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1. 发明申请

WO2007005935A3 NOREPINEPHRINE TRANSPORTER RADIOTRACERS AND METHODS OF SYNTHESES THEREOF 审中-公开
公开(公告)号：WO2007005935A3
公开(公告)日：2007-01-11
申请号：PCT/US2006/026138
申请日：2006-07-06
申请人： MOLECULAR NEUROIMAGING, LLC , TAMAGNAN, Gilles, D. , ALAGILLE, David
发明人： TAMAGNAN, Gilles, D. , ALAGILLE, David
IPC分类号： C07D265/30 , A61P25/22 , A61K31/5375 , A61P25/24 , A61K51/04 , A61P25/30
摘要： The present invention provides compounds and radiotracers thereof for locating, diagnosing, identifying, evaluating, detecting or quantitating NET by in vivo imaging. The invention also provides methods for locating, diagnosing, identifying, evaluating, detecting or quantitating NET, using radiotracers of high-affinity or labeled compounds of the invention, which exhibit low toxicity, can cross the blood-brain barrier and, preferably, distinguish among normal and abnormal brains. For example, a radiotracer of the invention can be administered to a patient in an amount suitable for in vivo imaging thereof. Preferably, radiotracers of the invention can also be used to locate, diagnosis, identify, evaluate, detect and quantitate NET in such diseases, disorders, conditions or maladies as, without limitation, depression, anxiety, ADHD and drug dependency.

2. 发明申请

WO2007005935A2 NOREPINEPHRINE TRANSPORTER RADIOTRACERS AND METHODS OF SYNTHESES THEREOF 审中-公开
标题翻译： NOREPINEPHRINE TRANSPORTER RADIOTRACERS及其合成方法
公开(公告)号：WO2007005935A2
公开(公告)日：2007-01-11
申请号：PCT/US2006026138
申请日：2006-07-06
申请人： MOLECULAR NEUROIMAGING LLC , TAMAGNAN GILLES D , ALAGILLE DAVID
发明人： TAMAGNAN GILLES D , ALAGILLE DAVID
IPC分类号： A61K51/00
CPC分类号： A61K51/0463
摘要： The present invention provides compounds and radiotracers thereof for locating, diagnosing, identifying, evaluating, detecting or quantitating NET by in vivo imaging. The invention also provides methods for locating, diagnosing, identifying, evaluating, detecting or quantitating NET, using radiotracers of high-affinity or labeled compounds of the invention, which exhibit low toxicity, can cross the blood-brain barrier and, preferably, distinguish among normal and abnormal brains. For example, a radiotracer of the invention can be administered to a patient in an amount suitable for in vivo imaging thereof. Preferably, radiotracers of the invention can also be used to locate, diagnosis, identify, evaluate, detect and quantitate NET in such diseases, disorders, conditions or maladies as, without limitation, depression, anxiety, ADHD and drug dependency.
摘要翻译：本发明提供了用于通过体内成像定位，诊断，鉴定，评价，检测或定量NET的化合物和放射性示踪剂。本发明还提供了用于定位，诊断，鉴定，评价，检测或定量测定NET的方法，使用显示低毒性的本发明的高亲和性或标记化合物的放射性示踪剂可以穿过血脑屏障，并且优选区分正常和异常的大脑。例如，本发明的放射性示踪剂可以以适于其体内成像的量给予患者。优选地，本发明的放射性示踪剂还可以用于定位，诊断，鉴定，评估，检测和定量这些疾病，病症，病症或疾病中的NET，而不限于抑郁，焦虑，ADHD和药物依赖性。

3. 发明申请

WO2008118122A2 COMPOUNDS AND AMYLOID PROBES THEREOF FOR THERAPEUTIC AND IMAGING USES 审中-公开
标题翻译：用于治疗和成像用途的化合物和淀粉样物质探针
公开(公告)号：WO2008118122A2
公开(公告)日：2008-10-02
申请号：PCT/US2007/011123
申请日：2007-05-08
申请人： MOLECULAR NEUROIMAGING, LLC
发明人： TAMAGNAN, Gilles, D. , ALAGILLE, David , BARBOSA, Herve DaCosta
IPC分类号： A61K51/00 , C07D498/02 , C07D487/04 , C07D277/84
CPC分类号： A61K31/424 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/421 , A61K51/0453 , A61K51/0455 , A61K51/0459 , C07D249/20 , C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention provides compounds and amyloid probes thereof that allow for an antemortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the regions of the brain. Preferably, an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain. An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits. Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation, Down's syndrome, familial AD and homozygotes for the apolipoprotein E4 allele. In one aspect, the compounds may be used in the treatment or prophylaxis of diseases that include, without limitation, AD and type 2 diabetes mellitus. The compounds and amyloid probes of the invention include analogs, salts, pharmaceutical compositions, derivatives, prodrugs, racemic mixtures or tautomeric forms thereof.
摘要翻译：本发明提供了化合物和淀粉样蛋白探针，其允许通过体内成像脑区域中的淀粉样蛋白和/或淀粉样蛋白沉积物来诊断AD并且通过淀粉样蛋白和/或淀粉样蛋白沉积物的淀粉样蛋白沉积物（斑块）的程度或进展来量化抗肿瘤方法。优选地，本发明的淀粉样蛋白探针可以穿过血脑屏障并将AD脑与正常脑区分开。淀粉样蛋白探针可以以适于淀粉样蛋白沉积物的体内成像的量施用于患者。本发明的淀粉样蛋白探针还可用于检测和定量疾病中的淀粉样蛋白沉积物，包括但不限于唐氏综合征，家族性AD和载脂蛋白E4等位基因的纯合子。一方面，所述化合物可用于治疗或预防包括但不限于AD和2型糖尿病的疾病。本发明的化合物和淀粉样蛋白探针包括类似物，盐，药物组合物，衍生物，前药，外消旋混合物或其互变异构形式。

4. 发明申请

WO2008118122A8 COMPOUNDS AND AMYLOID PROBES THEREOF FOR THERAPEUTIC AND IMAGING USES 审中-公开
标题翻译：用于治疗和成像用途的化合物和淀粉样物质探针
公开(公告)号：WO2008118122A8
公开(公告)日：2009-02-05
申请号：PCT/US2007011123
申请日：2007-05-08
申请人： MOLECULAR NEUROIMAGING LLC
发明人： TAMAGNAN GILLES D , ALAGILLE DAVID , BARBOSA HERVE DACOSTA
IPC分类号： A61K31/41
CPC分类号： A61K31/424 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/421 , A61K51/0453 , A61K51/0455 , A61K51/0459 , C07D249/20 , C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention provides compounds and amyloid probes thereof that allow for an anlsmortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the 5 regions of the brain Preferably an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation Down's syndrome familial AD and homozygotes for the apolipoprotein 10 E4 allele The compounds and amyloid probes of the invention include analogs, salts, pharmaceutical compositions derivatives prodrugs, racemic mixtures or tautomeric forms thereof.
摘要翻译：本发明提供其化合物和淀粉样蛋白探针，其允许通过在脑的5个区域中淀粉样蛋白和/或淀粉样蛋白沉积物的体内成像来诊断AD并且定量淀粉样蛋白沉积物（斑块）的程度或进展的惰性方法。优选地，本发明的淀粉样蛋白探针可以穿过血脑屏障并将AD脑与正常脑区分开。淀粉样蛋白探针可以以适于淀粉样蛋白沉积的体内成像的量施用给患者。本发明的淀粉样蛋白探针也可用于检测和在疾病中定量淀粉样蛋白沉积物，包括但不限于唐氏综合征家族性AD和载脂蛋白10 E4等位基因的纯合子本发明的化合物和淀粉样蛋白探针包括类似物，盐，药物组合物衍生物前药，外消旋混合物或其互变异构形式。

5. 发明申请

WO2007035823A3 PARTIAL MGLUR5 ANTAGONISTS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2007035823A3
公开(公告)日：2007-03-29
申请号：PCT/US2006/036680
申请日：2006-09-20
申请人： MOLECULAR NEUROIMAGING, LLC , TAMAGNAN, Gilles, D. , ALAGILLE, David
发明人： TAMAGNAN, Gilles, D. , ALAGILLE, David
IPC分类号： A61K31/4178 , C07D401/06
摘要： The present invention provides compounds and pharmaceutical compositions thereof, which can comprise non-competitive antagonistic activity, preferably, partial non-competitive antagonistic activity at the metabotropic glutamate receptors (mGluR5). The compounds and pharmaceutical composition of the invention can be used to treat diseases, disorders and conditions such as, for example, anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders and the like. The invention also provides uses, methods and articles or manufacture that include one or more compounds or pharmaceutical compositions of the invention.

6. 发明申请

WO2007035823A2 PARTIAL MGLUR5 ANTAGONISTS AND METHODS OF USE THEREOF 审中-公开
标题翻译：部分MGLUR5拮抗剂及其使用方法
公开(公告)号：WO2007035823A2
公开(公告)日：2007-03-29
申请号：PCT/US2006036680
申请日：2006-09-20
申请人： MOLECULAR NEUROIMAGING LLC , TAMAGNAN GILLES D , ALAGILLE DAVID
发明人： TAMAGNAN GILLES D , ALAGILLE DAVID
IPC分类号： A61K31/505
CPC分类号： A61K31/505 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/506 , C07D213/06 , C07D213/30 , C07D213/61 , C07D239/26 , C07D241/12 , C07D409/06
摘要： The present invention provides compounds and pharmaceutical compositions thereof, which can comprise non-competitive antagonistic activity, preferably, partial non-competitive antagonistic activity at the metabotropic glutamate receptors (mGluR5). The compounds and pharmaceutical composition of the invention can be used to treat diseases, disorders and conditions such as, for example, anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders and the like. The invention also provides uses, methods and articles or manufacture that include one or more compounds or pharmaceutical compositions of the invention.
摘要翻译：本发明提供其可以包含非竞争性拮抗活性的化合物及其药物组合物，优选代谢型谷氨酸受体（mGluR5）处的部分非竞争性拮抗活性。本发明的化合物和药物组合物可用于治疗疾病，病症和病症，例如焦虑症，癫痫症，精神分裂症和其他精神病，帕金森病，成瘾性疾病等。本发明还提供包括本发明的一种或多种化合物或药物组合物的用途，方法和制品或制造。

7. 发明申请

WO2008118122A3 COMPOUNDS AND AMYLOID PROBES THEREOF FOR THERAPEUTIC AND IMAGING USES 审中-公开
标题翻译：用于治疗和成像用途的化合物和淀粉样物质探针
公开(公告)号：WO2008118122A3
公开(公告)日：2008-11-27
申请号：PCT/US2007011123
申请日：2007-05-08
申请人： MOLECULAR NEUROIMAGING LLC
发明人： TAMAGNAN GILLES D , ALAGILLE DAVID , BARBOSA HERVE DACOSTA
IPC分类号： A61K31/41
CPC分类号： A61K31/424 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/421 , A61K51/0453 , A61K51/0455 , A61K51/0459 , C07D249/20 , C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention provides compounds and amyloid probes thereof that allow for an anlsmortem method of diagnosing AD and quantitating the extent or progression of amyloid deposits (plaques) by in vivo imaging of amyloid and/or amyloid deposits in the 5 regions of the brain Preferably an amyloid probe of the invention can cross the blood-brain barrier and distinguish AD brain from normal brain An amyloid probe can be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits Amyloid probes of the invention can also be used to detect and quantitate amyloid deposits in diseases including, without limitation Down's syndrome familial AD and homozygotes for the apolipoprotein 10 E4 allele The compounds and amyloid probes of the invention include analogs, salts, pharmaceutical compositions derivatives prodrugs, racemic mixtures or tautomeric forms thereof.
摘要翻译：本发明提供其化合物和淀粉样蛋白探针，其允许通过在脑的5个区域中淀粉样蛋白和/或淀粉样蛋白沉积物的体内成像来诊断AD并且定量淀粉样蛋白沉积物（斑块）的程度或进展的惰性方法。优选地，本发明的淀粉样蛋白探针可以穿过血脑屏障并将AD脑与正常脑区分开。淀粉样蛋白探针可以以适于淀粉样蛋白沉积的体内成像的量施用给患者。本发明的淀粉样蛋白探针也可用于检测和在疾病中定量淀粉样蛋白沉积物，包括但不限于唐氏综合征家族性AD和载脂蛋白10 E4等位基因的纯合子本发明的化合物和淀粉样蛋白探针包括类似物，盐，药物组合物衍生物前药，外消旋混合物或其互变异构形式。

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