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公开(公告)号：US20120083469A1
公开(公告)日：2012-04-05
申请号：US13090714
申请日：2011-04-20
申请人： Michael Van Zandt , Adam Golebiowski , Min Koo Ji , Darren Whitehouse , Todd Ryder , Paul Beckett
发明人： Michael Van Zandt , Adam Golebiowski , Min Koo Ji , Darren Whitehouse , Todd Ryder , Paul Beckett
IPC分类号： A61K31/69 , A61P9/00 , A61P1/00 , A61P37/00 , A61P31/00 , A61P11/00 , A61P9/12 , A61P9/10 , A61P19/02 , A61P21/04 , A61P25/00 , A61P31/18 , A61P1/04 , A61P17/06 , A61P29/00 , A61P17/02 , A61P15/00 , C12N9/99 , C07F5/02
CPC分类号： C07F5/025
摘要： Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.
摘要翻译： 根据式I和式II的化合物是精氨酸酶I和II活性的有效抑制剂：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，D，M，X和Y定义如上 在规范中。 本发明还提供了化合物的药物组合物及其用于治疗或预防与精氨酸酶活性相关的疾病或病症的方法。
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公开(公告)号：US20090082392A1
公开(公告)日：2009-03-26
申请号：US12103082
申请日：2008-04-15
IPC分类号： A61K31/343 , C07D307/80 , C07D307/91 , A61K31/437 , A61P3/10 , A61K31/404 , A61K31/215
CPC分类号： C07D263/57 , C07C69/736 , C07D209/08 , C07D277/66 , C07D307/80 , C07D307/91 , C07D307/92 , C07D405/10 , C07D417/04 , C07D471/04
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.
摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。 这些化合物包括可用于治疗糖尿病和其它PTP-1B介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶（PTP-1B）的抑制剂。 本发明的化合物也可用于治疗上述病症的药物组合物和方法。
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公开(公告)号：US09040703B2
公开(公告)日：2015-05-26
申请号：US13090714
申请日：2011-04-20
申请人： Michael Van Zandt , Adam Golebiowski , Min Koo Ji , Darren Whitehouse , Todd Ryder , Paul Beckett
发明人： Michael Van Zandt , Adam Golebiowski , Min Koo Ji , Darren Whitehouse , Todd Ryder , Paul Beckett
IPC分类号： C07F5/02 , A61K31/69 , A61P9/00 , A61P1/00 , A61P37/00 , A61P31/00 , A61P11/00 , A61P9/12 , A61P9/10 , A61P19/02 , A61P21/04 , A61P25/00 , A61P31/18 , A61P1/04 , A61P17/06 , A61P29/00 , A61P17/02 , A61P15/00 , C12N9/99
CPC分类号： C07F5/025
摘要： Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: where R1, R2, R3, R4, R5, R6, R7, R8, R9, D, M, X, and Y are defined as set forth in the specification. The invention also provides pharmaceutical compositions of the compounds and methods of their use for treating or preventing a disease or a condition associated with arginase activity.
摘要翻译： 根据式I和式II的化合物是精氨酸酶I和II活性的有效抑制剂：其中R1，R2，R3，R4，R5，R6，R7，R8，R9，D，M，X和Y定义如上 在规范中。 本发明还提供了化合物的药物组合物及其用于治疗或预防与精氨酸酶活性相关的疾病或病症的方法。
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公开(公告)号：US20070078135A1
公开(公告)日：2007-04-05
申请号：US11406532
申请日：2006-04-18
申请人： Jun Yuan , Qin Guo , He Zhao , Shaojing Hu , Darren Whitehouse , Wallace Pringle , Jianmin Mao , George Maynard , Jack Hammer , David Wustrow , Hongbin Li
发明人： Jun Yuan , Qin Guo , He Zhao , Shaojing Hu , Darren Whitehouse , Wallace Pringle , Jianmin Mao , George Maynard , Jack Hammer , David Wustrow , Hongbin Li
IPC分类号： A61K31/53 , A61K31/497 , A61K31/4965 , C07D403/02
CPC分类号： C07D403/14 , C07D213/28 , C07D213/61 , C07D213/74 , C07D239/42 , C07D239/54 , C07D241/12 , C07D241/20 , C07D241/24 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds of Formula I are provided. In which the variables are as described herein. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies and various in vitro assays.
摘要翻译： 提供式I化合物。 其中变量如本文所述。 这种化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人类，家养伴侣动物和家畜中的CB1调节有反应的病症，包括食欲障碍，肥胖症和成瘾性疾病。 还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究和各种体外测定的方法。
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公开(公告)号：US07465825B2
公开(公告)日：2008-12-16
申请号：US11283437
申请日：2005-11-18
IPC分类号： C07C229/00 , C07D333/00 , C07D307/91 , A01N43/12 , A01N43/08
CPC分类号： C07D307/79 , C07C271/22 , C07C311/29 , C07C317/14 , C07C317/32 , C07C323/52 , C07C323/65 , C07C2603/74 , C07D307/91
摘要： Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译： 公开了式（A）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗，瘦素抗性或高血糖相关的代谢紊乱。 本发明的化合物包括可用于治疗糖尿病和其它PTP介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶抑制剂，特别是蛋白质酪氨酸磷酸酶-1B（PTP-1B）。 还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。
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公开(公告)号：US07329680B2
公开(公告)日：2008-02-12
申请号：US10835818
申请日：2004-04-30
IPC分类号： C07D277/38 , A61K31/425
CPC分类号： C07D401/14 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D417/10 , C07D417/12
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗，瘦素抵抗或高血糖相关的代谢紊乱。 本发明的化合物包括可用于治疗糖尿病和其它PTP介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶抑制剂，特别是蛋白质酪氨酸磷酸酶-1B（PTP-1B）。 还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。
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公开(公告)号：US07358364B2
公开(公告)日：2008-04-15
申请号：US10823842
申请日：2004-04-14
IPC分类号： C07D471/00 , C07D498/00 , C07D513/00 , C07D405/00 , C07D307/87
CPC分类号： C07D263/57 , C07C69/736 , C07D209/08 , C07D277/66 , C07D307/80 , C07D307/91 , C07D307/92 , C07D405/10 , C07D417/04 , C07D471/04
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.
摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。 这些化合物包括可用于治疗糖尿病和其它PTP-1B介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶（PTP-1B）的抑制剂。 本发明的化合物也可用于治疗上述病症的药物组合物和方法。
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公开(公告)号：US07524878B2
公开(公告)日：2009-04-28
申请号：US10835924
申请日：2004-04-30
IPC分类号： A61K31/341 , A61K31/404 , C07D209/04 , C07D307/79
CPC分类号： C07D307/79 , C07C311/19 , C07C311/29 , C07D209/08 , C07D307/80 , C07D307/81 , C07D307/91 , C07D401/04
摘要： Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译： 公开了式（A）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗，瘦素抗性或高血糖相关的代谢紊乱。 本发明的化合物包括可用于治疗糖尿病和其它PTP介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶抑制剂，特别是蛋白质酪氨酸磷酸酶-1B（PTP-1B）。 还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。
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公开(公告)号：US20080146574A1
公开(公告)日：2008-06-19
申请号：US12029708
申请日：2008-02-12
IPC分类号： A61K31/53 , A61K31/497 , C07D403/14 , C07D405/10 , C07D239/24 , A61P3/10
CPC分类号： C07D401/14 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D417/10 , C07D417/12
摘要： The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia.Compounds of the invention include inhibitors of Protein tyrosine phosphatases, in particular Protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
摘要翻译： 本发明涉及式（I）的化合物和药学上可接受的盐：其可用于治疗与胰岛素抵抗，瘦素抵抗或高血糖相关的代谢紊乱。 本发明的化合物包括可用于治疗糖尿病和其它PTP介导的疾病如癌症，神经变性疾病等的蛋白质酪氨酸磷酸酶抑制剂，特别是蛋白质酪氨酸磷酸酶-1B（PTP-1B）。 还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。
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公开(公告)号：US20050069522A1
公开(公告)日：2005-03-31
申请号：US10637156
申请日：2003-08-08
申请人： Richard Colonno , Julie Lemm , Donald O'Boyle , Min Gao , Jeffrey Romine , Scott Martin , Lawrence Snyder , Michael Serrano-Wu , Milind Deshpande , Darren Whitehouse
发明人： Richard Colonno , Julie Lemm , Donald O'Boyle , Min Gao , Jeffrey Romine , Scott Martin , Lawrence Snyder , Michael Serrano-Wu , Milind Deshpande , Darren Whitehouse
IPC分类号： A61K31/00 , A61K31/426 , A61K38/20 , A61K38/21 , A61K45/06 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04 , A61K48/00
CPC分类号： C07D417/04 , A61K31/00 , A61K31/426 , A61K38/2013 , A61K38/204 , A61K38/208 , A61K38/21 , A61K38/212 , A61K45/06 , C07D277/42 , C07D417/06 , C07D417/12 , C07D417/14 , C07D513/04 , A61K2300/00
摘要： Disclosed are combination pharmaceutical agents for the treatment of an HCV infection comprising a compound effective to inhibit the function of the HCV NS5A protein and another compound having anti-HCV activity. Compounds which can inhibit the function of the NS5A protein having the structure of formula I are described wherein R, R′, R1, R2, and R3 are as defined in the specification. The other compounds having anti-HCV activity are effective to inhibit the function of a target selected from the group consisting of HCV metalloprotease, HCV serine protease, HCV polymerase, HCV helicase, HCV NS4B protein, HCV entry, HCV assembly, HCV egress, HCV NS5A protein, IMPDH and a nucleoside analog for the treatment of an HCV infection.
摘要翻译： 公开了用于治疗HCV感染的组合药剂，其包含有效抑制HCV NS5A蛋白的功能的化合物和另一种具有抗HCV活性的化合物。 描述了可以抑制具有式I结构的NS5A蛋白的功能的化合物，其中R，R'，R 1，R 2和R 3如说明书中所定义。 具有抗HCV活性的其它化合物可有效抑制选自HCV金属蛋白酶，HCV丝氨酸蛋白酶，HCV聚合酶，HCV解旋酶，HCV NS4B蛋白，HCV进入，HCV组装，HCV出血，HCV NS5A蛋白，IMPDH和用于治疗HCV感染的核苷类似物。
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