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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：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：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：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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公开(公告)号：US20130109672A1
公开(公告)日：2013-05-02
申请号：US13643594
申请日：2011-04-26
IPC分类号： C07D265/36 , C07D209/12 , C07D223/16 , C07D235/26 , C07D215/227 , C07D209/34
CPC分类号： C07D215/227 , C07D209/12 , C07D209/30 , C07D209/34 , C07D215/36 , C07D223/16 , C07D235/26 , C07D265/36
摘要： Disclosed are pyruvate kinase M2 activators which are compounds of Formula (I), including those of Formula (II), wherein A1, A2, L, R, R1 to R3, X1 to X3, k, n, and m are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer. A1-NR-L-A2 (I).
摘要翻译： 公开了作为式（I）化合物的丙酮酸激酶M2活化剂，包括式（II）的化合物，其中A1，A2，L，R，R1至R3，X1至X3，k，n和m如本文所定义 ，其可用于治疗可通过激活PKM2（例如癌症）治疗的许多疾病。 A1-NR-L-A2（I）。
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公开(公告)号：US20110112079A1
公开(公告)日：2011-05-12
申请号：US12812291
申请日：2009-01-08
申请人： Craig J. Thomas , Menghang Xia , Amanda P. Skoumbourdis , Christopher A. LeClair , Ruili Huang , Martin J. Walsh
发明人： Craig J. Thomas , Menghang Xia , Amanda P. Skoumbourdis , Christopher A. LeClair , Ruili Huang , Martin J. Walsh
IPC分类号： A61K31/542 , C07D487/04 , A61K31/5025 , C12N5/00 , A61P29/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P37/06 , A61P3/10 , A61P25/28 , A61P25/16 , A61P25/24 , C07D513/04
CPC分类号： C07D513/04 , C07D487/04
摘要： The invention related to compounds for formula I useful for inhibiting phosphodiesterase-4.
摘要翻译： 本发明涉及用于抑制磷酸二酯酶-4的式I化合物。
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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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8.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：US09206154B2
公开(公告)日：2015-12-08
申请号：US13579251
申请日：2011-04-08
IPC分类号： C07D401/06 , A61K31/517 , C07D239/91 , C07D405/06
CPC分类号： C07D401/06 , A61K31/517 , C07D239/91 , C07D405/06
摘要： TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.
摘要翻译： TSHR反向激动剂和中枢拮抗剂，可用于治疗格雷夫斯眶前病变，格雷夫斯甲状腺功能亢进症和/或甲状腺癌。
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公开(公告)号：US20110207784A1
公开(公告)日：2011-08-25
申请号：US13057667
申请日：2009-08-13
申请人： Craig J. Thomas , David J. Maloney , Ganesha Rai Bantukallu , Ahmed A. Sayed , Anton Simeonov , David L. Williams
发明人： Craig J. Thomas , David J. Maloney , Ganesha Rai Bantukallu , Ahmed A. Sayed , Anton Simeonov , David L. Williams
IPC分类号： A61K31/4245 , C07D271/08 , C07D413/10 , C07D413/04 , C07D413/14 , A61P33/12
CPC分类号： C07D271/08 , C07D413/04
摘要： The invention provides 1,2,5-oxadiazole-containing compounds of Formula (I), wherein R1, A, and R2 are as defined herein, that are useful in treating schistosomiasis. The invention also provides a composition comprising a pharmaceutically suitable carrier and at least one compound of the invention, and a method of treating schistosomiasis in a mammal.
摘要翻译： 本发明提供了可用于治疗血吸虫病的1,2,5-二恶唑的式（I）化合物，其中R1，A和R2如本文所定义。 本发明还提供包含药学上合适的载体和至少一种本发明化合物的组合物，以及哺乳动物治疗血吸虫病的方法。
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