Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1989-07-02
1991-09-03
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142325, 5142328, 544115, 544234, 546269, 546274, 546297, 549 23, 549401, 549404, 562440, 562461, A61K 3150, C07D48704, C07D40304, C07D23736
Patent
active
050455419
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to fused pyridazine compounds or their pharmaceutically acceptable salts or hydrates and the pharmaceutical use.
BACKGROUND ART
Heretofore, there have been known 8-amino-4,4a,5,6-tetrahydro-2H-benzo[h]cinnolin-3-one possessing platelet aggregation-suppressing actions, vasodilating actions, antiulcer actions and so on in Japanese Patent Application Laid-open (Kokai) No. 47468/1986; benzo[h]cinnoline derivatives possessing anxiolytic actions, platelet aggregationsuppressing actions, diuretic actions and antidotal actions against administration of an excessive amount of anxiolytics in Kokai No. 56169/1986; benzothiopyrano[4,3-c]pyridazine compounds possessing anxiolytic actions or antidotal actions against administration of an excessive amount of anxiolytics in W087/04162 and (1)benzopyrano[4,3-c]pyridazin-3-one compounds in Bulletin of the Chemical Society of Japan, vol. 55, pp. 2450-2455 (1982) respectively as fused pyridazine compounds exhibiting pharmacological activities.
Meanwhile, there is a growing trend toward increase of human diseases which are caused by disorders in immune function such as autoimmunity diseases, infectious diseases, immuno-deficiency diseases and so on.
It is known that an adrenal cortical hormone which is one of the widely-used therapeutic medicines for the immune disorder diseases exhibits a drastic effect thereon, while it brings about serious side effects such as immune function deficiency, infectious diseases and edema.
The object of this invention resides in providing compounds with low level of side effects, which are useful for the prophylaxis and therapy of various diseases associated with immune function deficiency.
DISCLOSURE OF INVENTION
As a result of the present inventors' studies, they found that the fused pyridazine compounds having aminoalkoxy substituents exhibited not only excellent immune functionimproving actions but also infection-phylactic actions and antitumor actions, and besides have few side effects and are extremely safe in the aspect of toxicities, which resulted in the completion of this invention.
This invention relates to the fused pyridazine compounds of the general formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and respectively hydrogen, a halogen, hydroxy, nitro, amino, cyano, trifluoromethyl, an alkyl, an alkoxy or an alkanoylamino; one of R.sub.a and R.sub.b is a group of the formula hydrogen, an alkyl or a phenylalkyl or a substituted phenyalkyl a group forming a heterocycle together with the adjacent nitrogen atom and Y stands for a straight- or branched-chain alkylene which may have hydroxy group as a substituent on the chain, and the other is hydrogen, or both of R.sub.a and R.sub.b are the same or different and respectively a group of the formula .dbd.CH-- or .dbd.N--; X is CH.sub.2, S, SO, SO.sub.2 or O; and the bond designated by a broken line in its part stands for a single bond or a double bond, or their pharmaceutically acceptable salts or hydrates and their pharmaceutical uses.
Throughout the present specification, the halogen means chlorine, bromine, fluorine or iodine; the alkyl means straight- or branched-chain alkyl having 1-8 carbon atoms such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl, heptyl or octyl; the alkoxy means a straight- or branched-chain alkoxy having 1-8 carbon atoms such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, tert-butoxy, pentyloxy, hexyloxy or octyloxy; the phenylalkyl means a phenylalkyl in which the alkyl moiety is a straight- or branched-chain having 1-4 carbon atoms such as benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl or 4-phenylbutyl; the substituted phenylalkyl is a phenylalkyl having, on the phenyl ring, 1 to 3 substituent(s) selected from halogens, hydroxy, nitro, amino, cyano, trifluoromethyl, alkyls, alkoxys and alkanoylaminos; the heterocyclic group formed together with the adjacent nitrogen atom means a 5- or 6-membered heterocyclic group such as 1-py
REFERENCES:
patent: 4602019 (1986-07-01), Sircar et al.
patent: 4692447 (1987-09-01), Cignarella et al.
patent: 4755511 (1988-07-01), Warrington
patent: 4843075 (1989-06-01), Nakao et al.
patent: 4849421 (1989-07-01), Nakao et al.
Hisadome Masao
Kawakami Minoru
Nakao Toru
Tahara Tetsuya
Bernhardt E.
Shah Mukund J.
Yoshitomi Pharmaceutical Industries Ltd.
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