公开(公告)号：US20180282337A1

公开(公告)日：2018-10-04

申请号：US15524581

申请日：2015-11-05

Applicant: Bayer Pharma Aktiengesellschaft

Inventor： Jan-Georg PETERS ,  Philipp RUBENBAUER ,  Daniel GÖTZ ,  Danja GROßBACH ,  Franz-Josef MAIS ,  Heiko SCHIRMER ,  Juergen STIEHL ,  Kai LOVIS ,  Andreas LENDER ,  Martin SEYFRIED ,  Theodor ZWEIFEL ,  Maurus MARTY ,  Günter WEINGÄRTNER

IPC: C07D487/04 ,  C07D233/24

Abstract: The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.

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：US20170327505A1

公开(公告)日：2017-11-16

申请号：US15524478

申请日：2015-11-05

Applicant: Bayer Pharma Aktiengesellschaft

Inventor： Jan-Georg PETERS ,  Jürgen STIEHL ,  Kai LOVIS

IPC: C07D487/04 ,  C07D295/088 ,  C07D265/30

CPC classification number: C07D487/04 ,  C07D233/24 ,  C07D265/30 ,  C07D295/088

Abstract: The present invention relates to a novel method of preparing copanlisib, and copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib.

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：US20210179541A1

公开(公告)日：2021-06-17

申请号：US16767724

申请日：2018-11-26

Applicant: Bayer Pharma Aktiengesellschaft

Inventor： Peter FEY ,  Philipp RUBENBAUER ,  Kai LOVIS ,  Britta OLENIK ,  Julia KUSEL ,  Felix SPINDLER

IPC: C07C233/88 ,  C07C231/02 ,  C07C231/12 ,  C07C51/09 ,  C07C227/18

Abstract: The present invention relates to a novel and improved process for preparing (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid of the formula (I), to the compound of the formula (I) in crystalline form and to their use for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular, cardiopulmonary and cardiorenal disorders.