AZEPINOINDOLE AND PYRIDOINDOLE DERIVATIVES AS PHARMACEUTICAL AGENTS

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EP 1 532 153 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:
	11.04.2012 Bulletin 2012/15

(45)	Mention of the grant of the patent:
	29.02.2012 Bulletin 2012/09

(21)	Application number: 03755523.2

(22)	Date of filing: 27.05.2003

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International Patent Classification (IPC):

C07D 487/04^(2006.01)
A61K 31/435^(2006.01)
A61P 31/10^(2006.01)
C07D 487/04^(2006.01)
C07D 209/00^(2006.01)
C07D 221/00^(2006.01)

C07D 471/04^(2006.01)
A61P 31/04^(2006.01)
A61K 31/55^(2006.01)
C07D 223/00^(2006.01)
C07D 471/04^(2006.01)
C07D 209/00^(2006.01)

(86)	International application number:
	PCT/US2003/016767

(87)	International publication number:
	WO 2003/099821 (04.12.2003 Gazette 2003/49)

(54)	AZEPINOINDOLE AND PYRIDOINDOLE DERIVATIVES AS PHARMACEUTICAL AGENTS AZEPINOINDOL UND PYRIDOINDOLDERIVATE ALS PHARMAZEUTISCHE MITTEL DERIVES D'AZEPINOINDOLE ET DE PYRIDOINDOLE UTILISES COMME AGENTS PHARMACEUTIQUES

(84)	Designated Contracting States:
	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

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Priority:

24.05.2002 US 383574 P

(43)	Date of publication of application:
	25.05.2005 Bulletin 2005/21

(73)	Proprietor: Exelixis, Inc.
	South San Francisco, CA 94083-0511 (US)

(72)	Inventors:
	MARTIN, Richard San Diego, CA 92130 (US) WANG, Tie-Lin San Diego, CA 92129 (US) FLATT, Brenton, Todd Poway, CA 92064 (US) GU, Xiao-Hui 3408 San Diego,CA 92122-5098 (US) GRIFFITH, Ronald Escondido, CA 92029 (US)

(74)	Representative: Grünecker, Kinkeldey, Stockmair & Schwanhäusser
	Anwaltssozietät Leopoldstrasse 4 80802 München 80802 München (DE)

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References cited: :

EP-A- 0 064 317
CH-A- 506 543

WO-A-01/05793

COSTA G ET A L: "Nouvelle voie d'accès à la série de l'hexahydroazépino[4,5-b]indole. Réarrangement de l'hexahydroindolo[2,3-a]quinolizine par action de BrCN" TETRAHEDRON, vol. 33, 1977, pages 315-320, XP009016240 GB
WANG TST: "Fisher indole synthesis, the syntesis of 1-acetyl-6:7-dihydro-2:3-benzindolo[2:3-4: 5]azepine" TETRAHEDRON LETTERS, vol. 19, 1975, pages 1637-1638, XP009016257 GB
WALSER A ET AL: "NUCLEOPHILIC DISPLACEMENT OF AROMATIC FLUORINE, INDOLOQUINOLINES AND BENZOFURANOQUINOLINES" JOURNAL OF HETEROCYCLIC CHEMISTRY, HETEROCORPORATION. PROVO, US, vol. 12, no. 2, 1 April 1975 (1975-04-01), pages 351-358, XP000562087 ISSN: 0022-152X
KOH H L ET AL: "CONFORMATIONAL AND STRUCTURAL FEATURES DETERMINING IN VITRO ANTIMALARIAL ACTIVITY IN SOME INDOLO[3,2-c]QUINOLINES, ANILINOQUINOLINES AND TETRAHYDROINDOLO[3,2-d]BENZAZEPINES" EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, EDITIONS SCIENTIFIQUE ELSEVIER, PARIS, FR, vol. 29, no. 2, 1994, pages 107-113, XP001064275 ISSN: 0223-5234
KUEHNE ME ET AL: "Biomimetic synthesis of indole alkaloids. 11. Synthesis of b-carboline and indoloazepine intermediates" THE JOURNAL OF ORGANIC CHEMISTRY, vol. 50, no. 7, 1985, page 919-924 XP002252365 USA
MACPHILLAMY HB ET AL: "The alkaloids of tabernanthe iboga. Part VI. The synthesis of the selenium dehydrogenation products from ibogamine" JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 80, 1958, pages 2172-2178, XP002252366 USA
BARAN PS ET AL: "a short synthetic route to (+)-austamide, (+)-deoxyisoaustamide, and (+)-hydrotoaustamide from a common precursor by a novel palladium-mediated indole dihydroindoloazocine cyclization" JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 124, no. 27, 2002, pages 7904-7905, XP002252367 USA

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