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(12) United States Patent (10) Patent No.: US 8,754,100 B2 Kitazawa Et Al

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(12) United States Patent (10) Patent No.: US 8,754,100 B2 Kitazawa Et Al USOO8754 100B2 (12) United States Patent (10) Patent No.: US 8,754,100 B2 Kitazawa et al. (45) Date of Patent: Jun. 17, 2014 (54) NITROGEN-CONTAINING FUSED 7,667,041 B2 2/2010 Kimura et al. HETEROCYCLIC COMPOUNDS AND THEIR 7,687,640 B2 3/2010 Kimura et al. USEAS BETAAMYLOD PRODUCTION 7,713,993 B2 5/2010 Kimura et al. INHIBITORS 7,880,009 B2 2/2011 Kimura et al. 7,897,632 B2 3/2011 Kimura et al. 7,935,815 B2 5/2011 Kimura et al. (75) Inventors: Noritaka Kitazawa, Tsukuba (JP); 7,973,033 B2 7/2011 Kimura et al. Daisuke Shinmyo, Tsukuba (JP): Koichi 8,008,293 B2 8/2011 Kimura et al. Ito, Tsukuba (JP); Nobuaki Sato, 8,048,878 B2 11/2011 Kimura et al. Tsukuba (JP); Daiju Hasegawa, 2011/0065360 A1 3/2011 Francis Tsukuba (JP); Toshiyuki Uemura, 2011/006.5696 A1 3/2011 Kimura et al. Tsukuba (JP); Toru Watanabe, Tsukuba 2011 OO86860 A1 4/2011 Kimura et al. (JP) 2011/0275822 A1 11/2011 Minamisono et al. 2012/0135981 A1 5, 2012 Wu et al. (73) Assignee: EISA R&D Management Co., Ltd., Tokyo (JP) FOREIGN PATENT DOCUMENTS (*) Notice: Subject to any disclaimer, the term of this EP 1992 618 A1 11, 2008 EP 2181992 A1 5, 2010 patent is extended or adjusted under 35 JP 2011-506335 A 3, 2011 U.S.C. 154(b) by 364 days. JP 2012-51806 A 3, 2012 JP 52.10152 B2 6, 2013 (21) Appl. No.: 13/138,504 UZ 4 136 C 4/2010 UZ 4 225 C 9, 2010 (22) PCT Filed: Feb. 24, 2010 WO 98.46605 * 10/1998 WO WO 2004f1 10350 A2 12/2004 (86). PCT No.: PCT/UP2O1 O/OS3368 (Continued) S371 (c)(1), (2), (4) Date: Nov. 16, 2011 OTHER PUBLICATIONS (87) PCT Pub. No.: WO2010/098487 Communication Under Rule 71(3) EPC issued Dec. 12, 2012, in PCT Pub. Date: Sep. 2, 2010 European Patent Application No. 08828870.9. (Continued) (65) Prior Publication Data US 2012/OO53171 A1 Mar. 1, 2012 Primary Examiner — Niloofar Rahmani Related U.S. Application Data (74) Attorney, Agent, or Firm — Birch, Stewart, Kolasch & (60) Provisional application No. 61/155,697, filed on Feb. Birch, LLP 26, 2009. (30) Foreign Application Priority Data (57) ABSTRACT A compound represented by the formula II: or a pharmaco Feb. 26, 2009 (JP) ................................. 2009-043337 logically acceptable salt or ester thereof, wherein Ring A (51) Int. Cl. represents a five-membered aromatic heterocyclic group or AOIN 43/42 (2006.01) the like fused with a non-aromatic ring group, which may be A6 IK3I/44 (2006.01) Substituted, Ring B represents a phenyl group or the like AOIN 43/40 (2006.01) which may be substituted, X1 represents a single bond or the C07D 471/02 (2006.01) like, R1 and R2 each representa C1-6 alkyl group or the like, CO7D 49/02 (2006.01) m represents an integer of 0 to 3, and n represents an integer CO7D 49.8/02 (2006.01) of 0 to 2, is effective as a therapeutic agent for a disease CO7D 40/00 (2006.01) caused by AB. (52) U.S. Cl. USPC ........... 514/300: 514/303: 514/338; 546/119; 54.6/121:546/273.4 (58) Field of Classification Search USPC ........ 546/119, 121, 273.4: 514/300, 303, 338 See application file for complete search history. (56) References Cited U.S. PATENT DOCUMENTS 5,922,724. A * 7, 1999 Teuber et al. ................. 514,256 7,618,960 B2 11/2009 Kimura et al. 20 Claims, No Drawings US 8,754,100 B2 Page 2 (56) References Cited Substantive Examination Clear Report issued Jun. 14, 2013, in Malaysian Patent Application No. PI 20052354. FOREIGN PATENT DOCUMENTS Reply filed Jun. 20, 2013, in Chinese Patent Application No. 20108.0009393.2, with English translation. WO WO 2007/102580 A1 9, 2007 Reply filed Jul. 10, 2013, in response to the Office Action issued May WO WO 2009,073,777 A1 6, 2009 2, 2013, in Mexican Patent Application No. MX/a/2011/008501, with WO WO 2010/025.197 A1 3, 2010 English translation. WO WO 2010-097372 A1 9, 2010 Official Action issued Aug. 16, 2013, in Russian Patent Application WO WO 2010-097395 A1 9, 2010 No. 2011 139132, with English translation. WO WO 2010/098488 A1 9, 2010 Communication pursuant to Article 94(3) EPC issued Jul. 30, 2013, WO WO 2010/098495 A1 9, 2010 in European Patent Application No. 05743758.4. OTHER PUBLICATIONS Notice Before Allowance issued Aug. 5, 2013, in Israeli Patent Appli cation No. 203778, with English translation. Extended European Search Report issued Jan. 22, 2013, in European Notification of Defects issued Aug. 12, 2013, in Israeli Patent Appli Patent Application No. 1219 1398.2. cation No. 213973, with English translation. Notification to Go through Formalities of Registration issued Dec. Notification of the Second Office Action issued Jul. 15, 2013, in 28, 2012, in Chinese Patent Application No. 20058.0020584.8, with Chinese Patent Application No. 20108.0009393.2, with English English translation. translation. Official Letter and Search Report issued Janaury 29, 2013, in Taiwan Office Action issued Aug. 23, 2013, in U.S. Appl. No. 12/974.447. Patent Application No. 97132893, with English translation. Response filed Aug. 13, 2013, in reply to the Invitation Pursuant to Response filed Feb. 13, 2013, in reply to the First Examination Report Rules 70a(2) and 70(2) EPC issued in European Patent Application issued Oct. 17, 2012, in Australian Patent Application No. No. 12191398.2. 2008292390. Response filed Aug. 29, 2013, in reply to the Office Action issued Jun. Response filed Janaury 22, 2013, in reply to the Subsequent Substan 25, 2013, in Mexican Patent Application No. MX/a/2010/002098, with English translation of claims. tive Examination Report issued Nov. 23, 2012. in Philippine Patent Response filed Jul. 25, 2013, in reply to the Office Action issued May Application No. 1-2010-500161. 7, 2013, in Israeli Patent Application No. 203778, with English Response filed Jan. 14, 2013, in reply to the First Office Action issued translation. in Chinese Patent Application No. 200880 104785.X. with English Reply filed Nov. 14, 2013, in response to the Non-Final Office Action translation. issued Aug. 23, 2013, in U.S. Appl. No. 12/974.447. Response filed Jan. 15, 2013, in reply to the Official Notice of Results International Search Report, dated Jul. 30, 2010 in PCT/JP2010/ of the Substantive Examination No. 38629/SHTT-SC2 issued Nov. O53368. 26, 2012, in Vietnamese Patent Application No. 1-2010-00393, with Examiner's Reportisued on Patent of Invention Application issued English translation. Jun. 15, 2012, in Chilean Patent Application No. 2098-2011, with Response filed Jan. 16, 2013, in reply to the Substantive Examination English translation. Adverse Report issued Dec. 31, 2012, in Malaysian Patent Applica Response filed Sep. 6, 2012, in reply to Examiner's Report Issued on tion No. PI 20052354. Patent of Invention Application issued Jun. 15, 2012, in Chilean Substantive Examination Adverse Report issued Dec. 31, 2012, in Patent Application No. 2098-2011, with English translation. Malaysian Patent Application No. PI 20052354. Amendment Order issued Jul. 17, 2012, in Thai Patent Application Response filed Mar. 4, 2013, in reply to the Request According to No. 1101001732, with English translation. Section 18 issued Nov. 13, 2012, in Israeli Patent Application No. Invitation to Respond to Written Opinion issued Dec. 18, 2012, in 214780, with English translation. Singapore Patent Application No. 201105886-4. Response filed Apr. 12, 2013, in reply to the Communication Under Search Report issued Nov. 15, 2012, in Singapore Patent Application Rule 71(3) EPC issued Dec. 13, 2012, in European Patent Applica No. 201105886-4. tion No. 10708824.7. Written Opinion issued Nov. 15, 2012, in Singapore Patent Applica First Office Action issued Feb. 5, 2013, in Chinese Patent Application tion No. 201105886-4. No. 201080009393.2, with English translation. Response filed Dec. 27, 2012 in reply to the Invitation to Respond to Notice of Acceptance issued Mar. 25, 2013, in Australian Patent Written Opinion issued Dec. 18, 2012, in Singapore Patent Applica Application No. 2008292390. tion No. 201105886-4. Notice of the Result of Substantive Examination of a Patent Appli Examination Report issued Dec. 7, 2012, in Pakistan Patent Appli cation issued Jun. 16, 2013, in GCC Patent Application No. 11619, cation No. 143/2010. with English translation. Examination Report issued Dec. 7, 2012, in Pakistan Patent Appli Notification of Defects Prior to Allowance issued May 7, 2013, in cation No. 657/2011. Israeli Patent Application No. 203778, with English translation. Response filed Dec. 21 2012, in reply to the Office Action issued Jul. Notification of Reason for Rejection issued May 7, 2013, in Japanese 17, 2012, in Thai Patent Application No. 1101001732, with English Patent Application No. 2009-530 168, with English Translation. translation. Notification to Grant Patent Right issued Jun. 6, 2013, in Chinese First Office Action issued Jan. 25, 2013, in Chinese Patent Applica Patent Application No. 200880 14785.X. with English translation. tion No. 2010600092889, with English translation. Office Action issued Jun. 25, 2013, in Mexican Patent Application Response filed Feb. 15, 2013, in reply to the Office Action issued Nov. No. MX/a/2010/002098, with English translation. 15, 2012, in Chilean Patent ApiNication No. 2098-2011, with English Office Action issued May 23, 2013, in Vietnamese Patent Application translation. No. 1-2010-00393, with English translation. Request for Substantive Examination filed Jan. 25, 2013, in Indone Reply filed Jun.
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