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1. 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。

2. 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.

3. 发明申请

WO2009010784A1 NEW COMPOUNDS 955 审中-公开
标题翻译：新化合物955
公开(公告)号：WO2009010784A1
公开(公告)日：2009-01-22
申请号：PCT/GB2008/050554
申请日：2008-07-09
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BESIDSKI, Yevgeni , CLAESSON, Alf , MACSARI, Istvan , SANDBERG, Lars
发明人： BESIDSKI, Yevgeni , CLAESSON, Alf , MACSARI, Istvan , SANDBERG, Lars
IPC分类号： C07D261/14 , C07D413/12 , C07D413/14 , A61K31/33 , A61P25/00
CPC分类号： C07D261/14 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I): wherein the substituents are as defined in the specification, are described and claimed. The invention further relates to pharmaceutical compositions containing said compounds and to the use of said compounds in therapy. The present invention also relates to processes for the preparation of said compounds.
摘要翻译：描述和要求保护的式（I）化合物：其中取代基如说明书中所定义。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。本发明还涉及制备所述化合物的方法。

4. 发明申请

WO2009005460A1 SMALL MOLECULE INHIBITORS OF NAVL.7 SODIUM CHANNELS FOR THE TREATMENT OF PAIN DISORDERS 审中-公开
标题翻译： NAVL.7小分子抑制剂用于治疗疼痛症状的钠通道
公开(公告)号：WO2009005460A1
公开(公告)日：2009-01-08
申请号：PCT/SE2008/050789
申请日：2008-06-27
申请人： ASTRAZENECA AB , BESIDSKI, Yevgeni , CLAESSON, Alf
发明人： BESIDSKI, Yevgeni , CLAESSON, Alf
IPC分类号： C07D277/28 , A61K31/415 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/47 , A61K31/4709 , A61K31/4965 , A61K31/497 , A61P29/00 , C07D213/38 , C07D215/14 , C07D233/61 , C07D241/42 , C07D277/64 , C07D403/06 , C07D417/06
CPC分类号： C07D213/38 , C07D215/14 , C07D233/61 , C07D241/42 , C07D277/28 , C07D277/64 , C07D401/06 , C07D417/06
摘要： The present invention relates to 2 -substituted, 1,1- diarylethanol compounds of formula I, which are inhibitors of the sodium channel NaVl.7, and the use of such compounds in the manufacture of medicaments for the treatment of pain.
摘要翻译：本发明涉及作为钠通道NaV1.7的抑制剂的式I的2-取代的1,1-二乙基乙醇化合物，以及这些化合物在制备用于治疗疼痛的药物中的用途。

5. 发明申请

WO2009005459A1 PHENYL-1,2, 3,4-TETRAHYDROISOQUINOLINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF A PAIN DISORDER 审中-公开
标题翻译：苯并-1,2,3,4-四氢喹啉酮衍生物及其在治疗疼痛症状中的应用
公开(公告)号：WO2009005459A1
公开(公告)日：2009-01-08
申请号：PCT/SE2008/050787
申请日：2008-06-27
申请人： ASTRAZENECA AB , BESIDSKI, Yevgeni , CLAESSON, Alf
发明人： BESIDSKI, Yevgeni , CLAESSON, Alf
IPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , A61P25/04 , C07D217/22 , C07D401/04 , C07D401/10
CPC分类号： C07D217/22 , C07D217/24 , C07D401/04
摘要： The present invention relates to new compounds and pharmaceutically-acceptable salts thereof, and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
摘要翻译：本发明涉及新化合物及其药学上可接受的盐，以及其制备中使用的新中间体，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。

6. 发明申请

WO2006115452A1 USE OF PYRAZOLYL-PYRIMIDINE DERIVATIVES IN THE TREATMENT OF PAIN 审中-公开
标题翻译：吡唑啉衍生物在治疗疼痛中的应用
公开(公告)号：WO2006115452A1
公开(公告)日：2006-11-02
申请号：PCT/SE2006/000476
申请日：2006-04-25
申请人： ASTRAZENECA AB , CLAESSON, Alf
发明人： CLAESSON, Alf
IPC分类号： A61K31/506 , A61K31/517 , A61P25/04 , A61P29/00
CPC分类号： A61K31/506
摘要： This invention relates to the use of a pyrazolyl-pyrimidine of the formula (I). n = 0,1,2 or 3 (I) in the manufacture of a medicament for use in the treatment or prophylaxis of pain. and to their pharmaceutical formulations and to their methods of use.
摘要翻译：本发明涉及式（I）的吡唑基 - 嘧啶的用途。在制备用于治疗或预防疼痛的药物中，n = 0,1,2或3（I）。以及它们的药物制剂及其使用方法。

7. 发明申请

WO2008054292A1 PYRAZOLYL DERIVATIVES WITH ANALGESIC ACTIVITY AND THEREFORE USEFUL IN THE TREATMENT OR PROPHYLAXIS OF PAIN. 审中-公开
标题翻译：具有镇痛活性并且因此用于治疗或预防疼痛的吡唑啉衍生物。
公开(公告)号：WO2008054292A1
公开(公告)日：2008-05-08
申请号：PCT/SE2007/000967
申请日：2007-10-31
申请人： ASTRAZENECA AB , CLAESSON, Alf
发明人： CLAESSON, Alf
IPC分类号： A61K31/444 , A61K31/4439 , A61P25/04 , A61P29/00
CPC分类号： A61K31/4439 , A61K31/444 , A61K31/455
摘要： This invention relates to new use of pyrazolyl derivatives and pharmaceutically acceptable salts thereof, which have been found to possess analgesic activity and are accordingly useful in the treatment or prophylaxis of pain conditions in the human or animal body, for example in the manufacture of medicaments for the treatment or prevention of pain in a warm blooded animal such as man.
摘要翻译：本发明涉及已经发现的吡唑基衍生物及其药学上可接受的盐的新用途，该吡唑基衍生物及其药学上可接受的盐已被发现具有止痛活性并因此可用于治疗或预防人或动物体内的疼痛状况，例如在制造用于治疗或预防温血动物例如人的疼痛的药物中。

8. 发明申请

WO2008054291A1 PYRAZOLYL DERIVATIVES WITH ANALGESIC ACTIVITY AND THEREFORE USEFUL IN THE TREATMENT OR PROPHYLAXIS OF PAIN. 审中-公开
标题翻译：具有活性活性的吡唑啉衍生物，因此可用于治疗或预防疼痛。
公开(公告)号：WO2008054291A1
公开(公告)日：2008-05-08
申请号：PCT/SE2007/000966
申请日：2007-10-31
申请人： ASTRAZENECA AB , CLAESSON, Alf
发明人： CLAESSON, Alf
IPC分类号： A61K31/506 , A61P25/04 , A61P29/00
CPC分类号： A61K31/506
摘要： This invention relates to new use of pyrazolyl derivatives and pharmaceutically acceptable salts thereof, which have been found to possess analgesic activity and are accordingly useful in the treatment or prophylaxis of pain conditions in the human or animal body, for example in the manufacture of medicaments for the treatment or prevention of pain in a warm blooded animal such as man.
摘要翻译：本发明涉及吡唑基衍生物及其药学上可接受的盐的新用途，其已被发现具有止痛活性，因此可用于治疗或预防人或动物体内的疼痛状况，例如制备用于治疗或预防温血动物如男性的疼痛。

9. 发明公开

EP1877057A1 USE OF PYRAZOLYL-PYRIMIDINE DERIVATIVES IN THE TREATMENT OF PAIN 审中-公开
标题翻译：吡唑嘧啶衍生物在疼痛的治疗
公开(公告)号：EP1877057A1
公开(公告)日：2008-01-16
申请号：EP06733332.8
申请日：2006-04-25
申请人： AstraZeneca AB
发明人： CLAESSON, Alf
IPC分类号： A61K31/506 , A61K31/517 , A61P25/04 , A61P29/00
CPC分类号： A61K31/506
摘要： This invention relates to the use of a pyrazolyl-pyrimidine of the formula (I). n = 0,1,2 or 3 (I) in the manufacture of a medicament for use in the treatment or prophylaxis of pain. and to their pharmaceutical formulations and to their methods of use.

10. 发明授权

EP1202994B1 NEW COMPOUNDS 有权
公开(公告)号：EP1202994B1
公开(公告)日：2004-04-14
申请号：EP00950173.5
申请日：2000-07-20
申请人： AstraZeneca AB
发明人： BERGE, Odd-Geir , CLAESSON, Alf , SWAHN, Britt-Marie
IPC分类号： C07D471/20 , C07D487/10 , C07D495/10 , C07D497/10 , A61K31/438 , A61K31/4747 , A61K31/4985
CPC分类号： C07D471/10 , C07D487/10 , C07D491/10
摘要： The present invention relates to certain spirooxindole derivatives of formula (I), and pharmaceutically acceptable salts thereof, which exhibit good analgesic properties and are particulary effective in the treatment of chronic pain.

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