(12) International Application Status Report

Received at International Bureau: 12 July 2006 (12.07.2006)

Information valid as of: Not available

Report generated on: 12 December 2019 (12.12.2019)

(10) Publication number: (43) Publication date: (26) Publication language:
WO 2007/00058204 January 2007 (04.01.2007) English (EN)

(21) Application number: (22) Filing date: (25) Filing language:
PCT/GB2006/00234427 June 2006 (27.06.2006) English (EN)

(31) Priority number(s): (32) Priority date(s): (33) Priority status:
0513176.8 (GB)28 June 2005 (28.06.2005) Priority document received (in compliance with PCT Rule 17.1)
0521278.2 (GB)19 October 2005 (19.10.2005) Priority document received (in compliance with PCT Rule 17.1)
0608846.2 (GB)04 May 2006 (04.05.2006) Priority document received (in compliance with PCT Rule 17.1)

(51) International Patent Classification:
C07D 413/12 (2006.01); C07D 417/12 (2006.01); C07D 403/12 (2006.01); A61K 31/506 (2006.01); A61P 5/02 (2006.01)

(71) Applicant(s):
TAKEDA CAMBRIDGE LIMITED [GB/GB]; 418 Cambridge Science Park Milton Road Cambridge CB4 0PA (GB) (for all designated states except US)
SHOWELL, Graham, Andrew [GB/GB]; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB) (for US only)
MILLER, David, John [GB/GB]; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB) (for US only)
GLEN, Angela [GB/GB]; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB) (for US only)
CUBILLO DE DIOS, Maria, Angeles [ES/GB]; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB) (for US only)
MERCHANT, Kevin [GB/GB]; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB) (for US only)
MANDAL, Ajay, Kumar [IN/GB]; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB) (for US only)

(72) Inventor(s):
SHOWELL, Graham, Andrew; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB)
MILLER, David, John; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB)
GLEN, Angela; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB)
CUBILLO DE DIOS, Maria, Angeles; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB)
MERCHANT, Kevin; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB)
MANDAL, Ajay, Kumar; Paradigm Therapeutics Ltd. 418 Cambridge Science Park Milton Road Cambridge CB4 0GP (GB)

(74) Agent(s):
GILL JENNINGS & EVERY LLP; Broadgate House 7 Eldon Street London EC2M 7LH (GB)

(54) Title (EN): HETEROCYCLIC NON-PEPTIDE GNRH ANTAGONISTS
(54) Title (FR): ANTAGONISTES NON-PEPTIDES HETEROCYCLIQUES DE GNRH

(57) Abstract:
(EN): A compound of formula (I): wherein either B is absent and A and Z are the same or different and are each hydrogen, halogen, alkyl, hydroxy, alkoxy, -CN, -C(Rc)2OH, -N(Rd)C(=X)Rc, -C(=X)N(Rc)(Rd), -S(O)m-Rc, -N(Rc)(Rd)S(O)2, -S(O)2N(Rc)(Rd), -N(Re)2, aryl optionally substituted with Ra or -O-aryl optionally substituted with Ra; or B is present and is -(CH2)n-, -C(Rb)2- or -O-, or B taken together with A or Z can be -C=C(Rb)-, -C(Rb)=C-, -CH2-CH(Rb)- or -CH(Rb)-CH2-; D is -O- or -S(O)m,-; E is a bond or is -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- or -N(Rd)(CH2)n-; F is -C(=X)-; G is -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- or -N(Rd)(CH2)n; J is a bond, -O-, -N(RC)C(=X)-, -C(=X)N(Rc)-, -S(O)m,-, -N(Rc)S(O)m-, -S(O)nN(Rc)-, -N(Re)- or -N(Rg)(Rh); K is a bond, alkylene, cycloalkylene, cycloalkenylene, arylene, heterocycloalkylene, heterocycloalkylene or heteroarylene; and L is hydrogen or a terminal group; has therapeutic utility.
(FR): Composé de formule (I) possédant une utilité thérapeutique. Dans ladite formule soit B est absent et A et Z sont identiques ou différents et représentent chacun hydrogène, halogène, alkyle, hydroxy, alcoxy, -CN, -C(Rc)2OH, -N(Rd)C(=X)Rc, -C(=X)N(Rc)(Rd), -S(O)m-Rc, -N(Rc)(Rd)S(O)2, -S(O)2N(Rc)(Rd), -N(Re)2, aryle éventuellement substitué par Ra ou -O-aryle éventuellement substitué par Ra; soit B est présent et représente -(CH2)n-, -C(Rb)2- ou -O-, soit B conjointement avec A ou Z peut être représenté par -C=C(Rb)-, -C(Rb)=C-, -CH2-CH(Rb)- ou-CH(Rb)-CH2-; D représente -O- ou -S(O)m,-; E représente une liaison ou -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- ou -N(Rd)(CH2)n-; F représente -C(=X)-; G représente -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- ou -N(Rd)(CH2)n; J représente une liaison, -O-, -N(RC)C(=X)-, -C(=X)N(Rc)-, -S(O)m,-, -N(Rc)S(O)m-, -S(O)nN(Rc)-, -N(Re)- ou -N(Rg)(Rh); K représente une liaison, alkylène, cycloalkylène, cycloalcénylène, arylène, hétérocycloalkylène, hétérocycloalkylène ou hétéroarylène; et L représente hydrogène ou un groupe terminal.

International search report:
Received at International Bureau: 31 October 2006 (31.10.2006) [EP]

International Report on Patentability (IPRP) Chapter II of the PCT:
Chapter II demand received: 02 February 2007 (02.02.2007)

(81) Designated States:
AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, 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, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, 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