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41. 发明申请

WO2011027156A1 BENZODIAZEPINE DERIVATIVES FOR TREATING HEPATITIS C INFECTION 审中-公开
标题翻译：用于治疗HEPATITIS C感染的苯二胺衍生物
公开(公告)号：WO2011027156A1
公开(公告)日：2011-03-10
申请号：PCT/GB2010/051446
申请日：2010-09-02
申请人： ARROW THERAPEUTICS LIMITED , BARNES, Michael, Christopher, Stratton , DENNISON, Helena, Jade , FLACK, Stephen, Sean , LUMLEY, James, Andrew , PANG, Pui, Shan , SPENCER, Keith, Charles
发明人： BARNES, Michael, Christopher, Stratton , DENNISON, Helena, Jade , FLACK, Stephen, Sean , LUMLEY, James, Andrew , PANG, Pui, Shan , SPENCER, Keith, Charles
IPC分类号： C07D243/24 , C07D401/12 , A61K31/5513 , A61P31/12
CPC分类号： C07D243/24 , C07D401/12
摘要： The invention concerns benzodiazepine derivatives of Formula (I) wherein W, X, L 1 , L 2 , L 3 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment or prophylaxis of hepatitis C virus infection.
摘要翻译：本发明涉及式（I）的苯并二氮杂衍生物，其中W，X，L 1，L 2，L 3，R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义。本发明还涉及制备这些化合物的方法，含有它们的药物组合物及其在治疗或预防丙型肝炎病毒感染中的用途。

42. 发明申请

WO2011012885A9 FULVESTRANT IN A DOSAGE OF 500MG FOR THE TREATMENT OF ADVANCED BREAST CANCER 审中-公开
公开(公告)号：WO2011012885A9
公开(公告)日：2011-02-03
申请号：PCT/GB2010/051228
申请日：2010-07-26
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , DIMERY, Isaiah, William , WEBSTER, Alan
发明人： DIMERY, Isaiah, William , WEBSTER, Alan
IPC分类号： A61K31/565 , A61P35/00
摘要： The present invention relates to fulvestrant at a dosage of 500mg for use in the treatment of a postmenopausal woman with advanced breast cancer who has progressed or recurred on endocrine therapy.

43. 发明申请

WO2011002409A1 5H-PYRROLO[3,4-£>]PYRAZIN-7-AMINE DERIVATIVES INHIBITORS OF BETA-SECRETASE 审中-公开
标题翻译： 5H-PYRROLO [3,4-]>β-分泌酶的吡嗪-7-胺衍生物抑制剂
公开(公告)号：WO2011002409A1
公开(公告)日：2011-01-06
申请号：PCT/SE2010/050761
申请日：2010-07-02
申请人： ASTRAZENECA AB , HOLENZ, Jörg , KARLSTRÖM, Sofia , KIHLSTRÖM, Jacob , KOLMODIN, Karin , LINDSTRÖM, Johan , RAKOS, Laszlo , ROTTICCI, Didier , SWAHN, Britt-Marie , VON BERG, Stefan
发明人： HOLENZ, Jörg , KARLSTRÖM, Sofia , KIHLSTRÖM, Jacob , KOLMODIN, Karin , LINDSTRÖM, Johan , RAKOS, Laszlo , ROTTICCI, Didier , SWAHN, Britt-Marie , VON BERG, Stefan
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Downs 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 Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
摘要翻译：本发明涉及新的式（I）化合物及其药物组合物。此外，本发明涉及用于治疗和/或预防诸如唐氏综合征，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的Aβ相关病理学的治疗方法，与认知障碍相关的疾病例如但不限于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，与诸如阿尔茨海默病或痴呆症的疾病相关的神经变性，包括混合血管和退行性起源的痴呆，老年性痴呆，老年性痴呆和与帕金森病相关的痴呆，进行性核上性麻痹或皮质基底变性。

44. 发明申请

WO2010151216A1 METHOD FOR TREATING A PATIENT AT RISK FOR DEVELOPING AN NSAID-ASSOCIATED ULCER 审中-公开
标题翻译：用于治疗患有风险的患者用于开发与NSAID相关的ULCER的方法
公开(公告)号：WO2010151216A1
公开(公告)日：2010-12-29
申请号：PCT/SE2010/050712
申请日：2010-06-23
申请人： ASTRAZENECA AB , POZEN Inc. , AULT, Brian , HWANG, Clara , ORLEMANS, Everardus , PLACHETKA, John R. , SOSTEK, Mark
发明人： AULT, Brian , HWANG, Clara , ORLEMANS, Everardus , PLACHETKA, John R. , SOSTEK, Mark
IPC分类号： A61K31/4439 , A61K9/24 , A61P19/02 , A61P29/00
CPC分类号： A61K31/4439 , A61K9/0053 , A61K9/209 , A61K31/192 , A61K45/06 , A61K2300/00
摘要： The present disclosure is directed to a method for treating a disease or disorder in a patient at risk of developing an NSAID-associated ulcer by administering a pharmaceutical composition in unit dose form comprising naproxen, or pharmaceutically acceptable salt thereof, and esomeprazole, or pharmaceutically acceptable salt thereof. The unit dose is designed to release at least a part of the esomeprazole independent of pH (e.g. at a pH of 0 or more) whereas the naproxen is not released until the pH or the surrounding medium is 3.5 or higher.
摘要翻译：本公开涉及一种通过以包含萘普生或其药学上可接受的盐和埃索美拉唑或其药学上可接受的盐的单位剂量形式的药物组合物来治疗患有NSAID相关性溃疡的患者的疾病或病症的方法的盐。设计单位剂量以独立于pH释放至少一部分艾美拉唑（例如在pH为0或更高），而萘普生没有释放直到pH或周围介质为3.5或更高。

45. 发明申请

WO2010144043A1 A NOVEL 4-METHYLBENZENESULPHONATE SALT AND A PROCESS FOR PREPARING A PHARMACEUTICAL COMPOSITION COMPRISING THE SALT 审中-公开
标题翻译：新型4-甲基苯磺酸盐和一种制备包含盐的药物组合物的方法
公开(公告)号：WO2010144043A1
公开(公告)日：2010-12-16
申请号：PCT/SE2010/050645
申请日：2010-06-10
申请人： ASTRAZENECA AB , METE, Antonio , NILSSON, Karolina , NYSTRÖM, Stefan , TROFAST, Eva
发明人： METE, Antonio , NILSSON, Karolina , NYSTRÖM, Stefan , TROFAST, Eva
IPC分类号： C07D453/02 , A61K31/439 , A61K9/14 , A61K9/72 , A61P11/00
CPC分类号： C07D453/02 , A61K9/0075 , A61K9/145 , A61K31/439
摘要： The invention provides a 4-methylbenzenesulphonate salt of the muscarinic antagonist (R)- 1-(4-fluorophenethyl)-3-((S)-2-phenyl-2-(piperidin-1 -yl)propanoyloxy)-1- azoniabicyclo[2.2.2]octane and its use in therapy,as well as a process for preparing a pharmaceutical composition comprising the salt and its use in therapy.
摘要翻译：本发明提供了毒蕈碱拮抗剂（R）-1-（4-氟苯乙基）-3 - （（S）-2-苯基-2-（哌啶-1-基）丙酰氧基）-1-氮鎓二
环己基的4-甲基苯磺酸盐 [2.2.2]辛烷及其在治疗中的应用，以及制备包含该盐及其在治疗中的用途的药物组合物的方法。

46. 发明申请

WO2010123443A1 PHARMACEUTICAL COMPOSITION COMPRISING 4-AMINO-8-(2-FLUORO-6-METHOXY-PHENYL)-N- PROPYLCINNOLINE-3-CARBOXAMIDE HYDROGEN SULPHATE. 审中-公开
标题翻译：包含4-氨基-8-（2-氟-6-甲氧基苯基）-N-丙氧基-3-羧酰胺氢化物的药物组合物。
公开(公告)号：WO2010123443A1
公开(公告)日：2010-10-28
申请号：PCT/SE2010/050427
申请日：2010-04-20
申请人： ASTRAZENECA AB , AVILOV, Dmytro , BROWN, Daniel , CREEKMORE, Richard , REUS MEDINA, Marilu , SCHULTZ, Sharon , SHARMA, Avadhesh
发明人： AVILOV, Dmytro , BROWN, Daniel , CREEKMORE, Richard , REUS MEDINA, Marilu , SCHULTZ, Sharon , SHARMA, Avadhesh
IPC分类号： A61K9/20 , A61K31/502 , A61K47/38 , A61K47/46 , A61K9/50 , A61P25/22
CPC分类号： A61K31/502 , A61K9/2018 , A61K9/2054
摘要： Disclosed is a pharmaceutical composition for a cinnoline derivative in the gastrointestinal environment. The composition comprising a solid cinnoline derivative and at least one pharmaceutical excipient selected from a filler, a binder, a disintegrant, a suspending agent, a coating agent, a sweetener, a flavoring, and a lubricant.
摘要翻译：公开了一种用于胃肠环境中的噌啉衍生物的药物组合物。所述组合物包含固体噌啉衍生物和至少一种选自填料，粘合剂，崩解剂，悬浮剂，包衣剂，甜味剂，调味剂和润滑剂的药用赋形剂。

47. 发明申请

WO2010123441A1 CRYSTALLINE FORM OF 4-AMINO-8-(2-FLUORO-6-METHOXY-PHENYL)-N-PROPYLCINNOLINE-3- CARBOXAMIDE HYDROGEN SULPHATE, FOR TREATMENT OF ANXIETY DISORDERS 审中-公开
标题翻译： 4-氨基-8-（2-氟-6-甲氧基苯基）-N-丙氧基-3-羰基氧化氢氢化钠的晶体形式，用于治疗无效疾病
公开(公告)号：WO2010123441A1
公开(公告)日：2010-10-28
申请号：PCT/SE2010/050425
申请日：2010-04-20
申请人： ASTRAZENECA AB , BLACK, Simon Nicholas , COSGROVE, Stephen David , McCORMICK, Marc , OSBORN, Jim , REID, Julie , WU, Dedong
发明人： BLACK, Simon Nicholas , COSGROVE, Stephen David , McCORMICK, Marc , OSBORN, Jim , REID, Julie , WU, Dedong
IPC分类号： A61K31/502 , A61P25/22
CPC分类号： C07D237/28
摘要： 4-Amino-8-(2-fluoro-6-methoxy-phenyl)-N-propylcinnoline-3-carboxamide hydrogen sulphate, polymorphs thereof, pharmaceutical compositions contain them, methods of making them are described. They are useful in treating anxiety disorders.
摘要翻译： 4-氨基-8-（2-氟-6-甲氧基 - 苯基）-N-丙基噌啉-3-甲酰胺硫酸氢盐，其多晶型物，含有它们的药物组合物，描述制备它们的方法。它们可用于治疗焦虑症。

48. 发明申请

WO2010122340A3 PROCESS FOR THE PREPARATION OF 4-(3-CHLORO-2-FLUORO-ANILINO)-7-METHOXY-6-[1-(N-METHYLCARBAMOYLMETHYL)-PIPERIDIN-4-YL]QUINAZOLINE 审中-公开
公开(公告)号：WO2010122340A3
公开(公告)日：2010-10-28
申请号：PCT/GB2010/050653
申请日：2010-04-22
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BOARDMAN, Kay, Alison , CUNNINGHAM, Oliver, Robert , GOUNDRY, William , LAFFAN, David, Dermot, Patrick
发明人： BOARDMAN, Kay, Alison , CUNNINGHAM, Oliver, Robert , GOUNDRY, William , LAFFAN, David, Dermot, Patrick
IPC分类号： C07D211/46 , C07D401/12 , C07C257/12
摘要： Processes for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N- methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline, salts thereof, and the intermediates used in the process are described.

49. 发明申请

WO2010117323A1 METHOD AND APPARATUS FOR PRODUCING HEAT ENERGY AND CARBON DIOXIDE 审中-公开
标题翻译：生产热能和二氧化碳的方法和装置
公开(公告)号：WO2010117323A1
公开(公告)日：2010-10-14
申请号：PCT/SE2010/050375
申请日：2010-04-06
申请人： ASTRAZENECA AB , BOSTRÖM, Jonas , CHENG, Leifeng , FEX, Tomas , KARLE, Michael , PETTERSEN, Daniel , SCHELL, Peter
发明人： BOSTRÖM, Jonas , CHENG, Leifeng , FEX, Tomas , KARLE, Michael , PETTERSEN, Daniel , SCHELL, Peter
IPC分类号： C07D413/04 , A61K31/4523 , A61P7/04
CPC分类号： C07D413/04
摘要： Formula I or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3, R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile, or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4; wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate; R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring; or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.
摘要翻译：式I或其药学上合适的盐，其中R 1和R 2独立地是氢，氘，芳基，杂芳基，任选被一个或多个取代基独立地被R 3取代的C 1 -C 8烷基，R 3是芳基，杂芳基，氟，含有一个或多个氟的C 1 -C 6烷基，含有一个或多个氘的C 1 -C 6烷基，含羟基的C 1 -C 6烷基，任选被一个或多个卤素取代的芳基和杂芳基，氟化烷氧基，氟化烷基，磺酰基，一个或多个氘，C 1-6烷基，C 1-6烷氧基，腈或R 3是任选被一个或多个下列基团取代的C 1-6烷基：COOR 4， OCOR4，CONR5R6，NR5COR6，OR4; 其中，R4为任选被一个或多个氟，氘，烷氧基，芳基羧酸酯，羧酸烷基酯取代的C 1-10烷基; R 5和R 6独立地选自氢，烷基或它们可以一起形成4-8元碳环; 或R 1和R 2形成任选地包含O或N并任选被C 1-10烷基或芳基取代的3-10元碳环，任选被R 3取代的杂芳基。

50. 发明申请

WO2010114471A1 NOVEL AMIDE DERIVATIVES OF STEROIDAL[3,2-C]PYRAZOLE COMPOUNDS WITH GLUCOCORTICOID ACTIVITY 审中-公开
标题翻译：具有葡萄糖激活活性的甾体[3,2-C]吡唑化合物的新型衍生物
公开(公告)号：WO2010114471A1
公开(公告)日：2010-10-07
申请号：PCT/SE2010/050354
申请日：2010-03-31
申请人： ASTRAZENECA AB , BURKAMP, Frank , GABOS, Balint , IVANOVA, Svetlana , LISIUS, Alice Ingrid Annéa
发明人： BURKAMP, Frank , GABOS, Balint , IVANOVA, Svetlana , LISIUS, Alice Ingrid Annéa
IPC分类号： C07J71/00 , A61K31/58 , A61P11/00 , A61P11/06 , A61P29/00
CPC分类号： C07J71/0047 , A61K31/58
摘要： The present invention provides compounds of formula (I) wherein n, R 1 , R 2 , X 1 , X 2 , X 3 , X 4, X 5 , R 3a , R 3b , R 4 , R 5 and R 6 are defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译：本发明提供式（I）化合物，其中n，R1，R2，X1，X2，X3，X4，X5，R3a，R3b，R4，R5和R6在本说明书中定义，其制备方法，药物组合物包含它们及其在治疗中的用途。

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