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    Kainate-binding human CNS receptors of the EAA4 family
    3.
    发明申请
    Kainate-binding human CNS receptors of the EAA4 family 审中-公开
    与CNA4家族的Kainate结合人CNS受体

    公开(公告)号：US20020168723A1

    公开(公告)日：2002-11-14

    申请号：US10126617

    申请日：2002-04-22

    申请人： NPS Allelix Corp.

    发明人： Rajender Kamboj ,  Candace E. Elliott ,  Stephen L. Nutt

    IPC分类号： C07K014/705 ,  C07H021/04 ,  G01N033/567 ,  C12P021/02 ,  C12N005/06

    CPC分类号： C07K14/70571

    摘要： Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors of the kainate-binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.

    摘要翻译： 兴奋性氨基酸（EAAs）如谷氨酸的神经传递通过膜结合表面受体介导。 已经分离了编码红藻氨酸结合型EAA受体的这些受体的一个家族的DNA，并且以受体蛋白为特征。 本文描述了产生作为异源膜结合产物的EAA受体的重组细胞系。 还描述了具有商业意义的本发明的相关方面。 包括使用细胞系作为发现调节EAA受体刺激的化合物的工具。

    Production of human parathyroid hormone from microorganisms
    5.
    发明申请
    Production of human parathyroid hormone from microorganisms 审中-公开
    从微生物生产人甲状旁腺激素

    公开(公告)号：US20070010439A1

    公开(公告)日：2007-01-11

    申请号：US11247585

    申请日：2005-10-12

    申请人： Kaare Gautvik ,  Peter Alestrom ,  Tordis Oyen ,  Odd Gabrielsen

    发明人： Kaare Gautvik ,  Peter Alestrom ,  Tordis Oyen ,  Odd Gabrielsen

    IPC分类号： A61K38/29 ,  C12N1/18 ,  C07K14/635

    CPC分类号： C07K14/635 ,  A61K38/00 ,  C07K2319/02 ,  C12N15/64 ,  C12N15/66 ,  C12N15/67 ,  C12N15/70 ,  C12N15/81

    摘要： The invention provides recombinant plasmids containing in DNA sequences coding for human preproparathyroid hormone. The invention further provides microorganisms, for example E. coli, transformed by these plasmids. The invention also provides a plasmid for insertion into yeast and a transformed yeast in which the plasmid contains DNA coding for parathyroid hormone. Parathyroid hormone is then secreted by the transformed yeast. Further the invention provides alternate polypeptides having parathyroid hormone activity, including PTH analogs, fragments and extensions, and provides alternate leader sequences and secretion signal sequences which can be used in the present invention. Finally, there are provided methods for purification of the secreted PTH hormone and/or derivatives.

    摘要翻译： 本发明提供含有编码人前甲状腺激素的DNA序列的重组质粒。 本发明还提供了由这些质粒转化的微生物，例如大肠杆菌。 本发明还提供了用于插入酵母的质粒和其中质粒含有编码甲状旁腺激素的DNA的转化酵母。 甲状旁腺激素然后被转化的酵母分泌。 此外，本发明提供了具有甲状旁腺激素活性的替代多肽，包括PTH类似物，片段和延伸，并提供可用于本发明的替代前导序列和分泌信号序列。 最后，提供了分泌的PTH激素和/或衍生物的纯化方法。

    Azaindoles having serotonin receptor affinity
    7.
    发明授权
    Azaindoles having serotonin receptor affinity 失效
    阿魏醇具有5-羟色胺受体亲和力

    公开(公告)号：US06916818B2

    公开(公告)日：2005-07-12

    申请号：US10739302

    申请日：2003-12-19

    申请人： Louise Edwards ,  Abdelmalik Slassi ,  Ashok Tehim ,  Tao Xin

    发明人： Louise Edwards ,  Abdelmalik Slassi ,  Ashok Tehim ,  Tao Xin

    IPC分类号： A61K31/498 ,  A61P25/18 ,  A61P25/24 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07D401/04 ,  A61K31/496

    CPC分类号： C07D471/04 ,  C07D519/00

    摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein: R represents a group of Formula II or Formula III; one of A, B D or E is a N atom, the remainder being CH groups; R1 is selected from the group consisting of SO2Ar, C(O)Ar, CH2Ar and Ar; R2, R3 and R4 are independently selected from the group consisting of H and alkyl; — represents a single or double bond, with the proviso that there is only one double bond in the ring at a time; n is an integer of from 1-3; Z is selected from the group consisting of C, CH and N, provided that when —is a double bond, Z is C and when — is a single bond, Z is selected from CH and N; Ar is an optionally substituted aryl group; with the proviso that when R is a group of Formula II, R1 is SO2Ar. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.

    摘要翻译： 本文描述的是具有对具有通式I的5-HT 6受体具有亲和性的化合物：其中：R代表式II或式III的基团; A，B D或E之一为N原子，其余为CH基团; R 1选自SO 2 Ar，C（O）Ar，CH 2 Ar和Ar; R 2，R 3和R 4独立地选自H和烷基; - 表示单键或双键，条件是每次只有一个双键; n为1-3的整数; Z选自C，CH和N，条件是当 - 双键，Z为C且当 - 为单键时，Z选自CH和N; Ar是任选取代的芳基; 条件是当R是式II的基团时，R 1是SO 2 Ar。 还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症的用途，例如精神分裂症。

    Compounds having 5-HT6 receptor antagonist activity
    8.
    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。