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1. 发明申请

WO2009015917A2 DIHYDROQUINONE AND DIHYDRONAPHTHRIDINE INHIBITORS OF JNK 审中-公开
标题翻译：二氢喹啉酮和二氢吲哚啉抑制剂
公开(公告)号：WO2009015917A2
公开(公告)日：2009-02-05
申请号：PCT/EP2008/055470
申请日：2008-05-05
申请人： F. HOFFMANN-LA ROCHE AG , ABBOT, Sarah C. , BOICE, Genevieve N. , GONG, Leyi , TAN, Yun-chou
发明人： ABBOT, Sarah C. , BOICE, Genevieve N. , GONG, Leyi , TAN, Yun-chou
CPC分类号： C07D215/48 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D471/04
摘要： Compounds fo Formula (I) are effective modulators of INK: wherein X s CR 11 or N; X2 s CH or N; R 1 and R 2 are each independently H, halo, CN, lower alkyl, or -Y 1 -Y 2 -Y 3 -R 8 , or R 1 and R 2 together form -O(CH 2 )nO-, where n is 1 or 2; Y 1 is -O- -C(O)- -C(O)O- -C(O)NR 9 -, -NR 9 C(O)- -S-, or -SO 2 -; Y 2 is lower alkylene or a bond; Y 3 is -O- -C(O)- -C(O)O-, -C(O)NR 9 -, -NR 9 C(O)- -SO 2 -, or a bond; R 8 is H, lower alkyl, cycloalkyl, heterocycloalkyl, or -NR 9 R 10 , wherein R 8 other than H is optionally substituted with lower alkyl, halo or -OH; R 9 and R 10 are each independently H or lower alkyl; R 3 is OH, lower alkyl, lower alkoxy, or -NR 9 R 10 ; R 4 is lower alkyl, phenyl, heterocyclyl, cycloalkyl, heterocycloalkyl, or heteroaryl, and is optionally substituted with lower alkyl, hydroxy, lower alkoxy, halo, nitro, amino, cyano, or halo-lower alkyl; R 5 and R 6 are each independently H, halo, cyano, lower alkyl, -CF 3 , lower alkoxy, -OCHF 2 , -NO 2 , or -NR 9 R 10 ; R 11 is H, lower alkyl, lower cycloalkyl, or phenyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的化合物是INK的有效调节剂：其中X s CR11或N; X2 s CH或N; R1和R2各自独立地为H，卤素，CN，低级烷基或-Y1-Y2-Y3-R8，或R1和R2一起形成-O（CH 2）n O-，其中n为1或2; Y1是-O-C（O）-C（O）O - （O）NR9-，-NR9C（O）-S-或-SO2-; Y2是低级亚烷基或键; Y 3是-O-C（O）-C（O）O-，-C（O）NR 9 - ，-NR 9 C（O）-SO 2 - 或键; R8是H，低级烷基，环烷基，杂环烷基或-NR9R10，其中除H之外的R8任选地被低级烷基，卤素或-OH取代; R9和R10各自独立地为H或低级烷基; R3是OH，低级烷基，低级烷氧基或-NR9R10; R 4是低级烷基，苯基，杂环基，环烷基，杂环烷基或杂芳基，并且任选被低级烷基，羟基，低级烷氧基，卤素，硝基，氨基，氰基或卤代低级烷基取代。 R 5和R 6各自独立地为H，卤素，氰基，低级烷基，-CF 3，低级烷氧基，-OCHF 2，-NO 2或-NR 9 R 10; R11是H，低级烷基，低级环烷基或苯基; 或其药学上可接受的盐。

2. 发明申请

WO2010046273A3 PYRIMIDINYL PYRIDONE INHIBITORS OF JNK 审中-公开
标题翻译：嘧啶的嘧啶基吡啶酮抑制剂
公开(公告)号：WO2010046273A3
公开(公告)日：2010-09-30
申请号：PCT/EP2009063327
申请日：2009-10-13
申请人： HOFFMANN LA ROCHE , BOICE GENEVIEVE N , GONG LEYI , MCCALEB KRISTEN LYNN , PALMER WYLIE SOLANG
发明人： BOICE GENEVIEVE N , GONG LEYI , MCCALEB KRISTEN LYNN , PALMER WYLIE SOLANG
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00
CPC分类号： C07D471/04
摘要： This application discloses novel pyrimidinyl pyridone derivatives according to Formulae I and II, wherein R1 and R2 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.
摘要翻译：该申请公开了根据式I和II的新型嘧啶基吡啶酮衍生物，其中R 1和R 2如本文所述定义，其抑制JNK。本文公开的化合物可用于调节JNK的活性并治疗与过量的JNK活性相关的疾病。该化合物可用于治疗自身免疫疾病，炎症，代谢疾病和神经疾病以及癌症。还公开了包含式I化合物的组合物和治疗方法，其包括将治疗有效量的式I化合物给予有需要的受试者。

3. 发明申请

WO2010046273A2 PYRIMIDINYL PYRIDONE INHIBITORS OF JNK 审中-公开
标题翻译：吡咯烷酮吡咯烷酮抑制剂
公开(公告)号：WO2010046273A2
公开(公告)日：2010-04-29
申请号：PCT/EP2009/063327
申请日：2009-10-13
申请人： F. HOFFMANN-LA ROCHE AG , BOICE, Genevieve N. , GONG, Leyi , MCCALEB, Kristen Lynn , PALMER, Wylie Solang
发明人： BOICE, Genevieve N. , GONG, Leyi , MCCALEB, Kristen Lynn , PALMER, Wylie Solang
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00
CPC分类号： C07D471/04
摘要： This application discloses novel pyrimidinyl pyridone derivatives according to Formulae I and II, wherein R 1 and R 2 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.
摘要翻译：本申请公开了根据式I和II的新型嘧啶基吡啶酮衍生物，其中R1和R2如本文所述限定，其抑制JNK。本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。这些化合物可用于治疗自身免疫性，炎性，代谢和神经疾病以及癌症。还公开了包含式I化合物和治疗方法的组合物，其包括向有需要的受试者施用治疗有效量的式I化合物。

4. 发明申请

WO2008138920A1 DIHYDROQUINONE AND DIHYDRONAPHTHRIDINE INHIBITORS OF JNK 审中-公开
标题翻译：二氢喹啉酮和二氢吲哚啉抑制剂
公开(公告)号：WO2008138920A1
公开(公告)日：2008-11-20
申请号：PCT/EP2008/055807
申请日：2008-05-13
申请人： F. HOFFMANN-LA ROCHE AG , ABBOT, Sarah C. , BOICE, Genevieve N. , BUETTELMANN, Bernd , GOLDSTEIN, David Michael , GONG, Leyi , HOGG, Joan Heather , IYER, Pravin , MCCALEB, Kristen Lynn , TAN, Yun-chou
发明人： ABBOT, Sarah C. , BOICE, Genevieve N. , BUETTELMANN, Bernd , GOLDSTEIN, David Michael , GONG, Leyi , HOGG, Joan Heather , IYER, Pravin , MCCALEB, Kristen Lynn , TAN, Yun-chou
IPC分类号： C07D215/48 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D471/04 , C07F7/18 , A61K31/4375 , A61K31/4709 , A61K31/47 , A61P37/00 , A61P29/00 , A61P3/00 , A61P25/00
CPC分类号： C07D215/48 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D471/04
摘要： Compounds of formula I or a pharmaceutically acceptable salt thereof are effective modulators of JNK: (formula) wherein X, Y, Z, R 4 , R 5 , R 6 and R 7 are as defined herein.
摘要翻译：式I化合物或其药学上可接受的盐是JNK的有效调节剂：（式）其中X，Y，Z，R 4，R 5，R 5， 6和R 7和R 7如本文所定义。

5. 发明申请

WO2006057904A1 STEREOSELECTIVE PREPARATION OF 4-ARYL PIPERIDINE AMIDES BY ASYMMETRIC HYDROGENATION OF A PROCHIRAL ENAMIDE AND INTERMEDIATES OF THIS PROCESS 审中-公开
标题翻译：通过非对称氢化方法和本方法的中间体对4-亚氨基哌啶类氨基酸的选择性制备
公开(公告)号：WO2006057904A1
公开(公告)日：2006-06-01
申请号：PCT/US2005/041839
申请日：2005-11-18
申请人： MERCK & CO., INC. , BOICE, Genevieve, N. , MCWILLIAMS, J., Christopher , MURRY, Jerry, A. , SAVARIN, Cecile, G.
发明人： BOICE, Genevieve, N. , MCWILLIAMS, J., Christopher , MURRY, Jerry, A. , SAVARIN, Cecile, G.
IPC分类号： C07D211/26
CPC分类号： C07D211/26
摘要： The present invention provides an efficient process for the preparation of enentiomerically enriched 4-aryl piperidine amides of structural formula (IV).
摘要翻译：本发明提供了制备结构式（IV）的致突变富集的4-芳基哌啶酰胺的有效方法。

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