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公开(公告)号:US20110015371A1
公开(公告)日:2011-01-20
申请号:US12800046
申请日:2010-05-05
申请人: Guy W. Bemis , Julian M. C. Golec , David J. Lauffer , Michael D. Mullican , Mark A. Murcko , David J. Livingston
发明人: Guy W. Bemis , Julian M. C. Golec , David J. Lauffer , Michael D. Mullican , Mark A. Murcko , David J. Livingston
IPC分类号: C07K5/10 , C07D213/76 , C07D413/12 , C07K5/08 , C07D233/90 , C07D207/34
CPC分类号: C07D243/08 , A61K38/00 , C07D243/12 , C07D263/56 , C07D413/04 , C07D487/04 , C07K5/0202 , C07K5/06052 , C07K5/0812
摘要: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
摘要翻译: 本发明涉及作为白介素-1和bgr的抑制剂的新型化合物。 转化酶。 本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制ICE活性,因此可有利地用作抗白介素-1介导的疾病(包括炎性疾病,自身免疫性疾病和神经变性疾病)的药物。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性的方法和用于治疗白细胞介素-1介导的疾病的方法。
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公开(公告)号:US20090048250A1
公开(公告)日:2009-02-19
申请号:US11841233
申请日:2007-08-20
申请人: Alex Aronov , David J. Lauffer , Huan Qiu Li , Ronald Charles Tomlinson , Pan Li
发明人: Alex Aronov , David J. Lauffer , Huan Qiu Li , Ronald Charles Tomlinson , Pan Li
IPC分类号: A61K31/5377 , C07D231/54 , A61K31/4152 , C07D471/04 , C07D413/04 , A61K31/437 , C07D403/02 , A61K31/53
CPC分类号: C07D403/14 , C07D407/14 , C07D409/14 , C07D471/04
摘要: The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK2, CDK2, MK2, SRC, SYK, and Aurora-2. Accordingly, compounds and compositions of the invention are useful for treating or lessening the severity of a variety of disorders, including, but not limited to, heart disease, diabetes, Alzheimer's disease, immunodeficiency disorders, inflammatory diseases, allergic diseases, autoimmune diseases, destructive bone disorders such as osteoporosis, proliferative disorders, infectious diseases and viral diseases.
摘要翻译: 本发明提供式I化合物:这些化合物及其药学上可接受的组合物通常用作激酶抑制剂,特别是作为PRAK,GSK3,ERK2,CDK2,MK2,SRC,SYK和Aurora-2的抑制剂。 因此,本发明的化合物和组合物可用于治疗或减轻各种障碍的严重性,包括但不限于心脏病,糖尿病,阿尔茨海默氏病,免疫缺陷病症,炎性疾病,过敏性疾病,自身免疫疾病,破坏性 骨质疏松症,增殖性疾病,感染性疾病和病毒性疾病等骨骼疾病。
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公开(公告)号:US07446199B2
公开(公告)日:2008-11-04
申请号:US10936470
申请日:2004-09-07
申请人: Alex Aronov , David J. Lauffer , Pan Li , Ronald C. Tomlinson
发明人: Alex Aronov , David J. Lauffer , Pan Li , Ronald C. Tomlinson
IPC分类号: C07D471/04 , C07D401/02
CPC分类号: C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译: 本发明涉及可用于蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病,病症或病症的方法。
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公开(公告)号:US07169800B2
公开(公告)日:2007-01-30
申请号:US10949027
申请日:2004-09-24
申请人: Alex Aronov , David J. Lauffer , Pan Li , Ronald C. Tomlinson
发明人: Alex Aronov , David J. Lauffer , Pan Li , Ronald C. Tomlinson
IPC分类号: A61K31/422 , C07D413/04
CPC分类号: C07D405/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04
摘要: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.
摘要翻译: 本发明涉及可用于蛋白激酶抑制剂的化合物。 本发明还提供了制备本发明化合物的方法,包含本发明化合物的药学上可接受的组合物,以及使用该组合物治疗各种疾病的方法。
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公开(公告)号:US06974809B2
公开(公告)日:2005-12-13
申请号:US10424576
申请日:2003-04-25
申请人: Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
发明人: Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
IPC分类号: A61K38/00 , A61K38/55 , A61P1/00 , A61P1/18 , A61P7/00 , A61P9/10 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07K5/02 , C07K5/023 , C07K5/097 , C07D491/00 , C07D495/00 , A61K31/55
CPC分类号: C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1β converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), interferon-γ-(“IFN-γ”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-γ production and methods for treating interleukin-1, apoptosis- and interferon-γ-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
摘要翻译: 本发明涉及作为白细胞介素-1β转换酶(“ICE”)抑制剂的新型化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制ICE活性,因此可有利地用作抗白细胞介素-1-(“IL-1”),细胞凋亡,干扰素-γ诱导因子(IGIF) 干扰素-γ-(“IFN-γ”)介导的疾病,过度饮食酒精摄入疾病或病毒性疾病,包括炎性疾病,自身免疫疾病,破坏性骨病,增殖性疾病,感染性疾病和退行性疾病。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1,凋亡和干扰素-γ介导的疾病的方法。 本发明还涉及制备本发明化合物的方法。
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公开(公告)号:US06329365B1
公开(公告)日:2001-12-11
申请号:US09326495
申请日:1999-06-04
申请人: Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
发明人: Julian M. C. Golec , David J. Lauffer , David J. Livingston , Michael D. Mullican , Mark A. Murcko , Philip L. Nyce , Andrea L. C. Robidoux , Marion W. Wannamaker
IPC分类号: A61K3155
CPC分类号: C07K5/0821 , A61K38/00 , C07K5/0202 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/475
摘要: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme (“ICE”). This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, excess dietary alcohol intake diseases, or viral diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to methods for inhibiting ICE activity and decreasing IGIF production and IFN-&ggr; production and methods for treating interleukin-1, apoptosis- and interferon-&ggr;-mediated diseases using the compounds and compositions of this invention. This invention also relates to methods of preparing the compounds of this invention.
摘要翻译: 本发明涉及作为白细胞介素-1β转换酶(“ICE”)抑制剂的新型化合物。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制ICE活性,因此可有利地用作抗白细胞介素-1-(“IL-1”),细胞凋亡,干扰素-γ诱导因子(IGIF) 干扰素-γ-(“IFN-γ”)介导的疾病,过度饮食酒精摄入疾病或病毒性疾病,包括炎性疾病,自身免疫疾病,破坏性骨病,增殖性疾病,感染性疾病和退行性疾病。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性和降低IGIF产生和IFN-γ产生的方法以及用于治疗白细胞介素-1,凋亡和干扰素-γ介导的疾病的方法。 本发明还涉及制备本发明化合物的方法。
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公开(公告)号:US06258948B1
公开(公告)日:2001-07-10
申请号:US09400639
申请日:1999-09-21
申请人: Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M. C. Golec , Yong Gu , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Philip Nyce , Andrea L. C. Robidoux , Michael Su , M. Woods Wannamaker , Keith P. Wilson , Robert E. Zelle
发明人: Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M. C. Golec , Yong Gu , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Philip Nyce , Andrea L. C. Robidoux , Michael Su , M. Woods Wannamaker , Keith P. Wilson , Robert E. Zelle
IPC分类号: C07D26702
CPC分类号: C07D243/12 , A61K38/00 , C07D401/06 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07K5/0202 , C07K5/06139 , C07K5/0821
摘要: The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention. This invention also relates to methods for preparing N-acylamino compounds.
摘要翻译: 本发明涉及作为白介素-IB转化酶抑制剂的新型化合物。 本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适用于抑制ICE活性,因此可有利地用作抗IL-1,细胞凋亡,IGIF和IFN-γ介导的疾病,炎性疾病,自身免疫性疾病 破坏性骨病,增殖性疾病,感染性疾病,退行性疾病和坏死性疾病。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性,治疗白细胞介素-1,细胞凋亡,IGIF-和IFN-γ介导的疾病以及减少IGIF和IFN-γ产生的方法。 本发明还涉及制备N-酰基氨基化合物的方法。
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公开(公告)号:US6008217A
公开(公告)日:1999-12-28
申请号:US575641
申请日:1995-12-20
申请人: Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M. C. Golec , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Robert E. Zelle
发明人: Mark James Batchelor , David Bebbington , Guy W. Bemis , Wolf Herman Fridman , Roger John Gillespie , Julian M. C. Golec , David J. Lauffer , David J. Livingston , Saroop Singh Matharu , Michael D. Mullican , Mark A. Murcko , Robert Murdoch , Robert E. Zelle
IPC分类号: A61K38/00 , C07K5/02 , C07D217/22 , A61K31/47 , C07D217/16
CPC分类号: C07K5/0202 , A61K38/00
摘要: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against an IL-1 mediated disease, an apoptosis mediated disease, AML, CML, melanoma, myeloma, Kaposi's sarcoma, graft vs host disease, rheumatoid arthritis, inflammatory bowel disorder, psoriasis, osteoarthritis, myeloma, apoptosis, sepsis, rheumatoid arthritis, asthma, Alzheimer's disease, Parkinson's disease, and ischemic heart disease diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
摘要翻译: 本发明涉及作为白细胞介素-1β转换酶抑制剂的新型化合物。 本发明的ICE抑制剂的特征在于具体的结构和物理化学特征。 本发明还涉及包含这些化合物的药物组合物。 本发明的化合物和药物组合物特别适合于抑制ICE活性,因此可有利地用作抗IL-1介导的疾病,细胞凋亡介导的疾病,AML,CML,黑素瘤,骨髓瘤,卡波西氏肉瘤,移植物 与宿主疾病,类风湿性关节炎,炎性肠病,牛皮癣,骨关节炎,骨髓瘤,凋亡,败血症,类风湿性关节炎,哮喘,阿尔茨海默病,帕金森病和缺血性心脏病疾病相关。 本发明还涉及使用本发明的化合物和组合物来抑制ICE活性的方法和用于治疗白细胞介素-1介导的疾病的方法。
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公开(公告)号:US5716929A
公开(公告)日:1998-02-10
申请号:US464964
申请日:1995-06-05
申请人: Guy W. Bemis , Julian M. C. Golec , David J. Lauffer , Michael D. Mullican , Mark A. Murcko , David J. Livingston
发明人: Guy W. Bemis , Julian M. C. Golec , David J. Lauffer , Michael D. Mullican , Mark A. Murcko , David J. Livingston
IPC分类号: C07D263/24 , A61K31/42 , A61K31/421 , A61K38/00 , A61K45/00 , A61P25/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07C229/22 , C07C233/41 , C07C233/83 , C07C311/30 , C07C317/26 , C07D521/00 , C07K5/02 , C07K5/023 , C07K5/04 , A61K38/05 , A61K38/06 , C07K5/06 , C07K5/08
CPC分类号: C07K5/0202 , A61K38/00
摘要: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
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公开(公告)号:US20180325898A1
公开(公告)日:2018-11-15
申请号:US16042206
申请日:2018-07-23
申请人: Paul S. Charifson , Kevin Michael Cottrell , Hongbo Deng , John P. Duffy , Huai Gao , Simon Giroux , Jeremy Green , Katrina Lee Jackson , Joseph M. Kennedy , David J. Lauffer , Mark Willem Ledeboer , Pan Li , John Patrick Maxwell , Mark A. Morris , Albert Charles Pierce , Nathan D. Waal , Jinwang Xu
发明人: Paul S. Charifson , Kevin Michael Cottrell , Hongbo Deng , John P. Duffy , Huai Gao , Simon Giroux , Jeremy Green , Katrina Lee Jackson , Joseph M. Kennedy , David J. Lauffer , Mark Willem Ledeboer , Pan Li , John Patrick Maxwell , Mark A. Morris , Albert Charles Pierce , Nathan D. Waal , Jinwang Xu
IPC分类号: A61K31/506 , A61K9/48 , C07D417/10 , A61K41/00 , C07D521/00 , C07D495/04 , C07D491/056 , C07D491/048 , C07D471/04 , C07D417/14 , C07D417/04 , C07D413/10 , C07D413/04 , C07D409/14 , C07D409/04 , C07D239/42 , C07D403/10 , C07D403/04 , C07D401/04 , C07D413/14 , C07D405/14 , C07D401/14 , A61K47/55 , A61K31/53 , A61K47/54 , A61K31/5377 , A61K9/20
CPC分类号: C07D401/14 , A61K9/20 , A61K9/48 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K41/0038 , A61K47/545 , A61K47/55 , C07D239/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/048 , C07D491/056 , C07D495/04 , C07D521/00
摘要: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
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