, Daejeon 34302 (KR). KWON, Hyun Jin; = (Munpyeongdong) 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 (KR). RYU, Jeong Hee; (Munpyeong- = = = — Bong) 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 (KR). BAN, Eun Hye; (Munpyeongdong) 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 (KR). = KIM, Yong Zu; (Munpyeongdong) 8-26, Munpyeongseo- ro, Daedeok-gu, Daejeon 34302 (KR). OH, Yeong Soo; = (Munpyeongdong) 8-26, Munpyeongseo-ro, Daedeok-gu, = — Daejeon 34302 (KR). CHAE, Jeiwook; (Munpyeongdong) 8-26, Munpyeongseo-ro, Daedeok-gu, Daejeon 34302 = (KR). = Agent: CHOI, Eun Sun; 5F, Sungwon Tower, 28, Yeong- (74) dong-daero 85-gil, Gangnam-gu, Seoul 06180 (KR). - 1-1 7r M (54) Title: NOVEL COMPOUNDS AS AUTOTAXIN INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING In THE SAME ei 1-1 (57) : The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions ei ---- or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical compo- GC sition containing the same. The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production 1-1 © of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney f'1 disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, 0 cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.
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