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Extract from the Register of European Patents

EP About this file: EP2049541

EP2049541 - N-[5-({2-[(CYCLOPROPYLCARBONYL)AMINO]IMIDAZO[1,2-B]PYRIDAZIN-6-YL}OXY)-2-METHYLPHENYL]-1,3-DIMETHYL-1H-PYRAZOLE-5-CARBOXAMIDE AS VEGFR INHIBITOR [Right-click to bookmark this link]
Former [2009/17]FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF
[2014/15]
StatusNo opposition filed within time limit
Status updated on  29.07.2016
Database last updated on 20.12.2024
Most recent event   Tooltip17.08.2018Lapse of the patent in a contracting state
New state(s): BG		published on 19.09.2018  [2018/38]
Applicant(s)For all designated states
Takeda Pharmaceutical Company Limited
1-1, Doshomachi 4-chome Chuo-ku
Osaka- shi, Osaka 541-0045 / JP
[2009/17]
Inventor(s)01 / SAKAI, Nozomu
c/o TAKEDA PHARMACEUTICAL COMPANY LIMITED
17-85, Jusohonmachi 2-chome
Yodogawa-ku
Osaka-shi, Osaka 532-8686 / JP
02 / IMAMURA, Shinichi
535 Pierce St., Apt. 1308
Albany, CA 94706 / US
03 / MIYAMOTO, Naoki
c/o TAKEDA PHARMACEUTICAL COMPANY LIMITED
10, Wadai
Tsukuba-shi, Ibaraki 300-4293 / JP
04 / HIRAYAMA, Takaharu
c/o TAKEDA PHARMACEUTICAL COMPANY LIMITED
10, Wadai
Tsukuba-shi, Ibaraki 300-4293 / JP
 [2015/39]
Former [2009/17]01 / SAKAI, Nozomu
TAKEDA PHARMACEUTICAL COMPANY LIMITED 17-85, Jusohonmachi 2-chome Yodogawa-ku
Osaka-shi Osaka 532-8686 / JP
02 / IMAMURA, Shinichi
535 Pierce St., Apt. 1308
Albany, CA 94706 / US
03 / MIYAMOTO, Naoki
TAKEDA PHARMACEUTICAL COMPANY LIMITED 10, Wadai
Tsukuba-shi Ibaraki 300-4293 / JP
04 / HIRAYAMA, Takaharu
TAKEDA PHARMACEUTICAL COMPANY LIMITED 10, Wadai
Tsukuba-shi Ibaraki 300-4293 / JP
Representative(s)Jones, Nicholas Andrew, et al
Withers & Rogers LLP
2 London Bridge
London SE1 9RA / GB
[N/P]
Former [2015/39]Jones, Nicholas Andrew, et al
Withers & Rogers LLP
4 More London Riverside
London, SE1 2AU / GB
Former [2009/17]Jones, Nicholas Andrew, et al
Withers & Rogers LLP Goldings House 2 Hays Lane London
SE1 2HW / GB
Application number, filing date07792327.403.08.2007
[2009/17]
WO2007JP65681
Priority number, dateJP2006021398104.08.2006         Original published format: JP 2006213981
JP2006033123007.12.2006         Original published format: JP 2006331230
JP2007014407230.05.2007         Original published format: JP 2007144072
[2009/17]
Filing languageEN
Procedural languageEN
PublicationType: A2 Application without search report
No.:WO2008016192
Date:07.02.2008
Language:EN
[2008/06]
Type: A2 Application without search report 
No.:EP2049541
Date:22.04.2009
Language:EN
The application published by WIPO in one of the EPO official languages on 07.02.2008 takes the place of the publication of the European patent application.
[2009/17]
Type: B1 Patent specification 
No.:EP2049541
Date:23.09.2015
Language:EN
[2015/39]
Search report(s)International search report - published on:EP08.05.2008
ClassificationIPC:C07D487/04
[2009/17]
CPC:
C07D487/04 (EP,KR,US); A61K31/5025 (KR); A61P11/06 (EP);
A61P13/12 (EP); A61P15/08 (EP); A61P17/06 (EP);
A61P19/02 (EP); A61P27/02 (EP); A61P29/00 (EP);
A61P35/00 (EP); A61P35/04 (EP); A61P43/00 (EP);
A61P9/00 (EP); A61P9/10 (EP); A61P9/12 (EP) (-)
Designated contracting statesAT,   BE,   BG,   CH,   CY,   CZ,   DE,   DK,   EE,   ES,   FI,   FR,   GB,   GR,   HU,   IE,   IS,   IT,   LI,   LT,   LU,   LV,   MC,   MT,   NL,   PL,   PT,   RO,   SE,   SI,   SK,   TR [2015/39]
Former [2009/17]AT,  BE,  BG,  CH,  CY,  CZ,  DE,  DK,  EE,  ES,  FI,  FR,  GB,  GR,  HU,  IE,  IS,  IT,  LI,  LT,  LU,  LV,  MC,  MT,  NL,  PL,  PT,  RO,  SE,  SI,  SK,  TR 
Extension statesAL30.01.2009
BA30.01.2009
HR30.01.2009
MK30.01.2009
RS30.01.2009
TitleGerman:N-[5-({2-[(CYCLOPROPYLCARBONYL)AMINO]IMIDAZO[1,2-B]PYRIDAZIN-6-YL}OXY)-2-METHYLPHENYL]-1,3-DIMETHYL-1H-PYRAZOL-5-CARBOXAMID ALS VEGFR HEMMSTOFFE[2015/19]
English:N-[5-({2-[(CYCLOPROPYLCARBONYL)AMINO]IMIDAZO[1,2-B]PYRIDAZIN-6-YL}OXY)-2-METHYLPHENYL]-1,3-DIMETHYL-1H-PYRAZOLE-5-CARBOXAMIDE AS VEGFR INHIBITOR[2015/19]
French:N-[5-({2-[(CYCLOPROPYLCARBONYL)AMINO]IMIDAZO[1,2-B]PYRIDAZIN-6-YL}OXY)-2-METHYLPHENYL]-1,3-DIMETHYL-1H-PYRAZOLE-5-CARBOXAMIDE EN TANT QU'INHIBITEURS DE VEGFR[2015/19]
Former [2009/17]KONDENSIERTES HETEROZYKLISCHES DERIVAT UND ANWENDUNG DAVON
Former [2009/17]FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF
Former [2009/17]DÉRIVÉ HÉTÉROCYCLIQUE FUSIONNÉ ET SON PROCÉDÉ D'UTILISATION
Entry into regional phase30.01.2009National basic fee paid 
30.01.2009Designation fee(s) paid 
30.01.2009Examination fee paid 
Examination procedure30.01.2009Amendment by applicant (claims and/or description)
30.01.2009Examination requested  [2009/17]
19.04.2012Despatch of a communication from the examining division (Time limit: M04)
02.08.2012Reply to a communication from the examining division
17.06.2013Despatch of a communication from the examining division (Time limit: M04)
23.10.2013Reply to a communication from the examining division
21.05.2014Communication of intention to grant the patent
16.09.2014Disapproval of the communication of intention to grant the patent by the applicant or resumption of examination proceedings by the EPO
03.11.2014Communication of intention to grant the patent
04.02.2015Disapproval of the communication of intention to grant the patent by the applicant or resumption of examination proceedings by the EPO
08.04.2015Communication of intention to grant the patent
05.08.2015Fee for grant paid
05.08.2015Fee for publishing/printing paid
05.08.2015Receipt of the translation of the claim(s)
Divisional application(s)The date of the Examining Division's first communication in respect of the earliest application for which a communication has been issued is  19.04.2012
Opposition(s)24.06.2016No opposition filed within time limit [2016/35]
Fees paidRenewal fee
25.08.2009Renewal fee patent year 03
19.08.2010Renewal fee patent year 04
24.08.2011Renewal fee patent year 05
23.08.2012Renewal fee patent year 06
08.08.2013Renewal fee patent year 07
08.08.2014Renewal fee patent year 08
12.08.2015Renewal fee patent year 09
Opt-out from the exclusive  Tooltip
competence of the Unified
Patent Court		 See the Register of the Unified Patent Court for opt-out data
Responsibility for the accuracy, completeness or quality of the data displayed under the link provided lies entirely with the Unified Patent Court.
Lapses during opposition  TooltipHU03.08.2007
AT23.09.2015
BE23.09.2015
BG23.09.2015
CY23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
MC23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SI23.09.2015
SK23.09.2015
TR23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
[2018/38]
Former [2018/33]HU03.08.2007
AT23.09.2015
BE23.09.2015
CY23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
MC23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SI23.09.2015
SK23.09.2015
TR23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2018/29]HU03.08.2007
AT23.09.2015
BE23.09.2015
CY23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
MC23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SI23.09.2015
SK23.09.2015
TR23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2018/28]HU03.08.2007
AT23.09.2015
BE23.09.2015
CY23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
MC23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SI23.09.2015
SK23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2017/23]AT23.09.2015
BE23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
MC23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SI23.09.2015
SK23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2017/03]AT23.09.2015
BE23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SI23.09.2015
SK23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2016/49]AT23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SI23.09.2015
SK23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2016/39]AT23.09.2015
CZ23.09.2015
DK23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SK23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2016/24]AT23.09.2015
CZ23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
PL23.09.2015
RO23.09.2015
SE23.09.2015
SK23.09.2015
GR24.12.2015
IS23.01.2016
PT25.01.2016
Former [2016/23]CZ23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
RO23.09.2015
SE23.09.2015
SK23.09.2015
GR24.12.2015
IS23.01.2016
Former [2016/22]CZ23.09.2015
EE23.09.2015
ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
SE23.09.2015
GR24.12.2015
IS23.01.2016
Former [2016/21]ES23.09.2015
FI23.09.2015
IT23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
SE23.09.2015
GR24.12.2015
Former [2016/20]ES23.09.2015
FI23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
SE23.09.2015
GR24.12.2015
Former [2016/14]FI23.09.2015
LT23.09.2015
LV23.09.2015
NL23.09.2015
SE23.09.2015
GR24.12.2015
Former [2016/10]FI23.09.2015
LT23.09.2015
LV23.09.2015
SE23.09.2015
GR24.12.2015
Former [2016/09]FI23.09.2015
LT23.09.2015
LV23.09.2015
GR24.12.2015
Former [2016/07]LT23.09.2015
Cited inInternational search[PX]WO2007013673  (ASTELLAS PHARMA INC [JP], et al) [PX] 1-25 * table 4 *;
 [PX]WO2007025090  (KALYPSYS INC [US], et al) [PX] 1-25 * the whole document *;
 [PX]WO2007025540  (SCHERING AG [DE], et al) [PX] 1-25 * the whole document *;
 [PX]WO2007038314  (BRISTOL MYERS SQUIBB CO [US], et al) [PX] 1-25 * table 1 *;
 [A]  - BULLOCK A N ET AL, "Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in Moloney Murine Leukemia Virus (PIM-1) Kinase", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, (20051027), vol. 48, no. 24, ISSN 0022-2623, pages 7604 - 7614, XP002405453 [A] 1-25 * figure 2 *

DOI:   http://dx.doi.org/10.1021/jm0504858
 [A]  - MOURAD AE ET AL, "synthesis of imidazo[1,2-b]pyridazines: fenbendazole, oxifenbendazole analogs and related derivatives", JOURNAL OF HETEROCYCLIC CHEMISTRY, HETEROCORPORATION. PROVO, US, (199310), vol. 30, ISSN 0022-152X, pages 1365 - 1372, XP002331979 [A] 1 * Examples *

DOI:   http://dx.doi.org/10.1002/jhet.5570300531
 [A]  - BARLIN G B ET AL, "Imidazo (1,2-b)pyridazines. II- 6-Alkylthio- and 6-Arylthio-3-methoxy-2-phenylimidazo(1,2-b)pyridazines", AUSTRALIAN JOURNAL OF CHEMISTRY, XX, XX, (1987), vol. 40, ISSN 0004-9425, pages 1491 - 1497, XP009095679 [A] 1 * pages 1496-97 *

DOI:   http://dx.doi.org/10.1071/CH9871491
 [A]  - BARLIN G B ET AL, "Imidazo(1,2-b)pyridazines. IV. Synthesis and Central Nervous System Activities of Some 3-Methoxy-6-phenoxy(substituted phenoxy and naphthyloxy)-2-phenylimidazo(1,2-b)pyridazines", AUSTRALIAN JOURNAL OF CHEMISTRY, XX, XX, (1988), vol. 41, ISSN 0004-9425, pages 1735 - 1742, XP009095689 [A] 1 * page 1739 *
 [A]  - TREBSE, P. ET AL., "A direct conversion of 5,6,7,8-Tetrahydro-2H-1-BenzoPyran-2,5-diones into substituted 1-Amino-5,6,7,8-Tetrahydroquinoline-2,5-diones", HETEROCYCLES, (2003), vol. 59, no. 1, pages 129 - 136, XP001537844 [A] 1 * Scheme 1 *
by applicant   - JERRY MARCH, Advanced Organic Chemistry, 4th Ed., UNKNOWN
    - RICHARD C. LAROCK, Comprehensive Organic Transformations, 2nd Ed., UNKNOWN
    - "Design of Molecules", IYAKUHIN no KAIHATSU, HIROKAWA SHOTEN, (1990), vol. 7, pages 163 - 198
The EPO accepts no responsibility for the accuracy of data originating from other authorities; in particular, it does not guarantee that it is complete, up to date or fit for specific purposes.