公开(公告)号：EP2828256A1

公开(公告)日：2015-01-28

申请号：EP13714246.9

申请日：2013-03-22

申请人： Novartis AG

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： 本发明涉及的方法和中间体螺吲哚酮化合物的制造中有用：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。

公开(公告)号：EP3578557A1

公开(公告)日：2019-12-11

申请号：EP19182727.8

申请日：2013-03-22

申请人： Novartis AG

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

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.

公开(公告)号：EP2007784A2

公开(公告)日：2008-12-31

申请号：EP07726952.0

申请日：2007-03-15

申请人： NOVARTIS AG

发明人： CERCUS, Jacques ,  FOULKES, Michael ,  HEINZ, Thomas ,  NIEDERER, Daniel ,  SCHMITZ, Beat

IPC分类号： C07H19/073

CPC分类号： C07H19/073

摘要： A novel method has been found to produce 2,2'-anhydro-1-(β-L- arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2'-anhydro-1- (β-L-arabinofuranosyl)thymine. According to these methods, synthesis of various L- nucleic acid derivatives, synthesis of which has been difficult till now.

公开(公告)号：EP2828256B1

公开(公告)日：2019-07-03

申请号：EP13714246.9

申请日：2013-03-22

申请人： Novartis AG

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

公开(公告)号：EP2382172A1

公开(公告)日：2011-11-02

申请号：EP09799106.1

申请日：2009-12-23

申请人： Novartis AG

发明人： MATHES, Christian ,  FOULKES, Michael ,  KESSELGRUBER, Martin

IPC分类号： C07B53/00 ,  C07C37/00 ,  C07C213/08 ,  C07C269/06 ,  C07C39/11 ,  C07C271/44 ,  C07C215/50 ,  C07C309/64

CPC分类号： C07C269/04 ,  C07B2200/07 ,  C07C37/002 ,  C07C213/02 ,  C07C213/08 ,  C07C303/28 ,  C07C303/30 ,  C07C309/66 ,  C07C215/50 ,  C07C39/11

摘要： A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drag substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.

公开(公告)号：EP1896411A2

公开(公告)日：2008-03-12

申请号：EP06754143.3

申请日：2006-06-06

申请人： Novartis AG

发明人： MICKEL, Stuart, John ,  SEDELMEIER, Gottfried ,  HIRT, Hans ,  SCHÄFER, Frank ,  FOULKES, Michael ,  PRIKOSZOVICH, Walter

IPC分类号： C07D207/08 ,  C07D207/16 ,  C07D407/04

CPC分类号： C07D405/04 ,  C07C237/22 ,  C07D207/08 ,  C07D307/32 ,  C07D307/33 ,  Y02P20/55

摘要： The invention related to a novel process, novel process Steps and novel intermediates useful in the synthesis of pharmaceutically active Compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a Compound of the formula (III), wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof, said manufacture comprising (preferably consisting in) reacting a Compound of the formula (I) with a reagent able to transform hydroxy into X where X is for example a leaving group.