142355-81-5Relevant articles and documents
Buspirone derivative and pharmacy composition comprising the same
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, (2017/01/02)
The present invention relates to a buspirone derivative and a pharmaceutical composition containing the same and, more specifically, to a novel buspirone derivative and a pharmaceutical composition for treating or preventing hypertension. The buspirone derivative according to the present invention corresponds to a novel derivative of buspirone wherein buspirone have already been known to be effective in the treatment of stress-induced diseases and the novel derivative is effective in the treatment of other diseases. Also, the pharmaceutical composition for treating and preventing blood pressure disorders according to the present invention can treat or prevent blood pressure disorders such as hypertension by using the buspirone derivative to newly widen the use range of buspirone. Particularly, the buspirone derivative enables buspirone, which has been used to treat only stress-induced diseases, to be used for a new purpose of treating hypertension. Also, the present invention has an effect of treating or preventing hypertension as the cause of essential hypertension or primary hypertension is examined closely instead of artificially lowering blood pressure.
Synthesis of cyclic prodrugs of Aggrastat and its analogue with a modified phenylpropionic acid linker
Song, Xiaoping,He, Henry T.,Siahaan, Teruna J.
, p. 549 - 552 (2007/10/03)
(formula presented) 1a, n=2; 1b, n=1 The objective of this work was to synthesize cyclic prodrugs 1a and 1b from Aggrastat 2a and its analogue 2b, respectively, to improve their membrane permeation. Cyclic prodrugs 1a and 1b were formed using an ester bond between the -COOH group of Aggrastat or its analogue and the phenylpropionic acid linker 3 and an amide bond between the piperidinylamine and the -COOH group of the linker 3, respectively, as outlined in Scheme 4.