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1. 发明授权

US5453414A 2-arylpyrimidines and herbicidal use thereof 失效
标题翻译： 2-芳基嘧啶及其除草用途
公开(公告)号：US5453414A
公开(公告)日：1995-09-26
申请号：US185579
申请日：1994-01-18
申请人： Colin M. Tice , Vincent A. Musco , Renee C. Roemmele , Harlow L. Warner
发明人： Colin M. Tice , Vincent A. Musco , Renee C. Roemmele , Harlow L. Warner
IPC分类号： A01N43/54 , C07D239/36 , C07D239/46 , C07D239/52 , C07D239/56 , C07D239/70 , C07D239/91 , C07D401/04 , C07D405/04 , C07D409/04 , C07D495/04 , C07F7/08 , A01N43/66 , A01N55/10
CPC分类号： C07D239/36 , A01N43/54 , C07D239/47 , C07D239/52 , C07D239/56 , C07D239/70 , C07D239/91 , C07D401/04 , C07D405/04 , C07D409/04 , C07D495/04 , C07F7/0812
摘要： A class of 2-arylpyrimidines which is useful in the control of weeds of the general formula: ##STR1## wherein R.sup.2 is an optionally substituted aromatic ring; R.sup.3 is a saturated or unsaturated alkyl group; R.sup.5 is selected from acyl, alkoxyalkyl, alkoxyimino, dialkoxyalkyl, formyl, hydroxyalkyl, and hydroxyimino; R.sup.6 is selected from hydrogen, halo, alkyl, haloalkyl, aryl, and alkoxy; and X is oxygen or sulfur.
摘要翻译：一类2-芳基嘧啶，其可用于控制下列通式的杂草：其中R 2是任选取代的芳环; R3是饱和或不饱和的烷基; R5选自酰基，烷氧基烷基，烷氧基亚氨基，二烷氧基烷基，甲酰基，羟基烷基和羟基亚氨基; R6选自氢，卤素，烷基，卤代烷基，芳基和烷氧基; X是氧或硫。

2. 发明授权

US5629264A 2-aryl-5,6-dihydropyrimidinones and herbicidal use thereof 失效
标题翻译： 2-芳基-5,6-二氢嘧啶酮及其除草用途
公开(公告)号：US5629264A
公开(公告)日：1997-05-13
申请号：US409293
申请日：1995-03-23
申请人： Colin M. Tice , Lois M. Bryman , Renee C. Roemmele
发明人： Colin M. Tice , Lois M. Bryman , Renee C. Roemmele
IPC分类号： A01N43/54 , C07D239/22 , C07D401/04 , C07D239/06
CPC分类号： C07D239/22 , A01N43/54 , C07D401/04
摘要： A class of 2-aryl-5,6-dihydropyrimidinones and compositions thereof which are useful in the control of weeds is of the general formula ##STR1## wherein Ar is a substituted or unsubstituted aryl or heteroaryl;R.sup.3 is an optionally substituted alkyl, alkenyl or alkynyl;R.sup.5a and R.sup.5b are each independently a hydrogen atom, halo, cyano or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy or alkylthio;R.sup.6a and R.sup.6b are each independently a hydrogen atom, halo, cyano, an optionally substituted alkyl, alkenyl, alkynyl, alkoxy or alkylthioalkyl, cycloalkyl, optionally substituted aryl, aryloxy, heterocyclyl or aralkyl, alkylamino, dialkylamino or dialkylaminocarbonyl;R.sup.5a and R.sup.6a taken together with the carbon atoms to which they are attached may form a fused 4-7 member ring containing 2-5 methylenes; andX is an oxygen or a sulfur atom.
摘要翻译：一类可用于防治杂草的2-芳基-5,6-二氢嘧啶酮及其组合物具有通式“IMAGE”，其中Ar是取代或未取代的芳基或杂芳基; R3是任选取代的烷基，烯基或炔基; R5a和R5b各自独立地为氢原子，卤素，氰基或任意取代的烷基，烯基，炔基，烷氧基或烷硫基; R6a和R6b各自独立地为氢原子，卤素，氰基，任选取代的烷基，烯基，炔基，烷氧基或烷硫基烷基，环烷基，任选取代的芳基，芳氧基，杂环基或芳烷基，烷基氨基，二烷基氨基或二烷基氨基羰基。 R5a和R6a与它们所连接的碳原子一起可以形成含有2-5个亚甲基的稠合4-7元环; X是氧或硫原子。

3. 发明授权

US09802936B2 Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex 有权
公开(公告)号：US09802936B2
公开(公告)日：2017-10-31
申请号：US11869474
申请日：2007-10-09
申请人： Colin M. Tice , Enrique L. Michelotti , Robert E. Hormann
发明人： Colin M. Tice , Enrique L. Michelotti , Robert E. Hormann
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.

4. 发明授权

US08927715B2 Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 有权
标题翻译： 11＆bgr-羟基类固醇脱氢酶抑制剂1型
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。

5. 发明授权

US08883778B2 Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1 有权
标题翻译： 11β-羟基类固醇脱氢酶的循环抑制剂1
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。

6. 发明授权

US08835426B2 Cyclic urea and carbamate inhibitors of 11β-hydroxysteroid dehydrogenase 1 有权
标题翻译：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。

7. 发明授权

US08828985B2 Carbamate and urea inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权
标题翻译： 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
申请人： David A. Claremon , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Linghang Zhuang
发明人： David A. Claremon , Suresh B. Singh , Colin M. Tice , Yuanjie Ye , Linghang Zhuang
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。

8. 发明授权

US08598160B2 Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效
标题翻译：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。

9. 发明授权

US08592409B2 Cyclic carbazate and semicarbazide inhibitors of 11β-hydroxysteroid dehydrogenase 1 失效
标题翻译： 11β-羟类固醇脱氢酶的环状肼基甲酸酯和氨基脲抑制剂1
公开(公告)号：US08592409B2
公开(公告)日：2013-11-26
申请号：US12863634
申请日：2009-01-21
申请人： David A. Claremon , Linghang Zhuang , Yuanjie Ye , Suresh B. Singh , Colin M. Tice , Salvacion Cacatian
发明人： David A. Claremon , Linghang Zhuang , Yuanjie Ye , Suresh B. Singh , Colin M. Tice , Salvacion Cacatian
IPC分类号： C07D265/10 , A61K31/417
CPC分类号： C07D265/10
摘要： This invention relates to novel compounds of the Formula (I), (Ia), (Ic), (Ie), (If), (Ig), (Ih), (Ii), 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），（Ia），（Ic），（Ie），（If），（Ig），（Ih），（Ⅰi），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11beta-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产生或抑制细胞中可的松转化为皮质醇的方法。

10. 发明申请

US20130040389A1 Bioavailable Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex 有权
标题翻译：用于通过蜕皮激素受体复合物调节外源基因表达的生物可利用的二酰基肼配体
公开(公告)号：US20130040389A1
公开(公告)日：2013-02-14
申请号：US13604001
申请日：2012-09-05
申请人： Robert Eugene HORMANN , David W. Potter , Orestes Chortyk , Colin M. Tice , Glenn Richard Carlson , Andrew Meyer , Thomas R. Opie
发明人： Robert Eugene HORMANN , David W. Potter , Orestes Chortyk , Colin M. Tice , Glenn Richard Carlson , Andrew Meyer , Thomas R. Opie
IPC分类号： C07C243/38 , C07D407/12 , C07C317/28 , C07D241/24 , C07D319/14 , C07D235/08 , C07D209/42 , C07D233/90 , C07D231/56 , C07D405/12 , C12N5/00 , C07D213/81
CPC分类号： C07C241/04 , A61K31/166 , A61K31/222 , A61K31/357 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/455 , A61K31/4965 , C07C243/18 , C07C243/24 , C07C243/38 , C07C251/08 , C07C251/38 , C07C255/66 , C07C281/10 , C07C309/59 , C07C315/02 , C07C317/44 , C07C317/46 , C07D209/42 , C07D213/81 , C07D213/82 , C07D213/86 , C07D213/87 , C07D231/14 , C07D231/56 , C07D235/06 , C07D235/24 , C07D237/24 , C07D239/52 , C07D241/24 , C07D271/12 , C07D317/68 , C07D319/08 , C07D319/18 , C07D319/20 , C07D405/12 , C12N9/0069 , C12N15/635 , C12P21/00 , Y02A50/471
摘要： The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and 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.
摘要翻译：本发明涉及用于基于核受体的诱导型基因表达系统的非甾体配体，以及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结合结构域; 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。

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