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1. 发明申请

WO2010133367A2 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：WO2010133367A2
公开(公告)日：2010-11-25
申请号：PCT/EP2010/003100
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
CPC分类号： C07K7/64 , A61K38/00
摘要： The instant invention relates to novel solid materials of {[(2S,5R,8S,11 S)-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， 12,15-五氧杂-1,4,7,10,13-五氮杂 - 环十五烷-2-基] - 乙酸}，其制备方法和所述固体材料在药物中的用途。

2. 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。

3. 发明申请

WO2010072295A1 NOVEL POLYMORPHIC FORMS OF 6-(1-METHYL-1H-PYRAZOL-4-YL)-2-{3-[5-(2-MORPHOLIN-4-YL-ETHOXY)-PYRIMIDIN-2-YL]-BENZYL}-2H-PYRIDAZIN-3-ONE DIHYDROGENPHOSPHATE AND PROCESSES OF MANUFACTURING THEREOF 审中-公开
标题翻译： 6-（1-甲基-1H-吡唑-4-基）-2- {3- [5-（2-吗啉-4-基 - 乙氧基） - 嘧啶-2-基] - 苯基} - 的新型多晶型 2H-吡啶-3-酮二氢异氰酸酯及其制备方法
公开(公告)号：WO2010072295A1
公开(公告)日：2010-07-01
申请号：PCT/EP2009/008358
申请日：2009-11-24
申请人： MERCK PATENT GMBH , BECKER, Axel , KUEHN, Clemens , SAAL, Christoph , SCHADT, Oliver , DORSCH, Dieter , KRIEGBAUM, Eva , STIEBER, Frank , DONINI, Cristina
发明人： BECKER, Axel , KUEHN, Clemens , SAAL, Christoph , SCHADT, Oliver , DORSCH, Dieter , KRIEGBAUM, Eva , STIEBER, Frank , DONINI, Cristina
IPC分类号： C07D403/14 , A61K31/506 , A61P35/02
CPC分类号： C07D403/14
摘要： The present invention relates to 6-(1-methyl-1 H-pyrazol-4-yl)-2-{3-[5-(2-morpholin- 4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2H-pyridazin-3-one dihydrogenphosphate, its solvates 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6-（1-甲基-1H-吡唑-4-基）-2- {3- [5-（2-吗啉-4-基 - 乙氧基） - 嘧啶-2-基] - 苄基 } -2H-哒嗪-3-酮磷酸二氢盐，其溶剂合物及其结晶修饰物。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。

4. 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“。

5. 发明申请

WO2010034384A1 NEUE KRISTALLFORM VON CALCIUM-3-ACETYLAMINOPROPAN-1-SULFONAT 审中-公开
标题翻译：钙-3- ACETYLAMINOPROPAN -1-磺酸盐的新晶型
公开(公告)号：WO2010034384A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/006150
申请日：2009-08-25
申请人： MERCK PATENT GMBH , MUERMANN, Antje , KUEHN, Clemens , BARTELS, Matthias , SAAL, Christoph , BOSC, Nathalie
发明人： MUERMANN, Antje , KUEHN, Clemens , BARTELS, Matthias , SAAL, Christoph , BOSC, Nathalie
IPC分类号： A61K31/185 , C07C309/15
CPC分类号： C07C309/15 , C07B2200/13
摘要： Die vorliegende Erfindung betrifft eine neue Kristallform von Calcium-3- Acetylaminopropan-1-sulfonat. Verfahren zu ihrer Herstellung sowie ihre Verwendung in Arzeneimitteln.
摘要翻译：本发明涉及钙3- Acetylaminopropan -1-磺酸盐的新结晶形式。其制备方法及其在Arzeneimitteln使用。

6. 发明申请

WO2011091839A1 LEUCHTSTOFFE 审中-公开
标题翻译：荧光粉
公开(公告)号：WO2011091839A1
公开(公告)日：2011-08-04
申请号：PCT/EP2010/007954
申请日：2010-12-28
申请人： MERCK PATENT GMBH , WINKLER, Holger , BARNEKOW, Peter , KUEHN, Clemens , PETRY, Ralf , VOSGROENE, Tim , JUESTEL, Thomas , UHLICH, Dominik , KATELNIKOVAS, Arturas , DUTCZAK, Danuta
发明人： WINKLER, Holger , BARNEKOW, Peter , KUEHN, Clemens , PETRY, Ralf , VOSGROENE, Tim , JUESTEL, Thomas , UHLICH, Dominik , KATELNIKOVAS, Arturas , DUTCZAK, Danuta
IPC分类号： C09K11/59
CPC分类号： C09K11/7734 , C09K11/0883
摘要： Die Erfindung betrifft Verbindungen der Formel (I), A 2-0,5y-χ Eu x Si 5 N 8-y O y (I), wobei A steht für ein oder mehrere Elemente ausgewählt aus Ca, Sr, Ba und x steht für einen Wert aus dem Bereich von 0,005 bis 1 und y steht für einen Wert aus dem Bereich von 0,01 bis 3, Mischungen davon, Verfahren zur Herstellung dieser Leuchtstoffe und Mischungen und deren Verwendung als Konversionsleuchtstoffe.
摘要翻译：本发明涉及式（I），A2-0,5y-的化合物？ EUX SI5 N8-Y Oy公司（I）其中A表示选自Ca中的一种或多种元素，Sr，Ba和x是0.005〜1和y的值是从0范围内的值， 01-3，它们的混合物，用于制备这些磷光体及其混合物以及它们作为转换的荧光体使用。

7. 发明申请

WO2017137147A1 CRYSTALLINE MODIFICATIONS OF N-(4,5-BISMETHANESULFONYL-2-METHYLBENZOYL)GUANIDINE HYDROCHLORIDE AND N-(4,5-BISMETHANESULFONYL-2-METHYLBENZOYL)GUANIDINE SALTS 审中-公开
标题翻译： N-（4,5-BISMETHANESULFONYL-2-METHYLBENZOYL）胍盐酸盐和N-（4,5-BISMETHANESULFONYL-2-METHYLBENZOYL）胍盐的结晶改性
公开(公告)号：WO2017137147A1
公开(公告)日：2017-08-17
申请号：PCT/EP2017/000102
申请日：2017-01-27
申请人： MERCK PATENT GMBH
发明人： BECKER, Axel , GALLON, Gilmary , SAAL, Christoph , KUEHN, Clemens
IPC分类号： C07C315/06 , C07C317/44 , A61K31/155
CPC分类号： C07C317/44 , A61K31/155 , C07B2200/13
摘要： The present invention relates to novel crystalline modifications of N-(4,5- bismethanesulfonyl-2-methylbenzoyl)guanidine hydrochloride, novel N-(4,5- bismethanesulfonyl-2-methylbenzoyl)guanidine salts and their crystalline modifications and processes of manufacturing and pharmaceutical formulations thereof.
摘要翻译：本发明涉及N-（4,5-双甲磺酰基-2-甲基苯甲酰基）盐酸胍，新颖的N-（4,5-双甲磺酰基-2-甲基苯甲酰基）胍盐和它们的结晶变体和制造过程及其药物制剂。

8. 发明申请

WO2023036873A1 SAMPLE HOLDER ARRANGEMENT FOR STRUCTURE ELUCIDATION WITH POROUS FRAMEWORKS 审中-公开
公开(公告)号：WO2023036873A1
公开(公告)日：2023-03-16
申请号：PCT/EP2022/074995
申请日：2022-09-08
申请人： MERCK PATENT GMBH , RIGAKU CORPORATION
发明人： JENNICHES, Judith , KUEHN, Clemens , SATO, Takashi
IPC分类号： G01N23/20025 , G01N23/207
摘要： The invention provides a sample holder arrangement (1) comprising (a) a sample holding part (3) and (b) a base part (30), wherein the sample holding part (3) comprises an open-ended tube (10), wherein the open-ended tube (10) comprises a first tube end (11) and a second tube end (19), wherein the open-ended tube (10) comprises a narrowing part (15), wherein in the narrowing part (15) an internal tube dimension reduces in a direction from the first tube end (11) to the second tube end (19), wherein a single crystal of a porous framework (20) is arranged within the open-ended tube (10) between the first tube end (11) and the second tube end (19), and wherein dimensions of the narrowing part (15) and dimensions of the single crystal of the porous framework (20) are chosen such that the single crystal of the porous framework (20) cannot escape from the open-ended tube (10) via the second tube end (19); and wherein the base part (30) is configured to host the sample holding part (3), wherein the sample holding part (3) is detachably associated to the base part (30).

9. 发明申请

WO2018178133A1 SOLID FORM OF (S)-[2-CHLORO-4-FLUORO-5-(7-MORPHOLIN-4-YLQUINAZOLIN-4-YL)PHENYL]-(6-METHOXY-PYRIDAZIN-3-YL)METHANOL 审中-公开
公开(公告)号：WO2018178133A1
公开(公告)日：2018-10-04
申请号：PCT/EP2018/057875
申请日：2018-03-28
申请人： MERCK PATENT GMBH
发明人： LANGE, Michael , KUEHN, Clemens , FUCHSS, Thomas , MAILLARD, David , BREUNING, Marcel , POMA, Marco , BURINI, Edoardo
IPC分类号： C07D403/10 , A61P35/00
摘要： The present invention relates to anhydrous disordered crystalline (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)methanol, as well as a method of making same, and pharmaceutical compositions and medical uses thereof.

10. 发明申请

WO2022152879A1 SOLVATED CRYSTALLINE POLYNUCLEAR METAL COMPLEX SOLVATED WITH A MIXTURE OF NON-POLAR AND POLAR SOLVENTS, SUCH SOLVATED CRYSTALLINE POLYNUCLEAR METAL COMPLEX INCLUDING A GUEST COMPOUND ANALYTE AND ITS USE IN A METHOD FOR DETERMINING MOLECULAR STRUCTURE OF THE GUEST COMPOUND ANALYTE 审中-公开
公开(公告)号：WO2022152879A1
公开(公告)日：2022-07-21
申请号：PCT/EP2022/050796
申请日：2022-01-14
申请人： MERCK PATENT GMBH
发明人： KUEHN, Clemens
IPC分类号： C07F3/00 , G01N23/00 , G01N23/20
摘要： The present invention is directed to solvated crystalline polynuclear metal complexeswhich solvation is with a polar solvent or a mixture of polar and non-polar solvent. These polar solvated crystalline metal complexes of the present invention can absorb an analyte guest compound, including an polar analyte guest compound, to form a crystal structure analysis sample. The molecular structure of the analyte guest compound can be determined by X-ray crystallography using the crystal structure analysis sample obtained with such solvated crystalline polynuclear metal complexes.

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