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：US06518048B2

公开(公告)日：2003-02-11

申请号：US09811862

申请日：2001-03-19

Applicant: Hans Iding ,  Beat Wirz ,  Ulrich Zutter

Inventor： Hans Iding ,  Beat Wirz ,  Ulrich Zutter

IPC: C12P1300

CPC classification number: C07D263/58 ,  C07C227/00 ,  C07C229/48 ,  C07C231/00 ,  C07C247/14 ,  C07C2601/14 ,  C07C2601/16 ,  C12P7/42 ,  C12P7/62 ,  C12P41/005 ,  Y02P20/55 ,  C07C233/52

Abstract: The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula starting from an isophthalic acid derivative of formula 4,5-Diamino shikimic acid derivatives are potent inhibitors of viral neuraminidase.

Abstract translation: 本发明提供了一种用于制备由式4,5间二苯二甲酸衍生物配制的4,5-二氨基莽草酸衍生物的多步合成。二氨基莽草酸衍生物是病毒神经氨酸酶的有效抑制剂。

公开(公告)号：US06277997B1

公开(公告)日：2001-08-21

申请号：US09693056

申请日：2000-10-20

Applicant: Michelangelo Scalone ,  Ulrich Zutter

Inventor： Michelangelo Scalone ,  Ulrich Zutter

IPC: C07D20740

CPC classification number: C07D401/06 ,  C07D405/06

Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.

Abstract translation: 本发明涉及制备式I化合物的方法，其中R1和R2如说明书中所定义，以及通过所述方法获得的新型中间体。

公开(公告)号：US5902882A

公开(公告)日：1999-05-11

申请号：US832253

申请日：1997-04-03

Applicant: Peter Karl Matzinger ,  Michelangelo Scalone ,  Ulrich Zutter

Inventor： Peter Karl Matzinger ,  Michelangelo Scalone ,  Ulrich Zutter

IPC: C07D223/08 ,  C07D223/12 ,  C07D498/04

CPC classification number: C07D223/12 ,  C07D223/08 ,  Y02P20/55

Abstract: A novel process for the manufacture of compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.

Abstract translation: 一种用于制备下式化合物的新方法，其中R1和R2独立地表示芳酰基。 本发明还涉及用于制备式I化合物的新方法中的新型中间体。

公开(公告)号：US5399720A

公开(公告)日：1995-03-21

申请号：US77475

申请日：1993-06-15

Applicant: Martin Karpf ,  Ulrich Zutter

Inventor： Martin Karpf ,  Ulrich Zutter

IPC: C07D20060101 ,  C07D305/12 ,  C07D309/30 ,  C07D309/32 ,  C07D309/38

CPC classification number: C07D305/12 ,  C07D309/30 ,  C07D309/32 ,  C07D309/38

Abstract: The invention relates to a novel process for producing a compound having the formula ##STR1## wherein R.sup.1, R.sup.2 and X are described herein, via corresponding .beta.-keto- and .beta.-hydroxy-.delta.-lactones, as well as novel intermediates which occur in the process.

Abstract translation: 本发明涉及通过相应的β-酮和β-羟基-δ-内酯生产具有式Ⅰ化合物的新方法，其中R 1，R 2和X如本文所述，以及发生的新型中间体 正在进行中。

公开(公告)号：US07312343B2

公开(公告)日：2007-12-25

申请号：US11140319

申请日：2005-05-27

Applicant: Rudolf Schmid ,  Ulrich Zutter

Inventor： Rudolf Schmid ,  Ulrich Zutter

IPC: C07D207/08 ,  C07C211/27

CPC classification number: C07D207/08 ,  C07C215/08 ,  C07C217/40 ,  C07C223/02 ,  C07C229/12 ,  C07C229/22 ,  C07C271/16 ,  C07C271/18 ,  C07C271/22

Abstract: Compounds of formula I and a process for the preparation of such compounds are disclosed.

Abstract translation: 公开了式I化合物及其制备方法。

公开(公告)号：US20060270853A1

公开(公告)日：2006-11-30

申请号：US11438034

申请日：2006-05-19

Applicant: Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes ,  Joseph Foricher ,  Bruno Lohri ,  Patrizio Mattei ,  Gerard Moine ,  Rudolf Schmid ,  Ulrich Zutter

Inventor： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes ,  Joseph Foricher ,  Bruno Lohri ,  Patrizio Mattei ,  Gerard Moine ,  Rudolf Schmid ,  Ulrich Zutter

IPC: C07D471/04 ,  C07F15/02 ,  C07D305/12

CPC classification number: C07D307/33 ,  C07D307/34 ,  C07D307/38 ,  C07D307/58 ,  C07D471/04

Abstract: This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

Abstract translation: 本发明涉及式（S）-4-氟甲基 - 二氢呋喃-2-酮新型中间体的制备方法及其制备吡啶并[2,1-a]异喹啉衍生物的用途 可用于治疗和/或预防与DPP IV有关的疾病的配方。

公开(公告)号：US06914140B1

公开(公告)日：2005-07-05

申请号：US09546143

申请日：2000-04-10

Applicant: Peter Karl Matzinger ,  Michelangelo Scalone ,  Ulrich Zutter

Inventor： Peter Karl Matzinger ,  Michelangelo Scalone ,  Ulrich Zutter

IPC: C07D223/08 ,  C07D223/12 ,  C07D498/04 ,  C07D201/16

CPC classification number: C07D223/12 ,  C07D223/08

Abstract: A novel process for the manufacture of compounds of the formula wherein R1 and R2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.

Abstract translation: 用于制备下式化合物的新方法其中R 1和R 2独立地代表芳酰基。 本发明还涉及用于制备式I化合物的新方法中的新型中间体。

公开(公告)号：US07619101B2

公开(公告)日：2009-11-17

申请号：US11438034

申请日：2006-05-19

Applicant: Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes ,  Joseph Foricher ,  Bruno Lohri ,  Patrizio Mattei ,  Gerard Moine ,  Rudolf Schmid ,  Ulrich Zutter

Inventor： Stefan Abrecht ,  Jean-Michel Adam ,  Alec Fettes ,  Joseph Foricher ,  Bruno Lohri ,  Patrizio Mattei ,  Gerard Moine ,  Rudolf Schmid ,  Ulrich Zutter

IPC: C07D307/00

CPC classification number: C07D307/33 ,  C07D307/34 ,  C07D307/38 ,  C07D307/58 ,  C07D471/04

Abstract: This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

Abstract translation: 本发明涉及式（S）-4-氟甲基 - 二氢呋喃-2-酮新型中间体的制备方法及其制备吡啶并[2,1-a]异喹啉衍生物的用途 可用于治疗和/或预防与DPP IV有关的疾病的配方。

公开(公告)号：US5481008A

公开(公告)日：1996-01-02

申请号：US298734

申请日：1994-08-31

Applicant: Emil A. Broger ,  Martin Karpf ,  Ulrich Zutter

Inventor： Emil A. Broger ,  Martin Karpf ,  Ulrich Zutter

IPC: B01J31/22 ,  C07B53/00 ,  C07B57/00 ,  C07B61/00 ,  C07D309/32 ,  C07D309/34 ,  C07D309/30

CPC classification number: C07D309/32

Abstract: A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,R.sup.3 is hydrogen, lower alkyl, optionally substituted benzyl, --CO--R.sup.4, --COOR.sup.4 or --CONR.sub.2.sup.4, andR.sup.4 is lower alkyl or aryl,comprising asymmetrically hydrogenating a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the above significance, in the presence of a complex of an optically active, preferably atropisomeric, diphospine ligand with a metal of Group VIII.

Abstract translation: 一种用于制备下式的光学活性化合物的催化方法，其中R 1和R 2为烷基，其任选地被除了α-或β-位之外的O原子中断，或任选取代的苄基，R 3 包括不对称氢化下式化合物，其中R1，R2和R3具有上述基团，其中R 1，R 2和R 3具有以下基团 在具有第VIII族金属的光学活性的，优选的阻转异构的双峰配体的络合物的存在下。