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

Italy joins the Federated Register

Click here for more information on the Federated Register.

2025-06-12

More...
blank Related links

Release notes
European Patent Register Assistant
European Patent Register User Manual
European Patent Register – pocket guide
FAQ - European Patent Register
Federated Register (Flyer)
Global Dossier (Flyer)
Register events
Deep link coverage
Federated Register content
The Patent Information Tour
Fair use charter

Extract from the Register of European Patents

EP About this file: EP1466916

EP1466916 - Peptide boronic acids useful in making salts thereof [Right-click to bookmark this link]
StatusNo opposition filed within time limit
Status updated on  29.08.2008
Database last updated on 14.03.2026
Most recent event   Tooltip20.08.2010Lapse of the patent in a contracting state
New state(s): TR		published on 22.09.2010  [2010/38]
Applicant(s)For all designated states
TRIGEN LIMITED
20 St James's Street
London SW1A 1ES / GB
[2004/42]
Inventor(s)01 / Madge, David Jonathan, c/o NCE Discovery Ltd.
Cruciform Building, Gower Street
London WC1E 6AU / GB
02 / Dolman, Mark, c/o NCE Discovery Ltd.
Cruciform Building, Gower Street
London WC1E 6AU / GB
03 / Combe-Marzelle, Sophie, Marie Trigen Limited
Clareville House 26/27 Oxendon Street
London SW1Y 4EL / GB
04 / Deadman, John, Joseph Amrad Corp. Limited
576 Swann Street
Richmond, Victoria 3121 / AU
05 / Kennedy, Anthony, James Trigen Limited
Clareville House 26/27 Oxendon Street
London SW1Y 4EL / GB
06 / Kakkar, Sanjay Kumar Trigen Limited
Clareville House, 26/27 Oxendon Street
London SW1Y 4EL / GB
07 / Walter, Armin Girindus AG
Werk Kunsebeck Kantstrasse 2
33777 Halle/Westf. / DE
08 / Olbrich, Alfred Girindus AG
Werk Kunsebeck Kantstrasse 2
33777 Halle/Westf. / DE
09 / Krimmer, Dieter Pharma Quick Develop. GmbH
Hinterbergstrasse 24
9330 Cham-Steinhausen / CH
10 / Weiland-Weibel, Andrea, Maria, Theresia
Pharma Quick Devlop. GmbH Hinterbergstrasse 24
6330 Cham-Steinhausen / CH
 [2004/42]
Representative(s)HGF
1 City Walk
Leeds LS11 9DX / GB
[N/P]
Former [2004/42]Harrison Goddard Foote
Belgrave Hall Belgrave Street
Leeds LS2 8DD / GB
Application number, filing date04076510.909.09.2003
[2004/42]
Priority number, dateGB2002002076409.09.2002         Original published format: GB 0220764
GB2002002082209.09.2002         Original published format: GB 0220822
GB2003000781704.04.2003         Original published format: GB 0307817
GB2003001123716.05.2003         Original published format: GB 0311237
GB2003001569104.07.2003         Original published format: GB 0315691
US2003048578608.07.2003         Original published format: US 485786
[2004/42]
Filing languageEN
Procedural languageEN
PublicationType: A1 Application with search report 
No.:EP1466916
Date:13.10.2004
Language:EN
[2004/42]
Type: B1 Patent specification 
No.:EP1466916
Date:24.10.2007
Language:EN
[2007/43]
Search report(s)(Supplementary) European search report - dispatched on:EP10.08.2004
ClassificationIPC:C07F5/02
[2004/42]
CPC:
C07D207/08 (EP,KR); C07F5/02 (KR); A61K31/69 (EP,KR);
A61K45/06 (EP); A61P13/12 (EP); A61P43/00 (EP);
A61P7/02 (EP); A61P9/00 (EP); A61P9/10 (EP);
C07F5/025 (EP); C07K5/06078 (EP); C07K5/06191 (EP);
A61K38/00 (EP) (-)
C-Set:
A61K31/69, A61K2300/00 (EP)
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 [2004/42]
Extension statesAL13.04.2005
LT13.04.2005
LV13.04.2005
MK13.04.2005
TitleGerman:Peptidborsäuren und deren Verwendung in der Herstellung von Salzen derselben[2004/42]
English:Peptide boronic acids useful in making salts thereof[2004/42]
French:Acides boroniques peptidiques utilises pour préparer leurs sels[2004/42]
Examination procedure24.05.2004Examination requested  [2004/42]
03.05.2005Despatch of a communication from the examining division (Time limit: M04)
08.09.2005Reply to a communication from the examining division
20.03.2006Despatch of a communication from the examining division (Time limit: M04)
12.07.2006Reply to a communication from the examining division
30.10.2006Communication of intention to grant the patent
09.03.2007Fee for grant paid
09.03.2007Fee for publishing/printing paid
25.04.2007Despatch of communication that the application is deemed to be withdrawn, reason: fee for grant / fee for printing not paid in time
Parent application(s)   TooltipEP03255590.6  / EP1400245
Opposition(s)25.07.2008No opposition filed within time limit [2008/40]
Request for further processing for:14.06.2007Request for further processing filed
14.06.2007Full payment received (date of receipt of payment)
Request granted
27.06.2007Decision despatched
Fees paidRenewal fee
30.09.2005Renewal fee patent year 03
02.10.2006Renewal fee patent year 04
01.10.2007Renewal 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  TooltipAT24.10.2007
BE24.10.2007
CY24.10.2007
CZ24.10.2007
DK24.10.2007
EE24.10.2007
FI24.10.2007
NL24.10.2007
RO24.10.2007
SI24.10.2007
SK24.10.2007
TR24.10.2007
BG24.01.2008
SE24.01.2008
GR25.01.2008
ES04.02.2008
PT24.03.2008
HU25.04.2008
[2010/38]
Former [2010/34]AT24.10.2007
BE24.10.2007
CY24.10.2007
CZ24.10.2007
DK24.10.2007
EE24.10.2007
FI24.10.2007
NL24.10.2007
RO24.10.2007
SI24.10.2007
SK24.10.2007
BG24.01.2008
SE24.01.2008
GR25.01.2008
ES04.02.2008
PT24.03.2008
HU25.04.2008
Former [2009/35]AT24.10.2007
BE24.10.2007
CY24.10.2007
CZ24.10.2007
DK24.10.2007
EE24.10.2007
FI24.10.2007
NL24.10.2007
RO24.10.2007
SI24.10.2007
SK24.10.2007
BG24.01.2008
SE24.01.2008
GR25.01.2008
ES04.02.2008
PT24.03.2008
Former [2009/22]AT24.10.2007
BE24.10.2007
CZ24.10.2007
DK24.10.2007
EE24.10.2007
FI24.10.2007
NL24.10.2007
RO24.10.2007
SI24.10.2007
SK24.10.2007
BG24.01.2008
SE24.01.2008
GR25.01.2008
ES04.02.2008
PT24.03.2008
Former [2009/13]AT24.10.2007
BE24.10.2007
CZ24.10.2007
DK24.10.2007
FI24.10.2007
NL24.10.2007
RO24.10.2007
SI24.10.2007
SK24.10.2007
BG24.01.2008
SE24.01.2008
GR25.01.2008
ES04.02.2008
PT24.03.2008
Former [2008/39]AT24.10.2007
BE24.10.2007
CZ24.10.2007
DK24.10.2007
NL24.10.2007
RO24.10.2007
SI24.10.2007
SK24.10.2007
BG24.01.2008
SE24.01.2008
ES04.02.2008
PT24.03.2008
Former [2008/35]AT24.10.2007
CZ24.10.2007
DK24.10.2007
NL24.10.2007
SI24.10.2007
BG24.01.2008
SE24.01.2008
ES04.02.2008
PT24.03.2008
Former [2008/29]AT24.10.2007
NL24.10.2007
SI24.10.2007
BG24.01.2008
SE24.01.2008
ES04.02.2008
PT24.03.2008
Former [2008/26]NL24.10.2007
SI24.10.2007
BG24.01.2008
SE24.01.2008
ES04.02.2008
PT24.03.2008
Former [2008/24]NL24.10.2007
BG24.01.2008
SE24.01.2008
ES04.02.2008
PT24.03.2008
Documents cited:Search[X] WO9800443  (THROMBOSIS RES INST et al.) [X] 1-6,10-18 * figure 1; claim 17 *
 [A] WO9421668  (DU PONT MERCK PHARMA et al.) [A] 1-26 * the whole document *
 [X]   SKORDALAKES E ET AL: "Crystallographic structures of human [alpha]-thrombin complexed to peptide boronic acids lacking a positive charge at P1. Evidence of novel interactions", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY 1997 UNITED STATES, vol. 119, no. 41, 1997, pages 9935 - 9936, XP002289631, ISSN: 0002-7863 [X] 1-5,10-17,19 * compound 1 *

DOI:   http://dx.doi.org/10.1021/ja9713338
 [X]   SKORDALAKES E ET AL: "Bifunctional peptide boronate inhibitors of thrombin: Crystallographic analysis of inhibition enhanced by linkage to an exosite 1 binding peptide", BIOCHEMISTRY, AMERICAN CHEMICAL SOCIETY. EASTON, PA, US, vol. 37, no. 41, 13 October 1998 (1998-10-13), pages 14420 - 14427, XP002262060, ISSN: 0006-2960 [X] 1-6,10-18 * compound 2 *

DOI:   http://dx.doi.org/10.1021/bi980225a
 [A]   ELGENDY S ET AL: "Design of a novel class of bifunctional thrombin inhibitors, synthesised by the first application of peptide boronates in solid phase chemistry", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 38, no. 18, 5 May 1997 (1997-05-05), pages 3305 - 3308, XP004059837, ISSN: 0040-4039 [A] 1-26 * figure - *

DOI:   http://dx.doi.org/10.1016/S0040-4039(97)00592-3
 [DA]   DEADMAN J ET AL: "STRUCTURE/FUNCTION ASPECTS OF NEUTRAL P1 RESIDUE PEPTIDE INHIBITORS OF THROMBIN", JOURNAL OF ENZYME INHIBITION, NEW YORK, NY, US, vol. 9, 1995, pages 29 - 41, XP000570970 [DA] 1-26 * figure 1; table 1 *
 [A]   WITYAK J ET AL: "Synthesis of thrombin inhibitor DuP 714", JOURNAL OF ORGANIC CHEMISTRY 1995 UNITED STATES, vol. 60, no. 12, 1995, pages 3717 - 3722, XP002289632, ISSN: 0022-3263 [A] 1-26 * compound 10 *

DOI:   http://dx.doi.org/10.1021/jo00117a024
 [DA]   DEADMAN J J ET AL: "CHARACTERIZATION OF A CLASS OF PEPTIDE BORONATES WITH NEUTRAL P1 SIDE CHAINS AS HIGHLY SELECTIVE INHIBITORS OF THROMBIN", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 38, no. 9, 28 April 1995 (1995-04-28), pages 1511 - 1522, XP000569517, ISSN: 0022-2623 [DA] 1-26 * compounds 8 - 15 *

DOI:   http://dx.doi.org/10.1021/jm00009a012
 [DA]   ELGENDY S ET AL: "FACILE ROUTES TO 1-HALO-1-ALKYL BORONIC ESTERS AS PRECURSORS FOR NOVEL THROMBIN INHIBITORS", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 50, no. 12, 21 March 1994 (1994-03-21), pages 3803 - 3812, XP000569519, ISSN: 0040-4020 [DA] 1-26 * compounds 6d & 6e *

DOI:   http://dx.doi.org/10.1016/S0040-4020(01)90400-4
 [DA]   TAPPARELLI C ET AL: "IN VITRO AND IN VIVO CHARACTERIZATION OF A NEUTRAL BORON-CONTAININGTHROMBIN INHIBITOR", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, US, vol. 268, no. 7, 5 March 1993 (1993-03-05), pages 4734 - 4741, XP000609100, ISSN: 0021-9258 [DA] 1-26 * figure 1 *
 [DA]   CLAESON G ET AL: "BENZYLOXYCARBONYL-D-PHE-PRO-METHOXYPROPYLBOROGLYCINE: A NOVEL INHIBITOR OF THROMBIN WITH HIGH SELECTIVITY CONTAINING A NEUTRAL SIDE CHAIN AT THE P1 POSITION", BIOCHEMICAL JOURNAL, PORTLAND PRESS, LONDON, GB, vol. 290, 1993, pages 309 - 312, XP000570507, ISSN: 0264-6021 [DA] 1-26 * compounds III & IV *
 [A]   CLAESON G ET AL: "NOVEL PEPTIDE MIMETICS AS HIGHLY EFFICIENT INHIBITORS OF THROMBIN BASED ON MODIFIED D-PHE-PRO-ARG SEQUENCES", AMERICAN PEPTIDE SYMPOSIUM, 1992, pages 824 - 825, XP000609384 [A] 1-26 * table 2, entry 2 *
 [A]   ELGENDY S ET AL: "NEW PEPTIDE BORONIC ACID INHIBITORS OF THROMBIN", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 33, no. 29, 14 July 1992 (1992-07-14), pages 4209 - 4212, XP000609104, ISSN: 0040-4039 [A] 1-26 * table 1, entries 2 & 6 *

DOI:   http://dx.doi.org/10.1016/S0040-4039(00)74691-0
 [A]   KETTNER C ET AL: "THE SELECTIVE INHIBITION OF THROMBIN BY PEPTIDES OF BOROARGININE*", JOURNAL OF BIOLOGICAL CHEMISTRY, AMERICAN SOCIETY OF BIOLOGICAL CHEMISTS, BALTIMORE, MD, US, vol. 265, no. 30, 25 October 1990 (1990-10-25), pages 18289 - 18297, XP000160262, ISSN: 0021-9258 [A] 1-26 * scheme 1, compound 4c *
ExaminationEP0471651
 WO9207869
   GUSTAFSSON D. ET AL: "The direct thrombin inhibitor melagatran and its oral prodrug H376/95: Intestinal absorption properties, biochemical and pharmacodynamic effects", THROMBOSIS RESEARCH, vol. 101, 2001, pages 171 - 181, XP001197148, ISSN: 0049-3848

DOI:   http://dx.doi.org/10.1016/S0049-3848(00)00399-6
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.