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US 2005/0239797 A1Published application
Isoquinoline and quinazoline derivatives having a combined 5HT1A, 5HT1B, and 5HT1D receptor activity
AssigneeSmithKline Beecham Corporation
InventorsLaramie Gaster, Thomas Heightman, Jean-Pierre Pilleux
Life of this patent
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Abstract
The invention relates to novel isoquinoline and quinazoline derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.
Claims15
A compound of formula (I) or a pharmaceutically acceptable salt thereof:
- in which R1 is selected from a group of formula (i) or (ii)
- 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, C1-6alkyl, C3-6cycloalkyl, CF3, C1-6alkoxy, OCF3, hydroxy, cyano, nitro, hydroxyC1-6alkyl, COC1-6alkyl, CO2R5, SO2R5, NR5R6, CONR5R6, and SO2NR5R6 where R5 and R6 are independently hydrogen or C1-16alkyl;
- n is 0, 1, 2 or 3;
- Group of formula (ii)
- in which P2 and P3 are independently as defined for P1 above;
- Rb 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 R7 and R8 are independently hydrogen or C1-6alkyl;
- R3 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 C1-6alkyl.
12 more elements
Dependencies are inferred from the claim text.