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1. 发明申请

WO2010120237A1 IMIDAZOLE SUBSTITUTED PYRIMIDINES USEFUL IN THE TREATMENT OF GLYCOGEN SYNTHASE KINASE 3 RELATED DISORDERS SUCH AS ALZHEIMER'S DISEASE 审中-公开
标题翻译：咪达唑替代吡咯啉可用于治疗糖尿病合成酶3相关疾病如阿尔茨海默病
公开(公告)号：WO2010120237A1
公开(公告)日：2010-10-21
申请号：PCT/SE2010/050404
申请日：2010-04-14
申请人： ASTRAZENECA AB , ARVIDSSON, Per, I , BURROWS, Jeremy, Nicholas , YNGVE, Ulrika , TJERNELD, Erica
发明人： ARVIDSSON, Per, I , BURROWS, Jeremy, Nicholas , YNGVE, Ulrika , TJERNELD, Erica
IPC分类号： C07D413/14 , A61K31/5377 , A61P17/14 , A61P25/18 , A61P25/24 , A61P25/28 , A61P27/06 , A61P29/00 , A61P3/10 , A61P35/00
CPC分类号： C07D405/14 , A61K31/5377 , C07D413/14
摘要： The present invention relates to a new compound of formula (I) wherein R 1 is hydrogen or fluoro; R 2 and R 3 are independently selected from hydrogen or methyl; or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, to the use for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as for the method of treatment of said disorders, comprising administering to a mammal, including human in need of such treatment, a therapeutically effective amount of said compound.
摘要翻译：本发明涉及新的式（I）化合物，其中R 1是氢或氟; R2和R3独立地选自氢或甲基; 或其药学上可接受的盐，含有所述化合物的药物制剂，以使用所述活性化合物在治疗中，用于治疗与糖原合酶激酶-3相关病症如阿尔茨海默病相关的病症的用途，以及治疗所述疾病的方法，包括向需要这种治疗的哺乳动物，包括给予治疗有效量的所述化合物施用。

2. 发明申请

WO2009145720A1 ISOINDOLINE DERIVATIVES COMPRISING ADDITIONAL HETEROCYCLIC GROUPS AND THEIR USE IN THE TREATMENT OF PAIN DISORDERS 审中-公开
标题翻译：包含其他杂环组的ISOINDOLINE衍生物及其在治疗疼痛症状中的应用
公开(公告)号：WO2009145720A1
公开(公告)日：2009-12-03
申请号：PCT/SE2009/050617
申请日：2009-05-29
申请人： ASTRAZENECA AB , ARVIDSSON, Per I , BESIDSKI, Yevgeni , CSJERNYIK, Gabor , SANDBERG, Lars
发明人： ARVIDSSON, Per I , BESIDSKI, Yevgeni , CSJERNYIK, Gabor , SANDBERG, Lars
IPC分类号： C07D401/14 , A61K31/4035 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61P25/02 , A61P25/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
CPC分类号： C07D401/14 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/14 , C07D409/12 , C07D409/14
摘要： Compounds of formula I are claimed wherein R 1 is hydrogen; C 1-3 alkyl, optionally substituted by one or more substituents independently selected from hydroxy, C 1-3 alkoxy andfluoro; C 1-3 alkoxy, optionally substituted by one or morefluoro; cyano; hydroxy or halo; m is 1,2 or 3; Het is C 5-6 heteroaryl substituted by 1 or 2 substituents R 2 ; R 2 is C 1-4 alkyl; C 1-4 haloalkyl;C 1-4 haloalkoxy; halo; C 1-4 alkoxy; or C 3-7 cycloalkyloxy, optionally substituted by one or morefluoro; D is C 5-6 heteroaryl; C 3-7 heterocycloalkyl; or C 3-7 cycloalkyl; wherein each D may optionally be substituted by one or more X4; X 4 is halo; or C 1-3 alkyl, optionally substituted by one or morefluoro; C 1-3 alkyl-O-C 1-3 alkyl, optionally substituted by one or morefluoro; C 1-3 alkoxy, optionally substituted by one or morefluoro; cyano; hydroxy; oxo; R 3 0(C=O); or R 4 (C=O); R 3 is C 1-4 alkyl; C 1-4 alkyl-O-C 1-4 alkyl; C 5-6 cycloalkyl; aryl; or aryl-C 1-2 alkyl; R 4 is C 1-4 alkyl; or C 5-6 heteroaryl; L 1 is C 1-4 alkylene; or a bond; and L 2 is C 1-3 alkylene. Compounds of the invention are useful in therapy, such as pain therapy.
摘要翻译：要求的式I化合物，其中R 1是氢; 任选被一个或多个独立地选自羟基，C 1-3烷氧基和氟的取代基取代的C 1-3烷基; 任选被一个或多个氟取代的C 1-3烷氧基; 氰基; 羟基或卤素; m为1,2或3; Het是被1或2个取代基R2取代的C5-6杂芳基; R2是C1-4烷基; C 1-4卤代烷基; C 1-4卤代烷氧基; 光环; C 1-4烷氧基; 或任选被一个或多个氟取代的C 3-7环烷氧基; D是C 5-6杂芳基; C 3-7杂环烷基; 或C 3-7环烷基; 其中每个D可以任选被一个或多个X 4取代; X4是卤素; 或任选被一个或多个氟取代的C 1-3烷基; 任选被一个或多个氟取代的C 1-3烷基-O-C 1-3烷基; 任选被一个或多个氟取代的C 1-3烷氧基; 氰基; 羟基; 氧; R3 0（C = O）; 或R 4（C = O）; R3是C1-4烷基; C 1-4烷基-O-C 1-4烷基; C5-6环烷基; 芳基; 或芳基-C 1-2烷基; R4是C1-4烷基; 或C5-6杂芳基; L1为C1-4亚烷基; 或债券; 并且L 2是C 1-3亚烷基。本发明的化合物可用于治疗，例如疼痛疗法。

3. 发明申请

WO2007040438A3 NOVEL IMIDAZO [4,5 -B] PYRIDINE DERIVATIVES AS INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3 FOR USE IN THE TREATMENT OF DEMENTIA AND NEURODEGENERATIVE DISORDERS 审中-公开
公开(公告)号：WO2007040438A3
公开(公告)日：2007-04-12
申请号：PCT/SE2006/001114
申请日：2006-10-02
申请人： ASTRAZENECA AB , ARVIDSSON, Per I , ARZEL, Erwan , BURROWS, Jeremy , CLAESSON, Martina , RAY, Colin , REIN, Tobias , ROTTICCI, Didier , SÖDERMAN, Peter
发明人： ARVIDSSON, Per I , ARZEL, Erwan , BURROWS, Jeremy , CLAESSON, Martina , RAY, Colin , REIN, Tobias , ROTTICCI, Didier , SÖDERMAN, Peter
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/501 , A61K31/551 , A61P19/08 , A61P25/00 , A61P25/28 , A61P3/10
摘要： The present invention relates to new compounds of formula (I) Wherein X is or Y; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.

4. 发明申请

WO2007040439A1 NEW COMPOUNDS II 审中-公开
标题翻译：新化合物II
公开(公告)号：WO2007040439A1
公开(公告)日：2007-04-12
申请号：PCT/SE2006/001115
申请日：2006-10-02
申请人： ASTRAZENECA AB , ARVIDSSON, Per I , ARZEL, Erwan , BURROWS, Jeremy , GYBÄCK, Helena , REIN, Tobias , ROTTICCI, Didier , SÖDERMAN, Peter
发明人： ARVIDSSON, Per I , ARZEL, Erwan , BURROWS, Jeremy , GYBÄCK, Helena , REIN, Tobias , ROTTICCI, Didier , SÖDERMAN, Peter
IPC分类号： C07D471/04 , A61K31/437 , A61P19/08 , A61P25/00 , A61P25/28 , A61P3/10
CPC分类号： C07D471/04
摘要： The present invention relates to new compounds of formula (I) as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及作为其盐的游离碱或其药学上可接受的盐，溶剂化物或溶剂化物的新的式（I）化合物，其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。

5. 发明申请

WO2007040438A2 NEW COMPOUNDS I 审中-公开
标题翻译：新化合物
公开(公告)号：WO2007040438A2
公开(公告)日：2007-04-12
申请号：PCT/SE2006001114
申请日：2006-10-02
申请人： ASTRAZENECA AB , ARVIDSSON PER I , ARZEL ERWAN , BURROWS JEREMY , CLAESSON MARTINA , RAY COLIN , REIN TOBIAS , ROTTICCI DIDIER , SOEDERMAN PETER
发明人： ARVIDSSON PER I , ARZEL ERWAN , BURROWS JEREMY , CLAESSON MARTINA , RAY COLIN , REIN TOBIAS , ROTTICCI DIDIER , SOEDERMAN PETER
IPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/501 , A61K31/551 , A61P3/10 , A61P19/08 , A61P25/00 , A61P25/28
CPC分类号： C07D471/04
摘要： The present invention relates to new compounds of formula (I) Wherein X is or Y; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及新的式（I）化合物，其中X是或Y; 作为其盐的游离碱或其药学上可接受的盐，溶剂合物或溶剂合物，其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。

6. 发明申请

WO2011059388A1 OXAZOLO[4,5-C]PYRIDINE SUBSTITUTED PYRAZINE 审中-公开
标题翻译： OXAZOLO [4,5-C]吡啶基取代的吡咯
公开(公告)号：WO2011059388A1
公开(公告)日：2011-05-19
申请号：PCT/SE2010/051243
申请日：2010-11-12
申请人： ASTRAZENECA AB , ÅHLIN, Kristofer , ARVIDSSON, Per I , HUERTA, Fernando , YNGVE, Ulrika
发明人： ÅHLIN, Kristofer , ARVIDSSON, Per I , HUERTA, Fernando , YNGVE, Ulrika
IPC分类号： C07D471/04 , A61K31/4965 , A61P19/00 , A61P23/00 , A61P35/00
CPC分类号： C07D498/04
摘要： The present invention relates to a compound of formula (I), wherein R 1 is hydrogen or methyl, or a pharmaceutically acceptable salt thereof, pharmaceutical formulations containing said compound, to the use of said active compound in therapy, as well as intermediates.
摘要翻译：本发明涉及式（I）化合物，其中R 1为氢或甲基，或其药学上可接受的盐，含有所述化合物的药物制剂，以及所述活性化合物在治疗中的用途以及中间体。

7. 发明申请

WO2009145719A1 ISOINDOLINE DERIVATIVES COMPRISING A CYANO GROUP AND THEIR USE IN THE TREATMENT OF PAIN DISORDERS 审中-公开
标题翻译：包含CYANO集团的ISOINDOLINE衍生物及其在治疗疼痛症状中的应用
公开(公告)号：WO2009145719A1
公开(公告)日：2009-12-03
申请号：PCT/SE2009/050616
申请日：2009-05-29
申请人： ASTRAZENECA AB , ÅHLIN, Kristofer , ARVIDSSON, Per I , BESIDSKI, Yevgeni , NILSSON, Linda I
发明人： ÅHLIN, Kristofer , ARVIDSSON, Per I , BESIDSKI, Yevgeni , NILSSON, Linda I
IPC分类号： C07D209/46 , A61K31/4035 , A61P25/04
CPC分类号： C07D209/46
摘要： Compounds of formula I are claimed, wherein R 1 is hydrogen, C 1_3 alkyl, C 1_3 alkoxy, cyano, hydroxy or halo; and wherein said C 1-3 alkyl is optionally substituted by one or more substituents independently selected from hydroxy, C 1_3 alkoxy andfluoro; and said C 1_3 alkoxy is optionally substituted by one or more fluoro; m is 1, 2 or 3; R 2 and R 3 is each and independently selected from hydrogen, C 1-4 haloalkyl, C 1-4 haloalkoxy, halo, C 1-4 alkoxy, C 1-4 alkyl and C 3_7 Cycloalkyloxy; wherein said C 3_7 cycloalkyloxy is optionally substituted by one or more fluoro; and R 2 and R 3 may not both be hydrogen; L 1 is C 1-4 alkylene, pentylene, or C 3-6 cycloalkylene, wherein said C 1-4 alkylene, pentylene or C 3-6 cycloalkylene may be optionally substituted by one or more X 4 ; X 4 is fluoro, C 1_3 alkyl, C 3_7 Cycloalkyl, C 1_3 alkylOCi_3alkyl, C 1_3 alkoxy, cyano, hydroxy, R 4 O(C=O)-, R 4 NR 5 (C=O)-, R 4 O(C=O)NR 5 -, R 4 NR 5 (C=O)NR 5 -, R 4 (C=O)O-, R 4 (C=O)NR5-, R 4 NR 5 (C=O)O-, R 4 NR 5( C=O)NR 5 -, C 5-6 heteroaryl(C=O), or C 5-6 heteroaryl; R 4 is C 1-4 alkylOC 1-4 alkyl, C 5-6 cycloalkyl, aryl, or aryl-C 1-2 alkyl; R 5 is H or methyl; and wherein said C 1-3 alkylOC 1-3 alkyl, C 1-3 alkoxy and C 1-4 alkylsulfonyl is optionally substituted by one or more fluoro; L 2 is C 1-3 alkylene, optionally substituted by one or more X 4 ; as well as pharmaceutically acceptable salt, or isomer thereof, or a salt of said isomer. Compounds of the invention are useful in therapy, such as pain therapy.
摘要翻译：要求的式I化合物，其中R 1是氢，C 1-3烷基，C 1-3烷氧基，氰基，羟基或卤素; 并且其中所述C 1-3烷基任选被一个或多个独立地选自羟基，C 1-3烷氧基和氟的取代基取代; 并且所述C 1-3烷氧基任选被一个或多个氟取代; m为1,2或3; R 2和R 3各自独立地选自氢，C 1-4卤代烷基，C 1-4卤代烷氧基，卤素，C 1-4烷氧基，C 1-4烷基和C 3-8环烷氧基; 其中所述C 3-7环烷氧基任选被一个或多个氟取代; R2和R3不能都是氢; L 1是C 1-4亚烷基，亚戊基或C 3-6亚环烷基，其中所述C 1-4亚烷基，亚戊基或C 3-6亚环烷基可任选被一个或多个X 4取代; X 4是氟，C 1-3烷基，C 3-8环烷基，C 1-3烷基C 1-3烷基，C 1-3烷氧基，氰基，羟基，R 4 O（C = O） - ，R 4 NR 5（C = O） - ，R 40（C = O）NR 5 - ，R 4 NR 5（C = O）NR 5 - R4（C = O）O-，R4（C = O）NR5-，R4NR5（C = O）O-，R4NR5（C = O）NR5-，C5-6杂芳基（C = O）杂; R 4是C 1-4烷基OC 1-4烷基，C 5-6环烷基，芳基或芳基-C 1-2烷基; R5是H或甲基; 并且其中所述C 1-3烷基OC 1-3烷基，C 1-3烷氧基和C 1-4烷基磺酰基任选被一个或多个氟取代; L2是任选被一个或多个X 4取代的C 1-3亚烷基; 以及其药学上可接受的盐或其异构体，或所述异构体的盐。本发明的化合物可用于治疗，例如疼痛疗法。

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