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1. 发明授权

US08518885B2 Heterocyclic peptide ketoamides 失效
标题翻译：杂环肽酮酰胺
公开(公告)号：US08518885B2
公开(公告)日：2013-08-27
申请号：US12866541
申请日：2008-07-16
申请人： James C. Powers , Jonathan D. Glass , Asli Ovat , Zhaozhao Li
发明人： James C. Powers , Jonathan D. Glass , Asli Ovat , Zhaozhao Li
IPC分类号： A61K38/05 , C07K5/06
CPC分类号： C07K5/06043 , C07K5/06052
摘要： A novel class of peptide α-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl α-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided.
摘要翻译：用于选择性抑制钙蛋白酶，选择性抑制半胱氨酸蛋白酶和通常抑制具有式M-AA2-AA1-CO-NH-（CH2）n-R3的所有半胱氨酸蛋白酶的新一类肽α-酮酰胺。肽基α-酮酰胺衍生物的合成方法。提供了抑制半胱氨酸蛋白酶，抑制钙蛋白酶和治疗由半胱氨酸蛋白酶和钙蛋白酶引起的疾病的组合物和方法。

2. 发明申请

US20110053858A1 HETEROCYCLIC PEPTIDE KETOAMIDES 失效
标题翻译：杂环酮类酮酸酯
公开(公告)号：US20110053858A1
公开(公告)日：2011-03-03
申请号：US12866541
申请日：2008-07-16
申请人： James C. Powers , Jonathan D. Glass , Asli Ovat , Zhaozhao Li
发明人： James C. Powers , Jonathan D. Glass , Asli Ovat , Zhaozhao Li
IPC分类号： A61K38/05 , C12N9/99 , C07D295/195 , C07D473/34 , C07D241/04 , C07D213/56 , C07C237/10 , A61P25/00 , A61P25/16 , A61P25/28
CPC分类号： C07K5/06043 , C07K5/06052
摘要： A novel class of peptide α-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl α-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided
摘要翻译：用于选择性抑制钙蛋白酶，选择性抑制半胱氨酸蛋白酶和通常抑制具有式M-AA2-AA1-CO-NH-（CH2）n-R3的所有半胱氨酸蛋白酶的新型肽α-酮酰胺。肽基α-酮酰胺衍生物的合成方法。提供了抑制半胱氨酸蛋白酶，抑制钙蛋白酶和治疗由半胱氨酸蛋白酶和钙蛋白酶引起的疾病的组合物和方法

3. 发明授权

US08013014B2 Aza-peptide epoxides 有权
标题翻译：氮杂肽环氧化物
公开(公告)号：US08013014B2
公开(公告)日：2011-09-06
申请号：US11338147
申请日：2006-01-24
申请人： James C. Powers , Jonathan D. Glass
发明人： James C. Powers , Jonathan D. Glass
IPC分类号： A61K31/335
CPC分类号： A61K38/05 , A61K31/336 , A61K31/401 , A61K31/405 , A61K38/06 , C07D303/48 , C07K5/0207 , C07K5/06026 , C07K5/06043 , C07K5/0808 , C07K5/0819 , C07K5/101 , C07K5/1021
摘要： Methods for treatment and/or prevention of nerve degeneration in mammals using aza-peptide epoxide caspase inhibitors are provided. Aspects of the present disclosure include aza-peptide epoxide compositions to treat or prevent diseases, for example stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis, neuropathies, Huntington's disease, dentatorubropallidoluysian atrophy, spinocerebellar atrophies, spinal bulbar muscular atrophy, diabetes, amyotrophic lateral sclerosis and other motor neuron diseases. The disclosed methods can be used in combination with calpain inhibitors to treat disease or pathological conditions related to the activity of caspases and calpain associated with a specific disease or condition. Such treatable conditions include stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis, neuropathies, Huntington's disease, dentatorubropallidoluysian atrophy, spinocerebellar atrophies, spinal bulbar muscular atrophy, nerve degeneration associated with diabetes, amyotrophic lateral sclerosis and other motor neuron diseases, nerve degeneration secondary to primary demyelinating disorders, among others.
摘要翻译：提供了使用氮杂 - 环氧化物半胱天冬酶抑制剂治疗和/或预防哺乳动物神经变性的方法。本公开的方面包括治疗或预防疾病，例如中风，阿尔茨海默氏病，帕金森病，多发性硬化，神经病，亨廷顿舞蹈病，齿状萎缩性萎缩症，脊髓小脑萎缩症，脊髓扩张肌肉萎缩症，糖尿病，肌萎缩性侧索的氮杂肽环氧化物组合物硬化症等运动神经元疾病。所公开的方法可以与钙蛋白酶抑制剂组合使用以治疗与特定疾病或病症相关的胱天蛋白酶和钙蛋白酶的活性相关的疾病或病理状况。这种可治疗的病症包括中风，阿尔茨海默氏病，帕金森病，多发性硬化症，神经病，亨廷顿舞蹈病，齿状萎缩性萎缩症，脊髓小脑萎缩，脊髓延髓肌肉萎缩，与糖尿病相关的神经变性，肌萎缩性侧索硬化等运动神经元疾病，继发于神经变性原发性脱髓鞘疾病等。

4. 发明授权

US07429560B2 Ketoamide inhibitors in chronic nerve disease 失效
标题翻译：酮酰胺抑制剂在慢性神经疾病中的应用
公开(公告)号：US07429560B2
公开(公告)日：2008-09-30
申请号：US10671360
申请日：2003-09-25
申请人： James C. Powers , Jonathan D. Glass
发明人： James C. Powers , Jonathan D. Glass
IPC分类号： A61K38/05
CPC分类号： A61K45/06 , A61K38/04 , A61K2300/00
摘要： Compositions and methods for treating neural pathologies are provided. In particular, compositions and methods for treating neural pathologies including axonal degeneration are provided. The compositions include peptide α-ketomides optionally in combination with a second therapeutic agent. Another aspect of the invention provides compositions and methods for treating hyperproliferative disorders. Exemplary compositions for treating hyperproliferative disorders include an anti-proliferative agent such as paclitaxel, in combination with a calpain inhibitor such as AK295.
摘要翻译：提供了治疗神经病变的组合物和方法。特别地，提供了用于治疗包括轴索变性的神经病变的组合物和方法。组合物包括任选与第二治疗剂组合的肽α-酮基转移酶。本发明的另一方面提供了用于治疗过度增殖性疾病的组合物和方法。用于治疗过度增殖性疾病的示例性组合物包括与钙蛋白酶抑制剂如AK295组合的抗增殖剂如紫杉醇。

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