C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/474.1, 260/3
C07D 295/12 (2006.01) C07C 93/14 (1985.01) C07C 101/72 (1985.01)
Patent
CA 1252785
A B S T R A C T PHENETHANOLAMINE COMPOUNDS The invention provides compounds of the general formula (I) Image (I) wherein m is an integer from 2 to 8 and n is an integer from 1 to 7 with the proviso that the sum total of m + n is 4 to 12; Ar represents a phenyl group substituted by one or more substituents selected from halogen atoms, or C1-6alkyl, -(CH2)qR, [where R is hydroxy, C1-6alkoxy, -NR3R4(where R3 and R4 each represents a hydrogen atom, or a C1-4 alkyl group, or -NR3R4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from -0- or -S- or a group -NH- or -N(CH3)-), -NR5COR6 (where R5 represents a hydrogen atom or a C1-4 alkyl group, and R6 represents a hydrogen atom or a C1-4 alkyl, C1-4 alkoxy, phenyl or -NR3R4 group), -NR5SO2R7 (where R7 represents a C1-4 alkyl, phenyl or -NR3R4 group), -COR8 (where R8 represents hydroxy, C1-4 alkoxy or -NR3R4), -SR9 (where R9 is a hydrogen atom, or a C1-4 alkyl or phenyl group), -SOR9, SO2R9, or -CN, and q represents an integer from 0 to 3], -O(CH2)rR10 [where R10 represents a hydroxy or C1-4 alkoxy group and r is an integer 2 or 3], or -NO2 groups, with the proviso that if the phenyl group Ar is substituted by only one or two substituents selected from halogen atoms or C1-3 alkyl or C1-3 alkoxy groups it contains at least one additional substituent which is different from those substituents; R1 and R2 each represents a hydrogen atom or a C1-3 alkyl group with the proviso that the SUM total of carbon atoms in R1 and R2 is not more than 4; and physiologically acceptable salts and solvates (e.g. hydrates) thereof. The compounds of formula (I) have a selective stimulant action at .beta.2-adrenoreceptors and are useful, in particular in the treatment of diseases associated with reversible airways abstruction such as asthma and chronic bronchitis.
479396
Finch Harry
Lunts Lawrence H. C.
Naylor Alan
Skidmore Ian F.
Glaxo Group Limited
Riches Mckenzie & Herbert Llp
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