利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

17 条记录 (耗时 0.013 秒)

    Benzo�d! isoxazole derivatives, compositions containing them and their use in therapy
    1.
    发明授权
    Benzo�d! isoxazole derivatives, compositions containing them and their use in therapy 失效
    苯并[d]异恶唑衍生物，含有它们的组合物及其在治疗中的用途

    公开(公告)号：US5707988A

    公开(公告)日：1998-01-13

    申请号：US464709

    申请日：1995-07-11

    申请人： Edward Andrew Boyd ,  Brenda Costall ,  Mary Elizabeth Kelly ,  Philip James Parsons

    发明人： Edward Andrew Boyd ,  Brenda Costall ,  Mary Elizabeth Kelly ,  Philip James Parsons

    IPC分类号： A61K31/435 ,  A61K31/437 ,  A61K31/495 ,  A61K31/4985 ,  A61K31/535 ,  A61K31/5383 ,  A61K31/54 ,  A61K31/542 ,  A61P25/00 ,  A61P25/22 ,  A61P25/28 ,  C07D498/04 ,  C07D513/04

    CPC分类号： C07D498/04

    摘要： Compounds of formula (I) ##STR1## in which X represents a group >O, >S, >C.dbd.O or >NR wherein R is hydrogen, C.sub.1-6 alkyl, phenyl or C.sub.7-12 phenalkyl, R.sub.1 and R.sub.2 each represent hydrogen or together represent an oxo group and R.sub.3, R.sub.4 and R.sub.5 each represent hydrogen or R.sub.1 represents hydrogen and two of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 together represent the second bond of a double bond joining positions 7 and 8, 8 and 9 or 9 and 10 with the remaining two of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 representing hydrogen, the compound optionally being in the form of a salt thereof formed with a physiologically acceptable inorganic or organic acid, are of value for the treatment of anxiety and in the improvement of learning ability and/or the reversal of amnesia.

    摘要翻译： PCT No.PCT / GB93 / 02501 Sec。 371日期：1995年7月11日 102（e）1995年7月11日PCT PCT 1993年12月7日PCT公布。 出版物WO94 / 14816 PCT 日本时间1994年7月7日，式（I）的化合物其中X代表基团> O，> S，> C = O或> NR，其中R是氢，C1-6烷基，苯基或C7- 12个苯基烷基，R1和R2各自表示氢或一起表示氧代基，R3，R4和R5各自表示氢或R1表示氢，R2，R3，R4和R5中的两个表示双键连接位置7的第二个键 和8,8和9或9和10，其余两个R2，R3，R4和R5代表氢，该化合物任选呈其与生理上可接受的无机或有机酸形成的盐的形式，对于 治疗焦虑和提高学习能力和/或逆转健忘症。

    Treatment of addiction to drugs and substances of abuse
    2.
    发明授权
    Treatment of addiction to drugs and substances of abuse 失效
    治疗药物和滥用药物成瘾

    公开(公告)号：US5462948A

    公开(公告)日：1995-10-31

    申请号：US115450

    申请日：1993-09-01

    申请人： Jens K. Perregaard ,  Brenda Costall

    发明人： Jens K. Perregaard ,  Brenda Costall

    IPC分类号： A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/445 ,  A61K31/535 ,  A61K31/54 ,  A61P25/02 ,  A61P25/20 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

    CPC分类号： A61K31/445

    摘要： 1-Aryl-3-(4-1piperidyl)-indole derivatives having general formula (I), ##STR1## wherein R.sup.1 is hydrogen, halogen, alkyl, alkoxy, hydroxy, cyano, nitro, alkylthio, trifluoromethyl, trifluoromethylthio, alkylsulfonyl, amino, alkylamino or dialkylaminio; R is optionally substituted phenyl or a heteroaromatic group; and R.sup.2 is hydrogen, cycloalkyl, alkyl or alkenyl, optionally substituted with one or two hydroxy groups, or R.sup.2 is a group of formula (IV), ##STR2## wherein n is an integer of from 2-6; W is O, S or N--R.sup.3, wherein R.sup.3 is H alkyl or cycloalkyl; U is N or CH, Z is --(CH.sub.2).sub.m --, m being 2 or 3, or Z is --CH.dbd.CH--, 1,2-phenylene, or --COCH.sub.2 -- or --CSCH.sub.2 --; V is O,S,CH.sub.2, or NR.sup.4, wherein R.sup.4 is hydrogen, optionally hydroxy substituted alkyl, alkenyl or cycloalkylmethyl; are useful in alleviating, relieving or suppressing withdrawal or abstinence symptons or suppressing the dependency of a drug or a substance of abuse.

    摘要翻译： 具有通式（I）的1-芳基-3-（4-1-哌啶基） - 吲哚衍生物，其中R1是氢，卤素，烷基，烷氧基，羟基，氰基，硝基，烷硫基，三氟甲基，三氟甲硫基， 烷基磺酰基，氨基，烷基氨基或二烷基氨基; R是任选取代的苯基或杂芳基; 并且R 2是任选被一个或两个羟基取代的氢，环烷基，烷基或链烯基，或者R 2是式（Ⅳ）基团，其中n是2-6的整数; W是O，S或N-R 3，其中R 3是H烷基或环烷基; U是N或CH，Z是 - （CH2）m-，m是2或3，或Z是-CH = CH-，1,2-亚苯基或-COCH2-或-CSCH2-; V是O，S，CH 2或NR 4，其中R 4是氢，任选羟基取代的烷基，烯基或环烷基甲基; 有助于缓解，缓解或抑制戒断或禁欲症状或抑制药物或滥用物质的依赖。

    Memory-enhancing compositions containing dioxopiperidine derivatives
    4.
    发明授权
    Memory-enhancing compositions containing dioxopiperidine derivatives 失效
    包含二氧代哌啶衍生物的记忆增强组合物

    公开(公告)号：US5177086A

    公开(公告)日：1993-01-05

    申请号：US729851

    申请日：1991-07-12

    申请人： Brenda Costall

    发明人： Brenda Costall

    IPC分类号： A61K31/445

    CPC分类号： A61K31/445

    摘要： Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl;n is 1 or 2;R.sub.2 represents hydrogen or methyl, provided that one R.sub.2 is hydrogen when n is 2;R.sub.3 represents hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.4 represents C.sub.1 -C.sub.2 alkyl;R.sub.5 and R.sub.6 independently represent hydrogen or methyl;m is 0 to 3; andeach Y is in a meta or para position and independently represents hydroxy, C.sub.1 -C.sub.2 alkoxy, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 hydroxyalkyl, halogen, or trifluoromethyl, provided that hydroxy and alkoxy are not in the para position,and not pharmacologically acceptable salts thereof have memory enhancing activity and are particularly useful in the treatment of cognitive deficiencies such as senile dementia.The presently preferred compound is 3-(3'methoxyphenyl)-3-(3'-N,N-dimethylaminopropyl)-4,4-dimethyl-2,6-dioxopiperidine (AGN 2979).

    摘要翻译： 式I的苯基-3-氨基烷基-4-甲基-2,6-二氧代哌啶（I）其中：R 1表示氢或C 1 -C 4烷基; n为1或2; R2表示氢或甲基，条件是当n为2时一个R 2为氢; R3表示氢或C1-C2烷基; R4代表C1-C2烷基; R5和R6独立地表示氢或甲基; m为0〜3; 并且每个Y是间位或对位，并且独立地表示羟基，C 1 -C 2烷氧基，C 1 -C 2烷基，C 1 -C 2羟基烷基，卤素或三氟甲基，条件是羟基和烷氧基不在对位，而不是药理学 其可接受的盐具有记忆增强活性，并且特别可用于治疗诸如老年性痴呆的认知缺陷。 目前优选的化合物是3-（3'-甲氧基苯基）-3-（3'-N，N-二甲基氨基丙基）-4,4-二甲基-2,6-二氧代哌啶（AGN 2979）。

    Antipsychotic compositions containing dioxopiperidine derivatives
    9.
    发明授权
    Antipsychotic compositions containing dioxopiperidine derivatives 失效
    含有二氧代哌啶衍生物的抗精神病药物组合物

    公开(公告)号：US4877800A

    公开(公告)日：1989-10-31

    申请号：US217450

    申请日：1988-07-11

    申请人： Brenda Costall

    发明人： Brenda Costall

    IPC分类号： A61K31/445 ,  A61P25/18 ,  C07D211/86

    CPC分类号： A61K31/445

    摘要： Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl;n is 1 or 2;R.sub.2 represents hydrogen or methyl, provided that one R.sub.2 is hydrogen when n is 2;R.sub.3 represents hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.4 represents C.sub.1 -C.sub.2 alkyl;R.sub.5 and R.sub.6 independently represent hydrogen or methyl;m is 0 to 3; and each Y is in a meta or para position and independently represents hydroxy, C.sub.1 -C.sub.2 alkoxy, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 hydroxyalkyl, halogen, or trifluoromethyl, provided that hydroxy and alkoxy are not in the para position, and pharmacologically acceptable salts thereof have antiposychotic activity without sedative side effects. They are particularly useful in the treatment of schizophrenia.The presently preferred compound is 3-(3'methoxyphenyl)-3-(3"-N,N-dimethylaminopropyl) -4,4-dimethyl-2,6-dioxopiperidine (AGN 2979).

    Pharmaceutical compositions
    10.
    发明授权
    Pharmaceutical compositions 失效
    药物组合物

    公开(公告)号：US5578626A

    公开(公告)日：1996-11-26

    申请号：US478142

    申请日：1995-06-07

    申请人： Edward A. Boyd ,  Brenda Costall ,  Mary E. Kelly ,  Philip J. Parsons

    发明人： Edward A. Boyd ,  Brenda Costall ,  Mary E. Kelly ,  Philip J. Parsons

    IPC分类号： A61K31/42 ,  A61K31/423 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  C07D261/20 ,  C07D413/04

    CPC分类号： C07D413/04 ,  C07D261/20

    摘要： Compounds of formula (I) ##STR1## in which R.sub.1 represents hydrogen, a C.sub.1-6 aliphatic hydrocarbyl group or a C.sub.1-4 aliphatic hydrocarbyl group substituted by a C.sub.3-6 alicyclic hydrocarbyl group or by a phenyl group, which phenyl group is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, R.sub.2 represents hydrogen, R.sub.3 represents hydrogen, a 5-or 6-membered ring aromatic heterocyclyl group containing one or two heteroatoms selected from nitrogen, oxygen and sulphur which is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, or a group AR wherein A is a straight chain C.sub.1-4 aliphatic hydrocarbyl group terminally substituted by R which is hydrogen, a phenyl group or a 5-or 6-membered ring aromatic heterocyclyl group containing one or two heteroatoms selected from nitrogen, oxygen and sulphur, which phenyl or heterocyclyl group R is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, R.sub.4 and R.sub.5 each represent hydrogen or together represent an oxo group and R.sub.6, R.sub.7 and R.sub.8 each represent hydrogen, or R.sub.4 represents hydrogen and two of R.sub.5, R.sub.6, R.sub.7 and R.sub.8 together represent the second bond of a double bond joining positions 4 and 5, 5 and 6 or 6 and 7 with the remaining two of R.sub.5, R.sub.6, R.sub.7 and R.sub.8 representing hydrogen, the compound optionally being in the form of a salt thereof formed with a physiologically acceptable inorganic or organic acid, are of value for the treatment of anxiety and in the improvement of learning ability and/or the reversal of amnesia.

    摘要翻译： 式（I）化合物其中R 1表示氢，C 1-6脂族烃基或C 3-6脂族烃基被C 3-6脂环族烃基或苯基取代的式（I）化合物，该苯基 基团是未取代的或被卤代或C 1-3卤代烷基取代，R 2表示氢，R 3表示氢，含有一个或两个选自氮，氧和硫的杂原子的5-或6-元环芳族杂环基，其是未取代的或 被卤素或C 1-3卤代烷基取代的基团，其中A是由R末端取代的直链C 1-4脂族烃基，其中R是氢，苯基或5-或6-元环芳族杂环基 含有一个或两个选自氮，氧和硫的杂原子，该苯基或杂环基R未被取代或被卤代或C 1-3卤代烷基取代，R 4和R 5各自表示氢或一起代表 发送氧代基，R6，R7和R8各自表示氢，或R4表示氢，R5，R6，R7和R8中的两个表示双键连接位置4和5，6和6和7的第二个键 剩余的R5，R6，R7和R8中的两个代表氢，任选呈其生理学上可接受的无机或有机酸形成的盐的化合物对于治疗焦虑和改善学习是有价值的 能力和/或逆转遗忘。