Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters
Reexamination Certificate
2000-12-20
2003-02-11
Vollano, Jean F. (Department: 1621)
Organic compounds -- part of the class 532-570 series
Organic compounds
Carboxylic acid esters
C560S037000, C562S444000, C564S192000
Reexamination Certificate
active
06518450
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention pertains to a compounded, innovative guaiacoxypropanolamine structures, upon laboratory testing on animals, has proven that it pharmacologically possesses &agr;/&bgr;-adrenergic blocking activity.
2. Background of the Invention
Adrenergic stimulant &bgr; blocker has been in use for 26 years in clinical application; currently, &bgr;-adrenergic blocker is not only used in cardiovascular diseases such as high blood pressure, angina-pectoris and cardiac arrhythmia, it is also used in symptoms of thyroid disorders, cardiomegalia, myocardial infarction, migraine, glaucoma, and gastric ulcer. In fact, it has a wide range of application. Yet traditional &bgr; blocker still has some unavoidable side-effects, such as it suppresses the cardiovascular function, increases the surrounding and artery vascular resistance, and restricts its clinical application. Therefore, where cardiolegalia is caused by coronary artery cramp, it is not suitable to prescribe&bgr;blocker for treatment. Recently developed medication that combines &agr; and &bgr; blockers has been used in treating some of the coronary vesicular diseases as it reduces the side-effect of traditional &bgr; blocker on one hand, and avoids reversal tachycardia caused by &bgr; blocker that generates a cardiac enlargement on the other. Typical &agr;/&bgr; blockers include labetalol(Trandate®), which is often used on patients suffering from emergency hypertension.
3. Prior Techniques
In terms of exploring chemical structure and structural activity relationship(SAR) which indicate that the structure of coxyethylamine has a blocking activity, there have been Augestein al et. in 1964, while Kierstead, R. W. al. et. have published in
J. Med. Chem
., Vol. 26, pp. 1561-69, 1983 that aryloxypropanolamine is the basic structure of &bgr; blocker. In addition, many ingredients found in Chinese traditional herbs also contain aryl groups, thus it inspires the interest in locating the composition that contains aryl, which include eugenol, isoeugenol, ferulic acid, capsaicin, and by using chemical reaction to infuse propanol-amine first, and then infusing the structure of guaiacolethylamine to enable the &agr;blocking activity, compounds such as eugenodilol, isoeugendilol, ferulidilol, capsinodilol are obtained. It is then further explored whether the compounded chemicals possess &agr;, &bgr; blocking activities, while examining their pharmaceutical properties.
SUMMARY OF THE INVENTION
The primary objective of this invention is to disclose a novel guaiacolethylamine structure as shown in formula I, and its compounding method.
One other objective of this invention is to utilize maximal experiment to verify that Formula I compound does possess &agr;/&bgr; guaiacolethylamine blocking activity.
This invention has one more objective, which is to take the compound in Formula I as the main ingredient and add various definitives so that the pharmaceutic combinations produced will possess &agr;/&bgr; guaiacolethylamine blocking activity.
REFERENCES:
patent: 3857891 (1974-12-01), Holmes et al.
patent: 3934032 (1976-01-01), Barrett et al.
patent: 4165384 (1979-08-01), Carlsson et al.
CA:131:242972 abs of JP11255719 Aug. 1999.*
CA: 132:137174 abs of WO2000005193 Feb. 2000.
Chang Chi Ping
National Science Council
Pacific Law Group LLP
Vollano Jean F.
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