blank Quick help
blank Maintenance news

Scheduled maintenance

Regular maintenance outages:
between 05.00 and 05.15 hrs CET (Monday to Sunday).

Other outages
Availability

2022.02.11

More...
blank News flashes

News Flashes

New version of the European Patent Register – SPC proceedings information in the Unitary Patent Register.

2024-07-24

More...
blank Related links

Extract from the Register of European Patents

EP About this file: EP2147014

EP2147014 - 17ALPHA-SUBSTITUTED STEROIDS AS SYSTEMIC ANTIANDROGENS AND SELECTIVE ANDROGEN RECEPTOR MODULATORS [Right-click to bookmark this link]
StatusNo opposition filed within time limit
Status updated on  23.12.2016
Database last updated on 18.01.2025
Most recent event   Tooltip20.07.2018Lapse of the patent in a contracting state
New state(s): IS, MT
published on 22.08.2018  [2018/34]
Applicant(s)For all designated states
Endorecherche, Inc.
2989 de la Promenade
Sainte-Foy, Quebec G1W 2J5 / CA
[2010/04]
Inventor(s)01 / LABRIE, Fernand
2989, de la Promenade
Québec City, Québec G1W 2J5 / CA
02 / GAUTHIER, Sylvain
152 Rue de la Modiste
St.-augustin-de-Desmaures, Québec G3A 2L2 / CA
03 / CLOUTIER, Julie
1393 Rue des Tourmalines
Lévis, Québec G6W 7P2 / CA
04 / MAILHOT, Josée
2575 Lalonde
Québec, Québec G1W 1M8 / CA
05 / POTVIN, Steeves
9580 Avenue Nantel
Québec, Québec G2B 5A2 / CA
06 / DION, Sylvain
236 Rue de la Rivière
St-Romuald, Québec G6W 7J1 / CA
07 / SANCÉAU, Jean-Yves
3775 Avenue Des Compagnons, App. 446
Québec, Québec G1X 5C3 / CA
 [2010/04]
Representative(s)Carpintero Lopez, Francisco, et al
Herrero & Asociados, S.L.
Agustín de Foxá, 4-10
28036 Madrid / ES
[N/P]
Former [2010/04]Carpintero Lopez, Francisco, et al
Herrero & Asociados, S.L. Alcalá 35
28014 Madrid / ES
Application number, filing date08748116.411.04.2008
[2010/04]
WO2008CA00672
Priority number, dateUS20070911452P12.04.2007         Original published format: US 911452 P
US20070911434P12.04.2007         Original published format: US 911434 P
US2008010037209.04.2008         Original published format: US 100372
[2010/04]
Filing languageEN
Procedural languageEN
PublicationType: A1 Application with search report
No.:WO2008124922
Date:23.10.2008
Language:EN
[2008/43]
Type: A1 Application with search report 
No.:EP2147014
Date:27.01.2010
Language:EN
The application published by WIPO in one of the EPO official languages on 23.10.2008 takes the place of the publication of the European patent application.
[2010/04]
Type: B1 Patent specification 
No.:EP2147014
Date:17.02.2016
Language:EN
[2016/07]
Search report(s)International search report - published on:CA23.10.2008
(Supplementary) European search report - dispatched on:EP05.10.2012
ClassificationIPC:C07J43/00, A61K31/565, A61K31/567, A61K31/58, A61P5/28, C07J41/00, C07J63/00
[2010/04]
CPC:
C07J41/0094 (EP,US); A61P35/00 (EP); A61P5/28 (EP);
C07J43/003 (EP,US); C07J63/008 (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,   MT,   NL,   NO,   PL,   PT,   RO,   SE,   SI,   SK,   TR [2016/07]
Former [2010/04]AT,  BE,  BG,  CH,  CY,  CZ,  DE,  DK,  EE,  ES,  FI,  FR,  GB,  GR,  HR,  HU,  IE,  IS,  IT,  LI,  LT,  LU,  LV,  MC,  MT,  NL,  NO,  PL,  PT,  RO,  SE,  SI,  SK,  TR 
TitleGerman:17ALPHA-SUBSTITUIERTE STEROIDE ALS SYSTEMISCHE ANTIANDROGENE UND SELEKTIVE ANDROGENREZEPTORMODULATOREN[2010/04]
English:17ALPHA-SUBSTITUTED STEROIDS AS SYSTEMIC ANTIANDROGENS AND SELECTIVE ANDROGEN RECEPTOR MODULATORS[2010/04]
French:STÉROÏDES 17-ALPHA-SUBSTITUÉS UTILISÉS COMME ANTI-ANDROGÈNES SYSTÉMIQUES ET MODULATEURS SÉLECTIFS DU RÉCEPTEUR DE L'ANDROGÈNE[2010/04]
Entry into regional phase11.11.2009National basic fee paid 
11.11.2009Search fee paid 
11.11.2009Designation fee(s) paid 
11.11.2009Examination fee paid 
Examination procedure11.11.2009Examination requested  [2010/04]
29.04.2013Amendment by applicant (claims and/or description)
15.10.2013Despatch of a communication from the examining division (Time limit: M06)
10.04.2014Reply to a communication from the examining division
07.09.2015Cancellation of oral proceeding that was planned for 11.09.2015
11.09.2015Date of oral proceedings (cancelled)
08.10.2015Communication of intention to grant the patent
03.12.2015Fee for grant paid
03.12.2015Fee for publishing/printing paid
03.12.2015Receipt 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  15.10.2013
Opposition(s)18.11.2016No opposition filed within time limit [2017/04]
Fees paidRenewal fee
26.04.2010Renewal fee patent year 03
25.04.2011Renewal fee patent year 04
25.04.2012Renewal fee patent year 05
29.04.2013Renewal fee patent year 06
28.04.2014Renewal fee patent year 07
27.04.2015Renewal fee patent year 08
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  TooltipAT17.02.2016
BE17.02.2016
CY17.02.2016
CZ17.02.2016
EE17.02.2016
ES17.02.2016
HR17.02.2016
IS17.02.2016
LT17.02.2016
LV17.02.2016
MC17.02.2016
PL17.02.2016
RO17.02.2016
SI17.02.2016
SK17.02.2016
TR17.02.2016
LU11.04.2016
MT30.04.2016
BG17.05.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
[2018/32]
Former [2018/29]AT17.02.2016
BE17.02.2016
CY17.02.2016
CZ17.02.2016
EE17.02.2016
ES17.02.2016
HR17.02.2016
LT17.02.2016
LV17.02.2016
MC17.02.2016
PL17.02.2016
RO17.02.2016
SI17.02.2016
SK17.02.2016
TR17.02.2016
LU11.04.2016
BG17.05.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2017/15]AT17.02.2016
BE17.02.2016
CZ17.02.2016
EE17.02.2016
ES17.02.2016
LT17.02.2016
LV17.02.2016
PL17.02.2016
RO17.02.2016
SI17.02.2016
SK17.02.2016
LU11.04.2016
BG17.05.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2017/04]AT17.02.2016
BE17.02.2016
CZ17.02.2016
EE17.02.2016
ES17.02.2016
LT17.02.2016
LV17.02.2016
PL17.02.2016
RO17.02.2016
SK17.02.2016
LU11.04.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2017/03]AT17.02.2016
BE17.02.2016
CZ17.02.2016
EE17.02.2016
ES17.02.2016
LT17.02.2016
LV17.02.2016
PL17.02.2016
RO17.02.2016
SK17.02.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2016/50]AT17.02.2016
CZ17.02.2016
EE17.02.2016
ES17.02.2016
LT17.02.2016
LV17.02.2016
PL17.02.2016
RO17.02.2016
SK17.02.2016
BE30.04.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2016/49]AT17.02.2016
EE17.02.2016
ES17.02.2016
LT17.02.2016
LV17.02.2016
PL17.02.2016
BE30.04.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2016/39]AT17.02.2016
ES17.02.2016
LT17.02.2016
LV17.02.2016
PL17.02.2016
BE30.04.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2016/38]AT17.02.2016
ES17.02.2016
LT17.02.2016
PL17.02.2016
BE30.04.2016
NO17.05.2016
GR18.05.2016
PT17.06.2016
Former [2016/36]AT17.02.2016
ES17.02.2016
LT17.02.2016
PL17.02.2016
BE30.04.2016
NO17.05.2016
GR18.05.2016
Former [2016/35]ES17.02.2016
NO17.05.2016
GR18.05.2016
Documents cited:Search[X]US2003203855  (POTTER BARRY VICTOR LLOYD [GB], et al) [X] 1,6,8 * page 22, paragraph [0358] * * page 24, paragraph [0388] * * page 1, paragraph [0011] * * page 20, paragraph [0344] *;
 [X]US2938030  (KARL HOFFMANN, et al) [X] 1,6,8 * column 1, lines 53-56; example 3 *;
 [X]US5914325  (DROESCHER PETER [DE], et al) [X] 1,6,8 * column 1, lines 11-38 * * page 2, lines 66-67 * * page 3, lines 1-2, 9-10 * * page 15, lines 18-21 *;
 [X]WO2005048956  (UNIV MASSACHUSETTS [US], et al) [X] 1,6,8 * 10th compound; pages 23-24; table 2 * * page 2, lines 21-25 *;
 [X]WO2004085457  (STERIX LTD [GB], et al) [X] 1,6,8 * page 75, paragraph 7 * * page 80, paragraph last * * page 81, paragraph 6 * * page 82, paragraphs 1,2 * * page 83, paragraph 1 *;
 [X]WO02068548  (SCHERING AG [DE]) [X] 1,6,8 * page 13, lines 7-8, 11-12, 15-16 * * page 3, paragraph l * * page 14, paragraph 1 * * page 15, paragraph 2 *
 [X]  - J. HEER ET AL, "Über Pyridyl-Steroide. II.", HELVETICA CHIMICA ACTA., CHVERLAG HELVETICA CHIMICA ACTA. BASEL., (1956), vol. 39, no. 6, ISSN 0018-019X, pages 1814 - 1820, XP002684164 [X] 1 * page 1815; compounds IIa, IIb *

DOI:   http://dx.doi.org/10.1002/hlca.19560390641
 [X]  - ROMER W ET AL, "Novel estrogens and their radical scavenging effects, iron-chelating, and total antioxidative activities: 17alpha-substituted analogs of DELTA<9(11)>-dehydro-17beta-estradiol", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, (19971101), vol. 62, no. 11, doi:10.1016/S0039-128X(97)00068-8, ISSN 0039-128X, pages 688 - 694, XP004099052 [X] 1,6,8 * page 690; figure 1 * * page 691; tables 1,2 *

DOI:   http://dx.doi.org/10.1016/S0039-128X(97)00068-8
 [X]  - HANSON ROBERT N ET AL, "Synthesis and evaluation of 17alpha-20E-21-(4-substituted phenyl)-19-norpregna-1,3,5(10),20-tetraene-3,17beta-diols as probes for the estrogen receptor alpha hormone binding domain.", JOURNAL OF MEDICINAL CHEMISTRY 3 JUL 2003 LNKD- PUBMED:12825929, (20030703), vol. 46, no. 14, ISSN 0022-2623, pages 2865 - 2876, XP002684165 [X] 1,6 * page 2867; compounds 4b, 4c, 5b, 5c * * page 2868; table 2 *

DOI:   http://dx.doi.org/10.1021/jm0205806
 [X]  - HANSON ROBERT N ET AL, "Synthesis and evaluation of (17alpha,20Z)-21-(4-substituted-phenyl)-19-norpregna-1,3,5(10),20-tetraene-3,17beta-diols as ligands for the estrogen receptor-alpha hormone binding domain: comparison with 20E-isomers.", JOURNAL OF MEDICINAL CHEMISTRY 30 JUN 2005 LNKD- PUBMED:15974584, (20050630), vol. 48, no. 13, ISSN 0022-2623, pages 4300 - 4311, XP002684166 [X] 1,6 * page 4302; table 2; compounds 5c, 5d, 6c, 6d *

DOI:   http://dx.doi.org/10.1021/jm040157s
 [X]  - BLICKENSTAFF R T ET AL, "Conjugates of steroids and anti-cancer agents. III. The synthesis of estrynamine and certain derivatives", STEROIDS, ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, US, vol. 48, no. 3-4, doi:10.1016/0039-128X(86)90005-X, ISSN 0039-128X, (19860901), pages 223 - 231, (19860901), XP025205710 [X] 1,6 * page 229; compound 11 * * page 231, paragraph 2 *

DOI:   http://dx.doi.org/10.1016/0039-128X(86)90005-X
 [X]  - K. KAM-WING LO ET AL, "Luminescent Tricarbonylrhenium(I) Polypyridine Estradiol Conjugates: Synthesis, Crystal Structure, and Photophysical, Electrochemical, and Protein-Binding Properties", ORGANOMETALLICS., ACS, WASHINGTON, DC., (2006), vol. 25, no. 13, ISSN 0276-7333, pages 3220 - 3227, XP002684167 [X] 1 * page 3221; compounds Py-est * * page 3227; figure 4; compound 1a *

DOI:   http://dx.doi.org/10.1021/om060193k
 [X]  - ARTERBURN JEFFREY B ET AL, "Synthesis of 17-alpha-substituted estradiol-pyridin-2-yl hydrazine conjugates as effective ligands for labeling with Alberto's complex fac-[Re(OH2)3(CO)3]+ in water.", THE JOURNAL OF ORGANIC CHEMISTRY 5 SEP 2003 LNKD- PUBMED:12946150, (20030905), vol. 68, no. 18, ISSN 0022-3263, pages 7063 - 7070, XP002684168 [X] 1 * page 7065; compounds 1,2,7a,9b *

DOI:   http://dx.doi.org/10.1021/jo034780g
 [X]  - ALLAN GILLIAN M ET AL, "Modification of estrone at the 6, 16, and 17 positions: novel potent inhibitors of 17beta-hydroxysteroid dehydrogenase type 1.", JOURNAL OF MEDICINAL CHEMISTRY 23 FEB 2006 LNKD- PUBMED:16480268, (20060223), vol. 49, no. 4, ISSN 0022-2623, pages 1325 - 1345, XP002684169 [X] 1,6 * page 1327; compounds 18a, 18b, 18c * * page 1334; table 5 * * page 1325, column 2, paragraph 2 *

DOI:   http://dx.doi.org/10.1021/jm050830t
International search[X]CA2001938  (ENDORECHERCHE INC [CA]);
 [X]CA2062973  (ENDORECHERCHE INC [CA]);
 [X]CA2323089  (ENDORECH INC [CA]);
 [X]CA2339368  (ENDORECH INC [CA]);
 [X]WO2004089971  (ENDORECH INC [CA], et al);
 [X]US3117140  (ERICH HECKER);
 [X]  - PONSOLD ET AL., "Anodic oxidation of ring A-aromatic steroids. Cyanation of the aromatic nucleus", TET. LETT., (1979), vol. 46, pages 4465 - 4466, XP000867285

DOI:   http://dx.doi.org/10.1016/S0040-4039(01)86620-X
 [X]  - HOLT ET AL., "Steroidal A Ring Aryl Carboxylic Acids: A New Class of Steroid 5alpha-Reductase Inhibitors", J. MED. CHEM., (1990), vol. 33, pages 937 - 942, XP008122019

DOI:   http://dx.doi.org/10.1021/jm00165a009
 [X]  - SHI ET AL., "Functionally Orthogonal Ligand-Receptor Pairs for the Selective Regulation of Gene Expression Generated by Manipulation of Charged Residues at the Ligand-Receptor Interface of ERalpha and ERbeta", J. AM. CHEM. SOC., (2002), vol. 124, pages 6921 - 6928, XP008122020

DOI:   http://dx.doi.org/10.1021/JA016897X
 [X]  - HECKER, "Neue Ostranabkömmlinge mit verschiedenen Substitutenten in 3-Stellung", CHEM. BER., (1962), vol. 95, no. 4, pages 977 - 984, XP009035301
 [X]  - DORFMAN ET AL., "Uterotrophic Activity of Various Phenolic Steroids", ACTA ENDOCRIN., (1966), vol. 52, no. 4, pages 619 - 626, XP008122097
 [X]  - PONSOLD ET AL., "Electrochemical transformation of steroids", CAPLUS, (1979), Database accession no. (1991:201156h), XP008115872
 [XP]  - LIU ET AL., "Synthesis of 4-Formyl Estrone Using a Positional Protecting Group and Its Conversion to Other C-4-Substituted Estrogens", J. ORG. CHEM., (2007), vol. 72, no. 23, pages 8824 - 8830, XP008122021

DOI:   http://dx.doi.org/10.1021/JO7017075
by applicantUS5411981
 US6071957
 US2004077605
 US2004077606
 EP0100172
 EP0002892
 EP0494819
 EP0578516
 EP0580459
 WO9518794
 WO9619458
 WO9700071
 WO9719064
 WO9723464
 WO9853826
 JP2002088073
 WO0037430
 WO0116108
 WO0116133
 WO0224702
 WO2004099188
 WO2004111012
 WO2004113309
 WO2005040136
 US2005250749
 US2006287327
 WO0200617
 WO2005120483
 US2005033074
 US2005250741
 US2006014739
 US2006009529
 US3742951
 US3797494
 US4568343
 EP0279982
 US5064654
 US5071644
 US5071657
 WO9946279
 WO2005000011
 WO2004089971
 FR19910000185
 FR19920008431
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.