公开(公告)号：US07670591B2

公开(公告)日：2010-03-02

申请号：US11763151

申请日：2007-06-14

申请人： Jonas Malmstrom ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Britt-Marie Swahn ,  David Wensbo

发明人： Jonas Malmstrom ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Britt-Marie Swahn ,  David Wensbo

IPC分类号： A61K51/04 ,  A61K31/443 ,  C07D413/04

CPC分类号： C07D413/04

摘要： The present invention relates to novel heteroaryl substituted benzoxazole derivatives and therapeutic uses for 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 heteroaryl substituted benzoxazole 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： 本发明涉及新颖的杂芳基取代的苯并恶唑衍生物和具有以下结构式（Ia）的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，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的苯并恶唑衍生物，其组合物，使用方法和制备此类化合物的方法。 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。

公开(公告)号：US20080027051A1

公开(公告)日：2008-01-31

申请号：US11763151

申请日：2007-06-14

申请人： Jonas Malmstrom ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Britt-Marie Swahn ,  David Wensbo

发明人： Jonas Malmstrom ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Britt-Marie Swahn ,  David Wensbo

IPC分类号： A61K31/443 ,  A61K31/506 ,  A61K31/5377 ,  A61P25/28 ,  A61P3/00 ,  C07D239/28 ,  C07D413/04 ,  C07D413/14

CPC分类号： C07D413/04

摘要： The present invention relates to novel heteroaryl substituted benzoxazole derivatives and therapeutic uses for 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 heteroaryl substituted benzoxazole 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： 本发明涉及新颖的杂芳基取代的苯并恶唑衍生物和具有以下结构式（Ia）的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，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的苯并恶唑衍生物，其组合物，使用方法和制备此类化合物的方法。 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。

公开(公告)号：US08163928B2

公开(公告)日：2012-04-24

申请号：US12162255

申请日：2007-01-25

申请人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmstrom ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Strom ,  David Wensbo

发明人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmstrom ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Strom ,  David Wensbo

IPC分类号： A61K51/00 ,  A61K51/04

CPC分类号： C07D417/04 ,  C07B59/002 ,  C07D513/04

摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole 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： 本发明涉及新颖的杂芳基取代的苯并噻唑衍生物，其前体，以及具有以下结构式（I）的化合物的治疗用途：[化学式应在此插入。 请参阅纸本]及其药学上可接受的盐，组合物和使用方法。 此外，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的苯并噻唑衍生物，其组合物，使用方法和制备此类化合物的方法。 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。

公开(公告)号：US08957215B2

公开(公告)日：2015-02-17

申请号：US13453579

申请日：2012-04-23

申请人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmstrom ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Strom ,  David Wensbo

发明人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmstrom ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Strom ,  David Wensbo

IPC分类号： C07D417/04 ,  C07D417/14 ,  C07B59/00 ,  C07D513/04

CPC分类号： C07D417/04 ,  C07B59/002 ,  C07D513/04

摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole 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： 本发明涉及新颖的杂芳基取代的苯并噻唑衍生物，其前体，以及具有以下结构式（I）的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，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的苯并噻唑衍生物，其组合物，使用方法和制备此类化合物的方法。 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。

公开(公告)号：US20090028787A1

公开(公告)日：2009-01-29

申请号：US12162255

申请日：2007-01-25

申请人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmstrom ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Strom ,  David Wensbo

发明人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmstrom ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Strom ,  David Wensbo

IPC分类号： A61K31/496 ,  C07D417/14 ,  C07D417/04 ,  A61K31/5377 ,  A61P25/28 ,  A61K49/00 ,  A61K31/4439 ,  C07D413/14

CPC分类号： C07D417/04 ,  C07B59/002 ,  C07D513/04

摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole 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： 本发明涉及新颖的杂芳基取代的苯并噻唑衍生物，其前体，以及具有以下结构式（I）的化合物的治疗用途：[化学式应在此插入。 请参阅纸本]及其药学上可接受的盐，组合物和使用方法。 此外，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的苯并噻唑衍生物，其组合物，使用方法和制备此类化合物的方法。 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。

公开(公告)号：US20100092385A1

公开(公告)日：2010-04-15

申请号：US12524019

申请日：2008-01-21

申请人： Michaela Vallin ,  Jonas Malmstrom ,  David Pyring ,  Can Slivo ,  David Wensbo

发明人： Michaela Vallin ,  Jonas Malmstrom ,  David Pyring ,  Can Slivo ,  David Wensbo

IPC分类号： A61K51/04 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/437 ,  C07D413/14 ,  C07D401/14 ,  C07D471/04 ,  A61P25/28 ,  A61K49/00 ,  A61K49/10

CPC分类号： C07D471/04 ,  A61K49/10 ,  A61K51/041 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0463

摘要： The present invention relates to novel heteroaryl substituted imidazopyridine derivatives, precursors thereof, and therapeutic uses of such compounds, having the structural formula (Ia) and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted imidazopyridine 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： 本发明涉及新颖的杂芳基取代的咪唑并吡啶衍生物，其前体和具有结构式（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，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的咪唑并吡啶衍生物，其组合物，使用方法和制备此类化合物的方法。 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。

公开(公告)号：US20120207679A1

公开(公告)日：2012-08-16

申请号：US13453579

申请日：2012-04-23

申请人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmström ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Ström ,  David Wensbo

发明人： Ylva Gravenfors ,  Catrin Jonasson ,  Jonas Malmström ,  Gunnar Nordvall ,  David Pyring ,  Can Slivo ,  Daniel Sohn ,  Peter Ström ,  David Wensbo

IPC分类号： A61K51/04 ,  A61K31/496 ,  C07D417/04 ,  A61P25/28 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  C07F7/18 ,  C07D417/14 ,  A61K31/4439

CPC分类号： C07D417/04 ,  C07B59/002 ,  C07D513/04

摘要： The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole 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： 本发明涉及新颖的杂芳基取代的苯并噻唑衍生物，其前体，以及具有以下结构式（I）的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，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型杂芳基取代的苯并噻唑衍生物，其组合物，使用方法和制备此类化合物的方法。 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。

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。

公开(公告)号：US20100098631A1

公开(公告)日：2010-04-22

申请号：US12529850

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： A61K51/00 ,  C07D209/04 ,  C07D401/04 ,  C07D403/04 ,  A61K31/4965 ,  A61K31/4439 ,  A61K31/405

CPC分类号： C07D401/04

摘要： The present invention relates to novel 2-heteroaryl substituted indole 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 indole 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-杂芳基取代的吲哚衍生物，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，本发明涉及适用于在活体患者中成像淀粉样蛋白沉积物的新型2-杂芳基取代的吲哚衍生物，其组合物，使用方法和制备此类化合物的方法。 更具体地说，本发明涉及一种体内淀粉样蛋白沉积物在体内成像以测定阿尔茨海默病的止血诊断以及测量阿尔茨海默氏病治疗剂的临床疗效的方法。

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。