Hydroxylamine derivatives
First Claim
1. A hydroxylamine derivative of the formula IwhereinR4 is hydrogen, carbamoyl, (1-4C)alkyl, (2-5C)alkanoyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C) alkylcarbamoyl, benzoyl or phenylsulphonyl and wherein the benzoyl or phenylsulphonyl group may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C)alkyl and (1-4C)alkoxy;
- R5 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, and (2-5C) alkanoyl;
R6 is hydrogen, (1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl and wherein each phenyl group may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C)alkyl and (1-4C) alkoxy;
R7 is hydrogen or (1-4C) alkyl;
Ar1 is phenylene which may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C)alkyl and (1-4C)alkoxy;
whereinA1 is a direct link to X1 ;
X1 is thio, sulphinyl or sulphonyl;
Ar2 is phenylene, which may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C) alkyl and (1-4C) alkoxy;
R1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; and
R2 and R3 together form a group of the formula --A2 --X2 --A3 -- which together with the carbon atom to which A2 and A3 are attached define a ring having 6 ring atoms, wherein each of A2 and A3 is independently (1-3C)alkylene and X2 is oxy, and which ring may optionally bear one or two substituents selected from hydroxy, (1-4C)alkyl and (1-4C)alkoxy;
or a pharmaceutically-acceptable salt thereof.
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Accused Products
Abstract
The invention concerns hydroxylamine derivatives of the formula I ##STR1## wherein R4 is hydrogen, carbamoyl, (1-4C)alkyl, (2-5C)alkanoyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C)alkylcarbamoyl, benzoyl or phenylsulphonyl;
R5 includes hydrogen, (1-4C)alkyl and (2-5C)alkanoyl;
R6 is hydrogen, (1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl;
R7 is hydrogen or (1-4C)alkyl;
Ar1 is phenylene;
A1 is a direct link to X1, or A1 is (1-4C)alkylene;
X1 is oxy, thio, sulphinyl or sulphonyl;
Ar2 is phenylene, pyridinediyl, pyrimidinediyl, thiophenediyl, furandiyl, thiazolediyl, oxazolediyl, thiadiazolediyl or oxadiazolediyl;
R1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; and
R2 and R3 together form a group of the formula --A2 --X2 --A3 -- which together with the carbon atom to which A2 and A3 are attached define a ring having 5 or 6 ring atoms, wherein each of A2 and A3 is independently (1-3C)alkylene and X2 is oxy, thio, sulphinyl, sulphonyl or imino;
or a pharmaceutically-acceptable salt thereof;
processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
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Citations
9 Claims
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1. A hydroxylamine derivative of the formula I
wherein R4 is hydrogen, carbamoyl, (1-4C)alkyl, (2-5C)alkanoyl, N-(1-4C)alkylcarbamoyl, N,N-di-(1-4C) alkylcarbamoyl, benzoyl or phenylsulphonyl and wherein the benzoyl or phenylsulphonyl group may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C)alkyl and (1-4C)alkoxy; -
R5 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, and (2-5C) alkanoyl; R6 is hydrogen, (1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl and wherein each phenyl group may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C)alkyl and (1-4C) alkoxy; R7 is hydrogen or (1-4C) alkyl; Ar1 is phenylene which may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C)alkyl and (1-4C)alkoxy; wherein A1 is a direct link to X1 ; X1 is thio, sulphinyl or sulphonyl; Ar2 is phenylene, which may optionally bear one or two substituents selected from halogeno, cyano, trifluoromethyl, (1-4C) alkyl and (1-4C) alkoxy; R1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; and R2 and R3 together form a group of the formula --A2 --X2 --A3 -- which together with the carbon atom to which A2 and A3 are attached define a ring having 6 ring atoms, wherein each of A2 and A3 is independently (1-3C)alkylene and X2 is oxy, and which ring may optionally bear one or two substituents selected from hydroxy, (1-4C)alkyl and (1-4C)alkoxy; or a pharmaceutically-acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9)
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Specification