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E30 SEM. O.C. Disclosed Is a Compound Represented by the Formula (1) (51) Int

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E30 SEM. O.C. Disclosed Is a Compound Represented by the Formula (1) (51) Int USOO9453000B2 (12) United States Patent (10) Patent No.: US 9.453,000 B2 Kimura et al. (45) Date of Patent: *Sep. 27, 2016 (54) POLYCYCLIC COMPOUND (56) References Cited (75) Inventors: Teiji Kimura, Tsukuba (JP); Noritaka U.S. PATENT DOCUMENTS Kitazawa, Tsukuba (JP); Toshihiko 3,470,167 A 9, 1969 Sarkar Kaneko, Tsukuba (JP); Nobuaki Sato, 3,989,816 A 1 1/1976 Rajadhyaksha Tsukuba (JP); Koki Kawano, Tsukuba 4,910,200 A 3, 1990 Curtze et al. (JP): Koichi Ito, Tsukuba (JP); 5,281,626 A 1/1994 Oinuma et al. M s Tak ishi Tsukub JP 5,563,162 A 10, 1996 Oku et al. amoru Takaishi Tsukuba (JP); 5,804,577 A 9, 1998 Hebeisen et al. Takeo Sasaki, Tsukuba (JP); Yu 5,985,856 A 11/1999 Stella et al. Yoshida, Tsukuba (JP); Toshiyuki 6,235,728 B1 5, 2001 Golik et al. Uemura, Tsukuba (JP); Takashi Doko, g R 1939. E. al. Its SE E. Shinmyo, 7,138.414 B2 11/2006 Schoenafingereatch et al. et al. sukuba (JP); Daiju Hasegawa, 7,300,936 B2 11/2007 Parker et al. Tsukuba (JP); Takehiko Miyagawa, 7,314,940 B2 1/2008 Graczyk et al. Hatfield (GB); Hiroaki Hagiwara, 7,618,960 B2 11/2009 Kimura et al. Tsukuba (JP) 7,667,041 B2 2/2010 Kimura et al. 7,687,640 B2 3/2010 Kimura et al. 7,713,993 B2 5/2010 Kimura et al. (73) Assignee: EISAI R&D MANAGEMENT CO., 7,737,141 B2 6/2010 Kimura et al. LTD., Tokyo (JP) 7,880,009 B2 2/2011 Kimura et al. 7,897,632 B2 3/2011 Kimura et al. (*) Notice: Subject to any disclaimer, the term of this 7,935,815 B2 5/2011 Kimura et al. patent is extended or adjusted under 35 SS R: 38H SA U.S.C. 154(b) by 1597 days. 8,048,878www. B2 11/2011 KimuraUa et al.a This patent is Subject to a terminal dis- 2001/0051642 A1 12/2001 Ahn et al. claimer. 2002/O128263 A1 9, 2002 Mutel et al. (Continued) (21) Appl. No.: 12/671,873 FOREIGN PATENT DOCUMENTS (22) PCT Filed: Aug. 28, 2008 CN 1668593. A 9, 2005 (86). PCT No.: PCT/UP2008/065.365 DE 3541716 A1 5, 1987 S 371 (c)(1), (Continued)Continued (2), (4) Date: Sep. 23, 2010 OTHER PUBLICATIONS (87) PCT Pub. No.: WO2009/028588 Communication pursuant to Article 94(3) EPC issued Jul. 30, 2013 in European Patent Application No. 05743758.4. PCT Pub. Date: Mar. 5, 2009 (Continued) (65) Prior Publication Data US 2011 FOOO9619 A1 Jan. 13, 2011 Primary Examiner — Susanna Moore (74) Attorney, Agent, or Firm — Birch, Stewart, Kolasch & (30) Foreign Application Priority Data Birch, LLP Aug. 31, 2007 (JP) ................................. 2007-225045 (57) ABSTRACT E30 SEM. O.C. Disclosed is a compound represented by the formula (1) (51) Int. Cl. (I) CO7D 47L/04 (2006.01) A6 IK 3/437 (2006.01) G) ()-X-G) CO7D 487/04 (2006.01) CO7D 49.8/04 (2006.01) CO7D 403/0 (2006.01) or a pharmacologically acceptable salt thereof, which is A61 P 25/28 (2006.01) effective as a therapeutic or prophylactic agent for a disease CO7D 403/04 (2006.01) induced by AB, wherein Ari represents an imidazolyl group (52) U.S. Cl. which may be substituted with a C1-6 alkyl group, or the CPC ........... C07D 403/10 (2013.01); C07D 471/04 like; Ara represents a phenyl group which may be substituted (2013.01); C07D 487/04 (2013.01); C07D with a C1-6 alkoxy group, or the like: X represents a double 498/04 (2013.01) bond, or the like; and Het represents a triazolyl group or the (58) Field of Classification Search like which may be substituted with a C1-6 alkyl group or the CPC ........................... A61K 31/437; C07D 471/04 like, or the like. USPC ........................................... 544/112: 514/299 See application file for complete search history. 4 Claims, No Drawings US 9,453,000 B2 Page 2 (56) References Cited JP 2007-523903. A 8, 2007 JP 2011-506335 A 3, 2011 U.S. PATENT DOCUMENTS JP 2012-51806 A 3, 2012 JP 52.10152 B2 6, 2013 2002/0183324 A1 12/2002 Jacobson et al. RU 2001 126135 A 7, 2003 2003. O195201 A1 10, 2003 Bo et al. TW 379224 B 1, 2000 2003/0208082 A1 11, 2003 Mutel et al. TW 20040O824 1, 2004 2003,0225070 A1 12, 2003 Mutel et al. UZ 4 136 C 4/2010 2004/0006062 A1 1/2004 Smallheer et al. UZ 4 225 C 9, 2010 2004/0034096 A1 2/2004 Jolidon et al. WO WO 87,02587 A1 5, 1987 2004/0038969 A1 2/2004 Doherty et al. WO WO 91/12237 A1 8/1991 2004/0063770 A1 4, 2004 Ahn et al. WO WO95/21832 A1 8/1995 2004/0087798 A1 5, 2004 Yamada WO WO 96,105.59 A1 4f1996 2004/O127494 A1 7, 2004 Parker et al. WO WO 97,14417 A1 4f1997 2004/O127555 A1 7, 2004 Snow et al. 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