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1. (WO1998052943) INDOLINE DERIVATIVES AS 5HT¿2C? RECEPTOR ANTAGONISTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/052943 International Application No.: PCT/EP1998/002992
Publication Date: 26.11.1998 International Filing Date: 13.05.1998
Chapter 2 Demand Filed: 25.11.1998
IPC:
C07D 401/12 (2006.01) ,C07D 401/14 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14
containing three or more hetero rings
Applicants:
SMITHKLINE BEECHAM PLC [GB/GB]; New Horizons Court Brentford Middlesex TW8 9EP, GB (AllExceptUS)
BROMIDGE, Steven, Mark [GB/GB]; GB (UsOnly)
Inventors:
BROMIDGE, Steven, Mark; GB
Agent:
WATERS, David, Martin; SmithKline Beecham Corporate Intellectual Property Two New Horizons Court Brentford Middlesex TW8 9EP, GB
GIDDINGS, Peter, John; SmithKline Beecham Corporate Intellectual Property Two New Horizons Court Brentford Middlesex TW8 9EP, GB
Priority Data:
9710523.323.05.1997GB
Title (EN) INDOLINE DERIVATIVES AS 5HT2C RECEPTOR ANTAGONISTS
(FR) DERIVES D'INDOLINE COMME ANTAGONISTES DU RECEPTEUR 5HT2C
Abstract:
(EN) A compound of formula (I) or a salt thereof, wherein: R1 is hydrogen or C1-6alkyl; R2, R3 and R4 groups are independently hydrogen, halogen or C1-6alkyl optionally substituted by one or more fluorine atoms. R5 and R6 groups are independently hydrogen or C1-6alkyl; X and Y are independently CH or nitrogen, provided that X is nitrogen when Y is nitrogen and both R5 and R6 are hydrogen. The compounds exhibit enhanced 5HT2C receptor antagonist activity profile. 5HT2C receptor antagonists are believed to be of potential use in the treatment of CNS disorders such as anxiety, depression, epilepsy, obsessive compulsive disorders, migraine, Alzheimer's disease, sleep disorders, feeding disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia, and also disorders associated with spinal trauma and/or head injury such as hydrocephalus. Compounds of the invention are also expected to be of use in the treatment of glaucoma, certain GI (gastrointestinal) disorders such as IBS (Irritable Bowel Syndrome) as well as microvascular diseases such as macular oedema and retinopathy.
(FR) L'invention concerne un composé présentant la formule (I) ou un sel de ce dernier. Dans la formule, R1 est de l'hydrogène ou alkyle C1-6; les groupes R2, R3 et R4 sont indépendamment de l'hydrogène, halogène, ou alkyle C1-6 éventuellement substitué par un ou plusieurs atomes de fluor.Les groupes R5 et R6 sont indépendamment de l'hydrogène ou alkyle C1-6. X et Y sont indépendamment CH ou azote, à condition que X représente de l'azote lorsque Y est de l'azote et R5 et R6 sont tous deux de l'hydrogène. Les composés présentent un effet antagoniste du récepteur 5HT2C amélioré. Ces antagonistes du récepteur 5HT2C présentent une utilité potentielle pour traiter les troubles du SNC tels que l'anxiété, la dépression, l'épilepsie, les troubles obssessivo-compulsifs, la migraine, la maladie d'Alzheimer, les troubles du sommeil, les troubles de l'alimentation tels que l'anorexie et la boulimie, les attaques de panique, le sevrage lors de l'abus de drogues telles que la cocaïne, l'éthanol, la nicotine et les benzodiazépines, la schizophrénie, et également des troubles associés à un trauma de la colonne vertébrale et/ou une blessure de la tête comme l'hydrocéphalie. Les composés selon l'invention peuvent permettre également de traiter le glaucome, certains troubles gastro-intestinaux comme le syndrome du côlon irritable ainsi que les maladies microvasculaires comme l'oedème maculaire et la rétinopathie.
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Designated States: CA, JP, US
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0984956JP2001526674 CA2290475