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Extract from the Register of European Patents

EP About this file: EP2275105

EP2275105 - Heterocyclic derivatives as opioid receptor modulators [Right-click to bookmark this link]
StatusNo opposition filed within time limit
Status updated on  11.08.2017
Database last updated on 28.03.2026
Most recent event   Tooltip06.03.2020Lapse of the patent in a contracting state
New state(s): TR		published on 08.04.2020  [2020/15]
Applicant(s)For all designated states
Janssen Pharmaceutica NV
Turnhoutseweg 30
2340 Beerse / BE
[2011/03]
Inventor(s)01 / Breslin, Henry J.
1974 Muhlenburg Drive
Lansdale, PA 19446 / US
02 / He, Wei
2002 Kestkal Circle
Audubon, PA 19403 / US
03 / Kavash, Robert W.
148 North Keswick Avenue
Glenside, PA 19038 / US
 [2016/40]
Former [2011/03]01 / Breslin, Henry J.
1974 Muhlenburg Drive
Lansdale, PA 19446 / US
02 / He, Wei
2002 Kestkal Circle
Audubon, PA 19403 / US
03 / Kavash, Robert W.
148 North Keswick Avenue
Glenside, PA 19038 / US
Representative(s)Kirsch, Susan Edith
Carpmaels & Ransford LLP
One Southampton Row
London WC1B 5HA / GB
[2016/40]
Former [2011/03]Kirsch, Susan Edith
Carpmaels & Ransford One Southampton Row London
WC1B 5HA / GB
Application number, filing date10180687.517.04.2003
[2011/03]
Priority number, dateUS20020376406P29.04.2002         Original published format: US 376406 P
US2003040000626.03.2003         Original published format: US 400006
[2011/03]
Filing languageEN
Procedural languageEN
PublicationType: A1 Application with search report 
No.:EP2275105
Date:19.01.2011
Language:EN
[2011/03]
Type: B1 Patent specification 
No.:EP2275105
Date:05.10.2016
Language:EN
[2016/40]
Search report(s)(Supplementary) European search report - dispatched on:EP08.11.2010
ClassificationIPC:A61K31/4439, A61K31/4725, A61P25/04, A61P1/00, C07D401/04, C07D413/04, C07D211/16, C07D405/14
[2011/03]
CPC:
C07D401/04 (EP,KR,US); A61P1/00 (EP); A61P1/04 (EP);
A61P1/10 (EP); A61P25/00 (EP); A61P25/04 (EP);
A61P43/00 (EP); C07D211/60 (EP,US); C07D217/26 (EP,US);
C07D413/04 (EP,US); C07D413/14 (KR) (-)
Designated contracting statesAT,   BE,   BG,   CH,   CY,   CZ,   DE,   DK,   EE,   ES,   FI,   FR,   GB,   GR,   HU,   IE,   IT,   LI,   LU,   MC,   NL,   PT,   RO,   SE,   SI,   SK,   TR [2016/40]
Former [2011/03]AT,  BE,  BG,  CH,  CY,  CZ,  DE,  DK,  EE,  ES,  FI,  FR,  GB,  GR,  HU,  IE,  IT,  LI,  LU,  MC,  NL,  PT,  RO,  SE,  SI,  SK,  TR 
Extension statesLT04.07.2011
LV04.07.2011
TitleGerman:Heterocyclische Derivate zur Verwendung als Modulatoren der Opioid-Rezeptoren[2015/51]
English:Heterocyclic derivatives as opioid receptor modulators[2011/03]
French:Dérivés hétérocycliques en tant que modulateurs de recepteurs d'opioides[2011/03]
Former [2011/03]Heterocyclische-Derivate zur Verwendung als Modulatoren der Opioid-Rezeptoren
Examination procedure04.07.2011Amendment by applicant (claims and/or description)
04.07.2011Examination requested  [2011/41]
28.10.2011Despatch of a communication from the examining division (Time limit: M04)
17.02.2012Reply to a communication from the examining division
02.08.2013Despatch of a communication from the examining division (Time limit: M04)
27.11.2013Reply to a communication from the examining division
06.02.2015Despatch of a communication from the examining division (Time limit: M04)
09.06.2015Reply to a communication from the examining division
17.11.2015Communication of intention to grant the patent
24.03.2016Disapproval of the communication of intention to grant the patent by the applicant or resumption of examination proceedings by the EPO
20.04.2016Communication of intention to grant the patent
23.08.2016Fee for grant paid
23.08.2016Fee for publishing/printing paid
23.08.2016Receipt of the translation of the claim(s)
Parent application(s)   TooltipEP03719805.8  / EP1499313
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 (EP20030719805) is  13.04.2006
Opposition(s)06.07.2017No opposition filed within time limit [2017/37]
Fees paidRenewal fee
28.09.2010Renewal fee patent year 03
28.09.2010Renewal fee patent year 04
28.09.2010Renewal fee patent year 05
28.09.2010Renewal fee patent year 06
28.09.2010Renewal fee patent year 07
28.09.2010Renewal fee patent year 08
12.04.2011Renewal fee patent year 09
28.03.2012Renewal fee patent year 10
12.04.2013Renewal fee patent year 11
25.03.2014Renewal fee patent year 12
10.04.2015Renewal fee patent year 13
11.04.2016Renewal fee patent year 14
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  TooltipAT05.10.2016
BE05.10.2016
CY05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
MC05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SI05.10.2016
SK05.10.2016
TR05.10.2016
BG05.01.2017
GR06.01.2017
PT06.02.2017
IE17.04.2017
LU17.04.2017
CH30.04.2017
LI30.04.2017
[2020/15]
Former [2019/46]AT05.10.2016
BE05.10.2016
CY05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
MC05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SI05.10.2016
SK05.10.2016
BG05.01.2017
GR06.01.2017
PT06.02.2017
IE17.04.2017
LU17.04.2017
CH30.04.2017
LI30.04.2017
Former [2018/23]AT05.10.2016
BE05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
MC05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SI05.10.2016
SK05.10.2016
BG05.01.2017
GR06.01.2017
PT06.02.2017
IE17.04.2017
LU17.04.2017
CH30.04.2017
LI30.04.2017
Former [2018/13]AT05.10.2016
BE05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
MC05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SI05.10.2016
SK05.10.2016
BG05.01.2017
GR06.01.2017
PT06.02.2017
LU17.04.2017
CH30.04.2017
LI30.04.2017
Former [2018/06]AT05.10.2016
BE05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
MC05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SI05.10.2016
SK05.10.2016
BG05.01.2017
GR06.01.2017
PT06.02.2017
Former [2017/52]AT05.10.2016
BE05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SI05.10.2016
SK05.10.2016
BG05.01.2017
GR06.01.2017
PT06.02.2017
Former [2017/38]AT05.10.2016
BE05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SK05.10.2016
BG05.01.2017
GR06.01.2017
PT06.02.2017
Former [2017/36]AT05.10.2016
BE05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
SK05.10.2016
GR06.01.2017
PT06.02.2017
Former [2017/35]AT05.10.2016
BE05.10.2016
CZ05.10.2016
DK05.10.2016
EE05.10.2016
FI05.10.2016
NL05.10.2016
RO05.10.2016
SE05.10.2016
GR06.01.2017
PT06.02.2017
Former [2017/33]AT05.10.2016
BE05.10.2016
DK05.10.2016
FI05.10.2016
NL05.10.2016
SE05.10.2016
GR06.01.2017
PT06.02.2017
Former [2017/29]AT05.10.2016
BE05.10.2016
FI05.10.2016
NL05.10.2016
SE05.10.2016
GR06.01.2017
PT06.02.2017
Documents cited:Search[Y] JPH05339240  
 [A] EP0506468  (LILLY CO ELI et al.)
 [X] US3023235  (FREDERICK LEONARD et al.)
 [X] US4563306  (SUGANO HIROSHI et al.)
 [X] US3763218  (KAISER A et al.)
 [YD]   BALBONI, G. ET AL.: "Opioid pseudopeptides containing heteroaromatic or heteroaliphatic nuclei", PEPTIDES, vol. 21, 2000, pages 1663 - 1671, XP002247104

DOI:   http://dx.doi.org/10.1016/S0196-9781(00)00315-6
 [YP]   BALBONI, G. ET AL.: "Evaluation of the Dmt-Tic pharmacophore: conversion of a potent delta-opioid receptor antagonist into a potent delta agonist and ligands with mixed properties.", J. MED. CHEM., vol. 45, no. 3, 2002, pages 713 - 720, XP002247105

DOI:   http://dx.doi.org/10.1021/jm010449i
 [Y]   PATENT ABSTRACTS OF JAPAN vol. 018, no. 182 (C - 1184) 29 March 1994 (1994-03-29)
 [Y]   SALVADORI, S. ET AL.: "Evolution of the Dmt-Tic pharmacophore: N-terminal methylated derivatives with extraordinary delta opioid antagonist activity.", J. MED. CHEM., vol. 40, no. 19, 1997, pages 3100 - 3108, XP002247213

DOI:   http://dx.doi.org/10.1021/jm9607663
 [Y]   OBASE H ET AL: "NEW ANTIHYPERTENSIVE AGENTS. II. STUDIES ON NEW ANALOG OF 4-PIPERIDYLBENZIMIDAZOLINONES", CHEMICAL AND PHARMACEUTICAL BULLETIN, PHARMACEUTICAL SOCIETY OF JAPAN. TOKYO, JP, vol. 30, no. 2, 1982, pages 474 - 483, XP000974108, ISSN: 0009-2363
 [X]   KRENITSKY P J ET AL: "Preparation of the 14-membered l,l-cycloisodityrosine subunit of RP 66453", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 43, no. 3, 14 January 2002 (2002-01-14), pages 407 - 410, XP004329390, ISSN: 0040-4039

DOI:   http://dx.doi.org/10.1016/S0040-4039(01)02194-3
 [X]   LEONARD, F. ET AL.: "Unnatural amino acids. II. Congeners of DL-3-carboxy-4-methoxyphenylalanine", J. MED. CHEM., vol. 10, 1967, pages 478 - 481, XP002258212

DOI:   http://dx.doi.org/10.1021/jm00315a040
 [X]   DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Frderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002258213, Database accession no. 5644822
 [X]   MAEDA, H. ET AL, CHEM. PHARM. BULL., vol. 36, no. 1, 1988, pages 190 - 201
Examination  MACCHIARULO A. ET AL.: "Conformational analysis of carboxyphenylglycine (CPG)derivatives: insight into bioactive and bioselective conformations ofgroup-I mGluRs antagonists", IL FARMACO, vol. 56, 2001, pages 891 - 898
   ANTONIO MACCHIARULO ET AL: "Conformational analysis of carboxyphenylglycine (CPG) derivatives: insight into bioactive and bioselective conformations of group-I mGluRs antagonists", IL FARMACO, vol. 56, no. 11, 1 November 2001 (2001-11-01), pages 891 - 898, XP055165120, ISSN: 0014-827X, DOI: 10.1016/S0014-827X(01)01155-7

DOI:   http://dx.doi.org/10.1016/S0014-827X(01)01155-7
by applicantWO9606855
   D.S. FRIES: "Principles of Medicinal Chemistry", 1995, WILLIAMS AND WILKINS, article "Analgesics", pages: 247 - 269
   J.V. ALDRICH: "Burger's Medicinal Chemistry and Drug Discovery", vol. 3, 1996, JOHN WILEY & SONS, INC., article "Analgesics", pages: 321 - 441
   PIERRE J.M. RIVIERE; JEAN-LOUIS JUNIEN: "Opioid receptors: Targets for new gastrointestinal drug development", DRUG DEVELOPMENT, 2000, pages 203 - 238
   PIERRE J. M. RIVIERE; JEAN-LOUIS JUNIEN: "Opioid receptors: Targets for new gastrointestinal drug development", DRUG DEVELOPMENT, 2000, pages 203 - 238
   P.W. SCHILLER ET AL., INT. J. PEPT. PROTEIN RES., vol. 41, no. 3, 1993, pages 313 - 316
   L.H. LAZARUS ET AL., PEPTIDES, vol. 21, 2000, pages 1663 - 1671
   M.P. WENTLAND ET AL., BIORG. MED. CHEM. LETTERS, vol. 11, 2001, pages 1717 - 1721
   M.P. WENTLAND ET AL., BIORG. MED. CHEM. LETTERS, vol. 11, 2001, pages 623 - 626
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   J. PHARM.SCI., vol. 66, no. 1, January 1997 (1997-01-01), pages 1
   H. BUNDGAARD: "Design of Prodrugs", 1985, ELSEVIER
   J.F.W. MCOMIE,: "Protective Groups in Orqanic Chemistry", 1973, PLENUM PRESS
   T.W. GREENE; P.G.M. WUTS: "Protective Groups in Orqanic Synthesis", 1991, JOHN WILEY & SONS
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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.