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    • 3. 发明授权
    • 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrates
    • 1-(5-异喹啉磺酰基)高哌嗪盐酸盐水合物
    • US5942505A
    • 1999-08-24
    • US930910
    • 1997-10-14
    • Hiromu KawakuboMasaru Ohno
    • Hiromu KawakuboMasaru Ohno
    • C07D401/12
    • C07D401/12
    • Disclosed is a 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate having a water content of from 2.5 to 15.5% by weight represented by the following formula (I): ##STR1## wherein n means a number in the range of from 1/2 to 3. Since the 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride hydrate of the present invention has excellent shapeability as compared to a 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride anhydride, a tablet having satisfactory hardness can be obtained even with a relatively low compression pressure in a tableting process. Further, due to a reduction in the compression pressure needed for tableting, various advantages are brought about, such as improved disintegratability of the resultant tablet when the tablet is orally taken, so that good dissolution of 1-(5-isoquinolinesulfonyl)homopiperazine hydrochloride from the tablet can be achieved, as well as suppression of abrasion of the die and punch used in producing tablets by compression, and the like.
    • PCT No.PCT / JP96 / 01698 Sec。 371日期1997年10月14日第 102(e)1997年10月14日PCT PCT 1996年6月19日PCT公布。 公开号WO97 / 02260 日期1997年1月23日公开是由下式(I)表示的水含量为2.5〜15.5重量%的1-(5-异喹啉磺酰基)高哌嗪盐酸氢氯化物,其中n表示在+ 由于本发明的1-(5-异喹啉磺酰基)高哌嗪盐酸水合物与1-(5-异喹啉磺酰基)高哌嗪盐酸酐相比具有优异的成形性,所以具有令人满意的硬度的片剂 即使在压片过程中压缩压力相对较低也能获得。 此外,由于压片所需的压缩压力降低,导致了各种优点,例如当口服片剂时所得片剂的崩解性提高,从而使得1-(5-异喹啉磺酰基)高哌嗪盐酸盐从 可以实现片剂,以及通过压缩抑制用于制造片剂的模具和冲头的磨损等。