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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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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。
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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。
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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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5.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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6.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：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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8.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：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：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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