公开(公告)号：WO2006063706A1

公开(公告)日：2006-06-22

申请号：PCT/EP2005/012991

申请日：2005-12-05

Applicant: F. HOFFMANN-LA ROCHE AG ,  BLISS, Fritz ,  LALONDE, Michel ,  SCHMID, Rudolf ,  TRUSSARDI, Rene

Inventor： BLISS, Fritz ,  LALONDE, Michel ,  SCHMID, Rudolf ,  TRUSSARDI, Rene

IPC: C07D207/08 ,  C07K5/02

CPC classification number: C07D207/08 ,  C07K5/0205

Abstract: The present invention relates to the manufacture of the compounds of formula (I) said compounds of formula (I) being valuable intermediates in the manufacture of Dolastatin 10 analogues, which are useful in the treatment of cancer.

Abstract translation: 本发明涉及式（I）化合物的制备，所述式（I）化合物是制造Dolastatin 10类似物的有价值的中间体，其可用于治疗癌症。

公开(公告)号：WO2006074873A3

公开(公告)日：2006-07-20

申请号：PCT/EP2006/000046

申请日：2006-01-05

Applicant: F. HOFFMANN-LA ROCHE AG ,  SCHMID, Rudolf ,  TRUSSARDI, Rene

Inventor： SCHMID, Rudolf ,  TRUSSARDI, Rene

IPC: C07C209/68 ,  C07C215/52 ,  C07C215/54 ,  C07D207/08

Abstract: The present invention relates to the manufacture of the compounds of formula (I) said compounds of formula (I), or their lithium salts, being valuable intermediates in the manufacture of Dolastatin analogues, which are useful in the treatment of cancer.

公开(公告)号：WO2006024436A1

公开(公告)日：2006-03-09

申请号：PCT/EP2005/009121

申请日：2005-08-24

Applicant: F. HOFFMANN-LA ROCHE AG ,  KARPF, Martin ,  TRUSSARDI, Rene

Inventor： KARPF, Martin ,  TRUSSARDI, Rene

IPC: C07C229/48 ,  C07C227/18 ,  C07C227/10

CPC classification number: C07C229/48 ,  C07C227/10 ,  C07C227/18 ,  C07C2601/16

Abstract: The present invention relates to a process for the preparation of a 4,5-diamino shikimic acid derivative of formula (I) and pharmaceutically acceptable addition salts thereof wherein R 1 , R 1’ are independent of each other H or alkyl, R 2 is an alkyl and R 3 , R 4 are independent of each other H or an alkanoyl, with the proviso that not to both R 3 and R 4 are H. 4,5-diamino shikimic acid derivatives of formula I, especially the (3R,4R,5S)-5­-amino-4-acetylamino-3- (1-ethyl-propoxy)-cyclohex-l-ene-carboxylic acid ethyl ester and its pharmaceutically acceptable additional salts are potent inhibitors of viral neuraminidase.

Abstract translation: 本发明涉及制备式（I）的4,5-二氨基莽虫酸衍生物及其药学上可接受的加成盐的方法，其中R

公开(公告)号：WO2009147068A1

公开(公告)日：2009-12-10

申请号：PCT/EP2009/056560

申请日：2009-05-28

Applicant: F. HOFFMANN-LA ROCHE AG ,  BACHMANN, Stephan ,  HILDBRAND, Stefan ,  JAPPY, James ,  PATEL, Dinesh Maganbhai ,  PFLEGER, Christophe ,  TIDSWELL, Robert John Ernest ,  TRUSSARDI, Rene

Inventor： BACHMANN, Stephan ,  HILDBRAND, Stefan ,  JAPPY, James ,  PATEL, Dinesh Maganbhai ,  PFLEGER, Christophe ,  TIDSWELL, Robert John Ernest ,  TRUSSARDI, Rene

IPC: C07C45/00 ,  C07C51/15 ,  C07C51/285 ,  C07C51/29 ,  C07C63/70 ,  C07C47/55 ,  C07C45/51

CPC classification number: C07C45/518 ,  C07C45/00 ,  C07C51/15 ,  C07C51/285 ,  C07C51/29 ,  C07C47/55 ,  C07C63/70

Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5- trifluoromethyl benzoic acid of the formula or of a salt thereof. 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.

Abstract translation: 本发明包括制备下式的3-氯-2-氟-5-三氟甲基苯甲酸或其盐的方法。 3-氯-2-氟-5-三氟甲基苯甲酸或其盐是用于制备活性药物或农药的多功能中间体。

公开(公告)号：WO2015086495A1

公开(公告)日：2015-06-18

申请号：PCT/EP2014/076831

申请日：2014-12-08

Applicant: F. HOFFMANN-LA ROCHE AG ,  HOFFMANN-LA ROCHE INC.

Inventor： TRUSSARDI, Rene ,  IDING, Hans

IPC: C12P7/22 ,  C12P13/00

CPC classification number: C12P17/14 ,  C07D265/30 ,  C12P7/02 ,  C12P7/22 ,  C12P13/008 ,  Y02P20/55

Abstract: The invention relates to a novel process for the preparation of chiral 2-(4-aminophenyl) morpholines of the formula (I) wherein R1 is hydrogen an amino protecting group. The chiral 2-(4-aminophenyl) morpholines of the formula I are key intermediates for the preparation of compounds that have a good affinity to the trace amine associated receptors (TAARs).

Abstract translation: 本发明涉及制备式（I）的手性2-（4-氨基苯基）吗啉的新方法，其中R1是氢氨基保护基。 式I的手性2-（4-氨基苯基）吗啉是制备与微量胺相关受体（TAAR）具有良好亲和力的化合物的关键中间体。