http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0983245-A1

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-18
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D217-04
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12
filingDate 1998-04-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5c2009e34d4f57dcac464356104b40aa
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7d252c4939d22e6f15e22668693a0106
publicationDate 2000-03-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0983245-A1
titleOfInvention Substituted tetrahydroisoquinoline derivatives as modulators of dopamine d3 receptors
abstract Compounds of formula (I) wherein: R1 represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, pentafluoroethyl, C¿1-4?alkyl, C1-4alkoxy, arylC1-4alkoxy, C1-4alkylthio, C1-4alkoxy C1-4alkyl, C3-6cycloalkylC1-4alkoxy, C1-4alkanoyl, C1-4alkoxycarbonyl, C1-4alkylsulphonyl, C1-4alkylsulphonyloxy, C1-4alkylsulphonylC1-4alkyl, arylsulphonyl arlysulphonyloxy, arylsulphonylC1-4alkyl, C1-4alkylsulphonamido, C1-4alkylamido, C1-4alkylsulphonamidoC1-4alkyl, C1-4alkylamidoC1-4alkyl, arylsulphomanido, arylcarboxamido, arylsulphonamidoC1-4alkyl, arylcarboxamidoC1-4alkyl, aroyl, aroylC1-4alkyl, or arylC1-4alkanoyl group; a group R?3¿OCO(CH¿2?)p, R?3CON(R4)(CH¿2)p, R3R4NCO(CH¿2?)p, or R?3R4¿NSO(CH¿2?)p where each of R?3 and R4¿ independently represents a hydrogen atom or a C¿1-4?alkyl group or R?3R4¿ forms part of a C¿3-6?azacycloalkane or C3-6(2-oxo)azacycloalkane ring and p represents zero or an integer from 1 to 4; or a group Ar?3¿-Z, wherein Ar3 represents an optionally substituted phenyl ring or an optionally substituted 5- or 6- membered aromatic heterocyclic ring and Z represents a bond O, S, or CH¿2?; s represents an integer from zero to 2 and r represents an integer from 1 to 4, such that the sum of s + r is 1 to 4; t represents an integer from zero to 1 and u represents an integer from zero to 2; R?2¿ represents a hydrogen atom or a C¿1-4?alkyl group; q is 1 or 2; A represents a group of the formula (a), (b) or (c): wherein Ar represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; or an optionally substituted bicyclic ring system; Ar?1 and Ar2¿ each independently represent an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; and Y represents a bond, -NHCO-, -CONH-, -CH¿2?-, or -(CH2)nY'(CH2)n-, wherein Y' represents O, S, SO2, or CO and m and n each represents zero or 1 such that the sum of m+n is zero or 1; providing that when A represents a group of formula (a), any substituent present in Ar ortho to the carboxamide moiety is necessarily a hydrogen or methoxy group; and salts thereof. Compounds of formula (I) and their salts have affinity for dopamine receptors, in particular the D3 receptor, and thus potential in the treatment of conditions wherein modulation of the D3 receptor is beneficial, e.g. as antipsychotic agents.
priorityDate 1997-05-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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