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：US09440992B2

公开(公告)日：2016-09-13

申请号：US12979720

申请日：2010-12-28

申请人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

发明人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

IPC分类号： A61K31/519 ,  A61P19/02 ,  A61P29/00 ,  C07D513/04 ,  A61P25/00 ,  A61P25/28 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06

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 R5 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R 5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：US20080214578A1

公开(公告)日：2008-09-04

申请号：US11910780

申请日：2006-04-03

申请人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

发明人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

IPC分类号： A61K31/519 ,  C07D513/04 ,  A61P11/06 ,  A61P25/00 ,  A61P9/10

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 R5 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-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R 5如说明书中所定义，及其药学上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CX 3 CR 1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，心脑血管动脉粥样硬化性疾病，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：US08088780B2

公开(公告)日：2012-01-03

申请号：US11910781

申请日：2006-04-03

申请人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

发明人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

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

CPC分类号： C07D413/04

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 R5 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R 5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，心脑血管动脉粥样硬化性疾病，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：US20070142386A1

公开(公告)日：2007-06-21

申请号：US10575534

申请日：2004-10-05

申请人： Gunnar Nordvall ,  Tobias Rein ,  Daniel Sohn ,  Ronald Zemribo

发明人： Gunnar Nordvall ,  Tobias Rein ,  Daniel Sohn ,  Ronald Zemribo

IPC分类号： A61K31/525 ,  A61K31/519 ,  C07D275/02 ,  C07D498/02

CPC分类号： C07D513/04 ,  C07D475/06

摘要： There are disclosed novel compounds of formula (I) wherein A, R1, R2, R3 and X 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, atherosclerosis and pain.

摘要翻译： 公开了新的式（I）化合物，其中A，R 1，R 2，R 3和X如说明书中所定义 及其药学上可接受的盐，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CX 3 CR 1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，动脉粥样硬化和疼痛。

公开(公告)号：US20110092519A1

公开(公告)日：2011-04-21

申请号：US12979720

申请日：2010-12-28

申请人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

发明人： Gunnar Nordvall ,  Colin Ray ,  Tobias Rein ,  Daniel Sohn

IPC分类号： A61K31/519 ,  C07D513/04 ,  A61P25/00 ,  A61P25/28 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00

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 R5 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R 5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。