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    • 2. 发明授权
    • Sulfonic acid derivative and its pharmaceutical application
    • 磺酸衍生物及其制药应用
    • US5496849A
    • 1996-03-05
    • US244141
    • 1994-05-17
    • Kiyotaka OhnoAtsushi OhtakeShintaro NishioKazuhiro HoshiShunji Tsukamoto
    • Kiyotaka OhnoAtsushi OhtakeShintaro NishioKazuhiro HoshiShunji Tsukamoto
    • C07D307/93A61K31/34C07D307/78C07D307/80
    • C07D307/93
    • The present invention discloses sulfonamide derivative represented by the following general formula: ##STR1## [wherein, R.sub.1 is(i) --COOR.sub.2 (where, R.sub.2 is (1) hydrogen, (2) a pharmacologically acceptable cation, or (3) an alkyl having 1 to 14 carbon atoms) or,(ii) --C(.dbd.O)--R.sub.3 (wherein, R.sub.3 represents an alkyl having 1 to 4 carbon atoms); A is(i) --(CH.sub.2)n-- (wherein, n represents an integer of 0 to 3),(ii) --CH.dbd.CH--, or the group:(iii) --O--C(R.sub.4) (R.sub.5)-- (wherein, R.sub.4 and R.sub.5 represent (1) hydrogen or (2) an alkyl having 1 to 4 carbon atoms, and R.sub.4 and R.sub.5 may be identical or different); and,w is NH or --O--], as well as a thromboxane A2 receptor antagonistic drug having said derivative for its active ingredient.Since the compound of the present invention has excellent thromboxane A2 receptor antagonistic action, it can be used as a thromboxane A2 receptor antagonist of high activity and long duration.
    • PCT No.PCT / JP93 / 01339 Sec。 371日期:1994年5月17日 102(e)日期1994年5月17日PCT提交1993年9月17日PCT公布。 出版物WO94 / 06785 日本3月3日公开本发明公开了由以下通式表示的磺酰胺衍生物:其中,R 1为(ⅰ)-COOR 2(其中,R 2为(1)氢),(2)药理学上可接受的阳离子 ,或(3)具有1至14个碳原子的烷基)或(ii)-C(= O)-R 3(其中,R 3表示具有1至4个碳原子的烷基); A是(i) - (CH 2)n - (其中,n表示0至3的整数),(ii)-CH = CH-或基团:(iii)-OC(R4)(R5) - ( 其中,R4和R5表示(1)氢或(2)具有1至4个碳原子的烷基,R4和R5可以相同或不同); 和w是NH或-O-],以及具有所述衍生物作为其活性成分的血栓素A2受体拮抗药。 由于本发明化合物具有优异的血栓素A2受体拮抗作用,因此可用作活性高且持续时间长的血栓烷A2受体拮抗剂。
    • 5. 发明授权
    • 2,5,6,7-tetranor-4,8-inter-m-phenylene PGI.sub.2, derivative,
manufacturing process thereof and its use
    • 2,5,6,7-四去甲-4,8-​​间间亚苯基PGI 2,其衍生物及其制备方法及其用途
    • US5401768A
    • 1995-03-28
    • US90995
    • 1993-07-13
    • Kiyotaka OhnoToshiya TakahashiAtsushi OhtakeHisanori WakitaShintaro Nishio
    • Kiyotaka OhnoToshiya TakahashiAtsushi OhtakeHisanori WakitaShintaro Nishio
    • C07D307/93C07D407/14C07D493/04A61K31/34
    • C07D407/14C07D307/93C07D493/04
    • Disclosed are 2,5,6,7-tetranor-4,8-inter-m-phemylene PGI.sub.2 derivatives such as 16-methyl-2,5,6,7-tetranor-4,8-inter-m-phenylene PGI.sub.2 and methyl ester thereof, 17-methyl-2,5,6,7-tetranor-4,8-inter-m-phenylene PGI.sub.2 and methyl ester thereof, 15-phenyl-2,5,6,7,16,17,18,19,20-nonanor-4,8-inter-m-phenylene PGI.sub.2, 16-methyl-17-phenyl-2,5,6,7,18,19,20-heptanor-4,8-inter-m-phenylene PGI.sub.2, 16,16-dimethyl-17-phenyl-2,5,6,7,18,19,20-heptanor-4,8-inter-m-phenylene PGI.sub.2, 16-methyl-16-phenoxy-2,5,6,7,17,18,19,20-octanor-4,8-inter-m-phenylene PGI.sub.2, 16-methyl-16-phenoxy-2,5,6,7,18,19,20-heptanor-4,8-inter-m-phenylene PGI.sub.2 and methyl ester thereof, and 3-decarboxy-3-hydroxymethyl-16-methyl-16-phenoxy-2,5,6,7,18,19,20-heptanor-4,8-inter-m-phenylene PGI.sub.2, which are useful as pharmaceuticals.These compounds are useful as an antiulcer drug, antihypertensive drug, antithrombus drug or the like.
    • PCT No.PCT / JP88 / 01048 Sec。 371日期1989年8月14日 102(e)日期1989年8月14日PCT提交1988年10月14日PCT公布。 出版物WO89 / 03387 日期:1989年4月20日。公开的是2,5,6,7-四去甲-4,8-​​间m-亚氨​​基PGI 2衍生物,如16-甲基-2,5,6,7-四去甲-4,8- 间 - 亚苯基PGI 2及其甲酯,17-甲基-2,5,6,7-四酮-4,8-​​间 - 间 - 亚苯基PGI 2及其甲酯,15-苯基-2,5,6, 7,16,17,18,19,20-壬腈-4,8-​​间间 - 亚苯基PGI2,16-甲基-17-苯基-2,5,6,7,18,19,20-庚酮-4 ,8-间 - 间 - 亚苯基PGI2,16,16-二甲基-17-苯基-2,5,6,7,18,19,20-庚烷-4,8-​​间间苯撑PGI2,16-甲基 -16-苯氧基-2,5,6,7,17​​,18,19,20-辛腈-4,8-​​间间苯撑PGI2,16-甲基-16-苯氧基-2,5,6,7, 18,19,20-庚酮-4,8-​​间 - 间 - 亚苯基PGI 2及其甲酯和3-脱羧基-3-羟甲基-16-甲基-16-苯氧基-2,5,6,7,18, 19,20-庚酮-4,8-​​间间 - 亚苯基PGI2,其可用作药物。 这些化合物可用作抗溃疡药,抗高血压药,抗血栓药物等。
    • 10. 发明授权
    • Detector device for mixing ratio for gasoline and alcohol or the like
    • 用于汽油和酒精等的混合比的检测装置
    • US4912319A
    • 1990-03-27
    • US160632
    • 1988-02-26
    • Shigeru MiyataYoshihiro MatsubaraKiyotaka Ohno
    • Shigeru MiyataYoshihiro MatsubaraKiyotaka Ohno
    • G01N21/41G01J1/16G01J1/44G01N21/43G01N21/85
    • G01N21/43G01J2001/1636G01J2001/444G01N21/85G01N2201/0621Y10S250/903
    • A detector device for mixing ratio for gasoline and alcohol include an optically permeable column, one end of which is coated with a light-reflective layer. The circumferential surface of the column is at least partly immersed in mixing liquid of gasoline and alcohol.The light beams enter the column to be incident on said circumferential surface of the column and reflect from the circumferential surface to be incident on said light reflective-layer to reflect therefrom. The reflected light beams impinge on a photo diode which outputs in accordance with the intensity of the light beams impinged.The diametrical and lengthwise dimension of the column being determined such as to provide incidence angles of the reflected light beams changing from a minimum angle corresponding to the critical angle when the mixing liquid ratio is at the lower limit of the predetermined range to a maximum angle corresponding to the critical angle when the mixing liquid ratio is at the upper limit of the predetermined range.
    • 用于汽油和醇的混合比的检测器装置包括光学透析柱,其一端涂覆有光反射层。 柱的圆周表面至少部分浸没在汽油和酒精的混合液体中。 光束进入柱入射到柱的所述圆周表面上并从圆周表面反射入射到所述光反射层上以从其反射。 反射光束照射到根据照射的光束的强度输出的光电二极管。 确定柱的直径和纵向尺寸,以便当混合液比在预定范围的下限至对应的最大角度时,提供从与临界角对应的最小角度改变的反射光束的入射角 当混合液体比例在预定范围的上限时达到临界角。