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11. 发明申请

WO2007147480A3 POLYMORPHIC FORMS AND PROCESS 审中-公开
标题翻译：多形态和过程
公开(公告)号：WO2007147480A3
公开(公告)日：2008-05-08
申请号：PCT/EP2007004711
申请日：2007-05-26
申请人： MERCK PATENT GMBH , SCHIEMANN KAI , EMDE ULRICH , SCHLUETER TOBIAS , SAAL CHRISTOPH , MAIWALD MICHAEL
发明人： SCHIEMANN KAI , EMDE ULRICH , SCHLUETER TOBIAS , SAAL CHRISTOPH , MAIWALD MICHAEL
IPC分类号： C07D491/04 , A61K31/436 , A61P35/02
CPC分类号： C07D491/04
摘要： The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula (I) wherein R 1 , R 2 , R 3 , R 6 , R 7 and Q are defined as in claim 1 as well as their crystalline forms for the treatment of proliferative diseases such as cancer.
摘要翻译：本发明涉及制备对映体富集或纯化的式（I）化合物的方法，其中R 1，R 2，R 3， R 6，R 7和Q如权利要求1中所定义，以及它们用于治疗增殖性疾病例如癌症的结晶形式。

12. 发明申请

WO2010078897A1 NOVEL POLYMORPHIC FORMS OF 3-(1-{3-[5-(1-METHYL-PIPERIDIN-4YLMETHOXY)-PYRIMIDIN-2-YL]-BENZYL}-6-OXO-1,6-DIHYDRO-PYRIDAZIN-3-YL)-BENZONITRILE HYDROCHLORIDE SALT AND PROCESSES OF MANUFACTURING THEREOF 审中-公开
标题翻译： 3-（1- {3- [5-（1-甲基 - 哌啶-4-基）甲基） - 嘧啶-2-基] - 苯基} -6-氧代-1,6-二氢吡啶-3-基的新型多晶型） - 苯并盐酸盐及其制备方法
公开(公告)号：WO2010078897A1
公开(公告)日：2010-07-15
申请号：PCT/EP2009/008684
申请日：2009-12-04
申请人： MERCK PATENT GMBH , BECKER, Axel , KUEHN, Clemens , SAAL, Christoph , SCHADT, Oliver , DORSCH, Dieter , BOKEL, Heinz-Hermann , STIEBER, Frank , DONINI, Christina
发明人： BECKER, Axel , KUEHN, Clemens , SAAL, Christoph , SCHADT, Oliver , DORSCH, Dieter , BOKEL, Heinz-Hermann , STIEBER, Frank , DONINI, Christina
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： A61K31/506 , A61K31/517 , A61K45/06 , C07D401/14 , C07D403/10
摘要： The present invention relates to hydrochloride solvates of 3-(1-{3-[5-(1-methyl-piperidin-4-ylmethoxy)-pyrimidin-2-yl]-benzyl}-6-oxo-1,6-dihydro-pyridazin-3-yl)-benzonitrile and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by the inhibition, regulation and/or modulation of signal transduction of kinases, in particular by the inhibition of tyrosine kinases, e.g. pathophysiological conditions such as cancer.
摘要翻译：本发明涉及3-（1- {3- [5-（1-甲基 - 哌啶-4-基甲氧基） - 嘧啶-2-基] - 苄基} -6-氧代-1,6-二氢 - 哒嗪-3-基） - 苄腈及其结晶修饰物。本发明进一步涉及制造这些结晶修饰的方法及其在治疗和/或预防生理和/或病理生理条件中的用途，其通过抑制，调节和/或调节引起，介导和/或传播的激酶的信号转导，特别是通过抑制酪氨酸激酶，例如病理生理条件如癌症。

13. 发明申请

WO2010133367A3 NOVEL SOLID MATERIALS OF {[2S, 5R,8S,11S)-5-BENZYL-11-(3-GUANIDINO-PROPYL)-8-ISOPROPYL-7-METHYL-3,6,9,12,15-PENTAOXO-1,4,7,10,13-PENTAAZA-CYCLOPENTADEC-2-YL]-ACETIC ACID} AND METHODS FOR OBTAINING THEM 审中-公开
标题翻译： {[2S，5R，8S，11S）-5-苄基-11-（3-胍基 - 丙基）-8-异丙基-7-甲基-3,6,9,12,15-戊氧羰基-1 ，4,7,10,13-PENTAAZA-CYCLOPENTADEC-2-YL] - 酸性酸]和获得它们的方法
公开(公告)号：WO2010133367A3
公开(公告)日：2011-10-27
申请号：PCT/EP2010003100
申请日：2010-05-20
申请人： MERCK PATENT GMBH , JONCZYK ALFRED , KUEHN CLEMENS , SEEMANN KERSTIN , SAAL CHRISTOPH , SCHOLZ GERALD , PETERSEN SOENKE , UNTENECKER HARALD , LANGE MICHAEL
发明人： JONCZYK ALFRED , KUEHN CLEMENS , SEEMANN KERSTIN , SAAL CHRISTOPH , SCHOLZ GERALD , PETERSEN SOENKE , UNTENECKER HARALD , LANGE MICHAEL
IPC分类号： C07K7/64 , A61K38/12 , A61P35/00
CPC分类号： C07K7/64 , A61K38/00
摘要： The instant invention relates to novel solid materials of {[(2S,5R,8S,11S)-5-Benzyl-11-(3-guanidino-propyl)-8-isopropyl-7-methyl-3,6,9,12,15-pentaoxo-1,4,7,10,13-pentaaza-cyclopentadec-2-yl]-acetic acid}, methods for producing them, and the use of said solid materials in pharmaceuticals.
摘要翻译：本发明涉及{[（2S，5R，8S，11S）-5-苄基-11-（3-胍基 - 丙基）-8-异丙基-7-甲基-3,6,9,12 ，15-五氧代-1,4,7,10,13-五氮杂 - 环戊烷-2-基] - 乙酸}，其制备方法和所述固体材料在药物中的用途。

14. 发明申请

WO2011047767A1 NOVEL POLYMORPHIC FORMS OF (S)-2-[-4-(3-FLUORO-BENZYLOXY)-BENZYLAMINO]-PROPIONAMIDE MESYLATE SALT AND PROCESSES OF MANUFACTURING THEREOF 审中-公开
标题翻译：（S）-2 - [ - 4-（3-氟 - 苄基） - 苯甲酰胺] - 丙二酰胺盐酸盐的新型多晶型及其制备方法
公开(公告)号：WO2011047767A1
公开(公告)日：2011-04-28
申请号：PCT/EP2010/005824
申请日：2010-09-23
申请人： MERCK PATENT GMBH , SCHLUETER, Doris , SAAL, Christoph , KUEHN, Clemens , SCHLUETER, Tobias
发明人： SCHLUETER, Doris , SAAL, Christoph , KUEHN, Clemens , SCHLUETER, Tobias
IPC分类号： C07C237/06 , A61K31/165 , A61P25/00
CPC分类号： C07C237/06
摘要： The present invention relates to (S)-2-[4-(3-Fluoro-benzyloxy)-benzylamino]- propionamide mesylate anhydrate and crystalline modifications thereof. The present invention further relates to processes of manufacturing these crystalline modifications as well as their use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions selected from the group consisting of "central nervous system disorders, epilepsy, Parkinson's disease, neurodegenerative processes, depression, spasm, hypnosis, analgesia, chronic pain, neuropathic pain, head pain conditions, migraine, headache, cluster headache, neuralgia, hemicrania, facial pain, arachnoiditis, severe headache, restless legs syndrome, addictive disorders, motor restlessness, creeping, burning, pulling sensations, drug abuse, severe alcoholism, reward deficiency syndrome, cognitive disorders, autism, dyslexia, attention deficit hyperactivity disorder, anxiety, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorder, Tourette's syndrome, mild cognitive impairment and disorders of learning in children, adolescents and adults, age associated memory impairment, age associated cognitive decline, Alzheimer's disease, Down's Syndrome, traumatic brain injury Huntington's disease, progressive supranuclear Palsy, HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis".
摘要翻译：本发明涉及（S）-2- [4-（3-氟 - 苄氧基） - 苄氨基] - 丙酰胺甲磺酸盐水合物及其结晶修饰物。本发明还涉及制造这些结晶修饰物的方法及其在治疗和/或预防选自“中枢神经系统疾病，癫痫，帕金森病，神经退行性过程中的生理和/或病理生理状况”中的用途，抑郁症，痉挛，催眠，镇痛，慢性疼痛，神经性疼痛，头痛症状，偏头痛，头痛，头痛，神经痛，血红素，面部疼痛，蛛网膜炎，严重头痛，不宁腿综合症，上瘾症，运动不安，灼热，拉扯感觉，药物滥用，严重酒精中毒，奖励缺陷综合征，认知障碍，自闭症，阅读障碍，注意力缺陷多动障碍，焦虑症，精神分裂症，强迫症，精神病，双相情感障碍，Tourette综合征，轻度认知障碍和学习障碍在儿童，青少年和成年人中，年龄与我相关多发性神经损伤，年龄相关认知衰退，阿尔茨海默病，唐氏综合征，创伤性脑损伤亨廷顿舞蹈病，进行性核上性麻痹，艾滋病毒，中风，血管疾病，Pick's或Creutzfeldt-Jacob疾病，多发性硬化症“。

15. 发明申请

WO2007147480A2 POLYMORPHIC FORMS AND PROCESS 审中-公开
标题翻译：多形态和过程
公开(公告)号：WO2007147480A2
公开(公告)日：2007-12-27
申请号：PCT/EP2007/004711
申请日：2007-05-26
申请人： MERCK PATENT GMBH , SCHIEMANN, Kai , EMDE, Ulrich , SCHLUETER, Tobias , SAAL, Christoph , MAIWALD, Michael
发明人： SCHIEMANN, Kai , EMDE, Ulrich , SCHLUETER, Tobias , SAAL, Christoph , MAIWALD, Michael
IPC分类号： C07D491/04 , A61K31/436 , A61P35/02
CPC分类号： C07D491/04
摘要： The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula (I) wherein R 1 , R 2 , R 3 , R 6 , R 7 and Q are defined as in claim 1 as well as their crystalline forms for the treatment of proliferative diseases such as cancer.
摘要翻译：本发明涉及制备对映体富集或纯化的式（I）化合物的方法，其中R 1，R 2，R 3， R 6，R 7和Q如权利要求1中所定义，以及它们用于治疗增殖性疾病例如癌症的结晶形式。

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