Tracheal smooth muscle relaxants

Details Tracheal smooth muscle relaxants Tracheal smooth muscle relaxants

2000-06-30

2002-12-17

Cook, Rebecca (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S826000

Reexamination Certificate

active

06495592

ABSTRACT:

TECHNICAL FIELD
The present invention relates to a tracheal smooth muscle relaxant in which a derivative of dibenz[b,f]oxepin or dibenzo[b,f]thiepin derivatives is an effective ingredient.
BACKGROUND ART
Xanthine derivatives such as theophylline and &bgr;
2
agents such as salbutamol have been known as drugs having a relaxing action to tracheal smooth muscles.
However, in those drugs which have been already known, their relaxing action of tracheal smooth muscles in airway diseases and pulmonary diseases such as bronchial asthma, acute and chronic bronchitis, pulmonary emphysema and upper esophagitis is not satisfactory in terms of a balance with the side effect.
In view of the above, an object of the present invention is to offer drugs having novel relaxing action to tracheal smooth muscle exhibiting far better action to airway diseases, etc.
DISCLOSURE OF THE INVENTION
In order to solve the above problems, the present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient.
[In the formula, X and Y each is any group selected from a group consisting of CH
2
, CHW
1
(where W
1
is halogen atom, hydroxyl group or lower alkoxy group) and C═O when the bond of X and Y is a single bond, while when it is a double bond, X and Y each is any group selected from a group consisting of CH and COW
2
(where W
2
is lower alkyl group or lower alkylcarbonyl group); Z is O, S, S═O or SO
2
; and R
1
~R
8
each is selected from a group consisting of hydrogen atom, VR
9
(where V is O, S, S═O or SO
2
; and R
9
is hydrogen atom, lower alkyl group, hydroxy lower alkyl group, lower acyl group, trihalomethyl group or carboxyl lower alkyl group), carboxyl lower alkyl group, hydroxy lower alkyl group, hydroxy lower alkenyl group, hydroxy lower alkynyl group, halogen atom, lower alkyl group, lower alkyl ketone, trihalomethyl group, trimethylsilylethynyl, nitro group, amino group, N-carbonyl lower alkyl group, lower alkylphenyl group and phenyl group].
BEST MODES FOR CONDUCTING THE INVENTION
As mentioned above, the present invention offers a tracheal muscle relaxant containing the dibenz[b,f]oxepin and dibenzo[b,f]thiepin derivatives represented by the above formula (1) or salt thereof as an effective ingredient and, in the formula (1), “lower alkyl” for R
1
~R
8
and R
9
means straight chain, branched chain or cyclic alkyl chain having up to eight carbon atoms while the pharmacologically (pharmaceutically) acceptable salt means sodium salt, potassium salt, calcium salt, ammonium salt, aluminum salt, etc.
The compound represented by the formula (1) has an excellent relaxant action to tracheal smooth muscle and has low toxicity and, therefore, it can be effectively used for airway diseases such as bronchia asthma and bronchitis, diseases accompanied by reversible obstruction of airway, asthma, acute and chronic bronchitis, chronic obstructive pulmonary diseases such as pulmonary emphysema, etc.
Incidentally, the above-mentioned compound and salt thereof can be manufactured by various chemical synthetic means and can be made into various dosage forms by conventional techniques in pharmaceutical preparations including oral preparations such as diluted powder, granules, tablets, coated tablets, ampoules and capsules; subcutaneous, intramuscular or intravenous injections; suppositories; etc. In the manufacture of those preparations, various additives such as commonly used diluents, binders, disintegrating agents, pH adjusting agents and solubilizers may be appropriately used. Dose of the above-mentioned compound of the present invention or salt thereof to a patient to be treated may vary depending upon age, type and symptom of disease, etc. of the patient but, usually, 1~5,000 mg/day may be administered to an adult once to several times daily.
As hereunder, methods for the manufacture of the dibenz[b,f]oxepin and dibenzo[b,f]thiepin derivatives which are effective ingredients for tracheal smooth muscle relaxants in accordance with the present invention, the result of the test of those compounds on tracheal smooth muscle relaxation, etc. will be exemplified whereby the embodiments of the present invention will be illustrated in more detail.
It goes without saying that the present invention is never limited by the following exemplifications.


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