Fiber-reactive dioxazine dyes containing two vinylsulfonyl moieties

    公开(公告)号:US4997937A

    公开(公告)日:1991-03-05

    申请号:US422339

    申请日:1989-10-16

    CPC classification number: C09B62/5033 C07C317/04

    Abstract: Dyes suitable for dyeing and printing cellulose-containing fiber materials which produce blue dyeings and prints having good fastness properties. These dyes are of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently of the other hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenoxy, carboxyl carbamoyl or C.sub.1 -C.sub.4 alkanoylamino; R.sub.3 is hydrogen, sulfo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen, carboxyl, carbamoyl, N-C.sub.1 -C.sub.4 alkylcarbamoyl, N,N-di-C.sub.1 -C.sub.4 alkylcarbamoyl, C.sub.1 -C.sub.4 alkylsulfonyl, sulfamoyl, N-C.sub.1 -C.sub.4 alkylsulfamoyl or N,N-di-C.sub.1 -C.sub.4 alkylsulfamoyl; R.sub.4 is a radical of the formula ##STR2## R.sub.5 and R.sub.6 are independently of each other hydrogen or unsubstituted or hydroxyl-, sulfo-, sulfato-, carboxyl-, cyano-, halogen-, C.sub.1 -C.sub.4 alkoxycarbonyl-, C.sub.1 -C.sub.4 alkanoyloxy- or carbamoyl-substituted and uninterrupted or, except in the case of methyl, --O--, --S-- or --NH--interrupted C.sub.1 -C.sub.6 alkyl; R' is hydrogen or C.sub.1 -C.sub.6 alkyl; t is an integer from 0 to 4; the phenyl radical (a) is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl substituted by hydroxyl-, sulfo or sulfato, C.sub.1 -C.sub.4 alkoxy, halogen, sulfo, carboxyl or hydroxy, and A is a radical of the formula ##STR3## where R' is as defined above, (alk) is C.sub.1 -C.sub.6 alkylene, T is hydrogen, halogen, hydroxyl, sulfato, carboxyl, cyano, C.sub.1 -C.sub.4 alkanoyloxy, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl or a radical --SO.sub.2 --Z, V is hydrogen, substituted or unsubstituted C.sub.1 -C.sub.4 alkyl or a radical of the formula -(alk)--CH.sub.2 --SO.sub.2 --Z, where (alk) is as defined above, Z is a radical of the formula --CH.dbd.CH.sub.2 l or --CH.sub.2 --CH.sub.2 --Y, Y is a leaving group selected from the group consisting of --OSO.sub.3 H, --SSO.sub.3 H, --OCOCH.sub.3, --OCO--C.sub.6 H.sub.5, OPO.sub.3 H.sub.2, --Cl, Br, --F, ##STR4## p, q and r are each independently of the others an integer from 1 to 6.

    Aminobenzamide derivatives
    83.
    发明授权
    Aminobenzamide derivatives 失效
    氨基苯甲酰胺衍生物

    公开(公告)号:US4985595A

    公开(公告)日:1991-01-15

    申请号:US279256

    申请日:1988-12-01

    CPC classification number: C07D295/192

    Abstract: Aminobenzamide derivatives of the formula (I) ##STR1## wherein: R.sub.1 and R.sub.2 each represents a lower alkoxy group,R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower acyl group, a lower alkoxycarbonyl group or --R.sub.5 --SO.sub.3 Z, wherein R.sub.5 represents a lower alkylene group and Z represents an alkali metal or an alkaline earth metal,R.sub.4 represents an amino group, a morpholino group or a lower alkylamino group which may be substituted with a hydroxyl group at the alkyl moiety thereof, with the proviso that, when R.sub.3 represents a hydrogen atom, R.sub.4 cannot be an amino group,Y represents a hydrogen atom, a halogen atom or a lower alkoxy group,n represents an integer of from 1 to 6,and salts thereof; are disclosed. These compounds have excellent anti-peptic ulcer activities, and chemical and physical stabilities.

    Abstract translation: 式(I)的氨基苯甲酰胺衍生物其中:R 1和R 2各自表示低级烷氧基,R 3表示氢原子,低级烷基,低级酰基,低级烷氧基羰基或-R 5 - SO 3 Z,其中R 5表示低级亚烷基,Z表示碱金属或碱土金属,R 4表示可以在其烷基部分被羟基取代的氨基,吗啉代基或低级烷基氨基, 条件是当R3表示氢原子时,R4不能为氨基,Y表示氢原子,卤原子或低级烷氧基,n表示1〜6的整数,及其盐类; 被披露。 这些化合物具有优异的抗消化性溃疡活性,以及​​化学和物理稳定性。

    Spasmolytically active tertiary amine derivatives
    86.
    发明授权
    Spasmolytically active tertiary amine derivatives 失效
    分解活性的叔胺衍生物

    公开(公告)号:US4889849A

    公开(公告)日:1989-12-26

    申请号:US294997

    申请日:1989-01-09

    CPC classification number: C07D295/194 C07D211/32 C07D211/58

    Abstract: The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is phenyl, or a 5- or 6-membered aromatic group containing 1 or 2 of the following hetero atoms: oxygen and/or sulphur and/or nitrogen;R.sub.1 and R.sub.2 may be equal or different and are hydrogen or substituents;R.sub.3 is a hydrogen atom or, together with R.sub.4, may form a ring consisting of 6 or 7 carbon atoms;R.sub.4 is a hydrogen atom or alkyl group having 1-3 carbon atoms;R.sub.5 is a straight, branched or cyclic alkyl group having 1-4 carbon atoms;R.sub.6 is a straight or branched, saturated or unsaturated alkylene group having a chain length of 2-6 carbon atoms;Z is the group NR.sub.12, wherein R.sub.12 is a hydrogen atom or an alkyl group having 1-3 carbon atoms, or Z is an oxygen atom;n has the value 0 or 1;X is a carbonyl group, thiocarbonyl group or SO.sub.2 group;R.sub.7 and R.sub.8, together with the nitrogen atom to which they are bound, constitute a fully or partly saturated heterocyclic ring consisting of 5-8 ring atoms and which may comprise in addition an O, N or S-atom as the second hetero atom, and may be substituted.

    Abstract translation: 本发明涉及式(1)的新的解压活性叔胺衍生物及其盐,其中符号具有以下含义:& A是苯基或5-或6-元芳基 含有1或2个以下杂原子:氧和/或硫和/或氮; R 1和R 2可以相同或不同,为氢或取代基; R3是氢原子,或者与R4一起可以形成由6或7个碳原子组成的环; R4是氢原子或具有1-3个碳原子的烷基; R5是具有1-4个碳原子的直链,支链或环状烷基; R6是链长2-6个碳原子的直链或支链饱和或不饱和亚烷基; Z是NR12基团,其中R12是氢原子或具有1-3个碳原子的烷基,或Z是氧原子; n的值为0或1; X是羰基,硫代羰基或SO2基团; R7和R8与它们所结合的氮原子一起构成由5-8个环原子组成的完全或部分饱和的杂环,并且另外可以包含作为第二杂原子的O,N或S-原子, 并且可以被替代。

    1,4-Disubstituted piperazines having dopaminergic activity
    88.
    发明授权
    1,4-Disubstituted piperazines having dopaminergic activity 失效
    具有多巴胺能活性的1,4-二取代哌嗪

    公开(公告)号:US4874765A

    公开(公告)日:1989-10-17

    申请号:US41206

    申请日:1987-04-22

    CPC classification number: C07D295/185 C07D295/088

    Abstract: The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the general formula (I) ##STR1## R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and stand for hydrogen or halogen or a trihalomethyl, lower alkyl, lower alkoxy, nitro, hydroxyl, aralkyloxy or an 1-(2-propenyl-4-piperazinyl) group;R.sub.5 stands for hydrogen or a C.sub.1-4 alkyl group;R.sub.6 represents a C.sub.3-6 alkyl, alkenyl, alkynyl group or a ##STR2## group, wherein R.sub.7 means a C.sub.2-5 alkyl, alkenyl or alkinyl group; andis 2 or 3,with the provisos that:R.sub.6 is different from isopropyl, n-butyl and isobutyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2;R.sub.6 is different from isopropyl group when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-chloro and n is 2; or when R.sub.2, R.sub.3, R.sub.4 and R.sub.5 stand for hydrogen, R.sub.1 means 2-methyl group and n is 2; andR.sub.6 is different from propionyl group when R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen and n means 2.The compounds of the general formula (I) are therapeutically useful for the treatment of diseases arising from a hypofunction of the dopaminergic system.

    Abstract translation: 本发明涉及通式(I)的新的1,4-二取代哌嗪衍生物,其药学上可接受的酸加成盐和季铵盐,含有它们的药物组合物及其制备方法。 在通式(I)中,R 1,R 2,R 3和R 4相同或不同,代表氢或卤素或三卤代甲基,低级烷基,低级烷氧基,硝基,羟基,芳烷氧基或1- (2-丙烯基-4-哌嗪基)基团; R5代表氢或C1-4烷基; R6表示C3-6烷基,烯基,炔基或者IMAGE基团,其中R7表示C2-5烷基,烯基或炔基; 并且为2或3,条件是:当R 2,R 3,R 4和R 5代表氢时,R 6不同于异丙基,正丁基和异丁基,R 1表示2-氯且n为2; 当R2,R3,R4和R5代表氢时,R6不同于异丙基,R1表示2-氯,n是2; 或当R2,R3,R4和R5代表氢时,R1表示2-甲基,n表示2; 当R 1,R 2,R 3,R 4和R 5为氢且n表示2时,R 6与丙酰基不同。通式(I)的化合物可治疗用于治疗多巴胺能系统功能低下的疾病。

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