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1. (WO2008101995) INDOLE DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2008/101995 International Application No.: PCT/EP2008/052141
Publication Date: 28.08.2008 International Filing Date: 21.02.2008
IPC:
C07D 413/04 (2006.01) ,C07D 417/04 (2006.01) ,A61K 31/425 (2006.01) ,A61K 31/433 (2006.01) ,A61K 31/4245 (2006.01) ,A61P 29/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425
Thiazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
433
Thiadiazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4245
Oxadiazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
Applicants:
ADAM, Julia [GB/GB]; GB (UsOnly)
N.V. ORGANON [NL/NL]; Kloosterstraat 6 NL-5349 AB Oss, NL (AllExceptUS)
Inventors:
ADAM, Julia; GB
Agent:
VAN WEZENBEEK, P.M.G.F. ; P.O. Box 20 NL-5340 BH Oss, NL
Priority Data:
07102870.822.02.2007EP
Title (EN) INDOLE DERIVATIVES
(FR) DÉRIVÉS D'INDOLE
Abstract:
(EN) The invention relates to indole derivative having the general Formula (I) wherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH;Y represents CH2, O, S or SO2;R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN orhalogen;R2, R2 ', R3, R3 ', R4,R4 ', R5 and R5 ' are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO-OR8; orone pair of geminal substituents R3 and R3 ' or R5 and R5 ' together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2and R5 together represent a methylene or an ethylene bridge, and R2 '2, R3, R3 ', R4, R4 ' and R5 ' are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH, (C1-4)alkyloxy, CO-NR9R10, CO-OR11or 1,2,4-oxadiazol-3-yl), SO2NR12R13or COOR14; R7 is H or halogen; R 8 is (C1-4)alkyl; R9and R10are independently hydrogen, (C1-4)alkyl or (C 3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11is H or (C1-4)alkyl; R12 and R13 are independently H or (C1-4)alkyl; R14is (C1-6)alkyl; or a pharmaceutically acceptable salt thereof,as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
(FR) L'invention concerne des dérivés d'indole de formule générale (I) où A représente un anneau hétérocyclique aromatique à cinq chaînons, où X1, X2 et X3 sont indépendamment sélectionnés parmi N, O, S et CH; Y représente CH2, O, S ou SO2;R1 désigne H, (C1-4)-alkyle, (C1-4)alkyloxy, CN orhalogène; R2, R2 ', R3, R3 ', R4,R4 ', R5 et R5 ' représentent indépendamment hydrogène, (C1-4)alkyle (éventuellement substitué avec OH) ou CO-OR8; ou une paire de substituants germinaux R3 et R3 ' ou R5 et R5 ' représentent ensemble un groupe céto; et les autres représentent tous hydrogène ou (C1-4)alkyle; ou R2 et R5 représentent ensemble un méthylène ou un pont éthylène, et R2 '2, R3, R3 ', R4, R4 ' et R5 ' désignent hydrogène: n est égal à 1 ou à 2; R6 représente H, (C1-4)alkyle (éventuellement substitué avec OH, (C1-4)alkyloxy, CO-NR9R10, CO-OR11ou 1,2,4-oxadiazol-3-yl), SO2NR12R13or COOR14; R7 désigne H ou halogène; R 8 désigne (C1-4)alkyle; ou un de ses sels pharmaceutiquement acceptable; comme agonistes du récepteur CB1 des cannabinoïdes, qui peuvent être utilisés dans le traitement de la douleur, telle que la douleur péri-opératoire, la douleur chronique, la douleur névropathique, la douleur liée au cancer ainsi que la douleur et l'hypertonie spastique associées à la sclérose en plaques.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MT, NL, NO, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)