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    CALCIUM RECEPTOR-ACTIVE MOLECULES
    3.
    发明申请
    CALCIUM RECEPTOR-ACTIVE MOLECULES 审中-公开
    钙受体活性分子

    公开(公告)号：WO1994018959A1

    公开(公告)日：1994-09-01

    申请号：PCT/US1993001642

    申请日：1993-02-23

    Applicant: BRIGHAM AND WOMEN'S HOSPITAL, INC. ,  NPS PHARMACEUTICALS, INC.

    Inventor： BRIGHAM AND WOMEN'S HOSPITAL, INC. ,  NPS PHARMACEUTICALS, INC. ,  NEMETH, Edward, F. ,  BROWN, Edward, M. ,  HEBERT, Steven, C. ,  VAN WAGENEN, Bradford, C. ,  BALANDRIN, Manuel, F. ,  FULLER, Forrest, H. ,  DEL MAR, Eric, G.

    IPC: A61K31/00

    CPC classification number: A61K31/70 ,  A01K2217/05 ,  A01K2217/075 ,  A01K2217/30 ,  A01K2227/10 ,  A01K2267/03 ,  A61K31/00 ,  A61K31/13 ,  A61K31/135 ,  A61K31/165 ,  A61K31/195 ,  A61K31/235 ,  A61K31/275 ,  A61K31/395 ,  A61K31/40 ,  A61K31/415 ,  A61K31/44 ,  A61K31/55 ,  C07K14/705 ,  C07K2319/00 ,  C12N15/8509

    Abstract: Method and composition useful for treating a patient having a disease characterized by an abnormal level of one or more components, the activity of which is regulated or affected by activity of one or more inorganic-ion receptor. Novel compounds useful in these methods and compositions are also provided. The method includes administering to the patient a therapeutically effective amount of a molecule active at one or more inorganic-ion receptors as an agent or antagonist. Preferably, the molecule is able to act as either a selective agonist or antagonist at a Ca receptor of one or more but not all cells chosen from the group consisting of parathyroid cells, bone osteoclasts, juxtaglomerular kidney cells, proximal tubule kidney cells, distal tubule kidney cell, cell of the thick ascending limb of Henle's loop and/or collecting duct, keratinocyte in the epidermis, parafollicular cell in the thyroid (C-cells), intestinal cell, trophoblast in the placenta, platelet, vascular smooth muscle cell, cardiac atrial cell, gastrin and glucagon secreting cells, kidney mesangial cell and mammary cell.

    Abstract translation: 用于治疗患有特征在于异常水平的一种或多种组分的患者的方法和组合物，其活性受一种或多种无机离子受体的活性调节或影响。 还提供了可用于这些方法和组合物的新型化合物。 该方法包括向患者施用治疗有效量的一种或多种作为药剂或拮抗剂的无机 - 离子受体活性的分子。 优选地，该分子能够作为一种或多种但不是全部选自甲状旁腺细胞，骨破骨细胞，近肾小球肾细胞，近端小管肾的Ca 2+受体的选择性激动剂或拮抗剂 细胞，远端肾小管肾细胞，亨利循环和/或收集管，上皮角质形成细胞，甲状腺旁淋巴细胞（C细胞），肠细胞，胎盘滋养细胞，血小板，血管平滑 肌肉细胞，心房心房细胞，胃泌素和胰高血糖素分泌细胞，肾系膜细胞和乳腺细胞。

    CHIMERIC RECEPTORS AND METHODS FOR IDENTIFYING COMPOUNDS ACTIVE AT METABOTROPIC GLUTAMATE RECEPTORS AND THE USE OF SUCH COMPOUNDS IN THE TREATMENT OF NEUROLOGICAL DISORDERS AND DISEASES
    5.
    发明申请
    CHIMERIC RECEPTORS AND METHODS FOR IDENTIFYING COMPOUNDS ACTIVE AT METABOTROPIC GLUTAMATE RECEPTORS AND THE USE OF SUCH COMPOUNDS IN THE TREATMENT OF NEUROLOGICAL DISORDERS AND DISEASES 审中-公开
    重要的受体和识别化合物在代谢谷氨酸受体中的作用及其在治疗神经疾病和疾病中的用途

    公开(公告)号：WO1997005252A2

    公开(公告)日：1997-02-13

    申请号：PCT/US1996012336

    申请日：1996-07-25

    Applicant: NPS PHARMACEUTICALS, INC.

    Inventor： NPS PHARMACEUTICALS, INC. ,  FULLER, Forrest, H. ,  KRAPCHO, Karen, J. ,  HAMMERLAND, Lance, G.

    IPC: C12N15/12

    CPC classification number: C07K14/705 ,  A01K2217/05 ,  A61K38/00 ,  C07K14/70571 ,  C07K2319/00

    Abstract: The present invention provides chimeric receptors. The chimeric receptors comprise at least one region homologous to a region of a metabotropic glutamate receptor and at least one region homologous to a region of a calcium receptor. The invention also includes methods of preparing such chimeric receptors, and methods of using such receptors to identify and characterize compounds which modulate the activity of metabotropic glutamate receptors or calcium receptors. The invention also relates to compounds and methods for modulating metabotropic glutamate receptor activity and binding to metabotropic glutamate receptors. Modulation of metabotropic glutamate receptor activity can be used for different purposes such as treating neurological disorders and diseases, inducing an analgesic effect, cognition enhancement, and inducing a muscle-relaxant effect.

    Abstract translation: 本发明提供了嵌合受体。 嵌合受体包含与代谢型谷氨酸受体的区域同源的至少一个区域和与钙受体的区域同源的至少一个区域。 本发明还包括制备这种嵌合受体的方法，以及使用这些受体来鉴定和表征调节代谢型谷氨酸受体或钙受体的活性的化合物的方法。 本发明还涉及用于调节代谢型谷氨酸受体活性并结合代谢型谷氨酸受体的化合物和方法。 代谢型谷氨酸受体活性的调节可用于治疗神经系统疾病和疾病，诱导止痛作用，认知增强和诱导肌肉松弛作用等不同目的。

    INSECTICIDAL TOXINS FROM BRACON HEBETOR
    7.
    发明申请
    INSECTICIDAL TOXINS FROM BRACON HEBETOR 审中-公开
    来自BRACON HEETETOR的杀虫毒素

    公开(公告)号：WO1996025429A1

    公开(公告)日：1996-08-22

    申请号：PCT/US1996002181

    申请日：1996-02-16

    Applicant: NPS PHARMACEUTICALS, INC.

    Inventor： NPS PHARMACEUTICALS, INC. ,  JOHNSON, Janice, H. ,  KRAL, Robert, M. ,  KRAPCHO, Karen

    IPC: C07K14/00

    CPC classification number: C07K14/43568 ,  A01N63/00 ,  A01N63/02 ,  C12N2799/026

    Abstract: This invention relates to the purification of a group of insecticidally effective toxins isolated from the wasp, Bracon hebetor, characterized by their neurotoxic effect on insect pest and low mammalian toxicity. The cDNA sequences for two of these toxins have been isolated, and the complete coding sequence is provided. This invention also discloses methods for producing recombinant toxins, as well as methods of utilizing these toxins as insecticidal agents.

    Abstract translation: 本发明涉及从黄蜂（Bracon hebetor）分离的一组杀虫有效毒素的纯化，其特征在于它们对害虫的神经毒性作用和低的哺乳动物毒性。 已经分离了两种这些毒素的cDNA序列，并提供了完整的编码序列。 本发明还公开了重组毒素的制备方法，以及利用这些毒素作为杀虫剂的方法。

    SYNTHETIC ARYL POLYAMINES AS EXCITATORY AMINO ACID NEUROTRANSMITTER ANTAGONISTS
    8.
    发明申请
    SYNTHETIC ARYL POLYAMINES AS EXCITATORY AMINO ACID NEUROTRANSMITTER ANTAGONISTS 审中-公开
    合成氨基聚氨酯作为激素氨基酸神经递质拮抗剂

    公开(公告)号：WO1993004036A1

    公开(公告)日：1993-03-04

    申请号：PCT/US1992006482

    申请日：1992-08-10

    Applicant: PFIZER INC. ,  NPS PHARMACEUTICALS, INC. ,  SACCOMANO, Nicholas, Alex ,  VOLKMANN, Robert, Alfred

    Inventor： PFIZER INC. ,  NPS PHARMACEUTICALS, INC.

    IPC: C07C233/40

    CPC classification number: C07C233/40 ,  C07D209/18 ,  C07D213/56 ,  C07F17/02

    Abstract: Compounds having the formula R-(CH2)m-CO-R' wherein R is a 5 to 7 member carbocyclic system or an 8 to 11 member carbobicyclic system or any such system substituted with one or more of F, Cl, Br, OH, C1 to C4 alkyl, C1 to C4 alkoxy, CF3, phenyl, amino, C1 to C4 alkylamino and di(C1 to C4 alkyl)amino; m is 0 or 1; R' is -[NH(CH2)n]xNH2; each n is independently 2 to 5; and x is 1 to 6, and their pharmaceutically acceptable acid addition salts are potent excitatory amino acid neurotransmitter antagonists. These compounds are useful as mammalian psychotherapeutants, as the active ingredient in pharmaceutical compositions for treating conditions in mammals which are mediated by excitatory amino acid neurotransmitters and in the control of invertebrate pests.

    Abstract translation: 具有式R-（CH 2）m -CO-R'的化合物，其中R是5至7个碳环系统或8至11个碳双环系统或任选被F，Cl，Br，OH中的一个或多个取代的系统 C1-C4烷基，C1-C4烷氧基，CF3，苯基，氨基，C1-C4烷基氨基和二（C1-C4烷基）氨基; m为0或1; R'是 - [NH（CH 2）n] x NH 2; 每个n独立地为2至5; x为1〜6，其药学上可接受的酸加成盐为有效的兴奋性氨基酸神经递质拮抗剂。 这些化合物可用作哺乳动物心理治疗剂，作为用于治疗由兴奋性氨基酸神经递质介导的哺乳动物和控制无脊椎动物害虫的药物组合物中的活性成分。

    TREATMENT OF SPASTICITY, CONVULSIONS BY ISOVALERIC ACID DERIVATIVES CNS DEPRESSANTS
    9.
    发明申请
    TREATMENT OF SPASTICITY, CONVULSIONS BY ISOVALERIC ACID DERIVATIVES CNS DEPRESSANTS 审中-公开
    通过ISO等级衍生物对中枢神经系统疾病的治疗

    公开(公告)号：WO1998008498A1

    公开(公告)日：1998-03-05

    申请号：PCT/US1997015272

    申请日：1997-08-29

    Applicant: NPS PHARMACEUTICALS, INC. ,  ARTMAN, Linda, D. ,  BALANDRIN, Manuel, F.

    Inventor： NPS PHARMACEUTICALS, INC.

    IPC: A61K31/16

    CPC classification number: A61K31/16 ,  A61K31/19 ,  A61K36/84

    Abstract: Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and its pharmaceutically acceptable salts, esters, and substituted amides, exhibit clinically significant pharmacological properties which implicate a treatment for a variety of pathological conditions, including spasticity and convulsions, which are ameliorated by effecting a mild depression of CNS activity. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.

    Abstract translation: 缬草的制备和提取物以及异戊酰胺，异戊酸及其药学上可接受的盐，酯和取代的酰胺显示出临床上显着的药理学性质，其涉及多种病理状况的治疗，包括痉挛性和惊厥性，其被改善 通过实现中枢神经系统活动的轻度抑制。 所讨论的组合物通常是非细胞毒性的，并且在对这种病理状况有症状的治疗有效的剂量下不引起无力或镇静作用。

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