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1.
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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公开(公告)号:US09624213B2
公开(公告)日:2017-04-18
申请号:US13820734
申请日:2012-02-01
申请人: Prabha 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 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.
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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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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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6.
公开(公告)号:US08268858B2
公开(公告)日:2012-09-18
申请号:US11961901
申请日:2007-12-20
申请人: Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
发明人: Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
IPC分类号: A61K31/437 , C07D471/04
CPC分类号: C07D471/04 , C07D519/00
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:US20080188514A1
公开(公告)日:2008-08-07
申请号:US11961901
申请日:2007-12-20
申请人: Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
发明人: Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
IPC分类号: A61K31/437 , C07D471/04 , A61P9/00 , A61P25/28 , A61P25/16 , A61P25/00 , A61P35/00 , A61P35/02
CPC分类号: C07D471/04 , C07D519/00
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:US20140038948A1
公开(公告)日:2014-02-06
申请号:US13926959
申请日:2013-06-25
申请人: Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
发明人: Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
IPC分类号: C07D285/16 , A61K31/5377 , A61K31/505 , A61K31/437 , A61K31/47 , C07D213/76 , A61K31/44 , C07D239/49 , C07D471/04 , C07D215/38 , C07D417/12 , A61K31/549 , A61K31/4439
CPC分类号: A61K31/44 , A61K31/415 , A61K31/42 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/549 , A61K45/06 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D231/40 , C07D239/48 , C07D239/49 , C07D261/14 , C07D263/48 , C07D285/135 , C07D285/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , A61K31/4427 , A61K2300/00
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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9.
公开(公告)号:US20100190777A1
公开(公告)日:2010-07-29
申请号:US12669450
申请日:2008-07-16
申请人: Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
发明人: Guoxian Wu , Jiazhong Zhang , Yong-Liang Zhu , Chao Zhang , Prabha N. Ibrahim , Songyuan Shi , Wayne Spevak , Dean R. Artis , James Tsai
IPC分类号: C07D213/75 , A61K31/54 , A61K31/5377 , A61K31/505 , A61K31/47 , A61K31/437 , A61K31/44 , A61K31/41 , A61K31/42 , A61K31/415 , A61K31/165 , C07D471/02 , C07D413/02 , C07D403/00 , A61K31/444 , C07D215/38 , A61P35/00 , C07D417/02 , C07D213/02 , C07D285/12 , C07D261/14 , C07D231/02 , C07C233/64
CPC分类号: A61K31/44 , A61K31/415 , A61K31/42 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/549 , A61K45/06 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D231/40 , C07D239/48 , C07D239/49 , C07D261/14 , C07D263/48 , C07D285/135 , C07D285/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , A61K31/4427 , A61K2300/00
摘要: Compounds of formula I 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. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.
摘要翻译: 描述了对蛋白激酶有活性的式I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。 式(I)其中Ar是任选取代的杂芳基; R2是氢,低级烷基或卤素; U选自-S(O)2 - , - C(X) - , - C(X)-N(R 10) - 和-S(O)2 -N(R 10) - ; R 3是任选取代的低级烷基,任选取代的C 3-6环烷基,任选取代的杂环烷基,任选取代的芳基或任选取代的杂芳基; 并且其中R 1,R 3,R 4,m,L 1,X R 10如本文所述。
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10.
公开(公告)号:US20110263595A1
公开(公告)日:2011-10-27
申请号:US13090969
申请日:2011-04-20
申请人: Jiazhong Zhang , Prabha N. Ibrahim , Wayne Spevak , James Tsai , Todd Ewing , Ying Zhang , Chao Zhang
发明人: Jiazhong Zhang , Prabha N. Ibrahim , Wayne Spevak , James Tsai , Todd Ewing , Ying Zhang , Chao Zhang
IPC分类号: A61K31/5377 , A61K31/506 , A61K31/437 , C07D487/04 , A61K31/519 , C07D413/14 , A61P19/02 , A61P19/10 , A61P9/00 , A61P25/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P1/00 , C07D471/04
CPC分类号: C07D487/04 , C07D471/04
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 one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC, 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, global ischemia, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, atherosclerosis, systemic lupus erythematosis, myelopreparation for autologous transplantation, transplant rejection, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, acute myeloid leukemia, melanoma, multiple myeloma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastoma, neurofibromatosis, osteolytic bone metastases, brain metasteses, gastrointestinal stromal tumors, 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,Kit,Flt3,TrkA,TrkB和TrkC激酶蛋白中的一种或多种上是有活性的。 还描述了其用于治疗疾病和病症的方法,包括与Fms,Kit,Flt3,TrkA,TrkB和TrkC中的一种或多种的活性相关的疾病和病症,包括类风湿性关节炎,骨关节炎,骨质疏松症,假体周围骨质溶解, 系统性硬化症,脱髓鞘疾病,多发性硬化症,Charcot玛丽牙综合征,肌萎缩性侧索硬化症,阿尔茨海默氏病,帕金森病,全球缺血,溃疡性结肠炎,克罗恩病,免疫性血小板减少性紫癜,动脉粥样硬化,系统性红斑狼疮,自体移植骨髓移植,移植排斥 肾小球肾炎,间质性肾炎,狼疮性肾炎,肾小管坏死,糖尿病性肾病,肾肥大,I型糖尿病,急性疼痛,炎性疼痛,神经性疼痛,急性骨髓性白血病,黑素瘤,多发性骨髓瘤,乳腺癌,前列腺癌,胰腺癌,肺癌 癌症,卵巢癌,神经胶质瘤,胶质母细胞瘤,神经元 骨质疏松症,溶骨性骨转移,脑转移,胃肠道间质瘤和巨细胞肿瘤。
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