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1. (WO2001032626) ISOQUINOLINE AND QUINAZOLINE DERIVATIVES HAVING A COMBINED 5HT1A, 5HT1B AND 5HT1D RECEPTOR ACTIVITY

Pub. No.:    WO/2001/032626    International Application No.:    PCT/EP2000/010908
Publication Date: Fri May 11 01:59:59 CEST 2001 International Filing Date: Fri Nov 03 00:59:59 CET 2000
IPC: A61K 31/437
A61K 31/47
A61K 31/505
C07D 217/22
C07D 239/94
C07D 471/04
Applicants: SMITHKLINE BEECHAM P.L.C.
GASTER, Laramie, Mary
HEIGHTMAN, Thomas, Daniel
PILLEUX, Jean-pierre
Inventors: GASTER, Laramie, Mary
HEIGHTMAN, Thomas, Daniel
PILLEUX, Jean-pierre
Title: ISOQUINOLINE AND QUINAZOLINE DERIVATIVES HAVING A COMBINED 5HT1A, 5HT1B AND 5HT1D RECEPTOR ACTIVITY
Abstract:
The invention relates to novel isoquinoline and quinazoline derivatives of formula (I) having 5HT1A, 5HT1B and 5HT1D receptor affinity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders in which R1 is selected from a group of formula (i) where P1 is phenyl, naphthyl, a 5 or 6 membered heteroaryl ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, a benzofused heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen and sulphur, or a pyridofused heterocyclic ring containing 1 to 3 nitrogen atoms; Ra is halogen, C¿1-6?alkyl, C3-6cycloyalkyl, CF3, C1-6alkoxy, OCF3, hydroxy, cyano, nitro, hydroxyC1-6alkyl, COC1-6alkyl, CO2R?5, SO¿2R?5, NR5R6, CONR5R6¿, and SO¿2NR?5R6 where R?5 and R6¿ are independently hydrogen or C¿1-6?alkyl; n is 0,1,2 or 3; or group of formula (ii) in which P?2 and P3¿ are independently as defined for P1 above; R?b and Rc¿ are independently as defined for Ra above; p and q are independently as defined for n above; L is a single bond or NH; R2 is hydrogen or together with the group R3 forms a further group -CH = CH- or (CR7R8)2 where R?7 and R8¿ are independently hydrogen or C¿1-6?alkyl; R?3¿ is hydrogen or together with R2 forms a further group as defined above; Y is N or CH; X is N or CH; R4 is hydrogen or C¿1-6?alkyl.