公开(公告)号：WO2019197571A1

公开(公告)日：2019-10-17

申请号：PCT/EP2019/059334

申请日：2019-04-11

Applicant: UNIVERSITÄT BIELEFELD ,  PHARMAZELL GMBH

Inventor： LÖWE, Jana ,  UTHOFF, Florian ,  HARMS, Christina ,  GRÖGER, Prof. Dr. Harald ,  DONSBACH, Dr. Kai

IPC: C12P41/00 ,  C12P5/00 ,  C12P17/14

Abstract: The present invention is directed to a process for the enantioselective biocatalytic preparation of 4-substituted 1-aminoindanes of general formula (S)-I: (l) and a process for the preparation of Ozanimod, preferably involving the enantioselective biocatalytic process of preparing (S)-4-substituted 1- aminoindanes of the above general formula, wherein R = -CN and Y = H.

公开(公告)号：WO2016023933A1

公开(公告)日：2016-02-18

申请号：PCT/EP2015/068514

申请日：2015-08-12

Applicant: PHARMAZELL GMBH

Inventor： HUMMEL, Werner ,  BAKONYI, Daniel

IPC: C12N9/04 ,  C12P33/02

CPC classification number: C12P33/02 ,  C12N9/0006 ,  C12Y101/0105 ,  C12Y101/01159 ,  C12Y101/01225

Abstract: Die Erfindung betrifft neuartige 3α-Hydroxysteroid Dehydrogenase-Mutanten, die für diese Enzym-Mutanten kodierenden Sequenzen, Verfahren zur Herstellung der Enzym-Mutanten und deren Verwendung bei enzymatischen Umsetzungen von Cholsäureverbindungen, und insbesondere bei der Herstellung von Ursodesoxycholsaure (UDCS); Gegenstand der Erfindung sind auch neuartige Verfahren zur Synthese von UDCS unter Verwendung der Enzym-Mutanten; sowie die Herstellung von UDCS unter Verwendung rekombinanter, mehrfach modifizierter Mikroorganismen.

Abstract translation: 本发明涉及新的3α羟基类固醇脱氢酶的突变体编码这些突变型酶的序列，制备，特别是在Ursodesoxycholsaure（UDC）的制造中的突变酶及其在Cholsäureverbindungen的酶反应使用的方法; 本发明还涉及一种用于UDC的使用突变型酶合成的新方法; 和UDC的使用重组生产，乘法修饰的微生物。

公开(公告)号：WO2014118802A1

公开(公告)日：2014-08-07

申请号：PCT/IN2014/000051

申请日：2014-01-27

Applicant: PHARMAZELL GMBH ,  PRATHA, Sridhar

Inventor： PRATHA, Sridhar ,  BURGER, Wolfgang ,  PALLA, Venkata Ramana ,  KAPUBALU, Suneel Kumar

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: The present invention provides an improved process for the preparation of pure Clopidogrel bisulfate Form-I of formula (I), which comprises: reacting S(+)-methyl-2- [2-(thiophen-2-yl)ethylamino]-2-(2-chlorophenyl) acetate hydrochloride (Formula II) with Formaldehyde and R-(-) Camphor sulphonic acid to yield S (+)-Clopidogrel camphor sulfonate salt (Formula III), which is on further treatment with C 1-5 carboxylic acid followed by sulphuric acid to get Clopidogrel Form-I.

Abstract translation: 本发明提供了制备式（I）的纯氯吡格雷硫酸氢盐形式I的改进方法，其包括：使S（+） - 甲基-2- [2-（噻吩-2-基）乙基氨基] -2 - （2-氯苯基）乙酸乙酯盐酸盐（式II）与甲醛和R - （ - ）樟脑磺酸反应得到S（+） - 氯吡格雷樟脑磺酸盐（式III），其进一步用C1-5羧酸处理 随后用硫酸得到氯吡格雷I型。

公开(公告)号：WO2012032185A1

公开(公告)日：2012-03-15

申请号：PCT/EP2011/065735

申请日：2011-09-12

Applicant: PHARMAZELL GMBH ,  GAAB, Stefan ,  HARTUNG, Alexander ,  AIGNER, Arno

Inventor： GAAB, Stefan ,  HARTUNG, Alexander ,  AIGNER, Arno

IPC: C07C227/42 ,  C07C229/64 ,  A61K31/606 ,  A61P29/00

CPC classification number: C07C227/42 ,  A61K31/606 ,  C07C229/64

Abstract: Die Erfindung betrifft ein Verfahren zur Herstellung von kristalliner 5-Aminosalicylsäure mit besonders hoher Stampf-und/oder Schüttdichte.

Abstract translation: 本发明涉及一种用于制备结晶5-氨基水杨酸的具有特别高的捣固和/或堆积密度的方法。

公开(公告)号：WO2021176068A1

公开(公告)日：2021-09-10

申请号：PCT/EP2021/055617

申请日：2021-03-05

Applicant: PHARMAZELL GMBH

Inventor： STAUNIG, Nicole ,  DONSBACH, Kai Oliver

IPC: C12N9/02 ,  C12P33/06

Abstract: Die vorliegende Patentanmeldung betrifft ein Enzym und Verfahren zur Hydroxylierung eines 7-Desoxy-Steroids mit der allgemeinen Formel (I) an Position 7 zu einem Steroid mit der allgemeinen Formel (II).

公开(公告)号：WO2020053334A1

公开(公告)日：2020-03-19

申请号：PCT/EP2019/074348

申请日：2019-09-12

Applicant: PHARMAZELL GMBH

Inventor： DONSBACH, Kai ,  PARIHAR, Jayprakash Ajitsingh ,  PRATHA, Sridhar ,  SATYAVARAPU, Chinnayya Setty ,  NALLURI, Leela Kumar ,  MATTURTI, Prasad

IPC: C07D271/06

Abstract: The present invention relates to an improved process for preparation of Ozanimod (I) or pharmaceutically acceptable salts thereof. The present invention also relates to an improved process for preparation of (S)-l-amino-2,3-dihydro- 1H-indene-4-carbonitrile (II) or its optically active acid salts.

公开(公告)号：WO2015197698A3

公开(公告)日：2016-02-25

申请号：PCT/EP2015064264

申请日：2015-06-24

Applicant: PHARMAZELL GMBH

Inventor： WEUSTER-BOTZ DIRK ,  SUN BOQIAO ,  QUIRIN CHRISTIAN

IPC: C12P33/00 ,  C12N9/04

CPC classification number: C12P33/00 ,  C12N9/0006 ,  C12Y101/01047 ,  C12Y101/0105 ,  C12Y101/01145 ,  C12Y101/01201

Abstract: The invention relates to novel biocatalytic processes, comprising the whole cell reduction of dehydrocholic acid (DHCS) compounds, novel 7ß-hydroxysteroid dehydrogenase mutants, to the sequences encoding said enzyme mutants, to methods for producing the enzyme mutants and to the use thereof in enzymatic conversion of cholic acid compounds, and especially in the production of ursodeoxycholic acid (UDCS); The invention also relates to novel methods for the synthesis of UDCS using the enzyme mutants; and in particular to a further improved method for producing UDCS using recombined whole-cell biocatalysts.

Abstract translation: 本发明涉及一种包括去氢胆酸的全细胞减少（深舱货轮）化合物，新7.beta.羟基类固醇脱氢酶的突变体编码这些突变型酶的序列新颖生物催化方法，用于制备突变体酶及其在酶反应使用的方法 Cholsäureverbindungen的，特别是在生产熊去氧胆酸（UDC）的; 本发明还涉及一种用于UDC的使用突变型酶合成的新方法; 并且特别是，对于使用重组全细胞生物催化剂制备UDC进一步改进的方法。

公开(公告)号：WO2009118176A3

公开(公告)日：2010-01-07

申请号：PCT/EP2009002190

申请日：2009-03-25

Applicant: PHARMAZELL GMBH ,  AIGNER ARNO ,  GROSS RALF ,  SCHMID ROLF ,  BRAUN MICHAEL ,  MAUER STEFFEN

Inventor： AIGNER ARNO ,  GROSS RALF ,  SCHMID ROLF ,  BRAUN MICHAEL ,  MAUER STEFFEN

IPC: C12N9/04

CPC classification number: C12P33/02 ,  C12N9/0006 ,  C12Y101/01176

Abstract: The invention relates to 12 a-hydroxysteroid dehydrogenases, nucleic acid sequences coding for the same, expression cassettes and vectors, recombinant microorganisms containing the corresponding coding nucleic acid sequences, a method for producing said 12 a-hydroxysteroid dehydrogenases, a method for enzymatic oxidation of 12 a-hydroxysteroids using said enzyme, a method for enzymatic reduction of 12-ketosteroids using said enzyme, a method for qualitative or quantitative determination of 12-ketosteroids and/or12a-hydroxysteroids using said 12a-hydroxysteroid dehydrogenases and a method for production of ursodesoxycholic acid, comprising the enzyme-catalysed cholic acid oxidation using said 12 a-hydroxysteroid dehydrogenases.

Abstract translation: 本发明涉及新的12-羟基类，用于编码的核酸序列，表达盒和载体; 含对应的编码核酸序列的重组微生物; 用于这种12A羟脱氢酶的制备方法; 过程用于使用这样的酶，用于酶还原的使用这样的酶12-酮甾族化合物的方法12A羟基甾类的酶促氧化; 一种用于定性或定量测定的使用根据本发明的图12A-羟基脱氢酶12酮类固醇和12a羟基甾族化合物的方法; 以及用于制备熊去氧胆酸，其包含根据本发明使用的酶催化Cholsäureoxidation12A羟基类脱氢酶的方法。

公开(公告)号：WO2018036982A1

公开(公告)日：2018-03-01

申请号：PCT/EP2017/071070

申请日：2017-08-22

Applicant: PHARMAZELL GMBH

Inventor： BAKONYI, Daniel ,  HUMMEL, Werner ,  GROSS, Ralf

IPC: C12P33/00 ,  C12P33/06 ,  C12N9/04

CPC classification number: C12P33/00 ,  C12N9/0006 ,  C12P33/06 ,  C12Y101/0105 ,  C12Y101/01159

Abstract: Die Erfindung betrifft ein weiteres chemisch-biokatalytisches Verfahren zur Herstellung von Ursodesoxycholsaure ausgehend von Chenodesoxycholsäure nach chemischer Oxidation zu 3,7-Diketo- Ursodesoxycholsäure und anschließender Umsetzung mit 7-beta- Hydroxysteroid-Dehydrogenase aus C. aerofaciens und 3-alpha- Hydroxysteroid-Dehydrogenase aus C. testosteroni.

Abstract translation:

本发明涉及一种进一步的化学生物催化过程从Chenodesoxychols BEAR酸制备Ursodesoxycholsaure的通过化学氧化3,7-二酮Ursodesoxychols BEAR酸和随后的道形成反应与7-β-羟基类 来自C. testosteroni的C. aerofaciens脱氢酶和3-α羟基类固醇脱氢酶。

公开(公告)号：WO2017220486A3

公开(公告)日：2017-12-28

申请号：PCT/EP2017/064924

申请日：2017-06-19

Applicant: PHARMAZELL GMBH

Inventor： BAKONYI, Daniel ,  HUMMEL, Werner ,  GROSS, Ralf

IPC: C12P33/00 ,  C12P33/02 ,  C12N9/04

Abstract: The present invention relates to a coupled biotransformation process of converting chenodeoxycholic acid (CDCA) and related compounds to ursodeoxycholic acid (UDCA) and related compounds. It also relates to the cloning, expression, and biochemical characterization of a novel NADP + -dependent 7α-hydroxysteroid dehydrogenase (7α-HSDH) from Clostridium difficile , cofactor switch mutants thereof, and their application for the oxidation of bile acids. A further aspect of the invention relates to novel NADP-dependent cofactor switch mutants of the NADP + -dependent 7α-HSDH of E. coli and their application for the oxidation of bile acids.