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Extract from the Register of European Patents

EP About this file: EP2257529

EP2257529 - PYRIDINES AND PYRAZINES AS INHIBITORS OF PI3K [Right-click to bookmark this link]
StatusNo opposition filed within time limit
Status updated on  07.11.2014
Database last updated on 18.11.2024
Most recent event   Tooltip22.06.2018Lapse of the patent in a contracting state
New state(s): MK		published on 25.07.2018  [2018/30]
Applicant(s)For all designated states
Novartis AG
Lichtstrasse 35
4056 Basel / CH
[2010/49]
Inventor(s)01 / BRUCE, Ian
Novartis Horsham Research Centre
Wimblehurst Road
Horsham Sussex RH12 5AB / GB
02 / BUDD, Emma
Novartis Horsham Research Centre
Wimblehurst Road
Horsham Sussex RH12 5AB / GB
03 / EDWARDS, Lee
Novartis Horsham Research Centre
Wimblehurst Road
Horsham Sussex RH12 5AB / GB
04 / HOWSHAM, Catherine
Novartis Horsham Research Centre
Wimblehurst Road
Horsham Sussex RH12 5AB / GB
 [2014/01]
Former [2010/49]01 / BRUCE, Ian
Novartis Horsham Research Centre Wimblehurst Road
Horsham Sussex RH12 5AB / GB
02 / BUDD, Emma
Novartis Horsham Research Centre Wimblehurst Road
Horsham Sussex RH12 5AB / GB
03 / EDWARDS, Lee
Novartis Horsham Research Centre Wimblehurst Road
Horsham Sussex RH12 5AB / GB
04 / HOWSHAM, Catherine
Novartis Horsham Research Centre Wimblehurst Road
Horsham Sussex RH12 5AB / GB
Representative(s)von Sprecher, Georg
Novartis Pharma AG
Patent Department
4002 Basel / CH
[2014/01]
Former [2010/49]von Sprecher, Georg
Novartis Pharma AG Patent Department
4002 Basel / CH
Application number, filing date09723200.317.03.2009
[2010/49]
WO2009EP53136
Priority number, dateEP2008015304519.03.2008         Original published format: EP 08153045
[2010/49]
Filing languageEN
Procedural languageEN
PublicationType: A2 Application without search report
No.:WO2009115517
Date:24.09.2009
Language:EN
[2009/39]
Type: A2 Application without search report 
No.:EP2257529
Date:08.12.2010
Language:EN
The application published by WIPO in one of the EPO official languages on 24.09.2009 takes the place of the publication of the European patent application.
[2010/49]
Type: B1 Patent specification 
No.:EP2257529
Date:01.01.2014
Language:EN
[2014/01]
Search report(s)International search report - published on:EP07.01.2010
ClassificationIPC:C07D213/73, C07D241/20, C07D401/06, C07D401/14, A61K31/497, A61K31/4965, A61K31/4427, A61P37/06, A61P37/08
[2010/49]
CPC:
C07D401/06 (EP,US); A61P1/00 (EP); A61P1/04 (EP);
A61P11/00 (EP); A61P17/00 (EP); A61P17/06 (EP);
A61P19/00 (EP); A61P19/02 (EP); A61P29/00 (EP);
A61P3/04 (EP); A61P3/10 (EP); A61P31/04 (EP);
A61P35/00 (EP); A61P37/00 (EP); A61P37/06 (EP);
A61P37/08 (EP); A61P9/00 (EP); A61P9/08 (EP);
A61P9/10 (EP); C07D241/20 (EP,US); C07D401/04 (EP,US);
C07D401/12 (EP,US); C07D401/14 (EP,US); C07D405/14 (EP,US);
C07D413/14 (EP,US) (-)
Designated contracting statesAT,   BE,   BG,   CH,   CY,   CZ,   DE,   DK,   EE,   ES,   FI,   FR,   GB,   GR,   HR,   HU,   IE,   IS,   IT,   LI,   LT,   LU,   LV,   MC,   MK,   MT,   NL,   NO,   PL,   PT,   RO,   SE,   SI,   SK,   TR [2010/49]
Extension statesAL19.10.2010
BA19.10.2010
RS19.10.2010
TitleGerman:PYRIDINE UND PYRAZINE ALS PI3K-HEMMER[2010/49]
English:PYRIDINES AND PYRAZINES AS INHIBITORS OF PI3K[2010/49]
French:PYRIDINES ET PYRAZINES EN TANT QU'INHIBITEURS DE PI3K[2010/49]
Entry into regional phase19.10.2010National basic fee paid 
19.10.2010Designation fee(s) paid 
19.10.2010Examination fee paid 
Examination procedure19.10.2010Examination requested  [2010/49]
09.12.2010Amendment by applicant (claims and/or description)
09.03.2011Despatch of a communication from the examining division (Time limit: M06)
08.09.2011Reply to a communication from the examining division
11.06.2012Despatch of a communication from the examining division (Time limit: M04)
19.09.2012Reply to a communication from the examining division
08.02.2013Despatch of a communication from the examining division (Time limit: M04)
09.04.2013Reply to a communication from the examining division
22.07.2013Communication of intention to grant the patent
21.11.2013Fee for grant paid
21.11.2013Fee for publishing/printing paid
Divisional application(s)EP13153246.7  / EP2597085
The date of the Examining Division's first communication in respect of the earliest application for which a communication has been issued is  09.03.2011
Opposition(s)02.10.2014No opposition filed within time limit [2014/50]
Fees paidRenewal fee
15.03.2011Renewal fee patent year 03
14.03.2012Renewal fee patent year 04
11.03.2013Renewal fee patent year 05
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  TooltipHU17.03.2009
AT01.01.2014
BE01.01.2014
BG01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
MC01.01.2014
MK01.01.2014
MT01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
TR01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
NO01.04.2014
GR02.04.2014
IS01.05.2014
PT02.05.2014
[2018/30]
Former [2016/33]HU17.03.2009
AT01.01.2014
BE01.01.2014
BG01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
MC01.01.2014
MT01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
TR01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
NO01.04.2014
GR02.04.2014
IS01.05.2014
PT02.05.2014
Former [2016/32]HU17.03.2009
AT01.01.2014
BE01.01.2014
BG01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
MC01.01.2014
MT01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
NO01.04.2014
GR02.04.2014
IS01.05.2014
PT02.05.2014
Former [2016/28]AT01.01.2014
BE01.01.2014
BG01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
MC01.01.2014
MT01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
NO01.04.2014
GR02.04.2014
IS01.05.2014
PT02.05.2014
Former [2016/27]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
MC01.01.2014
MT01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
NO01.04.2014
IS01.05.2014
PT02.05.2014
Former [2016/23]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
MT01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
NO01.04.2014
IS01.05.2014
PT02.05.2014
Former [2016/12]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
MT01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
IS01.05.2014
PT02.05.2014
Former [2015/24]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SI01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
IS01.05.2014
PT02.05.2014
Former [2015/08]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
CH31.03.2014
LI31.03.2014
IS01.05.2014
PT02.05.2014
Former [2015/07]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SK01.01.2014
IE17.03.2014
LU17.03.2014
IS01.05.2014
PT02.05.2014
Former [2014/50]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
NL01.01.2014
PL01.01.2014
RO01.01.2014
SE01.01.2014
SK01.01.2014
LU17.03.2014
IS01.05.2014
PT02.05.2014
Former [2014/49]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
NL01.01.2014
RO01.01.2014
SE01.01.2014
LU17.03.2014
IS01.05.2014
PT02.05.2014
Former [2014/48]AT01.01.2014
BE01.01.2014
CY01.01.2014
CZ01.01.2014
DK01.01.2014
EE01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
NL01.01.2014
SE01.01.2014
LU17.03.2014
IS01.05.2014
PT02.05.2014
Former [2014/41]AT01.01.2014
BE01.01.2014
CY01.01.2014
FI01.01.2014
HR01.01.2014
LT01.01.2014
LV01.01.2014
NL01.01.2014
SE01.01.2014
IS01.05.2014
PT02.05.2014
Former [2014/39]AT01.01.2014
CY01.01.2014
FI01.01.2014
LT01.01.2014
NL01.01.2014
SE01.01.2014
IS01.05.2014
PT02.05.2014
Former [2014/37]AT01.01.2014
CY01.01.2014
FI01.01.2014
LT01.01.2014
SE01.01.2014
IS01.05.2014
PT02.05.2014
Former [2014/36]LT01.01.2014
IS01.05.2014
Cited inInternational search[X]DE2051013  (SANDOZ AG (BASEL)) [X] 1-7 * page 4; compound VI * * page 32; example 10a *;
 [X]GB2073185  (STERLING DRUG INC) [X] 1-4 * page 1; compound I * * page 10; compounds F11-F41 *;
 [X]WO9743267  (KING S COLLEGE LONDON [GB], et al) [X] 1-7 * page 5; compound II * * page 9; example 1 * * page 10; examples 2-7; table coupling *;
 [X]WO0146691  (BIOSIGNAL PACKARD INC [CA], et al) [X] 1-7 * page 41, line 19 *;
 [X]WO03093297  (EXELIXIS INC [US], et al) [X] 1-7,9-13 * page 239, paragraphs 882,883 *;
 [X]WO2004076412  (SUGEN INC [US], et al) [X] 1-4 * page 220; compounds II-93 *;
 [X]WO2004085409  (BIOFOCUS DISCOVERY LTD [GB], et al) [X] 1-4 * page 105; compound 15 *;
 [X]US2006030583  (ARNOLD WILLIAM D [US], et al) [X] 1-7 * page 108, method 44; ; page 107, paragraph 369; page 109, paragraph 376; table 29, relating to method 44 *;
 [X]WO2006021881  (PFIZER [US], et al) [X] 1-3 * claims 1,22-24 *;
 [X]WO2006021886  (PFIZER [US], et al) [X] 1-3,9-10 * claims 1,14,15 *;
 [X]WO2006051270  (ASTRAZENECA AB [SE], et al) [X] 1-4,9-13 * claims 1,19 * * pages 78-79 * * page 149, line 22; example 88 *;
 [X]WO2007095588  (NOVARTIS AG [CH], et al) [X] 1-2,9-13 * claims 20,49,61 * * table 1; compounds 145,184,261 * * page 149; table 1; compound 6 *;
 [A]WO2008012326  (NOVARTIS AG [CH], et al) [A] 1-13 * page 76; compounds 73-A *;
 [XP]WO2008038955  (CHONG KUN DANG PHARM CORP [KR], et al) [XP] 1-7,9-13 * claims 1,18,19 * * page 17; table 6; compounds 421,426 *;
 [XP]WO2008053157  (CHROMA THERAPEUTICS LTD [GB], et al) [XP] 1-4,9-13 * claims 1,18-21 * * page 53; table 2 *;
 [XP]WO2008094992  (VERTEX PHARMA [US], et al) [XP] 1-7,9-13 * claims 1,96,99,101 * * pages 118-121 *;
 [X]  - KEENAN, MARTINE ET AL, "Highly efficient and flexible total synthesis of coelenterazine", CHEMICAL COMMUNICATIONS (CAMBRIDGE) , (3), 323-324 CODEN: CHCOFS; ISSN: 1359-7345, (1997), XP000652586 [X] 1-7 * page 323; figure 1; compound 6 *

DOI:   http://dx.doi.org/10.1039/a607460j
 [X]  - JONES, KEITH ET AL, "A Suzuki coupling approach to pyrazines related to coelenterazine", SYNLETT , (6), 509-510 CODEN: SYNLES; ISSN: 0936-5214, (1996), XP002485380 [X] 1-7 * page 510; compounds 7A-F *

DOI:   http://dx.doi.org/10.1055/s-1996-5489
 [A]  - TERANISHI K ET AL, "SYNTHESIS AND CHEMILUMINESCENCE OF COELENTERAZINE (OPLOPHORUS LUCIFERIN) ANALOGUES", BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN, CHEMICAL SOCIETY OF JAPAN, TOKYO, JP, (19901101), vol. 63, no. 11, ISSN 0009-2673, pages 3132 - 3140, XP002037163 [A] 1-7 * page 3133; compound 47 *
 [X]  - SATO N, "STUDIES ON PYRAZINES. THE SYNTHESIS OF 2-HYDROXY-6-PHENYLPYRAZINE AND ITS DERIVATIVES", JOURNAL OF HETEROCYCLIC CHEMISTRY, HETEROCORPORATION. PROVO, (19780601), vol. 15, no. 4, ISSN 0022-152X, pages 665 - 670, XP002049109 [X] 1-4 * page 665; figure III; compound 12 *

DOI:   http://dx.doi.org/10.1002/jhet.5570150428
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DOI:   http://dx.doi.org/10.1055/s-1980-28915
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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.