Title (en)

(Z)-2-CYANO-3-HYDROXY-BUT-2-ENOIC ACID-(4'-TRIFLUORMETHYLPHENYL)-AMIDE TABLET FORMULATIONS WITH IMPROVED

STABILITY

Title (de)
(Z)-2-CYANO-3-HYDROXY-BUT-2-ENOLSÄURE-(4'- TRIFLUORMETHYLPHENYL)-AMIDTABLETTENFORMULIERUNGEN MIT
VERBESSERTER STABILITÄT

Title (fr)
FORMULATIONS DE COMPRIMÉS D'ACIDE (Z)-2-CYANO-3-HYDROXY-BUT-2-ÉNOÏQUE-(4'-TRIFLUORMÉTHYLPHÉNYL)-AMIDE À STABILITÉ
AMÉLIORÉE

Publication
EP 2477611 B1 20170405 (EN)

Application
EP 10752585 A 20100914

Priority
  • EP 09290716 A 20090918
  • US 36338210 P 20100712
  • EP 2010063439 W 20100914
  • EP 10752585 A 20100914

Abstract (en)
[origin: WO2011032929A1] The invention relates to solid pharmaceutical compositions comprising (Z)-2- cyano-3-hydroxy-but-2-enoic acid-(4'-
trifluoromethylphenyl)-amide, as well as a process for the preparation of the same, methods of using such compositions to treat subjects suffering
from autoimmune diseases in particular systemic lupus erythematosus or chronic graft-versus-host disease, multiple sclerosis or rheumatoid arthritis.

IPC 8 full level (invention and additional information)

A61K 9/20  (2006.01); A61K 31/277  (2006.01)

CPC (invention and additional information)

C07C 255/44 (2013.01); A61K 9/2013 (2013.01); A61K 9/2054 (2013.01); A61K 9/2059 (2013.01); A61K 31/277 (2013.01)

Citation (examination)
AULTON M E (ED) ED - AULTON M E (ED) 2: "PHARMACEUTICS - THE SCIENCE OF DOSAGE FORM DESIGN , PASSAGE",
1 January 2002, PHARMACEUTICS : THE SCIENCE OF DOSAGE FORM DESIGN, LONDON : CHURCHILL LIVINGSTONE, GB,
PAGE(S) 404 - 410, ISBN: 978-0-443-05517-1, XP002396921

Citation (opposition)
Opponent : Wuesthoff & Wuesthoff Patentanwälte PartG mbB
  • US 2006024376 A1 20060202 - AVENTIS PHARMA LTD [JP]
  • EP 0787491 B1 20000726 - AVENTIS PHARMA INC [US]
  • EP 1381356 B1 20080528 - WILLIAMS JAMES W [US]
  • EP 1810676 B1 20081112 - AVENTIS PHARMA INC [US]
  • GB 2394660 A 20040505 - TIEFENBACHER PHARMACHEMIKALIEN [DE], et al
  • AUGSBURGER L.L. ET AL.: "Encyclopedia of Pharmaceutical Technology", 2007, article "Tablet formulation",
pages: 3641 - 3652, XP055449019
  • ARMSTRONG N.A.: "Encyclopedia of Pharmaceutical Technology", 2007, article "Tablet manufacture", pages:
3653 - 3672, XP055449024
Opponent : Dr Richard Cooke
  • US 2006024376 A1 20060202 - BARTLETT ROBERT R [DE], et al
  • EP 1381356 B1 20080528 - WILLIAMS JAMES W [US]
  • WO 2007118684 A1 20071025 - WIEBELITZ ULRIKE [DE]
  • US 4965276 A 19901023 - BARTLETT ROBERT R [DE], et al
  • ROWE ET AL.: "HANDBOOK OF PHARMACEUTICAL EXCIPIENTS", ISBN: 9781582120584, article
"COLLOIDAL SILICON DIOXIDE", pages: 188 - 190, XP003016902
  • FUJITA ET AL.: "Generation of formaldehyde by pharmaceutical excipients and its absorption by meglumine",
CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 57, no. 10, 28 July 2009 (2009-07-28), pages 1096 - 1099,
XP002566576
  • "PHARMACEUTICS - THE SCIENCE OF DOSAGE FORM DESIGN - Tablet Excipients", 2002, ISBN:
978-0-443-05517-1, pages: 404 - 410, XP002396921
  • AINLEY WADE ET AL: "The Handbook of Pharmaceutical Excipients", 1994, London, ISBN: 0853693056,
article "Starch", pages: 483 - 487, XP055452123
  • ALFONSO R GENNARO: "Remington: The Science and Practice of Pharmacy", 2000, ISBN: 0683306472,
article "Oral Solid Dosage Forms", pages: 861, 1047 - 1048, XP055452127
  • HERBERT A. LIEBERMANN ET AL: "Pharmaceutical Dosage Forms: Tablets", vol. 1, 1989, ISBN:
0824780442, article "Tablet Formulation and Design", pages: 105 - 109, XP055452132
  • WALTER LUND ET AL: "The Pharmaceutical Codex", 1994, ISBN: 0853692904, article "Oral Solids", pages: 6
- 9, XP055318927
  • PATRICK CRAWLEY: "Drug-excipient interactions", PHARMACEUTICAL TECHNOLOGY, March 2001
(2001-03-01), XP055452143
Opponent : Pentafarma, Sociedade Tecnico Medicinal S.A.
  • US 2006024376 A1 20060202 - WILLIAMS JAMES W [US]
  • EP 1990048 A2 20081112 - WIEBELITZ ULRIKE [DE]
  • WO 0160363 A1 20010823 - TEVA PHARMA [IL], et al
  • US 6221891 B1 20010424 - FAASCH HOLGER [DE], et al
  • O'CONNOR ET AL.: "A Phase II study of the safety and efficacy of teriflunomide in multiple sclerosis with
relapses.", NEUROLOGY, vol. 66, 2006, pages 894 - 900, XP002556504
  • KIBBE: "Handbook of pharmaceutical excipients", 2000

Designated contracting state (EPC)

AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK SM TR

Designated extension state (EPC)

BA ME RS

DOCDB simple family

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B2 20150917; BR 112012006184 A2 20160531; CA 2772275 A1 20110324; CL 2015000047 A1 20150612; CN 102596184 A 20120718; CN
102596184 B 20150311; CN 104666238 A 20150603; CN 104666238 B 20180406; CN 104666272 A 20150603; CN 104739821 A 20150701;
CN 104739821 B 20180406; CO 6511244 A2 20120831; CR 20120116 A 20120615; CR 20170078 A 20170522; CY 1119364 T1 20180214; DK
2477611 T3 20170710; DO P2012000070 A 20120531; EP 2477611 A1 20120725; EP 2477611 B1 20170405; ES 2625731 T3 20170720; GT
201200075 A 20140514; HK 1206244 A1 20160108; HK 1206245 A1 20160108; HN 2012000576 A 20150126; HR P20170904 T1 20170908; HU
E032963 T2 20171128; IL 218492 A 20160421; IL 218492 D0 20120430; IL 244809 D0 20160421; JP 2013505213 A 20130214; KR 101547880
B1 20150827; KR 20120089461 A 20120810; LT 2477611 T 20170626; MA 33585 B1 20120901; ME 02765 B 20180120; MX 2012003122 A
20120410; MX 336663 B 20160127; MY 155613 A 20151113; NZ 598744 A 20131129; NZ 617025 A 20140328; PE 14782012 A1 20121112;
PE 20312015 A1 20160114; PL 2477611 T3 20170929; PT 2477611 T 20170605; RS 56074 B1 20171031; RU 2012115459 A 20131027; RU
2015151938 A3 20190115; RU 2015151938 A 20190115; RU 2681079 C2 20190304; SI 2477611 T1 20170731; TN 2012000061 A1 20130919;
TW 201117838 A 20110601; TW 201517935 A 20150516; TW I468190 B 20150111; TW I522130 B 20160221; UA 107582 C2 20150126;
UA 115979 C2 20180125; US 2012172427 A1 20120705; US 2012208880 A1 20120816; US 2014235888 A1 20140821; US 2017247319 A1
20170831; US 8802735 B2 20140812; UY 32889 A 20110429