Extract from the Register of European Patents

EP About this file: EP2308861

EP2308861 - MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS [Right-click to bookmark this link]
Former [2011/15]Macrocyclic compounds useful as pharmaceuticals
[2015/20]
StatusNo opposition filed within time limit
Status updated on  05.01.2018
Database last updated on 19.03.2026
FormerThe patent has been granted
Status updated on  27.01.2017
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
Eisai R&D Management Co., Ltd.
6-10, Koishikawa 4-chome, Bunkyo-ku
Tokyo 112-8088 / JP
[2011/15]
Inventor(s)01 / Boivin, Roch
11 Oakland Road
Lawrence, MA 01843 / US
02 / Chiba, Kenichi
5-20-401, Oomachi
Tsuchiura-shi, Ibaraki / JP
03 / Muramoto, Kenzo
4-2-19 Ninomiya, Tsukuba-shi
Ibaraki 305-0051 / JP
04 / Shirota, Hiroshi
15 Greybirch Circle
Belmont, MA 02478 / US
05 / Du, Hong
7 Chandler Road
Andover Massachusetts 01810 / US
06 / Eguchi, Yoshihito
233-38, Toyoshiki
Kashiwa-shi, Chiba / JP
07 / Fujita, Masanori
128-3-6, Hitachinonishi
Ushiku-shi, Ibaraki / JP
08 / Gusovsky, Fabian
28 Algonquin Avenue
Andover, MA 01810 / US
09 / Goto, Masaki
1141-21, Naka
Tsuchiura-shi, Ibaraki / JP
10 / Harmange, Jean-Christophe
57 William Street
Andover, MA 01810 / US
11 / Inoue, Atsushi
2-10-15 Matsuhiro
Tsukuba-shi / JP
12 / Jiang, Yimin
16 Devonshire Lane
Londonderry, NH 03053 / US
13 / Kawada, Megumi
4-9 Kamiya 2-chome
Ushiku-shi, Ibaraki / JP
14 / Kawai, Takatoshi
2-11-33, Higashi
Tsukuba-shi, Ibaraki / JP
15 / Kawakami, Yoshiyuki
3-6-2 Tokodai, Tsukuba-shi
Ibaraki / JP
16 / KIMURA, Akifumi
7-2, Inarimae
Tsukuba-shi, Ibaraki / JP
17 / Kotake, Makoto
144-3-515, Abiko
Abiko-shi, Chiba / JP
18 / Kuboi, Yoshikazu
670-22 Shimohirooka
Tsukuba-shi, Ibaraki / JP
19 / Lemelin, Charles-André
C-38 Scotty Hollow Drive
North Chelmsford, MA 01863 / US
20 / Li, Xiang-Yi
329 High Plain Road
Andover, MA 01810 / US
21 / Matsushima, Tomohiro
10-2, Tagu 2-chome
Ushiku-shi, Ibaraki / JP
22 / Mizui, Yoshiharu
5-74, Ninomiya 4-Chome
Tsukuba-shi, Ibaraki / JP
23 / Sakurai, Hideki
2-2-34 Ninomiya
Tsukuba-shi, Ibaraki 305-0051 / JP
24 / Chow, Jesse
16 Stirling Avenue
Hooksett, NH 03106 / US
25 / Shen, Yong-Chun
21 Villa Roma Drive
Tewksbury, MA 01876 / US
26 / Spyvee, Mark
75 Laura Lane
Hampstead, NH 03841 / US
27 / Tanaka, Isao
2-5-16, Ninomiya
Tsukuba-shi, Ibaraki / JP
28 / Wang, John (Yuan)
344 River Road
Andover, MA 01810 / US
29 / Yamamoto, Satoshi
3-9-7, Misono
Moriya-shi, Ibaraki / JP
30 / Yoneda, Naoki
1-15-4-201 Azuma
Tsukuba-shi, Ibaraki / JP
 [2011/24]
Former [2011/15]01 / Boivin, Roch
11 Oakland Road
Lawrence, MA 01843 / US
02 / Chiba, Kenichi
5-20-401, Oomachi
Tsuchiura-shi, Ibaraki / JP
03 / Muramoto, Kenzo
4-2-19 Ninomiya, Tsukuba-shi
Ibaraki 305-0051 / JP
04 / Shirota, Hiroshi
15 Greybirch Circle
Belmont, MA 02478 / US
05 / Du, Hong
43 Upland Street
North Andover, MA 01845 / US
06 / Eguchi, Yoshihito
233-38, Toyoshiki
Kashiwa-shi, Chiba / JP
07 / Fujita, Masanori
128-3-6, Hitachinonishi
Ushiku-shi, Ibaraki / JP
08 / Gusovsky, Fabian
28 Algonquin Avenue
Andover, MA 01810 / US
09 / Goto, Masaki
1141-21, Naka
Tsuchiura-shi, Ibaraki / JP
10 / Harmange, Jean-Christophe
57 William Street
Andover, MA 01810 / US
11 / Inoue, Atsushi
2-10-15 Matsuhiro
Tsukuba-shi / JP
12 / Jiang, Yimin
16 Devonshire Lane
Londonderry, NH 03053 / US
13 / Kawada, Megumi
4-9 Kamiya 2-chome
Ushiku-shi, Ibaraki / JP
14 / Kawai, Takatoshi
2-11-33, Higashi
Tsukuba-shi, Ibaraki / JP
15 / Kawakami, Yoshiyuki
3-6-2 Tokodai, Tsukuba-shi
Ibaraki / JP
16 / KIMURA, Akifumi
7-2, Inarimae
Tsukuba-shi, Ibaraki / JP
17 / Kotake, Makoto
144-3-515, Abiko
Abiko-shi, Chiba / JP
18 / Kuboi, Yoshikazu
670-22 Shimohirooka
Tsukuba-shi, Ibaraki / JP
19 / Lemelin, Charles-André
C-38 Scotty Hollow Drive
North Chelmsford, MA 01863 / US
20 / Li, Xiang-Yi
329 High Plain Road
Andover, MA 01810 / US
21 / Matsushima, Tomohiro
10-2, Tagu 2-chome
Ushiku-shi, Ibaraki / JP
22 / Mizui, Yoshiharu
5-74, Ninomiya 4-Chome
Tsukuba-shi, Ibaraki / JP
23 / Sakurai, Hideki
2-2-34 Ninomiya
Tsukuba-shi, Ibaraki 305-0051 / JP
24 / Chow, Jesse
16 Stirling Avenue
Hooksett, NH 03106 / US
25 / Shen, Yong-Chun
21 Villa Roma Drive
Tewksbury, MA 01876 / US
26 / Spyvee, Mark
75 Laura Lane
Hampstead, NH 03841 / US
27 / Tanaka, Isao
2-5-16, Ninomiya
Tsukuba-shi, Ibaraki / JP
28 / Wang, John (Yuan)
344 River Road
Andover, MA 01810 / US
29 / Yamamoto, Satoshi
3-9-7, Misono
Moriya-shi, Ibaraki / JP
30 / Yoneda, Naoki
1-15-4-201 Azuma
Tsukuba-shi, Ibaraki / JP
Representative(s)Harris, Jennifer Lucy, et al
Kilburn & Strode LLP
Lacon London
84 Theobalds Road
London WC1X 8NL / GB
[N/P]
Former [2011/15]Harris, Jennifer Lucy, et al
Kilburn & Strode LLP 20 Red Lion Street
London WC1R 4PJ / GB
Application number, filing date10075633.707.03.2003
[2011/15]
Priority number, dateUS20020362883P08.03.2002         Original published format: US 362883 P
US20020380711P14.05.2002         Original published format: US 380711 P
[2011/15]
Filing languageEN
Procedural languageEN
PublicationType: A1 Application with search report 
No.:EP2308861
Date:13.04.2011
Language:EN
[2011/15]
Type: B1 Patent specification 
No.:EP2308861
Date:01.03.2017
Language:EN
[2017/09]
Search report(s)(Supplementary) European search report - dispatched on:EP24.02.2011
ClassificationIPC:C07D313/00, A61K31/335, A61P29/00, C07D225/06, C07D407/12, C07D491/04, C07D267/00, C07D493/04, A61K31/36, A61K31/395, A61P11/06, A61P17/06, A61P17/16, A61P19/04, A61P35/00, A61P37/06
[2011/15]
CPC:
C07D405/12 (EP,US); C07D313/00 (EP,CN,KR,US); A61K31/335 (EP,US);
A61K31/36 (EP,US); A61K31/395 (EP,CN,US); A61P1/00 (EP);
A61P1/04 (EP); A61P1/16 (EP); A61P11/00 (EP);
A61P11/02 (EP); A61P11/06 (EP); A61P11/08 (EP);
A61P13/02 (EP); A61P17/00 (EP); A61P17/02 (EP);
A61P17/04 (EP); A61P17/06 (EP); A61P17/16 (EP);
A61P19/00 (EP); A61P19/02 (EP); A61P19/04 (EP);
A61P19/10 (EP); A61P21/04 (EP); A61P25/00 (EP);
A61P25/02 (EP); A61P25/08 (EP); A61P25/28 (EP);
A61P27/02 (EP); A61P29/00 (EP); A61P3/10 (EP);
A61P31/04 (EP); A61P31/18 (EP); A61P33/06 (EP);
A61P35/00 (EP); A61P35/02 (EP); A61P37/00 (EP);
A61P37/02 (EP); A61P37/06 (EP); A61P37/08 (EP);
A61P43/00 (EP); A61P7/00 (EP); A61P7/04 (EP);
A61P9/00 (EP); A61P9/10 (EP); C07D231/12 (EP,US);
C07D233/56 (EP,US); C07D249/08 (EP,US); C07D401/12 (EP,US);
C07D407/12 (KR); C07D491/04 (EP,US); C07D491/044 (EP,US);
C07D493/04 (EP,US); Y02A50/30 (EP,US) (-)
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 [2017/09]
Former [2011/15]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 statesAL10.10.2011
LT10.10.2011
LV10.10.2011
MK10.10.2011
TitleGerman:MACROCYCLISCHE VERBINDUNGEN VERWENDBAR ALS ARZNEITMITTELN[2015/19]
English:MACROCYCLIC COMPOUNDS USEFUL AS PHARMACEUTICALS[2015/20]
French:COMPOSES MACROCYCLIQUES UTILES EN TANT QU'AGENTS PHARMACEUTIQUES[2015/19]
Former [2011/15]Macrocyclische verbindungen verwendbar als Arzneitmitteln
Former [2011/15]Macrocyclic compounds useful as pharmaceuticals
Former [2011/15]Composés macrocycliques utiles en tant qu'agents pharmaceutiques
Examination procedure10.10.2011Examination requested  [2011/46]
27.01.2012Amendment by applicant (claims and/or description)
02.11.2012Despatch of a communication from the examining division (Time limit: M06)
28.08.2013Reply to a communication from the examining division
13.03.2015Cancellation of oral proceeding that was planned for 17.03.2015
17.03.2015Date of oral proceedings (cancelled)
15.04.2015Communication of intention to grant the patent
14.08.2015Disapproval of the communication of intention to grant the patent by the applicant or resumption of examination proceedings by the EPO
04.09.2015Communication of intention to grant the patent
12.04.2016Despatch of communication that the application is deemed to be withdrawn, reason: fee for grant / fee for printing not paid in time
21.06.2016Fee for grant paid
21.06.2016Fee for publishing/printing paid
21.06.2016Receipt of the translation of the claim(s)
Parent application(s)   TooltipEP03721353.5  / EP1507773
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 (EP20030721353) is  21.09.2005
Opposition(s)04.12.2017No opposition filed within time limit [2018/06]
Request for further processing for:The application is deemed to be withdrawn due to failure to fulfill actions required for granting the patent
21.06.2016Request for further processing filed
21.06.2016Full payment received (date of receipt of payment)
Request granted
01.07.2016Decision despatched
The application is deemed to be withdrawn due to failure to reply to the examination report
28.08.2013Request for further processing filed
28.08.2013Full payment received (date of receipt of payment)
Request granted
09.09.2013Decision despatched
The application is deemed to be withdrawn due to failure to reply to the Extended European Search Report/Written Opinion of the International Searching Authority/International Preliminary Examination Report/Supplementary international search report/Supplementary European search report
27.01.2012Request for further processing filed
27.01.2012Full payment received (date of receipt of payment)
Request granted
10.02.2012Decision despatched
Fees paidRenewal fee
18.01.2011Renewal fee patent year 03
18.01.2011Renewal fee patent year 04
18.01.2011Renewal fee patent year 05
18.01.2011Renewal fee patent year 06
18.01.2011Renewal fee patent year 07
18.01.2011Renewal fee patent year 08
29.03.2011Renewal fee patent year 09
26.03.2012Renewal fee patent year 10
27.03.2013Renewal fee patent year 11
27.03.2014Renewal fee patent year 12
27.03.2015Renewal fee patent year 13
31.03.2016Renewal fee patent year 14
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Lapses during opposition  TooltipHU07.03.2003
AT01.03.2017
CY01.03.2017
CZ01.03.2017
DK01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SI01.03.2017
SK01.03.2017
TR01.03.2017
IE07.03.2017
LU07.03.2017
BE31.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
[2020/15]
Former [2019/46]HU07.03.2003
AT01.03.2017
CY01.03.2017
CZ01.03.2017
DK01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SI01.03.2017
SK01.03.2017
IE07.03.2017
LU07.03.2017
BE31.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2019/31]HU07.03.2003
AT01.03.2017
CZ01.03.2017
DK01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SI01.03.2017
SK01.03.2017
IE07.03.2017
LU07.03.2017
BE31.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2018/24]AT01.03.2017
CZ01.03.2017
DK01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SI01.03.2017
SK01.03.2017
IE07.03.2017
LU07.03.2017
BE31.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2018/13]AT01.03.2017
CZ01.03.2017
DK01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SI01.03.2017
SK01.03.2017
IE07.03.2017
LU07.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2018/10]AT01.03.2017
CZ01.03.2017
DK01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SK01.03.2017
LU07.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2018/09]AT01.03.2017
CZ01.03.2017
DK01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SK01.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2018/06]AT01.03.2017
CZ01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
MC01.03.2017
RO01.03.2017
SK01.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2017/51]AT01.03.2017
CZ01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
RO01.03.2017
SK01.03.2017
BG01.06.2017
GR02.06.2017
PT03.07.2017
Former [2017/49]AT01.03.2017
CZ01.03.2017
EE01.03.2017
ES01.03.2017
FI01.03.2017
IT01.03.2017
RO01.03.2017
SK01.03.2017
BG01.06.2017
GR02.06.2017
Former [2017/48]AT01.03.2017
CZ01.03.2017
ES01.03.2017
FI01.03.2017
BG01.06.2017
GR02.06.2017
Former [2017/42]AT01.03.2017
ES01.03.2017
FI01.03.2017
BG01.06.2017
GR02.06.2017
Documents cited:Search[ID] EP0606044  (SANDOZ LTD et al.)
 [ID] WO9613259  (COR THERAPEUTICS INC et al.)
 [ID] WO0038674  (NOVATION PHARMACEUTICALS INC et al.)
 [IP] WO0248136  (CHUGAI PHARMACEUTICAL CO LTD et al.)
 [I]   AGAMUSTA T. ET AL.: "Revised Structure and Stereochemistry of Hypothemycin", CHEM. PHARM. BULL., vol. 41, no. 2, 1993, pages 373 - 375, XP001152923
 [I]   TAKEHANA K. ET AL.: "A Radicicol-Related Macrocyclic Nonanketide Compound, Antibiotic LL-Z1640-2, Inhibits the JNK/p38 Pathways in Signal-Specific Manner", BIOCHEM. BIOPHYS. RES. COMM., vol. 257, 1999, pages 19 - 23, XP002244484

DOI:   http://dx.doi.org/10.1006/bbrc.1999.0401
by applicantGB323845
 EP0606044
 WO0038674
 JPH0840893
 WO9613259
 US5728726
 US5674892
 US5795910
 US5837224
 US6517889
 US6273913
 US6258121
 US6251136
 US6248127
 US6231600
 US6203551
 US6153252
 US6071305
 US5891507
 US5837313
 US2001027340
 US6515016
 US4768523
 US4776337
 US5041126
 US5052998
 US5064435
 US5089606
 US5147370
 US5176626
 US5213580
 US5328471
 US2002106339
 US4336243
 US4615699
 US4751087
   MCGAHREN ET AL., J ORG. CHEM., vol. 43, 1978, pages 2339
   THOMAS SORRELL: "Organic Chemistry", 1999, UNIVERSITY SCIENCE BOOKS
   . GREENE, T.W. AND WUTS, P.G.,: "Protective Groups in Organic Synthesis,3rd ed.", 1999, JOHN WILEY & SONS
   S.M. BERGE ET AL., J. PHARMACEUTICAL SCIENCES, vol. 66, 1977, pages 1 - 19
   T. HIGUCHI; V. STELLA: "Pro-drugs as Novel Delivery Systems", A.C.S. SYMPOSIUM SERIES, vol. 14
   EDWARD B. ROCHE,: "Bioreversible Carriers in Drug Design", 1987, AMERICAN PHARMACEUTICAL ASSOCIATION AND PERGAMON PRESS
   E. W. MARTIN: "Remington's Pharmaceutical Sciences, Sixteenth Edition,", 1980, MACK PUBLISHING CO.
   "Defense and Disease", J CLIN. INVESTIG., vol. 107, 2001, pages 7
   "Angiogenesis: Potentials for Pharmacologic Intervention in the Treatment of Cancer, Cardiovascular Diseases, and Chronic Inflammation", PHARMACOLOGICAL REVIEWS, vol. 52, 2000, pages 237
   "The Merck Manual", 1999, MERCK & CO.
   P. ANGEL ET AL.: "Function and regulation of AP-1 subunits in skin physiology and pathology", ONCOGENE, vol. 20, 2001, pages 2413 - 2423
   A. GRANDJEAN-LAQUERRIERE ET AL.: "Relative contribution of NF-kB and AP-1 in the modulation by Curcumin and pyrrolidine dithiocarbamate of the UVB-induced cytokine expression by keratinocytes", CYTOKINE, vol. 18, no. 3, 2002, pages 168 - 177
   "Angiogenesis: Potentials for Pharmacologic Intervention in the Treatment of Cancer, Cardiovascular Diseases, and chronic Inflammation", PHARMACOLOGICAL REVIEWS, vol. 52, 2000, pages 253
   PRESBITERO P. ET AL.: "Drug eluting stents do they make the difference?", MINERVA CARDIOANGIOL, vol. 50, no. 5, 2002, pages 431 - 442
   RUYGROK P.N. ET AL.: "Rapamycin in cardiovascular medicine", INTERN. MED J., vol. 33, no. 3, 2003, pages 103 - 109
   MARX S.O. ET AL.: "Bench to bedside: the development of rapamycin and its application to stent restenosis", CIRCULATION, vol. 104, no. 8, 2001, pages 852 - 855
   GOODMAN; GILMAN'S: "The Pharmacological Basis of Therapeutics", 2001, MCGRAW-HILL PRESS, pages: 155 - 173
   CHEN: "Activation of p38 MAP kinase and ERK are required for ultraviolet-B induced c-fos gene expression in human keratinocytes", ONCOGENE, vol. 18, 1999, pages 7469 - 7476
   LI ET AL.: "Rays and arrays: the transcriptional program in the response of human epidermal keratotinocutes to UVB illumination", THE FASEB JOURNAL, 17 September 2001 (2001-09-17)
   "Remington's Pharmaceutical Sciences, 16th Edition", 1980, MACK PUBLISHING COMPANY, pages: 1985
   MAIBACH H. I. AND SMITH H. E.: "Percutaneous Penetration Enhancers", 1995, CRC PRESS, INC.
   BUYUKTIMKIN ET AL.: "Transdermal and Topical Drug Delivery Systems", 1997, INTERPHARM PRESS INC., article "Chemical Means of Transdermal Drug Permeation Enhancement"
   GHOSH, T. K.; PFISTER, W. R.; YUM, S. I.: "Transdermal and Topical Drug Delivery Systems", INTERPHARM PRESS, INC., pages: 249 - 297
   PETERSON, T. A.; DREYER, S. J., PROCEED. INTERN. SYMP. CONTROL. REL. BIOACT. MATER., vol. 21, pages 477 - 478
   WESTER, R. C.; MAIBACH, H. I.: "Percutaneous Absorption, Mechanism, Methodology, Drug Delivery", 1989, MARCEL DEKKER, INC., article "Regional variation in Percutaneous Absorption", pages: 111 - 119
   "The Merck Manual", 1999
   FIESER; FIESER: "Reagents for Organic Synthesis", vol. 1-17, 1991, JOHN WILEY AND SONS
   RODD: "Chemistry of Carbon Compounds", vol. 1-5, 1989, ELSEVIER SCIENCE PUBLISHERS
   "Organic Reactions", vol. 1-40, 1991, JOHN WILEY AND SONS
   MARCH: "Advanced Organic Chemistry 5th ed.", 2001, JOHN WILEY AND SONS
   LAROCK: "Comprehensive Organic Transformations: A Guide to Functional Group Preparations", 1990, VCH PUBLISHERS
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.