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1. 发明授权

US07741361B2 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：US07741361B2
公开(公告)日：2010-06-22
申请号：US11305362
申请日：2005-12-16
申请人： Daniel Kuzmich , Darren DiSalvo , John Robinson Regan , David S. Thomson
发明人： Daniel Kuzmich , Darren DiSalvo , John Robinson Regan , David S. Thomson
IPC分类号： A61K31/404 , A61K31/18 , C07D209/04 , C07C307/02
CPC分类号： C07D471/04 , C07D209/08 , C07D209/16 , C07D209/86 , C07D215/06 , C07D215/233 , C07D231/56 , C07D235/14 , C07D307/79 , C07D333/58 , C07D401/04 , C07D403/04 , C07D413/04
摘要： Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 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：其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义的式（I）化合物或其互变异构体，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。

2. 发明申请

US20100152167A1 PYRIMIDINE DERIVATIVES 有权
标题翻译：吡嗪衍生物
公开(公告)号：US20100152167A1
公开(公告)日：2010-06-17
申请号：US12711364
申请日：2010-02-24
申请人： Georg DAHMANN , Frank HIMMELSBACH , Bernd KRIST , Martin LENTER , Alexander PAUTSCH , Gisela SCHNAPP , Martin STEEGMAIER , Helmut WITTNEBEN , Anthony S. PROKOPOWICZ , Walter SPEVAK , Andreas SCHOOP , Steffen STEURER
发明人： Georg DAHMANN , Frank HIMMELSBACH , Bernd KRIST , Martin LENTER , Alexander PAUTSCH , Gisela SCHNAPP , Martin STEEGMAIER , Helmut WITTNEBEN , Anthony S. PROKOPOWICZ , Walter SPEVAK , Andreas SCHOOP , Steffen STEURER
IPC分类号： A61K31/505 , C07D239/50 , C07D413/12 , A61K31/5377 , A61K31/506 , C07D403/04 , A61K31/55 , C07D403/12 , A61K31/551 , A61P31/00 , A61P35/00 , A61P9/00 , A61P19/08
CPC分类号： C07D239/48 , C07D231/12 , C07D233/56 , C07D239/50 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D451/04 , C07D451/06 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： The present invention relates to trisubstituted pyrimidines of formula (I) wherein0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
摘要翻译：本发明涉及式（I）的三取代嘧啶，其中0Ra至Re如权利要求1所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，其用于制备具有上述药物组合物的用途性质及其制备方法。

3. 发明申请

US20100136550A1 Methods and Compounds for the Diagnosis of Inflammatory Disease and Identification of Pharmacological Agents Useful in the Treatment of Inflammatory Disease 审中-公开
标题翻译：用于诊断炎症疾病的方法和化合物以及用于治疗炎性疾病的药理学鉴定
公开(公告)号：US20100136550A1
公开(公告)日：2010-06-03
申请号：US12567251
申请日：2009-09-25
申请人： Jun LI , Xiang John LI , Randall W. BARTON
发明人： Jun LI , Xiang John LI , Randall W. BARTON
IPC分类号： C12Q1/68
CPC分类号： C12Q1/485 , A61K38/00 , G01N33/6893 , G01N2333/9121 , G01N2500/00 , G01N2500/10 , G01N2500/20 , G01N2800/065 , G01N2800/52
摘要： Methods for the diagnosis of inflammatory bowel diseases and the identification of agents useful in the treatment of such diseases based upon the agent's effect on reducing Pim-2 expression.
摘要翻译：用于诊断炎症性肠病的方法以及基于该药对减少Pim-2表达的作用来鉴定可用于治疗这些疾病的药剂。

4. 发明申请

US20090171089A1 1,6 NAPHTHRIDINES USEFUL AS INHIBITORS OF SYK KINASE 有权
标题翻译：作为SYK KINASE的抑制剂有益的1,6萘普生
公开(公告)号：US20090171089A1
公开(公告)日：2009-07-02
申请号：US12399292
申请日：2009-03-06
申请人： Charles L. CYWIN , Scott E. JAKES , Joachim HEIDER , Mark A. BOBKO , Renee L. DES JARLAIS , Mark PLAYER , James RINKER , Michael WINTERS , Bao-ping ZHAO
发明人： Charles L. CYWIN , Scott E. JAKES , Joachim HEIDER , Mark A. BOBKO , Renee L. DES JARLAIS , Mark PLAYER , James RINKER , Michael WINTERS , Bao-ping ZHAO
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
摘要翻译：公开了式（I）的化合物：其中R 3，R 5，R 7和R 8在本文中定义，其可用作抑制剂SYK激酶，因此可用于治疗由不适当的肥大细胞活化引起的疾病，包括过敏性和炎性疾病。还公开了包含这些化合物的药物组合物和制备这些化合物的方法。

5. 发明授权

US07553966B2 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：US07553966B2
公开(公告)日：2009-06-30
申请号：US10944615
申请日：2004-09-17
申请人： Rajashehar Betageri , Thomas A. Gilmore , Christian Hanke Justus Joachim Harcken , Daniel Kuzmich , Hossein Razavi , Doris Riether , David S. Thomson , Ji Wang
发明人： Rajashehar Betageri , Thomas A. Gilmore , Christian Hanke Justus Joachim Harcken , Daniel Kuzmich , Hossein Razavi , Doris Riether , David S. Thomson , Ji Wang
IPC分类号： C07D215/38
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) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or 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（IA）和式（IB）的化合物，其中R1，R2，R3，R4，R5和R6如本文对式（IA）或式（IB）所定义，或其互变异构体，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。

6. 发明授权

US07514458B2 Anti-cytokine heterocyclic compounds 有权
标题翻译：抗细胞因子杂环化合物
公开(公告)号：US07514458B2
公开(公告)日：2009-04-07
申请号：US11668704
申请日：2007-01-30
申请人： Derek Cogan , Ming-Hong Hao , Victor Marc Kamhi , Craig Andrew Miller , Matthew Russell Netherton , Alan David Swinamer
发明人： Derek Cogan , Ming-Hong Hao , Victor Marc Kamhi , Craig Andrew Miller , Matthew Russell Netherton , Alan David Swinamer
IPC分类号： A61K31/4192 , A61K31/429 , A61K31/4025 , A61K31/402
CPC分类号： C07D417/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D513/04
摘要： Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
摘要翻译：公开的抑制细胞因子产生的式（I）化合物，其涉及炎症过程，因此可用于治疗涉及炎症的疾病和病理状态，例如慢性炎性疾病。还公开了制备这些化合物的方法和包含这些化合物的药物组合物。

7. 发明授权

US07462637B2 Derivatives of [6,7-dihydro-5H-imidazo[1,2--a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide 有权
标题翻译： [6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-磺酰基] - 吡咯烷-2-甲酸酰胺的衍生物
公开(公告)号：US07462637B2
公开(公告)日：2008-12-09
申请号：US10969698
申请日：2004-10-20
申请人： Terence A. Kelly , Jin Mi Kim , René Marc Lemieux , Matt Aaron Tschantz
发明人： Terence A. Kelly , Jin Mi Kim , René Marc Lemieux , Matt Aaron Tschantz
IPC分类号： A61K31/4188 , A61K31/5375 , C07D235/02 , C07D403/12
CPC分类号： C07D487/04 , A61K31/4188
摘要： Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
摘要翻译： 6,7-二氢-5H-咪唑并[1,2-a]咪唑-3-磺酰基]吡咯烷-2-甲酸酰胺的衍生物，其对CAM和白血球素蛋白的相互作用具有良好的抑制作用，因此可用于治疗炎症性疾病。

8. 发明授权

US07291733B2 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：US07291733B2
公开(公告)日：2007-11-06
申请号：US10960550
申请日：2004-10-07
申请人： Charles Lawrence Cywin , Roman Wolfgang Fleck , Eugene Richard Hickey , Weimin Liu , Tina Marie Morwick , John Robert Proudfoot , Denice M. Spero
发明人： Charles Lawrence Cywin , Roman Wolfgang Fleck , Eugene Richard Hickey , Weimin Liu , Tina Marie Morwick , John Robert Proudfoot , Denice M. Spero
IPC分类号： C07D491/00 , C07D498/00 , C07D513/00 , C07D515/00
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. 发明授权

US07268152B2 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：US07268152B2
公开(公告)日：2007-09-11
申请号：US10394157
申请日：2003-03-21
申请人： Younes Bekkali , Mario G. Cardozo , Christian Hanke Justus Joachim Harcken , Thomas M. Kirrane , Daniel Kuzmich , John Robert Proudfoot , Hossein Razavi , Hidenori Takahashi , David S. Thomson , Ji Wang , Renee Zindell
发明人： Younes Bekkali , Mario G. Cardozo , Christian Hanke Justus Joachim Harcken , Thomas M. Kirrane , Daniel Kuzmich , John Robert Proudfoot , Hossein Razavi , Hidenori Takahashi , David S. Thomson , Ji Wang , Renee Zindell
IPC分类号： C07D213/57 , A61K31/44
CPC分类号： C07C323/18 , C07C37/055 , C07C39/367 , C07C39/373 , C07C43/23 , C07C45/004 , C07C45/30 , C07C45/44 , C07C45/45 , C07C45/63 , C07C45/673 , C07C45/68 , C07C45/69 , C07C47/575 , C07C49/233 , C07C49/255 , C07C49/577 , C07C49/83 , C07C49/84 , C07C59/56 , C07C65/24 , C07C235/42 , C07C251/48 , C07C255/53 , C07C255/54 , C07C317/22 , C07C2601/02
摘要： Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or 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（IA）和式（IB）的化合物，其中R 1，R 2，R 3，R 4， >，R 5和R 6如本文对式（IA）或式（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。

10. 发明授权

US07256300B2 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：US07256300B2
公开(公告)日：2007-08-14
申请号：US11081063
申请日：2005-03-15
申请人： Thomas Wai-Ho Lee , John Robert Proudfoot
发明人： Thomas Wai-Ho Lee , John Robert Proudfoot
IPC分类号： C07D301/02
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 D′; 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'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。

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