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1. 发明申请

WO2008055874A1 CYCLOPENTENE DIOL MONOACETATE DERIVATIVES 审中-公开
标题翻译：环戊二醇单酸酯衍生物
公开(公告)号：WO2008055874A1
公开(公告)日：2008-05-15
申请号：PCT/EP2007/061886
申请日：2007-11-05
申请人： NOVARTIS AG , LAUMEN, Kurt
发明人： LAUMEN, Kurt
IPC分类号： C07C67/14 , C07C69/013
CPC分类号： C07C45/59 , C07B2200/07 , C07C67/08 , C12P7/62 , C12P41/004 , C12Y301/01003 , C07C49/707 , C07C69/013 , C07C69/16
摘要： A process for the preparation of organic compounds of formula (I), wherein R 1 is as described herein.
摘要翻译：制备式（I）的有机化合物的方法，其中R 1如本文所述。

2. 发明申请

WO2008009750A3 MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物可用作BACE抑制剂
公开(公告)号：WO2008009750A3
公开(公告)日：2008-03-20
申请号：PCT/EP2007057540
申请日：2007-07-20
申请人： NOVARTIS AG , LAUMEN KURT , MACHAUER RAINER , TINTELNOT-BLOMLEY MARINA , VEENSTRA SIEM JACOB
发明人： LAUMEN KURT , MACHAUER RAINER , TINTELNOT-BLOMLEY MARINA , VEENSTRA SIEM JACOB
IPC分类号： C07D245/06 , A61K31/395 , A61K31/4427 , A61P25/00 , C07D273/00 , C07D273/02 , C07D401/12 , C07D413/12 , C07D413/14
CPC分类号： C07D273/00 , C07D245/06 , C07D273/02 , C07D401/12 , C07D413/12 , C07D413/14
摘要： The invention relates to novel macrocyclic compounds of the Formula (I) in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及新的式（I）大环化合物，其中所有变量如说明书中所定义，游离碱形式或酸加成盐形式，它们的制备方法，它们作为药物和药物的用途，他们。

3. 发明申请

WO2005049585A1 MACROCYCLIC LACTAMS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：大肠杆菌及其药物用途
公开(公告)号：WO2005049585A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012497
申请日：2004-11-04
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , AUBERSON, Yves , BETSCHART, Claudia , GLATTHAR, Ralf , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VEENSTRA, Siem, Jacob
发明人： AUBERSON, Yves , BETSCHART, Claudia , GLATTHAR, Ralf , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , TROXLER, Thomas, J. , VEENSTRA, Siem, Jacob
IPC分类号： C07D245/02
CPC分类号： C07D245/02 , C07D255/00 , C07D273/00 , C07D281/00 , C07D471/08 , C07D513/08
摘要： The present invention relates to novel macrocyclic compounds of the formula (I) wherein R 1 , R 2 , R 3 , U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的新的大环化合物，其中R 1，R 2，R 3，U，V，W，X，Y，Z和n如说明书中所定义，大环中包括的环原子数环为14,15,16或17，以游离碱形式或以酸加成盐形式，其制备用作药物和包含它们的药物组合物。

4. 发明申请

WO2013139987A1 CHEMICAL PROCESS FOR PREPARING SPIROINDOLONES AND INTERMEDIATES THEREOF 审中-公开
标题翻译：用于制备螺旋体的化学方法及其中间体
公开(公告)号：WO2013139987A1
公开(公告)日：2013-09-26
申请号：PCT/EP2013/056170
申请日：2013-03-22
申请人： NOVARTIS AG , CROWE, Michael , FOULKES, Michael , FRANCESE, Giancarlo , GRIMLER, Dominique , KUESTERS, Ernst , LAUMEN, Kurt , LI, Yunzhong , LIN, Changxue , NAZOR, Jovana , RUCH, Thomas , SMITH, Derek , SONG, Shiwei , TENG, Shangjun
发明人： CROWE, Michael , FOULKES, Michael , FRANCESE, Giancarlo , GRIMLER, Dominique , KUESTERS, Ernst , LAUMEN, Kurt , LI, Yunzhong , LIN, Changxue , NAZOR, Jovana , RUCH, Thomas , SMITH, Derek , SONG, Shiwei , TENG, Shangjun
IPC分类号： C07D405/06 , C07D471/20 , C07D209/12 , C07D209/14 , C07D209/34 , C12P17/10
CPC分类号： C12P17/10 , C07D209/12 , C07D209/14 , C07D209/34 , C07D209/38 , C07D405/06 , C07D471/20 , C12N9/1096 , Y02P20/52
摘要： The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1'R,3'S)-5,7'-dichloro-6'-fluoro-3'-methyl-2',3',4',9'-tetrahydrospiro[indoline-3,1'-pyrido[3, 4-b]indol]-2-one and salts and hydrates and solvates thereof.
摘要翻译：本发明涉及可用于制备螺旋体酮化合物的方法和中间体，例如（1'R，3'S）-5,7'-二氯-6'-氟-3'-甲基-2'，3'，4' ，9'-四氢螺[二氢吲哚-3,1'-吡啶并[3,4-b]吲哚] -2-酮及其盐和水合物和溶剂化物。

5. 发明申请

WO1997041214A1 BIOCATALYSTS WITH AMINE ACYLASE ACTIVITY 审中-公开
标题翻译：生物钙与氨基酸酶活性
公开(公告)号：WO1997041214A1
公开(公告)日：1997-11-06
申请号：PCT/EP1997001866
申请日：1997-04-14
申请人： NOVARTIS AG , GHISALBA, Oreste , KITTELMANN, Matthias , LAUMEN, Kurt , WALSER-VOLKEN, Paula
发明人： NOVARTIS AG
IPC分类号： C12N09/80
CPC分类号： C12N9/80 , C12P41/007 , Y10S435/826 , Y10S435/893 , Y10S435/908
摘要： The invention belongs to the field of biotechnology. It concerns a biocatalyst, i.e. a dead or living microorganism or a polypeptide, preferably in isolated form, which exhibits acylase enzymatic activity without lipase- or esterase-activity. The biocatalyst is capable of stereoselectively hydrolysing a racemic acylamide which has an aliphatic acyl residue and which is not a derivative of a natural amino acid.
摘要翻译：本发明属于生物技术领域。它涉及生物催化剂，即死亡或活的微生物或多肽，优选分离形式，其显示没有脂肪酶或酯酶活性的酰基转移酶酶活性。该生物催化剂能够立体选择性水解具有脂肪族酰基残基并且不是天然氨基酸衍生物的外消旋酰基酰胺。

6. 发明申请

WO2007039079A1 PROCESS FOR THE SYNTHESIS OF BETA AMINO ACIDS 审中-公开
标题翻译：用于合成氨基酸的方法
公开(公告)号：WO2007039079A1
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009050
申请日：2006-09-18
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , GHISALBA, Oreste , LAUMEN, Kurt
发明人： GHISALBA, Oreste , LAUMEN, Kurt
IPC分类号： C12P13/00 , C12R1/15
CPC分类号： C12P13/04
摘要： A process for the synthesis of beta amino acids comprising the hydrolysis of N-acetyl methyl ester derivatives using a biocatalyst.
摘要翻译：一种用于合成β-氨基酸的方法，包括使用生物催化剂水解N-乙酰基甲酯衍生物。

7. 发明申请

WO2008009750A2 MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物可用作BACE抑制剂
公开(公告)号：WO2008009750A2
公开(公告)日：2008-01-24
申请号：PCT/EP2007/057540
申请日：2007-07-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GmbH , LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob
发明人： LAUMEN, Kurt , MACHAUER, Rainer , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem Jacob
IPC分类号： C07D245/06 , C07D401/12 , C07D413/14 , C07D413/12 , C07D273/02 , C07D273/00 , A61K31/395 , A61K31/4427 , A61P25/00
CPC分类号： C07D273/00 , C07D245/06 , C07D273/02 , C07D401/12 , C07D413/12 , C07D413/14
摘要： The invention relates to novel macrocyclic compounds of the Formula (I) in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及式（I）的新型大环化合物，其中所有变量如本说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和药物，其包含他们。

8. 发明申请

WO2007077004A1 MACROCYCLIC COMPOUNDS USEFUL AS BACE INHIBITORS 审中-公开
标题翻译：大环化合物可用作BACE抑制剂
公开(公告)号：WO2007077004A1
公开(公告)日：2007-07-12
申请号：PCT/EP2006/012569
申请日：2006-12-28
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , BETSCHART, Claudia , KOLLER, Manuel , LAUMEN, Kurt , LERCHNER, Andreas , MACHAUER, Rainer , MCCARTHY, Clive , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
发明人： BETSCHART, Claudia , KOLLER, Manuel , LAUMEN, Kurt , LERCHNER, Andreas , MACHAUER, Rainer , MCCARTHY, Clive , TINTELNOT-BLOMLEY, Marina , VEENSTRA, Siem, Jacob
IPC分类号： C07D245/04 , A61P25/00 , A61K31/33
CPC分类号： C07D245/04 , C07D273/00
摘要： The invention relates to novel macrocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
摘要翻译：本发明涉及式（I）的新型大环化合物，其中所有变量如说明书中所定义，游离碱形式或酸加成盐形式，其制备方法，用作药物和药物包括他们。

9. 发明申请

WO1992014830A1 ENZYMATIC REVERSE HYDROLYSIS OF HYDROPHILIC SUBSTRATES - PREPARATION OF AMPHIPHILIC COMPOUNDS 审中-公开
标题翻译：水解底物的酶反向水解 - 大分子化合物的制备
公开(公告)号：WO1992014830A1
公开(公告)日：1992-09-03
申请号：PCT/EP1992000307
申请日：1992-02-12
申请人： SCHNEIDER, Manfred, P. , LAUMEN, Kurt, E. , BERGER, Matthias
IPC分类号： C12P01/00
CPC分类号： C12P13/001 , C12P1/00 , C12P7/62 , C12P7/6436 , C12P7/6454 , C12P7/6481 , C12P9/00 , C12P13/00 , C12P13/02 , C12P13/04 , C12P19/00 , C12P19/02 , C12P19/44 , C12P21/02
摘要： The invention relates to methods for the production of amphiphilic products such as esters, sugar-esters, peptide-esters, glycolipids, glycoproteins, lipoproteins, peptides, and phosphates of alcohols, sugars, and nucleosides. The methods promote enzymatically catalyzed reactions between hydrophilic substrates such as glucerol, glucose, amino acids, and nucleosides, and second substrates such as free fatty acids, triglycerides, vinylesters, amino acids, and phosphates. The method is also applied to enzymatic reactions with saccharides and polyalcohols. The hydrophilic substrates are adsorbed to finely divided solid supports such as silica gel, diatomaceous earths, or activated chracoals in order to promote the dispersion of the hydrophilic substrates within hydrophobic substrates and solvents. Hydrophobic solvents such as n-hexane and t-butylmethylether may be included in the reaction mixtures. Reactions are conducted under non-aqueous conditions in order to promote reverse hydrolysis. Methods are provided for the production of isomerically pure 1,3-diglycerides. Further methods are disclosed for the production and specific precipitation of pure 1-monogycerides through the use of a reactor/separator system. Enzymes used in the methods include lipases from M. mihei and P. fluorescens, glycosidases such as beta - galactosidase, proteases such as chymotrypsin, and acid or alkaline phosphatases. Compositions are provided comprising alcohols, carbohydrates, amino acids, or peptides adsorbed onto solid supports such as silica gel.
摘要翻译：本发明涉及制备醇，糖和核苷类的两亲产物如酯，糖酯，肽 - 酯，糖脂，糖蛋白，脂蛋白，肽和磷酸酯的方法。这些方法促进亲水底物如葡萄糖，葡萄糖，氨基酸和核苷之间的酶催化反应，以及第二底物如游离脂肪酸，甘油三酸酯，乙烯基酯，氨基酸和磷酸酯。该方法也适用于与糖和多元醇的酶反应。为了促进亲水性底物在疏水性底物和溶剂中的分散，亲水性底物被吸附到细分散的固体载体如硅胶，硅藻土或活化的色母体上。疏水性溶剂如正己烷和叔丁基甲基醚可以包括在反应混合物中。反应在非水性条件下进行，以促进反向水解。提供了用于生产异构纯的1,3-甘油二酯的方法。公开了通过使用反应器/分离器系统来生产和特异性沉淀纯的1-单加氧化物的其它方法。用于该方法的酶包括来自M.mehei和荧光假单胞菌的脂肪酶，糖苷酶如β-半乳糖苷酶，蛋白酶如胰凝乳蛋白酶和酸或碱性磷酸酶。提供了包含醇，碳水化合物，氨基酸或吸附在固体支持物例如硅胶上的肽的组合物。

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