公开(公告)号：US20210253573A1

公开(公告)日：2021-08-19

申请号：US17271141

申请日：2019-08-22

Applicant: Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

Inventor： Johannes PLATZEK ,  Philipp RUBENBAUER ,  Hendricus Nicolaas Sebastiaan VAN DER HAAS ,  Sonja Elisabeth HOOGEVEEN ,  Matthijs Cornelis Maria VAN OERS ,  Reinerus Gerardus GIELING ,  Jeroen Alexander DEKKER

IPC: C07D471/04

Abstract: The present invention covers a method for preparing 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine (“the compound of formula (I)” in the following) as well as intermediate compounds useful in the preparation of the compound of formula (I). The present invention also covers polymorphic form B of the compound of formula (I) with very high purity.

公开(公告)号：US20240376103A1

公开(公告)日：2024-11-14

申请号：US18742346

申请日：2024-06-13

Applicant: Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

Inventor： Johannes PLATZEK ,  Kai LOVIS ,  Winfried JOENTGEN

IPC: C07D471/04

Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also to the preparation of the enantiomer (Ia) by racemate resolution using chiral substituted tartaric acid esters of the general formulae (IIIa) and (IIIb) where Ar represents a substituted or unsubstituted aromatic or heteroaromatic radical.

公开(公告)号：US20210163474A1

公开(公告)日：2021-06-03

申请号：US17050303

申请日：2019-04-23

Applicant: Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

Inventor： Johannes PLATZEK ,  Kai LOVIS ,  Winfried JOENTGEN

IPC: C07D471/04

Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and also to the preparation of the enantiomer (Ia) by racemate resolution using chiral substituted tartaric acid esters of the general formulae (IIIa) and (IIIb) where Ar represents a substituted or unsubstituted aromatic or heteroaromatic radical.

公开(公告)号：US20220098201A1

公开(公告)日：2022-03-31

申请号：US17310347

申请日：2020-01-27

Applicant: Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

Inventor： Jörg GRIES ,  Johannes PLATZEK ,  Claus-Christian HÄSELHOFF ,  Kai LOVIS

IPC: C07D487/04

Abstract: Compound (III) which is the crystalline form of [4-{[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrrolo[2, -f] [1,2,4]triazin-7-yl]methyl}piperazin-2-one hydrochloride] which is the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and its use in the control of disorders, including cancer.

公开(公告)号：US20190210979A1

公开(公告)日：2019-07-11

申请号：US16336217

申请日：2017-09-11

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： Johannes PLATZEK ,  Wilhelm TRENTMANN

IPC: C07D257/02

Abstract: A method is described for production of a high purity compound of the formula (I) in crystalline form of the modification A. In this, starting from high purity gadobutrol, the gadolinium is removed by decomplexation with oxalic acid, and then with a calcium salt the calcium complex is produced in high purity. During the crystallization, a water equivalent of 9-11 weight % is set. The crystalline form of the modification A of the compound of the formula (I) is used in the production of Gadovist.

公开(公告)号：US20180244670A1

公开(公告)日：2018-08-30

申请号：US15753849

申请日：2016-08-18

Applicant: BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： Johannes PLATZEK

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07B2200/07

Abstract: The present invention relates to a novel and improved process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I)

公开(公告)号：US20220356194A1

公开(公告)日：2022-11-10

申请号：US17691858

申请日：2022-03-10

Applicant: Bayer Pharma Aktiengesellschaft

Inventor： Jörg GRIES ,  Johannes PLATZEK

IPC: C07F5/02 ,  C07D333/54 ,  C07D333/72 ,  C07D487/04

Abstract: A process for preparing the benzothiophen-2-yl boronate of formula (VI) which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of proliferative disorders, such as cancer and tumor diseases.

公开(公告)号：US20200339606A1

公开(公告)日：2020-10-29

申请号：US16759139

申请日：2018-10-18

Applicant: Bayer Pharma Aktiengesellschaft

Inventor： Jörg GRIES ,  Johannes PLATZEK

IPC: C07F5/02 ,  C07D333/72 ,  C07D333/54 ,  C07D487/04

Abstract: A process for preparing the benzothiophen-2-yl boronate of formula (VI) which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of proliferative disorders, such as cancer and tumor diseases.

公开(公告)号：US20190144420A1

公开(公告)日：2019-05-16

申请号：US16097463

申请日：2017-04-25

Applicant: Bayer Pharma Aktiengesellschaft

Inventor： Tobias THALER ,  Johannes PLATZEK ,  Nicolas GUIMOND

IPC: C07D401/12

Abstract: The present invention relates to a novel method of preparing a 2-substituted indazole of formula (I) to novel intermediate compounds, and to the use of intermediate compounds for the preparation of said 2-substituted indazole.

公开(公告)号：US20190106407A1

公开(公告)日：2019-04-11

申请号：US16097065

申请日：2017-04-25

Applicant: Bayer Pharma Aktiengesellschaft

Inventor： Tobias THALER ,  Johannes PLATZEK ,  Nicolas GUIMOND

IPC: C07D401/12 ,  C07D231/56 ,  C07D213/54

Abstract: The present invention relates to a novel method of preparing a 2-substituted indazole of structure: (I), to intermediate compounds, and to the use of intermediate compounds for the preparation of said 2-substituted indazole.