JP2010168377A5

JP2010168377A5 -

Info

Publication number: JP2010168377A5
Application number: JP2009296903A
Authority: JP
Filing date: 2009-12-28
Publication date: 2013-01-31
Anticipated expiration: 2029-12-28

Claims

General formula (1)

[Wherein, R ¹ represents any group represented by the following (1-1) to (1-7).
(1-1) Group —CO— (CH ₂ ) _n —COR ²
(Here, n represents an integer of 1 to 4. R ² is (2-1) hydroxyl group; (2-2) hydroxyl group, lower alkanoyl group, lower alkanoyloxy group, lower alkoxycarbonyloxy group as a substituent, A lower alkoxy group which may have a cycloalkyloxycarbonyloxy group or a 5-methyl-2-oxo-1,3-dioxol-4-yl group; or (2-3) a hydroxy lower alkyl group as a substituent an amino group which.)
(1-3) group —CO— (CH ₂ ) _p —O—CO—NR ⁵ R ⁶
(Here, p represents an integer of 1 to 4. R ⁵ represents a lower alkyl group. R ⁶ represents a lower alkoxycarbonyl lower alkyl group.)
(1-4) Group —CO— (CH ₂ ) _q —X—R ⁷
(Here, q represents an integer of 1 to 4. X represents an oxygen atom, a sulfur atom or a sulfonyl group. R ⁷ represents a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group.)
(1-5) Group —CO—R ⁸
(Wherein R ⁸ is (8-1) a halogen atom, a lower alkanoyloxy group or a phenyl group on the alkyl group (the phenyl group is a dihydroxyphosphoryloxy group in which the hydroxy group may be substituted with a benzyl group, and An alkyl group which may be substituted), (8-2) a lower alkoxy group having a halogen atom, a lower alkanoyloxy group or a dihydroxyphosphoryloxy group as a substituent, (8-3) Represents a pyridyl group or (8-4) a lower alkoxyphenyl group.)
(1-6) a lower alkyl group substituted by a group selected from the group consisting of a lower alkylthio group, a dihydroxyphosphoryloxy group and a lower alkanoyloxy group
(1-7) Oh Lupe peptide residues having one or more protective groups]
A pharmaceutical comprising a benzazepine compound represented by the formula:

In the general formula (1), R ¹ is a group —CO— (CH ₂ ) _n —COOH (where n is an integer of 1 to 4), a group —CO—R ⁸ (where R ⁸ is an alkyl group). and indicating the one or more protecting Oh Lupe peptide residue selected from the group consisting of groups having a group a compound according to claim 1 or a pharmaceutical comprising a salt thereof.

In the general formula (1), R ¹ Gasa Rukoshiru - glycyl, glycyl - glycyl, glycyl - sarcosyl, glycyl - alanyl, alanyl - glycyl, sarcosyl - sarcosyl, glycyl - phenylalanyl, phenylalanyl - glycyl, phenylalanyl - phenylalanyl, glycyl - glycyl - glycyl, N, N- di-methylcarbamoyl Rugurishiru - glycyl, N- methyl -N- Echirugurishiru - glycyl, sarcosyl - consists glycyl - glycyl - glycyl and N, N- dimethylglycyl - glycyl The pharmaceutical which consists of the compound or its salt of Claim 1 which is a peptide residue selected from the group (each group may be protected by one or more protecting groups).

In general formula (1), R ¹ is sarkosyl-glycyl, glycyl-glycyl, glycyl-sarcosyl, glycyl-alanyl, alanyl-glycyl, glycyl-phenylalanyl, phenylalanyl-glycyl, phenylalanyl-phenylalanyl, Peptide residues selected from the group consisting of glycyl-glycyl-glycyl, N, N-dimethylglycyl-glycyl, N-methyl-N-ethylglycyl-glycyl and N, N-dimethylglycyl-glycyl-glycyl (each group 4 may be protected with one or more protecting groups), or a pharmaceutical comprising the compound or a salt thereof according to claim 3.

A pharmaceutical formulation comprising the benzazepine compound of claim 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable diluent and / or carrier.

The pharmaceutical preparation according to claim 5, which is used as a vasodilator, an antihypertensive agent, a diuretic or a platelet aggregation inhibitor.