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1. 发明申请

WO2008130319A3 NOVEL N-TETRAHYDRONAPHTALENE OR N-CHROMANE CARBOXAMIDE DERIVATIVES FOR THE TREATMENT OF PAIN 审中-公开
公开(公告)号：WO2008130319A3
公开(公告)日：2008-10-30
申请号：PCT/SE2008/050458
申请日：2008-04-22
申请人： ASTRAZENECA AB , BESIDSKI, Yevgeni , CLAESSON, Alf , CSJERNYIK, Gabor , GRAVENFORS, Ylva , KERS, Inger , SKOGHOLM, Karin , SOHN, Daniel
发明人： BESIDSKI, Yevgeni , CLAESSON, Alf , CSJERNYIK, Gabor , GRAVENFORS, Ylva , KERS, Inger , SKOGHOLM, Karin , SOHN, Daniel
IPC分类号： C07D405/12 , C07C235/54 , C07C309/65 , C07D211/46 , C07D217/04 , C07D249/06 , C07D263/34 , C07D265/30 , C07D295/088 , C07D295/135 , C07D295/155 , C07D295/192 , C07D311/74 , C07D401/12 , C07D413/12
摘要： The present invention relates to new compounds and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.

2. 发明申请

WO2012087237A1 COMPOUNDS AND THEIR USE AS BACE INHIBITORS 审中-公开
标题翻译：化合物及其作为BACE抑制剂的用途
公开(公告)号：WO2012087237A1
公开(公告)日：2012-06-28
申请号：PCT/SE2011/051555
申请日：2011-12-21
申请人： ASTRAZENECA AB , CSJERNYIK, Gabor , KARLSTRÖM, Sofia , KERS, Annika , KOLMODIN, Karin , NYLÖF, Martin , ÖHBERG, Liselotte , RAKOS, Laszlo , SANDBERG, Lars , SEHGELMEBLE, Fernando , SÖDERMAN, Peter , SWAHN, Britt-Marie , VON BERG, Stefan
发明人： CSJERNYIK, Gabor , KARLSTRÖM, Sofia , KERS, Annika , KOLMODIN, Karin , NYLÖF, Martin , ÖHBERG, Liselotte , RAKOS, Laszlo , SANDBERG, Lars , SEHGELMEBLE, Fernando , SÖDERMAN, Peter , SWAHN, Britt-Marie , VON BERG, Stefan
IPC分类号： C07D491/107 , A61K31/4184 , A61K31/4188 , A61K31/4439 , A61K31/506 , A61P25/28 , C07D401/04 , C07D235/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D491/20
CPC分类号： A61K31/497 , A61K31/4184 , A61K31/4188 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K45/06 , A61K2300/00 , C07D235/02 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D471/04 , C07D491/107 , C07D491/20
摘要： The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Αβ-related pathologies such as Down's syndrome, β- amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.
摘要翻译：本发明涉及式（I）化合物及其药物组合物。此外，本发明涉及用于治疗和/或预防β相关病理学的治疗方法，例如唐氏综合征，β-淀粉样变性血管病，例如但不限于脑淀粉样血管病或遗传性脑出血，与认知相关的疾病损伤例如但不限于MCI（“轻度认知障碍”），阿尔茨海默病，记忆丧失，与阿尔茨海默病相关的注意力缺陷症状，与诸如阿尔茨海默氏病或痴呆的疾病相关的神经变性，包括混合血管和退行性来源的痴呆，前老年痴呆症，老年痴呆症和与帕金森病相关的痴呆症。

3. 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。

4. 发明申请

WO2008130319A2 NEW COMPOUNDS 805 审中-公开
标题翻译：新化合物805
公开(公告)号：WO2008130319A2
公开(公告)日：2008-10-30
申请号：PCT/SE2008050458
申请日：2008-04-22
申请人： ASTRAZENECA AB , BESIDSKI YEVGENI , CLAESSON ALF , CSJERNYIK GABOR , GRAVENFORS YLVA , KERS INGER , SKOGHOLM KARIN , SOHN DANIEL
发明人： BESIDSKI YEVGENI , CLAESSON ALF , CSJERNYIK GABOR , GRAVENFORS YLVA , KERS INGER , SKOGHOLM KARIN , SOHN DANIEL
IPC分类号： C07D405/12 , C07C235/54 , C07C309/65 , C07D211/46 , C07D217/04
CPC分类号： C07C309/65 , C07C235/54 , C07C2602/10 , C07D211/46 , C07D217/04 , C07D405/12
摘要： The present invention relates to new compounds and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof.
摘要翻译：本发明涉及新化合物和含有所述化合物的药物组合物和所述化合物在治疗中的用途。本发明还涉及制备所述化合物的方法和可用于其制备的新中间体。

5. 发明申请

WO2009145721A1 ISOINDOLINE DERIVATIVES COMPRISING PHENYL GROUPS AND THEIR USE IN THE TREATMENT OF PAIN DISORDERS 审中-公开
标题翻译：包含苯基组合物的吲哚啉衍生物及其在治疗疼痛症状中的应用
公开(公告)号：WO2009145721A1
公开(公告)日：2009-12-03
申请号：PCT/SE2009/050618
申请日：2009-05-29
申请人： ASTRAZENECA AB , BESIDSKI, Yevgeni , CLAESSON, Alf , CSJERNYIK, Gabor , MACSÁRI, István , NILSSON, Linda I
发明人： BESIDSKI, Yevgeni , CLAESSON, Alf , CSJERNYIK, Gabor , MACSÁRI, István , NILSSON, Linda I
IPC分类号： C07D405/04 , A61K31/4035 , A61K31/4523 , A61K31/506 , A61P25/04 , C07D209/46 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/14
CPC分类号： C07D403/04 , C07D209/46 , C07D401/04 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/14
摘要： Compounds of formula I are claimed, (I) wherein R1 is hydrogen, C1-3alkyl, Ci_3alkoxy, cyano, hydroxy or halo; and wherein said Ci^alkyl is optionally substituted by one or more substituents independently selected from hydroxy, Ci^alkoxy andfluoro; and said Ci^alkoxy is optionally substituted by one or morefluoro; m is 1 or 2; R2 and R3 is each and independently selected from hydrogen, Ci_4haloalkyl, Ci_4haloalkoxy, halo, Ci_4alkoxy, Ci_4alkyl and C3_7cycloalkyloxy; wherein said C3. γcycloalkyloxy is optionally substituted by one or morefluoro; and R2 and R3 may not both be hydrogen; D is C3_7cycloalkyl or C3_7heterocycloalkyl; and wherein said Cs-jcycloalkyl or Cs- γheterocycloalkyl may optionally be substituted by one or more X*; X4 is halo, Ci_3alkyl, Ci_3alkyl0Ci_3alkyl, Ci_3alkoxy, benzyl, Ci_4alkylsulfonyl, oxo, R4O(C=O), R5(C=O), or C5.6 heteroaryl; wherein said Cisalkyl, CisalkylOCisalkyl, Ci^alkoxy and C i^alkylsulfonyl is optionally substituted by one or more fluoro; R4 is Ci_4alkyl, Ci_4alkyl0Ci_4alkyl, C5_6cycloalkyl, or aryl; R5 is Ci_4alkyl, Ci_4fluoroalkyl or Cs_6 heteroaryl; Li is Ci_4alkylene or a bond; L2 is Ci_3alkylene; with the exception of the compound 2-(cyclohexylmethyl)-3-oxo-N-[2-(trifluoromethyl)benzyl]isoindoline-l-carboxamide; as well as a pharmaceutically acceptable salt, or isomer thereof, or a salt of said isomer. The compounds of the invention are useful in therapy such as pain therapy.
摘要翻译：式I化合物要求保护（I）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 1-6烷基任选被一个或多个独立地选自羟基，C 1-6烷氧基和氟的取代基取代; 并且所述C 1-6烷氧基任选被一个或多个氟取代; m为1或2; 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 3-7环烷氧基; 其中所述C3。环烷氧基任选被一个或多个氟取代; R2和R3不能都是氢; D是C 3-7环烷基或C 3-7杂环烷基; 并且其中所述C 8 - 环烷基或C 5 -C 4杂环烷基可任选被一个或多个X *取代; X 4是卤素，C 1-3烷基，C 1-3烷基C 1-3烷基，C 1-3烷氧基，苄基，C 1-4烷基磺酰基，氧代，R 40（C = O），R 5（C = O）或C 5-6杂芳基; 其中所述C 1烷基，C 1 -C 6烷基，C 1烷基，C 1-6烷氧基和C 1-6烷基磺酰基任选被一个或多个氟取代; R4是C 1-4烷基，C 1-4烷基C 1-4烷基，C 5-6环烷基或芳基; R5是C 1-4烷基，C 1-4氟烷基或C 3-6杂芳基; Li是C 1-4亚烷基或键; L2是C 1-3亚烷基; 化合物2-（环己基甲基）-3-氧代-N- [2-（三氟甲基）苄基]异二氢吲哚-1-甲酰胺; 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如疼痛疗法。

6. 发明申请

WO2009145718A1 ISOINDOLINE DERIVATIVES COMPRISING AN ADDITIONAL HETEROCYCLIC GROUP AND THEIR USE IN THE TREATMENT OF PAIN DISORDERS 审中-公开
标题翻译：包含附加杂环组的ISOINDOLINE衍生物及其在治疗疼痛症状中的应用
公开(公告)号：WO2009145718A1
公开(公告)日：2009-12-03
申请号：PCT/SE2009/050615
申请日：2009-05-29
申请人： ASTRAZENECA AB , ARVIDSSON, Per , BESIDSKI, Yevgeni , CSJERNYIK, Gabor , LANGE, Tim , MACSÁRI, István , NILSSON, Linda
发明人： ARVIDSSON, Per , BESIDSKI, Yevgeni , CSJERNYIK, Gabor , LANGE, Tim , MACSÁRI, István , NILSSON, Linda
IPC分类号： C07D401/06 , A61K31/4035 , A61K31/4155 , A61K31/4192 , A61K31/422 , A61K31/444 , A61K31/497 , C07D403/06 , C07D413/06 , A61P25/04
CPC分类号： C07D401/06 , C07D209/46 , C07D403/06 , C07D413/06
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; wherein C 1-3 alkyl may optionally be substituted by one or more substituents independently selected from hydroxy, C 1-3 alkoxy orfluoro; and wherein Ci^alkoxy may optionally be substituted by one or more fluoro; m is 1 or 2; R 2 and R 3 is each and independently selected from hydrogen, Ci_4haloalkyl, C 1 _ 4 haloalkoxy, halo, C 1 _ 4 alkoxy, C 1 _ 4 alkyl and C 3 _ 7 cycloalkyloxy; and wherein said C 3 _ 7 cycloalkyloxy may optionally be substituted by one or more fluoro; and whereas both R 2 and R 3 can not be hydrogen; Het is selected from any one of pyridinyl, pyrazinyl, isoxazolyl, pyrazolyl, indolyl, triazolyl and pyrimidinyl, wherein each such heteroaryl may optionally be substituted by one or more X 4 ; X 4 is halo, C 1-3 alkyl, C 1-3 alkyl0C 1-3 alkyl, -CH(CH 3 )-O-C(CH 3 ) 3 ,C 1 _ 4 alkoxy, cyano, or hydroxyl, or Ci_2hydroxyalkyl;; and wherein said C 1-3 alkyl, C 1-3 alkylOC 1-3 alkyl, -CH(CH 3 )-O-C(CH 3 ) 3 , or C 1 _ 4 alkoxy may each optionally be substituted by one or more fluoro; L 1 is C 1 _ 4 alkylene, which may optionally be fluorinated or hydroxylated; and L 2 is C 1-3 alkylene; with the exception of the compounds: 2-[1-(1,5-dimethyl-lH-pyrazol-4-yl)ethyl]-5,7-dimethoxy-3-oxo-N-[2-(trifluoromethyl)benzyl]isoindoline-1-carboxamide; N-(4-fluorobenzyl)-3-oxo-2-(-pyridin-4-yletyl)isoindoline-1-carboxamide and N-(2-chlorobenzyl)-2[2-(1H-indol-3-yl)-1-methyletyl]-3-oxoisoindoline-1-carboxamide; The invention further relates to pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
摘要翻译：要求保护的式I化合物，其中R 1为氢，C 1-3烷基，C 1-3烷氧基，氰基，羟基或卤素; 其中C 1-3烷基可以任选被一个或多个独立地选自羟基，C 1-3烷氧基或氟的取代基取代; 并且其中C 1-6烷氧基可任选被一个或多个氟取代; m为1或2; 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 3-7环烷氧基; 并且其中所述C 3-7环烷氧基可任选被一个或多个氟取代; 而R2和R3不能是氢; Het选自吡啶基，吡嗪基，异恶唑基，吡唑基，吲哚基，三唑基和嘧啶基中的任一个，其中每个这样的杂芳基可以任选被一个或多个X 4取代; X 4是卤素，C 1-3烷基，C 1-3烷基C 1-3烷基，-CH（CH 3）-O-C（CH 3）3，C 1-4烷氧基，氰基或羟基或C 1-2羟烷基。并且其中所述C 1-3烷基，C 1-3烷基OC 1-3烷基，-CH（CH 3）-O-C（CH 3）3或C 1-4烷氧基各自任选被一个或多个氟取代; L 1是C 1-4亚烷基，其可以任选被氟化或羟基化; 和L2是C1-3亚烷基; 除了化合物之外：2- [1-（1,5-二甲基-1H-吡唑-4-基）乙基] -5,7-二甲氧基-3-氧代-N- [2-（三氟甲基）苄基] 异吲哚啉-1-甲酰胺; N-（4-氟苄基）-3-氧代-2 - （ - 吡啶-4-基）异吲哚啉-1-甲酰胺和N-（2-氯苄基）-2 [2-（1H-吲哚-3-基） 1-methyletyl] -3- oxoisoindoline -1-甲酰胺; 本发明还涉及含有所述化合物的药物组合物和所述化合物在治疗中的用途。

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