# US 5,707,998 A · Nitrogen-containing fused-heterocycle compounds

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- Number: US 5,707,998 A
- Document ID: US5707998A
- Status: Granted
- Kind: A
- Application number: 08/525,739
- Filed: 1995-09-25
- Granted: 1998-01-13
- Earliest claimed: 1993-03-31
- Assignees: Eisai Co., Ltd.
- Inventors: Yasutaka Takase; Nobuhisa Watanabe; Hideyuki Adachi; Kohtaro Kodama; Hiroki Ishihara; Takao Saeki; Shigeru Souda
- Web page: https://patentgrep.com/patent/US5707998A

## CPC

- C07D 231/12: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D 233/56: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
- C07D 249/08: 1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 405/14: containing three or more hetero rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention relates to a nitrogen-containing heterocyclic compound exhibiting an inhibitory activity against cGMP-PDE. The compound represented by the formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a group represented by the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 each represent hydrogen, lower alkyl or the like) or the like; R.sup.2 represents a group represented by the formula: ##STR2## (wherein R.sup.8 represents a carboxyl group which may be protected, or the like) or the like; and R.sup.3 represents a group represented by the formula: ##STR3## (wherein R.sup.6 and R.sup.7 each represent hydrogen, lower alkyl or the like) or the like.

## Claims

### Claim 1

A quinazoline derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR49## wherein R.sup.1 is selected from pyrazolyl, imidazolyl, substituted imidazolyl, triazolyl, tetrazolyl, piperidyl, a nitro group or a --NR.sup.5 R.sup.6 group wherein R.sup.5 and R.sup.6 may be the same or different from each other and each represent a hydrogen atom or a lower alkyl group;
R.sup.2 is a hydrogen atom with the proviso when R.sup.1 is an amino group, then R.sup.2 is not a hydrogen atom, a halogen atom or a group represented by the following formula ##STR50## wherein R7 is a hydrogen atom or a lower alkyl group; R.sup.3 and R.sup.4 each represent a halogen atom or a lower alkoxy group, or together form a methylenedioxy group or ethylenedioxy group.

### Claim 2 (depends on 1)

A composition comprising a compound of claim 1 together with a carrier or diluent.

### Claim 3 (depends on 1)

A method for treating ischemic heart disease, angina pectoris, hypertension, heart failure or asthma, which comprises administering a mammal with a pharmacologically effective amount of the compound as claimed in claim 1, or a pharmacologically acceptable salt thereof.

### Claim 4 (depends on 3)

The method as claimed in claim 3, in which the subject is a human being.