Patents by Inventor Ulrich Heiser
Ulrich Heiser 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).
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Patent number: 8269019Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: GrantFiled: March 10, 2011Date of Patent: September 18, 2012Assignee: Probiodrug AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Patent number: 8227498Abstract: 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: GrantFiled: April 18, 2008Date of Patent: July 24, 2012Assignee: Probiodrug AGInventors: Mirko Buchholz, Ulrich Heiser, Torsten Hoffmann, Livia Boehme
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Patent number: 8202897Abstract: 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: GrantFiled: April 18, 2008Date of Patent: June 19, 2012Assignee: Probiodrug AGInventors: Mirko Buchholz, Ulrich Heiser, Antje Harmann
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Patent number: 8188094Abstract: 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: GrantFiled: April 18, 2008Date of Patent: May 29, 2012Assignee: Probiodrug AGInventors: Mirko Buchholz, Ulrich Heiser, Robert Sommer
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Publication number: 20110262388Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
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Publication number: 20110224259Abstract: The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: March 3, 2011Publication date: September 15, 2011Applicant: PROBIODRUG AGInventors: Ulrich HEISER, Daniel RAMSBECK, Torsten HOFFMANN, Livia BOEHME, Hans-Ulrich DEMUTH
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Publication number: 20110224254Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20110224225Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: ApplicationFiled: March 10, 2011Publication date: September 15, 2011Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Publication number: 20110092501Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: September 13, 2010Publication date: April 21, 2011Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
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Patent number: 7897633Abstract: 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: GrantFiled: October 24, 2007Date of Patent: March 1, 2011Assignee: Probiodrug AGInventors: Stephan Schilling, Mirko Buchholz, Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
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Publication number: 20100273835Abstract: The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.Type: ApplicationFiled: July 10, 2008Publication date: October 28, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ingo Schulz
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Patent number: 7816325Abstract: The present application relates to the secondary binding site of dipeptidyl peptidase IV, its relationship amongst substrates and to the modulation of substrate specificity of dipeptidyl peptidase IV (DP IV, synonym: DPP IV, CD26, EC 3.4.14.5). The application relates further to compounds that bind to the secondary binding site of DP IV and their use to modulate the substrate specificity of DP IV; methods of treatment of various DP IV mediated disorders; and screening methods for the identification of secondary binding sites on DP IV and DP IV-like enzymes.Type: GrantFiled: June 29, 2006Date of Patent: October 19, 2010Assignee: OSI Pharmaceuticals, Inc.Inventors: Kerstin Kühn-Wache, Joachim Bär, Hans-Ulrich Demuth, Torsten Hoffmann, Ulrich Heiser, Wolfgang Brandt
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Publication number: 20100249149Abstract: are useful as inhibitors of cyclin dependent kinases such as CDK9.Type: ApplicationFiled: October 13, 2008Publication date: September 30, 2010Inventors: Hans Allgeier, Martin Augustin, Anke Müller, Luz Zeitlmann, Andreas Marquardt, Michael A. Pleiss, Ulrich Heiser, André Johannes Niestroj
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Patent number: 7803810Abstract: 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: GrantFiled: March 10, 2008Date of Patent: September 28, 2010Assignee: Probiodrug AGInventors: Daniel Ramsbeck, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20100159032Abstract: The present invention provides a method for the treatment of neuronal disorders, in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of at least one QC-inhibitor, optionally in combination with at least one agent, selected from the group consisting of PEP-inhibitors, LiCl, inhibitors of DP IV/DP IV-like enzymes, NPY-receptor ligands, NPY agonists, NPY antagonists, ACE-inhibitors, PIMT enhancers, inhibitors of beta secretases, inhibitors of gamma secretases and inhibitors of neutral endopeptidase, to a mammal in need thereof.Type: ApplicationFiled: December 3, 2009Publication date: June 24, 2010Applicant: PROBIODRUG AGInventors: Ingo Schulz, Stephan Schilling, Hans-Ulrich Demuth, Ulrich Heiser, Andre Johannes Niestroj, Steffen Rossner
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Patent number: 7741354Abstract: 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, hydroxylType: GrantFiled: November 8, 2007Date of Patent: June 22, 2010Assignee: Probiodrug AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz
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Patent number: 7732162Abstract: 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: GrantFiled: March 14, 2007Date of Patent: June 8, 2010Assignee: Probiodrug AGInventors: Torsten Hoffman, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
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Publication number: 20100125086Abstract: The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.Type: ApplicationFiled: September 4, 2009Publication date: May 20, 2010Applicant: PROBIODRUG AGInventors: Hans-Ulrich Demuth, Stephan Schilling, Michael Wermann, Holger Cynis, Astrid Kehlen, Daniel Friedrich, Torsten Hoffmann, Kathrin Gans, Jens-Ulrich Rahfeld, Ulrich Heiser, Michael Almstetter, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Thormann, Andreas Tremel
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Publication number: 20100119475Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.Type: ApplicationFiled: September 4, 2009Publication date: May 13, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Almstetter, Michael Thormann, Andreas Treml, Hans-Ulrich Demuth, Torsten Hoffman
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Publication number: 20100099721Abstract: Inhibitors of prolyl endopeptidase of formula 1 W—KCONH—X—CON—Y—CO—Z??(1) wherein K, W, X, Y and Z are specified in the description. The compounds are useful for the treatment of diseases such as mild cognitive impairment (MCI), Alzheimer's disease, Down Syndrome, Parkinson disease and Chorea Huntington.Type: ApplicationFiled: December 23, 2009Publication date: April 22, 2010Applicant: PROBIODRUG AGInventors: André J. Niestroj, Ulrich Heiser, Ingo Schulz, Jens-Ulrich Rahfeld, Joachim Baer, Hans-Ulrich Demuth