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    Benzo[1,3]dioxine derivatives and their use as LPAR5 antagonists
    2.
    发明授权
    Benzo[1,3]dioxine derivatives and their use as LPAR5 antagonists 有权
    苯并[1,3]二恶烷衍生物及其作为LPAR5拮抗剂的用途

    公开(公告)号：US09221784B2

    公开(公告)日：2015-12-29

    申请号：US14401041

    申请日：2013-05-16

    申请人： SANOFI

    发明人： Marc Nazare ,  Detlef Kozian ,  Martin Bossart ,  Werngard Czechtizky ,  Andreas Evers

    IPC分类号： C07D319/08 ,  C07D405/12 ,  C07D405/04 ,  C07D413/04 ,  A61K31/41 ,  A61K31/357 ,  A61K31/4245 ,  C07D403/12 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04

    CPC分类号： C07D319/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04

    摘要： The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中残基A，R1至R5，Z1和Z2具有权利要求中所示的含义。 式（I）的化合物是用于治疗各种疾病例如血栓栓塞性疾病或再狭窄的心血管疾病的有价值的药理活性化合物。 本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化 存在或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5的抑制。 本发明还涉及式（I）化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。

    Pyridine Derivatives And Their Use In The Treatment Of Conditions Associated With Pathological Thrombus Formation
    3.
    发明申请
    Pyridine Derivatives And Their Use In The Treatment Of Conditions Associated With Pathological Thrombus Formation 有权
    吡啶衍生物及其用于治疗与病理性血栓形成有关的病症

    公开(公告)号：US20150141471A1

    公开(公告)日：2015-05-21

    申请号：US14401056

    申请日：2013-05-16

    申请人： SANOFI

    发明人： Marc Nazare ,  Detlef Kozian ,  Andreas Evers ,  Werngard Czechtizky

    IPC分类号： C07D213/30

    CPC分类号： C07D213/30

    摘要： The present invention relates to compounds of the formula (I), wherein the residues R1 to R6, V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present, or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中残基R1至R6，V，G和M具有权利要求中所示的含义。 式I的化合物是用于治疗多种疾病，例如心血管疾病如血栓栓塞性疾病或再狭窄的有价值的药理活性化合物。 本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化 或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5的抑制。 本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。

    Pyrazole Derivatives And Their Use As LPAR5 Antagonists
    4.
    发明申请
    Pyrazole Derivatives And Their Use As LPAR5 Antagonists 有权
    吡唑衍生物及其作为LPAR5拮抗剂的用途

    公开(公告)号：US20150141477A1

    公开(公告)日：2015-05-21

    申请号：US14401050

    申请日：2013-05-16

    申请人： SANOFI

    发明人： Marc Nazare ,  Detlef Kozian ,  Andreas Evers ,  Werngard Czechtizky

    IPC分类号： C07D231/12 ,  C07D409/04 ,  C07D231/56

    CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D231/56 ,  C07D409/04

    摘要： The present invention relates to compounds of the formula (I), wherein the residues R1 to R5, V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中残基R1至R5，V，G和M具有权利要求中所示的含义。 式（I）的化合物是用于治疗各种疾病例如血栓栓塞性疾病或再狭窄的心血管疾病的有价值的药理活性化合物。 本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化 存在或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5的抑制。 本发明还涉及式（I）化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。

    Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation
    5.
    发明授权
    Pyridine derivatives and their use in the treatment of conditions associated with pathological thrombus formation 有权
    吡啶衍生物及其用于治疗与病理性血栓形成相关的病症

    公开(公告)号：US09346757B2

    公开(公告)日：2016-05-24

    申请号：US14401056

    申请日：2013-05-16

    申请人： SANOFI

    发明人： Marc Nazare ,  Detlef Kozian ,  Andreas Evers ,  Werngard Czechtizky

    IPC分类号： C07D213/24 ,  A61K31/44 ,  C07D213/30

    CPC分类号： C07D213/30

    摘要： The present invention relates to compounds of the formula (I), wherein the residues R1 to R6, V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present, or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中残基R1至R6，V，G和M具有权利要求中所示的含义。 式I的化合物是用于治疗多种疾病，例如心血管疾病如血栓栓塞性疾病或再狭窄的有价值的药理活性化合物。 本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化 或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5的抑制。 本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。

    Benzo[1,3]Dioxine Derivatives And Their Use As LPAR5 Antagonists
    6.
    发明申请
    Benzo[1,3]Dioxine Derivatives And Their Use As LPAR5 Antagonists 有权
    苯并[1,3]二恶嗪衍生物及其作为LPAR5拮抗剂的用途

    公开(公告)号：US20150111889A1

    公开(公告)日：2015-04-23

    申请号：US14401041

    申请日：2013-05-16

    申请人： SANOFI

    发明人： Marc Nazare ,  Detlef Kozian ,  Martin Bossart ,  Werngard Czechtizky ,  Andreas Evers

    IPC分类号： C07D319/08 ,  C07D405/12 ,  C07D413/04 ,  C07D405/04

    CPC分类号： C07D319/08 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04

    摘要： The present invention relates to compounds of the formula (I), wherein the residues A, R1 to R5, Z1 and Z2 have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中残基A，R1至R5，Z1和Z2具有权利要求中所示的含义。 式（I）的化合物是用于治疗各种疾病例如血栓栓塞性疾病或再狭窄的心血管疾病的有价值的药理活性化合物。 本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化 存在或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5的抑制。 本发明还涉及式（I）化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。

    Pyrazole derivatives and their use as LPAR5 antagonists
    9.
    发明授权
    Pyrazole derivatives and their use as LPAR5 antagonists 有权
    吡唑衍生物及其作为LPAR5拮抗剂的用途

    公开(公告)号：US09346762B2

    公开(公告)日：2016-05-24

    申请号：US14401050

    申请日：2013-05-16

    申请人： SANOFI

    发明人： Marc Nazare ,  Detlef Kozian ,  Andreas Evers ,  Werngard Czechtizky

    IPC分类号： C07D231/12 ,  C07D409/04 ,  C07D231/56 ,  A61K31/415

    CPC分类号： C07D231/12 ,  A61K31/415 ,  C07D231/56 ,  C07D409/04

    摘要： The present invention relates to compounds of the formula (I), wherein the residues R1 to R5, V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中残基R1至R5，V，G和M具有权利要求中所示的含义。 式（I）的化合物是用于治疗各种疾病例如血栓栓塞性疾病或再狭窄的心血管疾病的有价值的药理活性化合物。 本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小胶质细胞LPA受体LPAR5的不期望的活化 存在或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5的抑制。 本发明还涉及式（I）化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。