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1. 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。

2. 发明专利

CA2756137A1 IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 未知
公开(公告)号：CA2756137A1
公开(公告)日：2010-09-30
申请号：CA2756137
申请日：2010-03-23
申请人： SIEMENS MEDICAL SOLUTIONS
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
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.

3. 发明专利

CA2794004C IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 未知
公开(公告)号：CA2794004C
公开(公告)日：2016-04-26
申请号：CA2794004
申请日：2011-03-22
申请人： SIEMENS MEDICAL SOLUTIONS
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 , A61K31/4184 , A61K31/4353 , A61P25/00 , C07D401/02
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 ß-amyloid peptides are presented herein. The invention also relates to methods of imaging ?ß 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: X25-X28 are each independently CH, CR11, or N; X29 is CH, N, O or S; X30 is CH, C, or N; X31-34 are each independently CH, CR12, CR13 or N; RII-RU are each independently H, halogen, hydroxy, nitro, cyano, ammo, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy, (O-CH2- CH2)n-, alkenyL alkynyl, aryloxy, NRl0COOalkyl, NRl0 COOaryU NRW COalkyl, NR10 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein at least one carbon of R11-R13 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, NR10 COOaryl, NR10 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.

4. 发明专利

CA2756137C IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 未知
公开(公告)号：CA2756137C
公开(公告)日：2015-11-24
申请号：CA2756137
申请日：2010-03-23
申请人： SIEMENS MEDICAL SOLUTIONS
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： C07D487/04 , A61K51/04 , 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 .beta.-amyloid peptides are presented herein. The invention also relates to methods of imaging A.beta. 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.

5. 发明专利

CA2794004A1 IMAGING AGENTS FOR DETECTING NEUROLOGICAL DISORDERS 未知
公开(公告)号：CA2794004A1
公开(公告)日：2011-09-29
申请号：CA2794004
申请日：2011-03-22
申请人： SIEMENS MEDICAL SOLUTIONS
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 , A61K31/4184 , A61K31/4353 , A61P25/00 , C07D401/02
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 ß-amyloid peptides are presented herein. The invention also relates to methods of imaging ß 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: X25-X28 are each independently CH, CR11, or N; X29 is CH, N, O or S; X30 is CH, C, or N; X31-34 are each independently CH, CR12, CR13 or N; RII-RU are each independently H, halogen, hydroxy, nitro, cyano, ammo, alkyl, alkylaryl, alkylamino, alkylamine, arylamine, arylamino, alkoxy, (O-CH2- CH2)n-, alkenyL alkynyl, aryloxy, NRl0COOalkyl, NRl0 COOaryU NRW COalkyl, NR10 CO aryl, COOalkyl, COOaryl, COalkyl, COaryl, aryl, cycloalkyl, cycloalkylamino, cycloalkylamine, bicyclic, saturated heterocycle and unsaturated heterocycle, wherein at least one carbon of R11-R13 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, NR10 COOaryl, NR10 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.

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