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公开(公告)号：US06943161B2
公开(公告)日：2005-09-13
申请号：US10186161
申请日：2002-06-28
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 , A61P35/04
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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公开(公告)号：US07037916B2
公开(公告)日：2006-05-02
申请号：US10340398
申请日：2003-01-10
申请人： Shawn David Erickson , John J. Baldwin , Roland Ellwood Dolle, III , James Inglese , Michael H. J. Ohlmeyer , Koc-Kan Ho , Adolph C Bohnstedt , Steven G. Kultgen , Paolo Giovanni Martino Conti , Dirk Leysen , Jaap van der Louw
发明人： Shawn David Erickson , John J. Baldwin , Roland Ellwood Dolle, III , James Inglese , Michael H. J. Ohlmeyer , Koc-Kan Ho , Adolph C Bohnstedt , Steven G. Kultgen , Paolo Giovanni Martino Conti , Dirk Leysen , Jaap van der Louw
IPC分类号： A61K31/52 , C07D413/00 , C07D239/02 , C70D473/00
CPC分类号： C07D239/42 , C07D231/12 , C07D233/56 , C07D239/47 , C07D249/08 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12
摘要： Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed. The compounds are of the formula I In these compounds, Q is preferably unsubstituted and substituted heterocyclyl; U is usually hydrogen or fluorine; and V is preferably hydrogen, halogen, alkyl, —O—alkyl or —S-alkyl. A representative example is:
摘要翻译： 公开了含有嘧啶核的化合物及其用于治疗与不适当的白细胞介素-8受体活性有关的疾病和病症的用途。 化合物具有式I化合物。在这些化合物中，Q优选为未取代的和取代的杂环基; U通常是氢或氟; 且V优选为氢，卤素，烷基，-O-烷基或-S-烷基。 一个代表性的例子是：
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公开(公告)号：US20180000814A1
公开(公告)日：2018-01-04
申请号：US15623333
申请日：2017-06-14
IPC分类号： A61K31/485 , C12Q1/68
CPC分类号： A61K31/485 , C12Q1/6883 , C12Q2600/156
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.
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公开(公告)号：US08937067B2
公开(公告)日：2015-01-20
申请号：US13433656
申请日：2012-03-29
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： A61K31/502 , C07D237/00 , C07D319/18 , C07D295/26 , C07D495/14 , 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 compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 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）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H） 式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，
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5.发明申请COMPOUNDS AND METHODS OF USE THEREOF FOR TREATING NEURODEGENERATIVE DISORDERS 有权用于治疗神经损伤性疾病的化合物及其使用方法公开(公告)号：US20140187540A1
公开(公告)日：2014-07-03
申请号：US13985702
申请日：2012-02-15
申请人： Donald J. Zack , Cynthia Berlinicke , Laszlo Hackler , Zhiyong Yang , Joseph P. Steiner , Tomas Vojkovsky , Dana Ferraris , Barbara S. Slusher , James Inglese
发明人： Donald J. Zack , Cynthia Berlinicke , Laszlo Hackler , Zhiyong Yang , Joseph P. Steiner , Tomas Vojkovsky , Dana Ferraris , Barbara S. Slusher , James Inglese
IPC分类号： C07D403/12 , C07D401/14
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D453/02
摘要： Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
摘要翻译： 公开了用于治疗与神经变性或眼部疾病相关的病症的化合物，组合物，试剂盒和方法。
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公开(公告)号：US20200046693A1
公开(公告)日：2020-02-13
申请号：US16417167
申请日：2019-05-20
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.
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7.发明授权公开(公告)号：US08741259B2
公开(公告)日：2014-06-03
申请号：US13125045
申请日：2008-10-20
申请人： Marvin C. Gershengorn , Susanne Neumann , Bruce M. Raaka , Craig J. Thomas , James Inglese , Noel T. Southall , Steven Titus , Wei Zheng , Wenwei Huang , Gerd Krause , Gunnar Kleinau
发明人： Marvin C. Gershengorn , Susanne Neumann , Bruce M. Raaka , Craig J. Thomas , James Inglese , Noel T. Southall , Steven Titus , Wei Zheng , Wenwei Huang , Gerd Krause , Gunnar Kleinau
IPC分类号： A61K51/00 , C07D239/88 , C07D217/24 , A61K31/47 , A61P35/00 , A61K31/167 , A61K31/517 , C07C233/01
CPC分类号： C07D405/06 , A61K31/517 , A61K49/0004 , A61K51/00 , C07D239/91 , C07D401/06 , C07D405/14 , C07D487/04
摘要： Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
摘要翻译： 公开了可用作选择性TSHR激动剂的氧代 - 氢喹唑啉。 该化合物可用于检测或治疗甲状腺癌或治疗骨退行性疾病。
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公开(公告)号：US20120245141A1
公开(公告)日：2012-09-27
申请号：US13433656
申请日：2012-03-29
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： A61K31/496 , A61K31/495 , C07D243/08 , A61K31/551 , C07D405/12 , A61K31/453 , C07D405/14 , C07D319/18 , A61K31/357 , A61K31/4025 , A61K31/397 , C07D495/14 , A61K31/5025 , C07D215/22 , A61K31/4704 , A61P35/00 , A61P35/02 , C07D295/26
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 compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 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）的双磺酰胺哌嗪基化合物和2,4-二取代的4H-噻吩并[3,2-b]吡咯-2-（取代的苄基）哒嗪-3（2H） 式（II）的化合物，其中L和R 1至R 16如本文所定义，其可用于治疗可通过PKM2的活化治疗的许多疾病，例如癌症和贫血，
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9.发明申请公开(公告)号：US20110195018A1
公开(公告)日：2011-08-11
申请号：US13125045
申请日：2008-10-20
申请人： Marvin C. Gershengorn , Susanne Neumann , Bruce M. Raaka , Craig J. Thomas , James Inglese , Noel T. Southall , Steven Titus , Wei Zheng , Wenwei Huang , Gerd Krause , Gunnar Kleinau
发明人： Marvin C. Gershengorn , Susanne Neumann , Bruce M. Raaka , Craig J. Thomas , James Inglese , Noel T. Southall , Steven Titus , Wei Zheng , Wenwei Huang , Gerd Krause , Gunnar Kleinau
IPC分类号： A61K49/00 , C07D239/88 , C07D217/24 , A61K31/47 , A61P35/00 , A61K31/167 , A61K31/517 , C07C233/01
CPC分类号： C07D405/06 , A61K31/517 , A61K49/0004 , A61K51/00 , C07D239/91 , C07D401/06 , C07D405/14 , C07D487/04
摘要： Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
摘要翻译： 公开了可用作选择性TSHR激动剂的氧代 - 氢喹唑啉。 该化合物可用于检测或治疗甲状腺癌或治疗骨退行性疾病。
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公开(公告)号：US20060270841A1
公开(公告)日：2006-11-30
申请号：US10504446
申请日：2003-02-25
申请人： Amy Espeseth , Marc Ferrer , Osvaldo Flores , Daria Hazuda , James Inglese , Michael Miller , Bruce Register , Xiao-Ping Shi , Adam Simon , Paul Zuck
发明人： Amy Espeseth , Marc Ferrer , Osvaldo Flores , Daria Hazuda , James Inglese , Michael Miller , Bruce Register , Xiao-Ping Shi , Adam Simon , Paul Zuck
CPC分类号： C07K14/47 , C07K14/4702 , C07K14/4711 , C07K2319/00 , C07K2319/50 , G01N2500/10
摘要： The present invention provides DNA constructs, genetically engineered host cells, and methods for identifying inhibitors of amyloid precursor protein (APP) processing. The methods provide for the convenient identification, in a single assay, of inhibitors of β-secretase and γ-secretase as well as other forms of APP processing. The methods rely on fusion proteins of APP and transcription factors in which APP processing releases the transcription factors, allowing the transcription factors to activate transcription of a reporter gene. Inhibitors are identified as substances that block or diminish transcription factor release from the fusion protein, thereby causing a diminution of reporter gene readout.
摘要翻译： 本发明提供了DNA构建体，遗传工程化宿主细胞和用于鉴定淀粉样前体蛋白（APP）处理抑制剂的方法。 该方法提供了在单次测定中方便地鉴定β-分泌酶和γ-分泌酶抑制剂以及其它形式的APP处理。 该方法依赖于APP和转录因子的融合蛋白，其中APP处理释放转录因子，允许转录因子激活报告基因的转录。 抑制剂被鉴定为阻断或减少转录因子从融合蛋白释放的物质，从而导致报告基因读出的减少。
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