公开(公告)号：US20190233477A1

公开(公告)日：2019-08-01

申请号：US16093943

申请日：2017-04-13

Applicant: DSM Sinochem Pharmaceuticals Netherlands B.V. ,  Rijksuniversiteit Groningen

Inventor： Roelof Ary Lans Bovenberg ,  Ulrike Maria Muller ,  Arnold Jacob Mathieu Driessen ,  Pohl Carsten ,  Reto Daniel Zwahlen

IPC: C07K14/195 ,  C12P15/00 ,  C12P17/02 ,  C12P35/00 ,  C12P37/00 ,  C12N1/14

CPC classification number: C07K14/195 ,  C12N1/14 ,  C12P15/00 ,  C12P17/02 ,  C12P35/00 ,  C12P37/00

Abstract: The present invention relates to a method to improve the production of a secondary metabolite catalyzed by a non-ribosomal peptide synthetase comprising contacting in a eukaryotic host a eukaryotic non-ribosomal peptide synthetase with an MbtH-like protein. The present invention further relates to a composition comprising a eukaryotic non-ribosomal peptide synthetase that is not a hybrid and a prokaryotic MbtH and to a eukaryotic host cell comprising a non-ribosomal peptide synthetase and a polynucleotide allowing the expression of an MbtH-like protein.

公开(公告)号：US20180327807A1

公开(公告)日：2018-11-15

申请号：US15776949

申请日：2016-11-17

Applicant: DSM Sinochem Pharmaceuticals Netherlands B.V.

Inventor： Leendert Marinus HANEMAAIJER ,  Dhiredj Chandre JAGESAR

IPC: C12Q1/18

CPC classification number: C12Q1/18

Abstract: The present invention relates to a simple and easy-to-use method for the rapid determination of the presence of an antibiotic in a waste such as e.g. liquid or solid waste streams from plants. The present invention also relates to a kit comprising an as say and a manual for the rapid determination of the presence of an antibiotic in a waste.

公开(公告)号：US09820943B2

公开(公告)日：2017-11-21

申请号：US14915729

申请日：2014-09-01

Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.

Inventor： Rajinder Kapoor ,  Naresh Sharma ,  Neeraj Tewari

IPC: A61K9/14 ,  A61K31/43 ,  C12P37/04 ,  C07D499/00

CPC classification number: A61K9/14 ,  A61K31/43 ,  C07D499/00 ,  C12P37/04

Abstract: The present invention relates to amoxicillin trihydrate compositions having a surface area of from 1.0 to 2.5 m2·g−1 that are free of organic contaminants such as dichloromethane, isopropanol, pivalic acid and triethyl amine and that have a purity of from 97.0% to 99.99%. Furthermore, the present invention relates to a method for the preparation of said amoxicillin trihydrate compositions and to the use of said compositions for the treatment of a bacterial infection.

公开(公告)号：US09260423B2

公开(公告)日：2016-02-16

申请号：US14363986

申请日：2012-12-06

Applicant: DSM Sinochem Pharmaceuticals Netherlands B.V.

Inventor： Ben De Lange ,  Dennis Heemskerk ,  Karin Henderika Maria Bessembinder

IPC: C07D405/12 ,  C07D417/12 ,  C07D319/06

CPC classification number: C07D417/12 ,  C07D319/06 ,  C07D405/12

Abstract: The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.

Abstract translation: 本发明涉及制备用于合成己酸衍生的他汀类药物的前体的方法和所述前体在制备药物中的用途。

公开(公告)号：US20150112057A1

公开(公告)日：2015-04-23

申请号：US14128818

申请日：2012-06-21

Applicant: Harold Monro Moody ,  Claudia Cusan ,  Edwin Gerard Ijpeij

Inventor： Harold Monro Moody ,  Claudia Cusan ,  Edwin Gerard Ijpeij

IPC: C07D501/57 ,  C12P35/00

CPC classification number: C07D501/57 ,  C12P35/00

Abstract: The present invention relates to a crystalline form of an intermediate for cefoperazone of formula (1) and to a process for the preparation thereof by enzymatic condensation of a 3′-thiosubstituted β-lactam nucleus with a phenylglycine derivative.

Abstract translation: 本发明涉及式（1）的头孢哌酮的中间体的结晶形式及其通过3'-取代的β-内酰胺核与苯基甘氨酸衍生物的酶促缩合制备的方法。

公开(公告)号：US08987478B2

公开(公告)日：2015-03-24

申请号：US14363980

申请日：2012-12-06

Applicant: DSM Sinochem Pharmaceuticals Netherlands B.V.

Inventor： Ben De Lange ,  Dennis Heemskerk ,  Karin Henderika Maria Bessembinder

IPC: C07D319/06 ,  C07D417/12 ,  C07D233/96 ,  C07D405/12

CPC classification number: C07D417/12 ,  C07D233/96 ,  C07D319/06 ,  C07D405/12

Abstract: The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.

Abstract translation: 本发明涉及一种制备用于合成己酸衍生的他汀类药物的前体的方法以及所述前体在制备药物中的用途。

公开(公告)号：US20130296561A1

公开(公告)日：2013-11-07

申请号：US13979976

申请日：2012-01-13

Applicant: Karin Henderika Maria Bessembinder ,  Dennis Heemskerk ,  Ben De Lange

Inventor： Karin Henderika Maria Bessembinder ,  Dennis Heemskerk ,  Ben De Lange

IPC: C07D405/06

CPC classification number: C07D405/06 ,  C07D413/12 ,  C07D419/12

Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.

Abstract translation: 本发明涉及在碱金属烷氧基的存在下，通过醛和砜衍生物之间的朱莉娅 - 科奇宁斯基反应制备他汀类药物的方法。 所得衍生物适合作为他汀类化合物如西立伐他汀，氟伐他汀，匹伐他汀和罗苏伐他汀的结构单元。

公开(公告)号：US08263784B2

公开(公告)日：2012-09-11

申请号：US13126871

申请日：2009-10-27

Applicant: Ben De Lange ,  Dennis Heemskerk

Inventor： Ben De Lange ,  Dennis Heemskerk

IPC: C07D209/02

CPC classification number: C07D209/52

Abstract: The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril.

Abstract translation: 本发明涉及在含有钴和/或镍的催化剂存在下制备通式（1）的八氢环戊并[b]吡咯-2-羧酸及其酯的方法，以及使用一般化合物 式（1）中雷米普利的合成。

公开(公告)号：US09556233B2

公开(公告)日：2017-01-31

申请号：US14915997

申请日：2014-09-08

Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.

Inventor： Paulus Bernardus Maria Groen ,  Peter Philip Lankhorst ,  Burhan Özalp ,  Robertus Mattheus De Pater

IPC: C07K7/56

CPC classification number: C07K7/56

Abstract: The present invention relates to a novel cyclohexapeptide, to a method for the preparation of said cyclohexapeptide and to the use of said cyclohexapeptide.

Abstract translation: 本发明涉及一种新的环己肽，涉及制备所述环己肽的方法和所述环己肽的用途。

公开(公告)号：US20130296563A1

公开(公告)日：2013-11-07

申请号：US13979755

申请日：2012-01-13

Applicant: Ben De Lange

Inventor： Ben De Lange

IPC: C07D405/12 ,  C07D405/14 ,  C07D405/06

CPC classification number: C07D405/12 ,  C07D405/06 ,  C07D405/14 ,  C07D413/12 ,  C07D419/12

Abstract: The present invention relates to a process for the preparation of a 1-methyl-1H-tetrazole-5-thio derivative comprising reaction of a halomethyl substrate with 1-methyl-H-tetrazole-5-thiol to obtain a thio-ether compound, and oxidizing the thio-ether compound to the corresponding sulfone. In case of a chiral halomethyl substrate, the resulting chiral diol sulfone derivative is suitable as a building block for statin type compounds.

Abstract translation: 本发明涉及1-甲基-1H-四唑-5-硫代衍生物的制备方法，其包括卤甲基底物与1-甲基-4-四唑-5-硫醇的反应，得到硫代醚化合物， 并将硫代醚化合物氧化成相应的砜。 在手性卤代甲基底物的情况下，所得手性二醇砜衍生物适合作为他汀类化合物的结构单元。