Abstract: The invention relates to aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amide derivatives of general formula (1), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates processes for manufacture of the compounds according to the invention.
Type:
Grant
Filed:
November 12, 2015
Date of Patent:
January 22, 2019
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Rocco Mazzaferro, Marco Ferrara, Riccardo Giovannini, Iain Lingard
Abstract: Antibody molecules, in particular fully human antibodies that bind to human IGF-1 and cross-react with IGF-2 such that binding of IGF-1 and IGF-2 to the IGF-1 receptor is prevented and IGF-1 receptor-mediated signaling is inhibited. The antibodies do not bind to insulin and thus do not affect the mitogenic properties of insulin that are mediated by its binding to the insulin receptors. The antibodies are useful for the treatment of hyperproliferative diseases, in particular cancer.
Type:
Grant
Filed:
June 13, 2014
Date of Patent:
January 15, 2019
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Paul Adam, Eric Borges, Robert Rauchenberger, Gabriela Wochnik-Veltrup
Abstract: The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification: The invention also relates to methods of using compounds of Formula I, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.
Type:
Grant
Filed:
October 5, 2017
Date of Patent:
December 25, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Mandar Deodhar, Alison Dorothy Findlay, Jonathan Stuart Foot, Wolfgang Jarolimek, Ian Alexander Mcdonald, Alan Duncan Robertson, Craig Ivan Turner
Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
Type:
Grant
Filed:
December 29, 2015
Date of Patent:
December 18, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
John Edward Park, Gerald Juergen Roth, Armin Heckel, Nveed Chaudhary, Trixi Brandl, Georg Dahmann, Matthias Grauert
Abstract: An inhaler is proposed having an insertable container and a monitoring device for counting uses of the inhaler. The monitoring device is arranged in a detachable housing part or fitted onto a mouthpiece of the inhaler. A supply air current is detected by means of a pressure sensor. A position sensor may further be provided.
Abstract: The invention relates to new substituted heteroaryls of formula 1 or of formula 1? wherein A is either N or CH, wherein R2 is selected from the group consisting of —C1-3-alkyl, —C1-3-haloalkyl, F, Br, Cl, wherein Y is selected from —O— or —CH2—, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
Type:
Grant
Filed:
November 10, 2017
Date of Patent:
December 18, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Hoffmann, Georg Dahmann, Christian Gnamm, Daniel Robert Fandrick, John Scott, Clive McCarthy
Abstract: The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R1, R2, R3, R4, X, and Z? have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).
Abstract: The invention relates to a process for inactivating proteases by repeatedly changing the pH in the cell culture supernatant at the start of the process for the purification of biopharmaceuticals. The pH is adjusted first to 3-5, and then to 7-9.
Type:
Application
Filed:
August 9, 2018
Publication date:
December 6, 2018
Applicant:
Boehringer Ingelheim International GmbH
Inventors:
Alexander JACOBI, Dorothee AMBROSIUS, Philine DOBBERTHIEN, Christian ECKERMANN, Franz NOTHELFER
Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, R7, A, D, E, F, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.
Type:
Grant
Filed:
October 7, 2016
Date of Patent:
December 4, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Andreas Gollner, Joachim Broeker, Nina Kerres, Christiane Kofink, Juergen Ramharter, Harald Weinstabl
Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
September 6, 2017
Date of Patent:
November 27, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Pingrong Liu, Craig Andrew Miller, Maolin Yu, Zhonghua Zhang, Sabine Ruppel, Anil K. Padyana
Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
Type:
Grant
Filed:
November 16, 2017
Date of Patent:
November 27, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Joerg Bentzien, Angela Kay Berry, Todd Bosanac, Michael Jason Burke, Darren Todd Disalvo, Joshua Courtney Horan, Shuang Liang, Can Mao, Wang Mao, Yue Shen, Fariba Soleymanzadeh, Renee M. Zindell
Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1—, R2—, X, Y, and HET are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
September 6, 2017
Date of Patent:
November 27, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Jianwen Cui, Donghong Amy Gao, Pingrong Liu, Bryan Patrick McKibben, Craig Andrew Miller, Hossein Razavi, Elizabeth Spencer, Sabine Ruppel, Anil K. Padyana
Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R7, V, W, X, Y, n and q are defined herein, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases and synthetic intermediates.
Type:
Grant
Filed:
April 10, 2015
Date of Patent:
November 27, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Andreas Gollner, Christiane Kofink, Juergen Ramharter, Harald Weinstabl, Tobias Wunberg
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
January 28, 2016
Date of Patent:
November 20, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Michael Balestra, Jörg M. Bentzien, Jennifer Burke, Derek Cogan, Xin Guo, Keith R. Hornberger, John Lord, Kenneth M. Meyers, Zhaoming Xiong, Maolin Yu, Zhonghua Zhang
Abstract: This invention relates to methods for the synthesis of spiro[2.5]octane-5,7-dione and spiro[3.5]nonane-6,8-dione which are useful as intermediates in the manufacture of pharmaceutically active ingredients.
Type:
Grant
Filed:
February 26, 2018
Date of Patent:
November 20, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Xiangle Jin, Weitong Dong, Yan Fu, Jun Lu, Le Xie, Wei Xu, Jinsong Yang, Qian Zhu
Abstract: A nebulizer includes an insertable container and a securing mechanism for holding the container in the nebulizer such that the container can move back and forth but cannot be separated. The securing mechanism is formed by a metal unitary part. The securing mechanism forms a transportation lock for holding the container unmovable in the housing in a delivery state of the nebulizer. The securing mechanism forms a cage which encompasses the container.
Type:
Grant
Filed:
January 7, 2015
Date of Patent:
November 13, 2018
Assignee:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Alexander Bach, Jens Besseler, Holger Holakovsky, Manuel Daelman, Gilbert Wuttke
Abstract: The present invention relates to compounds of general formula I, wherein the groups R, R1, R2, R3, m and n are as defined herein, which compounds have valuable pharmacological properties, in particular their ability to bind to the GPR40 receptor 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 type 2 diabetes. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
Type:
Grant
Filed:
November 21, 2017
Date of Patent:
November 13, 2018
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Eckhardt, Holger Wagner, Stefan Peters