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1. 发明申请

US20050234091A1 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof 审中-公开
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其用途
公开(公告)号：US20050234091A1
公开(公告)日：2005-10-20
申请号：US11072819
申请日：2005-03-04
申请人： John Regan , Thomas Lee , David Thomson , Thomas Kirrane , Daniel Kuzmich , John Proudfoot , Younes Bekkali , Renee Zindell
发明人： John Regan , Thomas Lee , David Thomson , Thomas Kirrane , Daniel Kuzmich , John Proudfoot , Younes Bekkali , Renee Zindell
IPC分类号： A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4375 , A61K31/4741 , A61K31/4743 , A61K31/4745 , C07D471/02 , C07D471/04 , C07D491/02 , C07D491/04 , C07D495/04 , C07D498/02 , C07D498/04 , C07D513/04
CPC分类号： C07D491/04 , C07D471/04 , C07D495/04 , C07D513/04
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：式（I）的化合物，其中R 1，R 2，R 3，R 4，R 4， R 5和R 6如本文对式（IA）和式（IB）所定义，或其互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

2. 发明申请

US20050203128A1 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof 有权
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其用途
公开(公告)号：US20050203128A1
公开(公告)日：2005-09-15
申请号：US11072797
申请日：2005-03-04
申请人： Thomas Kirrane , Daniel Kuzmich , John Proudfoot
发明人： Thomas Kirrane , Daniel Kuzmich , John Proudfoot
IPC分类号： A61K31/405 , A61K31/47 , C07D215/14 , C07D311/58 , C07D405/06 , C07D471/04 , C07D45/02
CPC分类号： C07D471/04 , C07D215/14 , C07D311/58 , C07D405/06
摘要： Compounds of Formula (IA) and Formula (IB) where in R1 stands for the following group (the dashed line indicates the point of attachment) and R2, R3, R4, R5, R6, Y, Z, X1 and X2 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：其中在R 1中的式（IA）和式（IB）的化合物代表下列基团（虚线表示连接点），R 2，R 2， R 4，R 4，R 5，R 6，Y，Z，X 1，O 2，（IA）和式（IB）或其互变异构体，前药，溶剂合物或其盐如本文所定义; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

3. 发明申请

US20060014787A1 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof 审中-公开
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其用途
公开(公告)号：US20060014787A1
公开(公告)日：2006-01-19
申请号：US11223501
申请日：2005-09-09
申请人： Thomas Kirrane , Daniel Kuzmich , John Proudfoot , Hossein Razavi , David Thomson
发明人： Thomas Kirrane , Daniel Kuzmich , John Proudfoot , Hossein Razavi , David Thomson
IPC分类号： A61K31/47 , A61K31/506 , A61K31/4965 , A61K31/428 , A61K31/422 , A61K31/137
CPC分类号： C07D215/18 , C07D209/14 , C07D213/38 , C07D213/61 , C07D215/12 , C07D215/14 , C07D235/14 , C07D401/06 , C07D405/06 , C07D471/04
摘要： A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：式（IA）或式（IB）的化合物，其中R 1，R 2，R 3，R 4， R 5，R 5，R 6，R 7和R 8如本文所定义，或互变异构体，前药，溶剂化物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

4. 发明申请

US20050282881A1 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof 有权
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其用途
公开(公告)号：US20050282881A1
公开(公告)日：2005-12-22
申请号：US11185349
申请日：2005-07-20
申请人： Younes Bekkali , Rajashehar Betageri , Mario Cardozo , Thomas Gilmore , Thomas Kirrane , Daniel Kuzmich , John Proudfoot , Hidenori Takahashi , David Thomson , Renee Zindell
发明人： Younes Bekkali , Rajashehar Betageri , Mario Cardozo , Thomas Gilmore , Thomas Kirrane , Daniel Kuzmich , John Proudfoot , Hidenori Takahashi , David Thomson , Renee Zindell
IPC分类号： A61K31/343 , A61K31/404 , A61K31/405 , A61K31/4184 , A61K31/423 , A61K31/437 , A61K31/44 , A61K31/4402 , A61K31/4439 , A61P1/00 , A61P1/16 , A61P3/04 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P17/00 , A61P19/02 , A61P25/00 , A61P25/04 , A61P27/02 , A61P27/06 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/06 , A61P37/08 , C07C49/255 , C07C49/577 , C07D209/12 , C07D209/30 , C07D213/30 , C07D213/61 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/54 , C07D235/12 , C07D237/08 , C07D239/26 , C07D241/12 , C07D261/18 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/64 , C07D307/80 , C07D333/16 , C07D401/06 , C07D405/06 , C07D471/04 , C07D45/02
CPC分类号： C07D209/12 , C07D213/30 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D235/12 , C07D237/08 , C07D239/26 , C07D241/12 , C07D261/18 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/64 , C07D307/80 , C07D333/16 , C07D401/06 , C07D405/06 , C07D471/04
摘要： Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：其中R 1，R 2，R 3，R 4和R 4的式（IA）化合物式（IA）的定义如本文所定义，或其互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

5. 发明申请

US20050176706A1 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof 有权
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其用途
公开(公告)号：US20050176706A1
公开(公告)日：2005-08-11
申请号：US10947420
申请日：2004-09-22
申请人： Younes Bekkali , Rajashekhar Betageri , Michel Emmanuel , Abdelhakim Hammach , Christian Joachim Harcken , Thomas Kirrane , Daniel Kuzmich , Thomas Lee , Pingrong Liu , Usha Patel , John Proudfoot , Hossein Razavi , Doris Riether , Hidenori Takahashi , David Thomson , Ji Wang , Renee Zindell
发明人： Younes Bekkali , Rajashekhar Betageri , Michel Emmanuel , Abdelhakim Hammach , Christian Joachim Harcken , Thomas Kirrane , Daniel Kuzmich , Thomas Lee , Pingrong Liu , Usha Patel , John Proudfoot , Hossein Razavi , Doris Riether , Hidenori Takahashi , David Thomson , Ji Wang , Renee Zindell
IPC分类号： A61K31/4745 , A61K31/52 , A61K31/5377 , A61P5/44 , A61P5/46 , C07D209/08 , C07D213/75 , C07D237/20 , C07D239/42 , C07D307/79 , C07D319/06 , C07D319/08 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D471/02 , C07D471/04 , C07D487/04 , C07D491/02 , C07D491/04 , C07D495/04 , C07D498/02
CPC分类号： C07D213/75 , A61K31/4745 , A61K31/52 , C07D209/08 , C07D209/12 , C07D213/30 , C07D215/14 , C07D231/12 , C07D231/56 , C07D237/20 , C07D239/42 , C07D307/79 , C07D319/06 , C07D319/08 , C07D333/56 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：式（IA），（IB），（IC）和（ID）的化合物，其中R 1，R 2，R 3， R 4，R 5和R 6分别如式（IA），（IB），（IC）和（ID）或其互变异构体前药，溶剂化物或盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

6. 发明申请

US20060189647A1 Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and thereof 有权
标题翻译：糖皮质激素模拟物，其制备方法，药物组合物及其制备方法
公开(公告)号：US20060189647A1
公开(公告)日：2006-08-24
申请号：US11410408
申请日：2006-04-25
申请人： Younes Bekkali , Rajashehar Betageri , David Thomson , Doris Riether , Christian Hanke Justus Harcken , Daniel Kuzmich , John Proudfoot
发明人： Younes Bekkali , Rajashehar Betageri , David Thomson , Doris Riether , Christian Hanke Justus Harcken , Daniel Kuzmich , John Proudfoot
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D209/12 , C07D213/30 , C07D215/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D235/12 , C07D237/08 , C07D239/26 , C07D241/12 , C07D261/18 , C07D263/32 , C07D263/56 , C07D277/24 , C07D277/64 , C07D307/80 , C07D333/16 , C07D401/06 , C07D405/06 , C07D471/04
摘要： Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：其中R 1，R 2，R 3，R 4和R 4的式（IA）化合物式（IA）的定义如本文所定义，或其互变异构体，前药，溶剂合物或其盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

7. 发明申请

US20050101601A1 Substituted tricyclic heterocycles and their uses 有权
标题翻译：取代的三环杂环及其用途
公开(公告)号：US20050101601A1
公开(公告)日：2005-05-12
申请号：US10960550
申请日：2004-10-07
申请人： Charles Cywin , Roman Fleck , Eugene Hickey , Weimin Liu , Tina Morwick , John Proudfoot , Denice Spero
发明人： Charles Cywin , Roman Fleck , Eugene Hickey , Weimin Liu , Tina Morwick , John Proudfoot , Denice Spero
IPC分类号： A61K31/4365 , A61K31/4375 , A61K31/519 , A61K31/53 , C07D495/14 , A61K31/5377 , C07D498/14
CPC分类号： C07D495/14
摘要： Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds.
摘要翻译：公开了以下所示的式（I），（II）和（III）的取代的三环杂环化合物，其中R 1，R 2，R 3，本文描述了它们作为抗炎剂是有活性的。还公开了使用和制备这些化合物的方法。

8. 发明申请

US20080008720A1 Substituted Tricyclic Heterocycles and their Uses 审中-公开
标题翻译：取代三环杂环及其用途
公开(公告)号：US20080008720A1
公开(公告)日：2008-01-10
申请号：US11836590
申请日：2007-08-09
申请人： Charles Cywin , Roman Fleck , Eugene Hickey , Weimin Liu , Tina Morwick , John Proudfoot , Denice Spero
发明人： Charles Cywin , Roman Fleck , Eugene Hickey , Weimin Liu , Tina Morwick , John Proudfoot , Denice Spero
IPC分类号： A61K31/551 , A61K31/4365 , A61K31/519 , A61P11/08 , A61P19/02 , A61P35/00 , A61P37/08 , C07D471/14 , C07D243/08 , A61P37/00 , A61P29/00 , A61P17/06 , A61K39/00 , A61K31/53
CPC分类号： C07D495/14
摘要： Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds.
摘要翻译：公开了以下所示的式（I），（II）和（III）的取代的三环杂环化合物，其中R 1，R 2，R 3，本文描述了它们作为抗炎剂是有活性的。还公开了使用和制备这些化合物的方法。

9. 发明申请

US20050234250A1 Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 有权
标题翻译：某些三氟甲基取代的醇的立体选择性合成
公开(公告)号：US20050234250A1
公开(公告)日：2005-10-20
申请号：US11081063
申请日：2005-03-15
申请人： Thomas Lee , John Proudfoot
发明人： Thomas Lee , John Proudfoot
IPC分类号： C07D301/02 , C07D303/08 , C07D303/22 , C07D407/06 , C07D33/02
CPC分类号： C07D303/22 , C07D301/02 , C07D303/08 , C07D407/06
摘要： A process for stereoselective synthesis of a compound of Formula (X) or Formula (X′) wherein R1, R2, and R3 are as defined herein, the process comprising: (a) reacting the starting material of formula A with a chiral sulfoxide anion source in a suitable solvent to prepare a compound of formula C or C′; (b) reducing the sulfoxide of formula C or C′ in a suitable solvent to obtain the compound of formula D or D1; and (c) cyclizing the compound of formula D or D′ in a suitable solvent to form the epoxide compound of Formula (X) or Formula (X′), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
摘要翻译：用于立体选择性合成式（X）或式（X'）的化合物的方法，其中R 1，R 2和R 3，所述方法包括：（a）使式A的原料与手性亚砜阴离子源在合适的溶剂中反应以制备式C或C'的化合物; （b）在合适的溶剂中还原式C或C'的亚砜，得到式D或D 1的化合物; 和（c）在合适的溶剂中使式D或D'化合物环化以形成式（X）或式（X'）的环氧化合物或其互变异构体，前药，溶剂合物或盐; 含有这些化合物的药物组合物，以及调节糖皮质激素受体功能的方法和治疗由糖皮质激素受体功能介导的疾病状态或病症的方法，或其特征在于使用这些化合物的患者的炎症，过敏或增殖过程。

10. 发明申请

US20060030608A1 Anti aromatase compounds pharmaceutical compositions and uses thereof 审中-公开
标题翻译：抗芳香酶化合物药物组合物及其用途
公开(公告)号：US20060030608A1
公开(公告)日：2006-02-09
申请号：US11137281
申请日：2005-05-25
申请人： Richard Nelson , Pingrong Liu , John Proudfoot , Doris Riether , Christian Hanke Harcken , David Thomson
发明人： Richard Nelson , Pingrong Liu , John Proudfoot , Doris Riether , Christian Hanke Harcken , David Thomson
IPC分类号： A61K31/424 , A61K31/42 , A61K31/416 , A61K31/4184
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04 , C07D497/04
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating estrogen receptor activity in a cell or patient or treating an estrogen receptor-mediated disorder, particularly breast and other cancers, in a patient in need thereof by administering an effective amount of compound of the invention thereto.
摘要翻译：式（I）的化合物，其中R 1，R 2，R 3，R 4，R 4，（I）和式（IB）或其互变异构体，前药，溶剂合物或其盐如本文所定义，含有这些化合物的药物组合物，以及通过给予有效量的本发明化合物，调节细胞或患者中雌激素受体活性的方法或治疗有需要的患者中的雌激素受体介导的病症，特别是乳腺癌和其它癌症。

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