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1. (WO1994012494) USE OF DIMETHYLBENZOFURANS AND DIMETHYLBENZOPYRANS AS 5-HT¿3? ANTAGONISTS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/1994/012494 International Application No.: PCT/EP1993/003206
Publication Date: 09.06.1994 International Filing Date: 15.11.1993
Chapter 2 Demand Filed: 03.06.1994
IPC:
A61K 31/505 (2006.01) ,A61K 31/506 (2006.01) ,C07D 211/58 (2006.01) ,C07D 401/12 (2006.01) ,C07D 405/14 (2006.01)
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06
having no double bonds between ring members or between ring members and non-ring members
36
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56
Nitrogen atoms
58
attached in position 4
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
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14
containing three or more hetero rings
Applicants:
VAN DAELE, Georges, Henri, Paul [BE/BE]; BE (UsOnly)
BOSMANS, Jean-Paul, René, Marie, André [BE/BE]; BE (UsOnly)
VAN LAERHOVEN, Willy, Joannes, Carolus [BE/BE]; BE (UsOnly)
JANSSEN PHARMACEUTICA N.V. [BE/BE]; Turnhoutseweg 30 B-2340 Beerse, BE (AllExceptUS)
Inventors:
VAN DAELE, Georges, Henri, Paul; BE
BOSMANS, Jean-Paul, René, Marie, André; BE
VAN LAERHOVEN, Willy, Joannes, Carolus; BE
Agent:
QUAGHEBEUR, Luc; Janssen Pharmaceutica N.V. Patent Dept. Turnhoutseweg 30 B-2340 Beerse, BE
Priority Data:
979,01320.11.1992US
Title (EN) USE OF DIMETHYLBENZOFURANS AND DIMETHYLBENZOPYRANS AS 5-HT3 ANTAGONISTS
(FR) UTILISATION DE DIMETHYLBENZOFURANNES ET DE DIEMTHYLBENZOPYRANNES COMME ANTAGONISTES DE LA 5-HT3
Abstract:
(EN) Method of treating 5-HT3-mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I), the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R1 and R2 represent hydrogen, or R1 and R2 taken together form a bivalent radical of formula (a): -CH = CH-CH = CH-, (b): -CH = C(Cl)-CH = CH- or (c): -CH = CH-C(Cl) = CH-; n represents 2, 3 or 4; R3 represents hydrogen or methoxy; m represents 1 or 2; R4 represents hydrogen, amino or C1-3-alkylcarbonylamino; and R5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.
(FR) L'invention concerne le traitement de troubles liés à la 5-HT3, consistant à administrer par la voie générale une dose efficace d'un composé de la formule (I), un sel d'addition d'acide de ce composé acceptable sur le plan pharmaceutique, ou encore une de ses formes stéréochimiquement isomères. Dans cette formule, R1 et R2 représentent l'hydrogène, ou R1 et R2 pris ensemble forment un radical bivalent de la formule (a): -CH = CH-CH = CH-, (b): -CH = C(Cl)-CH = CH- ou (c): -CH = CH-C(Cl) = CH-; n représente 2, 3 ou 4; R3 représente un hydrogène ou un méthoxy; m représente 1 ou 2; R4 représente un hydrogène, un amino ou un alkylcarbonylamino C1-3; et R5 représente un hydrogène ou un halo. L'invention concerne également de nouveaux composés des compositions les contenant et des procédés pour la préparation de ces composés et de leurs intermédiaires.
Designated States: AU, BB, BG, BR, CA, CZ, FI, HU, JP, KP, KR, LK, LV, MG, MN, MW, NO, NZ, PL, RO, RU, SD, SK, UA, US
European Patent Office (EPO) (AT, BE, CH, DE, DK, ES, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)