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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。
    • 8. 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。