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1.发明授权Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex 有权通过蜕皮激素受体复合物调节外源基因表达的酮配体公开(公告)号：US08129355B2
公开(公告)日：2012-03-06
申请号：US11889988
申请日：2007-08-17
CPC分类号： C07D487/04 , C07C233/31 , C07C233/76 , C07C235/46 , C07C235/48 , C07C235/50 , C07C235/54 , C07C237/32 , C07C271/20 , C07C275/24 , C07C311/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D211/56 , C07D211/58 , C07D309/14 , C07D317/54 , C07D319/18 , C07D321/08 , C07D335/02 , C07F9/36 , C07K14/70567 , C07K14/721 , C12Q1/6897
摘要： This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
摘要翻译： 本发明涉及一种调节外源基因表达的方法，其中蜕皮激素受体复合物包含：DNA结合域; 配体结合域; 反式激活域 并且配体与包含以下的DNA构建体接触：外源基因和应答元件; 其中外源基因处于响应元件的控制之下，并且在配体存在下DNA结合结构域与响应元件的结合导致基因的激活或抑制。 配体包括一类酮。
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2.发明授权公开(公告)号：US09802936B2
公开(公告)日：2017-10-31
申请号：US11869474
申请日：2007-10-09
IPC分类号： C07D487/04 , C07C233/31 , C07C233/76 , C07C235/46 , C07C235/48 , C07C235/50 , C07C235/54 , C07C237/32 , C07C271/20 , C07C275/24 , C07C311/20 , C07D207/14 , C07D211/56 , C07D211/58 , C07D309/14 , C07D317/54 , C07D319/18 , C07D321/08 , C07D335/02 , C07F9/36 , C07K14/705 , C07K14/72 , C12Q1/68
CPC分类号： C07D487/04 , C07C233/31 , C07C233/76 , C07C235/46 , C07C235/48 , C07C235/50 , C07C235/54 , C07C237/32 , C07C271/20 , C07C275/24 , C07C311/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D211/56 , C07D211/58 , C07D309/14 , C07D317/54 , C07D319/18 , C07D321/08 , C07D335/02 , C07F9/36 , C07K14/70567 , C07K14/721 , C12Q1/6897
摘要： This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
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3.发明申请Ketone Ligands for Modulating the Expression of Exogenous Genes Via An Ecdysone Receptor Complex 有权用于通过蜕皮激素受体复合物调节外源基因表达的酮配体公开(公告)号：US20090111183A1
公开(公告)日：2009-04-30
申请号：US11869474
申请日：2007-10-09
IPC分类号： C12N15/06 , C07D319/16 , C07D263/52 , C07D263/08
CPC分类号： C07D487/04 , C07C233/31 , C07C233/76 , C07C235/46 , C07C235/48 , C07C235/50 , C07C235/54 , C07C237/32 , C07C271/20 , C07C275/24 , C07C311/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D211/56 , C07D211/58 , C07D309/14 , C07D317/54 , C07D319/18 , C07D321/08 , C07D335/02 , C07F9/36 , C07K14/70567 , C07K14/721 , C12Q1/6897
摘要： This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
摘要翻译： 本发明涉及一种调节外源基因表达的方法，其中蜕皮激素受体复合物包含：DNA结合域; 配体结合域; 反式激活域 并且配体与包含以下的DNA构建体接触：外源基因和应答元件; 其中外源基因处于响应元件的控制之下，并且在配体存在下DNA结合结构域与响应元件的结合导致基因的激活或抑制。 配体包括一类酮。
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4.发明授权Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex 有权用于通过蜕皮激素受体复合物调节外源基因表达的酮配体公开(公告)号：US07375093B2
公开(公告)日：2008-05-20
申请号：US10614116
申请日：2003-07-03
CPC分类号： C07D487/04 , C07C233/31 , C07C233/76 , C07C235/46 , C07C235/48 , C07C235/50 , C07C235/54 , C07C237/32 , C07C271/20 , C07C275/24 , C07C311/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D211/56 , C07D211/58 , C07D309/14 , C07D317/54 , C07D319/18 , C07D321/08 , C07D335/02 , C07F9/36 , C07K14/70567 , C07K14/721 , C12Q1/6897
摘要： This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
摘要翻译： 本发明涉及一种调节外源基因表达的方法，其中蜕皮激素受体复合物包含：DNA结合域; 配体结合域; 反式激活域 并且配体与包含以下的DNA构建体接触：外源基因和应答元件; 其中外源基因处于响应元件的控制之下，并且在配体存在下DNA结合结构域与响应元件的结合导致基因的激活或抑制。 配体包括一类酮。
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5.发明申请公开(公告)号：US20080125465A1
公开(公告)日：2008-05-29
申请号：US11889988
申请日：2007-08-17
IPC分类号： A61K31/445 , C07D319/16 , C07D263/52 , C07C233/57 , C07D211/56 , A61P43/00 , A61K31/352 , A61K31/423 , A61K31/165
CPC分类号： C07D487/04 , C07C233/31 , C07C233/76 , C07C235/46 , C07C235/48 , C07C235/50 , C07C235/54 , C07C237/32 , C07C271/20 , C07C275/24 , C07C311/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/14 , C07D211/56 , C07D211/58 , C07D309/14 , C07D317/54 , C07D319/18 , C07D321/08 , C07D335/02 , C07F9/36 , C07K14/70567 , C07K14/721 , C12Q1/6897
摘要： This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.
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公开(公告)号：US08927715B2
公开(公告)日：2015-01-06
申请号：US12310457
申请日：2007-08-24
申请人： David A. Claremon , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Salvacion Cacatian , Wei He , Robert Simpson , Zhenrong Xu , Wei Zhao
发明人： David A. Claremon , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Salvacion Cacatian , Wei He , Robert Simpson , Zhenrong Xu , Wei Zhao
IPC分类号： A61K31/5377 , C07D471/10 , A61K31/438 , C07D221/20 , C07D401/10 , A61K31/496 , C07D413/10 , A61P3/00 , A61P9/12 , A61P9/00 , A61P25/22 , A61P25/28 , A61P25/24 , A61P15/08 , C07D211/26 , C07D413/06 , C07D211/22 , C07D491/107 , C07D211/16 , C07D211/34 , C07D401/08 , C07D401/06
CPC分类号： C07D221/20 , C07D211/16 , C07D211/22 , C07D211/26 , C07D211/34 , C07D401/06 , C07D401/08 , C07D413/06 , C07D471/10 , C07D491/107
摘要： This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
摘要翻译： 本发明涉及式（I *）的新化合物，其药学上可接受的盐及其药物组合物，其可用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病的治疗。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇的产生或抑制细胞中可的松转化为皮质醇的方法。
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公开(公告)号：US08883778B2
公开(公告)日：2014-11-11
申请号：US13381123
申请日：2010-06-30
申请人： David A. Claremon , Katerina Leftheris , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Wei Zhao , Linghang Zhuang
发明人： David A. Claremon , Katerina Leftheris , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Wei Zhao , Linghang Zhuang
IPC分类号： C07D413/10 , C07D413/04 , C07D241/04 , A61K31/675 , A61K31/5377 , A61K31/541
CPC分类号： C07D265/10 , C07D413/10
摘要： Disclosed are compounds represented by Formula (I): or pharmaceutically acceptable salts, enantiomers or diastereomers thereof. Also disclosed are pharmaceutical compositions comprising the compounds of Formula (I) or pharmaceutically acceptable salts, enantiomers or diastereomers thereof for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. Values for the variables of Formula (I) are defined herein.
摘要翻译： 公开了由式（I）表示的化合物或其药学上可接受的盐，对映异构体或非对映异构体。 还公开了包含式（I）化合物或其药学上可接受的盐，对映异构体或非对映异构体的药物组合物，用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病的治疗。 式（I）的变量的值在本文中定义。
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8.发明授权Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1 有权环氧尿素和氨基甲酸酯抑制剂11＆bgr-羟基类固醇脱氢酶1公开(公告)号：US08835426B2
公开(公告)日：2014-09-16
申请号：US12449752
申请日：2008-02-26
申请人： David A. Claremon , Gerard McGeehan , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Wei Zhao
发明人： David A. Claremon , Gerard McGeehan , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Wei Zhao
IPC分类号： A61K31/421 , C07D263/22 , C07D263/24 , A61K31/535 , C07D265/10 , C07D233/34 , C07D239/10 , C07D401/10 , C07D267/06 , C07D413/10 , C07D233/32
CPC分类号： C07D263/22 , C07D233/32 , C07D233/34 , C07D239/10 , C07D263/24 , C07D265/10 , C07D267/06 , C07D401/10 , C07D413/10
摘要： This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
摘要翻译： 本发明涉及式（I）的新化合物，其药学上可接受的盐及其药物组合物，其可用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病的治疗。 本发明还涉及式（I）的新型化合物的药物组合物及其用于减少或控制细胞中皮质醇的产生或抑制细胞中可的松转化为皮质醇的方法。
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9.发明授权Carbamate and urea inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权11-β-羟基类固醇脱氢酶的氨基甲酸酯和尿素抑制剂1公开(公告)号：US08828985B2
公开(公告)日：2014-09-09
申请号：US13769256
申请日：2013-02-15
IPC分类号： A61K31/397 , C07C15/20 , C07D205/00
CPC分类号： C07D487/08 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/56 , C07D401/12 , C07D403/12 , C07D417/12 , C07D487/04
摘要： This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
摘要翻译： 本发明涉及式（I）的药学上可接受的盐的新型化合物及其药物组合物，其可用于治疗与哺乳动物中11β-HSD1的调节或抑制相关的疾病的治疗。 本发明还涉及式（I）的新型化合物的药物组合物及其用于减少或控制细胞中皮质醇的产生或抑制细胞中可的松转化为皮质醇的方法。
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10.发明授权Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶1的抑制剂公开(公告)号：US08598160B2
公开(公告)日：2013-12-03
申请号：US12867374
申请日：2009-02-13
申请人： David A. Claremon , Linghang Zhuang , Yuanjie Ye , Suresh B. Singh , Colin M. Tice , Robert D. Simpson
发明人： David A. Claremon , Linghang Zhuang , Yuanjie Ye , Suresh B. Singh , Colin M. Tice , Robert D. Simpson
IPC分类号： C07D211/16 , C07D243/04 , C07D265/10 , A61K31/4402 , A61P3/04
CPC分类号： C07D243/04 , C07D211/76 , C07D265/10
摘要： This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 1a1-3-1j1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
摘要翻译： 本发明涉及式（I）的新型化合物，式I-I26 1a1-3-1j1-3中任一项或其药学上可接受的盐及其药物组合物，其可用于治疗与 调节或抑制哺乳动物中的11beta-HSD1。 本发明进一步涉及新化合物的药物组合物及其用于减少或控制细胞中皮质醇产生或抑制细胞中可的松转化为皮质醇的方法。
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