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1. 发明申请

WO2004007484A1 FUMARATE SALTS 审中-公开
公开(公告)号：WO2004007484A1
公开(公告)日：2004-01-22
申请号：PCT/SE2003/001207
申请日：2003-07-14
申请人： ASTRAZENECA AB , KIRSCHNER, Alan , MCCABE, James , WILLIAMS, Emyr , YMEN, Ingvar
发明人： KIRSCHNER, Alan , MCCABE, James , WILLIAMS, Emyr , YMEN, Ingvar
IPC分类号： C07D405/14
CPC分类号： C07D311/24
摘要： The present invention relates to novel crystalline forms of 6-fluoro-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid [4-(4-propionyl-piperazin-1-yl)-phenyl]-amide fumarate salt. The present invention also relates to the use of said compounds for the treatment of depression, generalized anxiety, eating disorders, dementia, panic disorder, sleep disorders, gastrointestinal disorders, motor disorders, endocrine disorders, vasospasm, or sexual dysfunction, pharmaceutical compositions containing them and processes for obtaining them.
摘要翻译：本发明涉及6-氟-8-（4-甲基 - 哌嗪-1-基）-4-氧代-4H-色烯-2-羧酸[4-（4-丙酰基 - 哌嗪-1-基） - 基） - 苯基] - 酰胺富马酸盐。本发明还涉及所述化合物用于治疗抑郁症，广泛性焦虑症，进食障碍，痴呆症，恐慌症，睡眠障碍，胃肠道疾病，运动障碍，内分泌紊乱，血管痉挛或性功能障碍的用途，含有它们的药物组合物以及获得它们的过程。

2. 发明申请

WO2004007487A1 CRYSTALLINE FORMS 审中-公开
标题翻译：晶体形式
公开(公告)号：WO2004007487A1
公开(公告)日：2004-01-22
申请号：PCT/SE2003/001210
申请日：2003-07-14
申请人： ASTRAZENECA AB , KIRSCHNER, Alan , MCCABE, James , PIERSON, Edward , WILLIAMS, Emyr , YMÉN, Ingvar
发明人： KIRSCHNER, Alan , MCCABE, James , PIERSON, Edward , WILLIAMS, Emyr , YMÉN, Ingvar
IPC分类号： C07D405/14
CPC分类号： C07D311/24
摘要： The present invention relates to novel crystalline forms of 6-fluoro-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid [4-(4-propionyl-piperazin-1-yl)-phenyl]-amide. The present invention also relates to the use of said compounds for the treatment of depression, generalized anxiety, eating disorders, dementia, panic disorder, sleep disorders, gastrointestinal disorders, motor disorders, endocrine disorders, vasospasm, or sexual dysfunction, pharmaceutical compositions containing them and processes for obtaining them.
摘要翻译：本发明涉及6-氟-8-（4-甲基 - 哌嗪-1-基）-4-氧代-4H-色烯-2-羧酸[4-（4-丙酰基 - 哌嗪-1-基）基） - 苯基] - 酰胺。本发明还涉及所述化合物用于治疗抑郁症，广泛性焦虑症，进食障碍，痴呆症，恐慌症，睡眠障碍，胃肠道疾病，运动障碍，内分泌紊乱，血管痉挛或性功能障碍的用途，含有它们的药物组合物以及获得它们的过程。

3. 发明申请

WO2004007486A1 MALEATE SALTS 审中-公开
公开(公告)号：WO2004007486A1
公开(公告)日：2004-01-22
申请号：PCT/SE2003/001209
申请日：2003-07-14
申请人： ASTRAZENECA AB , KIRSCHNER, Alan , MCCABE, James , PIERSON, Edward , WILLIAMS, Emyr , YMÉN, Ingvar
发明人： KIRSCHNER, Alan , MCCABE, James , PIERSON, Edward , WILLIAMS, Emyr , YMÉN, Ingvar
IPC分类号： C07D405/14
CPC分类号： C07D311/24
摘要： The present invention relates to novel crystalline forms of 6-fluoro-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid [4-(4-propionyl-piperazin-1-yl)-phenyl]-amide maleate salt. The present invention also relates to the use of said compounds for the treatment of depression, generalized anxiety, eating disorders, dementia, panic disorder, sleep disorders, gastrointestinal disorders, motor disorders, endocrine disorders, vasospasm, or sexual dysfunction, pharmaceutical compositions containing them and processes for obtaining them.
摘要翻译：本发明涉及6-氟-8-（4-甲基 - 哌嗪-1-基）-4-氧代-4H-色烯-2-羧酸[4-（4-丙酰基 - 哌嗪-1-基） - 基） - 苯基] - 酰胺马来酸盐。本发明还涉及所述化合物用于治疗抑郁症，广泛性焦虑症，进食障碍，痴呆症，恐慌症，睡眠障碍，胃肠道疾病，运动障碍，内分泌紊乱，血管痉挛或性功能障碍的用途，含有它们的药物组合物以及获得它们的过程。

4. 发明申请

WO2004007485A1 BESYLATE SALTS 审中-公开
标题翻译：乙酸盐
公开(公告)号：WO2004007485A1
公开(公告)日：2004-01-22
申请号：PCT/SE2003/001208
申请日：2003-07-14
申请人： ASTRAZENECA AB , KIRSCHNER, Alan , MCCABE, James , WILLIAMS, Emyr , YMÉN, Ingvar
发明人： KIRSCHNER, Alan , MCCABE, James , WILLIAMS, Emyr , YMÉN, Ingvar
IPC分类号： C07D405/14
CPC分类号： C07D311/24
摘要： The present invention relates to novel crystalline forms of 6-fluoro-8-(4-methyl-piperazin-1-yl)-4-oxo-4H-chromene-2-carboxylic acid [4-(4-propionyl-piperazin-1-yl)-phenyl]-amide besylate salt. The present invention also relates to the use of said compounds for the treatment of depression, generalized anxiety, eating disorders, dementia, panic disorder, sleep disorders, gastrointestinal disorders, motor disorders, endocrine disorders, vasospasm, or sexual dysfunction, pharmaceutical compositions containing them and processes for obtaining them.
摘要翻译：本发明涉及6-氟-8-（4-甲基 - 哌嗪-1-基）-4-氧代-4H-色烯-2-羧酸[4-（4-丙酰基 - 哌嗪-1-基） - 基） - 苯基] - 酰胺苯磺酸盐。本发明还涉及所述化合物用于治疗抑郁症，广泛性焦虑症，进食障碍，痴呆症，恐慌症，睡眠障碍，胃肠道疾病，运动障碍，内分泌紊乱，血管痉挛或性功能障碍的用途，含有它们的药物组合物以及获得它们的过程。

5. 发明申请

WO2005012290A1 PIPERIDYL-QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为酪氨酸激酶抑制剂的哌啶 - 喹喔啉衍生物
公开(公告)号：WO2005012290A1
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003259
申请日：2004-07-27
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BRADBURY, Robert, Hugh , HENNEQUIN, Laurent, Francois, Andre , KETTLE, Jason, Grant , MCCABE, James , TURNER, Andrew
发明人： BRADBURY, Robert, Hugh , HENNEQUIN, Laurent, Francois, Andre , KETTLE, Jason, Grant , MCCABE, James , TURNER, Andrew
IPC分类号： C07D401/12
CPC分类号： C04B35/632 , C07D401/12
摘要： The invention concerns quinazoline derivatives of formula (I) wherein R 1 and R 2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB, particularly EGF, receptor tyrosine kinases.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物，其中R 1和R 2具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对erbB特别是EGF受体酪氨酸激酶的抑制敏感的肿瘤中的抗增殖剂的药物中的用途。

6. 发明申请

WO2008075073A1 NOVEL CRYSTALLINE COMPOUND USEFUL AS GLK ACTIVATOR 审中-公开
标题翻译：新型晶体化合物作为GLK激活剂有用
公开(公告)号：WO2008075073A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/004925
申请日：2007-12-20
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , MCCABE, James , TOMKINSON, Gary, Peter
发明人： MCCABE, James , TOMKINSON, Gary, Peter
IPC分类号： C07D403/14 , A61K31/496 , A61P3/10
CPC分类号： C07D403/14
摘要： A novel crystalline form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1-methylethyl)oxy]-N-1H-pyrazol-3-ylbenzamide is described in the specification. This compound is a glucokinase (GLK or GK) activator and useful as a pharmaceutical agent in the treatment or prevention of a disease or medical condition mediated through GLK, leading to a decreased glucose threshold for insulin secretion. Processes for the manufacture of the crystalline form, pharmaceutical compositions comprising the crystalline form and the use of the crystalline form in medical treatment are also described.
摘要翻译： 3 - {[5-（氮杂环丁烷-1-基羰基）吡嗪-2-基]氧基} -5 - [（1-甲基乙基）氧基] -N- 1H-吡唑-3-基苯甲酰胺的新型结晶形式描述于规格。该化合物是葡萄糖激酶（GLK或GK）激活剂，可用作治疗或预防通过GLK介导的疾病或医学病症的药物，导致胰岛素分泌的葡萄糖阈值降低。还描述了用于制造结晶形式的方法，包含结晶形式的药物组合物和在医疗中使用结晶形式。

7. 发明申请

WO2005061488A1 MALEATE SALTS OF A QUINAZOLINE DERIVATIVE USEFUL AS AN ANTIANGIOGENIC AGENT 审中-公开
标题翻译：喹诺酮衍生物作为抗生素代谢物的有效盐
公开(公告)号：WO2005061488A1
公开(公告)日：2005-07-07
申请号：PCT/GB2004/005359
申请日：2004-12-18
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , MCCABE, James
发明人： MCCABE, James
IPC分类号： C07D403/12
CPC分类号： C07D403/12 , A61K31/517 , A61K45/06 , C07C57/145
摘要： The present invention relates to AZD2171 maleate salt, to particular crystalline forms of AZD2171 maleate salt, to processes for their preparation, to pharmaceutical compositions containing them as active ingredient, to their use in the manufacture of medicaments for use in the production of antiangiogenic and/or vascular permeability reducing effects in warm-blooded animals such as humans, and to their use in methods for the treatment of disease states associated with angiogenesis and/or increased vascular permeability.
摘要翻译：本发明涉及AZD2171马来酸盐，AZD2171马来酸盐的特定结晶形式，其制备方法，含有它们作为活性成分的药物组合物，用于制备用于生产抗血管生成和/ 或血管通透性降低效果，以及它们在治疗与血管生成相关的疾病状态和/或增加血管通透性的方法中的用途。

8. 发明申请

WO2006007175A1 GAME FOR THE RULES OF GOLF 审中-公开
标题翻译：高尔夫规则的游戏
公开(公告)号：WO2006007175A1
公开(公告)日：2006-01-19
申请号：PCT/US2005/018104
申请日：2005-05-20
申请人： GOLF EDUCATORS, LLC , THURMAN, Glenn, H. , MCCABE, James
发明人： THURMAN, Glenn, H. , MCCABE, James
IPC分类号： A63F9/18
CPC分类号： G09B19/0038 , A63F9/18 , A63F2001/0491 , G09B3/00
摘要： A game that teaches the rules of golf by presenting questions of hypothetical situations to the players. Each player attempt to answer a question. If the player answers the question correctly, the player receives a score ranging from par to several strokes below par. If the player incorrectly answers the question, the player receives a score ranging from par to several strokes above par. The player's actual score for each hole may be predetermined according to the complexity of the question or may be in part dictated by chance such as by rolling a dice. The player records his score on a scorecard. The game continues until a number of holes or rounds have been played. The score for each player are tallied. The winner is the one who obtains the lowest score.
摘要翻译：通过向玩家呈现假想情境的问题来教导高尔夫规则的游戏。每个玩家尝试回答一个问题。如果玩家正确地回答了问题，玩家会收到一个从par到几个笔画以下的分数。如果玩家错误地回答了问题，玩家会收到一个范围从par到几个笔画以上的分数。玩家的每个洞的实际得分可以根据问题的复杂性而预先确定，或者可以部分地由机会决定，例如通过滚动骰子。玩家将记分记录在记分卡上。游戏继续进行，直到发生了一些孔或圆。每个玩家的得分都计算在内。获胜者是得分最低的人。

9. 发明申请

WO2020016302A1 A XINAFOATE SALT OF A JAK INHIBITING COMPOUND 审中-公开
公开(公告)号：WO2020016302A1
公开(公告)日：2020-01-23
申请号：PCT/EP2019/069252
申请日：2019-07-17
申请人： ASTRAZENECA AB
发明人： PETTERSEN, Anna, Matilda, Angelica , MCCABE, James , AURELL, Carl-Johan
IPC分类号： C07D403/04 , A61P11/06 , A61K31/506
摘要： The present disclosure relates to salts of compounds of Formula (I) prepared as a xinafoate (1-hydroxy-2-naphthoate) salt (Formula (Ia)), pharmaceutically acceptable compositions comprising same and methods of using the same.

10. 发明申请

WO2017050938A1 COMPOUNDS AND METHODS FOR INHIBITING JAK 审中-公开
标题翻译：用于抑制JAK的化合物和方法
公开(公告)号：WO2017050938A1
公开(公告)日：2017-03-30
申请号：PCT/EP2016/072616
申请日：2016-09-22
申请人： ASTRAZENECA AB
发明人： ÅSTRAND, Annika, Birgitta, Margareta , GRIMSTER, Neil, Patrick , KAWATKAR, Sameer , KETTLE, Jason, Grant , NILSSON, Magnus, K. , RUSTON, Linette, Lys , SU, Qibin , VASBINDER, Melissa, Marie , WINTER-HOLT, Jon, James , WU, Dedong , YANG, Wenzhan , GRECU, Tudor , MCCABE, James , WOESSNER, Richard, Donald , CHUAQUI, Claudio, Edmundo
IPC分类号： C07D403/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/14
摘要： Disclosed are compounds of formula (I), pharmaceutical compositions comprising such compounds and methods/uses of using the same, for example, for treating a JAK-related disorder, such as cancer, cancer cachexia or an immune disorder: (I) wherein R 1 is methyl or ethyl; R 2 is selected from methyl, ethyl, methoxy and ethoxy; R 3 is selected from hydrogen, chlorine, fluorine, bromine and methyl; R 4 is selected from methyl, ethyl and -CH 2 OCH 3 ; R 5 and R 6 are each individually methyl or hydrogen; and R 7 is selected from methyl, ethyl, -(CH 2 ) 2 OH and –(CH 2 ) 2 OCH 3 , or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了式（I）化合物，包含这些化合物的药物组合物和使用该化合物的方法/用途，例如用于治疗JAK相关病症，例如癌症，癌症恶病质或免疫病症：（I）其中R1 是甲基或乙基; R2选自甲基，乙基，甲氧基和乙氧基; R3选自氢，氯，氟，溴和甲基; R4选自甲基，乙基和-CH 2 OCH 3; R5和R6各自为甲基或氢; 并且R 7选自甲基，乙基， - （CH 2）2 OH和 - （CH 2）2 OCH 3）或其药学上可接受的盐。

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