Esters
    61.
    发明授权
    Esters 失效
    酯类

    公开(公告)号:US4708441A

    公开(公告)日:1987-11-24

    申请号:US766318

    申请日:1985-08-16

    摘要: Compounds of the formula ##STR1## wherein X.sup.2 is a single covalent bond or --COO--; X.sup.1 is a single covalent bond, --COO--, --CH.sub.2 CH.sub.2 -- or when X.sup.2 is --COO--, X.sup.1 also can be p--C.sub.6 H.sub.4 --, p--C.sub.6 H.sub.4 --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 --p--C.sub.6 H.sub.4, p--C.sub.6 H.sub.4 --COO-- or --COO--p--C.sub.6 H.sub.4 ; ring A is a benzene ring or trans-1,4-cyclohexylene; ring B is a benzene ring or when X.sup.2 is --COO-- and X.sup.1 is a single covalent bond, --COO-- or --CH.sub.2 CH.sub.2 --, ring B also can be trans-1,4-cyclohexylene; Z.sup.1, Z.sup.2 and Z.sup.3 individually are hydrogen or when positioned on a benzene ring which is not linked directly with a further ring via a single covalent bond, Z.sup.1, Z.sup.2 and Z.sup.3 also can be halogen, cyano or methyl; Y.sup.2 is cyano, nitro, 2,2-dicyanovinyl or when Y.sup.1 is hydrogen Y.sup.2 also can be 2,2-dicyano-1-methylvinyl; Y.sup.1 is halogen, cyano, C.sub.1 -C.sub.3 -alkyl or, when X.sup.1 includes a benzene ring of --COO-- or Y.sup.2 is nitro or at least one of Z.sup.1 and Z.sup.2 is other than hydrogen, Y.sup.1 also can be hydrogen; and R.sup.1 is C.sub.1 -C.sub.12 -alkyl or when positioned on a benzene ring R.sup.1 also can be C.sub.1 -C.sub.12 -alkoxy, their manufacture and use in liquid crystalline mixtures are described.

    摘要翻译: 其中X 2是单个共价键或-COO-; X 1是单个共价键,-COO - , - CH 2 CH 2 - 或当X 2是-COO-时,X 1也可以是对-C 6 H 4 - ,p-C 6 H 4 -CH 2 CH 2 - , - CH 2 CH 2-p-C 6 H 4,p-C 6 H 4 -CO 2 - 或-COO-p-C6H4; 环A是苯环或反式-1,4-亚环己基; 环B为苯环,或者当X2为-COO-且X1为单一共价键时,可以为-COO-或-CH2CH2-,环B也可为反式-1,4-亚环己基; Z1,Z2和Z3分别为氢或当位于不与另一个环通过单个共价键直接连接的苯环上时,Z 1,Z 2和Z 3也可以是卤素,氰基或甲基; Y2是氰基,硝基,2,2-二氰基乙烯基或当Y1是氢时,Y2也可以是2,2-二氰基-1-甲基乙烯基; Y1是卤素,氰基,C1-C3-烷基,或当X1包括-COO-或Y2的苯环是硝基或Z1和Z2中的至少一个不是氢时,Y1也可以是氢; R1为C1-C12烷基,或者当位于苯环R1上时,也可以是C1-C12-烷氧基,它们在液晶混合物中的制备和应用被描述。

    Nicotinates of alkanediols having hypolipidaemic activity and
pharmaceutical compositions containing them
    65.
    发明授权
    Nicotinates of alkanediols having hypolipidaemic activity and pharmaceutical compositions containing them 失效
    具有降血脂活性的烷二醇的烟碱和含有它们的药物组合物

    公开(公告)号:US4454145A

    公开(公告)日:1984-06-12

    申请号:US369579

    申请日:1982-04-19

    摘要: New compounds of general formula ##STR1## and salts therewith of pharmaceutically acceptable acids, wherein R and R.sub.1 independently represent a hydrogen atom or a straight or branched alkyl group having from 1 to 5 carbon atoms, and n is an integer from 4 to 12; and of general formula ##STR2## wherein R'.sub.1 represents a straight or branched alkyl group having from 2 to 4 carbon atoms, W represents hydroxymethyl or the COOM group in which M stands for a hydrogen atom, an alkali metal or an equivalent of an alkali earth metal and n is an integer from 6 to 8. The compounds are useful in treating hyperlipidaemia.

    摘要翻译: 新的通式为I的化合物及其与药学上可接受的酸的盐,其中R和R 1独立地表示氢原子或具有1至5个碳原子的直链或支链烷基,n是4至12的整数 ; 和通式为其中R'1表示具有2至4个碳原子的直链或支链烷基,W表示羟甲基或COOM基团,其中M代表氢原子,碱金属或等同物 碱土金属,n为6-8的整数。这些化合物可用于治疗高脂血症。

    Pyrrolo[3,4-d][2]benzazepines
    67.
    发明授权
    Pyrrolo[3,4-d][2]benzazepines 失效
    吡咯并[3,4-d] [2]苯并吖庚因

    公开(公告)号:US4428878A

    公开(公告)日:1984-01-31

    申请号:US404664

    申请日:1982-08-03

    摘要: The present invention relates to compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR2## wherein R.sub.11 is hydrogen, hydroxy, alkoxy, amino and mono- or di-lower alkylamino; and R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, hydroxymethyl, the group ##STR3## wherein R.sub.11 is hydrogen, hydroxy, trihalomethyl, alkoxy, amino and mono- or di-lower alkylamino; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or alkynyl, the group ##STR4## C.sub.2 to C.sub.7 carboxylic acids and the esters and amides thereof, hydroxy C.sub.2 to C.sub.7 alkyl and amino or mono- or di-lower alkyl amino C.sub.2 to C.sub.7 alkyl; R.sub.4 is selected from the group consisting of hydrogen, acyloxy, straight chain lower alkoxy and hydroxy; R.sub.5 is halogen or hydrogen; R.sub.6 is halogen with the proviso that if one of R.sub.1 or R.sub.3 is hydroxymethyl or the group ##STR5## wherein R.sub.11 is as above then the remaining substituent is selected from the group consisting of hydrogen, lower alkyl and C.sub.3 to C.sub.7 alkenyl or alkynyl, and R.sub.2 is hydrogen and the further proviso that (A) when R.sub.4 is acyloxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is the group ##STR6## (B) when R.sub.4 is hydroxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl, and R.sub.2 is hydrogen or (C) when R.sub.4 is alkoxy then R.sub.1 and R.sub.3 are hydrogen, lower alkyl, C.sub.3 to C.sub.7 alkenyl or C.sub.3 to C.sub.7 alkynyl,and the pharmaceutically acceptable salts thereof which exhibit activity as sedatives and anxiolytics.Also disclosed are certain 5,6 dihydro derivatives, N-oxides and quarternary iminium salts of the pyrrolobenzazepines.

    摘要翻译: 本发明涉及式IMA的化合物,其中R 1选自氢,低级烷基,C 3至C 7链烯基或炔基,羟甲基,其中R 11为氢,羟基,烷氧基,氨基 和单 - 或二 - 低级烷基氨基; R 3选自氢,低级烷基,C 3至C 7烯基或炔基,羟甲基,其中R 11为氢,羟基,三卤甲基,烷氧基,氨基和一或二低级烷基氨基; R2选自氢,低级烷基,C3至C7烯基或炔基,基团C2至C7羧酸及其酯和酰胺,羟基C2至C7烷基和氨基或单 - 或二 - 低级烷基氨基C2至C7烷基; R4选自氢,酰氧基,直链低级烷氧基和羟基; R5是卤素或氢; R6是卤素,条件是如果R 1或R 3中的一个是羟甲基或其中R 11如上所述的基团,则剩余的取代基选自氢,低级烷基和C 3至C 7烯基或炔基,以及 R2为氢,另外条件是(A)当R 4为酰氧基时,R 1和R 3为氢,低级烷基,C 3至C 7链烯基或C 3至C 7炔基,R 2为当R 4为羟基时的基团 那么R 1和R 3为氢,低级烷基,C 3至C 7链烯基或C 3至C 7炔基,R 2为氢或(C)当R 4为烷氧基时,R 1和R 3为氢,低级烷基,C 3至C 7链烯基或C 3至C 7 炔基及其药学上可接受的盐,其显示出作为镇静剂和抗焦虑药的活性。 还公开了吡咯并氮杂吖庚因的某些5,6二氢衍生物,N-氧化物和季铵盐。