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    • 8. 发明申请
    • AROMATIC ESTERS OR AMIDES OF CARBOXYLIC ACID AND SULFONIC ACID
    • 芳香酯或羧酸和硫酸的氨基酸
    • WO1985001048A1
    • 1985-03-14
    • PCT/CH1984000127
    • 1984-08-14
    • SANDOZ AG
    • SANDOZ AGRICHARDSON, Brian, P.ENGEL, GünterGIGER, Rudolf, K., A.VASELLA, Andrea
    • C07D401/12
    • C07D221/22C07D209/36C07D221/24C07D401/12C07D405/12C07D451/04C07D451/06C07D451/12C07D451/14C07D453/02
    • Aromatic esters of amides of carboxylic acid and sulfonic acid having the formula A-B-C-D, wherein A represents groups having the formulas (I), X-Y representing -CH = CH-, -O-C-H2 or N = CH-; Z representing -CH2-, -NR3-, -O- or -S-; R1 and R2 representing hydrogen, halogen, alkyl, alkoxy, hydroxy, amino, alkylamino, dialkylamino, mercapto or alkylthio; R3 representing hydrogen, alkyl, alkenyl, aryl or aralkyl and R4, R5, R6, R7 representing hydrogen, amino, nitro, alkylamino, dialkylamino, halogen, alkoxy, alkyl, alkylanoylamino, pyrrolyl, sulfamoyl or carbamoyl; wherein B represents -CO- or -SO2-; wherein C represents -O- or -NH-; wherein D represents groups having the formulas (II), R8 representing hydrogen, alkyl, alkenyl or aralkyl and n being equal to 2, 3 or 4; acid addition salts thereof or quaternary amonium salts thereof, production process thereof and utilization thereof as analgesics, particularly as antimigraine agents and antiarhythmics.
    • 具有式A-B-C-D的羧酸和磺酸的酰胺的芳族酯,其中A表示具有式(I)的基团,表示-CH = CH-,-O-C-H 2或N = CH-的X-Y; Z表示-CH 2 - , - NR 3 - , - O-或-S-; R 1和R 2代表氢,卤素,烷基,烷氧基,羟基,氨基,烷基氨基,二烷基氨基,巯基或烷硫基; R3代表氢,烷基,烯基,芳基或芳烷基,R4,R5,R6,R7代表氢,氨基,硝基,烷基氨基,二烷基氨基,卤素,烷氧基,烷基,烷酰基氨基,吡咯基,氨磺酰基或氨基甲酰基; 其中B表示-CO-或-SO 2 - ; 其中C表示-O-或-NH-; 其中D表示具有式(II)的基团,R 8表示氢,烷基,烯基或芳烷基,n等于2,3或4; 其酸加成盐或其季铵盐,其制备方法和作为止痛剂的使用,特别是作为抗偏头痛药和抗心律失常药。
    • 9. 发明申请
    • FLUORALKYLATEDCARBAPENEM DERIVATIVES
    • 氟代甲基丙烯酸衍生物
    • WO1984000547A1
    • 1984-02-16
    • PCT/EP1983000193
    • 1983-07-23
    • SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.SANDOZ AGSANDOZ-PATENT-GMBH
    • SANDOZ-ERFINDUNGEN VERWALTUNGSGESELLSCHAFT M.B.H.SANDOZ AGSANDOZ-PATENT-GMBHMAK, Ching, PongFLIRI, Hans
    • C07D487/04
    • C07D477/20C07D205/08C07D477/10C07D499/88C07F7/10
    • Compounds of formula (I), wherein, R1 represents hydrogen or methyl and R2 represents hydrogen or lower alkyl, lower alkenyl or cycloalkyl each of which may be unsubstituted or mono- or polysubstituted by amino, mono- or di-(lower)-alkylamino, lower acylamino, carboxy, lower alkoxycarbonyl or carbamoyl; a group of formula IIc: (CH2)p-R7, wherein R7 represents phenyl or a 5- or 6-membered saturated or unsaturated heterocycle containing one or more heteroatoms selected from 0, S and/or N and which may be unsubstituted or mono- or polysubstituted by fluoro, chloro, bromo, amino, mono- or di-(lower)-alkylamino, hydroxy, lower alkoxy, mercapto, alkylthio, phenylthio, sulfamoyl, guanidino, nitro, cyano, lower acylamino, carboxyl, alkoxycarbonyl or carbamoyl and p is 0, 1, 2 or 3; or a group of formula (II), (IIa), (IIb), wherein R4, R5 and R6 may be the same or different and each represents hydrogen or lower alkyl or R4 and R6 and/or R5 and one of the CH2 groups may be joined to form a ring as may R5 and R6 in formula II and R4 and R5 in IIa and IIb, which rings may be unsubstituted or mono- or poly-substituted by alkyl, hydroxy, carboxy or di-(lower)-alkylamino, m is 2 or 3, and n is 1, 2 or 3 with the proviso that when R1 is hydrogen and the group containing it has R-configuration, R2 is other than acetylaminoethyl; or protected forms and/or physiologically-hydrolysable and acceptable ester forms thereof; in free acid or salt form or in the form of zwitter-ions. The compounds exhibit chemotherapeutic properties and are particularly indicated for use as anti-bacterially active antibiotics.
    • 式(I)化合物,其中R 1表示氢或甲基,R 2表示氢或低级烷基,低级烯基或环烷基,其各自可以是未取代的或被氨基,单 - 或二 - (低级) - 烷基氨基 ,低级酰基氨基,羧基,低级烷氧基羰基或氨基甲酰基; 式IIc的基团:(CH 2)p -R 7,其中R 7表示苯基或含有一个或多个选自O,S和/或N的杂原子的5或6元饱和或不饱和杂环,并且其可以是未取代的或单 羟基,低级烷氧基,巯基,烷硫基,苯硫基,氨磺酰基,胍基,硝基,氰基,低级酰氨基,羧基,烷氧基羰基或氨基甲酰基 p为0,1,2或3; 或式(II),(IIa),(IIb)的基团,其中R 4,R 5和R 6可以相同或不同,并且各自表示氢或低级烷基或R 4和R 6和/或R 5和一个CH 2基团 可以结合形成环,如式II中的R 5和R 6,以及IIa和IIb中的R 4和R 5,该环可以是未被取代的或被烷基,羟基,羧基或二(低级) - 烷基氨基 ,m为2或3,n为1,2或3,条件是当R 1为氢且含有R基团时,R 2为乙酰氨基乙基; 或受保护的形式和/或其生理上可水解和可接受的酯形式; 以游离酸或盐的形式或以两性离子的形式存在。 该化合物具有化学治疗性质,特别指出用作抗细菌活性抗生素。