公开(公告)号：US20220324865A1

公开(公告)日：2022-10-13

申请号：US17055190

申请日：2019-05-10

Applicant: Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

Inventor： Steffen MUELLER ,  Rudolf SCHOHE-LOOP ,  Nuria ORTEGA HERNANDEZ ,  Frank SUESSMEIER ,  Eloisa JIMENEZ NUNEZ ,  Thomas BRUMBY ,  Niels LINDNER ,  Christoph GERDES ,  Elisabeth POOK ,  Anja BUCHMUELLER ,  Fabienne Zdenka GAUGAZ ,  Dieter LANG ,  Stefanie ZIMMERMANN ,  Alexander Helmut Michael EHRMANN ,  Michael GERISCH ,  Lutz LEHMANN ,  Andreas TIMMERMANN ,  Martina SCHAEFER ,  Georg SCHMIDT ,  Karl-Heinz SCHLEMMER ,  Markus FOLLMANN ,  Elisabeth KERSTEN ,  Vivian WANG ,  Xiang GAO ,  Yafeng WANG

IPC: C07D487/04 ,  A61P7/02

Abstract: The invention relates to substituted dihydropyrazolo pyrazine carboxamide derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and diabetes, and also urogenital and ophthalmic disorders.

公开(公告)号：US20240182431A1

公开(公告)日：2024-06-06

申请号：US18278750

申请日：2022-03-14

Applicant: Bayer Aktiengesellschaft

Inventor： Thomas BRUMBY ,  Jessica LOHRKE ,  Simon Anthony HERBERT ,  Olaf PANKNIN ,  Thomas FRENZEL ,  Claudia GREEN ,  Gregor JOST ,  Hubertus PIETSCH ,  Markus BERGER ,  Sven WITTROCK

IPC: C07D257/02 ,  A61K49/08 ,  C07F5/00

CPC classification number: C07D257/02 ,  A61K49/085 ,  C07F5/003

Abstract: The present invention relates to a new class of compounds of general formula (I), the Gd3+ chelate complexes thereof, to methods of preparing said compounds, and to the use of said compounds as MRI contrast agents. Formula (I)

公开(公告)号：US20240156999A1

公开(公告)日：2024-05-16

申请号：US18275375

申请日：2022-01-31

Applicant: Bayer Aktiengesellschaft ,  Bayer AS

Inventor： Thomas BRUMBY ,  Alan CUTHBERTSON ,  Bård INDREVOLL ,  Waqas RAFIQUE ,  Vilde Roko KROGSTIE ,  Véronique CRUCIANI ,  Alexander KRISTIAN

IPC: A61K51/10 ,  A61K51/04 ,  A61P35/00 ,  C07D413/14

CPC classification number: A61K51/1096 ,  A61K51/0482 ,  A61P35/00 ,  C07D413/14

Abstract: The present invention covers compounds of general formula (I): [(C)n-L]-(V)m (I) where C is a chelator and n>1, L is a multi-functional linker moiety comprising multiple functional groups for the covalent attachment of chelator such as a polyamine or polyacid-containing backbone or amino acid containing polymer comprising side-chains with amino, thiol or carboxylic acid moieties such as lysine, cysteine or glutamic acid and V is a tissue targeting moiety where m=1-5 which preferentially coupled through a coupling moiety to either the multifunctional linker moiety L or directly to the chelator moiety C, and stereoisomers, tautomers, N-oxides, hydrates, solvates, and salts thereof, and mixtures of same.

公开(公告)号：US20220008562A1

公开(公告)日：2022-01-13

申请号：US17295647

申请日：2019-11-21

Applicant: BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT

Inventor： Stephan HOLZSCHUH ,  Thomas FRENZEL ,  Gregor JOST ,  Jessica LOHRKE ,  Wolfgang EBERT ,  Thomas BRUMBY ,  Wolfgang HALFBRODT

IPC: A61K49/10 ,  A61K49/08 ,  A61K49/12

Abstract: The present disclosure relates to a liquid pharmaceutical formulation comprising a DOSA-derived tetra-chelate of formula (I), in which M is an ion of a paramagnetic metal, preferably a Gd3+ ion, and R1, R2, R3, R4 and R5 are as defined in the claims, in a pharmaceutical acceptable solvent. The present disclosure also relates to a method of preparation of said liquid pharmaceutical formulation and to a method of imaging involving said liquid pharmaceutical formulation.