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    Compounds having 5-HT6 receptor antagonist activity
    41.
    发明授权
    Compounds having 5-HT6 receptor antagonist activity 失效
    具有5-HT 6受体拮抗剂活性的化合物

    公开(公告)号：US06897215B1

    公开(公告)日：2005-05-24

    申请号：US10111404

    申请日：2000-11-04

    申请人： Tao Xin ,  Methvin Isaac ,  Abdelmalik Slassi

    发明人： Tao Xin ,  Methvin Isaac ,  Abdelmalik Slassi

    IPC分类号： A61K31/437 ,  A61K31/4985 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Novel 6-bicyclopiperazinyl-1-arylsulfonylindole and 6-bicyclopiperidinyl-1-arylsulfonylindole compounds are disclosed which are useful as 5-HT6 receptor antagonists in the treatment of central nervous system disorders such as schizophrenia, depression, ADHD, and cognition and memory dysfunction The compounds are Formula I wherein: R1 is H or C1-4 alkyl; X is CH, —C—OR3, ═C, or —N and Y is C-R2 or N; R3 is H or —C(O)-R4; R4 is H or a labile prodrug group; n is 1 or 2; m and o are, independently, 0, 1, or 2 with the proviso that m+o is 1 or 2; and Ar is an aryl or heteroaryl group optionally substituted with 1-3 substitutents.

    摘要翻译： 公开了新的6-双环哌嗪基-1-芳基磺酰基吲哚和6-双环哌啶基-1-芳基磺酰基吲哚化合物，其可用作治疗中枢神经系统疾病如精神分裂症，抑郁症， ADHD和认知和记忆功能障碍化合物是式I，其中：R 1是H或C 1-4烷基; X是CH，-C-OR 3，-C或-N，Y是C-R 2或N; R3是H或-C（O）-R4; R4是H或不稳定的前药基团; n为1或2; m和o独立地为0,1或2，条件是m + o为1或2; 并且Ar是任选被1-3个取代基取代的芳基或杂芳基。

    Unsaturated amino acid derivatives
    43.
    发明授权
    Unsaturated amino acid derivatives 失效
    不饱和氨基酸衍生物

    公开(公告)号：US6103743A

    公开(公告)日：2000-08-15

    申请号：US369686

    申请日：1999-08-06

    申请人： Stanley Charles Bell ,  Kathleen Da Silva ,  Allen Hopper ,  Methvin Isaac ,  Eric A. Meade ,  Vassil Ilya Ognyanov ,  Abdelmalik Slassi

    发明人： Stanley Charles Bell ,  Kathleen Da Silva ,  Allen Hopper ,  Methvin Isaac ,  Eric A. Meade ,  Vassil Ilya Ognyanov ,  Abdelmalik Slassi

    IPC分类号： A61K31/198 ,  A61K31/381 ,  A61K31/4406 ,  C07C229/36 ,  A61K31/44 ,  A61K31/195 ,  A61K31/21 ,  A61K31/24 ,  A61K31/38

    CPC分类号： A61K31/381 ,  A61K31/198 ,  A61K31/4406 ,  C07C229/36

    摘要： Described herein are compounds having the general formula: ##STR1## Ar.sub.1 and Ar.sub.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sub.1 or Ar.sub.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sub.1 and Ar.sub.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;R is H, alkyl or the counter ion for a basic addition salt;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, alkyl and benzyl;R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently selected from the group consisting of H and alkyl;and a stereoisomer, salt, solvate and hydrate thereof.Also described is the use of these compounds as pharmaceuticals for the treatment of diseases in which inhibition of glycine transport via the GlyT-2 transporter is indicated.

    摘要翻译： 本文描述的是具有以下通式的化合物：Ar 1和Ar 2是独立选择的芳基，任选地被选自烷基，环烷基，烷氧基，烷酰基，芳烷基，芳烷氧基，卤素，NO 2，Ph，CF 3，CN， OH，亚甲二氧基，亚乙二氧基，SO 2 NRR'，NRR'，CO 2 R（其中R和R'独立地选自H和烷基）和可以如上取代的第二芳基; 其中任何环烷基或芳基取代基通过可以是单键的桥连元件连接到Ar 1或Ar 2上，亚乙烯基，亚乙炔基，Z基，-Z-（CH 2）n - 基， - （CH 2） ）nZ-基或-Z-（CH2）nZ-基，其中Z表示O原子，S原子，NH基或N-烷基，n是1至4的整数; 其中Ar1和Ar2可以通过单键连接到它们连接的中心原子上，亚烷基，亚烯基或亚炔基; R为H，烷基或碱式加成盐的抗衡离子; R1和R2独立地选自H，烷基和苄基; R3，R4，R5和R6独立地选自H和烷基; 和其立体异构体，盐，溶剂化物和水合物。 还描述了这些化合物作为药物用于治疗通过GlyT-2转运蛋白抑制甘氨酸转运的疾病的用途。