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Extract from the Register of European Patents

EP About this file: EP2848617

EP2848617 - DIARYL[A, G]QUINOLIZIDINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USES THEREOF [Right-click to bookmark this link]
StatusNo opposition filed within time limit
Status updated on  18.11.2022
Database last updated on 12.07.2024
FormerThe patent has been granted
Status updated on  10.12.2021
FormerGrant of patent is intended
Status updated on  28.07.2021
FormerExamination is in progress
Status updated on  03.07.2021
FormerGrant of patent is intended
Status updated on  09.06.2021
FormerExamination is in progress
Status updated on  10.01.2017
Most recent event   Tooltip27.04.2024Lapse of the patent in a contracting state
New state(s): MK		published on 29.05.2024  [2024/22]
Applicant(s)For all designated states
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
555 Zuchongzhi Road
Zhangjiang, Pudong
Shanghai 201203 / CN
[2015/12]
Inventor(s)01 / LIU, Hong
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
02 / ZHEN, Xuechu
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
03 / SUN, Haifeng
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
04 / ZHU, Liyuan
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
05 / QIAN, Wangke
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
06 / YU, Leiping
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
07 / LI, Zeng
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
08 / ZHOU, Shengbin
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
09 / CAI, Wenxian
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
10 / JIANG, Hualiang
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
11 / CHEN, Kaixian
555 Zuchongzhi Road
Zhangjiang
Pudong
Shanghai 201203 / CN
 [2015/12]
Representative(s)Kador & Partner Part mbB
Corneliusstraße 15
80469 München / DE
[N/P]
Former [2022/02]Kador & Partner PartG mbB
Corneliusstraße 15
80469 München / DE
Former [2015/12]Kador & Partner
Corneliusstraße 15
80469 München / DE
Application number, filing date13787305.509.05.2013
[2022/02]
WO2013CN00549
Priority number, dateCN20121014290309.05.2012         Original published format: CN201210142903
[2015/12]
Filing languageZH
Procedural languageEN
PublicationType: A1 Application with search report
No.:WO2013166862
Date:14.11.2013
Language:ZH
[2013/46]
Type: A1 Application with search report 
No.:EP2848617
Date:18.03.2015
Language:EN
[2015/12]
Type: B1 Patent specification 
No.:EP2848617
Date:12.01.2022
Language:EN
[2022/02]
Search report(s)International search report - published on:CN14.11.2013
(Supplementary) European search report - dispatched on:EP22.01.2015
ClassificationIPC:C07D455/03, A61K31/4375, A61P25/00, A61P25/18
[2015/12]
CPC:
C07D471/14 (EP,US); A61P25/00 (EP); A61P25/06 (EP);
A61P25/16 (EP); A61P25/18 (EP); A61P25/20 (EP);
A61P25/24 (EP); A61P25/30 (EP); A61P25/36 (EP);
A61P43/00 (EP); C07D455/03 (EP,US); C07D491/147 (EP,US);
C07D491/22 (EP,US); C07D495/14 (EP,US); C07D495/22 (EP,US) (-)
Designated contracting statesAL,   AT,   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,   RS,   SE,   SI,   SK,   SM,   TR [2015/12]
Extension statesBANot yet paid
MENot yet paid
TitleGerman:DIARYL[A,G-]CHINOLIZIDINVERBINDUNG, HERSTELLUNGSVERFAHREN DAFÜR, PHARMAZEUTISCHE ZUSAMMENSETZUNG UND VERWENDUNGEN DAVON[2015/12]
English:DIARYL[A, G]QUINOLIZIDINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USES THEREOF[2015/12]
French:COMPOSÉ DIARYL[A, G]QUINOLIZIDINE, SON PROCÉDÉ DE PRÉPARATION, COMPOSITION PHARMACEUTIQUE, ET LEURS UTILISATIONS[2015/12]
Entry into regional phase08.12.2014Translation filed 
08.12.2014National basic fee paid 
08.12.2014Search fee paid 
08.12.2014Designation fee(s) paid 
08.12.2014Examination fee paid 
Examination procedure08.12.2014Examination requested  [2015/12]
05.08.2015Amendment by applicant (claims and/or description)
10.12.2015Despatch of a communication from the examining division (Time limit: M06)
04.05.2016Reply to a communication from the examining division
08.09.2016Despatch of a communication from the examining division (Time limit: M04)
09.01.2017Reply to a communication from the examining division
18.05.2017Despatch of a communication from the examining division (Time limit: M06)
27.11.2017Reply to a communication from the examining division
11.07.2018Despatch of a communication from the examining division (Time limit: M04)
08.11.2018Reply to a communication from the examining division
27.01.2020Despatch of a communication from the examining division (Time limit: M04)
20.05.2020Reply to a communication from the examining division
30.07.2020Despatch of a communication from the examining division (Time limit: M04)
09.12.2020Reply to a communication from the examining division
09.06.2021Communication of intention to grant the patent
01.07.2021Disapproval of the communication of intention to grant the patent by the applicant or resumption of examination proceedings by the EPO
29.07.2021Communication of intention to grant the patent
02.12.2021Fee for grant paid
02.12.2021Fee for publishing/printing paid
02.12.2021Receipt 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  10.12.2015
Opposition(s)13.10.2022No opposition filed within time limit [2022/51]
Fees paidRenewal fee
27.05.2015Renewal fee patent year 03
31.03.2016Renewal fee patent year 04
24.05.2017Renewal fee patent year 05
22.05.2018Renewal fee patent year 06
23.05.2019Renewal fee patent year 07
29.05.2020Renewal fee patent year 08
21.05.2021Renewal fee patent year 09
Opt-out from the exclusive  Tooltip
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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  TooltipHU09.05.2013
AL12.01.2022
AT12.01.2022
CY12.01.2022
CZ12.01.2022
DK12.01.2022
EE12.01.2022
FI12.01.2022
HR12.01.2022
LT12.01.2022
LV12.01.2022
MC12.01.2022
MK12.01.2022
PL12.01.2022
RO12.01.2022
RS12.01.2022
SK12.01.2022
SM12.01.2022
BG12.04.2022
NO12.04.2022
GR13.04.2022
IE09.05.2022
LU09.05.2022
IS12.05.2022
PT12.05.2022
[2024/22]
Former [2024/20]HU09.05.2013
AL12.01.2022
AT12.01.2022
CY12.01.2022
CZ12.01.2022
DK12.01.2022
EE12.01.2022
FI12.01.2022
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LT12.01.2022
LV12.01.2022
MC12.01.2022
PL12.01.2022
RO12.01.2022
RS12.01.2022
SK12.01.2022
SM12.01.2022
BG12.04.2022
NO12.04.2022
GR13.04.2022
IE09.05.2022
LU09.05.2022
IS12.05.2022
PT12.05.2022
Former [2024/18]HU09.05.2013
AL12.01.2022
AT12.01.2022
CZ12.01.2022
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BG12.04.2022
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GR13.04.2022
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Documents cited:Search[X]JPS5024299  (NIPPON CHEMIPHAR CO) [X] 1-4,7 * the whole document *;
 [X]WO2010075469  (CVI PHARMACEUTICALS LTD [GB], et al) [X] 1-4 * page 161 - page 174; examples 11, 19, 30, 33-34, 39, 62, 72, 74 *;
 [X]  - JB BREMNER ET AL, "Synthesis of Some Thieno Analogs of the Protoberberine and Protopine Skeletons. X-Ray Crystal Structure of 9,10-Dimethoxy-5-methyl-4,5,6,7,12,13-hexahydrothieno[3,2-e][3]benzazeci n-12-one", AUSTRALIAN JOURNAL OF CHEMISTRY: AN INTERNATIONAL JOURNAL FOR CHEMICAL SCIENCE, C S I R O PUBLISHING, AU, (19880101), vol. 41, no. 1, doi:10.1071/CH9880111, ISSN 0004-9425, pages 111 - 126, XP009179859 [X] 1-4,7 * page 112 - page 113; compounds 5, 11 *

DOI:   http://dx.doi.org/10.1071/CH9880111
 [X]  - K T Potts ET AL, "Synthesis of y-Carbolines", Chemical Communications, (19660101), pages 857 - 858, URL: http://pubs.rsc.org/en/content/articlepdf/1966/c1/c19660000857, (20150107), XP055160215 [X] 1-4,7 * 2,3-benzo; page 858; compound III *
 [X]  - KNOLKER H-J ET AL, "Transition metal complexes in organic synthesis. Part 62:<1> Total synthesis of (+/-)-demethoxycarbonyldihydrogambirtannine and norketoyobyrine by an iron-mediated [2+2+1] cycloaddition", TETRAHEDRON LETTERS, PERGAMON, GB, (20000624), vol. 41, no. 26, doi:10.1016/S0040-4039(00)00766-8, ISSN 0040-4039, pages 5035 - 5038, XP004222004 [X] 1-4,7 * page 5035; compounds 1a, 1b *

DOI:   http://dx.doi.org/10.1016/S0040-4039(00)00766-8
 [X]  - DIKER K ET AL, "Trapping of Iminiums by the Indole Nucleus during Catalytic Hydrogenation of Nitriles: a Rapid Synthesis of Tetrahydro-beta-carbolines", TETRAHEDRON LETTERS, PERGAMON, GB, (19950403), vol. 36, no. 14, doi:10.1016/0040-4039(95)00293-L, ISSN 0040-4039, pages 2497 - 2500, XP004028321 [X] 1-4,7 * page 2498 - page 2499; compounds 6-7, 13 *

DOI:   http://dx.doi.org/10.1016/0040-4039(95)00293-L
 [X]  - JAMES SHORT ET AL, "Notes- New Synthesis of 18-Hydroxy-17-methoxy-15,16,17,18,19,20-hexadehydroyohimbane Hydrochloride.", THE JOURNAL OF ORGANIC CHEMISTRY, (19610701), vol. 26, no. 7, doi:10.1021/jo01351a621, ISSN 0022-3263, pages 2560 - 2561, XP055160238 [X] 1-4,7 * page 2560; compound IVb *

DOI:   http://dx.doi.org/10.1021/jo01351a621
 [X]  - OLIVER KOEPLER ET AL, "Synthesis and DNA binding properties of novel benzo[b]isoquino[2,3-h]-naphthyridines", ORGANIC & BIOMOLECULAR CHEMISTRY, (20050101), vol. 3, no. 15, doi:10.1039/b503281d, ISSN 1477-0520, page 2848, XP055160243 [X] 1-3,7 * page 2850; compound 17 *

DOI:   http://dx.doi.org/10.1039/b503281d
 [X]  - Uttam Kumar Panit ET AL, "SYNTHETIC ENTRY INTO YOHIMBINOID ALKALOIDS AND NOVEL SYNTHESIS OF ( )-17-METHOXY-HEXAHYDROYOHIMBANE", Tetrahedron, (19870101), pages 4235 - 4239, URL: http://ac.els-cdn.com/S0040402001834669/1-s2.0-S0040402001834669-main.pdf?_tid=f7beea74-9668-11e4-bc6c-00000aab0f6c&acdnat=1420634010_ea59f437d911fdd1f56e2f99dbeb3d77, (20150107), XP055160272 [X] 1-4 * page 4236; compound 11 *
 [X]  - K. WEISE ET AL, "Aufbau eines Yohimban-ähnlichen heterocyclus Zweistufensynthese von Benzofuro-benzo-chinolizidin", TETRAHEDRON LETTERS, (19710101), vol. 12, no. 17, doi:10.1016/S0040-4039(01)96673-0, ISSN 0040-4039, pages 1231 - 1232, XP055160274 [X] 1-4,7 * page 1232; compound V *

DOI:   http://dx.doi.org/10.1016/S0040-4039(01)96673-0
 [X]  - ROBIN D. CLARK ET AL, "Stereospecific synthesis of the (3a[alpha],11[alpha],12a[alpha])-decahydrobenzo[ a ]pyrrolo[3,2- g ]quinolizine ring system", JOURNAL OF HETEROCYCLIC CHEMISTRY, (19930501), vol. 30, no. 3, doi:10.1002/jhet.5570300338, ISSN 0022-152X, pages 829 - 831, XP055160279 [X] 1-4,7 * page 829; compound 7 *

DOI:   http://dx.doi.org/10.1002/jhet.5570300338
 [X]  - GLENN C. MORRISON ET AL, "1,4,4a,5,6,8,9,14,14a,14b-1)ecahydrobenz[[alpha]]in(iolo[2,3-g]quinolizinones. A system isomeric with yohimbane", JOURNAL OF HETEROCYCLIC CHEMISTRY, (19711201), vol. 8, no. 6, doi:10.1002/jhet.5570080625, ISSN 0022-152X, pages 1025 - 1026, XP055160284 [X] 1-4,7 * page 1025; compound 2 *

DOI:   http://dx.doi.org/10.1002/jhet.5570080625
 [X]  - S Jeganathan ET AL, "Studies on Heterocyclic Compounds; I. Synthesis of Thiophene Derivatives of Protoberberine Alkaloids", Synthesis, (19790301), pages 195 - 196, URL: https://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-1979-28614.pdf, (20150107), XP055160290 [X] 1-4,7 * page 195; compound 6a *

DOI:   http://dx.doi.org/10.1055/s-1979-28614
 [X]  - GEORGE R. LENZ, "The synthesis of 8-oxoberbines containing a heterocyclic D-ring by enamide photocyclizations", JOURNAL OF HETEROCYCLIC CHEMISTRY, (19790401), vol. 16, no. 3, doi:10.1002/jhet.5570160304, ISSN 0022-152X, pages 433 - 437, XP055160294 [X] 1-4,7 * page 433 - page 434; compounds 4, 7 *

DOI:   http://dx.doi.org/10.1002/jhet.5570160304
 [X]  - V. BOEKELHEIDE ET AL, "The Synthesis of 1,2-Benzo-7,8-(2',3'-indolo)-tetrahydroquinolizine 1", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, (19521001), vol. 74, no. 19, doi:10.1021/ja01139a054, ISSN 0002-7863, pages 4920 - 4923, XP055160298 [X] 1-4,7 * page 4920; compound II *

DOI:   http://dx.doi.org/10.1021/ja01139a054
 [X]  - Chihiro Ito, "Chemopreventive Activity of Isoquinoline Alkaloids from Corydalis Plants", Planta Medica, (20010101), pages 473 - 475, URL: https://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-2001-15815.pdf, (20150107), XP055160350 [X] 1-4,7 * page 473; figure 1; compounds 3-5 *

DOI:   http://dx.doi.org/10.1055/s-2001-15815
 [X]  - Y-.R. Wu, "Two New Quaternary Alkaloids and Anti-Hepatitis B Virus Active Constituents from Corydalis saxicola", Planta Medica, doi:10.1055/s-2007-98154, (20070101), pages 787 - 791, URL: https://www.thieme-connect.de/products/ejournals/pdf/10.1055/s-2007-981549.pdf, (20150107), XP055160353 [X] 1-4,7 * page 788; compound 5 *

DOI:   http://dx.doi.org/10.1055/s-2007-981549
 [X]  - Thomas Nógrádi, "Untersuchungen über Rauwolfia-Alkaloid-Modelle II 2-Substituierte Indole, Tetrahydrocarbolin- und Hexadehydro-yohimban-Derivate", Monatshefte für Chemie, (19570101), pages 1087 - 1094, URL: http://download.springer.com/static/pdf/356/art%3A10.1007%2FBF00906089.pdf?auth66=1420711766_81fc88890625b641de8221ea9d379426&ext=.pdf, (20150108), XP055160529 [X] 1-4,7 * page 1089; compound XIII *
 [X]  - SCHAPER K-J, "Free-wilson-type analysis of non-additive substituent effects on THPB", QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIPS, VCH PUBLISHERS, DEERFIELD BEACH, FL, US, (19990101), vol. 18, no. 4, ISSN 0931-8771, pages 354 - 360, XP008123720 [X] 1-4,7 * page 356; compound 9 *
 [X]  - JEGANATHAN ET AL, "STUDIES ON HETEROCYCLIC COMPOUNDS VI: Synthesis of Thiophene Isosters of Protoberberine Alkaloids", PHOSPHORUS AND SULFUR AND THE RELATED ELEMENTS, GORDON AND BREACH - HARWOOD ACADEMIC, CH, (19810301), vol. 11, doi:0.1080/03086648108077411, ISSN 0308-664X, pages 125 - 137, XP009181842 [X] 1-4,7 * page 127; compounds 12-13 * * page 129 - page 130; compounds 19, 25 *

DOI:   http://dx.doi.org/0.1080/03086648108077411
International search[X]EP0524004  (SYNTEX INC [US]);
 [X]WO2008014661  (SHANGHAI INST MATERIA MEDICA [CN], et al);
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