公开(公告)号：US20110105537A1

公开(公告)日：2011-05-05

申请号：US13009384

申请日：2011-01-19

申请人： Rolf Johansson ,  Sofia Karlström ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

发明人： Rolf Johansson ,  Sofia Karlström ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

IPC分类号： A61K31/519 ,  C07D513/04 ,  A61P25/00 ,  A61P9/00 ,  A61P19/02 ,  A61P11/00 ,  A61P11/06

CPC分类号： C07D513/04

摘要： There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

摘要翻译： 公开了式（I）的新的5,7-二取代[1,3]噻唑并[4,5-d]嘧啶-2（3H） - 酮衍生物，其中R 1，R 2，R 3，R 4和n如 说明书及其药学上可接受的盐以及其制备方法，包含它们的药物组合物及其在治疗中的用途。 式（I）化合物是CX3CR1受体拮抗剂，因此特别可用于治疗或预防神经变性疾病，脱髓鞘疾病，心血管和脑血管动脉粥样硬化疾病，外周动脉疾病，类风湿性关节炎，肺疾病如COPD，哮喘或 疼痛。

公开(公告)号：US07960395B2

公开(公告)日：2011-06-14

申请号：US11862743

申请日：2007-09-27

申请人： Rolf Johansson ,  Sofia Karlström ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

发明人： Rolf Johansson ,  Sofia Karlström ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P11/06 ,  A61P9/10 ,  A61P37/06

CPC分类号： C07D513/04

摘要： There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

摘要翻译： 公开了式（I）的新的5,7-二取代[1,3]噻唑并[4,5-d]嘧啶-2（3H） - 酮衍生物，其中R 1，R 2，R 3，R 4和n如 说明书及其药学上可接受的盐以及其制备方法，包含它们的药物组合物及其在治疗中的用途。 式（I）化合物是CX3CR1受体拮抗剂，因此特别可用于治疗或预防神经变性疾病，脱髓鞘疾病，心血管和脑血管动脉粥样硬化疾病，外周动脉疾病，类风湿性关节炎，肺疾病如COPD，哮喘或 疼痛。

公开(公告)号：US20100035899A1

公开(公告)日：2010-02-11

申请号：US12442831

申请日：2007-09-27

申请人： Rolf Johansson ,  Sofia Karlstrom ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

发明人： Rolf Johansson ,  Sofia Karlstrom ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

IPC分类号： A61K31/519 ,  C07D417/14 ,  A61P9/10 ,  A61P25/00

CPC分类号： C07D513/04

摘要： There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

摘要翻译： 公开了式（I）的新的5-取代的7-取代的7-氨基 - [1,3]噻唑并[4,5-d]嘧啶衍生物，其中R 1，R 2，R 3，R 4和n如说明书中所定义， 其可接受的盐及其制备方法，包含它们的药物组合物及其在治疗中的用途。 式（I）化合物是CX3CR1受体拮抗剂，因此特别可用于治疗或预防神经变性疾病，脱髓鞘疾病，心血管和脑血管动脉粥样硬化疾病，外周动脉疾病，类风湿性关节炎，肺疾病如COPD，哮喘或 疼痛。

公开(公告)号：US08158785B2

公开(公告)日：2012-04-17

申请号：US12442831

申请日：2007-09-27

申请人： Rolf Johansson ,  Sofia Karlstrom ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

发明人： Rolf Johansson ,  Sofia Karlstrom ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

IPC分类号： A61K31/519 ,  A61P9/10 ,  A61P25/00 ,  C07D417/14

CPC分类号： C07D513/04

摘要： There are disclosed novel 5-substituted 7-amino-[1,3]thiazolo[4,5-d]pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

摘要翻译： 公开了式（I）的新的5-取代的7-取代的7-氨基 - [1,3]噻唑并[4,5-d]嘧啶衍生物，其中R 1，R 2，R 3，R 4和n如说明书中所定义， 其可接受的盐及其制备方法，包含它们的药物组合物及其在治疗中的用途。 式（I）化合物是CX3CR1受体拮抗剂，因此特别可用于治疗或预防神经变性疾病，脱髓鞘疾病，心血管和脑血管动脉粥样硬化疾病，外周动脉疾病，类风湿性关节炎，肺疾病如COPD，哮喘或 疼痛。

公开(公告)号：US20080318981A1

公开(公告)日：2008-12-25

申请号：US11862743

申请日：2007-09-27

申请人： Rolf Johansson ,  Sofia Karlstrom ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

发明人： Rolf Johansson ,  Sofia Karlstrom ,  Annika Kers ,  Gunnar Nordvall ,  Tobias Rein ,  Can Slivo

IPC分类号： A61K31/519 ,  A61P25/00 ,  A61P9/00 ,  A61P11/00 ,  C07D513/04

CPC分类号： C07D513/04

摘要： There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4 and n are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain.

摘要翻译： 公开了式（I）的新的5,7-二取代[1,3]噻唑并[4,5-d]嘧啶-2（3H） - 酮衍生物，其中R 1，R 2，R 3，R 4和n如 说明书及其药学上可接受的盐以及其制备方法，包含它们的药物组合物及其在治疗中的用途。 式（I）化合物是CX3CR1受体拮抗剂，因此特别可用于治疗或预防神经变性疾病，脱髓鞘疾病，心血管和脑血管动脉粥样硬化疾病，外周动脉疾病，类风湿性关节炎，肺疾病如COPD，哮喘或 疼痛。

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：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：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。