Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-02-03
2000-07-04
Stockton, Laura L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544 89, 546 14, 546165, 5462717, 546256, 5462734, 5462737, 548217, 5483044, 5483061, 5483064, 5483051, 5483071, 5483074, 5483094, 5483101, 5483104, 5483107, 549471, 5142302, 514314, 514333, 514 63, 514375, 514387, 514388, 514394, 514395, 514469, A61K 31415, A61K 3142, A61K 3144, A61K 3134, C07D40112, C07D40114, C07D40312, C07D40512
Patent
active
060839619
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to heterocyclic compounds and salts thereof which have activities as bradykinin antagonists and are useful for treating several diseases.
One object of this invention is to provide heterocyclic compounds and salts thereof which possess activities as bradykinin antagonists.
Another object of this invention is to provide processes for the preparation of said heterocyclic compounds and salts thereof.
A further object of this invention is to provide a pharmaceutical composition comprising, as an active ingredient, said heterocyclic compounds and salts thereof.
Still further object of this invention is to provide an agent for the prevention and/or the treatment of bradykinin or its analogues mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, comprising said heterocyclic compounds and salts thereof as an active ingredient.
BACKGROUND ART
Heterocyclic compounds having activities as bradykinin antagonists have been known as described in EP-A-596,406 and EP-A-622,361.
DISCLOSURE OF THE INVENTION
The object heterocyclic compounds of this invention are new and can be represented by the following general formula ##STR4## wherein a group of the formula: ##STR5## is a group of the formula: ##STR6## X is O, S or N--R.sup.5, R.sup.1 is lower alkyl, halo(lower)alkyl, lower alkylamino (lower) alkyl, hydroxy(lower) alkyl, lower alkoxy(lower)alkyl, lower alkoxy, lower alkylthio, lower alkylamino, acyl(lower)alkyl, acyl, hydroxy, mercapto, aryl or ar(lower)alkyl, and alkylamino(lower)alkyl, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, lower alkoxy, lower alkylthio, lower alkylamino, acyl(lower)alkyl, acyl, aryl or ar(lower)alkyl, or having O, S or N or lower alkenylene optopnally having O, S or N,
The object compound [I] or its salt can be prepared by processes as illustrated in the following reaction schemes. ##STR7## wherein ##STR8## R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A are each as defined above.
In the above and subsequent description of the present specification and claims, suitable examples of the various definitions to be included within the scope of the invention are explained in detail in the following.
The term "lower" is intended to mean a group having 1 to 6 carbon atom(s), unless otherwise provided.
In this respect, the term "lower" in lower alkenyl moiety, lower alkynyl moiety, heterocyclic(lower)alkenyl moiety and ar(lower)alkenyl moiety in the various definitions is intended to mean a group having 2 to 6 carbon atoms.
Further, the term "lower" in lower alkenoyl moiety, lower alkynoyl moiety, cyclo(lower)alkyl moiety, cyclo(lower)alkenyl moiety, ar(lower)alkenoyl moiety, ar(lower)alkynoyl moiety and heterocyclic(lower)alkenoyl moiety in the various definitions is intended to mean a group having 3 to 6 carbon atoms.
Suitable "halogen" may be fluorine, chlorine, bromine and iodine.
Suitable "aryl" and aryl moiety in the term "ar(lower)alkenoyl" may be phenyl, naphthyl, phenyl substituted with lower alkyl [e.g. tolyl, xylyl, mesityl, cumenyl, di(tert-butyl)phenyl, etc.] and the like, in which preferable one is phenyl, naphthyl and tolyl.
Suitable "lower alkyl" and lower alkyl moiety in the terms "acyl(lower)alkyl", "lower alkylamino(lower)alkyl", "hydroxy(lower)alkyl", "lower alkoxy(lower)alkyl", "heterocyclic(lower)alkyl", "lower alkylthio" and "lower alkylamino" may be straight or branched one such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl or the like, in which preferable one is C.sub.1 -C.sub.4 alkyl such as methyl, ethyl, propyl, isobutyl or tert-butyl.
Suitable "lower alkoxy" and lower alkoxy moiety in the term "lower alkoxy(lower)alkyl" may be straight or branched one such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy, pentyloxy, hexyloxy or the like, in which preferable one is C.sub.1 -C.sub.4 alkoxy such as methoxy, ethoxy or isopropoxy.
Suitable "lower alkylene" may be a straight or branched one such as methylene, ethylene, trimethylene, methylmethyl
REFERENCES:
patent: 5106862 (1992-04-01), Briving et al.
patent: 5563162 (1996-10-01), Oku et al.
patent: 5574042 (1996-11-01), Oku et al.
patent: 5750699 (1998-05-01), Oku et al.
Abe Yoshito
Inoue Takayuki
Kayakiri Hiroshi
Oku Teruo
Satoh Shigeki
Fujisawa Pharmaceutical Co. Ltd.
Stockton Laura L.
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