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公开(公告)号:US20080153802A1
公开(公告)日:2008-06-26
申请号:US11642591
申请日:2006-12-21
IPC分类号: C07C275/54 , A61K31/197 , A61K31/381 , A61K31/404 , C07D209/18 , C07D265/30 , C07D487/00 , C07D333/50 , C07D213/46 , A61K31/44 , A61K31/5375 , A61K31/55
CPC分类号: C07C275/54 , C07C323/44 , C07C323/59 , C07C323/60 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07D209/26 , C07D213/40 , C07D213/56 , C07D223/16 , C07D333/60
摘要: Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.
摘要翻译: 公开了作为模拟仅含BH3蛋白质的α螺旋肽模拟物,含有它们的组合物,其与细胞靶向部分的缀合及其在调节细胞死亡中的用途的苯甲酰脲衍生物。 苯甲酰脲衍生物能够结合并中和原始存活的Bcl-2蛋白。 还描述了苯甲酰脲衍生物在治疗和/或预防与细胞死亡调节相关的疾病或病症中的用途。
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公开(公告)号:US07956216B2
公开(公告)日:2011-06-07
申请号:US11642591
申请日:2006-12-21
IPC分类号: C07C229/00 , A61K31/195
CPC分类号: C07C275/54 , C07C323/44 , C07C323/59 , C07C323/60 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07D209/26 , C07D213/40 , C07D213/56 , C07D223/16 , C07D333/60
摘要: Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.
摘要翻译: 公开了作为模拟仅含BH3蛋白质的α螺旋肽模拟物,含有它们的组合物,其与细胞靶向部分的缀合及其在调节细胞死亡中的用途的苯甲酰脲衍生物。 苯甲酰脲衍生物能够结合并中和原始存活的Bcl-2蛋白。 还描述了苯甲酰脲衍生物在治疗和/或预防与细胞死亡调节相关的疾病或病症中的用途。
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公开(公告)号:US20070197430A1
公开(公告)日:2007-08-23
申请号:US11571160
申请日:2005-06-24
申请人: Jonathan Baell , Andrew Wei , Denis Scanlon
发明人: Jonathan Baell , Andrew Wei , Denis Scanlon
CPC分类号: C07K16/2803 , A61K38/00 , A61K47/6811 , A61K47/6849 , A61K2039/505 , C07K1/02 , C07K1/04 , C07K7/06 , C07K7/08 , C07K7/54 , C07K7/56 , C07K7/60 , C07K14/4747 , C07K16/00 , C07K2319/00
摘要: Conformationally constrained peptides that mimic BH3-only proteins and their conjugation to antibodies and other cell targeting compounds, compositions containing the conjugates and their use in the regulation of cell death are disclosed. The conformationally constrained peptides are capable of binding to and neutralising pro-survival Bcl-2 proteins. Processes for preparing the conformationally constrained peptides conjugated to antibodies and other cell targeting compounds and use of the conjugates in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also disclosed.
摘要翻译: 公开了模拟仅含有BH3的蛋白质及其与抗体和其他细胞靶向化合物的缀合的构象约束肽,其含有缀合物的组合物及其在调节细胞死亡中的用途。 构象约束的肽能够结合和中和原始存活的Bcl-2蛋白。 还公开了制备与抗体和其它细胞靶向化合物缀合的构象约束肽的方法和缀合物用于治疗和/或预防与细胞死亡调节相关的疾病或病症的用途。
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公开(公告)号:US20060057144A1
公开(公告)日:2006-03-16
申请号:US10861227
申请日:2004-06-03
申请人: Jonathan Baell , Thomas Garrett , P. Hogarth , Barry Matthews , Thomas McCarthy , Geoffrey Pietersz , Maree Powell , Ian McKenzie , Kelly Maxwell , Vidana Epa
发明人: Jonathan Baell , Thomas Garrett , P. Hogarth , Barry Matthews , Thomas McCarthy , Geoffrey Pietersz , Maree Powell , Ian McKenzie , Kelly Maxwell , Vidana Epa
IPC分类号: A61K38/17 , A61K39/395
CPC分类号: C07K14/70535 , A61K38/00
摘要: This invention relates to a method of inhibiting FC receptor binding of immunoglobulin comprising the use of a Fc receptor modulating compound which binds to defined surfaces on a Fc receptor. The present invention also relates to a method for treating a variety of diseases using a Fc receptor modulating compound.
摘要翻译: 本发明涉及一种抑制免疫球蛋白FC受体结合的方法,包括使用Fc受体调节化合物,其结合Fc受体上的限定表面。 本发明还涉及使用Fc受体调节化合物治疗各种疾病的方法。
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公开(公告)号:US20050261301A1
公开(公告)日:2005-11-24
申请号:US10507925
申请日:2003-03-20
申请人: Jonathan Baell , Heike Wulff , Andrew Harvey , Raymond Norton , George Chandy
发明人: Jonathan Baell , Heike Wulff , Andrew Harvey , Raymond Norton , George Chandy
IPC分类号: A61K31/343 , A61P29/00 , A61P37/00 , A61P37/06 , C07D307/86 , C07D405/14 , C07D409/14 , C07D417/14 , A61K31/506 , A61K31/381 , A61K31/427 , A61K31/4433 , A61K31/497 , A61K31/501 , C07D45/14
CPC分类号: C07D417/14 , C07D307/86 , C07D405/14 , C07D409/14
摘要: Various divalent ligands based on khellinone derivatives are described. These derivatives can be useful in the modulation of potassium channel activity in cells, including among others Kv1.3 channels found in T-cells. The compounds may also be useful in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis.
摘要翻译: 描述了基于凯芬酮衍生物的各种二价配体。 这些衍生物可用于细胞中钾通道活性的调节,包括在T细胞中发现的Kv1.3通道。 所述化合物还可用于治疗或预防自身免疫性和炎性疾病,包括多发性硬化。
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公开(公告)号:US20050176813A1
公开(公告)日:2005-08-11
申请号:US10507782
申请日:2003-03-14
申请人: Jonathan Baell , Heike Wulff , George Chandy , Raymond Norton
发明人: Jonathan Baell , Heike Wulff , George Chandy , Raymond Norton
IPC分类号: C07D333/54 , A61K31/12 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/423 , A61K31/428 , A61K31/443 , A61K31/47 , A61K31/4709 , A61K31/472 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/06 , A61P3/10 , A61P5/14 , A61P7/00 , A61P7/02 , A61P7/06 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/00 , A61P13/10 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/14 , A61P17/16 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/28 , A61P27/02 , A61P27/12 , A61P27/14 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/14 , A61P31/18 , A61P31/20 , A61P31/22 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P39/00 , A61P41/00 , A61P43/00 , C07C49/755 , C07C49/84 , C07D215/26 , C07D217/02 , C07D263/54 , C07D277/62 , C07D307/86 , C07D307/91 , C07D405/06 , C07D405/10 , C07D407/06 , C07D409/06
CPC分类号: A61K31/47 , A61K31/343 , A61K31/381 , A61K31/403 , A61K31/404 , A61K31/41 , A61K31/423 , A61K31/428
摘要: Various chalcone derivatives of the general formula (I) are described and the variables, A, B, m and R1 to R10 are as defined in the specification. These derivatives can be useful in the modulation of potassium channel activity in cells and may be useful in the treatment or prevention of autoimmune and inflammatory diseases.
摘要翻译: 描述通式(I)的各种查耳酮衍生物,并且变量A,B,m和R 1至R 10如说明书中所定义。 这些衍生物可用于调节细胞中钾通道活性,并且可用于治疗或预防自身免疫性和炎性疾病。
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公开(公告)号:US20070032417A1
公开(公告)日:2007-02-08
申请号:US10540390
申请日:2003-12-24
申请人: Jonathan Baell
发明人: Jonathan Baell
CPC分类号: C07K7/02 , A61K38/00 , C07K14/4747
摘要: Conformationally constrained peptides that mimic BH3-only proteins, compositions containing them and their use in the regulation of cell death are disclosed. The conformationally constrained peptides are capable of binding to and neutralising pro-survival Bcl-2 proteins. Processes for preparing the conformationally constrained peptides and their use in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also disclosed.
摘要翻译: 公开了模拟仅含有BH3的蛋白质的构象约束肽,含有它们的组合物及其在调节细胞死亡中的用途。 构象约束的肽能够结合和中和原始存活的Bcl-2蛋白。 还公开了制备构象约束肽及其在治疗和/或预防与细胞死亡调节相关的疾病或病症中的用途的方法。
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