Abstract: The invention relates to Spirocyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide of general formula (I) which are inhibitors of phosphodiesterase 2, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
Type:
Grant
Filed:
October 20, 2020
Date of Patent:
July 4, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Christoph Hoenke, Barbara Bertani, Marco Ferrara, Giacomo Fossati, Sara Frattini, Riccardo Giovannini, Scott Hobson
Abstract: The present invention relates to novel 2-[thiophen-2-yl)formamido]-N-(phenyl)-2-methylpropanamides of formula A and pharmaceutically acceptable salts thereof, wherein R1 to R3 are as defined herein. The invention also relates to processes for the preparation of these compound, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions in which inhibition of the indoleamine 2,3-dioxygenase 1 (IDO1) enzyme may be beneficial.
Type:
Grant
Filed:
November 4, 2021
Date of Patent:
July 4, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Stephan Georg Mueller, Kelly Allers, Klaus Klinder, Ursula Mueller-Vieira, Henning Priepke, Alexander Pautsch
Abstract: The disclosure relates to compounds specific for IL23A and TNF-alpha, compositions comprising the compounds, and methods of use thereof. Nucleic acids, cells, and methods of production related to the compounds and compositions are also disclosed.
Type:
Grant
Filed:
August 26, 2020
Date of Patent:
June 20, 2023
Assignees:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH, MACROGENICS, INC.
Inventors:
Rachel Rebecca Barrett, Leslie S. Johnson, Sanjaya Singh, Kathleen Last-Barney, Daw-Tsun Shih, Patricia Giblin, Scott Brodeur, Nelamangala Nagaraja
Abstract: The present invention relates to a method for rescue of Vesicular Stomatitis Virus (VSV) from DNA in a HEK293 cell line or a HEK293 cell line adapted to suspension growth comprising (a) providing cells from a HEK293 cell line or a HEK293 cell line adapted to suspension growth in cell culture, (b) transfecting the cells with at least one plasmid, wherein the at least one plasmid comprises (i) an expression cassette comprising a VSV genomic cDNA; (ii) at least one expression cassette encoding VSV nucleoprotein (N) protein, VSV phosphoprotein (P) protein, and VSV large (L) protein; and (iii) an expression cassette encoding SV40 Large T antigen; (c) culturing the transfected cells; and (d) harvesting the cell culture supernatant comprising the rescued VSV.
Type:
Application
Filed:
July 8, 2022
Publication date:
June 15, 2023
Applicant:
Boehringer Ingelheim International GmbH
Abstract: The present invention relates to certain SGLT-2 inhibitors for treating, preventing, protecting against and/or delaying the progression of chronic kidney disease in patients, for example patients with prediabetes, type 1 or type 2 diabetes mellitus.
Type:
Grant
Filed:
November 10, 2020
Date of Patent:
June 6, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Uli Christian Broedl, Odd-Erik Johansen, Eric Williams Mayoux, Nima Soleymanlou, Maximilian von Eynatten, Hans-Juergen Woerle, David Z.I. Cherney, Bruce A. Perkins
Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing the same.
Type:
Grant
Filed:
October 13, 2021
Date of Patent:
May 30, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Florian Paul Christian Binder, Thomas Martin Fleck, Jens Willwacher
Abstract: Disclosed are antibodies and fragments thereof that target the A-domain of Neuropilin-1 (Nrp1A). Also disclosed are methods of using the anti-Nrp1A antibodies for the treatment of various diseases or disorders.
Type:
Grant
Filed:
September 24, 2020
Date of Patent:
May 30, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Nina Zippel, Pankaj Gupta, Fei Han, Sarah Low, Juergen Prestle, Leo Thomas
Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing the same.
Type:
Grant
Filed:
October 13, 2021
Date of Patent:
May 30, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Martin Thomas Fleck, Florian Paul Christian Binder, Jens Willwacher
Abstract: A nebulizer for a fluid, includes a container containing the fluid; a housing part which can be detached from the nebulizer for replacing the container; an inner part; a retaining element connected with and not detachable from the inner part, where the housing part is releasable fixed to the inner part by the retaining element; a delivery mechanism for dispensing the fluid; a manually depressible actuator member, which is a separate part from the retaining element and acts on the retaining element, and wherein the actuator member is depressed to elastically deform or flex the retaining element to allow detachment of the housing part.
Type:
Grant
Filed:
December 15, 2020
Date of Patent:
May 9, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Jens Besseler, Frank Herrmann, Holger Holakovsky, Herbert Argauer, Josef Gatz, Andreas Gorshoefer
Abstract: The present invention relates to the identification of a genomic integration site for heterologous polynucleotides in Chinese Hamster Ovary (CHO) cells resulting in high RNA and/or protein production. More specifically it relates to CHO cells comprising at least one heterologous polynucleotide stably integrated into the S100A gene cluster of the CHO genome and to methods for the production of said CHO cells. Further, the invention relates to a method for the production of a protein of interest using said CHO cell and to the use of said CHO cell for producing a protein of interest at high yield. Integration within these specific target regions leads to reliable, stable and high yielding production of an RNA and/or protein of interest, encoded by the heterologous polynucleotide.
Type:
Application
Filed:
December 6, 2022
Publication date:
April 27, 2023
Applicant:
Boehringer Ingelheim International GmbH
Inventors:
Markus Mueller, Jochen Schaub, Christian Bernloehr, Jennifer Koenitzer
Abstract: An injection device, in particular an auto-injector, with a single-use part for dispensing an injection solution has a sensor for acquiring a signal, with which an indicator can be determined, which represents a state or a change in state in a process for dispensing the injection solution with the single-use part. Additionally, the injection device has a reusable part, which is held in a detachable manner by coupling to the single-use part and is coupled via a signal connection, wherein the single-use part has the sensor, and/or wherein the reusable part has a reporting system for detecting the single-use part.
Type:
Application
Filed:
February 25, 2021
Publication date:
April 27, 2023
Applicant:
Boehringer Ingelheim International GmbH
Abstract: The invention relates to 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-heteroaryl pyrrolidine derivatives of general formula (I) for use as a medicament, pharmaceutical compositions comprising at least a compound of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.
Type:
Application
Filed:
September 9, 2022
Publication date:
April 27, 2023
Applicants:
Boehringer Ingelheim International GmbH, Arena Pharmaceuticals, Inc.
Inventors:
Kai Gerlach, Daniela Gavina Berta, Marco Ferrara, Kirsten Gutsche, Ursula Mueller-Vieira, Scott Hobson, Frank Runge, Graeme Semple, Viktor Vintonyak, Yifeng Xiong
Abstract: The present invention relates to new [1,3]diazino[5,4-d]pyrimidines and derivatives of Formula (I) wherein the groups R1, R2, R3 and R4 have the meanings given in the claims and specification, their use as inhibitors of HER2 and its mutants, pharmaceutical compositions which contain such compounds and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
Type:
Grant
Filed:
April 6, 2021
Date of Patent:
March 21, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Birgit Wilding, Dietrich Boese, Harald Engelhardt, Julian Fuchs, Ralph Neumueller, Mark Petronczki, Dirk Scharn, Matthias Treu
Abstract: Methods of protein production in continuous perfusion mammalian cell culture bioreactors are provided. Methods for continuous perfusion culture by allowing cells to self-regulate the rate of addition of perfusion medium to the bioreactor via a pH change are presented. Compositions comprising the perfusion medium as well as the process advantages of using hi-end pH control of perfusion or HIPCOP are also presented.
Type:
Grant
Filed:
May 27, 2016
Date of Patent:
March 7, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Gregory Walter Hiller, Matthew Paul Gagnon, Ana Maria Ovalle
Abstract: The present invention relates to compounds of general formula I, wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
Type:
Grant
Filed:
January 28, 2019
Date of Patent:
February 21, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Thomas Trieselmann, Cedrickx Godbout, Christoph Hoenke, Viktor Vintonyak
Abstract: This invention relates to thienopyrimidinones and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune diseases and CNS-related diseases.
Type:
Grant
Filed:
September 1, 2021
Date of Patent:
February 14, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Martin Thomas Fleck, Florian Paul Christian Binder, Georg Dahmann, Joerg P. Hehn, Annekatrin Charlotte Heimann, Uta Friederike Lessel, Jens Willwacher
Abstract: The invention describes anti-cancer therapies comprising using an LRP5 antagonist in combination with an anti-PD1 antibody, each as described herein.
Type:
Grant
Filed:
March 26, 2020
Date of Patent:
February 14, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Vittoria Zinzalla, Markus Johann Bauer, Barbara Drobits-Handl
Abstract: It is disclosed an improved multi-step process for the preparation of a highly concentrated liquid formulation containing biomolecules comprising the steps of (a) a first ultrafiltration UF1; (b) a first diafiltration DF1; (c) a second diafiltration DF2; and (d) a second ultrafiltration UF2; wherein an aqueous solution of one or more salts, as liquid medium B, is used for step (b) and water or an aqueous solution of one or more salts, as liquid medium C, is used for step (c), wherein the one or more salts used for step (b) are the same or different from the one or more salts used for step (c) and wherein the liquid medium B has an ionic strength which is higher than the ionic strength of the liquid medium C. The process according to the present invention allows the preparation of well-defined highly concentrated formulations containing biomolecules, particularly proteins, intended for pharmaceutical or non-pharmaceutical use.
Type:
Grant
Filed:
August 11, 2017
Date of Patent:
February 7, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Patrick Garidel, Sven Bahrenburg, Torsten Schultz-Fademrecht, Andrea Eiperle
Abstract: The present invention relates to anti-SIRP? (Signal regulatory protein alpha) antibodies and antigen-binding fragments thereof for therapeutic and diagnostic methods and compositions using them.
Type:
Grant
Filed:
June 2, 2022
Date of Patent:
February 7, 2023
Assignees:
Boehringer Ingelheim International GmbH, OSE Immmnotherapeatics SA
Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
Type:
Grant
Filed:
October 14, 2020
Date of Patent:
March 7, 2023
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Cédrickx Godbout, Thomas Trieselmann, Viktor Vintonyak