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    Compounds and their use as BACE inhibitors
    1.
    发明申请
    Compounds and their use as BACE inhibitors 审中-公开
    化合物及其作为BACE抑制剂的用途

    公开(公告)号：US20120165346A1

    公开(公告)日：2012-06-28

    申请号：US13331231

    申请日：2011-12-20

    申请人： Karin Kolmodin ,  Britt-Marie Swahn ,  Jacob Kihlström ,  Johan Lindström ,  Sofia Karlström ,  Marie Sundström ,  Stefan Von Berg

    发明人： Karin Kolmodin ,  Britt-Marie Swahn ,  Jacob Kihlström ,  Johan Lindström ,  Sofia Karlström ,  Marie Sundström ,  Stefan Von Berg

    IPC分类号： A61K31/506 ,  A61P25/28 ,  A61P25/00 ,  C07D401/14 ,  A61K31/444

    CPC分类号： C07D401/14 ,  C07D403/14

    摘要： The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

    摘要翻译： 本发明涉及新的式（I）化合物及其药物组合物。 此外，本发明涉及用于治疗和/或预防与疾病相关的病症如唐氏综合征和淀粉样血管病变的治疗方法，例如但不限于脑淀粉样血管病或遗传性脑出血，与 认知障碍，例如但不限于MCI（“轻度认知障碍”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与诸如阿尔茨海默氏病或​​痴呆症的疾病相关的神经变性，包括混合血管和退行性来源的痴呆， 老年性痴呆，老年性痴呆和与帕金森病相关的痴呆，进行性核上性麻痹或皮质基底变性。

    5,7-disubstituted thiazolo[4,5-d]pyrimidines for the selective inhibition of chemokine receptors
    2.
    发明授权
    5,7-disubstituted thiazolo[4,5-d]pyrimidines for the selective inhibition of chemokine receptors 有权
    5,7-二取代噻唑并[4,5-d]嘧啶，用于选择性抑制趋化因子受体

    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。

    Substituted isoindoles for the treatment and/or prevention of Aβ- related pathologies
    5.
    发明授权
    Substituted isoindoles for the treatment and/or prevention of Aβ- related pathologies 失效
    取代的异吲哚，用于治疗和/或预防相关病理

    公开(公告)号：US08030500B2

    公开(公告)日：2011-10-04

    申请号：US12618212

    申请日：2009-11-13

    申请人： Jörg Holenz ,  Sofia Karlström ,  Karin Kolmodin ,  Johan Lindström ,  Laszlo Rakos ,  Didier Rotticci ,  Peter Söderman ,  Britt-Marie Swahn ,  Stefan Von Berg

    发明人： Jörg Holenz ,  Sofia Karlström ,  Karin Kolmodin ,  Johan Lindström ,  Laszlo Rakos ,  Didier Rotticci ,  Peter Söderman ,  Britt-Marie Swahn ,  Stefan Von Berg

    IPC分类号： C07D209/44

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10

    摘要： The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

    摘要翻译： 本发明涉及新的式（I）化合物及其药物组合物。 此外，本发明涉及用于治疗和/或预防与疾病相关的疾病如唐氏综合征和淀粉样血管病，例如但不限于脑淀粉样血管病或遗传性脑出血的治疗方法，与 认知障碍，例如但不限于MCI（“轻度认知障碍”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与诸如阿尔茨海默病或痴呆的疾病相关的神经变性，包括混合血管和退行性来源的痴呆， 老年性痴呆，老年性痴呆和与帕金森病相关的痴呆，进行性核上性麻痹或皮质基底变性。

    5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES FOR THE SELECTIVE INHIBITION OF CHEMOKINE RECEPTORS
    6.
    发明申请
    5,7-DISUBSTITUTED THIAZOLO[4,5-D]PYRIMIDINES FOR THE SELECTIVE INHIBITION OF CHEMOKINE RECEPTORS 审中-公开
    5,7-取代的噻唑并[4,5-D]嘧啶，用于选择性抑制化合物受体

    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。

    NEW COMPOUNDS 578
    7.
    发明申请
    NEW COMPOUNDS 578 失效
    新化合物578

    公开(公告)号：US20100125082A1

    公开(公告)日：2010-05-20

    申请号：US12618212

    申请日：2009-11-13

    申请人： Jörg HOLENZ ,  Sofia KARLSTRÖM ,  Karin KOLMODIN ,  Johan LINDSTRÖM ,  Laszlo RAKOS ,  Didier ROTTICCI ,  Peter SÖDERMAN ,  Britt-Marie SWAHN ,  Stefan VON BERG

    发明人： Jörg HOLENZ ,  Sofia KARLSTRÖM ,  Karin KOLMODIN ,  Johan LINDSTRÖM ,  Laszlo RAKOS ,  Didier ROTTICCI ,  Peter SÖDERMAN ,  Britt-Marie SWAHN ,  Stefan VON BERG

    IPC分类号： A61K31/497 ,  C07D401/14 ,  C07D401/04 ,  A61K31/496 ,  A61K31/444 ,  A61K31/4439 ,  A61P25/28

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10

    摘要： The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

    摘要翻译： 本发明涉及新的式（I）化合物及其药物组合物。 此外，本发明涉及用于治疗和/或预防与疾病相关的疾病如唐氏综合征和淀粉样血管病，例如但不限于脑淀粉样血管病或遗传性脑出血的治疗方法，与 认知障碍，例如但不限于MCI（“轻度认知障碍”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与诸如阿尔茨海默病或痴呆的疾病相关的神经变性，包括混合血管和退行性来源的痴呆， 老年性痴呆，老年性痴呆和与帕金森病相关的痴呆，进行性核上性麻痹或皮质基底变性。