公开(公告)号：EP1973924A1

公开(公告)日：2008-10-01

申请号：EP07700180.8

申请日：2007-01-04

申请人： SANDOZ AG

发明人： LUDESCHER, Johannes ,  GRIESSER, Ulrich ,  LANGES, Christoph

IPC分类号： C07H17/08 ,  A61K31/7048

CPC分类号： C07H17/08

摘要： The present invention relates to stable amorphous 3-De[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L- ribohexopyranosy l)oxy]- 1 1 , 12-dideoxy-6-O-methy 1-3-oxo- 12,11 -[oxycarbonyl[[4-[4-(3-pyridinyl)- 1 H- imidazol-l-yl]butyl]imino]]erythromycin (telithromycin), methods for the preparation thereof, the use of stable amorphous telithromycin in the treatment of bacterial infections and to pharmaceutical compositions comprising stable amorphous telithromycin.

公开(公告)号：EP1844036A1

公开(公告)日：2007-10-17

申请号：EP06704096.4

申请日：2006-01-27

申请人： SANDOZ AG

发明人： LUDESCHER, Johannes ,  STURM, Hubert

IPC分类号： C07D401/12 ,  A61K31/496

CPC分类号： C07D215/227 ,  C07B2200/13

摘要： The present invention relates to acid addition salts of aripiprazole , a process for preparing said acid addition salts and their use to prepare or purify aripiprazole in the form of a free base or in the form of a pharmaceutically acceptable salt.

公开(公告)号：EP1765767A1

公开(公告)日：2007-03-28

申请号：EP05766090.4

申请日：2005-07-04

申请人： SANDOZ AG

发明人： GARCIA, Rafael ,  LUDESCHER, Johannes ,  RIFA, Jordi ,  DIAGO, José

IPC分类号： C07C227/16 ,  C07C229/28

CPC分类号： C07C227/16 ,  C07C2601/14 ,  C07C229/28

摘要： The present invention relates to a new process for the preparation of gabapentin by the neutralization of an acid addition salt of gabapentin in an organic solvent or a mixture of organic solvents with a quaternary ammonium hydroxide.

摘要翻译： 本发明涉及通过中和加巴喷丁的酸加成盐在有机溶剂或有机溶剂与季铵氢氧化物的混合物中制备加巴喷丁的新方法。

公开(公告)号：EP1667987A2

公开(公告)日：2006-06-14

申请号：EP04765061.9

申请日：2004-09-10

申请人： SANDOZ AG

发明人： GREIL, Julia ,  LUDESCHER, Johannes ,  WOLF, Siegfried

IPC分类号： C07D307/88

CPC分类号： C07D307/88

摘要： The present invention relates to a new and economically attractive process for the production of mycophenolate mofetil in a high degree of pharmaceutically acceptable purity, which comprises the reaction of a reactive derivative of mycophenolic acid with 4-(2-hydroxyethyl)morpholine under acidic reaction conditions and the subsequent extraction of the pure mycophenolate mofetil through salt formation and release of the free base. A further aspect of the invention relates to the purification of mycophenolate mofetil by removing its by products, in particular its dimeric by-products, by means of treatment with a primary or secondary amine.

摘要翻译： 本发明涉及一种以高度药学上可接受的纯度生产霉酚酸吗啉乙酯的新的且经济上有吸引力的方法，其包括霉酚酸的反应性衍生物与4-（2-羟乙基）吗啉在酸性反应条件下反应 并随后通过盐形成和游离碱的释放来提取纯麦考酚酸吗乙酯。 本发明的另一方面涉及通过用伯胺或仲胺处理除去其副产物，特别是其二聚副产物来纯化麦考酚酸吗啉乙酯。

公开(公告)号：EP2379522B1

公开(公告)日：2018-02-28

申请号：EP09784096.1

申请日：2009-12-18

申请人： Sandoz AG

发明人： LUDESCHER, Johannes ,  WIESER, Josef ,  LAUS, Gerhard

IPC分类号： C07D401/04

CPC分类号： C07D401/04

摘要： The present invention is directed to a crystalline form of 2-[6-[3(R)-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-ylmethyl]-benzonitrile, a process for the preparation of said crystalline form and the use thereof in the manufacture of a pharmaceutical composition.

公开(公告)号：EP1554289B1

公开(公告)日：2011-03-09

申请号：EP03787771.9

申请日：2003-08-12

申请人： SANDOZ AG

发明人： KREMMINGER, Peter ,  WOLF, Siegfried ,  LUDESCHER, Johannes

IPC分类号： C07D501/00 ,  A61K31/546

CPC分类号： C07D501/00

摘要： 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula (I), in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula (I) in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.

公开(公告)号：EP2129671A2

公开(公告)日：2009-12-09

申请号：EP08717054.4

申请日：2008-02-22

申请人： Sandoz AG

发明人： LUDESCHER, Johannes ,  WIESER, Josef ,  PICHLER, Arthur ,  GRIESSER, Ulrich ,  BRAUN, Doris

IPC分类号： C07D413/06 ,  A61K31/5377 ,  A61P9/08

CPC分类号： C07D413/06

摘要： Novel polymorph form III of Aprepitant and a method for preparation of novel form III is disclosed. New processes for the preparation of Aprepitant form II are disclosed. The processes involve transformation of form III to form II by heating in decalin and the precipitation of form II from a solvent or solvent mixture by cooling and/or addition of addition of seed crystals or an anti solvent. Solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A process for the preparation of the solid dispersion by evaporation of a solution of Aprepitant and the carrier in a suitable solvent is disclosed. Stable Aprepitant form II is disclosed. Further pharmaceutical compositions containing Aprepitant form II, III or solid dispersions containing Aprepitant form II in a suitable carrier are disclosed. A methanol solvate of Aprepitant is disclosed.

公开(公告)号：EP2064173A1

公开(公告)日：2009-06-03

申请号：EP07785846.2

申请日：2007-06-25

申请人： Sandoz AG

发明人： LUDESCHER, Johannes ,  GRIESSER, Ulrich ,  BRAUN, Doris ,  WIESER, Josef

IPC分类号： C07C211/30 ,  A61K31/135

CPC分类号： C07C211/30

摘要： The present invention relates to the polymorph form II of Cinacalcet hydrochloride, methods for the preparation of pure form II of Cinacalcet hydrochloride, and pharmaceutical compositions comprising the new polymorphic form in an pharmaceutically effective amount The present invention also provides novel solvates of Cinacalcet hydrochloride, methods for the preparation of these solvates, the use of these novel solvates for the preparation of pure Cinacalcet hydrochloride, the use of these novel solvates for the preparation of polymorphic form II of Cinacalcet hydrochloride and pharmaceutical compositions comprising the acetic acid solvate of Cinacalcet hydrochloride.

公开(公告)号：EP1951747A1

公开(公告)日：2008-08-06

申请号：EP06818498.5

申请日：2006-11-13

申请人： SANDOZ AG

发明人： LUDESCHER, Johannes ,  MACHER, Ingolf ,  STORM, Ole ,  BERTEL, Stephan

IPC分类号： C07K7/56 ,  C07K1/113

CPC分类号： C07K7/56 ,  A61K38/00

摘要： The present invention relates to novel processes for preparing certain aza cyclohexapeptide compounds, e.g. caspofungin, novel intermediates used in said processes and a process for preparing said intermediates. In particular, the intermediates have formula (II), wherein X is amino or substituted amino, and contains a cyano/nitrile functionality.

公开(公告)号：EP1068211B1

公开(公告)日：2007-09-19

申请号：EP99917938.5

申请日：1999-03-31

申请人： SANDOZ AG

发明人： DECRISTOFORO, Martin ,  LUDESCHER, Johannes ,  STURM, Hubert

IPC分类号： C07D501/22 ,  C07D277/74

CPC分类号： C07D501/00 ,  C07D277/74

摘要： A process for the purification of cefixime via a novel tert.octylamine salt of a cefixime intermediate which may be crystalline and which may be produced in a one pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.