Anxiolytic-R-n(1-azabicyclo[2.2.2]oct-3-yl) benzamides and thiobenzamides
    44.
    发明授权
    Anxiolytic-R-n(1-azabicyclo[2.2.2]oct-3-yl) benzamides and thiobenzamides 失效
    溶解-R-n(1-氮杂双环[2.2.2]辛-3-基)苯甲酰胺和硫代苯甲酰胺

    公开(公告)号:US5206246A

    公开(公告)日:1993-04-27

    申请号:US735174

    申请日:1991-07-23

    CPC classification number: C07D453/02

    Abstract: Compounds of general formula I ##STR1## wherein: X represents oxygen or sulphur; each of R.sup.1 and R.sup.3 independently represents hydrogen or a C.sub.1 -C.sub.4 alkyl group;Ar represents:a phenyl ring optionally substituted by one, two or three C.sub.1 -C.sub.4 alkoxy groups and/or by one or two halogen atoms;a phenyl ring of the general formula ##STR2## wherein R.sup.2 represents halogen, 4,5-benzo, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.4 alkylcarbonyl or Am, wherein Am represents amino, methylamino or dimethylamino,R.sup.4 represents C.sub.1 -C.sub.8 alkyl,n is 1 or 2; ora pyrimidinyl moiety of the general formula ##STR3## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl; and their N-oxides and pharmaceutically acceptable salts are useful as anxiolytic agents. A preferred compound is R-(+)-4-amino-N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-methoxybenzamide.

    Abstract translation: 通式I的化合物其中:X表示氧或硫; R 1和R 3各自独立地表示氢或C 1 -C 4烷基; Ar表示:任选被一个,两个或三个C 1 -C 4烷氧基和/或一个或两个卤素原子取代的苯环; 其中R 2表示卤素,4,5-苯并,C 1 -C 8烷氧基,C 1 -C 4烷基羰基或Am,其中A m表示氨基,甲氨基或二甲基氨基,R 4表示C 1 -C 8烷基,n 是1或2; 或通式为“IMAGE”的嘧啶基部分,其中R 5为C 1 -C 4烷基; 其N-氧化物和药学上可接受的盐可用作抗焦虑剂。 优选的化合物是R - (+) - 4-氨基-N-(1-氮杂双环[2.2.2]辛-3-基)-5-氯-2-甲氧基苯甲酰胺。

    Derivatives of 1-[3-(4-hydroxyphenyl) 1-hydroxy 1-propyl] benzene
substituted in position 2 by an aminoalkyleneoxy chain, the method of
preparing same and the application thereof to therapeutics
    45.
    发明授权
    Derivatives of 1-[3-(4-hydroxyphenyl) 1-hydroxy 1-propyl] benzene substituted in position 2 by an aminoalkyleneoxy chain, the method of preparing same and the application thereof to therapeutics 失效
    通过氨基亚烷氧基链在位置2取代的1- [3-(4-羟基苯基)1-羟基-1-丙基]苯的衍生物,其制备方法及其在治疗学中的应用

    公开(公告)号:US5144029A

    公开(公告)日:1992-09-01

    申请号:US637075

    申请日:1991-01-03

    CPC classification number: C07D295/088

    Abstract: The present invention relates to compounds of formula: ##STR1## in which: R.sub.3 is hydrogen, 2-tetrahydropyranyl or benzyl;R.sub.1 and R.sub.2 are such that:either R.sub.1 represents a methoxy group in which case R.sub.2 is a group chosen from the following: hydroxyl; C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.5 -C.sub.7 cycloalkloxy; benzyloxy;or R.sub.2 represents a methoxy group in which case R.sub.1 is a group chosen from the following: hydroxyl; C.sub.2 -C.sub.8 alkyloxy; C.sub.2 -C.sub.8 alkyloxy substituted by a methoxy group; C.sub.1 -C.sub.4 trifluoroalkyloxy; C.sub.3 -C.sub.4 alkenyloxy; C.sub.5 -C.sub.7 cycloalkyloxy; benzyloxy; C.sub.1 -C.sub.4 alkylthio;n=2 or 3; andp=4, 5 or 6,as well as their addition salts with mineral or organic acids, said compounds and salts being useful as drugs.

    Abstract translation: 本发明涉及下式的化合物:其中:R3是氢,2-四氢吡喃基或苄基; R1和R2是这样的:R 1表示甲氧基,在这种情况下,R 2是选自以下的基团:羟基; C1-C4烷基; C2-C8烷氧基; C5-C7环烷氧基; 苄氧基; 或R 2表示甲氧基,其中R 1为选自以下的基团:羟基; C2-C8烷氧基; 被甲氧基取代的C2-C8烷氧基; C 1 -C 4三氟烷氧基; C3-C4烯氧基; C5-C7环烷基氧基; 苄氧基; C1-C4烷硫基; n = 2或3; 和p = 4,5或6,以及它们与矿物或有机酸的加成盐,所述化合物和盐可用作药物。

    Memory enhancing-R-N-(1-azabicyclo[2.2.2.]oct-3-yl)benzamides and
thiobenzamides
    46.
    发明授权
    Memory enhancing-R-N-(1-azabicyclo[2.2.2.]oct-3-yl)benzamides and thiobenzamides 失效
    记忆增强-R-N-(1-氮杂双环[2.2.2]辛-3-基)苯甲酰胺和硫代苯甲酰胺

    公开(公告)号:US5017580A

    公开(公告)日:1991-05-21

    申请号:US389309

    申请日:1989-08-03

    CPC classification number: A61K31/435 A61K31/505

    Abstract: Compounds of general formula I ##STR1## wherein: X represents oxygen or sulphur;each of R.sup.1 and R.sup.3 independently represents hydrogen or a C.sub.1 -C.sub.4 alkyl group;Ar represents:a phenyl ring optionally substituted by one, two or three C.sub.1 -C.sub.4 alkoxy groups and/or by one or two halogen atoms; a phenyl ring of the general formula ##STR2## wherein R.sup.2 represents halogen, 4,5-benzo, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.4 alkylcarbonyl or Am, wherein Am represents amino, methylamino or dimethylamino,R.sup.4 represents C.sub.1 -C.sub.8 alkyl,n is 1 or 2; ora pyrimidinyl moiety of the general formula ##STR3## wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl; and their N-oxides and pharmaceutically acceptable salts are useful as memory- and/or learning-enhancing agents. A preferred compound is R-(+)-4-amino-N-(1-azabicyclo[2.2.2]oct-3-yl)-5-chloro-2-methoxybenzamide.

    Rear-steering control device for automotive vehicle with four-wheel
steering
    47.
    发明授权
    Rear-steering control device for automotive vehicle with four-wheel steering 失效
    具有四轮转向的机动车后转向控制装置

    公开(公告)号:US4993730A

    公开(公告)日:1991-02-19

    申请号:US475317

    申请日:1990-02-05

    CPC classification number: B62D7/1527

    Abstract: A rear steering control device for an automotive vehicle, wherein the finger carrying the roller portion is secured to a hub rigidly secured in coaxial relationship to both adjacent ends of both rear steering drag rods, respectively, and the drive shaft is coupled to a disc formed with peripheral teeth for rotating it about its axis when locking the front wheels so that the cam-like groove causes the rear steering drag rods to be moved in parallel relation to the axis.

    Abstract translation: 一种用于机动车辆的后转向控制装置,其中携带滚子部分的手指分别固定到与两个后转向牵引杆的两个相邻端部以同轴关系牢固地固定的轮毂,并且驱动轴联接到形成的盘 具有用于在锁定前轮时绕其轴线旋转的外围齿,使得凸轮状凹槽使得后转向牵引杆平行于轴线移动。

    5-aminoethyloxazolidin-2-one derivatives
    48.
    发明授权
    5-aminoethyloxazolidin-2-one derivatives 失效
    5-氨基乙基恶唑烷-2-酮衍生物

    公开(公告)号:US4897409A

    公开(公告)日:1990-01-30

    申请号:US92126

    申请日:1987-09-02

    CPC classification number: C07D263/20

    Abstract: A mixture of the 4 stereoisomers of formula (I) below, each of the pairs of corresponding racemic diastereoisomers and each of the enantiomers corresponding to each pair, that is to say each of said stereoisomers: ##STR1## in which R.sub.1 represents: a hydrogen atom,an alkoxy group comprising from 1 to 4 carbon atoms,a trifluoromethyl group, orone or two halogen atoms;and the pair (R.sub.2, R.sub.3) has one of the following meanings: (H, H), (H, C.sub.1 -C.sub.4 alkyl), (C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl), as well as their organic and inorganic acid addition salts.The compounds of formula (I) are therapeutically useful.

    Abstract translation: 下述式(I)的4种立体异构体的混合物,每对相应的外消旋非对映异构体和对应于每一对的每个对映体,也就是说每种所述立体异构体:其中R 1表示 :氢原子,含有1至4个碳原子的烷氧基,三氟甲基或一个或两个卤素原子; (R2,R3)具有以下含义:(H,H),(H,C1-C4烷基),(C1-C4烷基,C1-C4烷基),以及它们的有机和无机酸 加成盐。 式(I)化合物在治疗上是有用的。

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