Certain s-triazolo[3,4-c]thieno[2,3-e][1,4]diazepine compounds are known to exhibit useful pharmacological activities against the central nervous system such as antianxiety or anticonvulsant activities as disclosed in U.S. Pat. No. 3,904,641.
Japan. J. Pharmacol., vol. 44, p. 381-391 (1987) discloses that the similar type of the compounds exhibits antagonistic activity on platelet-activating factor (hereinunder also referred to as PAF), and further EP-A 194416 discloses that another type of the compounds having a carboxylic acid amide derivatives as the side chain exhibit antagonistic activity on PAF.
According to the elucidation of the structure of platelet-activating factor, its physiological roles have been investigated, and various PAF-induced inflammatory diseases such as allergic diseases, anaphylactic shocks, vascular diseases as DIC (disseminated intravascular coagulation syndrome), myocardial diseases, asthma, pulmonary edema and adult respiratory diseases have been known. The PAF-antagonistic compounds are considered to be very useful for the prevention and treatment of above-mentioned diseases. It is known that certain thienotriazolodiazepine compounds exhibit PAF-antagonist activity as mentioned above. However, such compounds are not sufficient in view of the separation from the effect on the central nervous system, the potency, the effectiveness by the oral administration or the duration of activity.
USPTO Backgrounds
USPTO Backgrounds