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    HUMAN METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE mGluR6, NUCLEIC ACIDS ENCODING SAME AND USES THEREOF
    3.
    发明申请
    HUMAN METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE mGluR6, NUCLEIC ACIDS ENCODING SAME AND USES THEREOF 审中-公开
    人代谢型谷氨酸受体亚型mGluR6，

    公开(公告)号：WO1996029404A1

    公开(公告)日：1996-09-26

    申请号：PCT/US1996003662

    申请日：1996-03-18

    Applicant: SIBIA NEUROSCIENCES, INC. ,  DAGGETT, Lorrie, P. ,  LU, Chin-Chun

    Inventor： SIBIA NEUROSCIENCES, INC.

    IPC: C12N15/12

    CPC classification number: G01N33/5008 ,  A01K2217/05 ,  C07K14/70571 ,  G01N33/502 ,  G01N33/5058 ,  G01N33/5091 ,  G01N2333/70571

    Abstract: In accordance with the present invention, there are provided nucleic acids encoding human metabotropic glutamate receptor subtype mGluR6, and the proteins encoded thereby. In addition to being useful for the production of metabotropic glutamate receptor subtype mGluR6, nucleic acids of the invention are also useful as probes, thus enabling those skilled in the art, without undue experimentation, to identify and isolate related human receptor subunits. In addition to disclosing a novel metabotropic glutamate receptor subtype, mGluR6, the present invention also comprises methods for using the invention receptor subtype to identify and characterize compounds which affect the function of such receptor subtype, e.g., agonists, antagonists, and modulators of glutamate receptor function.

    Abstract translation: 根据本发明，提供了编码人代谢型谷氨酸受体亚型mGluR6的核酸和由其编码的蛋白质。 除了可用于生产代谢型谷氨酸受体亚型mGluR6之外，本发明的核酸也可用作探针，因此使本领域技术人员无需过度的实验来鉴定和分离相关的人受体亚单位。 除了揭示一种新型代谢型谷氨酸受体亚型mGluR6之外，本发明还包括使用本发明受体亚型鉴定和表征影响这种受体亚型的功能的化合物的方法，例如激动剂，拮抗剂和谷氨酸受体调节剂 功能。

    NOVEL SUBSTITUTED ARYL COMPOUNDS USEFUL AS MODULATORS OF ACETYLCHOLINE RECEPTORS
    4.
    发明申请
    NOVEL SUBSTITUTED ARYL COMPOUNDS USEFUL AS MODULATORS OF ACETYLCHOLINE RECEPTORS 审中-公开
    作为乙酰胆碱受体调节剂的新型取代的芳基化合物有用

    公开(公告)号：WO1997019059A1

    公开(公告)日：1997-05-29

    申请号：PCT/US1996018569

    申请日：1996-11-14

    Applicant: SIBIA NEUROSCIENCES, INC. ,  VERNIER, Jean, Michel ,  MCDONALD, Ian, A.

    Inventor： SIBIA NEUROSCIENCES, INC.

    IPC: C07D207/08

    CPC classification number: C07D207/08 ,  C07D207/12 ,  C07D209/94 ,  C07D211/54

    Abstract: In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect, compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of displacing one or more acetylcholine receptor ligands, e.g., H-nicotine, from mammalian neuronal membrane binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity at acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia (including AIDS dementia); cognitive dysfunction (including disorders of attention, focus and concentration), disorders of extrapyramidal motor function such as Parkinson's disease, progressive supramuscular palsy, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, anxiety and psychosis; substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders or nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma, cardiovascular dysfunction including hypertension and cardiac arrhythmias, as well as co-medication uses in surgical applications.

    Abstract translation: 已经发现，根据本发明，已经发现了促进参与神经传递的配体释放的新一类取代的芳基化合物（含有醚，酯，酰胺，酮或硫醚取代基）。 在特定方面，本发明的化合物能调节乙酰胆碱受体。 本发明的化合物能够从哺乳动物神经元膜结合位点置换一个或多个乙酰胆碱受体配体，例如3 H-尼古丁。 本发明化合物可以充当乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂。 具有乙酰胆碱受体活性的化合物的治疗适应症包括中枢神经系统的疾病如阿尔茨海默氏病和涉及记忆丧失和/或痴呆（包括AIDS痴呆）的其它疾病; 认知功能障碍（包括注意力集中和集中注意力），锥体外系运动功能障碍，如帕金森病，进行性超肌肉麻痹，亨廷顿疾病，吉列斯·杜列特综合症和迟发性运动障碍; 情绪和情绪障碍，如抑郁，焦虑和精神病; 药物滥用，包括戒断症状和替代治疗; 神经分泌障碍和食物摄入异常，包括贪食症和厌食症; 疾病或疼痛的伤害和控制; 自主神经障碍包括胃肠蠕动功能障碍和功能障碍，如炎性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤，包括高血压和心律失常的心血管功能障碍，以及在外科应用中的共用药用途。

    HUMAN NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR COMPOSITIONS AND METHODS EMPLOYING SAME
    5.
    发明申请
    HUMAN NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR COMPOSITIONS AND METHODS EMPLOYING SAME 审中-公开
    人神经碱性乙酰胆碱受体组合物及其使用方法

    公开(公告)号：WO1996041876A1

    公开(公告)日：1996-12-27

    申请号：PCT/US1996009775

    申请日：1996-06-07

    Applicant: SIBIA NEUROSCIENCES, INC. ,  ELLIOTT, Kathryn, J. ,  HARPOLD, Michael, M.

    Inventor： SIBIA NEUROSCIENCES, INC.

    IPC: C12N15/12

    CPC classification number: G01N33/5008 ,  C07K14/70571 ,  G01N33/566

    Abstract: Nucleic acid molecules encoding human neuronal nicotinic acetylcholine receptor alpha and beta subunits, mammalian and amphibian cells containing the nucleic acid molecules, and methods for producing alpha and beta subunits are provided. In particular, nucleic acid molecules encoding alpha 6 subunits and molecules encoding beta 3 subunits of human neuronal nicotinic acetylcholine receptors are provided. In addition, combinations of a plurality of subunits, such as one or more of alpha 1, alpha 2, alpha 3, alpha 4, alpha 5, alpha 6 and/or alpha 7 subunits in combination with one or more of beta 3 subunits or such as one or more of beta 2, beta 3 and/or beta 4 subunits in combination with an alpha 6 subunit are provided.

    Abstract translation: 提供了编码人神经元烟碱乙酰胆碱受体α和β亚基的核酸分子，含有核酸分子的哺乳动物和两栖动物细胞，以及用于产生α和β亚基的方法。 特别地，提供了编码α6亚基的核酸分子和编码人神经元烟碱乙酰胆碱受体的β3亚基的分子。 此外，多个亚基的组合，例如α1，α2，α3，α4，α5，α6和/或α7亚基中的一个或多个与β3亚基中的一个或多个的组合或 例如与α6亚基组合的β2，β3和/或β4亚基中的一个或多个。

    SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATIOSUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECN AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS EPTORS
    6.
    发明申请
    SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATIOSUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECN AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS EPTORS 审中-公开
    取代的吡啶衍生物，其制备用吡啶衍生物，其制备及其作为乙酰胆碱受体调节剂的作用及其作为乙酰胆碱受体调节剂的用途

    公开(公告)号：WO9631475A3

    公开(公告)日：1997-02-06

    申请号：PCT/US9605078

    申请日：1996-04-04

    Applicant: SIBIA NEUROSCIENCES INC ,  COSFORD NICHOLAS D ,  VERNIER JEAN MICHEL

    Inventor： COSFORD NICHOLAS D ,  VERNIER JEAN-MICHEL

    IPC: A61K31/44 ,  A61K31/55 ,  A61P25/04 ,  A61P25/28 ,  A61P43/00 ,  C07D213/38 ,  C07D213/48 ,  C07D213/61 ,  C07D213/82 ,  C07D401/06 ,  C07F7/08 ,  A61K31/695 ,  C07F7/18

    CPC classification number: C07D401/06 ,  C07D213/38 ,  C07F7/0814

    Abstract: In accordance with the present invention, there are provided compounds having the structure (I), wherein: A, B, N?α, Rα, Z, R2, R4, R5 and R6¿ are defined as in the description. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia (including AIDS dementia); disorders of attention and focus (such as attention deficit disorders); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

    Abstract translation: 根据本发明，提供了一类作为乙酰胆碱受体调节剂的吡啶化合物。 本发明的化合物从其结合位点取代乙酰胆碱受体配体。 本发明化合物可用作乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂，并且可用于各种治疗应用，例如治疗阿尔茨海默氏病和涉及记忆丧失和/或痴呆的其它病症（包括AIDS痴呆） ; 注意力集中障碍（如注意力缺陷障碍）; 锥体外系运动功能紊乱，如帕金森病，亨廷顿疾病，吉列斯·杜列特综合征和迟发性运动障碍; 情绪和情绪障碍如抑郁，恐慌，焦虑和精神病; 药物滥用，包括戒断综合征和替代治疗; 神经内分泌障碍和食物摄入异常，包括贪食症和厌食症; 伤害感受障碍和疼痛控制; 自主神经障碍包括胃肠蠕动功能障碍和功能障碍，如炎性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤; 心血管功能障碍，包括高血压和贲门节律不正，外科手术中的喜剧等。

    SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS
    7.
    发明申请
    SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS 审中-公开
    取代的吡啶衍生物，其制备及其作为乙酰胆碱受体的调节剂

    公开(公告)号：WO1996031475A2

    公开(公告)日：1996-10-10

    申请号：PCT/US1996005078

    申请日：1996-04-04

    Applicant: SIBIA NEUROSCIENCES, INC. ,  COSFORD, Nicholas, D. ,  VERNIER, Jean-Michel

    Inventor： SIBIA NEUROSCIENCES, INC.

    IPC: C07D213/38

    CPC classification number: C07D401/06 ,  C07D213/38 ,  C07F7/0814

    Abstract: In accordance with the present invention, there are provided compounds having the structure (I), wherein: A, B, N , R , Z, R , R , R and R are defined as in the description. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia (including AIDS dementia); disorders of attention and focus (such as attention deficit disorders); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowels syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

    Abstract translation: 根据本发明，提供具有结构（I）的化合物，其中：A，B，N，R，Z，R 2，R 4，R 5， 和R 6如在说明书中所定义。 本发明的化合物从其结合位点取代乙酰胆碱受体配体。 本发明化合物可以充当乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂，并且可用于各种治疗应用，例如治疗阿尔茨海默氏病和涉及记忆丧失和/或痴呆的其它病症（包括AIDS痴呆） ; 注意力障碍（如注意力缺陷障碍）; 锥体外系运动功能紊乱，如帕金森病，亨廷顿疾病，吉列斯·杜列特综合征和迟发性运动障碍; 心情和情绪障碍如抑郁，恐慌，焦虑和精神病; 药物滥用，包括戒断综合征和替代治疗; 神经内分泌障碍和食物摄入失调，包括贪食症和厌食症; 伤害感受障碍和疼痛控制; 自主神经障碍包括胃肠蠕动功能障碍和功能障碍，如炎性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤; 心血管功能障碍，包括高血压和贲门节律不正，外科手术中的喜剧等。

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