Extract from the Register of European Patents

About this file: EP1951676

EP1951676 - N-ACYL BENZAZEPINE DERIVATIVES AS LXR MODULATORS [Right-click to bookmark this link]
Former [2008/32]LXR MODULATORS
[2013/07]
StatusNo opposition filed within time limit
Status updated on  23.05.2014
Database last updated on 22.06.2019
Most recent event   Tooltip24.07.2015Lapse of the patent in a contracting state
New state(s): BG, HU, LU
published on 26.08.2015  [2015/35]
Applicant(s)For all designated states
Bristol-Myers Squibb Company
Route 206 and Province Line Road
Princeton, NJ 08543 / US
[N/P]
Former [2013/29]For all designated states
Bristol-Myers Squibb Company
Route 206 and Province Line Road
Princeton, NJ 08543-4000 / US
Former [2008/32]For all designated states
Bristol-Myers Squibb Company
Route 206 and Province Line Road
Princeton, NJ 08543-4000 / US
Inventor(s)01 / CHAO, Hannguang J.
c/o Bristol-Myers Squibb Company
311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
02 / TUERDI, Huji
c/o Bristol-Myers Squibb Company
311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
03 / KICK, Ellen K.
c/o Bristol-Myers Squibb Company
311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
04 / YANG, Wu
c/o Bristol-Myers Squibb Company
311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
 [2013/29]
Former [2008/32]01 / CHAO, Hannguang J.
c/o Bristol-Myers Squibb Company 311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
02 / TUERDI, Huji
c/o Bristol-Myers Squibb Company 311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
03 / KICK, Ellen K.
c/o Bristol-Myers Squibb Company 311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
04 / YANG, Wu
c/o Bristol-Myers Squibb Company 311 Pennington-Rocky Hill Road
Pennington, New Jersey 08534 / US
Representative(s)Beacham, Annabel Rose
Dehns
St Bride's House
10 Salisbury Square
London EC4Y 8JD / GB
[N/P]
Former [2013/29]Beacham, Annabel Rose
Dehns St Bride's House 10 Salisbury Square London
EC4Y 8JD / GB
Former [2008/32]Beacham, Annabel Rose
Frank B. Dehn & Co. St Bride's House 10 Salisbury Square
London EC4Y 8JD / GB
Application number, filing date06826273.219.10.2006
[2008/32]
WO2006US40882
Priority number, dateUS20050728964P21.10.2005         Original published format: US 728964 P
US2006058267318.10.2006         Original published format: US 582673
[2008/32]
Filing languageEN
Procedural languageEN
PublicationType: A2  Application without search report
No.:WO2007050425
Date:03.05.2007
Language:EN
[2007/18]
Type: A2 Application without search report 
No.:EP1951676
Date:06.08.2008
Language:EN
The application has been published by WIPO in one of the EPO official languages on 03.05.2007
[2008/32]
Type: B1 Patent specification 
No.:EP1951676
Date:17.07.2013
Language:EN
[2013/29]
Search report(s)International search report - published on:EP10.01.2008
ClassificationInternational:C07D223/16, C07D401/06, C07D403/06, C07D405/06, C07D409/06, A61K31/538, A61P9/10
[2013/07]
Former International [2008/32]C07D223/16, C07D265/28, C07D267/14, C07D279/10, C07D281/10, C07D401/06, C07D401/12, C07D403/06, C07D405/06, C07D409/06, C07D417/06, A61K31/538, A61P9/10
Designated contracting statesAT,   BE,   BG,   CH,   CY,   CZ,   DE,   DK,   EE,   ES,   FI,   FR,   GB,   GR,   HU,   IE,   IS,   IT,   LI,   LT,   LU,   LV,   MC,   NL,   PL,   PT,   RO,   SE,   SI,   SK,   TR [2008/32]
TitleGerman:N-ACYL-BENZAZEPINDERIVATE ALS LXR-MODULATOREN[2013/07]
English:N-ACYL BENZAZEPINE DERIVATIVES AS LXR MODULATORS[2013/07]
French:DERIVES DE N-ACYLE-BENZAZEPINE COMME MODULATEURS DE LXR[2013/07]
Former [2008/32]LXR-MODULATOREN
Former [2008/32]LXR MODULATORS
Former [2008/32]MODULATEURS DE LXR
Entry into regional phase15.05.2008National basic fee paid 
15.05.2008Designation fee(s) paid 
15.05.2008Examination fee paid 
Examination procedure15.05.2008Amendment by applicant (claims and/or description)
15.05.2008Examination requested  [2008/32]
05.08.2009Despatch of a communication from the examining division (Time limit: M06)
10.02.2010Reply to a communication from the examining division
25.07.2011Despatch of a communication from the examining division (Time limit: M04)
15.11.2011Reply to a communication from the examining division
06.12.2011Despatch of a communication from the examining division (Time limit: M04)
11.04.2012Reply to a communication from the examining division
08.02.2013Communication of intention to grant the patent
07.06.2013Fee for grant paid
07.06.2013Fee for publishing/printing paid
Divisional application(s)EP11006453.2  / EP2392567
The date of the Examining Division's first communication in respect of the earliest application for which a communication has been issued is  05.08.2009
Opposition(s)22.04.2014No opposition filed within time limit [2014/26]
Fees paidRenewal fee
14.10.2008Renewal fee patent year 03
13.10.2009Renewal fee patent year 04
12.10.2010Renewal fee patent year 05
11.10.2011Renewal fee patent year 06
11.10.2012Renewal fee patent year 07
Lapses during opposition  TooltipHU19.10.2006
AT17.07.2013
BE17.07.2013
BG17.07.2013
CY17.07.2013
CZ17.07.2013
DK17.07.2013
EE17.07.2013
FI17.07.2013
IT17.07.2013
LT17.07.2013
LV17.07.2013
MC17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
SK17.07.2013
TR17.07.2013
GR18.10.2013
IE19.10.2013
LU19.10.2013
ES28.10.2013
CH31.10.2013
LI31.10.2013
IS17.11.2013
PT18.11.2013
[2015/34]
Former [2015/32]AT17.07.2013
BE17.07.2013
CY17.07.2013
CZ17.07.2013
DK17.07.2013
EE17.07.2013
FI17.07.2013
IT17.07.2013
LT17.07.2013
LV17.07.2013
MC17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
SK17.07.2013
TR17.07.2013
GR18.10.2013
IE19.10.2013
ES28.10.2013
CH31.10.2013
LI31.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/48]AT17.07.2013
BE17.07.2013
CY17.07.2013
CZ17.07.2013
DK17.07.2013
EE17.07.2013
FI17.07.2013
IT17.07.2013
LT17.07.2013
LV17.07.2013
MC17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
SK17.07.2013
GR18.10.2013
IE19.10.2013
ES28.10.2013
CH31.10.2013
LI31.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/34]AT17.07.2013
BE17.07.2013
CY17.07.2013
CZ17.07.2013
DK17.07.2013
EE17.07.2013
FI17.07.2013
IT17.07.2013
LT17.07.2013
LV17.07.2013
MC17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
SK17.07.2013
GR18.10.2013
ES28.10.2013
CH31.10.2013
LI31.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/25]AT17.07.2013
BE17.07.2013
CY17.07.2013
CZ17.07.2013
DK17.07.2013
EE17.07.2013
FI17.07.2013
IT17.07.2013
LT17.07.2013
LV17.07.2013
MC17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
SK17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/24]AT17.07.2013
BE17.07.2013
CY17.07.2013
CZ17.07.2013
DK17.07.2013
EE17.07.2013
FI17.07.2013
IT17.07.2013
LT17.07.2013
LV17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
SK17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/23]AT17.07.2013
BE17.07.2013
CY17.07.2013
CZ17.07.2013
DK17.07.2013
EE17.07.2013
FI17.07.2013
LT17.07.2013
LV17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
SK17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/22]AT17.07.2013
BE17.07.2013
CY17.07.2013
DK17.07.2013
FI17.07.2013
LT17.07.2013
LV17.07.2013
NL17.07.2013
PL17.07.2013
RO17.07.2013
SE17.07.2013
SI17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/21]AT17.07.2013
BE17.07.2013
CY17.07.2013
DK17.07.2013
FI17.07.2013
LT17.07.2013
LV17.07.2013
NL17.07.2013
PL17.07.2013
SE17.07.2013
SI17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/18]AT17.07.2013
BE17.07.2013
CY17.07.2013
FI17.07.2013
LT17.07.2013
LV17.07.2013
NL17.07.2013
PL17.07.2013
SE17.07.2013
SI17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/14]CY26.06.2013
AT17.07.2013
BE17.07.2013
FI17.07.2013
LT17.07.2013
LV17.07.2013
NL17.07.2013
PL17.07.2013
SE17.07.2013
SI17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/12]CY26.06.2013
AT17.07.2013
BE17.07.2013
FI17.07.2013
LT17.07.2013
LV17.07.2013
PL17.07.2013
SE17.07.2013
SI17.07.2013
GR18.10.2013
ES28.10.2013
IS17.11.2013
PT18.11.2013
Former [2014/11]CY26.06.2013
AT17.07.2013
BE17.07.2013
FI17.07.2013
LT17.07.2013
PL17.07.2013
SE17.07.2013
IS17.11.2013
PT18.11.2013
Former [2014/10]CY26.06.2013
AT17.07.2013
BE17.07.2013
LT17.07.2013
SE17.07.2013
IS17.11.2013
PT18.11.2013
Former [2014/09]AT17.07.2013
BE17.07.2013
LT17.07.2013
SE17.07.2013
PT18.11.2013
Former [2014/08]LT17.07.2013
PT18.11.2013
Cited inInternational search[X]WO0054759  (TULARIK INC [US]) [X] 1-10 * examples 13.3,13.4,18.22-18.27; claims 10-13,40-45,48 *;
 [X]US5141935  (TAKENAKA MITSUAKI [JP], et al) [X] 1-7 * claims 3,10; compound 31 *;
 [X]EP0149974  (CIBA GEIGY AG [CH]) [X] 1-7 * claims 14-24; table 1; compounds 1.47, 1.48 *;
 [X]EP0196570  (UBE INDUSTRIES [JP]) [X] 1-7 * claims 2,3; compounds 3, 8-10, 18-25 *;
 [X]WO8908654  (PFIZER [US]) [X] 1-7 * Formula IV (page 6) and Prep. ex. 1, last compound *;
 [X]EP0272914  (ORTHO PHARMA CORP [US]) [X] 1-7 * example 3; claim 12 *;
 [X]  - SALVADOR A ET AL, "PRELIMINARY STUDIES OF SUPERCRITICAL-FLUID CHROMATOGRAPHY ON POROUS GRAPHITIC CARBON WITH METHYLATED CYCLODEXTRIN AS CHIRAL SELECTOR", CHROMATOGRAPHIA, WIESBADEN, DE, (2001), vol. 53, no. 3/4, ISSN 0009-5893, pages 207 - 209, XP001020347 [X] 1-7 * figure 1 *
 [X]  - SAWADA YOSHIHIRO ET AL, "Synthesis and insecticidal activity of benzoheterocyclic analogues of N'-benzoyl-N-(tert-butyl)benzohydrazide. Part 1. Design of benzoheterocyclic analogues", PEST MANAGEMENT SCIENCE, WILEY & SONS, BOGNOR REGIS, GB, (2003), vol. 59, no. 1, ISSN 1526-498X, pages 25 - 35, XP002421908 [X] 1-7 * page 31, paragraph 2.2.15 *

DOI:   http://dx.doi.org/10.1002/ps.604
 [X]  - ZHOU, YONG-GUI ET AL, "Synthesis and Highly Enantioselective Hydrogenation of Exocyclic Enamides: (Z)-3-Arylidene-4-acetyl-3,4-dihydro-2H-1,4-benzoxazines", JOURNAL OF ORGANIC CHEMISTRY , 70(5), 1679-1683 CODEN: JOCEAH; ISSN: 0022-3263, (20050802), pages 1679 - 1683, XP002445231 [X] 1-7 * table 2; compound 5E *

DOI:   http://dx.doi.org/10.1021/jo048212s
 [X]  - COUDERT, G. ET AL, "A new synthesis of 3,4-dihydro-2H-1,4-benzoxazines using solid-liquid phase-transfer catalysis", SYNTHESIS , (7), 541-3 CODEN: SYNTBF; ISSN: 0039-7881, (1979), pages 541 - 543, XP002445232 [X] 1-7 * table 1; compounds 2F,G *

DOI:   http://dx.doi.org/10.1055/s-1979-28754
Examination US2005101600
  US6495542
  US4107303
  EP0530657
  EP0294647
    - REES A. H., SIMON K.: "Some derivatives of 1-benzazepine", CANADIAN JOURNAL OF CHEMISTRY, vol. 47, 2011, pages 1227-1230,
    - AUGUSTINE R L ET AL: "Synthesis of dl-deethylibogamine", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, EASTON.; US, vol. 34, no. 4, 1 January 1969 (1969-01-01), pages 1070-1075, XP002331119, ISSN: 0022-3263, DOI: DOI:10.1021/JO01256A065

DOI:   http://dx.doi.org/10.1021/jo01256a065
    - HASSNER A ET AL: "Conformation of medium sized ring amines. NMR studies of N-acyl derivatives", TETRAHEDRON LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 18, no. 35, 1 January 1977 (1977-01-01), pages 3023-3026, XP026615036, ISSN: 0040-4039, DOI: DOI:10.1016/S0040-4039(01)83145-2 [retrieved on 1977-01-01]

DOI:   http://dx.doi.org/10.1016/S0040-4039(01)83145-2
by applicantWO0182917
 WO0037077
 US6184215
 US6187814
 WO9832444
 WO0049992
 WO0017334
 WO0103705
 WO0078972
 WO0054759
 US4107303
 WO0040965
 US4231938
 US4444784
 US4739073
 US4346227
 EP0491226
 US5273995
 USRE37314E
 EP0304063
 US5011930
 US3983140
 US4448784
 US4450171
 US4804770
 EP0738510
 EP0363934
 US3234093
 US3485852
 US4097578
 US3847988
 EP0100172
 US6017924
 WO0116108
 WO0116133
 WO0116139
 WO0200617
 WO0216310
 US2002099096
 US2003022868
 WO03011302
 WO03011824
    - EVANS, SCIENCE, (1988), vol. 240, pages 889 - 895,
    - GLASS, ENDOCR. REV., (1994), vol. 15, pages 391 - 407,
    - LEVIN ET AL., NATURE, (1992), vol. 355, pages 359 - 361,
    - HEYMAN ET AL., CELL, (1992), vol. 68, pages 397 - 406,
    - MANGELSDORF ET AL., CELL, (1995), vol. 83, pages 841 - 850,
    - CHIANG ET AL., J. BIOL. CHEM., (2000), vol. 275, pages 10918 - 10924,
    - URIZAR ET AL., J. BIOL. CHEM., (2000), vol. 275, pages 39313 - 39317,
    - GILBERT, EVERETT E. ET AL., J ORG. CHEM., (1965), vol. 30, no. 4, pages 1001 - 3,
    - DYKER; MARKWITZ, SYNTHESIS, (1998), vol. 12, pages 1750 - 1754,
    - FUKUYAMA, TETRAHEDRON LETT., (1985), vol. 26, page 6291,
    - PETITOU, TETRAHEDRON LETT., (1988), vol. 29, page 1398,
    - ORG REACTIONS, (1965), vol. 14, pages 1 - 15,
    - CORBET; MIGNANI, CHEMICAL REVIEWS, (2006), vol. 106, no. 7, pages 2651 - 2710,
    - BELLINA, SYNTHESIS, (2004), pages 2419 - 2440,
    - METH. ENZYMOL, (1981), vol. 71, pages 455 - 509,
    - TUCKER; CHESTERTON, J. MED. CHEM., (1988), vol. 31, pages 885 - 887,
    - HOFBAUER ET AL., J. BONE MINER. RES., (1999), vol. 14, pages 1330 - 1337,