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11. 发明授权

US11065247B2 Compositions and methods for the treatment of Zellweger spectrum disorder 有权
公开(公告)号：US11065247B2
公开(公告)日：2021-07-20
申请号：US16417167
申请日：2019-05-20
申请人： Joseph Hacia , Nancy E. Braverman , Patricia Dranchak , James Inglese
发明人： Joseph Hacia , Nancy E. Braverman , Patricia Dranchak , James Inglese
IPC分类号： A61K31/485 , C12Q1/6883
摘要： Provided herein are methods of treating Zellweger spectrum disorder (ZSD) in a subject in need thereof or improving peroxisome assembly in a cell in need thereof comprising administering to the subject a therapeutically effective amount of Compounds of Formula I or II.

12. 发明申请

US20110195958A1 ACTIVATORS OF HUMAN PYRUVATE KINASE 有权
标题翻译：人类激素激酶的激活剂
公开(公告)号：US20110195958A1
公开(公告)日：2011-08-11
申请号：US13123297
申请日：2009-10-09
申请人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
发明人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
IPC分类号： A61K31/55 , A61K31/5025 , A61K31/497 , C07D487/14 , C07D405/12 , C07D405/14 , A61P35/02 , A61P35/00
CPC分类号： A61K31/496 , A61K31/445 , A61K31/495 , A61K31/5025 , C07D295/26 , C07D319/18 , C07D495/14
摘要： Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.
摘要翻译：公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基和哌啶基化合物，2,4-二取代的4H-噻吩并[3,2-c]吡咯-2-（取代的苄基）哒嗪-3（2H）（III）的式（II）和6-（3,4-二甲基苯基氨基磺酰基）-3,4-二氢-1H-喹啉-2-酮的酮，其中L，R1，R2，R11至R16，R21和 R22如本文所定义，其可用于治疗可通过PKM2的激活治疗的许多疾病，例如癌症和贫血。

13. 发明授权

US06406869B1 Fluorescent capture assay for kinase activity employing anti-phosphotyrosine antibodies as capture and detection agents 失效
标题翻译：使用抗磷酸酪氨酸抗体作为捕获和检测剂的激酶活性的荧光捕获测定
公开(公告)号：US06406869B1
公开(公告)日：2002-06-18
申请号：US09425549
申请日：1999-10-22
申请人： J. Fraser Glickman , James Inglese , Bassam Damaj
发明人： J. Fraser Glickman , James Inglese , Bassam Damaj
IPC分类号： G01N33543
CPC分类号： G01N33/573 , C12Q1/48 , G01N2333/91235
摘要： A method for determining the level of tyrosine kinase activity in a biological sample is disclosed. The method employs an anti-phosphotyrosine antibody as both the capture agent and the detecting agent. The detecting antibody is labeled with a lanthanide ion, such as europium, as the signal generating entity. The method is particularly well suited to high throughput screening, for example, for compounds which modulate tyrosine kinase activity.
摘要翻译：公开了确定生物样品中酪氨酸激酶活性水平的方法。该方法采用抗磷酸酪氨酸抗体作为捕获剂和检测剂。检测抗体用镧系离子如铕标记，作为信号发生实体。该方法特别适用于高通量筛选，例如调节酪氨酸激酶活性的化合物。

14. 发明申请

US20210315885A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF ZELLWEGER SPECTRUM DISORDER 有权
公开(公告)号：US20210315885A1
公开(公告)日：2021-10-14
申请号：US17351826
申请日：2021-06-18
申请人： Joseph Hacia , Nancy E. Braverman , Patricia Dranchak , James Inglese
发明人： Joseph Hacia , Nancy E. Braverman , Patricia Dranchak , James Inglese
IPC分类号： A61K31/485 , C12Q1/6883
摘要： Provided herein are methods of treating Zellweger spectrum disorder (ZSD) in a subject in need thereof or improving peroxisome assembly in a cell in need thereof comprising administering to the subject a therapeutically effective amount of Compounds of Formula I or II.

15. 发明申请

US20050164311A1 Biological assay detection method 审中-公开
标题翻译：生物检测方法
公开(公告)号：US20050164311A1
公开(公告)日：2005-07-28
申请号：US10484859
申请日：2002-08-02
申请人： James Inglese , Marc Ferrer , Aaron Hamilton
发明人： James Inglese , Marc Ferrer , Aaron Hamilton
IPC分类号： G01N33/531 , C07K5/10 , C07K7/06 , C07K7/08 , C12Q1/34 , C12Q1/37 , C12Q1/42 , C12Q1/48 , C12Q1/527 , G01N33/53 , G01N33/542 , G01N33/573
CPC分类号： G01N33/573 , G01N33/542
摘要： The invention is a method for detecting a reaction product which signals the presence of a reaction product inducer such as an enzyme. The method enables the recognition of epitopes that form the basis of a detection strategy without the need for specific antibodies to the epitope. In the method, a directly or indirectly labeled modular domain and a biotinylated form of the cognate peptide ligand are used as the basis for a measurable interaction. The peptide ligand can be masked by modifications through, for example, phosphorylation of the Ser or Thr residue, or extension of the amino acid sequence beyond the C-terminal Val. Because the masked residues are critical to binding of the labeled modular domain, masking of at least one of the residues prevents binding. Upon treatment of the masked residue by the appropriate enzyme, (e.g., treatment of the phosphorylated residue with a phosphatase enzyme, or treatment of the extended residue with a protease enzyme, the peptide is converted to the original unmasked ligand that is capable of binding to the labeled modular domain and forming a measurable complex.
摘要翻译：本发明是检测反应产物诱导剂如酶的信号的反应产物的方法。该方法能够识别构成检测策略基础的表位，而不需要针对表位的特异性抗体。在该方法中，使用直接或间接标记的模块结构域和生物素化形式的同源肽配体作为可测量相互作用的基础。可以通过例如Ser或Thr残基的磷酸化或氨基酸序列延伸超过C末端Val的修饰来掩蔽肽配体。因为掩蔽的残基对于标记的模块结构域的结合至关重要，所以至少一个残基的掩蔽防止结合。在通过适当的酶处理掩蔽的残留物（例如用磷酸酶处理磷酸化残基或用蛋白酶处理延长的残基时），将肽转化为能够结合到标记的模块化领域并形成可衡量的复杂。

16. 发明授权

US06806056B2 Fluorescent capture assay for kinase activity employing an anti-phosphotyrosine antibody as both the capture agent and detecting agent 失效
标题翻译：使用抗磷酸酪氨酸抗体作为捕获剂和检测剂的荧光捕获测定激酶活性
公开(公告)号：US06806056B2
公开(公告)日：2004-10-19
申请号：US10125784
申请日：2002-04-18
申请人： J. Fraser Glickman , James Inglese , Bassam Damaj , Maria L. Webb , Jonathan J. Burbaum
发明人： J. Fraser Glickman , James Inglese , Bassam Damaj , Maria L. Webb , Jonathan J. Burbaum
IPC分类号： G01N33567
CPC分类号： G01N33/573 , C12Q1/48 , G01N2333/91235
摘要： A method for determining the level of tyrosine kinase activity in a biological sample is disclosed. The method employs an anti-phosphotyrosine antibody as both the capture agent and the detecting agent. The detecting antibody is labeled with a fluorescent label, for instance, Cy5, Cy5.5 or Cy7 or a lanthanide ion, such as europium, as the signal generating entity. The method is particularly well suited to high throughput screening, for example, for compounds which modulate tyrosine kinase activity.
摘要翻译：公开了确定生物样品中酪氨酸激酶活性水平的方法。该方法采用抗磷酸酪氨酸抗体作为捕获剂和检测剂。检测抗体用荧光标记（例如Cy5，Cy5.5或Cy7）或镧系元素离子如铕标记，作为信号发生实体。该方法特别适用于高通量筛选，例如调节酪氨酸激酶活性的化合物。

17. 发明授权

US06335176B1 Incorporation of phosphorylation sites 失效
标题翻译：掺入磷酸化位点
公开(公告)号：US06335176B1
公开(公告)日：2002-01-01
申请号：US09174216
申请日：1998-10-16
申请人： James Inglese , Joseph Fraser Glickman
发明人： James Inglese , Joseph Fraser Glickman
IPC分类号： C07K1113
CPC分类号： C07K7/06 , C07K1/1072 , C07K1/113
摘要： A reagent is described for incorporating phosphorylation sites into compounds, particularly into proteins and peptides. The reagent has the structure A—B—C wherein A is a moiety that is specifically reactive with a reactive side chain in the compound, B is a linking moiety, and C is a peptide sequence that contains a kinase substrate.
摘要翻译：描述了将磷酸化位点掺入化合物，特别是蛋白质和肽中的试剂。试剂具有其中A是与化合物中的反应性侧链特异性反应的部分的结构，B是连接部分，C是含有激酶底物的肽序列。

18. 发明授权

US5876946A High-throughput assay 失效
标题翻译：高通量测定
公开(公告)号：US5876946A
公开(公告)日：1999-03-02
申请号：US868280
申请日：1997-06-03
申请人： Jonathan J. Burbaum , Thomas D.Y. Chung , Gregory L. Kirk , James Inglese , Daniel Chelsky
发明人： Jonathan J. Burbaum , Thomas D.Y. Chung , Gregory L. Kirk , James Inglese , Daniel Chelsky
IPC分类号： G01N33/50 , C12Q1/25 , C40B30/04 , G01N33/15 , G01N33/543 , G01N33/68 , G01N33/53
CPC分类号： C40B30/04 , C12Q1/25 , G01N33/54313 , G01N33/6845 , G01N33/6869 , G01N2500/00
摘要： A homogeneous high throughput assay is described which screens compounds for enzyme inhibition, or receptor or other target binding. Inhibition (or binding) by the library compounds causes a change in the amount of an optically detectable label that is bound to suspendable cells or solid supports. The amounts of label bound to individual cells or solid supports are microscopically determined, and compared with the amount of label that is not bound to individual cells or solid supports. The degree of inhibition or binding is determined using this data. Confocal microscopy, and subsequent data analysis, allow the assay to be carried out without any separation step, and provide for high throughput screening of very small assay volumes using very small amounts of test compound.
摘要翻译：描述了筛选用于酶抑制的化合物或受体或其它靶结合的均匀高通量测定。由文库化合物的抑制（或结合）导致与可悬浮细胞或固体支持物结合的光学可检测标记物的量的变化。显微镜测定与单个细胞或固体支持物结合的标记物的量，并与不与单个细胞或固体支持物结合的标记物的量进行比较。使用该数据确定抑制或结合的程度。共聚焦显微镜和随后的数据分析允许在没有任何分离步骤的情况下进行测定，并且使用非常少量的测试化合物提供非常小的测定体积的高通量筛选。

19. 发明授权

US08841305B2 Activators of the human pyruvate kinase M2 receptor 有权
标题翻译：人类丙酮酸激酶M2受体的活化剂
公开(公告)号：US08841305B2
公开(公告)日：2014-09-23
申请号：US13123297
申请日：2009-10-09
申请人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
发明人： Craig J. Thomas , Douglas S. Auld , James Inglese , Amanda P. Skoumbourdis , Jian-Kang Jiang , Matthew B. Boxer
IPC分类号： C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D401/12 , A61K31/4965 , A61K31/497 , A61P33/00
CPC分类号： A61K31/496 , A61K31/445 , A61K31/495 , A61K31/5025 , C07D295/26 , C07D319/18 , C07D495/14
摘要： Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.
摘要翻译：公开了丙酮酸激酶M2活化剂，其为式（I）的双磺酰胺哌嗪基和哌啶基化合物，2,4-二取代的4H-噻吩并[3,2-c]吡咯-2-（取代的苄基）哒嗪-3（2H）（III）的式（II）和6-（3,4-二甲基苯基氨基磺酰基）-3,4-二氢-1H-喹啉-2-酮的酮，其中L，R1，R2，R11至R16，R21和 R22如本文所定义，其可用于治疗可通过PKM2的激活治疗的许多疾病，例如癌症和贫血。

20. 发明申请

US20050277642A1 Pyrimidine kinase inhibitors 审中-公开
标题翻译：嘧啶激酶抑制剂
公开(公告)号：US20050277642A1
公开(公告)日：2005-12-15
申请号：US11198968
申请日：2005-08-08
申请人： Shawn Erickson , James Inglese , Jeffrey Letourneau , Christopher Riviello
发明人： Shawn Erickson , James Inglese , Jeffrey Letourneau , Christopher Riviello
IPC分类号： C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D521/00 , A61K31/53 , A61K31/506 , C07D43/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14
摘要： Compounds that selectively inhibit inappropriate kinase activities and methods for their preparation are disclosed. In one embodiment, the compounds are represented by Formula I, As selective inhibitors of inappropriate kinase activities, the compounds of the present invention are useful in the treatment of conditions associated with such activity, including, but not limited to, inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting inappropriate kinase activities and methods of treating conditions associated with such activities.
摘要翻译：公开了选择性抑制不适当激酶活性的化合物及其制备方法。在一个实施方案中，化合物由式I代替，作为不适当激酶活性的选择性抑制剂，本发明的化合物可用于治疗与此类活性相关的病症，包括但不限于炎性和自身免疫应答，糖尿病，哮喘，牛皮癣，炎症性肠病，移植排斥反应和肿瘤转移。还公开了抑制不适当的激酶活性的方法和治疗与这些活性相关的病症的方法。

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