(12) International Application Status Report

Received at International Bureau: 04 March 2010 (04.03.2010)

Information valid as of: 06 August 2010 (06.08.2010)

Report generated on: 23 July 2019 (23.07.2019)

(10) Publication number: (43) Publication date: (26) Publication language:
WO 2010/09566326 August 2010 (26.08.2010) Japanese (JA)

(21) Application number: (22) Filing date: (25) Filing language:
PCT/JP2010/05237417 February 2010 (17.02.2010) Japanese (JA)

(31) Priority number(s): (32) Priority date(s): (33) Priority status:
61/202,321 (US)18 February 2009 (18.02.2009) Priority document received (in compliance with PCT Rule 17.1)

(51) International Patent Classification:
C07D 401/14 (2006.01); A61K 31/454 (2006.01); A61K 31/506 (2006.01); A61K 31/519 (2006.01); A61K 31/5377 (2006.01); A61K 31/55 (2006.01); A61P 1/00 (2006.01); A61P 1/02 (2006.01); A61P 1/04 (2006.01); A61P 1/08 (2006.01); A61P 1/12 (2006.01); A61P 1/16 (2006.01); A61P 1/18 (2006.01); A61P 3/04 (2006.01); A61P 3/06 (2006.01); A61P 3/10 (2006.01); A61P 7/00 (2006.01); A61P 9/00 (2006.01); A61P 9/04 (2006.01); A61P 9/10 (2006.01); A61P 9/12 (2006.01); A61P 11/00 (2006.01); A61P 13/10 (2006.01); A61P 13/12 (2006.01); A61P 15/00 (2006.01); A61P 17/02 (2006.01); A61P 17/06 (2006.01); A61P 19/02 (2006.01); A61P 19/06 (2006.01); A61P 19/10 (2006.01); A61P 21/04 (2006.01); A61P 25/00 (2006.01); A61P 25/02 (2006.01); A61P 25/28 (2006.01); A61P 27/02 (2006.01); A61P 27/12 (2006.01); A61P 27/16 (2006.01); A61P 29/00 (2006.01); A61P 31/00 (2006.01); A61P 35/00 (2006.01); A61P 35/02 (2006.01); A61P 43/00 (2006.01); C07D 405/14 (2006.01); C07D 413/14 (2006.01); C07D 487/04 (2006.01)

(71) Applicant(s):
TAKEDA PHARMACEUTICAL COMPANY LIMITED [JP/JP]; 1-1, Doshomachi 4-chome, Chuo-ku, Osaka-shi, Osaka 5410045 (JP) (for all designated states except US)
RIKIMARU, Kentaro [JP/JP]; c/o TAKEDA PHARMACEUTICAL COMPANY LIMITED, 17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka-shi, Osaka 5328686 (JP) (for US only)
IMOTO, Hiroshi [JP/US]; #206, 1742 Sand Hill Road, Palo Alto, California 94304 (US) (for US only)
KAMAURA, Masahiro [JP/JP]; c/o TAKEDA PHARMACEUTICAL COMPANY LIMITED, 17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka-shi, Osaka 5328686 (JP) (for US only)

(72) Inventor(s):
RIKIMARU, Kentaro; c/o TAKEDA PHARMACEUTICAL COMPANY LIMITED, 17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka-shi, Osaka 5328686 (JP)
IMOTO, Hiroshi; #206, 1742 Sand Hill Road, Palo Alto, California 94304 (US)
KAMAURA, Masahiro; c/o TAKEDA PHARMACEUTICAL COMPANY LIMITED, 17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka-shi, Osaka 5328686 (JP)

(74) Agent(s):
TAKASHIMA, Hajime; Meiji Yasuda Seimei Osaka Midosuji Bldg., 1-1, Fushimimachi 4-chome, Chuo-ku, Osaka-shi, Osaka 5410044 (JP)

(54) Title (EN): FUSED HETEROCYCLIC RING COMPOUND
(54) Title (FR): COMPOSÉ À NOYAU HÉTÉROCYCLIQUE FUSIONNÉ
(54) Title (JA): 縮合複素環化合物

(57) Abstract:
(EN): Disclosed is a compound represented by formula (I) or a salt thereof, which has GPR 119 agonist action and excellent medicinal effects useful for prevention/treatment of diabetes, adiposis and the like. In the formula, P represents a substituted 6-membered aromatic ring; Q represents a (substituted) 6-membered aromatic ring; A1 represents CR4aR4b, NR4c, O, S, SO, SO2 (wherein R4a-R4c each represents H or the like); L1 represents a (substituted) C1-5 alkylene; L2 represents a bond, a (substituted) C1-3 alkylene; L3 and L4 each represents a (substituted) C1-3 alkylene; R1 represents H, X, CN, a (substituted) hydrocarbon, a (substituted) heterocyclic ring or a (substituted) OH, or alternatively combines with A1 to form a (substituted) 4- to 8-membered (heterocyclic) ring; R2 represents H, CN or a (substituted) hydrocarbon; and R3a represents -COSRA1 or a (substituted) 5- or 6-membered aromatic ring (wherein RA1 represents a (substituted) hydrocarbon or a (substituted) heterocyclic ring).)
(FR): L'invention concerne un composé représenté par la formule (I) ou un sel de ce composé, qui présente une action d'antagoniste GPR119 et des effets médicinaux excellents utiles à la prévention/au traitement des diabètes, de l'adipose et des maladies similaires. Dans la formule, P représente un noyau aromatique substitué à 6 chaînons; Q représente un noyau aromatique (substitué) à 6 chaînons; A1 représente un groupe CR4aR4b, NR4c, O, S, SO ou SO2 (où R4a à R4c représentent chacun un atome H ou un élément similaire); L1 représente un groupe alkylène en C1 à C5 (substitué); L2 représente un liaison, un groupe alkylène en C1 à C3 (substitué); L3 et L4 représentent chacun un groupe alkylène en C1 à C3 (substitué); R1 représente un atome H, X, un groupe CN, un hydrocarbure (substitué), un noyau hétérocyclique (substitué) ou un groupe OH (substitué), ou se combine sinon à A1 pour former un noyau (hétérocyclique) (substitué) à 4 à 8 chaînons; R2 représente un atome H, un groupe CN ou un hydrocarbure (substitué); et R3a représente -COSRA1 ou un noyau aromatique (substitué) à 5 ou 6 chaînons (où RA1 représente un hydrocarbure (substitué) ou un noyau hétérocyclique (substitué)).
(JA):  GPR119アゴニスト作用を有し、糖尿病、肥満症等の予防・治療に有用であり、かつ優れた薬効を有する、下記式(1)で表される化合物またはその塩。 P:置換6 員芳香環、Q:(置換)6 員芳香環 A1:CR4aR4b,NR4c,O,S,SO,SO2 {R4a-4c:H 等} L1:(置換)C1-5 アルキレン、L2:結合,(置換)C1-3 アルキレン、 L3-4:(置換)C1-3 アルキレン、 R1:H,X,CN,(置換)炭化水素,(置換)複素環,(置換)OH 又はA1 と共に(置換)4-8員(複素)環、R2:H,CN,(置換)炭化水素、R3a:-COSRA1,(置換)5-6 員芳香環{RA1:(置換)炭化水素,(置換)複素環}

International search report:
Received at International Bureau: 18 March 2010 (18.03.2010) [JP]

International Report on Patentability (IPRP) Chapter II of the PCT:
Not available

(81) Designated States:
AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, 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, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, 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
European Patent Office (EPO) : 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, SE, SI, SK, SM, TR
African Intellectual Property Organization (OAPI) : BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG
African Regional Intellectual Property Organization (ARIPO) : BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW
Eurasian Patent Organization (EAPO) : AM, AZ, BY, KG, KZ, MD, RU, TJ, TM