ACTIVATORS OF CLASS I HISTONE DEACETYLASES (HDACS) AND USES THEREOF

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EP 2 734 510 B8

(12)	CORRECTED EUROPEAN PATENT SPECIFICATION
	Note: Bibliography reflects the latest situation

(15)	Correction information:
	Corrected version no 1 (W1 B1)

(48)	Corrigendum issued on:
	29.05.2019 Bulletin 2019/22

(45)	Mention of the grant of the patent:
	07.11.2018 Bulletin 2018/45

(21)	Application number: 12766735.0

(22)	Date of filing: 20.07.2012

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International Patent Classification (IPC):

C07D 307/40^(2006.01)
C07D 411/12^(2006.01)
C07C 217/54^(2006.01)
A61P 25/28^(2006.01)

C07D 405/12^(2006.01)
C07D 487/04^(2006.01)
A61K 31/55^(2006.01)

(86)	International application number:
	PCT/US2012/047609

(87)	International publication number:
	WO 2013/016193 (31.01.2013 Gazette 2013/05)

(54)	ACTIVATORS OF CLASS I HISTONE DEACETYLASES (HDACS) AND USES THEREOF AKTIVATOREN DER KLASSE I HISTON-DEACETLYASEN (HDACS) UND VERWENDUNGEN DAVON ACTIVATEURS D'HISTONE DÉSACÉTYLASES DE CLASSE I (HDAC) ET UTILISATIONS DE CEUX-CI

(84)	Designated Contracting States:
	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 RS SE SI SK SM TR

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Priority:

22.07.2011 US 201161510885 P

(43)	Date of publication of application:
	28.05.2014 Bulletin 2014/22

(60)	Divisional application:
	18196929.6 / 3483150

(73)	Proprietors:
	Massachusetts Institute of Technology Cambridge, MA 02139 (US) The General Hospital Corporation d/b/a Massachusetts General Hospital Boston, MA 02114 (US)

(72)	Inventors:
	TSAI, Li-Huei Cambridge, MA 02138 (US) PAN, Ling Charlestown, MA 02129 (US) HAGGARTY, Stephen, J. Dorchester, MA 02125 (US) PATNAIK, Debasis Quincy, MA 02171 (US)

(74)	Representative: Cornish, Kristina Victoria Joy et al
	Kilburn & Strode LLP Lacon London 84 Theobalds Road London WC1X 8NL London WC1X 8NL (GB)

(56)

References cited: :

EP-A2- 0 263 438
WO-A1-2010/044342
WO-A1-2010/114116
JP-A- 2000 229 972
JP-A- 2010 215 759
JP-A- 2010 267 847
US-A- 4 617 316

WO-A1-2010/044342
WO-A1-2010/114116
WO-A2-2010/011318
JP-A- 2000 229 972
JP-A- 2010 215 759
JP-A- 2010 267 847

WEIXIAO BAO ET AL: "Carbazole nematic liquid crystals", LIQUID CRYSTALS: AN INTERNATIONAL JOURNAL OF SCIENCE AND TECHNOLOGY, TAYLOR & FRANCIS, GB, vol. 37, no. 10, 1 October 2010 (2010-10-01), pages 1289-1303, XP001558136, ISSN: 0267-8292, DOI: 10.1080/02678292.2010.504862
KATHARINE GERAMITA ET AL: "2,7-Substituted Hexafluoroheterofluorenes as Potential Building Blocks for Electron Transporting Materials", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 74, no. 2, 16 January 2009 (2009-01-16), pages 820-829, XP055189883, ISSN: 0022-3263, DOI: 10.1021/jo802171t
PENG GAO ET AL: "Conjugated Ladder-Type Heteroacenes Bearing Pyrrole and Thiophene Ring Units: Facile Synthesis and Characterization", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 73, no. 23, 5 December 2008 (2008-12-05), pages 9207-9213, XP055188442, ISSN: 0022-3263, DOI: 10.1021/jo801898g
PRASAD APPUKKUTTAN ET AL: "Microwave-Enhanced Cadogan Cyclization: An Easy Access to the 2-Substituted Carbazoles and other Fused Heterocyclic Systems", SYNLETT, no. 1, 1 January 2005 (2005-01-01), pages 127-133, XP055200196, ISSN: 0936-5214, DOI: 10.1055/s-2004-836030
QINHUA HUANG ET AL: "Synthesis of Substituted Naphthalenes and Carbazoles by the Palladium-Catalyzed Annulation of Internal Alkynes", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 68, no. 19, 1 September 2003 (2003-09-01), pages 7342-7349, XP055200198, ISSN: 0022-3263, DOI: 10.1021/jo034449x
KUMAR U K S ET AL: "Benzoannelation of 2-methylindole via 1-N-Carboxy-2-methylindole Dianion: A Direct Regiospecific Route to Substituted and Annelated Carbazoles", TETRAHEDRON LETTERS, PERGAMON, GB, vol. 39, no. 14, 2 April 1998 (1998-04-02) , pages 2029-2032, XP004109614, ISSN: 0040-4039, DOI: 10.1016/S0040-4039(98)00164-6
ALAN R. KATRITZKY ET AL: "Efficient Syntheses of Substituted Carbazoles and Cyclopent[ b ]indoles from 1-Methyl-3-(benzotriazol-1-ylmethyl)indole ", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 61, no. 21, 1 January 1996 (1996-01-01), pages 7558-7563, XP055200201, ISSN: 0022-3263, DOI: 10.1021/jo9604954
P. VAN DOREN ET AL: "Diels-alder reactions of pyrano[3,4-b]indol-3-ones with olefinic compounds : Synthesis of (1,2-dihydro)carbazoles", TETRAHEDRON, vol. 45, no. 21, 1 January 1989 (1989-01-01), pages 6761-6770, XP055200202, ISSN: 0040-4020, DOI: 10.1016/S0040-4020(01)89146-8
KEUMI, TAKAHASHI ET AL: "Studies on dibenzofuran and its derivatives. XXVIII. Electrophilic substitutions of 2,8-dimethoxy- and 2,8-diethyldibenzfurane", NIPPON KAGAKU KAISHI, vol. 1, 1987, pages 35-39, XP002741905,
KEUMI, TAKASHI ET AL: "Derivatives of dibenzofuran. XVIII. Orientation in the Friedel-Crafts benzoylation of 2- and 3-methyldibenzofurans", NIPPON KAGAKU KAISHI, vol. 9, 1974, pages 1708-1711, XP002741906,
WIRTH H O ET AL: "SYNTHESE UND EIGENSCHAFTEN VON OXYDO-P-OLIGOPHENYLENEN 18. MITTEILUNG UEBER POLY- UND OLIGOPHENYLENE", MAKROMOLEKULARE CHEMIE, MACROMOLECULAR CHEMISTRY AND PHYSICS, WILEY - V C H VERLAG GMBH & CO. KGAA, vol. 86, no. 16, 1 January 1965 (1965-01-01), pages 139-167, XP009012341, ISSN: 0025-116X, DOI: 10.1002/MACP.1965.020860115
WEIXIAO BAO ET AL: "Carbazole nematic liquid crystals", LIQUID CRYSTALS: AN INTERNATIONAL JOURNAL OF SCIENCE AND TECHNOLOGY, TAYLOR & FRANCIS, GB, vol. 37, no. 10, 1 October 2010 (2010-10-01), pages 1289-1303, XP001558136, ISSN: 0267-8292, DOI: 10.1080/02678292.2010.504862
KATHARINE GERAMITA ET AL: "2,7-Substituted Hexafluoroheterofluorenes as Potential Building Blocks for Electron Transporting Materials", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 74, no. 2, 16 January 2009 (2009-01-16), pages 820-829, XP055189883, ISSN: 0022-3263, DOI: 10.1021/jo802171t
PENG GAO ET AL: "Conjugated Ladder-Type Heteroacenes Bearing Pyrrole and Thiophene Ring Units: Facile Synthesis and Characterization", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 73, no. 23, 5 December 2008 (2008-12-05), pages 9207-9213, XP055188442, ISSN: 0022-3263, DOI: 10.1021/jo801898g
PRASAD APPUKKUTTAN ET AL: "Microwave-Enhanced Cadogan Cyclization: An Easy Access to the 2-Substituted Carbazoles and other Fused Heterocyclic Systems", SYNLETT, no. 1, 1 January 2005 (2005-01-01), pages 127-133, XP055200196, ISSN: 0936-5214, DOI: 10.1055/s-2004-836030
QINHUA HUANG ET AL: "Synthesis of Substituted Naphthalenes and Carbazoles by the Palladium-Catalyzed Annulation of Internal Alkynes", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 68, no. 19, 1 September 2003 (2003-09-01), pages 7342-7349, XP055200198, ISSN: 0022-3263, DOI: 10.1021/jo034449x
KUMAR U K S ET AL: "Benzoannelation of 2-methylindole via 1-N-Carboxy-2-methylindole Dianion: A Direct Regiospecific Route to Substituted and Annelated Carbazoles", TETRAHEDRON LETTERS, PERGAMON, GB, vol. 39, no. 14, 2 April 1998 (1998-04-02) , pages 2029-2032, XP004109614, ISSN: 0040-4039, DOI: 10.1016/S0040-4039(98)00164-6
ALAN R. KATRITZKY ET AL: "Efficient Syntheses of Substituted Carbazoles and Cyclopent[ b ]indoles from 1-Methyl-3-(benzotriazol-1-ylmethyl)indole ", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 61, no. 21, 1 January 1996 (1996-01-01), pages 7558-7563, XP055200201, ISSN: 0022-3263, DOI: 10.1021/jo9604954
P. VAN DOREN ET AL: "Diels-alder reactions of pyrano[3,4-b]indol-3-ones with olefinic compounds : Synthesis of (1,2-dihydro)carbazoles", TETRAHEDRON, vol. 45, no. 21, 1 January 1989 (1989-01-01), pages 6761-6770, XP055200202, ISSN: 0040-4020, DOI: 10.1016/S0040-4020(01)89146-8
KEUMI, TAKAHASHI ET AL: "Studies on dibenzofuran and its derivatives. XXVIII. Electrophilic substitutions of 2,8-dimethoxy- and 2,8-diethyldibenzfurane", NIPPON KAGAKU KAISHI, vol. 1, 1987, pages 35-39, XP002741905,
KEUMI, TAKASHI ET AL: "Derivatives of dibenzofuran. XVIII. Orientation in the Friedel-Crafts benzoylation of 2- and 3-methyldibenzofurans", NIPPON KAGAKU KAISHI, vol. 9, 1974, pages 1708-1711, XP002741906,
WIRTH H O ET AL: "SYNTHESE UND EIGENSCHAFTEN VON OXYDO-P-OLIGOPHENYLENEN 18. MITTEILUNG UEBER POLY- UND OLIGOPHENYLENE", MAKROMOLEKULARE CHEMIE, MACROMOLECULAR CHEMISTRY AND PHYSICS, WILEY - V C H VERLAG GMBH & CO. KGAA, vol. 86, no. 16, 1 January 1965 (1965-01-01), pages 139-167, XP009012341, ISSN: 0025-116X, DOI: 10.1002/MACP.1965.020860115

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