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US 6,586,630 B1Granted
Ethylamine derivatives
AssigneeChugai Seiyaku Kabushiki Kaisha
InventorsHiroharu Matsuoka, Tsutomu Sato
Life of this patent
Estimating the term…
Abstract
The object of the present invention is to provide ethylamine derivatives that function as a motilin receptor antagonist and that are useful as medicines. The invention provides compounds represented by the general formula (1): wherein R1 represents a phenyl group or the like, R2 represents a hydrogen atom and the like, R3 represents a hydrogen atom and the like, R4 represents a hydrogen atom and the like, R5 represents an alkyl group and the like, R7 represents a hydrogen atom and the like and R8 represents a heterocyclic ring and the like; or a hydrate or pharmaceutically acceptable salt thereof and a medicine which comprises the above compound or a hydrate or pharmaceutically acceptable salt thereof as an active ingredient.
Claims20
A compound represented by the general formula (1):
- wherein
- R1 is an optionally substituted phenyl group, a straight-chained or branched alkenyl group having 2-6 carbon atoms or a straight-chained or branched alkynyl group having 2-6 carbon atoms;
- R2 is a hydrogen atom, an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms, an amino group or a hydroxy group;
- R3 is a hydrogen atom, an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms, an optionally substituted amino group or a hydroxy group;
- R4 is a hydrogen atom, a methyl group or an ethyl group;
- R5 is an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-7 carbon atoms or an optionally substituted phenyl group;
- R6 is a hydrogen atom, a methyl-group or an ethyl group;
- R7 is a hydrogen atom, an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms or —CO—N(R9)R10;
- R8 is of the general formula (2)
- R9 and R10, which may be the same or different, each represent a hydrogen atom or an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms;
- R11 is a hydroxy group or a halogen atom;
- R12, when R11 is a hydroxy group, represents a substituted straight-chained or branched alkyl group having 1-6 carbon atoms, a substituted straight-chained or branched alkenyl group having 2-6 carbon atoms, a substituted straight-chained or branched alkynyl group having 2-6 carbon atoms, a straight-chained or branched acyl group having 2-6 carbon atoms, a straight-chained or branched alkylsulfonyl group having 1-5 carbon atoms or an amino group mono- or di-substituted with a straight-chained or branched alkyl group having 1-5 carbon atoms, and R12, when R11 is a halogen atom, represents an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms, an optionally substituted straight-chained or branched alkenyl group having 2-6 carbon atoms, an optionally substituted straight-chained or branched alkynyl group having 2-6 carbon atoms, a straight-chained or branched acyl group having 2-6 carbon atoms, a straight-chained or branched alkylsulfonyl group having 1-5 carbon atoms or an amino group mono- or di-substituted with a straight-chained or branched alkyl group having 1-5 carbon atoms;
- X is a carbonyl group or a methylene group;
- and
- Y is a carbonyl group or a methylene group;
- or a hydrate or pharmaceutically acceptable salt thereof.
13 more elements
A compound represented by the general formula (1):
- wherein
- R1 is an optionally substituted phenyl group, a straight-chained or branched alkenyl group having 2-6 carbon atoms or a straight-chained or branched alkynyl group having 2-6 carbon atoms;
- R2 is a hydrogen atom, an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms, an amino group or a hydroxy group;
- R3 is a hydrogen atom, an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms, an optionally substituted amino group or a hydroxy group;
- R4 is a hydrogen atom, a methyl group or an ethyl group;
- R5 is an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms, a cycloalkyl group having 3-7 carbon atoms or an optionally substituted phenyl group;
- R6 is a hydrogen atom, a methyl group or an ethyl group;
- R7 is a hydrogen atom, an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms or —CO—N(R9)R10;
- R8 is of general formula (2)
- R9 and R10, which may be the same or different, each represent a hydrogen atom or an optionally substituted straight-chained or branched alkyl group having 1-3 carbon atoms;
- R11 is a hydroxy group or a halogen atom;
- R12, when R11 is a hydroxy (group, represents a substituted straight-chained or branched alkyl group having 1-6 carbon atoms, a substituted straight-chained or branched alkenyl group having 2-6 carbon atoms, a substituted straight-chained or branched alkynyl group having 2-6 carbon atoms, a straight-chained or branched acyl group having 2-6 carbon atoms, a straight-chained or branched alkylsulfonyl group having 1-5 carbon atoms or an amino group mono- or all-substituted with a straight-chained or branched alkyl group having 1-5 carbon atoms, and R12, when R11 is a halogen atom, represents an optionally substituted straight-chained or branched alkyl group having 1-6 carbon atoms, an optionally substituted straight-chained or branched alkenyl group having 2-6 carbon atoms, an optionally substituted straight-chained or branched alkynyl group having 2-6 carbon atoms, a straight-chained or branched acyl group having 2-6 carbon atoms, a straight-chained or branched alkylsulfonyl group having 1-5 carbon atoms or an amino group mono- or di-substituted with a straight-chained or branched alkyl group having 1-5 carbon atoms;
- X is a carbonyl group or a methylene group;
- and
- Y is a carbonyl group or a methylene group;
- or a hydrate or pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.