公开(公告)号：US08642802B2

公开(公告)日：2014-02-04

申请号：US13606052

申请日：2012-09-07

Applicant: Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

Inventor： Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

IPC: C07C51/16

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通用的中间体 用于制备活性药物或农药。

公开(公告)号：US20120330055A1

公开(公告)日：2012-12-27

申请号：US13606052

申请日：2012-09-07

Applicant: Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

Inventor： Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

IPC: C07C51/295

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.

公开(公告)号：US20120130121A1

公开(公告)日：2012-05-24

申请号：US13365353

申请日：2012-02-03

Applicant: Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

Inventor： Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

IPC: C07C51/29 ,  C07C51/285 ,  C07C51/305 ,  C07C51/16

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通用的中间体 用于制备活性药物或农药。

公开(公告)号：US20110054174A1

公开(公告)日：2011-03-03

申请号：US12859795

申请日：2010-08-20

Applicant: Stephan Bachmann ,  Alec Fettes ,  Hans Iding ,  Beat Wirz ,  Ulrich Zutter

Inventor： Stephan Bachmann ,  Alec Fettes ,  Hans Iding ,  Beat Wirz ,  Ulrich Zutter

IPC: C07D241/20 ,  C07C233/01 ,  C12P17/12

CPC classification number: C07D241/20 ,  C07C259/06

Abstract: The present invention relates to a process for the preparation of a compound of formula I, wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen.(R)-2-phenyl propionic acid derivatives of formula I are key intermediates in the synthesis of 5-substituted-pyrazine or pyridine glucokinase activators of the formula Xa, which have the potential to be useful for the treatment and/or prophylaxis of type II diabetes.

Abstract translation: 本发明涉及制备式I化合物的方法，其中R 1为C 1-6 - 烷基且R 2为氢或卤素。 式I的（R）-2-苯基丙酸衍生物是合成式Xa的5-取代 - 吡嗪或吡啶葡萄糖激酶活化剂的关键中间体，其具有可用于治疗和/或预防类型 II型糖尿病

公开(公告)号：US20090306423A1

公开(公告)日：2009-12-10

申请号：US12474434

申请日：2009-05-29

Applicant: Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

Inventor： Stephan Bachmann ,  Stefan Hildbrand ,  James Jappy ,  Dinesh Maganbhai Patel ,  Christophe Pfleger ,  Robert John Ernest Tidswell ,  Rene Trussardi

IPC: C07C51/16 ,  C07C51/00 ,  C07C51/29

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：US20130253201A1

公开(公告)日：2013-09-26

申请号：US13897087

申请日：2013-05-17

Applicant: Stephan Bachmann ,  Michelangelo Scalone ,  Patrick Schnider

Inventor： Stephan Bachmann ,  Michelangelo Scalone ,  Patrick Schnider

IPC: C07C51/36 ,  C07D401/04 ,  C07D211/60

CPC classification number: C07C51/36 ,  C07D207/16 ,  C07D211/60 ,  C07D401/04

Abstract: The present invention relates to a process for the preparation of cis substituted cyclic β-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme wherein X, Ar, n, and m are defined herein and corresponding salts thereof.

Abstract translation: 本发明涉及按照以下方案制备具有高非对映选择性和对映选择性的顺式取代的环状β-芳基或杂芳基羧酸衍生物的方法，其中X，Ar，n和m在本文中定义， 其相应的盐。

公开(公告)号：US20130059833A1

公开(公告)日：2013-03-07

申请号：US13598848

申请日：2012-08-30

Applicant: Stephan Bachmann ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

Inventor： Stephan Bachmann ,  Alexander Flohr ,  Katrin Groebke Zbinden ,  Matthias Koerner ,  Bernd Kuhn ,  Jens-Uwe Peters ,  Markus Rudolph

IPC: C07D471/04 ,  C07D403/14 ,  A61K31/4184 ,  C07D413/14 ,  A61K31/4245 ,  C07D401/14 ,  A61K31/4439 ,  A61K31/4178 ,  A61K31/5377 ,  C07D417/14 ,  A61K31/428 ,  A61K31/4155 ,  A61K31/4196 ,  A61K31/4192 ,  A61K31/541 ,  A61P25/18 ,  A61K31/437

CPC classification number: C07D471/04 ,  C07D231/14 ,  C07D233/90 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.

Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 5，W，X，X 1，Y，Y 1，Z和Z 1如说明书和权利要求书中所定义，以及生理上可接受的盐 其中。 这些化合物抑制PDE10A，可用于治疗CNS疾病如精神分裂症，阿尔茨海默病和帕金森病。

公开(公告)号：US20110040091A1

公开(公告)日：2011-02-17

申请号：US12843081

申请日：2010-07-26

Applicant: Stephan Bachmann ,  Alec Fettes ,  Michelangelo Scalone

Inventor： Stephan Bachmann ,  Alec Fettes ,  Michelangelo Scalone

IPC: C07D241/20 ,  C07C315/00

CPC classification number: C07D261/04 ,  B01J31/189 ,  B01J31/2295 ,  B01J31/2409 ,  B01J31/2433 ,  B01J2231/645 ,  B01J2531/0205 ,  B01J2531/821 ,  B01J2531/822 ,  B01J2531/827 ,  B01J2531/842 ,  C07B53/00 ,  C07B2200/07 ,  C07C315/02 ,  C07C315/04 ,  C07C2601/08 ,  C07D241/20 ,  C07D333/30 ,  C07D409/04 ,  C07C317/44

Abstract: The present invention relates to a process for the preparation of (R)-2-phenyl propionic acid derivatives of the formula wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen, or of a salt thereof.

Abstract translation: 本发明涉及制备下式的（R）-2-苯基丙酸衍生物的方法：其中R 1为C 1-6 - 烷基且R 2为氢或卤素，或其盐。

公开(公告)号：US20090012311A1

公开(公告)日：2009-01-08

申请号：US12145686

申请日：2008-06-25

Applicant: Stephan Bachmann ,  Philippe Pflieger ,  Goesta Rimmler ,  Michelangelo Scalone

Inventor： Stephan Bachmann ,  Philippe Pflieger ,  Goesta Rimmler ,  Michelangelo Scalone

IPC: C07D209/04 ,  C07C271/06

CPC classification number: C07C271/28 ,  C07D209/08 ,  C07F7/081

Abstract: A process for the preparation of indole derivatives of formula (I): which are useful as intermediates in the preparation of pharmaceutically active compounds.

Abstract translation: 制备式（I）的吲哚衍生物的方法：其可用作药物活性化合物的制备中的中间体。

公开(公告)号：US20070276142A1

公开(公告)日：2007-11-29

申请号：US10589256

申请日：2005-02-11

Applicant: Nis Halland ,  Karl Jorgensen ,  Mauro Marigo ,  Alan Braunton ,  Stephan Bachmann ,  Doris Schluter

Inventor： Nis Halland ,  Karl Jorgensen ,  Mauro Marigo ,  Alan Braunton ,  Stephan Bachmann ,  Doris Schluter

IPC: C07D207/04 ,  C07C45/00 ,  C07D211/00 ,  C07D211/70 ,  C07D317/72

CPC classification number: C07D207/08 ,  C07B53/00 ,  C07C45/63 ,  C07F7/1804 ,  C07F7/188 ,  C07C47/14 ,  C07C47/24 ,  C07C49/16 ,  C07C49/463 ,  C07C47/353 ,  C07C47/277 ,  C07C47/17

Abstract: A process for the catalytic asymmetric synthesis of an optically active compound of the formula (1a) or (1b) wherein R is an organic group; X is halogen; R1 and R2 which may the same or different represents H, or an organic group or R1 and R2 may be bridged together forming part of a ring system; R and R2 may be bridged together forming part of a ring system; with the provisio that R and R1 are different and R2, when different from H, is attached though a carbon-carbon bond, comprising the step of reacting a compound of the formula (2) with a halogenation agent in the presence of a catalytic amount of a chiral nitrogen containing organic compound.

Abstract translation: 一种用于催化不对称合成式（1a）或（1b）的光学活性化合物的方法，其中R是有机基团; X是卤素; R 1和R 2可以相同或不同，表示H或有机基团或R 1和R 2， SUB>可以桥接在一起形成环系统的一部分; R和R 2可以桥连在一起形成环系的一部分; 条件是R和R 1不同，R 2与H不同时，通过碳 - 碳键连接，包括使下列化合物与 式（2）与卤化剂在催化量的手性含氮有机化合物存在下反应。