TETRAHYDROQUINOLINE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS

• Main Authors: NOGUCHI, Hirohide, ANDO, Kazuo, SONE, Toshihiko, ARANO, Yoshimasa, TOYOSHIMA, Kazuki, MATSUBARA, Koki
• Format: Patent
• Language: English
• Published: 27.08.2019
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 20 September 2018 (20.09.2018) WIP0 I PCT omit IIl °nolo mu im im ono iflo (10) International Publication Number WO 2018/168818 Al (51) International Patent Classification: C07D 215/48 (2006.01) A61P 37/00 (2006.01) A61K 31/47 (2006.01) A61P 43/00 (2006.01) A61K 31/4709 (2006.01) CO7D 215/20 (2006.01) A61K 31/4747 (2006.01) CO7D 221/04 (2006.01) A61K 31/5375 (2006.01) CO7D 401/06 (2006.01) A61K 31/5386 (2006.01) CO7D 401/12 (2006.01) A61P 9/06 (2006.01) CO7D 405/12 (2006.01) A61P 13/12 (2006.01) CO7D 417/12 (2006.01) A61P 19/00 (2006.01) CO7D 491/08 (2006.01) A61P 25/00 (2006.01) CO7D 498/10 (2006.01) A61P 29/00 (2006.01) COIF 7/18 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/JP2018/009627 (22) International Filing Date: 13 March 2018 (13.03.2018) (25) Filing Language: English (26) Publication Language: English = (30) Priority Data: 2017-047794 13 March 2017 (13.03.2017) JP (71) Applicants: RAQUALIA PHARMA INC. [JP/JP]; 1-21-19 Meieki Minami, Nakamura-ku, Nagoya-shi, Aichi, 4500003 (JP). ASAHI KASEI PHARMA CORPO- RATION [JP/JP]; 1-1-2 Yurakucho, Chiyoda-ku, Tokyo, 1000006 (JP). (72) Inventors: NOGUCHI, Hirohide; c/o RaQualia Phar- ma Inc., 1-21-19 Meieki Minami, Nakamura-ku, Nagoya- shi, Aichi, 4500003 (JP). ARANO, Yoshimasa; c/o RaQualia Pharma Inc., 1-21-19 Meieki Minami, Nakamu- ra-ku, Nagoya-shi, Aichi, 4500003 (JP). ANDO, Kazuo; c/o RaQualia Pharma Inc., 1-21-19 Meieki Minami, Naka- mura-ku, Nagoya-shi, Aichi, 4500003 (JP). TOYOSHI- MA, Kazuki; c/o Asahi Kasei Pharma Corporation, 1-105, Kanda Jinbocho, Chiyoda-ku, Tokyo, 1018101 (JP). SONE, Toshihiko; c/o Asahi Kasei Pharma Corporation, 1-105, Kanda Jinbocho, Chiyoda-ku, Tokyo, 1018101 (JP). MATSUBARA, Koki; c/o Asahi Kasei Pharma Corpora- tion, 1-105, Kanda Jinbocho, Chiyoda-ku, Tokyo, 1018101 (JP). (74) Agent: IWATANI, Ryo; KEIHAN Dojima Bldg. 6F, 1-31, Dojima 2-chome, Kita-ku, Osaka-shi, Osaka, 5300003 (JP). (81) Designated States (unless otherwise indicated, for every kind of national protection available): 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, DJ, DK, DM, DO, 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, KR, KW, KZ, LA, LC, LK, LR, LS, 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, SA, 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) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (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). Published: - with international search report (Art. 21(3)) 1-1 0 (57) : The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable \" salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the 0 treatment of various disorders which are mediated via the P2X7 receptor. (54) Title: TETRAHYDROQUINOLINE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS