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1. 发明申请

WO2012010538A3 NOVEL PROCESSES FOR THE MANUFACTURE OF PROPANE-1-SULFONIC ACID {3-[5-(4-CHLORO-PHENYL)-1H-PYRROLO[2,3-B]PYRIDINE-3-CARBONYL]-2,4-DIFLUORO-PHENYL}-AMIDE 审中-公开
标题翻译：丙酸1-磺酸（3- [5-（4-氯 - 苯基）-1H-吡唑并[2,3-b]吡啶-3-羰基] -2,4-二氟苯基的制备新方法 } - 酰胺
公开(公告)号：WO2012010538A3
公开(公告)日：2013-02-21
申请号：PCT/EP2011062207
申请日：2011-07-18
申请人： HOFFMANN LA ROCHE , BRUMSTED COREY JAMES , MOORLAG HENDRIK , RADINOV ROUMEN NIKOLAEV , REN YI , WALDMEIER PIUS
发明人： BRUMSTED COREY JAMES , MOORLAG HENDRIK , RADINOV ROUMEN NIKOLAEV , REN YI , WALDMEIER PIUS
IPC分类号： C07D213/73 , C07D213/74 , C07D213/75 , C07D471/04
CPC分类号： C07D471/04 , C07D213/73 , C07D213/74 , C07D213/75 , C07F5/04 , C07F7/0812
摘要： According to the present invention there are provided novel processes for the manufacture of the compound of formula (1) as well as novel synthesis routes for key intermediates used in those processes.
摘要翻译：根据本发明，提供了制备式（1）化合物的新方法以及用于这些方法的关键中间体的新型合成路线。

2. 发明申请

WO2007096261A2 PROCESS FOR THE PREPARATION OF DIOXANE DERIVATIVES 审中-公开
标题翻译：制备二氧化物衍生物的方法
公开(公告)号：WO2007096261A2
公开(公告)日：2007-08-30
申请号：PCT/EP2007051316
申请日：2007-02-12
申请人： HOFFMANN LA ROCHE , HARTUNG THOMAS , JENNY CHRISTIAN , MONTAVON FRANCOIS , WALDMEIER PIUS
发明人： HARTUNG THOMAS , JENNY CHRISTIAN , MONTAVON FRANCOIS , WALDMEIER PIUS
CPC分类号： C07D319/06 , C07D263/32 , C07D263/36 , C07D413/06
摘要： The present invention is concerned with a novel process for the preparation of compounds of formula (I), wherein R 1 and R 2 are as defined in the description and claims. The compounds of formula (I) are pharmaceutically active substances.
摘要翻译：本发明涉及制备式（I）化合物的新方法，其中R 1和R 2如在说明书和权利要求书中所定义。式（I）化合物是药物活性物质。

3. 发明申请

WO2008107334A3 PROCESS FOR THE SYNTHESIS OF GLYT-1 INHIBITORS 审中-公开
标题翻译：合成GLYT-1抑制剂的方法
公开(公告)号：WO2008107334A3
公开(公告)日：2008-10-23
申请号：PCT/EP2008052244
申请日：2008-02-25
申请人： HOFFMANN LA ROCHE , PFLEGER CHRISTOPHE , WALDMEIER PIUS , WANG SHAONING
发明人： PFLEGER CHRISTOPHE , WALDMEIER PIUS , WANG SHAONING
IPC分类号： A61K31/497 , A61P25/00 , C07D213/74
CPC分类号： C07D213/74 , C07D295/18
摘要： Process for preparation of a compound of formula (I) wherein Het is a 6-membered heteroaryl group, containing one, two or three nitrogen atoms; R 1 is (C 1 -C 6 )-alkyl, (C 3 -C 6 )-cycloalkyl, NR 4 R 5 or (C 1 -C 6 )-alkyl subtituted by halogen; R 2 is hydroxy, halogen, NO 2 , CN, (C 1 -C 6 )-alkyl, (C 3 -C 6 )-cycloalkyl, (C 1 -C 6 )-alkyl substituted by halogen, (C 1 -C 6 )-alkyl substituted by hydroxy, (CH 2 ) o -(C 1 -C 6 )-alkoxy, (C 1 -C 6 )-alkoxy substituted by halogen, NR 4 R 5 , C(O)R 6 or SO 2 R 7 ; R 3 is (C 1 -C 6 )-alkyl, (C 3 -C 6 )-cycloalkyl or (C 1 -C 6 )-alkyl subtituted by halogen; R 4 and R 5 independently from each other are hydrogen or (C 1 -C 6 )-alkyl; R 6 is hydrogen, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy or NR 4 R 5 ; R 7 is (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl optionally subtituted by halogen, (CH 2 ) o -(C 3 -C 6 )-cycloalkyl, (CH 2 ) o -(C 3 -C 6 )-alkoxy or NR 4 R 5 ; n is 0, 1, 2 or 3; o is 0, 1 or 2; and pharmaceutically acceptable acid addition salts thereof, characterized in that it comprises the steps of a) reacting a compound of formula (21) with a compound of formula: R 3 OH 8 to a compound of formula (11) and b) coupling the compound of formula (11) in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula (15) to obtain a compound of formula (I).
摘要翻译：制备其中Het是含有一个，两个或三个氮原子的6元杂芳基的式（I）化合物的方法; R 1是（C 1 -C 6 - ） - 烷基，（C 3 -C 6）烷基（C 1 -C 6 - 环烷基，NR 4 R 5或（C 1 -C 6 - ） - 烷基（C 1 -C 6）用卤素取代; R 2是羟基，卤素，NO 2，CN，（C 1 -C 6 - ） - 烷基，（C 3 -C 6） - 环烷基，（C 1 -C 6 -C 6 - ）被卤素取代的烷基，（C 1 -C 6 -C 6） - 被羟基取代的烷基，（CH 2）2 - （C C 1 -C 6烷氧基，（C 1 -C 6 -C 6） - 被卤素取代的烷氧基，NR C（O）R 6或SO 2 R 7，其中R 1，R 2，R 3， ; R 3是（C 1 -C 6 - ） - 烷基，（C 3 -C 6）烷基（C 1 -C 6 - - 环烷基或（C 1 -C 6 -C 6 - ）被卤素取代的烷基; R 4和R 5彼此独立地为氢或（C 1 -C 6 -C 6 - ） - 烷基; R 6是氢，（C 1 -C 6 - ） - 烷基，（C 1 -C 3 - 亚<！ - SIPO < > 6） - 烷氧基或NR 4 R 5; R 6是（C 1 -C 6） - 烷基，（C 1 -C 6）烷基，（C 1 -C 6 - （CH 3） - （C 3 -C 6） - （C 3 -C 6） - （C 3 -C 6） - （C 3 -C 6）（C 3 -C 6） - （C 3 -C 6） - 烷氧基或（C 1 -C 6） - 烷氧基， NR ^{4 - [R ^{5 ; n为0,1,2或3; o为0,1或2; 其特征在于其包括以下步骤：a）使式（21）化合物与式R 3 OH的化合物与式（11）化合物反应）和b）在偶联剂或相应的酰卤化物存在下将式（11）化合物与式（15）化合物偶合，得到式（I）化合物。}}

4. 发明申请

WO2009068463A3 PROCESS FOR THE PREPARATION OF ISOINDOLE DERIVATIVES AS WELL AS A PROCESS FOR THE PREPARATION OF THEIR INTERMEDIATES 审中-公开
标题翻译：制备异吲哚衍生物的方法以及制备它们的中间体的方法
公开(公告)号：WO2009068463A3
公开(公告)日：2009-09-11
申请号：PCT/EP2008065820
申请日：2008-11-19
申请人： HOFFMANN LA ROCHE , PFLEGER CHRISTOPHE , SPURR PAUL , TRUSSARDI RENE , WALDMEIER PIUS , WANG SHAONING
发明人： PFLEGER CHRISTOPHE , SPURR PAUL , TRUSSARDI RENE , WALDMEIER PIUS , WANG SHAONING
IPC分类号： C07D209/44
CPC分类号： C07D209/44 , C07D471/04
摘要： The invention is concerned with a new scalable process for the preparation of compounds of formula (I) comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula (II) or a salt thereof.
摘要翻译：本发明涉及用于制备式（I）化合物的新型可缩放方法，其包括用于制备关键中间体二羟基吡咯衍生物式（II）或其盐的新方法。

5. 发明申请

WO2009068463A2 PREPARATION OF DIHYDROPYRROL DERIVATIVES AS INTERMEDIATES 审中-公开
标题翻译：作为中间体的二氢吲哚衍生物的制备
公开(公告)号：WO2009068463A2
公开(公告)日：2009-06-04
申请号：PCT/EP2008065820
申请日：2008-11-19
申请人： HOFFMANN LA ROCHE , PFLEGER CHRISTOPHE , SPURR PAUL , TRUSSARDI RENE , WALDMEIER PIUS , WANG SHAONING
发明人： PFLEGER CHRISTOPHE , SPURR PAUL , TRUSSARDI RENE , WALDMEIER PIUS , WANG SHAONING
IPC分类号： C07D209/44
CPC分类号： C07D209/44 , C07D471/04
摘要： The invention is concerned with a new scalable process for the preparation of compounds of formula (I) comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula (II) or a salt thereof.
摘要翻译：本发明涉及用于制备式（I）化合物的新的可伸缩方法，其包括制备关键中间体的新方法，二氢吡咯衍生物式（II）或其盐。

6. 发明专利

JP2001270865A METHOD FOR PRODUCING ETHANESULFONYLPIPERIDINE DERIVATIVE 失效
公开(公告)号：JP2001270865A
公开(公告)日：2001-10-02
申请号：JP2001082991
申请日：2001-03-22
申请人： HOFFMANN LA ROCHE
发明人： CRAMERI YVO , SCALONE MICHELANGELO , WALDMEIER PIUS , WIDMER ULRICH
IPC分类号： A61K31/445 , A61P25/04 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07B53/00 , C07B61/00 , C07C315/04 , C07C317/22 , C07D211/42 , C07D211/74
摘要： PROBLEM TO BE SOLVED: To provide a method for selectivity producing an ethanesulfonylpiperidine derivative enantio-selectivity in a high yield without passing through an unstable intermediate. SOLUTION: This method for producing the ethanesulfonylpiperidine derivative having a stereo specific structure comprises reacting a protected amino acid ester with a 4-substituted butyric acid derivative in the presence of a base, then cyclizing, bezylating the obtained protected 3-oxopiperidine carboxylic acid alkyl salt, then decarboxylating in the presence of a strong acid, asymmetrically hydrogenating in the presence of a ruthenium complex containing a chiral disphosphine ligand and a chiral diamine, de-protecting the protection group (the order of the asymmetric hydrogenation and the de-protection can be reversed) and then reacting the de-protected product with a sulfone derivative.

7. 发明专利

JP2001151755A METHOD FOR PRODUCING PYRIDINE DERIVATIVE 失效
公开(公告)号：JP2001151755A
公开(公告)日：2001-06-05
申请号：JP2000360682
申请日：2000-11-28
申请人： HOFFMANN LA ROCHE
发明人： HILPERT HANS , HOFFMANN-EMERY FABIENNE , RIMMLER GOESTA , ROGERS-EVANS MARK , STAHR HELMUT WERNER , WALDMEIER PIUS
IPC分类号： A61K31/496 , A61K31/5377 , A61P1/08 , A61P25/18 , A61P25/22 , A61P25/24 , C07D213/75 , C07D213/76 , C07D213/82
摘要： PROBLEM TO BE SOLVED: To provide a new method for producing a pyridine derivative. SOLUTION: This method is to produce a compound represented by formula I [wherein R1 is a lower alkyl or an aryl; R2 and R2' are each H, a halogen or the like or are combined with each other into CH=CH-CH=CH; R3 and R3' are each H or a lower alkyl or form a cycloalkyl together with carbon atom combined with R3 and R3'; R4 is H, a lower alkyl, N(R5)2 or the like; R5s are each H, a lower alkyl or the like; R6 is H, hydroxyl, a lower alkyl or the like; X is C(O)N(R5) or N(R5)C(O); and (n) is 0 to 4].

8. 发明专利

SI2768827T1 POSTOPEK ZA PRIPRAVO IZOKSAZOLIL-METOKSI-NIKOTINSKIH KISLIN 未知
公开(公告)号：SI2768827T1
公开(公告)日：2017-04-26
申请号：SI201230864
申请日：2012-10-17
申请人： HOFFMANN LA ROCHE
发明人： DOTT PASCAL , HANLON STEVEN PAUL , HILDBRAND STEFAN , IDING HANS , THOMAS ANDREW , WALDMEIER PIUS
IPC分类号： C07D413/00 , C07D487/00

9. 发明专利

BRPI0715096B1 preparação de (s) -1,1,1-triflúor-2-propanol enantiomericamente puro por hidrogenação assimétrica de 1,1,1-trifluoracetona 未知
公开(公告)号：BRPI0715096B1
公开(公告)日：2016-11-08
申请号：BRPI0715096
申请日：2007-07-17
申请人： HOFFMANN LA ROCHE
发明人： PUENTENER KURT , WALDMEIER PIUS
IPC分类号： C07C29/145 , C07C31/38
摘要： patente de invenção: "preparação de (s)-1,1,1-triflúor-2- propanol enantiomericamente puro por hidrogenação assimétrica de 1,1 ,1-trifluoracetona". a invenção refere-se à preparação de , 1,1 -triflúor-2- propanol enantiomericamente puro por uma hidrogenação assimétrica de 1,1,1 -trifluoracetona cujo processo compreende hidrogenação de 1 ,1,1- trifluoracetona na presença de um complexo de rutênio fosfina representado pela fórmula ru(e)(e')(l)(a) onde e, e' são ambos cloro ou e é hidrogênio e e' é bh4; l é um ligante de difosfina quiral; e a é uma diamina opcionalmente quiral compreendendo as variantes a) na presença de uma base fraca e com ou sem aditivo no caso em que e e e' são ambos cloro ou b) na 15 ausência de base e aditivo no caso em que e e e' são hidrogênio e bh4.

10. 发明专利

SI2595958T1 NOVI POSTOPKI ZA PROIZVODNJO (3-(5-(4-KLORO-FENIL)-1H-PIROLO(2,3-B)PIRIDIN-3-KARBONIL)-2,4-DIFLUORO- FENIL)-AMIDA PROPAN-1-SULFONSKE KISLINE 未知
公开(公告)号：SI2595958T1
公开(公告)日：2015-07-31
申请号：SI201130506
申请日：2011-07-18
申请人： HOFFMANN LA ROCHE
发明人： BRUMSTED COREY JAMES , MOORLAG HENDRIK , RADINOV ROUMEN NIKOLAEV , REN YI , WALDMEIER PIUS
IPC分类号： C07D213/00 , C07D471/00

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