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1. 发明申请

WO2004040003A2 NUCLEOTIDE-BINDING PROTEIN-DIRECTED PROBES AND METHODS OF THEIR SYNTHESIS AND USE 审中-公开
标题翻译：核苷酸结合蛋白质定向探针及其合成和使用方法
公开(公告)号：WO2004040003A2
公开(公告)日：2004-05-13
申请号：PCT/US2003/034550
申请日：2003-10-29
申请人： ACTIVX BIOSCIENCES, INC. , CAMPBELL, David, Alan , SZARDENINGS, Anna, Katrin , SHREDER, Kevin, Robert , BETANCORT, Juan, Manuel , WINN, David
发明人： CAMPBELL, David, Alan , SZARDENINGS, Anna, Katrin , SHREDER, Kevin, Robert , BETANCORT, Juan, Manuel , WINN, David
IPC分类号： C12Q
CPC分类号： C07H19/23 , C07D405/12 , C07D405/14 , C07D473/00 , C07D487/14 , G01N33/573
摘要： The present invention provides nucleotide binding protein-directed affinity probes ("NBAPS"), and methods of their preparation and use. The subject methods and compositions can provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of nucleotide binding proteins in a complex protein mixture, preferably kinases, and most preferably active forms of kinases, using NBAPs that bind to target nucleotide binding protein(s). The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.
摘要翻译：本发明提供了核苷酸结合蛋白指导的亲和探针（“NBAPS”），以及它们的制备和使用方法。主题方法和组合物可以提供增强的简单性和准确性，以鉴定复杂蛋白质混合物（优选激酶）中核苷酸结合蛋白的存在，量或活性的变化，优选激酶的活性形式，使用结合靶核苷酸的NBAP 结合蛋白（一种或多种）。本文所述的概况分析方法可以具有导致鉴定复杂蛋白质混合物中的靶核苷酸结合蛋白的多个步骤。

2. 发明申请

WO2013176698A1 CARBOLINE AND CARBAZOLE BASED IMAGING AGENTS FOR DETECTING NEUROLOGICAL DYSFUNCTION 审中-公开
标题翻译：基于CARBOLINE和CARBAZOLE的成像剂用于检测神经性功能障碍
公开(公告)号：WO2013176698A1
公开(公告)日：2013-11-28
申请号：PCT/US2012/061912
申请日：2012-10-25
申请人： ELI LILLY AND COMPANY , SZARDENINGS, Anna Katrin , KOLB, Hartmuth C. , WALSH, Joseph C. , CHEN, Gang , GANGADHARMATH, Umesh B. , KASI, Dhanalakshmi , LIU, Changhui , SINHA, Anjana , WANG, Eric , YU, Chul , ZHANG, Wei , CHEN, Kai , MOCHARLA, Vani P. , SCOTT, Peter J.H.
发明人： SZARDENINGS, Anna Katrin , KOLB, Hartmuth C. , WALSH, Joseph C. , CHEN, Gang , GANGADHARMATH, Umesh B. , KASI, Dhanalakshmi , LIU, Changhui , SINHA, Anjana , WANG, Eric , YU, Chul , ZHANG, Wei , CHEN, Kai , MOCHARLA, Vani P. , SCOTT, Peter J.H.
IPC分类号： C07D209/88 , C07D403/12 , C07D471/04 , C07D471/14 , A61K51/04 , A61K49/10 , C07B59/00
CPC分类号： C07D209/88 , C07B59/002 , C07D209/80 , C07D403/12 , C07D471/04 , C07D471/14
摘要： Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, allowing the com¬ pound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal mal is suffering from or is at risk of developing Alzheimer's Disease. The claimed compounds have the structure of formula (I) wherein: L is N or CR5, M is N or CR6; P is N or CR7; and Q is N or CR8; X is a bond or is Cl-14alkyl, wherein at least one carbon is optionally replaced by C(O), 0, S, S02, or NH, NH-Cl-8alkyl, and wherein at least one H of Cl-8alkyl is optionally replaced by halo, OH, Cl-6alkyl; wherein at least one halo is optionally replaced with a radionuclide or a fluorescent tag. The other variables are as defined in the claims.
摘要翻译：本文公开了在哺乳动物中诊断阿尔茨海默氏病或其倾向的化合物和方法，所述方法包括向哺乳动物施用诊断有效量的放射性标记化合物，允许该组分分布于脑组织中，并使脑成像组织，其中与正常对照水平的结合相比，化合物与脑组织的结合增加表明哺乳动物的马曾患有或有发展为阿尔茨海默病的风险。所要求保护的化合物具有式（I）的结构，其中：L是N或CR 5，M是N或CR 6; P为N或CR7; Q为N或CR8; X是一个键或是C 1-4烷基，其中至少一个碳任选地被C（O），O，S，SO 2或NH，NH-C 1-8烷基取代，并且其中至少一个C 1-8烷基的H 任选被卤素，OH，C 1-6烷基取代; 其中至少一个卤素任选被放射性核素或荧光标记替代。其他变量如权利要求中所定义。

3. 发明申请

WO2011119565A1 IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 审中-公开
标题翻译：用于检测神经疾病的成像剂
公开(公告)号：WO2011119565A1
公开(公告)日：2011-09-29
申请号：PCT/US2011/029368
申请日：2011-03-22
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , CASHION, Daniel, Kurt , CHEN, Gang , KASI, Dhanalakshmi , KOLB, Hartmuth C. , LIU, Changhui , SINHA, Anjana , SZARDENINGS, Anna, Katrin , WANG, Eric , YU, Chul , ZHANG, Wei , GANGADHARMATH, Umesh, B. , WALSH, Joseph, C.
发明人： CASHION, Daniel, Kurt , CHEN, Gang , KASI, Dhanalakshmi , KOLB, Hartmuth C. , LIU, Changhui , SINHA, Anjana , SZARDENINGS, Anna, Katrin , WANG, Eric , YU, Chul , ZHANG, Wei , GANGADHARMATH, Umesh, B. , WALSH, Joseph, C.
IPC分类号： C07D235/04 , C07D401/02 , A61K31/4184 , A61K31/4353 , A61P25/00
CPC分类号： C07D235/04 , A61K51/04 , C07B59/002 , C07D215/06 , C07D235/14 , C07D277/62 , C07D401/02 , C07D401/04 , C07D403/06 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04
摘要： Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Αβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders. Formula (V) or a pharmaceutically acceptable salt thereof, and stereoisomers thereof, wherein: X 25 -X 28 are each independently CH, CR 11 , or N; X 29 is CH, N, O or S; X 30 is CH, C, or N; X 31-34 are each independently CH, CR 12 , CR 13 or N; RII-RU are each independently H, halogen, hydroxy, nitro, cyano, ammo, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy,— (O-CH 2 - CH 2 ) n -, alkenyL alkynyl, aryloxy, NRl0COOalkyl, NRl0 COOaryU NRW COalkyl, NR 10 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein at least one carbon of R 11 -R 13 is optionally replaced with N, Q, S, triazole, or halo, and, wherein at least one hydrogen is optionally replaced with halo, amine, amino, alkoxy, nitro, alkyl, alkenyL alkynyl, aryloxy, alkylaryl, alkylamino, alkylamine, NRioCOOalkyl, NR 10 COOaryl, NR 10 COalkyl, NR,0 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic saturated heterocycle and unsaturated heterocycle, a leaving group, CN, OH or a radioactive isotope.
摘要翻译：式（I） - （V）的成像剂和用于检测神经障碍的方法包括向需要的患者施用能够结合tau蛋白和β-淀粉样肽的式（I） - （V）化合物。本发明还涉及成像β和tau聚集体的方法，包括引入可检测量的包含放射性标记的式（I） - （V）化合物的药物制剂，并检测与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物患者。这些方法和组合使得临床前诊断和监测AD和其他神经障碍的进展。式（V）或其药学上可接受的盐及其立体异构体，其中：X25-X28各自独立地为CH，CR11或N; X29是CH，N，O或S; X30是CH，C或N; X31-34各自独立地为CH，CR12，CR13或N; RII-RU各自独立地为H，卤素，羟基，硝基，氰基，氨基，烷基，烷基芳基，烷基氨基，烷基胺，芳基胺，芳基氨基，烷氧基， - （O-CH 2 -CH 2）n - 烯基炔基，芳氧基，NR 10 COO烷基， NR10 COOaryU NRW CO烷基，NR10CO芳基，COO烷基，COO芳基，CO烷基，芳基，芳基，环烷基，环烷基氨基，环烷基胺，双环，饱和杂环和不饱和杂环，其中R11-R13的至少一个碳任选被N，Q，烷基，烯基炔基，芳氧基，烷基芳基，烷基氨基，烷基胺，NROCOO烷基，NR10 COO芳基，NR10CO烷基，NR 芳基，环烷基，环烷基氨基，环烷基胺，双环饱和杂环和不饱和杂环，离去基团，CN，OH或放射性同位素。

4. 发明申请

WO2004040003A3 NUCLEOTIDE-BINDING PROTEIN-DIRECTED PROBES AND METHODS OF THEIR SYNTHESIS AND USE 审中-公开
标题翻译：核蛋白结合蛋白质指导的探针及其合成与使用方法
公开(公告)号：WO2004040003A3
公开(公告)日：2004-12-23
申请号：PCT/US0334550
申请日：2003-10-29
申请人： ACTIVX BIOSCIENCES INC , CAMPBELL DAVID ALAN , SZARDENINGS ANNA KATRIN , SHREDER KEVIN ROBERT , BETANCORT JUAN MANUEL , WINN DAVID
发明人： CAMPBELL DAVID ALAN , SZARDENINGS ANNA KATRIN , SHREDER KEVIN ROBERT , BETANCORT JUAN MANUEL , WINN DAVID
IPC分类号： C07D405/12 , C07D405/14 , C07D473/00 , C07D487/14 , C07H19/23 , G01N33/573 , A61K38/00
CPC分类号： C07H19/23 , C07D405/12 , C07D405/14 , C07D473/00 , C07D487/14 , G01N33/573
摘要： The present invention provides nucleotide binding protein-directed affinity probes ("NBAPS"), and methods of their preparation and use. The subject methods and compositions can provide enhanced simplicity and accuracy in identifying changes in the presence, amount, or activity of nucleotide binding proteins in a complex protein mixture, preferably kinases, and most preferably active forms of kinases, using NBAPs that bind to target nucleotide binding protein(s). The profiling methods described herein can have a number of steps leading to the identification of target nucleotide binding protein(s) in a complex protein mixture.
摘要翻译：本发明提供了核苷酸结合蛋白质指导的亲和探针（“NBAPS”）及其制备和使用方法。本发明的方法和组合物可以使用结合靶核苷酸的NBAP来鉴定复合蛋白混合物中优选激酶，最优选活性形式的激酶中核苷酸结合蛋白的存在，量或活性的变化的简单性和准确性结合蛋白。本文描述的谱分析方法可以具有导致鉴定复合蛋白质混合物中的靶核苷酸结合蛋白的多个步骤。

5. 发明申请

WO2013028664A1 PSMA IMAGING AGENTS 审中-公开
标题翻译： PSMA成像代理
公开(公告)号：WO2013028664A1
公开(公告)日：2013-02-28
申请号：PCT/US2012/051674
申请日：2012-08-21
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , WANG, Eric , KOLB, Hartmuth C. , SZARDENINGS, Anna Katrin , LIU, Changhui , WALSH, Joseph C. , CHEN, Gang , SINHA, Anjana , KASI, Dhanalakshmi , YU, Chul , GANGADHARMATH, Umesh B. , ZHANG, Wei , ZHAO, Tieming , MOCHARLA, Vani P.
发明人： WANG, Eric , KOLB, Hartmuth C. , SZARDENINGS, Anna Katrin , LIU, Changhui , WALSH, Joseph C. , CHEN, Gang , SINHA, Anjana , KASI, Dhanalakshmi , YU, Chul , GANGADHARMATH, Umesh B. , ZHANG, Wei , ZHAO, Tieming , MOCHARLA, Vani P.
IPC分类号： A61K51/08 , C07K5/02 , C07K5/06 , C07D223/16 , A61P35/00
CPC分类号： C07K5/0215 , A61K38/00 , A61K51/0453 , A61K51/088 , C07D207/16 , C07D209/48 , C07D213/81 , C07D213/82 , C07D233/78 , C07D233/96 , C07D239/60 , C07D249/04 , C07D249/06 , C07D251/30 , C07D263/34 , C07D277/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07K5/06026 , C07K5/06113
摘要： Compounds for targeting and agents for imaging, Prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
摘要翻译：公开了靶向化合物和成像剂，前列腺特异性膜抗原（PSMA）。还公开了合成化合物和成像剂的方法以及PSMA成像方法。所公开的成像剂适用于PET和SPECT成像。

6. 发明申请

WO2010111303A3 IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 审中-公开
公开(公告)号：WO2010111303A3
公开(公告)日：2010-09-30
申请号：PCT/US2010/028360
申请日：2010-03-23
申请人： SIEMENS MEDICAL SOLUTIONS USA, INC. , GANGADHARMATH, Umesh, B. , KOLB, Hartmuth, C. , SCOTT, Peter, J.H. , WALSH, Joseph, C. , ZHANG, Wei , SZARDENINGS, Anna, Katrin , SINHA, Anjana , CHEN, Gang , WANG, Eric , MOCHARLA, Vani, P. , YU, Chul , LIU, Changhui , CASHION, Daniel, Kurt , KASI, Dhanalakshmi
发明人： GANGADHARMATH, Umesh, B. , KOLB, Hartmuth, C. , SCOTT, Peter, J.H. , WALSH, Joseph, C. , ZHANG, Wei , SZARDENINGS, Anna, Katrin , SINHA, Anjana , CHEN, Gang , WANG, Eric , MOCHARLA, Vani, P. , YU, Chul , LIU, Changhui , CASHION, Daniel, Kurt , KASI, Dhanalakshmi
IPC分类号： A61K51/04 , C07D215/00 , C07D235/04 , C07D263/52 , C07D277/62 , C07B59/00
摘要： Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering ti a patient in need compounds of formula (I) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disoders.

7. 发明申请

WO2003079014A1 TETHERED ACTIVITY-BASED PROBES AND USES THEREOF 审中-公开
标题翻译：基于活动的活动探索及其用途
公开(公告)号：WO2003079014A1
公开(公告)日：2003-09-25
申请号：PCT/US2003/007898
申请日：2003-03-12
申请人： ACTIVX BIOSCIENCES, INC. , SHREDER, Kevin, Robert , CAMPBELL, David, Alan , SZARDENINGS, Anna, Katrin
发明人： SHREDER, Kevin, Robert , CAMPBELL, David, Alan , SZARDENINGS, Anna, Katrin
IPC分类号： G01N33/53
CPC分类号： C40B30/04
摘要： Methods and compositions are described for analyzing complex protein mixtures, such as proteomes, using activity-based probes. In particular, probes that specifically react with and bind to the active form of one or more target proteins are employed. Labeled proteins and/or peptides can be sequestered using a tABP covalently bound (“tethered”) to a solid phase, and, upon cleavage of the tether, can be related to the identity, presence, amount, or activity of active members of the desired target protein class. The methods and compositions described herein can be used, for example, to provide diagnostic information concerning pathogenic states, in identifying proteins that may act as therapeutic targets, and in drug discovery.
摘要翻译：描述了使用基于活性的探针分析复合蛋白质混合物（如蛋白质组）的方法和组合物。特别地，使用与一种或多种靶蛋白的活性形式特异性反应并结合的探针。标记的蛋白质和/或肽可以使用共价结合（“系留”）到固相的tABP隔离，并且在系链切割时可以与所述系统的活性成员的身份，存在，量或活性相关所需目标蛋白质类。本文描述的方法和组合物可用于例如提供关于致病状态的诊断信息，鉴定可用作治疗靶标的蛋白质，以及在药物发现中。

8. 发明申请

WO1996023813A1 PEPTIDES AND COMPOUNDS THAT BIND TO SH2 DOMAINS 审中-公开
标题翻译：封装到SH2域的肽和化合物
公开(公告)号：WO1996023813A1
公开(公告)日：1996-08-08
申请号：PCT/US1996001544
申请日：1996-01-31
申请人： AFFYMAX TECHNOLOGIES N.V. , PATEL, Dinesh, V. , GORDEEV, Mikhail, F. , GORDON, Eric , GROVE, J., Russell , HART, Charles, P. , KIM, Moon, H. , SZARDENINGS, Anna, Katrin
发明人： AFFYMAX TECHNOLOGIES N.V.
IPC分类号： C07K07/00
CPC分类号： C07K14/705 , A61K38/00 , C07K1/047
摘要： The present invention generally relates to peptides and compounds which bind to the SH2 domain or domains of various proteins, as well as methods for identifying such peptides and compounds. These peptides and compounds have application as agonists and antagonists of SH2 domain containing proteins, and as diagnostic or therapeutic agents for the diagnosis or treatment of disease conditions.
摘要翻译：本发明一般涉及与各种蛋白质的SH2结构域或结构域结合的肽和化合物，以及用于鉴定这些肽和化合物的方法。这些肽和化合物可用作具有SH2结构域的蛋白质的激动剂和拮抗剂，以及用于诊断或治疗疾病状况的诊断或治疗剂。

9. 发明申请

WO1996000391A1 METHODS FOR THE SYNTHESIS OF DIKETOPIPERAZINES 审中-公开
标题翻译：合成二氯吡啶的方法
公开(公告)号：WO1996000391A1
公开(公告)日：1996-01-04
申请号：PCT/US1995007964
申请日：1995-06-23
申请人： AFFYMAX TECHNOLOGIES N.V. , CAMPBELL, David , GALLOP, Mark, A. , GORDON, Eric, M. , LOOK, Gary, C. , PATEL, Dinesh , SZARDENINGS, Anna, Katrin
发明人： AFFYMAX TECHNOLOGIES N.V.
IPC分类号： G01N33/53
CPC分类号： C07D241/08 , G01N33/54353 , G01N33/68
摘要： Libraries of diverse diketopiperazines bound to a support and methods for synthesizing diketopiperazines on a solid support are described. These libraries have utility in the area of drug design as they can be screened against biological substances to identify compounds which have desirable biological activity.
摘要翻译：描述了结合支持物的多种二酮哌嗪的文库和在固体载体上合成二酮哌嗪的方法。这些图书馆在药物设计领域具有实用性，因为它们可以针对生物物质进行筛选，以鉴别具有理想生物活性的化合物。

10. 发明申请

WO2010111303A2 IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 审中-公开
标题翻译：用于检测神经疾病的成像剂
公开(公告)号：WO2010111303A2
公开(公告)日：2010-09-30
申请号：PCT/US2010028360
申请日：2010-03-23
申请人： SIEMENS MEDICAL SOLUTIONS , GANGADHARMATH UMESH B , KOLB HARTMUTH C , SCOTT PETER J H , WALSH JOSEPH C , ZHANG WEI , SZARDENINGS ANNA KATRIN , SINHA ANJANA , CHEN GANG , WANG ERIC , MOCHARLA VANI P , YU CHUL , LIU CHANGHUI , CASHION DANIEL KURT , KASI DHANALAKSHMI
发明人： GANGADHARMATH UMESH B , KOLB HARTMUTH C , SCOTT PETER J H , WALSH JOSEPH C , ZHANG WEI , SZARDENINGS ANNA KATRIN , SINHA ANJANA , CHEN GANG , WANG ERIC , MOCHARLA VANI P , YU CHUL , LIU CHANGHUI , CASHION DANIEL KURT , KASI DHANALAKSHMI
IPC分类号： A61K51/04 , C07B59/00 , C07D215/00 , C07D235/04 , C07D263/52 , C07D277/62
CPC分类号： A61K51/0455 , A61K51/04 , A61K51/0453 , A61K51/0459 , A61K51/0463 , C07B59/002 , C07D215/06 , C07D235/14 , C07D277/62 , C07D401/04 , C07D403/06 , C07D413/10 , C07D413/14 , C07D487/04
摘要： Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering ti a patient in need compounds of formula (I) capable of binding to tau proteins and ß-amyloid peptides are presented herein. The invention also relates to methods of imaging Aß and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disoders.
摘要翻译：式（I）的成像剂和用于检测神经障碍的方法包括给予需要能够结合tau蛋白和β-淀粉样蛋白肽的式（I）化合物的化合物。本发明还涉及成像Aβ和tau聚集体的方法，包括引入可检测量的包含放射性标记的式（I）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。这些方法和组合使得AD和其他神经系统解剖器的临床前诊断和监测进展。

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