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1. 发明申请

US20070037817A1 Acetylenic piperazines as metabotropic glutamate receptor antagonists 审中-公开
标题翻译：乙酸哌嗪作为代谢型谷氨酸受体拮抗剂
公开(公告)号：US20070037817A1
公开(公告)日：2007-02-15
申请号：US11498836
申请日：2006-08-04
申请人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Peter Dove , Erwan Arzel
发明人： Louise Edwards , Methvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Peter Dove , Erwan Arzel
IPC分类号： A61K31/498 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, B, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR 5 mediated disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或溶剂化物：其中Ar 1，A，B，R 1，m和n如说明书中所定义。本发明还包括药物组合物及其制备方法及其制备方法以及治疗mGluR5介导的病症的方法。

2. 发明申请

US20080194571A1 Acetylenic Piperazines as Metabotropic Glutamate Receptor Antagonists 审中-公开
标题翻译：乙酸哌嗪作为代谢型谷氨酸受体拮抗剂
公开(公告)号：US20080194571A1
公开(公告)日：2008-08-14
申请号：US11997523
申请日：2006-08-04
申请人： Louise Edwards , Mithvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Peter Dove , Erwan Arzel
发明人： Louise Edwards , Mithvin Isaac , Abdelmalik Slassi , Guang-Ri Sun , Peter Dove , Erwan Arzel
IPC分类号： A61K31/4985 , C07D487/04 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, A, B, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses of, and processes of making the compounds, as well as methods of medical treatment of mGluR 5 mediated disorders.
摘要翻译：本发明涉及式I化合物或其药学上可接受的盐或溶剂化物：其中Ar 1，A，B，R 1，m和n如说明书中所定义。本发明还包括药物组合物及其制备方法及其制备方法以及治疗mGluR5介导的病症的方法。

3. 发明申请

US20090131454A1 New compounds 067 失效
标题翻译：新化合物067
公开(公告)号：US20090131454A1
公开(公告)日：2009-05-21
申请号：US12285988
申请日：2008-10-17
申请人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
发明人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
IPC分类号： A61K31/497 , C07D401/14 , C07D403/14 , A61K31/506 , A61K31/4439
CPC分类号： C07D401/14 , C07D403/14
摘要： The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.
摘要翻译：本发明涉及新化合物，它们在治疗中的用途和包含所述新化合物的药物组合物。

4. 发明授权

US07960422B2 Pharmaceutically active compounds containing tetrazolyl and triazolyl rings 失效
标题翻译：含有四唑基和三唑基环的药物活性化合物
公开(公告)号：US07960422B2
公开(公告)日：2011-06-14
申请号：US12285988
申请日：2008-10-17
申请人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
发明人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
IPC分类号： A61K31/41
CPC分类号： C07D401/14 , C07D403/14
摘要： Compounds of formula (I) wherein R1 is as well as pharmaceutically acceptable salts, hydrates and/or enantiomers thereof are useful as compounds that exhibit activity at metabotropic glutamate receptors.
摘要翻译：其中R 1及其药学上可接受的盐，水合物和/或对映异构体的式（I）化合物可用作在代谢型谷氨酸受体上显示活性的化合物。

5. 发明申请

US20090227539A1 Boron compounds useful in bnct 有权
标题翻译：硼化合物可用于bnct
公开(公告)号：US20090227539A1
公开(公告)日：2009-09-10
申请号：US11990634
申请日：2006-08-17
申请人： Lars-Inge Olsson , Erwan Arzel , Arne Eek
发明人： Lars-Inge Olsson , Erwan Arzel , Arne Eek
IPC分类号： A61K31/69 , C07D475/00 , C07F5/02 , C07F15/00 , A61K31/555 , A61K31/4985
CPC分类号： C07F5/027 , C07D475/04
摘要： The present invention relates to novel boron comprising compounds, to pharmaceutical compositions comprising said compounds, to the therapeutic use of said compounds, and to a process for preparation of said compounds. The compounds are useful in boron neutron capture therapy (BNCT).
摘要翻译：本发明涉及包含新化合物的化合物，包含所述化合物的药物组合物，所述化合物的治疗用途以及所述化合物的制备方法。这些化合物可用于硼中子俘获治疗（BNCT）。

6. 发明申请

US20080221149A1 Novel 2-Heteroaryl Substituted Benzothiophenes and Benzofuranes 709 有权
标题翻译：新型2-杂芳基取代的苯并噻吩和苯并呋喃709
公开(公告)号：US20080221149A1
公开(公告)日：2008-09-11
申请号：US12042795
申请日：2008-03-05
申请人： Erwan Arzel , Britt-Marie Swahn , David Wensbo
发明人： Erwan Arzel , Britt-Marie Swahn , David Wensbo
IPC分类号： A61K31/4745 , A61K31/416 , A61K31/405 , C07D498/02 , C07D471/02 , C07D405/02 , C07D409/02
CPC分类号： C07D405/04 , C07D409/04 , C07D471/04
摘要： The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measureing clinical efficacy of Alzheimer's disease therapeutic agents.
摘要翻译：本发明涉及新的2-杂芳基取代的苯并噻吩和苯并呋喃衍生物及其前体，以及具有以下结构式（Ia）的这类化合物及其药学上可接受的盐，组合物和使用方法的治疗用途。此外，本发明涉及适用于生活患者淀粉样蛋白沉积物成像，其组成，使用方法和制备这些化合物的方法的新型2-杂芳基取代的苯并噻吩和苯并呋喃衍生物。更具体地说，本发明涉及在体内淀粉样蛋白沉积物在体内成像以使阿尔茨海默病的抗原异常诊断以及阿尔茨海默病治疗剂的临床疗效的测定方法。

7. 发明申请

US20080255106A1 Novel 2-Phenyl-Imidazo[4,5-B]Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase for the Treatment of Dementia and Neurodegenerative Disorders 审中-公开
标题翻译：新型2-苯基 - 咪唑并[4,5-B]吡啶衍生物作为糖原合酶激酶抑制剂治疗痴呆和神经退行性疾病
公开(公告)号：US20080255106A1
公开(公告)日：2008-10-16
申请号：US12088897
申请日：2006-10-02
申请人： Per I. Arvidsson , Erwan Arzel , Jeremy Burrows , Helena Gyback , Tobias Rein , Didier Rotticci , Peter Soderman
发明人： Per I. Arvidsson , Erwan Arzel , Jeremy Burrows , Helena Gyback , Tobias Rein , Didier Rotticci , Peter Soderman
IPC分类号： A61K31/437 , A61P25/00 , C07D471/04 , A61K31/541 , A61K31/496 , A61P3/10 , A61K31/5377
CPC分类号： C07D471/04
摘要： Compounds of formula I wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation and new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
摘要翻译：其中R 1，R 2，R 3，R 4，R 5，R 5，R 4， R 6和R 7如说明书中所定义，作为其盐或其盐的碱或其药学上可接受的盐，溶剂化物或溶剂合物，其方法为制剂和其中使用的新中间体，含有所述化合物的药物制剂和所述化合物在治疗中的用途。

8. 发明授权

US08183247B2 Boron compounds useful in BNCT 有权
标题翻译：硼化合物可用于BNCT
公开(公告)号：US08183247B2
公开(公告)日：2012-05-22
申请号：US11990634
申请日：2006-08-17
申请人： Lars-Inge Olsson , Erwan Arzel , Arne Eek
发明人： Lars-Inge Olsson , Erwan Arzel , Arne Eek
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07F5/027 , C07D475/04
摘要： The present invention relates to novel boron comprising compounds, to pharmaceutical compositions comprising said compounds, to the therapeutic use of said compounds, and to a process for preparation of said compounds. The compounds are useful in boron neutron capture therapy (BNCT).
摘要翻译：本发明涉及包含新化合物的化合物，包含所述化合物的药物组合物，所述化合物的治疗用途以及所述化合物的制备方法。这些化合物可用于硼中子俘获治疗（BNCT）。

9. 发明授权

US07772256B2 2-heteroaryl substituted benzothiophenes and benzofuranes 709 有权
标题翻译： 2-杂芳基取代的苯并噻吩和苯并呋喃709
公开(公告)号：US07772256B2
公开(公告)日：2010-08-10
申请号：US12042795
申请日：2008-03-05
申请人： Erwan Arzel , Britt-Marie Swahn , David Wensbo
发明人： Erwan Arzel , Britt-Marie Swahn , David Wensbo
IPC分类号： A61K31/443 , C07D405/04
CPC分类号： C07D405/04 , C07D409/04 , C07D471/04
摘要： The present invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel 2-heteroaryl substituted benzothiophene and benzofuran derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
摘要翻译：本发明涉及新的2-杂芳基取代的苯并噻吩和苯并呋喃衍生物及其前体，以及具有以下结构式（Ia）的这类化合物及其药学上可接受的盐，组合物和使用方法的治疗用途。此外，本发明涉及适用于生活患者淀粉样蛋白沉积物成像，其组成，使用方法和制备这些化合物的方法的新型2-杂芳基取代的苯并噻吩和苯并呋喃衍生物。更具体地说，本发明涉及一种在体内淀粉样蛋白沉积物在体内成像以使阿尔茨海默病的止血诊断成为可能并测量阿尔茨海默病治疗剂的临床疗效的方法。

10. 发明申请

US20090105252A1 Pyrimidine Derivatives and Their Use in Therapy as well as the Use of Pyrimidine Derivatives in the Manufacture of a Medicament for Prevention and/or Treatment of Alzheimer's Disease 审中-公开
标题翻译：嘧啶衍生物及其在治疗中的应用以及嘧啶衍生物在制造预防和/或治疗阿尔茨海默病药物中的应用
公开(公告)号：US20090105252A1
公开(公告)日：2009-04-23
申请号：US12089008
申请日：2006-10-02
申请人： Lars Andersson , Erwan Arzel , Stefan Berg , Jeremy Burrows , Sven Hellberg , Fernando Huerta , Torben Pedersen , Tobias Rein , Didier Rotticci , Karin Staaf , Dominika Turek
发明人： Lars Andersson , Erwan Arzel , Stefan Berg , Jeremy Burrows , Sven Hellberg , Fernando Huerta , Torben Pedersen , Tobias Rein , Didier Rotticci , Karin Staaf , Dominika Turek
IPC分类号： A61K31/5377 , C07D403/02 , A61K31/506 , C07D413/14 , A61P25/28 , C07D403/14 , A61K31/496
CPC分类号： C07D405/14 , A61K31/506 , C07D401/14 , C07D403/04 , C07D409/14
摘要： Compounds of formula I wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
摘要翻译：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如说明书中所定义的式I化合物或其盐，溶剂化物或其盐的溶剂合物，其制备方法，新的其中使用的中间体，含有所述化合物的药物制剂和所述化合物在治疗中的用途。

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