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公开(公告)号:US10314845B2
公开(公告)日:2019-06-11
申请号:US15865703
申请日:2018-01-09
Applicant: GLAXOSMITHKLINE LLC
Inventor: Rosanna Tedesco , Junya Qu , Robert Sanchez , Ralph A. Rivero
IPC: A61K31/5377 , C07D235/08 , C07D235/10 , C07D235/24 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K31/337
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
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公开(公告)号:US20150246889A1
公开(公告)日:2015-09-03
申请号:US14712991
申请日:2015-05-15
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: C07D235/08
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
Abstract translation: 本发明涉及苯并咪唑衍生物用于调节的用途,特别是抑制磷酸肌醇3'OH激酶家族(以下称为PI3激酶),适当的是PI3Kα,PI3Kδ,PI3K&bgr和/或PI3Kγ的活性或功能。 合适地,本发明涉及苯并咪唑在治疗一种或多种疾病状态中的用途,所述疾病状态选自:自身免疫性疾病,炎性疾病,心血管疾病,神经变性疾病,过敏,哮喘,胰腺炎,多器官衰竭,肾脏疾病,血小板聚集, 癌症,精子活力,移植排斥反应,移植物排斥反应和肺损伤。 更合适地,本发明涉及PI3K&bgr; 用于治疗癌症的选择性苯并咪唑化合物。
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公开(公告)号:US10660898B2
公开(公告)日:2020-05-26
申请号:US16393210
申请日:2019-04-24
Applicant: GLAXOSMITHKLINE LLC
Inventor: Rosanna Tedesco , Junya Qu , Robert Sanchez , Ralph A. Rivero
IPC: A61K31/5377 , A61K31/337 , C07D235/10 , C07D235/24 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D235/08 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
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公开(公告)号:US09872860B2
公开(公告)日:2018-01-23
申请号:US14844051
申请日:2015-09-03
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: A61K31/5377
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
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公开(公告)号:US09156797B2
公开(公告)日:2015-10-13
申请号:US14712991
申请日:2015-05-15
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: C07D413/04 , C07D413/10 , C07D235/08
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
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公开(公告)号:US08865912B2
公开(公告)日:2014-10-21
申请号:US14164414
申请日:2014-01-27
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: C07D235/08 , C07D235/24 , C07D417/10 , C07D413/10 , C07D405/10 , C07D409/10 , C07D405/04 , C07D403/10 , C07D403/04 , C07D235/10 , C07D401/10 , C07D413/04 , C07D417/04
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
Abstract translation: 本发明涉及苯并咪唑衍生物用于调节的用途,特别是抑制磷酸肌醇3'OH激酶家族(以下称为PI3激酶),适当的是PI3Kα,PI3Kδ,PI3K&bgr和/或PI3Kγ的活性或功能。 合适地,本发明涉及苯并咪唑在治疗一种或多种疾病状态中的用途,所述疾病状态选自:自身免疫性疾病,炎性疾病,心血管疾病,神经变性疾病,过敏,哮喘,胰腺炎,多器官衰竭,肾脏疾病,血小板聚集, 癌症,精子活力,移植排斥反应,移植物排斥反应和肺损伤。 更合适地,本发明涉及PI3K&bgr; 用于治疗癌症的选择性苯并咪唑化合物。
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公开(公告)号:US20140142321A1
公开(公告)日:2014-05-22
申请号:US14164414
申请日:2014-01-27
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: C07D235/08
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
Abstract translation: 本发明涉及苯并咪唑衍生物用于调节的用途,特别是抑制磷酸肌醇3'OH激酶家族(以下称为PI3激酶),适当的是PI3Kα,PI3Kδ,PI3K&bgr和/或PI3Kγ的活性或功能。 合适地,本发明涉及苯并咪唑在治疗一种或多种疾病状态中的用途,所述疾病状态选自:自身免疫性疾病,炎性疾病,心血管疾病,神经变性疾病,过敏,哮喘,胰腺炎,多器官衰竭,肾脏疾病,血小板聚集, 癌症,精子活力,移植排斥反应,移植物排斥反应和肺损伤。 更合适地,本发明涉及PI3K&bgr; 用于治疗癌症的选择性苯并咪唑化合物。
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公开(公告)号:US08674090B2
公开(公告)日:2014-03-18
申请号:US14031136
申请日:2013-09-19
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: C07D413/04 , C07D413/10
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
Abstract translation: 本发明涉及苯并咪唑衍生物用于调节,特别是抑制磷酸肌醇3'OH激酶家族(以下称为PI3激酶),适当地PI3Kα,PI3Kdelta,PI3Kβ和/或PI3Kgamma的活性或功能的用途。 合适地,本发明涉及苯并咪唑在治疗一种或多种疾病状态中的用途,所述疾病状态选自:自身免疫性疾病,炎性疾病,心血管疾病,神经变性疾病,过敏,哮喘,胰腺炎,多器官衰竭,肾脏疾病,血小板聚集, 癌症,精子活力,移植排斥反应,移植物排斥反应和肺损伤。 更合适地,本发明涉及用于治疗癌症的PI3Kβ选择性苯并咪唑化合物。
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公开(公告)号:US09062003B2
公开(公告)日:2015-06-23
申请号:US14481098
申请日:2014-09-09
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: A61K31/5377 , C07D235/08 , C07D235/10 , C07D235/24 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K31/337
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
Abstract translation: 本发明涉及苯并咪唑衍生物用于调节的用途,特别是抑制磷酸肌醇3'OH激酶家族(以下称为PI3激酶),适当的是PI3Kα,PI3Kδ,PI3K&bgr和/或PI3Kγ的活性或功能。 合适地,本发明涉及苯并咪唑在治疗一种或多种疾病状态中的用途,所述疾病状态选自:自身免疫性疾病,炎性疾病,心血管疾病,神经变性疾病,过敏,哮喘,胰腺炎,多器官衰竭,肾脏疾病,血小板聚集, 癌症,精子活力,移植排斥反应,移植物排斥反应和肺损伤。 更合适地,本发明涉及PI3K&bgr; 用于治疗癌症的选择性苯并咪唑化合物。
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公开(公告)号:US20140378456A1
公开(公告)日:2014-12-25
申请号:US14481098
申请日:2014-09-09
Applicant: GlaxoSmithKline LLC
Inventor: Junya Qu , Ralph A. Rivero , Robert Sanchez , Rosanna Tedesco
IPC: C07D235/08 , A61K31/337
CPC classification number: A61K31/5377 , A61K31/337 , C07D235/08 , C07D235/10 , C07D235/24 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10
Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazoles compounds for treating cancer.
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