Alkylenediamine derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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Details

5142265, 544 49, 544 50, A61K 3154, C07D27902

Patent

active

057734372

DESCRIPTION:

BRIEF SUMMARY
This is a 371 of PCT/JP95/00632 filed Mar. 31, 1995.


FIELD OF THE INVENTION

The present invention relates to a novel alkylenediamine derivative which shows a function to relieve urinating contraction and therefore is of value as an active ingredient of a therapeutic agent for treating dysuria.


BACKGROUND OF THE INVENTION

Heretofore, flavoxate hydrochloride and oxybutynin hydrochloride which directly function peripherally on urinary bladder have been used as therapeutic agents for treating dysuria. However, these compounds may give certain side-effects to other organs such as digestive apparatus.
EP-0579169-A1 (Japanese Patent Provisional Publication H6-80645) describes an alkylenediamine of the formula (A): ##STR1## in which each of R.sup.1A and R.sup.2A independently represents a phenyl, naphthyl or aromatic heterocyclic group which may have one to five same or different substituents selected from the group consisting of alkyl, halogen, haloalkyl, hydroxyl, alkoxy, aryloxy, aralkyloxy, nitro, amino, alkylamino, aralkylamino, arylamino, acylamino, carboxyl, alkoxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, amide, sulfo, alkoxysulfonyl, aralkyloxysulfonyl, aryloxysulfonyl, sulfonamide, and 1H-tetrazol-5-yl; each of R.sup.3A and R.sup.4A independently represents hydrogen, alkyl, aralkyl or aryl, otherwise R.sup.3A and R.sup.4A are combined in conjunction with the nitrogen atom to which R.sup.3A and R.sup.4A are attached to form 5 to 7 membered ring which may contain oxygen, sulfur or nitrogen and which may have a substituent selected from the group consisting of alkyl, aralkyl, phenyl, hydroxyl, alkoxy, carboxyl, alkoxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, and amide; X.sup.A represents oxygen, sulfur or imino; A represents oxygen or sulfur; Z.sup.A represents --CH.sub.2 --, --CO--, or --CS--; m.sup.A is an integer of 0 to 4; n.sup.A is an integer of 0 to 4; each of p.sup.A and q.sup.A independently is an integer of 0 to 5 under the condition that the total of p.sup.A and q.sup.A is in the range of 1 to 5, or its pharmacologically acceptable salt is of value as an active ingredient of a therapeutic agent for treating dysuria, because the compound can relieve urinating contraction which is observed under high intracystic pressure, and therefore is employable for treating nervous dysuria, chronic prostatitis, chronic cystitis, dysuria caused by neurogenic bladder or unstable bladder, incontinence of urine, urgency of micturition, and residual urine.
The object of the invention is to provide a novel alkylenediamine derivative showing a function to relieve urinating contraction which is observed under high intracystic pressure.


DISCLOSURE OF THE INVENTION

The present invention resides in an alkylenediamine derivative of benzothiazine type which is represented by the formula (1): ##STR2## in which
R.sup.1 represents an atom or a group selected from the group consisting of hydrogen, alkyl having 1-8 carbon atoms, halogen, haloalkyl having 1-4 carbon atoms, hydroxyl, alkoxy having 1-8 carbon atoms, aryloxy having 4-10 carbon atoms, aralkyloxy having 5-14 carbon atoms (its alkyl portion has 1-4 carbon atoms), nitro, amino, cyano, alkylamino having 1-8 carbon atoms, aralkylamino having 5-14 carbon atoms (its alkyl portion has 1-4 carbon atoms), arylamino having 4-10 carbon atoms, aliphatic acylamino having 1-8 carbon atoms, carboxyl, alkoxycarbonyl having 2-9 carbon atoms, aralkyloxycarbonyl having 6-15 carbon atoms (its alkyl portion has 1-4 carbon atoms), aryloxycarbonyl having 5-11 carbon atoms, carbamoyl, sulfo, alkoxysulfonyl having 1-8 carbon atoms, aralkyloxysulfonyl having 5-14 carbon atoms (its alkyl portion has 1-4 carbon atoms), aryloxysulfonyl having 4-10 carbon atoms, sulfonamide, and 1H-tetrazol-5-yl;
R.sup.2 represents hydrogen, hydroxyl, alkyl having 1-8 carbon atoms, alkenyl having 2-9 carbon atoms, alkoxy having 1-8 carbon atoms, or an aryl having 4-10 carbon atoms, aralkyl having 5-14 carbon atoms (its alkyl portion has 1-4 carbon atoms) or aromatic heterocyclic group which may

REFERENCES:
patent: 3712889 (1973-01-01), Sianesi et al.
patent: 4272531 (1981-06-01), DeMarinis
patent: 5037841 (1991-08-01), Schohe et al.
patent: 5274097 (1993-12-01), Schohe et al.
Orazi et al., J. Het. Chem., 23, 1701-8, Nov. 1986.
Sianesi et al., J. Med. Chem., 16(10), 1133-37, 1973.

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