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1. 发明专利

AU3061092A RECOMBINANT AMYLOID PRECURSOR PROTEIN INHIBITOR DOMAIN AND TREATMENT OF VARIOUS DISEASE STATES 未知
公开(公告)号：AU3061092A
公开(公告)日：1993-06-07
申请号：AU3061092
申请日：1992-10-30
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
发明人： STEVEN L WAGNER , ROBERT SIEGEL , GREGORY P THILL , MICHAEL M HARPOLD , WILLIAM T. COMER
IPC分类号： A61K38/00 , C07K14/81 , C12N1/19 , C12N15/15 , C12N15/81 , C12Q1/02 , C12Q1/37

2. 发明专利

AU2495792A HUMAN CALCIUM CHANNEL COMPOSITIONS AND METHODS 未知
公开(公告)号：AU2495792A
公开(公告)日：1993-03-16
申请号：AU2495792
申请日：1992-08-14
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
发明人： MICHAEL MILLER HARPOLD , STEVEN BRADLEY ELLIS , MARK EDWARD WILLIAMS , DANIEL HOWARD FELDMAN , ANN FRANCIS MCCUE , ROBERT BRENNER
IPC分类号： C12N5/10 , A61K38/00 , C07K14/705 , C12N15/09 , C12N15/12 , C12P21/02 , C12Q1/68 , C12R1/91

3. 发明申请

WO1996020949A1 PEPTIDE AND PEPTIDE ANALOG PROTEASE INHIBITORS 审中-公开
标题翻译：肽和肽类似物蛋白酶抑制剂
公开(公告)号：WO1996020949A1
公开(公告)日：1996-07-11
申请号：PCT/US1996000359
申请日：1996-01-05
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , MCDONALD, Ian, Alexander , ALBRECHT, Elisabeth , MUNOZ, Benito , ROWE, Blake, Alan , SIEGEL, Robert, Steven , WAGNER, Steven, Lee
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
IPC分类号： C07K05/06
CPC分类号： C07K5/0808 , A61K38/00 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06139 , C07K5/06165 , C07K5/06191
摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I) and (II), in which R1 is preferably 2-methyl propene, 2-butene, cyclohexyl or cyclohexylmethyl; R2, R4, and R8 are each independently methyl or ethyl; R3 is preferably iso-butyl or phenyl; R5 is preferably iso-butyl; R6 is H or methyl; R7 - (Q)n is preferably benzyloxycarbonyl or acetyl; Q is preferably -C(O)-; RB is preferably iso-butyl; RA = -(T)m-(D)m-R1, in which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C3-4 alkenyl; and X is preferably a alpha -ketoester or alpha -ketoamide or aldehyde.
摘要翻译：提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。其中R 1优选为2-甲基丙烯，2-丁烯，环己基或环己基甲基;式（I）和（II） R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R 7 - （Q）n优选为苄氧基羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X优选为α-酮酯或α-酮酰胺或醛。

4. 发明申请

WO1995004822A1 HUMAN CALCIUM CHANNEL COMPOSITIONS AND METHODS USING THEM 审中-公开
标题翻译：人体钙通道组合物及其使用方法
公开(公告)号：WO1995004822A1
公开(公告)日：1995-02-16
申请号：PCT/US1994009230
申请日：1994-08-11
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , HARPOLD, Michael, M. , ELLIS, Steven, B. , WILLIAMS, Mark, E. , McCUE, Ann, F. , GILLESPIE, Alison
IPC分类号： C12N15/12
CPC分类号： G01N33/6872 , C07K14/705 , C12Q1/6876 , C12Q2600/158 , G01N33/5008 , G01N33/502 , G01N33/5091
摘要： Isolated DNA encoding each of human calcium chanel alpha 1-, alpha 2-, beta - and gamma -subunits, including subunits that arise as splice variants of primary transcripts, is provided. In particular DNA clones encoding each of the alpha 1A-1, alpha 1A-2, alpha 1E-1, alpha 1C-2, alpha 1E-3, beta 3-1, beta 2C, beta 2D, beta 2E and beta 4 subunits of human calcium channels are provided. Cells and vectors containing the DNA, subunit specific antibodies and nucleic acid probes and methods for identifying compounds that modulate the activity of human calcium channels are also provided.
摘要翻译：提供了编码人类钙通道α1-，α2-，β-和γ-亚基的各自的分离的DNA，包括作为初级转录物的剪接变体产生的亚单位。特别是编码α1A-1，α1A-2，α1E-1，α1C-2，α1E-3，β3-1，β2C，β2A，β2E和β4亚单位的每个的DNA克隆的人钙通道。还提供了含有DNA，亚单位特异性抗体和核酸探针的细胞和载体以及用于鉴定调节人钙通道活性的化合物的方法。

5. 发明申请

WO1994029449A1 HUMAN METABOTROPIC GLUTAMATE RECEPTORS, NUCLEIC ACIDS ENCODING SAME AND USES THEREOF 审中-公开
标题翻译：人类代谢谷氨酸受体，编码其的核酸及其用途
公开(公告)号：WO1994029449A1
公开(公告)日：1994-12-22
申请号：PCT/US1994006273
申请日：1994-06-03
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , DAGGETT, Lorrie , ELLIS, Steven, B. , LIAW, Chen , PONTSLER, Aaron , JOHNSON, Edwin, C. , HESS, Stephen, D.
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
IPC分类号： C12N15/12
CPC分类号： G01N33/5091 , A01K2217/05 , C07K14/70571 , G01N33/5008 , G01N33/502 , G01N33/5058 , G01N2333/70571
摘要： In accordance with the present invention, there are provided nucleic acids encoding human metabotropic glutamate receptor subtypes and the proteins encoded thereby. In a particular embodiment, the invention 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 also comprises 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.
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的核酸和由此编码的蛋白质。在一个具体实施方案中，本发明的核酸编码人代谢型谷氨酸受体的mGluR1，mGluR2，mGluR3和mGluR5亚型。除了可用于代谢型谷氨酸受体亚型的生产之外，这些核酸也可用作探针，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。除了揭示新型代谢型谷氨酸受体亚型之外，本发明还包括使用这种受体亚型来鉴定和表征影响这些受体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。

6. 发明申请

WO1994024284A1 HUMAN N-METHYL-D-ASPARTATE RECEPTOR SUBUNITS, NUCLEIC ACIDS ENCODING SAME AND USES THEREFOR 审中-公开
标题翻译：人类N-甲基-D-孕激素受体亚型，编码其的核酸及其用途
公开(公告)号：WO1994024284A1
公开(公告)日：1994-10-27
申请号：PCT/US1994004387
申请日：1994-04-20
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , DAGGETT, Lorrie, P. , ELLIS, Steven, B. , LIAW, Chen, Wang , LU, Chin-Chun
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
IPC分类号： C12N15/12
CPC分类号： G01N33/5008 , A01K2217/05 , A61K38/00 , C07K14/70571 , G01N33/502 , G01N33/5041 , G01N33/5058 , G01N33/5091 , G01N33/6872 , G01N2333/70571
摘要： In accordance with the present invention, there are provided nucleic acids encoding human NMDA receptor protein subunits and the proteins encoded thereby. The NMDA receptor subunits of the invention comprise components of NMDA receptors that have cation-selective channels and bind glutamate and NMDA. In one aspect of the invention, the nucleic acids encode NMDAR1 and NMDAR2 subunits of human NMDA receptors. In a preferred embodiment, the invention nucleic acids encode NMDAR1, NMDAR2A, NMDAR2B, NMDAR2C and NMDAR2D subunits of human NMDA receptors. In addition to being useful for the production of NMDA receptor proteins subunit, 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. Functional glutamate receptors can be assembled, in accordance with the present invention, from a plurality of one type of NMDA receptor subunit protein (homomeric) or from a mixture of two or more types of subunit proteins (heteromeric). In addition to disclosing novel NMDA receptor protein subunits, the present invention also comprises methods for using such receptor subunits to identify and characterize compounds which affect the function of such receptors, e.g., agonists, antagonists, and modulators of glutamate receptor function. The invention also comprises methods for determining whether unknown protein(s) are functional as NMDA receptor subunits.
摘要翻译：根据本发明，提供了编码人NMDA受体蛋白质亚基的核酸和由此编码的蛋白质。本发明的NMDA受体亚基包含具有阳离子选择性通道并结合谷氨酸和NMDA的NMDA受体的组分。在本发明的一个方面，核酸编码人NMDA受体的NMDAR1和NMDAR2亚基。在优选的实施方案中，本发明核酸编码人NMDA受体的NMDAR1，NMDAR2A，NMDAR2B，NMDAR2C和NMDAR2D亚基。除了可用于制备NMDA受体蛋白亚基之外，这些核酸也可用作探针，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。功能性谷氨酸受体可以根据本发明从多种一种NMDA受体亚基蛋白（同型）或两种或更多种亚基蛋白（异聚体）的混合物组装。除了公开新的NMDA受体蛋白质亚基之外，本发明还包括使用这些受体亚基来鉴定和表征影响这些受体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。本发明还包括用于确定未知蛋白质是否作为NMDA受体亚基起作用的方法。

7. 发明申请

WO1996020725A2 PEPTIDE, PEPTIDE ANALOG AND AMINO ACID ANALOG PROTEASE INHIBITORS 审中-公开
标题翻译：肽，肽类似物和氨基酸类似物蛋白酶抑制剂
公开(公告)号：WO1996020725A2
公开(公告)日：1996-07-11
申请号：PCT/US1996000360
申请日：1996-01-05
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , MUNOZ, Benito , MCDONALD, Ian, Alexander , ALBRECHT, Elisabeth
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
IPC分类号： A61K38/55
CPC分类号： C07K5/0808 , A61K38/00 , C07C237/22 , C07K5/0202 , C07K5/0205 , C07K5/06043 , C07K5/06078 , C07K5/06165 , C07K5/06191
摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III), in which R1 is preferably 2-methyl propene, 2-butene, norleucine; R2, R4, and R8 are each independently methyl or ethyl; R3 is preferably iso-butyl or phenyl; R5 is preferably iso-butyl; R6 is H or methyl; R7 - (Q)n is preferably benzyloxycarbonyl or acetyl; Q is preferably -C(O)-; RB is preferably iso-butyl; RA = -(T)m-(D)m-R1, in which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C3-4 alkenyl; and X is an alcohol, particularly a secondary alcohol.
摘要翻译：提供了化合物和化合物用于治疗以淀粉样蛋白沉积为特征的疾病的方法。其中R 1优选为2-甲基丙烯，2-丁烯，正亮氨酸;式（I），（II）和（III） R2，R4和R8各自独立地为甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R 7 - （Q）n优选为苄氧基羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X是醇，特别是仲醇。

8. 发明申请

WO1996015123A1 PYRIDINE MODULATORS OF ACETYLCHOLINE RECEPTORS 审中-公开
标题翻译：乙酰胆碱受体的吡啶类调节剂
公开(公告)号：WO1996015123A1
公开(公告)日：1996-05-23
申请号：PCT/US1995013068
申请日：1995-10-16
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , MC DONALD, Ian, A. , WHITTEN, Jeffrey, P. , COSFORD, Nicholas, D.
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D405/14 , C07F7/0814
摘要： In accordance with the present invention, there is provided a class of pyridine compounds of formula (I) which are modulators of acetylcholine receptors. 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 disorder); 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，提供了一类式（I）的吡啶化合物，其是乙酰胆碱受体的调节剂。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。

9. 发明申请

WO1996011931A1 POLYCYCLIC FUSED RING MODULATORS OF ACETYLCHOLINE RECEPTORS 审中-公开
标题翻译：乙酰胆碱受体的多环融合环调节剂
公开(公告)号：WO1996011931A1
公开(公告)日：1996-04-25
申请号：PCT/US1995012905
申请日：1995-09-28
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , WHITTEN, Jeffrey, P. , MCDONALD, Ian, A. , VERNIER, Jean-Michel
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
IPC分类号： C07D471/04
CPC分类号： C07D491/14 , C07D471/04
摘要： In accordance with the present invention, there is provided a class of polycyclic fused ring compounds of formula (I) which are modulators of acetylcholine receptors. 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.
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式（I）的多环稠环化合物。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。

10. 发明申请

WO1996005488A1 AUTOMATED SYSTEM AND METHOD FOR SIMULTANEOUSLY PERFORMING A PLURALITY OF SIGNAL-BASE ASSAYS 审中-公开
标题翻译：自动化系统和方法同时执行大量信号基准测试
公开(公告)号：WO1996005488A1
公开(公告)日：1996-02-22
申请号：PCT/US1995008261
申请日：1995-06-30
申请人： SCIENCE APPLICATIONS INTERNATIONAL CORPORATION , THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC.
发明人： SCIENCE APPLICATIONS INTERNATIONAL CORPORATION , THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ASSOCIATES, INC. , McNEIL, John, A. , AKONG, Michael, A. , MIERZESKI, Donald, J. , VELICELEBI, Gonul , KARLTON, David, P.
IPC分类号： G01J03/30
CPC分类号： G01N35/0099 , B01J2219/00315 , B01J2219/00585 , B01J2219/00659 , B01J2219/00689 , B01J2219/00695 , B01J2219/00702 , C40B60/14 , G01N33/5302 , G01N33/5304 , G01N35/0092 , G01N35/028 , G01N35/1065 , G01N2035/00752 , G01N2035/0093 , Y10T436/115831
摘要： An automated detection system includes a robotic fluid-handling system for performing a plurality of assays; a detection system for imaging the assays as they are performed; and a computer control, data acquisition, and data analysis system for controlling the operation of the fluid-handling and detection system and for collecting and analyzing imaging data. The automated detection system comprises a pipettor for simultaneously distributing a predetermined amount of a liquid and a signal-generating element to each of the plurality of wells; an excitation source for simultaneously exposing the wells to excitation radiation; a detector for simultaneously detecting signal emitted from each of the wells over a period of time comprising a single imager for optically imaging the plurality of wells simultaneously; and computerized controller for simultaneously coordinating the pipettor, the excitation source, and the detector. Further, a method for performing simultaneous assays includes the steps of simultaneously distributing a predetermined amount of a liquid solution to each of a plurality of samples, simultaneously exposing the wells to excitation radiation, simultaneously detecting signals emitted from the wells using a detector comprising a single imaging means, and simultaneously controlling and coordinating the distribution, excitation, and detection using a computerized controller.
摘要翻译：一种自动检测系统，包括用于执行多个测定的机器人流体处理系统; 用于在进行测定时对分析进行成像的检测系统; 以及用于控制流体处理和检测系统的操作并用于收集和分析成像数据的计算机控制，数据采集和数据分析系统。该自动检测系统包括移液器，用于同时将预定量的液体和信号产生元件分配到多个孔中的每一个; 用于同时将阱暴露于激发辐射的激发源; 检测器，用于同时检测在一段时间内从每个孔发射的信号，包括单个成像器，用于同时对多个孔进行光学成像; 和计算机控制器，用于同时协调移液器，激发源和检测器。此外，用于执行同时测定的方法包括以下步骤：将预定量的液体溶液分配到多个样品中的每一个，同时将孔暴露于激发辐射，同时使用检测器检测从孔发射的信号，所述检测器包括单个成像装置，并且使用计算机控制器同时控制和协调分布，激励和检测。

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