US 5,397,780 AGranted

Pyrroloazepine derivative

AssigneeSuntory Limited

InventorsAkira Mizuno, Hidetsura Cho, Mikiko Miya, Toshio Tatsuoka, Takafumi Ishihara

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Abstract

This invention provides a pyrroloazepine derivative represented by the following formula (I): ##STR1## where the substituents are defined in the specification. The pyrroloazepine derivatives according to the present invention are drugs having excellent anti-.alpha..sub.1 action and anti-serotonin action and feature high safety. They can therefore be used, for example, as novel therapeutics for circulatory diseases.

Claims12

Dependent claims

A pyrroloazepine represented by the following formula (I):

##STR67## wherein the dashed line indicates the presence or absence of a bond and when the bond indicated by the dashed line is present, Z.sub.1 represents a hydrogen atom but, when the bond indicated by the dashed line is absent, Z.sub.1 represents a hydrogen atom and Z.sub.2 represents a hydroxyl group or Z.sub.1 and Z.sub.2 are taken together to form an oxygen atom or a group NOR.sub.1 in which R.sub.1 represents a hydrogen atom, a branched or linear C.sub.1-4 alkyl group, a C.sub.6 -C.sub.10 aryl group or C.sub.8 -C.sub.16 aralkyl group, said aryl or aralkyl group optionally substituted by one or more halogen atoms, C.sub.1 -C.sub.4 alkyl groups, or C.sub.1 -C.sub.4 alkoxy groups;
R represents a hydrogen atom, a branched or linear C.sub.1-8 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.3-8 cycloalkyl-alkyl group, a C.sub.6-10 aryl or C.sub.7-20 aralkyl group, said aryl or aralkyl group optionally substituted by one or more halogen atoms, C.sub.1-4 alkyl groups, and/or C.sub.1-4 alkoxy groups;
A represents a branched or linear C.sub.2-10 alkylene, a branched or linear C.sub.4 -C.sub.10 alkenylene, or a branched or linear C.sub.4-10 alkynylene group, said alkylene, alkenylene, or alkynylene optionally having one or more hydrogen atoms substituted by a hydroxyl group;
and Y represents a group:
##STR68## in which R.sub.2 and R.sub.3 may be the same or different and individually represent a hydrogen atom, a branched or linear C.sub.1-8 alkyl group which may be substituted by a lower alkoxy group or a C.sub.6-10 aryloxyl group, a C.sub.6-10 aryl group, a C.sub.7-20 aralkyl group or a partially-saturated naphthyl group, said aryloxyl, aryl, aralkyl, or partially-saturated naphthyl group optionally substituted-by one or more halogen atoms, C.sub.1-4 alkyl groups, C.sub.1-4 alkoxy groups, and/or hydroxyl groups, or a group:
##STR69## in which R.sub.4 and R.sub.5 may be the same or different and individually represent a hydrogen atom or a branched or linear C.sub.1-8 alkyl group;
B represents a carbonyl group, a sulfonyl group, a C.sub.1-10 alkylene group, a C.sub.2-10 alkenylene, or a phenylmethylene group optionally substituted by one or more halogen atoms, C.sub.1-4 alkyl groups, or C.sub.1-4 alkoxy groups;
m stands for 1 or 2;
n stands for 0 or 1;
and D represents a C.sub.1-4 alkoxy group, a pyridyl, pyrimidyl or furanyl group, a C.sub.6-10 aryl group optionally substituted with one or more hydroxyl groups, halogen atoms, C.sub.1-4 alkyl groups, C.sub.1-4 alkoxy groups, and/or benzyloxy groups or a 1,4-benzodioxanyl group, or a physiologically acceptable salt thereof.

7 more elements

Dependencies are inferred from the claim text.

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Abstract

A pyrroloazepine represented by the following formula (I):

##STR67## wherein the dashed line indicates the presence or absence of a bond and when the bond indicated by the dashed line is present, Z.sub.1 represents a hydrogen atom but, when the bond indicated by the dashed line is absent, Z.sub.1 represents a hydrogen atom and Z.sub.2 represents a hydroxyl group or Z.sub.1 and Z.sub.2 are taken together to form an oxygen atom or a group NOR.sub.1 in which R.sub.1 represents a hydrogen atom, a branched or linear C.sub.1-4 alkyl group, a C.sub.6 -C.sub.10 aryl group or C.sub.8 -C.sub.16 aralkyl group, said aryl or aralkyl group optionally substituted by one or more halogen atoms, C.sub.1 -C.sub.4 alkyl groups, or C.sub.1 -C.sub.4 alkoxy groups;
R represents a hydrogen atom, a branched or linear C.sub.1-8 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.3-8 cycloalkyl-alkyl group, a C.sub.6-10 aryl or C.sub.7-20 aralkyl group, said aryl or aralkyl group optionally substituted by one or more halogen atoms, C.sub.1-4 alkyl groups, and/or C.sub.1-4 alkoxy groups;
A represents a branched or linear C.sub.2-10 alkylene, a branched or linear C.sub.4 -C.sub.10 alkenylene, or a branched or linear C.sub.4-10 alkynylene group, said alkylene, alkenylene, or alkynylene optionally having one or more hydrogen atoms substituted by a hydroxyl group;
and Y represents a group:
##STR68## in which R.sub.2 and R.sub.3 may be the same or different and individually represent a hydrogen atom, a branched or linear C.sub.1-8 alkyl group which may be substituted by a lower alkoxy group or a C.sub.6-10 aryloxyl group, a C.sub.6-10 aryl group, a C.sub.7-20 aralkyl group or a partially-saturated naphthyl group, said aryloxyl, aryl, aralkyl, or partially-saturated naphthyl group optionally substituted-by one or more halogen atoms, C.sub.1-4 alkyl groups, C.sub.1-4 alkoxy groups, and/or hydroxyl groups, or a group:
##STR69## in which R.sub.4 and R.sub.5 may be the same or different and individually represent a hydrogen atom or a branched or linear C.sub.1-8 alkyl group;
B represents a carbonyl group, a sulfonyl group, a C.sub.1-10 alkylene group, a C.sub.2-10 alkenylene, or a phenylmethylene group optionally substituted by one or more halogen atoms, C.sub.1-4 alkyl groups, or C.sub.1-4 alkoxy groups;
m stands for 1 or 2;
n stands for 0 or 1;
and D represents a C.sub.1-4 alkoxy group, a pyridyl, pyrimidyl or furanyl group, a C.sub.6-10 aryl group optionally substituted with one or more hydroxyl groups, halogen atoms, C.sub.1-4 alkyl groups, C.sub.1-4 alkoxy groups, and/or benzyloxy groups or a 1,4-benzodioxanyl group, or a physiologically acceptable salt thereof.

7 more elements