Patents by Inventor Niklas Heine

Niklas Heine has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 9079905
    Abstract: The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I). wherein A, R1-R5 and x are as defined herein, and their use as medicaments for improving perception, concentration, learning and/or memory in patients in need thereof.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: July 14, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Christian Eickmeier, Dennis Fiegen, Thomas Fox, Riccardo Giovannini, Niklas Heine, Martin Hendrix, Holger Rosenbrock, Gerhard Schaenzle
  • Patent number: 9018391
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: April 28, 2015
    Assignees: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Cornelia Dorner-Ciossek, Ulrike Gross, Niklas Heine, Achim Sauer
  • Patent number: 9006226
    Abstract: The present invention relates to dihydropteridinones, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: April 14, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Christian Eickmeier, Claudia Heine, Niklas Heine, Alexander Weber
  • Patent number: 8962641
    Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: February 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Annekatrin Heimann, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20150025088
    Abstract: The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). wherein R1 is a 5 or 6 membered aromatic heteroaryl-group, R2 is an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, m=1 or 2 and n is 0, 1 or 2. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Niklas HEINE, Christian EICKMEIER, Marco FERRERA, Riccardo GIOVANNINI, Holger ROSENBROCK, Gerhard SCHAENZLE
  • Patent number: 8912201
    Abstract: The invention relates to novel 6-cycloalkyl-pyrazolopyrimidinones according to formula (I) wherein R1, R2, D, m and n are as defined herein. The invention also relates to medicaments comprising these compounds and methods of using these compounds in the treatment of diseases and conditions, particularly diseases or conditions concerning deficits in perception, concentration, learning or memory.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: December 16, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Niklas Heine, Christian Eickmeier, Marco Ferrara, Riccardo Giovannini, Holger Rosenbrock, Gerhard Schaenzle
  • Publication number: 20140350025
    Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and R1 is the group V—W—*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.
    Type: Application
    Filed: November 22, 2013
    Publication date: November 27, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Cornelia DORNER-CIOSSEK, Christian EICKMEIER, Dennis FIEGEN, Thomas FOX, Klaus FUCHS, Niklas HEINE, Holger ROSENBROCK, Gerhard SCHAENZLE
  • Publication number: 20140343083
    Abstract: Pyrrolidine derivatives which are inhibitors of acetyl-CoA carboxylase(s) and their use in the treatment of obesity and type-2 diabetes. An exemplary compound is 2-(4-(1-[5-Chloro-6-(2-hydroxy-2-methyl-propoxy)-pyrimidin-4-yl]-(R)-pyrrolidin-3-yloxy)-phenyl)-N-cyclopropyl-propionamide.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Niklas HEINE, Martin FLECK, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8877741
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20140315882
    Abstract: The invention relates to new pyrrolidine derivatives of the formula wherein R1 to R3, Ar, L T and n are as defined in the description and claims, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: April 7, 2014
    Publication date: October 23, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Martin FLECK, Annekatrin HEIMANN, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Patent number: 8865716
    Abstract: The present invention relates to spiroheterocycl-dihydropyrimidines, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christian Eickmeier, Kai Gerlach, Niklas Heine, Alexander Weber, Ulrike Gross
  • Patent number: 8835472
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: September 16, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Niklas Heine, Joerg Kley, Thorsten Lehmann-Lintz, Heike Neubauer, Bernd Nosse
  • Patent number: 8809345
    Abstract: The invention relates to novel pyrazolopyrimidinones according to formula (I): wherein X, D, Ra, Rb, Rc, Rd, Re, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds and methods of using these compounds in the treatment of various diseases concerning deficits in perception, concentration, learning or memory.
    Type: Grant
    Filed: February 9, 2012
    Date of Patent: August 19, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Niklas Heine, Riccardo Giovannini
  • Publication number: 20140213568
    Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 31, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Publication number: 20140200223
    Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
    Type: Application
    Filed: December 18, 2013
    Publication date: July 17, 2014
    Inventors: Salvacion Cacatian, David A. Claremon, Lawrence Wayne Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian Mckeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
  • Publication number: 20140100211
    Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 10, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
  • Publication number: 20140073641
    Abstract: The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, wherein i.) the nitrogen atom of the pyrazolo-group that is next to the pyrimidino-group is attached to a non-aromatic, organic heterocycle having at least one ring hetero atom selected from O, N and S and ii.) to the C-atom between the two nitrogen atoms of the pyrimidinone-ring a second substituent is bound via an optionally substituted methylene-bridge. According to one aspect of the invention the new compounds are for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease.
    Type: Application
    Filed: November 12, 2013
    Publication date: March 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Cornelia DORNER-CIOSSEK, Christian EICKMEIER, Dennis FIEGEN, Thomas FOX, Klaus FUCHS, Niklas HEINE, Holger ROSENBROCK, Gerhard SCHAENZLE
  • Patent number: 8669271
    Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: March 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Matthias Eckhardt, Niklas Heine, Elke Langkopf, Bernd Nosse
  • Patent number: 8664388
    Abstract: The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Grant
    Filed: June 14, 2012
    Date of Patent: March 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Fuchs, Niklas Heine, Christian Eickmeier, Sandra Handschuh, Cornelia Dorner-Ciossek, Stefan Hoerer
  • Publication number: 20140057927
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Application
    Filed: August 27, 2013
    Publication date: February 27, 2014
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Cornelia Dorner-Ciossek, Ulrike Gross, Niklas Heine, Achim Sauer