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    • 7. 发明授权
    • Benzenesulfonylamine compounds, process for preparing them and
pharmaceutical compositions
    • 苯磺酰胺化合物,其制备方法和药物组合物
    • US6013667A
    • 2000-01-11
    • US32587
    • 1998-02-27
    • Gilbert LavielleBernard CimetiereTony VerbeurenSerge SimonetJean-Jacques Descombes
    • Gilbert LavielleBernard CimetiereTony VerbeurenSerge SimonetJean-Jacques Descombes
    • A61K31/18A61K31/195A61K31/215A61P7/02A61P9/08A61P9/10C07C303/40C07C311/16C07C311/19C07C311/21C07C381/00A61K31/21
    • C07C311/19C07C311/21C07C381/00C07C2102/10
    • Compounds of formula (I): in which:R.sub.a and R.sub.b, identical or different, represent hydrogen or alkyl or together form a bond,R.sub.C represents hydroxyl optionally substituted alkoxy, or optionally substituted amino,R.sub.1 represents hydrogen or --O--NO.sub.2, --O--NO, or --S--NO,R.sub.2 and R.sub.3, identical or different, represent hydrogen, alkyl, or optionally substituted phenyl,X represents oxygen or --NH--CO--,m represents 0 or 1,n represents an integer such that 0.ltoreq.n.ltoreq.6,p represents 0 or 1,R.sub.4 represents hydrogen, optionally substituted alkyl, optionally substituted phenyl, or a group as defined in the description,R.sub.5 represents hydrogen or alkyl,R.sub.6 represents hydrogen or alkyl,or R.sub.5 and R.sub.6 together form a chain --(CH.sub.2).sub.t -- in which t represents 1 or 2,q represents 0, 1, or 2,r represents an integer such that 0.ltoreq.r.ltoreq.6,R.sub.d and R.sub.e, identical or different, represent hydrogen, halogen, alkyl, alkoxy, hydroxyl, or trihaloalkyl, it being understood that at least one --O--NO.sub.2, O--NO, or S--NO groupis present in R.sub.1, R.sub.4 or R.sub.c ; process of preparing same, pharmaceutical compositions thereof, and their use as TXA.sub.2 -receptor antagonists and NO donors.
    • 式(I)化合物:其中:R a和R b相同或不同,代表氢或烷基或一起形成键,RC表示羟基任选取代的烷氧基或任选取代的氨基,R 1表示氢或-O-NO 2, O-NO或-S-NO,R 2和R 3相同或不同,表示氢,烷基或任选取代的苯基,X表示氧或-NH-CO-,m表示0或1,n表示整数,使得 0表示0或1,R4表示氢,任选取代的烷基,任选取代的苯基或说明书中定义的基团,R 5表示氢或烷基,R 6表示氢或烷基,或 R5和R6一起形成链 - (CH 2)t-,其中t表示1或2,q表示0,1或2,r表示0以及r和r的整数, 相同或不同,代表氢,卤素,烷基,烷氧基,羟基或三卤代烷基,应理解至少有一个-O-NO 2,O-NO或S-NO基团存在于 R1,R4或Rc; 其制备方法,其药物组合物及其作为TXA2受体拮抗剂和NO供体的用途。