(19)
(11)EP 1 327 631 A3

(12)EUROPEAN PATENT APPLICATION

(88)Date of publication A3:
11.02.2004 Bulletin 2004/07

(43)Date of publication A2:
16.07.2003 Bulletin 2003/29

(21)Application number: 03006453.9

(22)Date of filing:  16.04.1992
(51)Int. Cl.7C07D 471/04, C07D 495/04, C07D 487/04, C07D 403/14, C07D 405/14, C07D 401/06, C07D 473/28, C07D 403/10, A61K 31/435, A61K 31/505, A61K 31/41
// (C07D471/04, 235:00, 221:00),(C07D471/04, 235:00),(C07D495/04, 333:00, 221:00),(C07D487/04, 239:00, 231:00)
(84)Designated Contracting States:
AT BE CH DE DK ES FR GB GR IT LI LU NL PT SE

(30)Priority: 16.04.1991 JP 17347391
05.07.1991 JP 26334191
25.09.1991 JP 31562991

(62)Application number of the earlier application in accordance with Art. 76 EPC:
92106621.3 / 0518033

(71)Applicant: Takeda Chemical Industries, Ltd.
Osaka-shi, Osaka 541-0045 (JP)

(72)Inventors:
  • Naka, Takehiko
    Kobe, Hyogo 658 (JP)
  • Inada, Yoshiyuki
    Kawanishi, Hyogo 666 (JP)

(74)Representative: Best, Michael, Dr. et al
Lederer & Keller Patentanwälte Prinzregentenstrasse 16
80538 München
80538 München (DE)

  


(54)Fused heterocyclic compounds, their production and use as angiotensin II antagonists


(57) Fused heterocyclic compounds of the formula (I): wherein R1 is an optionally substituted hydrocarbon residue which may be attached through a hetero atom; R2 is a group capable of forming an anion or a group convertible thereinto; R3 is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hetero atom; X is a direct bond or a spacer having an atomic length of two or less between the R3 group and the ring W group; W is an optionally substituted aromatic hydrocarbon or heterocyclic residue which contains at least one hetero atom;
a,c and d are independently selected from the group consisting of one or two optionally substituted carbon atoms and one or two optionally substituted hetero atoms; b and e are independently selected from the group consisting of one optionally substituted carbon atom and one optionally substituted nitrogen atom; the dotted line is a bond to form one double bond; n is an integer of 1 or 2 and when a, which is an optionally substituted carbon atom, is taken together with R1, the following group: may form a ring group; provided that when is a benzimidazole, thieno[3,4-d]imidazole, or thieno[2,3-d]imidazole ring, at least one of the group: and R3 is an optionally substituted heterocyclic residue ; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.