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1. 发明申请

WO2005021483A2 PURIFICATION PROCESS 审中-公开
标题翻译：净化过程
公开(公告)号：WO2005021483A2
公开(公告)日：2005-03-10
申请号：PCT/EP2004/009587
申请日：2004-08-27
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BEUTLER, Ulrich , PENN, Gerhard
发明人： BEUTLER, Ulrich , PENN, Gerhard
IPC分类号： C07C209/84
CPC分类号： C07C209/84 , C07C211/30
摘要： Purification process for the preparation of the allylamine pharmaceutical terbinafine of formula (I), in free base form or acid addition salt form, by distilling crude terbinafine base, preferably by short path distillation, e.g. at a temperature above 100°C and reduced pressure, e.g. 0.2 mbar, and recovering the purified product in free base or acid addition salt form.
摘要翻译：用游离碱形式或酸加成盐形式制备式（I）的烯丙胺药物特比萘芬的纯化方法，通过蒸馏粗特比萘芬碱，优选通过短程蒸馏，例如，在高于100℃的温度和减压下，例如， 0.2毫巴，并回收游离碱或酸加成盐形式的纯化产物。

2. 发明申请

WO2006089746A1 PURIFICATION PROCESS 审中-公开
标题翻译：净化过程
公开(公告)号：WO2006089746A1
公开(公告)日：2006-08-31
申请号：PCT/EP2006/001656
申请日：2006-02-23
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BEUTLER, Ulrich , FÜNFSCHILLING, Peter , PENN, Gerhard , ROTH, Alfons
发明人： BEUTLER, Ulrich , FÜNFSCHILLING, Peter , PENN, Gerhard , ROTH, Alfons
IPC分类号： C07C209/84 , C07C211/30 , A61K31/137 , A61P31/10
CPC分类号： C07C211/30 , C07C209/84
摘要： Process for the purification from non-metal contaminants of the allylamine pharmaceutical terbinafine of formula (I) in free base form or acid addition salt form, by distilling crude terbinafine base, preferably by short path distillation, e.g. at a temperature above 100°C and reduced pressure, e.g. 0.2 mbar (method A), optionally together with salt formation of the resultant product under simultaneous precipitation of pure trans isomer (method B), and recovering the pure product in free base or acid addition salt form. Detection of non-metal contaminants such as substance A of formula (II) is preferably effected by RP HPLC analysis with UV detection.
摘要翻译：从游离碱形式或酸加成盐形式的式（I）的烯丙胺药物特比萘芬的非金属污染物纯化的方法，通过蒸馏粗特比萘芬碱，优选通过短程蒸馏，例如，在高于100℃的温度和减压下，例如， 0.2mbar（方法A），任选地与所得产物在同时沉淀纯反式异构体（方法B）下形成盐，并以游离碱或酸加成盐形式回收纯产物。检测非金属污染物如式（II）的物质A优选通过具有UV检测的RP HPLC分析来进行。

3. 发明申请

WO2004087668A1 A PROCESS FOR THE PREPARATION OF 5-(HALOACETYL)-8-(SUBSTITUTED OXY)-(1H)-QUINOLIN-2-ONES 审中-公开
标题翻译：制备5-（HALOACETYL）-8-（取代的氧） - （1H） - 喹啉-2-酮的方法
公开(公告)号：WO2004087668A1
公开(公告)日：2004-10-14
申请号：PCT/EP2004/003479
申请日：2004-04-01
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , LOHSE, Olivier , PENN, Gerhard , SCHILLING, Hanspeter
发明人： LOHSE, Olivier , PENN, Gerhard , SCHILLING, Hanspeter
IPC分类号： C07D215/26
CPC分类号： C07D215/26 , Y02P20/55
摘要： The invention relates to a process for preparing 5-(α-haloacetyl)-8-substituted oxy-( 1H )-quinolin-2-ones. The process involves (i) reacting (a) 8-hydroxy-( 1H )-quinolin-2-one with an acylating agent and a Lewis acid to form 5-acetyl-8-hydroxy-( 1H )-quinolin-2-one; or (b) 8-hydroxy-( lH )-quinolin-2-one with an acylating agent to form 8-acetoxy-( lH )-quinolin-2-one, and treating, in-situ, the 8-acetoxy-( 1H )-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-( 1H )-quinolin-2-one; or (c) 8-acetoxy-( 1H )-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-( lH )-quinolin-2-one; (ii) reacting the 5-acetyl-8-hydroxy-( 1H )-quinolin-2-one prepared in Step (i) with a compound having the Formula RL in the presence of a base and a solvent to form 5-acetyl-8-substituted oxy-( 1H )-quinolin-2-one, wherein R is a protecting group and L is a leaving group; and (iii) reacting the 5-acetyl-8-substituted oxy-( 1H )-quinolin-2-one with a halogenating agent in the presence of a solvent to form a 5-(α-haloacetyl)-8-substituted oxy-( 1H )-quinolin-2-one.
摘要翻译：本发明涉及制备5-（α-卤代乙酰基）-8-取代的氧基 - （1H） - 喹啉-2-酮的方法。该方法包括（i）使（a）8-羟基 - （1H） - 喹啉-2-酮与酰化剂和路易斯酸反应，形成5-乙酰基-8-羟基 - （1H） - 喹啉-2-酮 ; 或（b）8-羟基 - （1H） - 喹啉-2-酮与酰化剂反应形成8-乙酰氧基 - （1H） - 喹啉-2-酮，并原位处理8-乙酰氧基 - （ 1H） - 喹啉-2-酮与路易斯酸形成5-乙酰基-8-羟基 - （1H） - 喹啉-2-酮; 或（c）8-乙酰氧基 - （1H） - 喹啉-2-酮与路易斯酸形成5-乙酰基-8-羟基 - （1H） - 喹啉-2-酮; （ii）使步骤（i）中制备的5-乙酰基-8-羟基 - （1H） - 喹啉-2-酮与碱式和溶剂存在下的具有式RL的化合物反应，形成5-乙酰基 - 8-取代的氧 - （1H） - 喹啉-2-酮，其中R是保护基，L是离去基团; 和（iii）使5-乙酰基-8-取代的氧基 - （1H） - 喹啉-2-酮与卤化剂在溶剂存在下反应，形成5-（α-卤代乙酰基）-8-取代的氧 - （1H） - 喹啉-2-酮。

4. 发明申请

WO2017051326A1 NEW PROCESSES AND INTERMEDIATES USEFUL IN SYNTHESIS OF NEP INHIBITORS 审中-公开
标题翻译：新方法和中间体有用于合成NEP抑制剂
公开(公告)号：WO2017051326A1
公开(公告)日：2017-03-30
申请号：PCT/IB2016/055628
申请日：2016-09-21
申请人： NOVARTIS AG , MARTIN, Benjamin , PENN, Gerhard , SCHENKEL, Berthold , BOURNE, Samuel , LAU, Shing-Hing , LEY, Steven
发明人： MARTIN, Benjamin , PENN, Gerhard , SCHENKEL, Berthold , BOURNE, Samuel , LAU, Shing-Hing , LEY, Steven
IPC分类号： C07C69/653 , C07C313/06 , C07C229/34 , C07C47/23
CPC分类号： C07C313/06 , C07B2200/07 , C07C2/861 , C07C45/36 , C07C45/41 , C07C67/31 , C07C67/317 , C07C67/343 , C07C227/20 , C07C381/00 , C07C2523/44 , C07C2531/04 , C07C229/34 , C07C69/738 , C07C69/732 , C07C69/616 , C07C47/23 , C07C15/50
摘要： The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors such as sacubitril, and prodrugs thereof.
摘要翻译：本发明涉及可用于合成药物活性化合物，特别是中性肽链内切酶（NEP）抑制剂例如茜素的新方法，新工艺步骤和新型中间体及其前药。

5. 发明申请

WO2010018154A1 PROCESSES FOR THE PREPARATION OF 4-OXO-OCTAHYDRO-INDOLE-1-CARBOCYLIC ACID METHYL ESTER AND DERIVATIVES THEREOF 审中-公开
标题翻译：制备4-氧代 - 氯代 - 吲哚-1-羧酸甲酯及其衍生物的方法
公开(公告)号：WO2010018154A1
公开(公告)日：2010-02-18
申请号：PCT/EP2009/060351
申请日：2009-08-10
申请人： NOVARTIS AG , KUESTERS, Ernst , ACEMOGLU, Murat , LUSTENBERGER, Philipp , SEDELMEIER, Gottfried , SCHMIDT, Beat , PENN, Gerhard
发明人： KUESTERS, Ernst , ACEMOGLU, Murat , LUSTENBERGER, Philipp , SEDELMEIER, Gottfried , SCHMIDT, Beat , PENN, Gerhard
IPC分类号： C07D209/08 , C07C271/24 , C07D203/14
CPC分类号： C07D209/08 , C07C271/24 , C07C2601/14 , C07D203/14
摘要： The present invention relates to a process for the production of (3aR, 4S, 7aR)-4-hydroxy-4-m-tolylethynyl-octahydro-indole-1-carboxylic acid methyl ester (I), of carbamic acid (2-chloroethyl)(3-oxocyclohexyl)-alkyl ester enantiomers (II), and of 1-carbalkoxy-4-ketoperhydroindole enantiomers (III).
摘要翻译：本发明涉及一种制备（3aR，4S，7aR）-4-羟基-4-间甲酰基乙炔基 - 八氢 - 吲哚-1-甲酸甲酯（I）的方法，其中将氨基甲酸（2-氯乙基）（3-氧代环己基） - 烷基酯对映异构体（II）和1-烷氧基-4-酮戊二酸对映异构体（III）。

6. 发明授权

EP1289997B1 MACROLIDES 有权
标题翻译： MAKROLIDE
公开(公告)号：EP1289997B1
公开(公告)日：2004-01-07
申请号：EP01956441.8
申请日：2001-05-21
申请人： Novartis AG , Novartis Pharma GmbH
发明人： FLEISSNER, Gerhard , HÄCKER, Helmut , KÜSTERS, Ernst , PENN, Gerhard
IPC分类号： C07D498/18 , A61K31/436 , A61P37/06
CPC分类号： C07D498/18
摘要： The compounds of formula (I) wherein the substituents have various significances, whereby one of R2 to R4 is ethyl. They can be prepared by fermentation, or by replacement of hydroxy with chloro under simultaneous or concomittant epimerization. They are indicated for use as pharmaceuticals in the prevention or treatment of inflammatory conditions and of conditions requiring immunosuppression, optionally in combination or association with further pharmaceutically active and compatible agents, e.g. macrolactam macrolides such as pimecrolimus.

7. 发明授权

EP1613599B1 A PROCESS FOR THE PREPARATION OF 5-(HALOACETYL)-8-(SUBSTITUTED OXY)-(1H)-QUINOLIN-2-ONES 有权转让
标题翻译： PRODUCING 5-（卤代乙酰基）的方法-8（取代的氧） - （1H） - 喹啉-2-酮
公开(公告)号：EP1613599B1
公开(公告)日：2010-12-15
申请号：EP04725035.2
申请日：2004-04-01
申请人： Novartis AG , Novartis Pharma GmbH
发明人： LOHSE, Olivier , PENN, Gerhard , SCHILLING, Hanspeter
IPC分类号： C07D215/26
CPC分类号： C07D215/26 , Y02P20/55
摘要： The invention relates to a process for preparing 5-(α-haloacetyl)-8-substituted oxy-(1H)-quinolin-2-ones. The process involves (i) reacting (a) 8-hydroxy-(1H)-quinolin-2-one with an acylating agent and a Lewis acid to form 5-acetyl-8-hydroxy-(1H)-quinolin-2-one; or (b) 8-hydroxy-(lH)-quinolin-2-one with an acylating agent to form 8-acetoxy-(lH)-quinolin-2-one, and treating, in-situ, the 8-acetoxy-(1H)-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-(1H)-quinolin-2-one; or (c) 8-acetoxy-(1H)-quinolin-2-one with a Lewis acid to form 5-acetyl-8-hydroxy-(lH)-quinolin-2-one; (ii) reacting the 5-acetyl-8-hydroxy-(1H)-quinolin-2-one prepared in Step (i) with a compound having the Formula RL in the presence of a base and a solvent to form 5-acetyl-8-substituted oxy-(1H)-quinolin-2-one, wherein R is a protecting group and L is a leaving group; and (iii) reacting the 5-acetyl-8-substituted oxy-(1H)-quinolin-2-one with a halogenating agent in the presence of a solvent to form a 5-(α-haloacetyl)-8-substituted oxy-(1H)-quinolin-2-one.

8. 发明公开

EP1856026A1 PURIFICATION PROCESS 审中-公开
标题翻译：纯化方法
公开(公告)号：EP1856026A1
公开(公告)日：2007-11-21
申请号：EP06723088.8
申请日：2006-02-23
申请人： Novartis AG , NOVARTIS-PHARMA GMBH
发明人： BEUTLER, Ulrich , FÜNFSCHILLING, Peter , PENN, Gerhard , ROTH, Alfons
IPC分类号： C07C209/84 , C07C211/30 , A61K31/137 , A61P31/10
CPC分类号： C07C211/30 , C07C209/84
摘要： Process for the purification from non-metal contaminants of the allylamine pharmaceutical terbinafine of formula (I) in free base form or acid addition salt form, by distilling crude terbinafine base, preferably by short path distillation, e.g. at a temperature above 100°C and reduced pressure, e.g. 0.2 mbar (method A), optionally together with salt formation of the resultant product under simultaneous precipitation of pure trans isomer (method B), and recovering the pure product in free base or acid addition salt form. Detection of non-metal contaminants such as substance A of formula (II) is preferably effected by RP HPLC analysis with UV detection.

9. 发明公开

EP1694631A2 PROCESS FOR THE PURIFICATION OF TERBINAFINE 审中-公开
标题翻译：法提纯特比萘芬的
公开(公告)号：EP1694631A2
公开(公告)日：2006-08-30
申请号：EP04764561.9
申请日：2004-08-27
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BEUTLER, Ulrich , PENN, Gerhard
IPC分类号： C07C209/84 , C07C211/27
CPC分类号： C07C209/84 , C07C211/30
摘要： Purification process for the preparation of the allylamine pharmaceutical terbinafine of formula (I), in free base form or acid addition salt form, by distilling crude terbinafine base, preferably by short path distillation, e.g. at a temperature above 100°C and reduced pressure, e.g. 0.2 mbar, and recovering the purified product in free base or acid addition salt form.

10. 发明授权

EP0994880B1 CRYSTALLINE MACROLIDES AND PROCESS FOR THEIR PREPARATION 失效
标题翻译： CRYSTAL大环内酯类及其制备方法
公开(公告)号：EP0994880B1
公开(公告)日：2005-01-19
申请号：EP98936392.4
申请日：1998-06-26
申请人： Novartis AG , Novartis Pharma GmbH
发明人： DOSENBACH, Cornelia , GRASSBERGER, Maximilian , HARTMANN, Otto , HORVATH, Amarylla , MUTZ, Jean-Paul , PENN, Gerhard , PFEFFER, Sabine , WIECKHUSEN, Dierk
IPC分类号： C07D498/18
CPC分类号： C07D498/18 , C30B7/00
摘要： 33-Epichloro-33-desoxyascomycin of formula (I) and various tautomeric or solvated forms thereof, in crystalline form, such as Form A and Form B. Their preparation involves appropriately converting amorphous compound of formula (I), or compound of formula (I) in other than Form A, or compound of formula (I) in other than Form B, respectively, from a solution thereof under crystallization-inducing conditions or conditions inducing preferential crystallization of Form A or B, respectively. Such crystals are particularly indicated for use in the preparation of topical galenical forms of the compound for pharmaceutical use, e.g. creams, emulsions and ointments.

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