Global Patent Index - EP 0983245 A1

EP 0983245 A1 2000-03-08 - SUBSTITUTED TETRAHYDROISOQUINOLINE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS

Title (en)

SUBSTITUTED TETRAHYDROISOQUINOLINE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS

Title (de)

SUBSTITUIERTE TETRAHYDROISOCHINOLINEDERIVATE ALS DOPAMINE D3 REZEPTOR-MODULATOREN

Title (fr)

DERIVES DE TETRAHYDROISOQUINOLEINE DERIVES SUBSTITUES SERVANT DE MODULATEURS DE RECEPTEURS DE LA DOPAMINE D3

Publication

EP 0983245 A1 (EN)

Application

EP 98924263 A

Priority

  • EP 9802584 W
  • GB 9709303 A

Abstract (en)

[origin: WO9851671A1] Compounds of formula (I) wherein: R<1> represents a substituent selected from: a hydrogen or halogen atom; a hydroxy, cyano, nitro, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, pentafluoroethyl, C1-4alkyl, 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(CH2)p, R<3>CON(R<4>)(CH2)p, R<3>R<4>NCO(CH2)p, or R<3>R<4>NSO(CH2)p where each of R<3> and R<4> independently represents a hydrogen atom or a C1-4alkyl group or R<3>R<4> forms part of a C3-6azacycloalkane 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 Ar<3> 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 CH2; 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 C1-4alkyl 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 Ar<2> 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-, -CH2-, 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.

IPC 1-7 (main, further and additional classification)

C07D 217/04; A61K 31/47; C07D 401/12

IPC 8 full level (invention and additional information)

A61K 31/472 (2006.01); A61K 31/4725 (2006.01); A61P 25/18 (2006.01); A61P 43/00 (2006.01); C07D 217/04 (2006.01); C07D 401/12 (2006.01)

CPC (invention and additional information)

C07D 401/12 (2013.01); C07D 217/04 (2013.01)

Citation (search report)

See references of WO 9851671A1

Designated contracting state (EPC)

BE CH DE ES FR GB IT LI NL

EPO simple patent family

WO 9851671 A1 19981119; CA 2288850 A1 19981119; EP 0983245 A1 20000308; GB 9709303 D0 19970625; JP 2001525813 A 20011211

INPADOC legal status


2002-05-22 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20011101

2000-03-08 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 19991111

2000-03-08 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): BE CH DE ES FR GB IT LI NL