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filingDate 2000-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_53eea07040e8455bbbf6e6e5ce0a4c24
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publicationDate 2000-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber NO-20001937-L
titleOfInvention 2-substituted 1,2-benzisothiazole derivatives and their use as serotonin antagonists (5-HT1A, 5-HT1B and 5-HT1D)
abstract The invention relates to 2-substituted 1,2-benzoisothiazole derivatives of formula I A¿B¿Ar wherein R 1 and R 2 are, independently, (C 1 e) alkyl, R 3, R 4 are independently hydrogen, branched or straight chain ( C 1-6 alkyl, OH, branched or straight chain O- (C 1- 5) alkyl, F, Cl, Br, 1, trifluoromethyl, NR 5 R 6, CO 2 R 7, nitro, cyano, pyrrolyl, a phenylalkyl C may be substituted on the aromatic system by F, Cl, Br, 1, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, trifluoromeryl, hydroxyl, amino, cyano or nitro, R 5 and R 6 are, independently, hydrogen, branched or straight-chain (C1-6) alkyl, COPh, CO2tBu, CO- (C1-6 alkyl or together is a 5- or 6-membered ring which may contain a second nitrogen (e.g. piperazine), R7 is hydrogen and (branched or straight chain C1-12) alkyl, A is branched or straight chain (C1-10) alkyl or straight chain or branched (C2-10) alkyl, comprising at least one group Z selected from O, S, NR7, cyclopropyl, CHOH, a double or a triple bond, B is 1,4-piperidinylene, 1,2,3,6-tetrahydro-1,4-pyridinylene, 1,4-piperazinylene and the corresponding cyclic compounds extended by a methylene group, the bond to A being through a nitrogen atom in B and Ar is phenyl unsubstituted or substituted by branched or straight chain (C 1-6) alkyl, branched or straight chain O- (d 6) alkyl, OH, F, Cl, Br, 1, trifluoromethyl, NR5R6, CO2R7, cyano or phenyl or is tetralinyl, indanyl, condensed aromatic systems such as naphthyl which is unsubstituted or substituted by (C 1-4) alkyl or O (d- 2 heteroatoms selected independently of one another from O and N, and which may also be condensed to other aromatic residues such as quinoline, isoquinoline, phthalazine, indole and quinazoline, which themselves may be substituted with phenyl; and R3 and R4 have the meanings set forth in the specification. The invention also relates to the preparation of the invented derivatives and their use as serotonin antagonists.
priorityDate 1997-10-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 57.