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1. 发明申请

US20120142697A1 Salt forms of 4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl) pyrimidin-2-ylamino)phenyl]-benzamide 失效
标题翻译：盐形式的4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺
公开(公告)号：US20120142697A1
公开(公告)日：2012-06-07
申请号：US13368811
申请日：2012-02-08
申请人： Hans Michael Bürger , Paul William Manley , Michael Mutz
发明人： Hans Michael Bürger , Paul William Manley , Michael Mutz
IPC分类号： A61K31/506 , A61P35/00 , A61P35/02 , C07D403/14
CPC分类号： C07D401/04
摘要： The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.
摘要翻译：本发明涉及4 - [（4-甲基-1-哌嗪基）甲基] -N- [4-甲基-3 - [[4-（3-吡啶基）-2-嘧啶基]氨基]苯基的酸加成盐（D）（ - ）酒石酸盐或（L）（+）酒石酸盐，盐酸盐，柠檬酸盐，苹果酸盐等的酒石酸盐，富马酸盐，琥珀酸盐，苯甲酸盐，苯磺酸盐，双羟萘酸盐，甲酸盐，丙二酸盐，1,5-萘二磺酸盐，水杨酸盐，环己烷磺酸盐，乳酸盐，扁桃酸盐盐，戊二酸水杨酸盐，己二酸盐，方酸盐，香草酸盐，草酰乙酸盐，抗坏血酸盐和硫酸盐。

2. 发明授权

US08513256B2 Salt forms of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide 失效
标题翻译：盐形式的4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺
公开(公告)号：US08513256B2
公开(公告)日：2013-08-20
申请号：US13368811
申请日：2012-02-08
申请人： Hans Michael Bürger , Paul William Manley , Michael Mutz
发明人： Hans Michael Bürger , Paul William Manley , Michael Mutz
IPC分类号： A61K31/497 , A61K31/505 , C07D403/14 , C07D239/02 , C07D401/14
CPC分类号： C07D401/04
摘要： The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.
摘要翻译：本发明涉及4 - [（4-甲基-1-哌嗪基）甲基] -N- [4-甲基-3 - [[4-（3-吡啶基）-2-嘧啶基]氨基]苯基的酸加成盐（D）（ - ）酒石酸盐或（L）（+）酒石酸盐，盐酸盐，柠檬酸盐，苹果酸盐等的酒石酸盐，富马酸盐，琥珀酸盐，苯甲酸盐，苯磺酸盐，双羟萘酸盐，甲酸盐，丙二酸盐，1,5-萘二磺酸盐，水杨酸盐，环己烷氨基磺酸盐，乳酸盐，扁桃酸盐盐，戊二酸水杨酸盐，己二酸盐，方酸盐，香草酸盐，草酰乙酸盐，抗坏血酸盐和硫酸盐。

3. 发明申请

US20140051853A1 Salt forms of 4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide 审中-公开
标题翻译：盐形式的4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺
公开(公告)号：US20140051853A1
公开(公告)日：2014-02-20
申请号：US13946000
申请日：2013-07-19
申请人： Hans Michael Bürger , Paul William Manley , Michael Mutz
发明人： Hans Michael Bürger , Paul William Manley , Michael Mutz
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.
摘要翻译：本发明涉及4 - [（4-甲基-1-哌嗪基）甲基] -N- [4-甲基-3 - [[4-（3-吡啶基）-2-嘧啶基]氨基]苯基的酸加成盐（D）（ - ）酒石酸盐或（L）（+）酒石酸盐，盐酸盐，柠檬酸盐，苹果酸盐等的酒石酸盐，富马酸盐，琥珀酸盐，苯甲酸盐，苯磺酸盐，双羟萘酸盐，甲酸盐，丙二酸盐，1,5-萘二磺酸盐，水杨酸盐，环己烷氨基磺酸盐，乳酸盐，扁桃酸盐盐，戊二酸水杨酸盐，己二酸盐，方酸盐，香草酸盐，草酰乙酸盐，抗坏血酸盐和硫酸盐。

4. 发明申请

US20080249104A1 Salt Forms of 4- (4-Methylpiperazin-1-Ylmethyl) -N- [4-Methyl-3- (4-Pyridin-3-Yl) Pyrimidin-2-Ylamino) Phenyl]- Benzamide 审中-公开
标题翻译：盐形式的4-（4-甲基哌嗪-1-基甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶-2-基]氨基）苯基] - 苯甲酰胺
公开(公告)号：US20080249104A1
公开(公告)日：2008-10-09
申请号：US10597287
申请日：2005-02-03
申请人： Hans Michael Burger , Paul William Manley , Michael Mutz
发明人： Hans Michael Burger , Paul William Manley , Michael Mutz
IPC分类号： A61K31/506 , C07D401/14 , A61P35/04
CPC分类号： C07D401/04
摘要： The present invention relates to acid addition salts of 4-[(4-methyl-1-piperazinyl)methyl]-N-(4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide, which are selected from the group consisting of a tartrate salt, such as a (D)(−) tartrate salt or a (L)(+) tartrate salt, a hydrochloride salt, a citrate salt, a malate salt, a fumarate salt, a succinate salt, a benzoate salt, a benzenesulfonate salt, a pamoate salt, a formate salt, a malonate salt, a 1,5-naphthalenedisulfonate salt, a salicylate salt, a cyclohexanesulfamate salt, a lactate salt, a mandelate salt, aq glutarate salt, an adipate salt, a squarate salt, a vanillate salt, an oxaloacetate salt, an ascorbate salt and a sulfate salt.
摘要翻译：本发明涉及4 - [（4-甲基-1-哌嗪基）甲基] -N-（4-甲基-3 - [[4-（3-吡啶基）-2-嘧啶基]氨基]苯基的酸加成盐（D）（ - ）酒石酸盐或（L）（+）酒石酸盐，盐酸盐，柠檬酸盐，苹果酸盐等的酒石酸盐，富马酸盐，琥珀酸盐，苯甲酸盐，苯磺酸盐，双羟萘酸盐，甲酸盐，丙二酸盐，1,5-萘二磺酸盐，水杨酸盐，环己烷氨基磺酸盐，乳酸盐，扁桃酸盐盐，戊二酸水杨酸盐，己二酸盐，方酸盐，香草酸盐，草酰乙酸盐，抗坏血酸盐和硫酸盐。

5. 发明授权

US08846706B2 Crystalline form K of imatinib mesylate 有权
标题翻译：甲磺酸伊马替尼的晶型K
公开(公告)号：US08846706B2
公开(公告)日：2014-09-30
申请号：US13183600
申请日：2011-07-15
申请人： Michael Mutz
发明人： Michael Mutz
IPC分类号： A61K31/505 , C07D401/04 , C07D401/14
CPC分类号： C07D401/04 , C07D401/14
摘要： Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterization are disclosed.
摘要翻译：公开了甲磺酸伊马替尼（F，G，H，I和K）的结晶形式及其各自的表征。

6. 发明授权

US08530522B2 Organic compounds 有权
标题翻译：有机化合物
公开(公告)号：US08530522B2
公开(公告)日：2013-09-10
申请号：US13128825
申请日：2009-11-10
申请人： Guido Jordine , Michael Mutz
发明人： Guido Jordine , Michael Mutz
IPC分类号： A61K31/137 , C07C215/28 , A61P37/06
CPC分类号： C07C215/28 , A61K31/137 , C07B2200/13
摘要： The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.
摘要翻译：本发明涉及2-氨基-2- [2-（4-（C 2 -C 20 - 烷基 - 苯基）乙基]丙烷-1,3-二醇的结晶形式和水合物，特别是在治疗或预防各种自身免疫病症。

7. 发明授权

US08507515B2 Crystalline form G of imatinib mesylate 失效
标题翻译：甲磺酸伊马替尼的结晶形式G.
公开(公告)号：US08507515B2
公开(公告)日：2013-08-13
申请号：US13183557
申请日：2011-07-15
申请人： Michael Mutz
发明人： Michael Mutz
IPC分类号： A61K31/505
CPC分类号： C07D401/04 , C07D401/14
摘要： Crystalline forms of imatinib mesylate (F, G, H, I and K) and their respective characterization are disclosed.
摘要翻译：公开了甲磺酸伊马替尼（F，G，H，I和K）的结晶形式及其各自的表征。

8. 发明申请

US20120115840A1 HEMIFUMARATE SALT OF 1-[4-[1-(4-CYCLOHEXYL-3-TRIFLUOROMETHYL-BENZYLOXYIMINO)-ETHYL]-2-ETHYL-BENZYL]-AZETIDINE-3-CARBOXYLIC ACID 审中-公开
标题翻译： 1- [4- [1-（4-环丙基-3-三氟甲基 - 苯甲酰基） - 乙基] -2-乙基苯基] - 三羟甲基-3-羧酸的盐酸盐
公开(公告)号：US20120115840A1
公开(公告)日：2012-05-10
申请号：US13140478
申请日：2009-12-16
申请人： Lech Ciszewski , Marilyn De La Cruz , Piotr H. Karpinski , Michael Mutz , Christian Riegert , Caspar Vogel , Ricardo Schneeberger
发明人： Lech Ciszewski , Marilyn De La Cruz , Piotr H. Karpinski , Michael Mutz , Christian Riegert , Caspar Vogel , Ricardo Schneeberger
IPC分类号： A61K31/397 , A61P21/00 , A61P37/08 , A61P29/00 , C07D205/04 , A61P37/06
CPC分类号： C07D205/04 , A61K31/397 , C07C57/15
摘要： This invention relates to a hemifumarate salt of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this salt, to processes for forming this salt and to its use in medical treatment. In addition, the present invention also relates to new polymorphic forms of the hemifumarate salt form of Compound I, as well as to pharmaceutical compositions comprising these polymorphic forms, to processes for obtaining them, and their use in medical treatment.
摘要翻译：本发明涉及1-（4- {1 - [（E）-4-环己基-3-三氟甲基 - 苄氧亚氨基] - 乙基} -2-乙基 - 苄基） - 氮杂环丁烷-3-羧酸的半富马酸盐 I），包含该盐的药物组合物，用于形成该盐的方法及其在医疗中的用途。此外，本发明还涉及化合物I的半富马酸盐形式的新多晶形式，以及包含这些多晶型形式的药物组合物，其获得方法及其在医疗中的用途。

9. 发明授权

US08163747B2 Acid addition salts, hydrates and polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide and formulations comprising these forms 有权
标题翻译： 5-（2,4-二羟基-5-异丙基 - 苯基）-4-（4-吗啉-4-基甲基 - 苯基） - 异恶唑-3-甲酸乙酰胺的酸加成盐，水合物和多晶型物和包含这些形式的制剂
公开(公告)号：US08163747B2
公开(公告)日：2012-04-24
申请号：US12529090
申请日：2008-02-28
申请人： Martin James Drysdale , Brian William Dymock , Christoph Krell , Michael Mutz , Holger Petersen , Weijia Zheng
发明人： Martin James Drysdale , Brian William Dymock , Christoph Krell , Michael Mutz , Holger Petersen , Weijia Zheng
IPC分类号： A61K31/535 , C07D413/10
CPC分类号： C07D295/155 , A61K31/5377 , C07D261/18
摘要： The present invention relates to new salt forms of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide, in particular the mesylate, hydrochloride, tartrate, phosphate and hemi fumarate salt thereof; to crystalline forms of such salts; to polymorphs of 5-(2,4-dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide; to hydrates and polymorphs of the new salt forms mentioned above; to the use of the new salt forms mentioned above for the manufacture of a medicament for the treatment of a disorder mediated by Hsp90; to a method for treating a disorder mediated by Hsp90 using the new salt forms; to formulations comprising such salt forms, in particular aqueous solutions suitable for intravenous administration; and to amber glass containers being filled with such formulations.
摘要翻译：本发明涉及5-（2,4-二羟基-5-异丙基 - 苯基）-4-（4-吗啉-4-基甲基 - 苯基） - 异恶唑-3-甲酸乙酰胺的新盐形式，特别是甲磺酸盐，盐酸盐，酒石酸盐，磷酸盐和半富马酸盐; 到这种盐的结晶形式; 5-（2,4-二羟基-5-异丙基 - 苯基）-4-（4-吗啉-4-基甲基 - 苯基） - 异恶唑-3-甲酸乙酰胺的多晶型物; 到上述新盐形式的水合物和多晶型物; 使用上述新的盐形式来制备用于治疗由Hsp90介导的病症的药物; 涉及使用新的盐形式治疗由Hsp90介导的病症的方法; 包括这种盐形式的制剂，特别是适于静脉内施用的水溶液; 以及填充这种制剂的琥珀色玻璃容器。

10. 发明申请

US20120015027A1 F, G, H, I and K Crystal Forms of Imatinib Mesylate 失效
标题翻译： F，G，H，I和K晶型的伊马替尼甲磺酸盐
公开(公告)号：US20120015027A1
公开(公告)日：2012-01-19
申请号：US13183557
申请日：2011-07-15
申请人： Michael Mutz
发明人： Michael Mutz
IPC分类号： A61K31/506 , A61P35/02 , A61P35/04 , C07D401/14 , A61K9/48
CPC分类号： C07D401/04 , C07D401/14
摘要： The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, certain processes for their preparation, pharmaceutical compositions containing these crystal forms, their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.
摘要翻译：本发明涉及4-（4-甲基哌嗪-1-基甲基）-N-甲基-3-甲基苯磺酸的甲磺酸加成盐的F晶型，G晶型，H型晶型，I-晶型和K-晶型， [4-甲基-3-（4-（吡啶-3-基）嘧啶-2-基氨基）苯基] - 苯甲酰胺，其制备方法，含有这些晶体形式的药物组合物，其在诊断方法或治疗中的用途治疗温血动物，以及其用作中间体或用于制备用于诊断方法或用于治疗温血动物，特别是人的药物制剂的用途。

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