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公开(公告)号:US20080096887A1
公开(公告)日:2008-04-24
申请号:US11959784
申请日:2007-12-19
申请人: Kenneth He Huang , Jeron Eaves , Gunnar Hanson , James Veal , Thomas Barta , Lifeng Geng , Lindsay Hinkley
发明人: Kenneth He Huang , Jeron Eaves , Gunnar Hanson , James Veal , Thomas Barta , Lifeng Geng , Lindsay Hinkley
IPC分类号: A61K31/404 , A61K31/416 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61P19/02 , A61P25/00 , A61P29/00 , A61P3/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P9/00 , C07D209/08 , C07D231/56 , C07D401/02 , C07D405/02 , C07D409/02 , C07D413/02
CPC分类号: C07D409/12 , A61K31/404 , A61K31/416 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/00 , A61K45/06 , A61N5/10 , C07D209/08 , C07D209/14 , C07D231/54 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译: 公开了式I的化合物和药学上可接受的盐,其中R 1,R 2,R 3,R 4, R 5,R 6,R 7,n,Q 1,Q 2, 3,Q 3,Y和X 1 -X 4个如本文所定义。 式I化合物可用于治疗与细胞增殖相关的疾病和/或病症,例如癌症,炎症,关节炎,血管生成等。 还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。
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公开(公告)号:US20060084688A1
公开(公告)日:2006-04-20
申请号:US11046645
申请日:2005-01-28
申请人: Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Theresa Fletcher , John Freskos , Daniel Getman , Gunnar Hanson , Susan Hockerman , Carol Howard , Stephen Kolodziej , Madeleine Li , Joseph McDonald , Deborah Mischke , Patrick Mullins , Joseph Rico , Nathan Stehle , Clara Villamil
发明人: Thomas Barta , Daniel Becker , Louis Bedell , Terri Boehm , Jeffery Carroll , Gary DeCrescenzo , Theresa Fletcher , John Freskos , Daniel Getman , Gunnar Hanson , Susan Hockerman , Carol Howard , Stephen Kolodziej , Madeleine Li , Joseph McDonald , Deborah Mischke , Patrick Mullins , Joseph Rico , Nathan Stehle , Clara Villamil
IPC分类号: A61K31/426 , A61K31/421 , A61K31/4166 , A61K31/19
CPC分类号: C07D231/12 , A61K31/19 , A61K31/4166 , A61K31/421 , A61K31/426 , C07C317/44 , C07D207/48 , C07D211/54 , C07D211/66 , C07D211/86 , C07D211/94 , C07D211/96 , C07D225/02 , C07D233/56 , C07D239/04 , C07D249/08 , C07D263/06 , C07D265/06 , C07D279/06 , C07D281/08 , C07D309/08 , C07D309/28 , C07D319/06 , C07D325/00 , C07D335/02 , C07D337/04 , C07D401/06 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9, and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. The administered enzyme inhibitor corresponds in structure to formula (I), below, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are both hydrido or R1 and R2 together with the atoms to which they are bonded form a 5- to 8-membered ring containing one, two, or three heteroatoms in the ring that are oxygen, sulfur, or nitrogen. R3 in formula (I) is an optionally substituted aryl or optionally substituted heteroaryl radical. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.
摘要翻译: 公开了一种处理方法,其包括施用有效量的显示出一种或多种基质金属蛋白酶(MMP)酶如MMP-2,MMP-9和MMP-13的优异抑制活性的芳香族砜异羟肟酸,同时显示 至少对具有与病理基质金属蛋白酶活性相关的病症的宿主的MMP-1的抑制显着降低。 施用的酶抑制剂在结构上对应于下式(I)或其药学上可接受的盐,其中R 1和R 2都是氢或R 2, 1和R 2与它们所键合的原子一起形成在环中含有一个,两个或三个杂原子的5-至8-元环,其为氧,硫, 或氮气。 式(I)中的R 3是任选取代的芳基或任选取代的杂芳基。 还公开了具有这些选择活性的金属蛋白酶抑制剂化合物,制备这种化合物的方法和使用抑制剂的药物组合物。
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公开(公告)号:US20050080141A1
公开(公告)日:2005-04-14
申请号:US10496091
申请日:2002-11-19
申请人: Heinrich Schostarez , Gunnar Hanson
发明人: Heinrich Schostarez , Gunnar Hanson
IPC分类号: C07D295/04 , A61K31/00 , A61K31/13 , A61K31/165 , A61K31/18 , A61K31/216 , A61K31/27 , A61K31/341 , A61K31/353 , A61K31/397 , A61K31/4035 , A61K31/404 , A61K31/4172 , A61K31/4184 , A61K31/426 , A61K31/439 , A61K31/4402 , A61K31/4409 , A61K31/445 , A61K31/4453 , A61K31/46 , A61K31/472 , A61K31/495 , A61K31/5375 , A61K31/5386 , A61K31/54 , A61K31/553 , A61P25/28 , A61P43/00 , C07D209/42 , C07D209/44 , C07D211/14 , C07D211/38 , C07D211/40 , C07D211/78 , C07D213/40 , C07D213/42 , C07D215/12 , C07D215/18 , C07D217/04 , C07D217/14 , C07D221/26 , C07D233/61 , C07D233/64 , C07D235/06 , C07D265/10 , C07D267/10 , C07D277/20 , C07D277/30 , C07D295/10 , C07D295/12 , C07D307/84 , C07D311/24 , C07D487/08 , C07D498/18 , A61K31/16
摘要: The present invention relates to the treatment of Alzheimer's disease and other similar diseases, and more specifically to the use of compounds that inhibit beta-secretase, an enzyme that cleaves amyloid precursor protein to produce A beta peptide, a major component of the amyloid plaques found in the brains of Alzheimer's sufferers, in such methods.
摘要翻译: 本发明涉及阿尔茨海默病和其他类似疾病的治疗,更具体地涉及抑制β-分泌酶的化合物的使用,该酶分解淀粉样蛋白前体蛋白以产生Aβ肽,发现淀粉样蛋白斑的主要成分 在阿尔茨海默病患者的大脑中,以这种方法。
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公开(公告)号:US08299268B2
公开(公告)日:2012-10-30
申请号:US13186175
申请日:2011-07-19
申请人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
发明人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
IPC分类号: C07D263/34
CPC分类号: C07D498/22
摘要: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.
摘要翻译: 本发明涉及可用于制备重氮酰胺类似物的新型大环内酰胺中间体。 本发明还涉及用于制备这种大环内酰胺的新的电化学氧化环化,以及它们进一步阐明以提供重氮酰胺类似物。
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公开(公告)号:US20080051389A1
公开(公告)日:2008-02-28
申请号:US11726602
申请日:2007-03-21
申请人: Gunnar Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
发明人: Gunnar Hanson , David Thomas , Nizal Chandrakumar , Susan Harran
IPC分类号: A61K31/4025 , A61K31/4192 , A61K31/551 , A61P29/00 , A61P35/00 , A61P37/00 , C07D403/06 , C07D403/10 , C07D403/14 , C07D487/14
CPC分类号: C07D207/16 , C07D249/04 , C07D403/06 , C07D403/10 , C07D403/14 , C07D487/14
摘要: The invention provides small molecule mimics of the Smac peptide that are dimer- or dimer-like compounds having two amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
摘要翻译: 本发明提供Smac肽的小分子模拟物,其是具有通过接头连接的两个含酰胺的结构域的二聚体或二聚体样化合物。 这些化合物可用于促进凋亡。 本发明包括包含这些化合物的药物组合物和使用它们来治疗包括癌症和自身免疫疾病的病症的方法。
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公开(公告)号:US08642554B2
公开(公告)日:2014-02-04
申请号:US12101733
申请日:2008-04-11
申请人: Gunnar Hanson , Haizhou Sun
发明人: Gunnar Hanson , Haizhou Sun
CPC分类号: A61K38/06 , A61K38/05 , A61K45/06 , C07D207/16 , C07D403/14 , C07D409/14 , C07K5/06 , C07K5/08
摘要: The invention provides small molecule mimics of the Smac peptide that are dimer-like or trimer-like compounds having two or three amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.
摘要翻译: 本发明提供Smac肽的小分子模拟物,其是具有通过连接体连接的具有两个或三个含酰胺的结构域的二聚体样或三聚体样化合物。 这些化合物可用于促进凋亡。 本发明包括包含这些化合物的药物组合物和使用它们来治疗包括癌症和自身免疫疾病的病症的方法。
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公开(公告)号:US20110021784A1
公开(公告)日:2011-01-27
申请号:US12896898
申请日:2010-10-03
申请人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
发明人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
IPC分类号: C07D498/22 , C07D209/26 , C25B3/02
CPC分类号: C07D498/22
摘要: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.
摘要翻译: 本发明涉及可用于制备重氮酰胺类似物的新型大环内酰胺中间体。 本发明还涉及用于制备这种大环内酰胺的新的电化学氧化环化,以及它们进一步阐明以提供重氮酰胺类似物。
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公开(公告)号:US07851620B2
公开(公告)日:2010-12-14
申请号:US12134984
申请日:2008-06-06
申请人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
发明人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
IPC分类号: C07D498/22 , C07D263/00 , C07D263/34
CPC分类号: C07D498/22
摘要: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.
摘要翻译: 本发明涉及可用于制备重氮酰胺类似物的新型大环内酰胺中间体。 本发明还涉及用于制备这种大环内酰胺的新的电化学氧化环化,以及它们进一步阐明以提供重氮酰胺类似物。
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19.
公开(公告)号:US20050197338A1
公开(公告)日:2005-09-08
申请号:US10970769
申请日:2004-10-21
申请人: He Huang , Michael Stealey , Gunnar Hanson , Patrick Lennon , Bruce Hamper , Jin Xie , David Oburn , Serge Wolfson , Theresa Fletcher , Richard Heier , Matthew Reding , Michael Clare
发明人: He Huang , Michael Stealey , Gunnar Hanson , Patrick Lennon , Bruce Hamper , Jin Xie , David Oburn , Serge Wolfson , Theresa Fletcher , Richard Heier , Matthew Reding , Michael Clare
IPC分类号: A61K31/415 , A61K31/416 , A61K31/422 , A61K31/427 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/53 , C07D231/38 , C07D231/40 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10
CPC分类号: C07D403/10 , C04B35/632 , C07D231/38 , C07D401/12 , C07D403/04 , C07D405/10 , C07D409/10 , C07D413/10
摘要: Compounds of Formula I: wherein X1, X2, L1, A, R, L2, R1, R12, R12a, R13, R14 and R14a are as defined herein, are disclosed.
摘要翻译: 式I的化合物:其中X 1,X 2,L 1,A,R,L 2, R 1,R 12,R 12,R 13,R 14和R 14,和 R 14a如本文所定义。
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公开(公告)号:US07982051B2
公开(公告)日:2011-07-19
申请号:US12896898
申请日:2010-10-03
申请人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
发明人: Gunnar Hanson , Charles Caldwell , Patrick G. Harran , Susan Harran , Qi Wei , Ming Zhou
IPC分类号: C07D263/34 , C07D209/20
CPC分类号: C07D498/22
摘要: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.
摘要翻译: 本发明涉及可用于制备重氮酰胺类似物的新型大环内酰胺中间体。 本发明还涉及用于制备这种大环内酰胺的新的电化学氧化环化,以及它们进一步阐明以提供重氮酰胺类似物。
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