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61.发明申请公开(公告)号：US20110112062A1
公开(公告)日：2011-05-12
申请号：US12988374
申请日：2009-04-21
IPC分类号： A61K31/397 , C07D205/04 , C07D207/50 , C07D211/56 , C07D487/04 , C07D239/42 , C07D239/84 , C07D403/12 , A61K31/4025 , A61K31/454 , A61K31/506 , A61K31/517 , A61K31/501 , A61K31/407 , A61P43/00
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, II, III, IHa, NIb, IV, IVa, IVb, IVc, IVd, IVe, V, Va, Vb1 V1, V1a, VIb, VII, Vi1a, VIIb, VIII, V111a, VIIIb, IX, IXa, X, and Xa, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-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，II，III，IIIa，NIb，IV，IVa，IVb，IVc，IVd，IVe，V，Va，Vb1 V1，V1a，VIb，VII，Vi1a，VIIb， V111a，VIIIb，IX，IXa，X和Xa，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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62.发明授权公开(公告)号：US08399504B2
公开(公告)日：2013-03-19
申请号：US12988374
申请日：2009-04-21
IPC分类号： A61K31/40
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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63.发明申请CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权11BETA-羟基脱氢酶脱氢酶的碳酸盐和尿素抑制剂1公开(公告)号：US20130244994A1
公开(公告)日：2013-09-19
申请号：US13769256
申请日：2013-02-15
IPC分类号： C07D487/08 , C07D403/12 , C07D211/56 , C07D205/04 , C07D207/14
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： 本发明涉及其可药用盐的式（I）的新化合物及其药物组合物，其可用于治疗与哺乳动物中的11beta-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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64.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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65.发明申请CYCLIC UREA AND CARBAMATE INHIBITORS OF 11 BETA-HYDROXYSTEROID DEHYDROGENASE 1 有权11个羟基脱氢酶脱氢酶的环状尿素和碳酸氢盐抑制剂公开(公告)号：US20100197675A1
公开(公告)日：2010-08-05
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： A61K31/535 , C07D263/20 , C07D265/10 , C07D233/32 , A61K31/421 , A61K31/4166 , A61P3/04
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 11 β-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：US08383629B2
公开(公告)日：2013-02-26
申请号：US12919370
申请日：2009-02-26
申请人： David A. Claremon , Colin M. Tice , Yuanjie Ye , Suresh B. Singh , Wei He , Wei Zhao , Robert D. Simpson
发明人： David A. Claremon , Colin M. Tice , Yuanjie Ye , Suresh B. Singh , Wei He , Wei Zhao , Robert D. Simpson
IPC分类号： A61K31/497 , A61K31/44 , C07D241/04 , C07D401/04
CPC分类号： C07D471/10 , C07D221/20
摘要： This invention relates to novel compounds of the Formulae I or II and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD 1 in mammals. Formula (I).
摘要翻译： 本发明涉及式I或II的新化合物及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。 式（I）。
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公开(公告)号：US20110136821A1
公开(公告)日：2011-06-09
申请号：US12919370
申请日：2009-02-26
申请人： David A. Claremon , Colin M. Tice , Yuanjie Ye , Suresh B. Singh , Wei He , Wei Zhao , Robert D. Simpson
发明人： David A. Claremon , Colin M. Tice , Yuanjie Ye , Suresh B. Singh , Wei He , Wei Zhao , Robert D. Simpson
IPC分类号： A61K31/496 , C07D221/20 , A61K31/438 , C07D471/10 , C07D403/14 , A61P3/00 , A61P5/00
CPC分类号： C07D471/10 , C07D221/20
摘要： This invention relates to novel compounds of the Formulae I or II and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 β-HSD 1 in mammals. Formula (I).
摘要翻译： 本发明涉及式I或II的新化合物及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。 式（I）。
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68.发明申请Cycloalkyl Lactame Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1 失效环烷基乳糖衍生物作为11-β-羟基甾体脱氢酶抑制剂1公开(公告)号：US20110071139A1
公开(公告)日：2011-03-24
申请号：US12867374
申请日：2009-02-13
申请人： David A. Claremon , Linghang Zhuang , Yuanjieq Ye , Suresh B. Singh , Colin M. Tice , Robert D. Simpson
发明人： David A. Claremon , Linghang Zhuang , Yuanjieq Ye , Suresh B. Singh , Colin M. Tice , Robert D. Simpson
IPC分类号： A61K31/551 , C07D265/10 , A61K31/535 , A61P3/10 , A61P3/04 , A61P9/12 , A61P5/50 , A61P3/06 , A61P9/10 , A61P25/28 , A61P25/22 , A61P25/24 , A61P31/06 , A61P31/08 , A61P17/06 , A61P19/10 , C07D211/76 , A61K31/451 , C07D243/04
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 Ia1-3-Ij1-3 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 Ia1-3-Ij1-3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11和bd-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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公开(公告)号：US20110105504A1
公开(公告)日：2011-05-05
申请号：US12933027
申请日：2009-03-18
申请人： David A. Claremon , Linghang Zhuang , Yuanjle Ye , Suresh B. Singh , Colin M. Tice , Gerard McGeehan
发明人： David A. Claremon , Linghang Zhuang , Yuanjle Ye , Suresh B. Singh , Colin M. Tice , Gerard McGeehan
IPC分类号： A61K31/5377 , C07D263/10 , C07D263/14 , C07D413/10 , C07D413/04 , A61K31/421 , A61K31/4439 , A61K31/422 , A61K31/433 , A61K31/497 , A61P43/00
CPC分类号： C07D263/22 , C07D233/32 , C07D263/24 , C07D401/04 , C07D403/06 , C07D409/10 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/10
摘要： This invention relates to novel compounds of the Formula (I) and 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.
摘要翻译： 本发明涉及式（I）的新化合物及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。
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70.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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