Patents by Inventor Mirko Buchholz

Mirko Buchholz 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: 8227498
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: July 24, 2012
    Assignee: Probiodrug AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Torsten Hoffmann, Livia Boehme
  • Patent number: 8202897
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and R1, B and Y are as described throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: June 19, 2012
    Assignee: Probiodrug AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Antje Harmann
  • Patent number: 8188094
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined throughout the description and the claims.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: May 29, 2012
    Assignee: Probiodrug AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Robert Sommer
  • Patent number: 7897633
    Abstract: The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
    Type: Grant
    Filed: October 24, 2007
    Date of Patent: March 1, 2011
    Assignee: Probiodrug AG
    Inventors: Stephan Schilling, Mirko Buchholz, Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
  • Patent number: 7803810
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoisomers and polymorphs thereof wherein: R1 represents C2-8alkyl; C2-8alkenyl; —(C1-6alkyl)-aryl; —(C1-6alkyl)-heteroaryl; —(C1-6alkyl)-carbocyclyl; —(C1-6alkyl)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C1-4alkyl, C1-4-fluoroalkyl, C1-4alkoxy, C1-4-fluoroalkoxy, hydroxy, —SO2(C1-4alkyl), —SO2N(C1-4alkyl)(C1-4alkyl), —SOC1-4alkyl, —SOC3-6cycloalkyl —C(O)O(C1-4alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from —C1-4 alkyl, —C1-4 alkoxy, hydroxyl, halogen and oxo; R2 represents H; C1-4alkyl or halogen; R3 represents H; C1-4alkyl or halogen; and R4 represents H; C1-4alkyl or halogen.
    Type: Grant
    Filed: March 10, 2008
    Date of Patent: September 28, 2010
    Assignee: Probiodrug AG
    Inventors: Daniel Ramsbeck, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
  • Patent number: 7741354
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, —C(O)O-alkyl and —C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)O-alkyl and —C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R2 together with R4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: June 22, 2010
    Assignee: Probiodrug AG
    Inventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz
  • Patent number: 7732162
    Abstract: The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: June 8, 2010
    Assignee: Probiodrug AG
    Inventors: Torsten Hoffman, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
  • Publication number: 20100040575
    Abstract: Physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screening for such effectors, and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of conditions that can be treated by modulation of QC-activity. Preferred compositions additionally comprise inhibitors of DP IV or DP IV-like enzymes for the treatment or alleviation of conditions that can be treated by modulation of QC- and DP IV-activity.
    Type: Application
    Filed: July 21, 2009
    Publication date: February 18, 2010
    Applicant: PROBIODRUG AG
    Inventors: Torsten Hoffmann, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
  • Patent number: 7655684
    Abstract: Compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Corea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: February 2, 2010
    Assignee: Probiodrug AG
    Inventors: Stephan Schilling, Andre Johannes Niestroj, Ulrich Heiser, Hans-Ulrich Demuth, Mirko Buchholz
  • Publication number: 20090269301
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently repre
    Type: Application
    Filed: November 8, 2007
    Publication date: October 29, 2009
    Applicant: PROBIODRUG AG
    Inventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
  • Publication number: 20090018087
    Abstract: The present invention relates to novel inhibitors of glutaminyl cyclase and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's disease, Down Syndrome, Parkinson disease, Chorea Huntington, pathogenic psychotic conditions, schizophrenia, impaired food intake, sleep-wakefulness, impaired homeostatic regulation of energy metabolism, impaired autonomic function, impaired hormonal balance, impaired regulation, body fluids, hypertension, fever, sleep dysregulation, anorexia, anxiety related disorders including depression, seizures including epilepsy, drug withdrawal and alcoholism, neurodegenerative disorders including cognitive dysfunction and dementia.
    Type: Application
    Filed: October 24, 2007
    Publication date: January 15, 2009
    Applicant: PROBIODRUG AG
    Inventors: Stephan Schilling, Mirko Buchholz, Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
  • Publication number: 20080292582
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers, stereoisomers and polymorphs thereof, wherein A, B and R? are as defined throughout the description and the claims.
    Type: Application
    Filed: April 18, 2008
    Publication date: November 27, 2008
    Applicant: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Antje Hamann
  • Publication number: 20080286231
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Application
    Filed: April 18, 2008
    Publication date: November 20, 2008
    Applicant: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Andre J. Niestroj, Robert Sommer
  • Publication number: 20080267912
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Application
    Filed: April 18, 2008
    Publication date: October 30, 2008
    Applicant: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Torsten Hoffmann, Livia Boehme
  • Publication number: 20080267911
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: R1 represents and R2, R3, R4, R5, R6, X1, X2, X3, X4, Y and Z are as defined throughout the description and the claims.
    Type: Application
    Filed: April 18, 2008
    Publication date: October 30, 2008
    Applicant: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser
  • Publication number: 20080262065
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and R1, B and Y are as described throughout the description and the claims.
    Type: Application
    Filed: April 18, 2008
    Publication date: October 23, 2008
    Applicant: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Antje Harmann
  • Publication number: 20080260688
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined throughout the description and the claims.
    Type: Application
    Filed: April 18, 2008
    Publication date: October 23, 2008
    Applicant: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Robert Sommer
  • Publication number: 20080262063
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.
    Type: Application
    Filed: April 18, 2008
    Publication date: October 23, 2008
    Applicant: PROBIODRUG AG
    Inventors: Mirko Buchholz, Ulrich Heiser, Andre J. Niestroj
  • Publication number: 20080234313
    Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoisomers and polymorphs thereof wherein: R1 represents C2-8alkyl; C2-8alkenyl; —(C1-6alkyl)-aryl; —(C1-6alkyl)-heteroaryl; —(C1-6alkyl)-carbocyclyl; —(C1-6alkyl)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C1-4alkyl, C1-4-fluoroalkyl, C1-4alkoxy, C1-4-fluoroalkoxy, hydroxy, —SO2(C1-4alkyl), —SO2N(C1-4alkyl)(C1-4alkyl), —SOC1-4alkyl, —SOC3-6cycloalkyl —C(O)O(C1-4alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from —C1-4 alkyl, —C1-4 alkoxy, hydroxyl, halogen and oxo; R2 represents H; C1-4alkyl or halogen; R3 represents H; C1-4alkyl or halogen; and R4 represents H; C1-4alkyl or halogen.
    Type: Application
    Filed: March 10, 2008
    Publication date: September 25, 2008
    Applicant: PROBIODRUG AG
    Inventors: Daniel Ramsbeck, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
  • Publication number: 20080221086
    Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(he
    Type: Application
    Filed: November 8, 2007
    Publication date: September 11, 2008
    Applicant: PROBIODRUG AG
    Inventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj