C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/237, 260/305
C07D 403/10 (2006.01) A61K 31/415 (2006.01) C07D 209/04 (2006.01) C07D 209/10 (2006.01) C07D 209/26 (2006.01) C07D 209/30 (2006.01) C07D 403/06 (2006.01) C07D 403/14 (2006.01) C07D 521/00 (2006.01)
Patent
CA 2030177
ABSTRACT INDOLE DERIVATIVES The invention provides compounds of the general formula (1): (I) Image or a physiologically acceptable salt or a solvate (e g. hydrates) thereof in which R1 represents a hydrogen atom or a halogen atom or a group selected from C1-6 alkyl, C2 6 alkenyl, fluoroC1-6alkyl, -CHO, -CO2H or -COR4; R2 represents a hydrogen atom or a halogen atom or the group Ar; R3 represents a hydrogen atom or a group selected from C1-6alkyl, C3-6alkenyl, C1-6alkoxy, -COR4, -SO2R4 or the group Ar; R4 represents a group selected from C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxy or thegroup NR12R13; Ar represents the group Image ; R5 represents a group selected from -CO2H, -NHSO2CF3 or a C-linked tetrazolyl group; R6 and R7 which may be the same or different each independently represent a hydrogen atom or a halogen atom or a C1-6alkyl group; Het represents an N-linked imidazolyl group substituted at the 2-position by a C1-6alkyl, C2-6alkenyl or a C1-6alkylthio group, the imidazolyl group optionallybeing substituted by one or two further substituents selected from a halogen atom or a group selccted from cyano, nitro, C1-6alkyl, C2 6alkenyl, fluoroC1 6alkyl, -(CH2)mR8, -(CH2)nCOR9, or -(CH2)pNR10COR11; or Het represents an N-linked benzimidazolyl group substituted at the 2-position by a C1-6alkyl, C2-6alkenyl or a C1-6alkylthio group; R8 represents a hydroxy or C1-6alkoxy group; R9 represents a hydrogen atom or a group selected from hydroxy, C1-6alkyl, C1-6alkoxy, phenyl, phenoxy or the group -NR12R13; R10 represents a hydrogen atom or a C1-6alkyl group; R11 represents a hydrogen atom or a group selected from C1 6alkyl, C1 6alkoxy, phenyl, phenoxy or the group -NR12R13; R12 and R13 which may be the same or different each independently represent a hydrogen atom or a C1-4alkyl group or -NR12Rl3 forms a saturated heterocyclic ring which has 5 or 6 ring members and may optionally contain in the ring one oxygen atom; m represents an integer from 1 to 4; n represents an integer from 0 to 4; and p represents an integer from 1 to 4; provided that one of R2 and R3 represents the group Ar, and that when R2 represents the group Ar, R3 represents a hydrogen atom or a group selected from C1-6 alkyl, C3-6 alkenyl, C1-6alkoxy -COR4 or-SO2R4, and that when R3 represents the group Ar, R2 represents a hydrogen atom or a halogen atom. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
Cardwell Kevin S.
Dowle Michael D.
Jack Torquil I. M.
Middlemiss David
Ross Barry C.
Cardwell Kevin S.
Dowle Michael D.
Fetherstonhaugh & Co.
Glaxo Group Limited
Jack Torquil I. M.
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