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1. 发明专利

JP2005160480A Human metabotropic glutamate receptor, nucleic acid encoding the same and use of the same 审中-公开
标题翻译：人代谢谷氨酸受体，核酸编码及其使用
公开(公告)号：JP2005160480A
公开(公告)日：2005-06-23
申请号：JP2004340504
申请日：2004-11-25
申请人： Sibia Neurosciences Inc , シビア・ニューロサイエンシーズ・インコーポレイテッド
发明人： DAGGETT LORRIE , ELLIS STEVEN B , LIAW CHEN , PONTSLER AARON , JOHNSON EDWIN C , HESS STEPHEN D
IPC分类号： G01N33/566 , A61K39/395 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07K14/705 , C07K16/28 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/00 , C12N5/10 , C12N15/02 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12Q1/02 , C12Q1/68 , C12R1/91 , G01N33/15 , G01N33/50 , G01N33/53
CPC分类号： G01N33/5091 , A01K2217/05 , C07K14/70571 , G01N33/5008 , G01N33/502 , G01N33/5058 , G01N2333/70571
摘要： PROBLEM TO BE SOLVED: To provide nucleic acids-encoding human metabotropic glutamate receptor subtypes 2 and 5 and a protein encoded with the same. SOLUTION: This invention relates to the nucleic acids encoding human metabotropic glutamate receptor subtypes mGluR2 and mGluR5. The nucleic acids are useful for production of metabotropic glutamate receptor subtypes, the 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 new metabotropic glutamate receptor subtype, this invention also comprises methods for using the invention receptor subtype to identify and characterize compounds which affect the function of receptor subtypes, e.g., agonists, antagonists, and modulators of glutamate receptor function. COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：待解决的问题：提供编码编码人代谢型谷氨酸受体亚型2和5的核酸以及用其编码的蛋白质。解决方案：本发明涉及编码人代谢型谷氨酸受体亚型mGluR2和mGluR5的核酸。核酸可用于产生代谢型谷氨酸受体亚型，本发明的核酸也可用作探针，因此使得本领域技术人员无需过多的实验来鉴定和分离相关的人受体亚单位。除了揭示新的代谢型谷氨酸受体亚型之外，本发明还包括使用本发明受体亚型鉴定和表征影响受体亚型功能的化合物的方法，例如激动剂，拮抗剂和谷氨酸受体功能的调节剂。版权所有（C）2005，JPO＆NCIPI

2. 发明专利

JP2006254915A Human metabotropic glutamate receptor, nucleic acid encoding same and use thereof 审中-公开
标题翻译：人代谢谷氨酸受体，核酸编码及其用途
公开(公告)号：JP2006254915A
公开(公告)日：2006-09-28
申请号：JP2006085289
申请日：2006-03-27
申请人： Sibia Neurosciences Inc , シビア・ニューロサイエンシーズ・インコーポレイテッド
发明人： DAGGETT LORRIE , ELLIS STEVEN B , LIAW CHEN , PONTSLER AARON , JOHNSON EDWIN C , HESS STEPHEN D
IPC分类号： C12N15/09 , G01N33/566 , A61K39/395 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P37/02 , A61P43/00 , C07K14/705 , C07K16/28 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/00 , C12N5/10 , C12N15/02 , C12N15/12 , C12P21/02 , C12P21/08 , C12Q1/02 , C12Q1/68 , C12R1/91 , G01N33/15 , G01N33/50 , G01N33/53
CPC分类号： G01N33/5091 , A01K2217/05 , C07K14/70571 , G01N33/5008 , G01N33/502 , G01N33/5058 , G01N2333/70571
摘要： PROBLEM TO BE SOLVED: To provide a nucleic acid encoding human metabotropic glutamate receptor protein subtypes 2 and 5, and to provide a protein encoding the same. SOLUTION: This nucleic acid encoding the subtypes of human metabotropic glutamate receptor mGluR2 and mGlmR5 and useful for producing the metabotropic glutamate receptor subtypes. A probe capable of identifying and isolating related receptor subunits. A method for using the receptor subunits to identify and property-analyze a compound [for example, the agonist, antagonist and modulator (activity-modulating factor) of glutamate receptor functions] giving effects on the functions of a new metabotropic glutamate receptor. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：提供编码人代谢型谷氨酸受体蛋白亚型2和5的核酸，并提供编码它的蛋白质。解决方案：编码人代谢型谷氨酸受体mGluR2和mGlmR5亚型的核酸，可用于产生代谢型谷氨酸受体亚型。能够识别和分离相关受体亚基的探针。使用受体亚基来鉴定和分析化合物[例如，谷氨酸受体功能的激动剂，拮抗剂和调节剂（活性调节因子）]并对新代谢型谷氨酸受体的功能产生影响的方法。版权所有（C）2006，JPO＆NCIPI

3. 发明专利

JP2004147653A Human metabotropic glutamate receptors, nucleic acids encoding the same and use of the same 审中-公开
公开(公告)号：JP2004147653A
公开(公告)日：2004-05-27
申请号：JP2003362046
申请日：2003-10-22
申请人： Sibia Neurosciences Inc , シビア・ニューロサイエンシーズ・インコーポレイテッド
发明人： DAGGETT LORRIE P , ELLIS STEVEN B , LIAW CHEN , PONTSLER AARON , JOHNSON EDWIN C , HESS STEPHEN D
IPC分类号： G01N33/566 , A61K39/395 , A61K45/00 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07K14/705 , C07K16/28 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/00 , C12N5/10 , C12N15/02 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12Q1/02 , C12Q1/68 , C12R1/91 , G01N33/15 , G01N33/50 , G01N33/53
CPC分类号： G01N33/5091 , A01K2217/05 , C07K14/70571 , G01N33/5008 , G01N33/502 , G01N33/5058 , G01N2333/70571
摘要： PROBLEM TO BE SOLVED: To provide a nucleic acid encoding human metabotropic glutamate receptor subtypes and the protein encoded thereby. SOLUTION: The nucleic acids encode mGluR1, mGluR2, mGluR3 and mGluR5 subtypes of human metabotropic glutamate receptors. In addition to being useful for the production of metabotropic glutamate receptor subtypes, these nucleic acids 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 novel metabotropic glutamate receptor subtypes, the present invention includes methods for using such receptor subtypes to identify and characterize compounds which affect the function of such receptors, e.g., agonists, antagonists, and modulators of glutamate receptor function. COPYRIGHT: (C)2004,JPO

4. 发明申请

WO9902497A3 PYRIDINE DERIVATIVES 审中-公开
标题翻译：吡啶衍生物
公开(公告)号：WO9902497A3
公开(公告)日：1999-04-01
申请号：PCT/EP9804266
申请日：1998-07-09
申请人： NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , SIBIA NEUROSCIENCES INC , ALLGEIER HANS , AUBERSON YVES , BIOLLAZ MICHEL , COSFORD NICHOLAS DAVID , GASPARINI FABRIZIO , HECKENDORN ROLAND , JOHNSON EDWIN CARL , KUHN RAINER , VARNEY MARK ANDREW , VELICELEBI GOENUEL
发明人： ALLGEIER HANS , AUBERSON YVES , BIOLLAZ MICHEL , COSFORD NICHOLAS DAVID , GASPARINI FABRIZIO , HECKENDORN ROLAND , JOHNSON EDWIN CARL , KUHN RAINER , VARNEY MARK ANDREW , VELICELEBI GOENUEL
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61P9/10 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/50 , C07D213/52 , C07D213/53 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/89 , C07D215/12 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D409/06 , C07D413/06 , C07F7/08
CPC分类号： C07D213/06 , C07D213/16 , C07D213/26 , C07D213/30 , C07D213/50 , C07D213/52 , C07D213/53 , C07D213/55 , C07D213/56 , C07D213/57 , C07D213/65 , C07D213/74 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/89 , C07D215/12 , C07D401/06 , C07D401/10 , C07D405/06 , C07D409/06 , C07F7/0812
摘要： Compounds of the formula (I), wherein X and R1 to R5 are as defined in the description, are useful for treating disorders mediated full or in part by mGluR5.
摘要翻译：式（I）化合物，其中X和R 1至R 5如说明书中所定义，可用于治疗全部或部分由mGluR5介导的病症。

5. 发明申请

WO9928342A3 LOW-VOLTAGE ACTIVATED CALCIUM CHANNEL COMPOSITIONS AND METHODS 审中-公开
标题翻译：低压激活的钙通道组合物和方法
公开(公告)号：WO9928342A3
公开(公告)日：1999-08-26
申请号：PCT/US9825671
申请日：1998-12-03
申请人： SIBIA NEUROSCIENCES INC , WILLIAMS MARK , STAUDERMAN KENNETH , HARPOLD MICHAEL , HANS MICHAEL , URRUTIA ARTURO , WASHBURN MARK S
发明人： WILLIAMS MARK , STAUDERMAN KENNETH , HARPOLD MICHAEL , HANS MICHAEL , URRUTIA ARTURO , WASHBURN MARK S
IPC分类号： G01N33/483 , A61K38/00 , A61K45/00 , A61P1/16 , A61P5/00 , A61P9/00 , A61P11/00 , A61P13/00 , A61P25/00 , C07K14/705 , C12N1/15 , C12N1/19 , C12N5/10 , C12N15/09 , C12Q1/00 , C12Q1/68 , G01N33/566 , C12N15/12 , C07K16/28 , G01N33/68
CPC分类号： C07K14/705 , A61K38/00
摘要： Isolated nucleic acid encoding low voltage activated calcium channel subunits, including subunits encoded by nucleic acid that arises as splice variants of primary transcripts, is provided. Cells and vectors containing the nucleic acid and methods for identifying compounds that modulate the activity of calcium channels that contain these subunits are also provided.
摘要翻译：提供了编码低电压活化钙通道亚基的分离的核酸，包括由作为初级转录物的剪接变体产生的核酸编码的亚基。还提供了含有核酸的细胞和载体以及鉴定调节含有这些亚基的钙通道活性的化合物的方法。

6. 发明申请

WO1996029404A1 HUMAN METABOTROPIC GLUTAMATE RECEPTOR SUBTYPE mGluR6, NUCLEIC ACIDS ENCODING SAME AND USES THEREOF 审中-公开
标题翻译：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
申请人： SIBIA NEUROSCIENCES, INC. , DAGGETT, Lorrie, P. , LU, Chin-Chun
发明人： SIBIA NEUROSCIENCES, INC.
IPC分类号： C12N15/12
CPC分类号： G01N33/5008 , A01K2217/05 , C07K14/70571 , G01N33/502 , G01N33/5058 , G01N33/5091 , G01N2333/70571
摘要： 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.
摘要翻译：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。

7. 发明申请

WO1997019059A1 NOVEL SUBSTITUTED ARYL COMPOUNDS USEFUL AS MODULATORS OF ACETYLCHOLINE RECEPTORS 审中-公开
标题翻译：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
申请人： SIBIA NEUROSCIENCES, INC. , VERNIER, Jean, Michel , MCDONALD, Ian, A.
发明人： SIBIA NEUROSCIENCES, INC.
IPC分类号： C07D207/08
CPC分类号： C07D207/08 , C07D207/12 , C07D209/94 , C07D211/54
摘要： 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.
摘要翻译：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。

8. 发明申请

WO1996041876A1 HUMAN NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR COMPOSITIONS AND METHODS EMPLOYING SAME 审中-公开
标题翻译：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
申请人： SIBIA NEUROSCIENCES, INC. , ELLIOTT, Kathryn, J. , HARPOLD, Michael, M.
发明人： SIBIA NEUROSCIENCES, INC.
IPC分类号： C12N15/12
CPC分类号： G01N33/5008 , C07K14/70571 , G01N33/566
摘要： 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.
摘要翻译：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。

9. 发明申请

WO9631475A3 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
标题翻译：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
申请人： SIBIA NEUROSCIENCES INC , COSFORD NICHOLAS D , VERNIER JEAN MICHEL
发明人： COSFORD NICHOLAS D , VERNIER JEAN-MICHEL
IPC分类号： 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分类号： C07D401/06 , C07D213/38 , C07F7/0814
摘要： 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.
摘要翻译：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。

10. 发明申请

WO1996031475A2 SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS 审中-公开
标题翻译：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
申请人： SIBIA NEUROSCIENCES, INC. , COSFORD, Nicholas, D. , VERNIER, Jean-Michel
发明人： SIBIA NEUROSCIENCES, INC.
IPC分类号： C07D213/38
CPC分类号： C07D401/06 , C07D213/38 , C07F7/0814
摘要： 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.
摘要翻译：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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