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1.
公开(公告)号:US20090286782A1
公开(公告)日:2009-11-19
申请号:US12467194
申请日:2009-05-15
申请人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
发明人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
IPC分类号: A61K31/5377 , C07D487/04 , A61K31/519 , A61P19/02 , A61P35/00
CPC分类号: C07D487/04 , A61K31/519
摘要: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.
摘要翻译: 其化合物及其盐,其制剂,其缀合物,其衍生物,其形式及用途。 在某些方面和实施方案中,所述的化合物或其盐,其制剂,其缀合物,其衍生物,其形式在Fms蛋白激酶或Kit蛋白激酶中的至少一种上是有活性的。 还描述了其用于治疗疾病和病症的方法,包括与Fms蛋白激酶和/或Kit蛋白激酶(包括类风湿性关节炎,骨关节炎,骨质疏松症,骨质疏松症,系统性硬化症,脱髓鞘疾病, 多发性硬化症,Charcot玛丽牙综合征,肌萎缩性侧索硬化,阿尔茨海默病,帕金森病,溃疡性结肠炎,克罗恩病,免疫性血小板减少性紫癜,自体移植用骨髓制剂,移植排斥,肾炎,肾病,I型糖尿病,急性疼痛, 神经性疼痛,乳腺癌,前列腺癌,胰腺癌,肺癌,卵巢癌,神经胶质瘤,成胶质细胞瘤,神经纤维瘤病,溶骨性骨转移和巨细胞肿瘤。
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2.
公开(公告)号:US08912204B2
公开(公告)日:2014-12-16
申请号:US13411919
申请日:2012-03-05
申请人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
发明人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
IPC分类号: A01N43/90 , A61K31/519 , C07D487/00 , C07D487/04
CPC分类号: C07D487/04 , A61K31/519
摘要: Compounds of Formula I: and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.
摘要翻译: 描述了式I化合物及其盐,其制剂,其结合物,其衍生物,其形式及其用途。 在某些方面和实施方案中,所述的化合物或其盐,其制剂,其缀合物,其衍生物,其形式在Fms蛋白激酶或Kit蛋白激酶中的至少一种上是有活性的。 还描述了其用于治疗疾病和病症的方法,包括与Fms蛋白激酶和/或Kit蛋白激酶(包括类风湿性关节炎,骨关节炎,骨质疏松症,骨质疏松症,系统性硬化症,脱髓鞘疾病, 多发性硬化症,Charcot玛丽牙综合征,肌萎缩性侧索硬化,阿尔茨海默病,帕金森病,溃疡性结肠炎,克罗恩病,免疫性血小板减少性紫癜,自体移植用骨髓制剂,移植排斥,肾炎,肾病,I型糖尿病,急性疼痛, 神经性疼痛,乳腺癌,前列腺癌,胰腺癌,肺癌,卵巢癌,神经胶质瘤,成胶质细胞瘤,神经纤维瘤病,溶骨性骨转移和巨细胞肿瘤。
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3.
公开(公告)号:US20120053177A1
公开(公告)日:2012-03-01
申请号:US13243748
申请日:2011-09-23
申请人: Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
发明人: Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
IPC分类号: A61K31/5377 , A61P35/00 , A61K31/496 , A61K31/506 , C12N9/99 , A61K31/437
CPC分类号: C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译: 描述了对蛋白激酶有活性的化合物,以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。
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公开(公告)号:US08415469B2
公开(公告)日:2013-04-09
申请号:US12616079
申请日:2009-11-10
申请人: Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , Jianming Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
发明人: Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , Jianming Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
IPC分类号: C07D413/14 , C07D401/14 , C07D471/04 , C07F7/02
CPC分类号: C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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5.
公开(公告)号:US20120165329A1
公开(公告)日:2012-06-28
申请号:US13411919
申请日:2012-03-05
申请人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
发明人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
IPC分类号: A61K31/519 , A61K31/5377 , A61P35/00 , A61P35/02 , A61P9/00 , A61P9/12 , A61P9/10 , A61P9/04 , A61P29/00 , A61P37/00 , A61P37/08 , A61P11/06 , A61P19/02 , A61P25/00 , A61P1/00 , A61P37/06 , A61P7/00 , A61P1/04 , A61P17/00 , A61P27/02 , A61P25/06 , A61P17/06 , A61P11/00 , A61P3/10 , A61P3/04 , A61P19/10 , A61P13/12 , A61P13/00 , A61P21/04 , A61P25/28 , A61P35/04 , A61P1/16 , A61P31/20 , A61P31/14 , A61P31/16 , A61P31/04 , A61P1/18 , A61P25/16 , A61P11/02 , A61P19/08 , A61P3/00 , C07D487/04
CPC分类号: C07D487/04 , A61K31/519
摘要: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.
摘要翻译: 其化合物及其盐,其制剂,其缀合物,其衍生物,其形式及用途。 在某些方面和实施方案中,所述的化合物或其盐,其制剂,其缀合物,其衍生物,其形式在Fms蛋白激酶或Kit蛋白激酶中的至少一种上是有活性的。 还描述了其用于治疗疾病和病症的方法,包括与Fms蛋白激酶和/或Kit蛋白激酶(包括类风湿性关节炎,骨关节炎,骨质疏松症,骨质疏松症,系统性硬化症,脱髓鞘疾病, 多发性硬化症,Charcot玛丽牙综合征,肌萎缩性侧索硬化,阿尔茨海默病,帕金森病,溃疡性结肠炎,克罗恩病,免疫性血小板减少性紫癜,自体移植用骨髓制剂,移植排斥,肾炎,肾病,I型糖尿病,急性疼痛, 神经性疼痛,乳腺癌,前列腺癌,胰腺癌,肺癌,卵巢癌,神经胶质瘤,成胶质细胞瘤,神经纤维瘤病,溶骨性骨转移和巨细胞肿瘤。
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6.
公开(公告)号:US08158636B2
公开(公告)日:2012-04-17
申请号:US12467194
申请日:2009-05-15
申请人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
发明人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
IPC分类号: A01N43/90 , A61K31/519 , C07D487/00
CPC分类号: C07D487/04 , A61K31/519
摘要: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.
摘要翻译: 其化合物及其盐,其制剂,其缀合物,其衍生物,其形式及用途。 在某些方面和实施方案中,所述的化合物或其盐,其制剂,其缀合物,其衍生物,其形式在Fms蛋白激酶或Kit蛋白激酶中的至少一种上是有活性的。 还描述了其用于治疗疾病和病症的方法,包括与Fms蛋白激酶和/或Kit蛋白激酶(包括类风湿性关节炎,骨关节炎,骨质疏松症,骨质疏松症,系统性硬化症,脱髓鞘疾病, 多发性硬化症,Charcot Marie Tooth综合征,肌萎缩性侧索硬化,阿尔茨海默病,帕金森病,溃疡性结肠炎,克罗恩病,免疫性血小板减少性紫癜,自体移植用骨髓制剂,移植排斥,肾炎,肾病,I型糖尿病,急性疼痛, 神经性疼痛,乳腺癌,前列腺癌,胰腺癌,肺癌,卵巢癌,神经胶质瘤,成胶质细胞瘤,神经纤维瘤病,溶骨性骨转移和巨细胞肿瘤。
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公开(公告)号:US20150166547A1
公开(公告)日:2015-06-18
申请号:US14571186
申请日:2014-12-15
申请人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
发明人: Prabha N. Ibrahim , Ryan Bremer , Jiazhong Zhang , Marika Nespi , Hanna Cho
IPC分类号: C07D487/04
CPC分类号: C07D487/04 , A61K31/519
摘要: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.
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公开(公告)号:US20100256365A1
公开(公告)日:2010-10-07
申请号:US12616079
申请日:2009-11-10
申请人: Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
发明人: Prabha N. Ibrahim , Dean R. Artis , Ryan Bremer , Gaston Habets , Shumeye Mamo , Marika Nespi , Chao Zhang , Jiazhong Zhang , Yong-Liang Zhu , Rebecca Zuckerman , Brian West , Yoshisa Suzuki , James Tsai , Klaus-Peter Hirth , Gideon Bollag , Wayne Spevak , Hanna Cho , Samuel J. Gillette , Guoxian Wu , Hongyao Zhu , Shenghua Shi
IPC分类号: C07D413/14 , C07D401/14 , C07F7/02 , C07D471/04
CPC分类号: C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
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公开(公告)号:US07605168B2
公开(公告)日:2009-10-20
申请号:US11219635
申请日:2005-09-02
申请人: Prabha N. Ibrahim , Ryan Bremer , Sam Gillette , Hanna Cho , Marika Nespi , Shumeye Mamo , Chao Zhang , Dean R. Artis , Byunghun Lee , Rebecca Zuckerman
发明人: Prabha N. Ibrahim , Ryan Bremer , Sam Gillette , Hanna Cho , Marika Nespi , Shumeye Mamo , Chao Zhang , Dean R. Artis , Byunghun Lee , Rebecca Zuckerman
IPC分类号: A61K31/437 , A61K31/403 , C07D471/02 , C07D405/02
CPC分类号: C07D471/04 , C07D209/12 , C07D401/12 , C07D405/04 , G06F19/16 , G06F19/706
摘要: Compounds are described that are active on PDE4. Also described are crystal structures of PDE4B determined using X-ray crystallography, the use of PDE4B crystals and structural information for identifying molecular scaffolds, for developing ligands that bind to and modulate PDE4B, and for identifying improved ligands based on known ligands.
摘要翻译: 描述了在PDE4上有活性的化合物。 还描述了使用X射线晶体学测定的PDE4B的晶体结构,使用PDE4B晶体和用于鉴定分子支架的结构信息,用于开发结合和调节PDE4B的配体,以及基于已知配体鉴定改进的配体。
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10.
公开(公告)号:US20140128373A1
公开(公告)日:2014-05-08
申请号:US13820734
申请日:2012-02-01
申请人: Prabha N. Ibrahim , Chao Zhang , Wayne Spevak , Jiazhong Zhang , Guoxian Wu , Jack Lin , Hanna Cho , Marika Nespi , Songyuan Shi , Todd Ewing , Ying Zhang
发明人: Prabha N. Ibrahim , Chao Zhang , Wayne Spevak , Jiazhong Zhang , Guoxian Wu , Jack Lin , Hanna Cho , Marika Nespi , Songyuan Shi , Todd Ewing , Ying Zhang
IPC分类号: C07D471/04 , A61K31/506 , A61K31/437 , A61K31/5377
CPC分类号: A61K31/506 , A61K31/437 , A61K31/5377 , C07D471/04
摘要: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译: 描述了对蛋白激酶有活性的化合物,以及制备和使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。
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