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1. 发明申请

WO2003105837A1 CALCIUM SALTS OF INDOLE DERIVED STATINS 审中-公开
标题翻译：单位衍生统计的钙盐
公开(公告)号：WO2003105837A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/006195
申请日：2003-06-12
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , CHEN, Guang-Pei , KAPA, Prasad, Koteswara , SUTTON, Paul, Allen
发明人： CHEN, Guang-Pei , KAPA, Prasad, Koteswara , SUTTON, Paul, Allen
IPC分类号： A61K31/405
CPC分类号： C07D209/24
摘要： The present invention provides calcium salts of indole derived statins of the formula (IA) wherein R 1 , is alkyl, cycloalkyl or aralkyl; R 2 , R 3 and R 4 are independently hydrogen, halogen or alkyl; R 5 and R 6 are independently hydrogen, halogen, alkyl, cycloalkyl, aralkyl, alkoxy or aralkoxy; and the hydroxyl group at the 3position is in the R-configuration and at the 5position in the S-configuration; or an enantiomer thereof; or a hydrate thereof; as obtainable by the methods of the present invention. More specifically, the invention provides a calcium salt of formula (IA) wherein R 1 , is isopropyl, R 2 is fluorine and R 3 , R 4 R 5 and R 6 are hydrogen, designated herein as Fluvastatin calcium, in a highly crystalline form. Furthermore, the present invention is directed to methods for the preparation of the crystalline Fluvastatin calcium, and to pharmaceutical compositions comprising the crystalline form.
摘要翻译：本发明提供式（IA）的吲哚衍生的他汀类钙盐，其中R 1是烷基，环烷基或芳烷基; R2，R3和R4独立地是氢，卤素或烷基; R5和R6独立地是氢，卤素，烷基，环烷基，芳烷基，烷氧基或芳烷氧基; 并且3位上的羟基处于R-构型，在5-构型中为5位; 或其对映体; 或其水合物; 如通过本发明的方法可获得的。更具体地，本发明提供式（IA）的钙盐，其中R 1是异丙基，R 2是氟，并且R 3，R 4 R 5和R 6是氢，在本文中称为氟伐他汀钙，为高度结晶形式。此外，本发明涉及制备结晶氟伐他汀钙的方法以及包含结晶形式的药物组合物。

2. 发明申请

WO2003087038A1 CRYSTAL FORMS OF N-(TRANS-4-ISOPROPYLCYCLOHEXYLCARBONYL)-D-PHENYLALANINE 审中-公开
标题翻译： N-（反式-4-异丙基环戊二烯基） - 苯甲酰胺的晶体形式
公开(公告)号：WO2003087038A1
公开(公告)日：2003-10-23
申请号：PCT/EP2003/003864
申请日：2003-04-14
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , SUTTON, Paul, Allen
发明人： SUTTON, Paul, Allen
IPC分类号： C07C233/63
CPC分类号： C07C233/63 , C07B2200/13 , C07C231/22 , C07C2601/14
摘要： New crystal forms of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine, also known as nateglinide, may be produced by dissolving nateglinide in any of its forms, including solvates, in an organic solvent to form a solution followed by precipitation of nateglinide from the solution, and isolating and drying the precipitated crystal form of nateglinide. The precipitation of nateglinide may be induced either by cooling the solution, or by addition of another solvent which is miscible with the first solvent but in which nateglinide is only poorly soluble, or by combination of the two. Depending on the solvent a specific crystal form of nateglinide may be obtained, e.g., the R'-type crystal form of nateglinide produced by the described method has a different melting point, infra red spectra and X-ray diffraction patterns from the previously known crystal forms of nateglinide.
摘要翻译： N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（也称为那格列奈）的新结晶形式可以通过将那格列奈以任何形式（包括溶剂化物）溶解在有机溶剂中来形成溶液，然后沉淀那格列奈，并分离和干燥那格列奈沉淀的晶体形式。那格列奈的沉淀可以通过冷却溶液，或通过加入与第一溶剂混溶但其中那格列奈仅溶于难溶性的另一种溶剂，或通过两者的组合来诱导。取决于溶剂，可以获得那格列奈的特定结晶形式，例如，通过所述方法制备的那格列奈的R'型晶型具有不同的熔点，红外光谱和来自先前已知的晶体的X射线衍射图那格列奈的形式

3. 发明申请

WO2007015870A2 CRYSTALLINE FORMS OF 4-METHYL-N-[3-(4-METHYL-IMIDAZOL-1-YL)-5-TRIFLUOROMETHYL-PHENYL]-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-BENZAMIDE 审中-公开
标题翻译： 4-甲基-N- [3-（4-甲基 - 咪唑-1-基）-5-三氟甲基 - 苯基] -3-（4-吡啶-3-基 - 嘧啶-2-基氨基）苯甲酰胺的结晶形式
公开(公告)号：WO2007015870A2
公开(公告)日：2007-02-08
申请号：PCT/US2006/027875
申请日：2006-07-18
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , MANLEY, Paul, W. , SHIEH, Wen-Chung , SUTTON, Paul, Allen , KARPINSKI, Piotr, H. , WU, Raeann , MONNIER, Stéphanie , BROZIO, Jörg
发明人： MANLEY, Paul, W. , SHIEH, Wen-Chung , SUTTON, Paul, Allen , KARPINSKI, Piotr, H. , WU, Raeann , MONNIER, Stéphanie , BROZIO, Jörg
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14
摘要： Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.
摘要翻译：（4-甲基 - 咪唑-1-基）-5-三氟甲基 - 苯基] -3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯甲酰胺游离碱及其盐通过各种方法制备。

4. 发明申请

WO2007056546A1 PHARMACEUTICAL COMBINATIONS OF AN ANGIOTENSIN RECEPTOR ANTAGONIST AND AN NEP INHIBITOR 审中-公开
标题翻译： ANGIOTENSIN受体拮抗剂和NEP抑制剂的药物组合
公开(公告)号：WO2007056546A1
公开(公告)日：2007-05-18
申请号：PCT/US2006/043710
申请日：2006-11-08
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FENG, Lili , GODTFREDSEN, Sven, Erik , KARPINSKI, Piotr , SUTTON, Paul, Allen , PRASHAD, Mahavir , GIRGIS, Michael, J. , HU, Bin , LIU, Yugang
发明人： FENG, Lili , GODTFREDSEN, Sven, Erik , KARPINSKI, Piotr , SUTTON, Paul, Allen , PRASHAD, Mahavir , GIRGIS, Michael, J. , HU, Bin , LIU, Yugang
IPC分类号： A61K31/216 , A61K31/41 , A61P3/10 , A61P9/00 , A61P9/10
CPC分类号： A61K31/216 , A61K31/41 , A61K31/4422 , A61K31/5415 , A61K45/06 , A61K2300/00 , C07C233/47 , C07D207/50 , C07D257/04
摘要： A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.
摘要翻译：联合的原药或血管紧张素受体拮抗剂和NEPi的化合物用于治疗高血压。

5. 发明申请

WO2007015871A1 SALTS OF 4-METHYL-N-[3-(4-METHYL-IMIDAZOL-1-YL)-5-TRIFLUOROMETHYL-PHENYL]-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-BENZAMIDE 审中-公开
标题翻译： 4-甲基-N- [3-（4-甲基咪唑-1-基）-5-三氟甲基苯基] -3-（4-吡啶-3-基） - 吡咯烷-2-基氨基] - 苯甲酰胺的盐
公开(公告)号：WO2007015871A1
公开(公告)日：2007-02-08
申请号：PCT/US2006/027878
申请日：2006-07-18
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , MANLEY, Paul, W. , SHIEH, Wen-Chung , SUTTON, Paul, Allen , KARPINSKI, Piotr, H. , WU, Raeann , MONNIER, Stéphanie , BROZIO, Jörg
发明人： MANLEY, Paul, W. , SHIEH, Wen-Chung , SUTTON, Paul, Allen , KARPINSKI, Piotr, H. , WU, Raeann , MONNIER, Stéphanie , BROZIO, Jörg
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14
摘要： Salts of 4-methyl-N-[3-(4-methyl-imidazol-l-yl)-5-trifluoromethyl-phenyl]-3-(4- pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.
摘要翻译： 4-甲基-N- [3-（4-甲基 - 咪唑-1-基）-5-三氟甲基 - 苯基] -3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯甲酰胺的盐为由各种过程准备。

6. 发明申请

WO2003076393A1 SALTS OF NATEGLINIDE 审中-公开
标题翻译： NATEGLINIDE的销售
公开(公告)号：WO2003076393A1
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002447
申请日：2003-03-10
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , SUTTON, Paul, Allen , VIVILECCHIA, Richard, Victor , PARKER, David, John , DE LA CRUZ, Marilyn
发明人： SUTTON, Paul, Allen , VIVILECCHIA, Richard, Victor , PARKER, David, John , DE LA CRUZ, Marilyn
IPC分类号： C07C233/63
CPC分类号： A61K31/192 , C07C233/63 , C07C2601/14
摘要： The present invention relates to salts of organic acid, in particular salt of nateglinide, combined preparations comprising one or more salts of nateglinide and, optionally, one or more additional ingredients and the use thereof in pharmaceutical compositions for preventing or treating diabetes, cardiovascular diseases, or conditions associated therewith.
摘要翻译：本发明涉及有机酸的盐，特别是那格列奈的盐，包含那格列奈的一种或多种盐，任选的一种或多种另外的成分的组合制剂及其用于预防或治疗糖尿病，心血管疾病的药物组合物中的用途，或与之相关的条件。

7. 发明公开

EP1910336A1 SALTS OF 4-METHYL-N-[3-(4-METHYL-IMIDAZOL-1-YL)-5-TRIFLUOROMETHYL-PHENYL]-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-BENZAMIDE 有权转让
标题翻译： 4-甲基-N- [3-（4-甲基咪唑-1-基）-5-三氟甲基苯基] -3-（4-吡啶-3-基 - 嘧啶-2-基）氨基] - 苯甲酰基 - 单乙基氯化物 - MONOHYDRAT-SALZ
公开(公告)号：EP1910336A1
公开(公告)日：2008-04-16
申请号：EP06787733.2
申请日：2006-07-18
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： MANLEY, Paul, W. , SHIEH, Wen-Chung , SUTTON, Paul, Allen , KARPINSKI, Piotr, H. , WU, Raeann , MONNIER, Stéphanie , BROZIO, Jörg
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14
摘要： Salts of 4-methyl-N-[3-(4-methyl-imidazol-l-yl)-5-trifluoromethyl-phenyl]-3-(4- pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.

8. 发明授权

EP1910336B1 MONOHYDROCHLORIDE MONOHYDRATE SALT OF 4-METHYL-N-[3-(4-METHYL-IMIDAZOL-1-YL)-5-TRIFLUOROMETHYL-PHENYL]-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-BENZAMIDE 有权转让
标题翻译： 4-甲基-N- [3-（4-甲基 - 咪唑-1-基）-5-三氟甲基 - 苯基] -3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯甲酰胺单盐酸盐盐一水合物
公开(公告)号：EP1910336B1
公开(公告)日：2011-06-29
申请号：EP06787733.2
申请日：2006-07-18
申请人： Novartis AG , Novartis Pharma GmbH
发明人： MANLEY, Paul, W. , SHIEH, Wen-Chung , SUTTON, Paul, Allen , KARPINSKI, Piotr, H. , WU, Raeann , MONNIER, Stéphanie , BROZIO, Jörg
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14
摘要： Salts of 4-methyl-N-[3-(4-methyl-imidazol-l-yl)-5-trifluoromethyl-phenyl]-3-(4- pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.

9. 发明公开

EP1497258A1 CRYSTAL FORMS OF N-(TRANS-4-ISOPROPYLCYCLOHEXYLCARBONYL)-D-PHENYLALANINE 审中-公开
标题翻译： KRISTALLFORMEN VON N-（TRANS-4-异丙基环己基羰基）-D-苯丙氨酸
公开(公告)号：EP1497258A1
公开(公告)日：2005-01-19
申请号：EP03746296.7
申请日：2003-04-14
申请人： Novartis AG , Novartis Pharma GmbH
发明人： SUTTON, Paul, Allen
IPC分类号： C07C233/63 , C07C231/22
CPC分类号： C07C233/63 , C07B2200/13 , C07C231/22 , C07C2601/14
摘要： New crystal forms of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine, also known as nateglinide, may be produced by dissolving nateglinide in any of its forms, including solvates, in an organic solvent to form a solution followed by precipitation of nateglinide from the solution, and isolating and drying the precipitated crystal form of nateglinide. The precipitation of nateglinide may be induced either by cooling the solution, or by addition of another solvent which is miscible with the first solvent but in which nateglinide is only poorly soluble, or by combination of the two. Depending on the solvent a specific crystal form of nateglinide may be obtained, e.g., the R'-type crystal form of nateglinide produced by the described method has a different melting point, infra red spectra and X-ray diffraction patterns from the previously known crystal forms of nateglinide.
摘要翻译： N-（反式-4-异丙基环己基羰基）-D-苯丙氨酸（也称那格列奈）的新结晶形式可以通过将那格列奈以任何形式（包括溶剂化物）溶解在有机溶剂中来形成溶液，然后沉淀那格列奈，并分离和干燥那格列奈的沉淀晶体形式。那格列奈的沉淀可以通过冷却溶液或通过加入与第一溶剂混溶但其中那格列奈仅溶于难溶性的另外的溶剂或两者的组合来诱导。取决于溶剂，可以获得那格列奈的特定结晶形式，例如，由所述方法制备的那格列奈的R'型晶型具有不同的熔点，红外光谱和来自先前已知的晶体的X射线衍射图那格列奈的形式。

10. 发明授权

EP1912973B1 CRYSTALLINE FORMS OF 4-METHYL-N-[3-(4-METHYL-IMIDAZOL-1-YL)-5-TRIFLUOROMETHYL-PHENYL]3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-BENZAMIDE 无效
标题翻译： 4-甲基-N- [3-（4-甲基 - 咪唑-1-基）-5-三氟甲基 - 苯基]结晶形式-3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯甲酰胺盐
公开(公告)号：EP1912973B1
公开(公告)日：2012-06-13
申请号：EP06800109.8
申请日：2006-07-18
申请人： Novartis AG , Novartis Pharma GmbH
发明人： MANLEY, Paul, W. , SHIEH, Wen-Chung , SUTTON, Paul, Allen , KARPINSKI, Piotr, H. , WU, Raeann , MONNIER, Stéphanie , BROZIO, Jörg
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14
摘要： Crystalline forms of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide free base and salts thereof are prepared by various processes.

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