C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 451/00 (2006.01) A61K 31/47 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 451/04 (2006.01) C07D 451/14 (2006.01) C07D 453/00 (2006.01) C07D 453/02 (2006.01) C07D 471/08 (2006.01) C07D 498/08 (2006.01) C07D 513/08 (2006.01)
Patent
CA 2081350
2081350 9117161 PCTABS00008 Isoquinoline derivatives (I) having 5-HT3 receptor antagonist activity, a process for their preparation and their use as pharmaceuticals. In formula (I) E is NH or O, R1 is hydrogen, halogen, alkyl, alkoxy, hydroxy or nitro; Z is an azacyclic or azabicyclic side chain, such as a group of formula (a), (b) or (c) wherein; p is 1 or 2; q is 1 to 3; r is 1 to 3; R3 or R4 is hydrogen or alkyl, and Y is a group -CH2-X-CH2- wherein X is -CH2-, oxygen, sulphur or X is a bond; and (I) when the group CO-E-Z is in the 1-position and either R2 is in the 3-position and is hydrogen, alkyl, or alkoxy, or R2 is in the 4-position and is hydrogen CF3, alkyl, acyl, acylamino (substituted) phenyl or (substituted) amino, (substituted) aminocarbonyl or (substituted) aminosulphonyl; (II) the group CO-E-Z- is in the 3-position and either R2 is in the 1-position and is hydrogen, alkyl or alkoxy or R2 is in the 4-position and is hydrogen or alkoxy.
Beecham Group P.l.c.
Borden Ladner Gervais Llp
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