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1. 发明申请

US20070010457A1 Caspase inhibitors and uses thereof 有权
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US20070010457A1
公开(公告)日：2007-01-11
申请号：US11522375
申请日：2006-09-14
申请人： Anita Diu-Hercend , Julian Golec , Thierry Hercend , Ronald Knegtel , Paul Lang , Andrew Miller , Karen Miller , Michael Mortimore , Peter Weber
发明人： Anita Diu-Hercend , Julian Golec , Thierry Hercend , Ronald Knegtel , Paul Lang , Andrew Miller , Karen Miller , Michael Mortimore , Peter Weber
IPC分类号： A61K38/04 , A61K31/497 , A61K31/4709 , A61K31/454
CPC分类号： C07D401/06 , C07D211/60 , C07D405/06 , C07D409/06 , C07D417/06
摘要： The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-y inducing factor-(IGIF), interferon-γ-(“IFN-γ”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention. This invention also relates to methods for inhibiting caspase and TNF-alpha activity and decreasing IGIF production and IFN-γ production and methods for treating caspase-, interleukin-1, apoptosis-, and interferon-γ-, and TNF-alpha mediated diseases using the compounds and compositions of this invention.
摘要翻译：本发明涉及新型的式I化合物，其为半胱天冬酶和TNF-α抑制剂。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半胱天冬酶和TNF-α活性，因此可有利地用作抗半胱天冬酶，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”）或TNF-α介导的疾病，包括炎性疾病，自身免疫性疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及制备本发明化合物的方法。本发明还涉及用于抑制半胱天冬酶和TNF-α活性并减少IGIF产生和IFN-γ产生的方法以及用于治疗半胱天冬酶，白细胞介素-1，细胞凋亡和干扰素γ和TNF-α介导的疾病的方法，其使用本发明的化合物和组合物。

2. 发明授权

US07960398B2 Regulation of TNF-alpha 失效
标题翻译：调节TNF-α
公开(公告)号：US07960398B2
公开(公告)日：2011-06-14
申请号：US10419327
申请日：2003-04-17
申请人： Karen Miller , Anita Diu-Hercend , Thierry Hercend , Paul Lang , Peter Weber , Julian Golec , Michael Mortimore
发明人： Karen Miller , Anita Diu-Hercend , Thierry Hercend , Paul Lang , Peter Weber , Julian Golec , Michael Mortimore
IPC分类号： A61K31/517
CPC分类号： C07D235/24 , A61K38/00 , C07C233/64 , C07C233/83 , C07C235/52 , C07C237/22 , C07C237/42 , C07C255/57 , C07C271/22 , C07C271/28 , C07C2601/14 , C07D209/42 , C07D209/86 , C07D211/60 , C07D217/24 , C07D233/90 , C07D239/90 , C07D401/06 , C07D405/12 , C07D409/06 , C07D417/06 , C07D455/04 , C07D487/04 , C07F9/3264 , C07F9/65128 , C07K5/0202 , G01N33/6863 , G01N2333/525 , G01N2500/04 , Y02A50/411
摘要： The present invention relates to methods for identifying compounds useful for regulating TNF-alpha levels and/or activity. The invention also relates to methods for decreasing TNF-alpha levels and/or activity. Compounds and compositions according to this invention are useful for treating TNF-mediated diseases. The invention also relates to kits comprising the compounds and compositions herein and a tool for measuring TNF-alpha activity and/or levels.
摘要翻译：本发明涉及用于鉴定可用于调节TNF-α水平和/或活性的化合物的方法。本发明还涉及降低TNF-α水平和/或活性的方法。根据本发明的化合物和组合物可用于治疗TNF介导的疾病。本发明还涉及包含本文的化合物和组合物的试剂盒以及用于测量TNF-α活性和/或水平的工具。

3. 发明授权

US07807659B2 Caspase inhibitors and uses thereof 有权
标题翻译：胱天蛋白酶抑制剂及其用途
公开(公告)号：US07807659B2
公开(公告)日：2010-10-05
申请号：US11522375
申请日：2006-09-14
申请人： Anita Diu-Hercend , Julian Golec , Thierry Hercend , Ronald Knegtel , Paul Lang , Andrew Miller , Karen Miller , Michael Mortimore , Peter Weber
发明人： Anita Diu-Hercend , Julian Golec , Thierry Hercend , Ronald Knegtel , Paul Lang , Andrew Miller , Karen Miller , Michael Mortimore , Peter Weber
IPC分类号： A61K31/675 , A01N57/00
CPC分类号： C07D401/06 , C07D211/60 , C07D405/06 , C07D409/06 , C07D417/06
摘要： The present invention relates to novel classes of compounds of formula I which are caspase and TNF-alpha inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase and TNF-alpha activity and consequently, can be advantageously used as agents against caspase-, interleukin-1-(“IL-1”), apoptosis-, interferon-γ inducing factor-(IGIF), interferon-γ-(“IFN-γ”), or TNF-alpha mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases. This invention also relates to processes for preparing the compounds of this invention. This invention also relates to methods for inhibiting caspase and TNF-alpha activity and decreasing IGIF production and IFN-γ production and methods for treating caspase-, interleukin-1, apoptosis-, and interferon-γ-, and TNF-alpha mediated diseases using the compounds and compositions of this invention.
摘要翻译：本发明涉及新型的式I化合物，其为半胱天冬酶和TNF-α抑制剂。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半胱天冬酶和TNF-α活性，因此可有利地用作抗半胱天冬酶，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”）或TNF-α介导的疾病，包括炎性疾病，自身免疫性疾病，破坏性骨病，增殖性疾病，感染性疾病和退行性疾病。本发明还涉及制备本发明化合物的方法。本发明还涉及用于抑制半胱天冬酶和TNF-α活性并减少IGIF产生和IFN-γ产生的方法以及用于治疗半胱天冬酶，白细胞介素-1，细胞凋亡和干扰素-γ以及TNF-α介导的疾病的方法本发明的化合物和组合物。

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