Nitrogen-containing fused-heterocycle compounds

• US 5,707,998 A
• Filed: 09/25/1995
• Issued: 01/13/1998
• Est. Priority Date: 03/31/1993
• Status: Expired due to Term

• Current Assignee: Eisai R & D Management Company Limited (Eisai Medical Research Incorporated)
• Original Assignee: Eisai Company Limited (Eisai Medical Research Incorporated)
• Inventors: Saeki, Takao, Watanabe, Nobuhisa, Adachi, Hideyuki, Takase, Yasutaka, Ishihara, Hiroki, Souda, Shigeru, Kodama, Kohtaro
• Primary Examiner(s): Grumbling, Matthew V.
• Application Number:
  US08/525,739
• Time in Patent Office: 841 Days
• Field of Search: 544/283, 544/291, 544/293, 514/259, 514/260
• US Class Current: 514/266.22
• CPC Class Codes: C07D 231/12 with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• CPC Class Codes: C07D 233/56 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
• CPC Class Codes: C07D 249/08 1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
• CPC Class Codes: C07D 405/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 405/14 containing three or more hetero rings

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 R¹ represents a group represented by the formula: --NR⁴ R⁵ (wherein R⁴ and R⁵ each represent hydrogen, lower alkyl or the like) or the like; R² represents a group represented by the formula: ##STR2## (wherein R⁸ represents a carboxyl group which may be protected, or the like) or the like; and R³ represents a group represented by the formula: ##STR3## (wherein R⁶ and R⁷ each represent hydrogen, lower alkyl or the like) or the like.

Claims

1. A quinazoline derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof:

##STR49## wherein R¹ is selected from pyrazolyl, imidazolyl, substituted imidazolyl, triazolyl, tetrazolyl, piperidyl, a nitro group or a --NR⁵ R⁶ group wherein R⁵ and R⁶ may be the same or different from each other and each represent a hydrogen atom or a lower alkyl group;

R² is a hydrogen atom with the proviso when R¹ is an amino group, then R² 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;

R³ and R⁴ each represent a halogen atom or a lower alkoxy group, or together form a methylenedioxy group or ethylenedioxy group.

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

3. 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.

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