Patents by Inventor André J. Niestroj
André J. Niestroj 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: 9656991Abstract: 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: May 23, 2017Assignee: PROBIODRUG AGInventors: Mirko Buchholz, Ulrich Heiser, André J. Niestroj, Robert Sommer
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Patent number: 9512082Abstract: 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: December 6, 2016Assignee: PROBIODRUG AGInventors: Mirko Buchholz, Ulrich Heiser, André J. Niestroj
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Patent number: 9126987Abstract: 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; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.Type: GrantFiled: November 28, 2007Date of Patent: September 8, 2015Assignee: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Mirko Buchholz, Andre J. Niestroj
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Patent number: 8809010Abstract: Provided herein are methods for treating and preventing neurodegenerative disease in a mammal by administering an inhibitor of glutaminyl cyclase (QC). Neurodegenerative diseases treatable or preventable according to methods described herein include mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia.Type: GrantFiled: July 21, 2009Date of Patent: August 19, 2014Assignee: Probiodrug AGInventors: Torsten Hoffmann, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
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Patent number: 8420684Abstract: 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(heType: GrantFiled: November 8, 2007Date of Patent: April 16, 2013Assignee: Probiodrug AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Patent number: 8278345Abstract: 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 repreType: GrantFiled: November 8, 2007Date of Patent: October 2, 2012Assignee: Probiodrug AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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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: 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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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: 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
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Publication number: 20100040575Abstract: 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: ApplicationFiled: July 21, 2009Publication date: February 18, 2010Applicant: PROBIODRUG AGInventors: Torsten Hoffmann, Stephan Schilling, Andre J. Niestroj, Hans-Ulrich Demuth, Ulrich Heiser, Mirko Buchholz
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Patent number: 7625939Abstract: The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.Type: GrantFiled: May 14, 2008Date of Patent: December 1, 2009Assignee: Probiodrug AGInventors: Ulrich Heiser, Andre J. Niestroj, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20090269301Abstract: 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 repreType: ApplicationFiled: November 8, 2007Publication date: October 29, 2009Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20080293618Abstract: The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases.Type: ApplicationFiled: May 14, 2008Publication date: November 27, 2008Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ulf-Torsten Gaertner, Hans-Ulrich Demuth
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Publication number: 20080286231Abstract: 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: ApplicationFiled: April 18, 2008Publication date: November 20, 2008Applicant: PROBIODRUG AGInventors: Mirko Buchholz, Ulrich Heiser, Andre J. Niestroj, Robert Sommer
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Publication number: 20080262063Abstract: 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: ApplicationFiled: April 18, 2008Publication date: October 23, 2008Applicant: PROBIODRUG AGInventors: Mirko Buchholz, Ulrich Heiser, Andre J. Niestroj
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Publication number: 20080234313Abstract: 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: ApplicationFiled: March 10, 2008Publication date: September 25, 2008Applicant: PROBIODRUG AGInventors: Daniel Ramsbeck, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20080221086Abstract: 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(heType: ApplicationFiled: November 8, 2007Publication date: September 11, 2008Applicant: PROBIODRUG AGInventors: Michael Thormann, Michael Altmstetter, Andreas Treml, Ulrich Heiser, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20080214620Abstract: 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; carbocyclyl which may optionally be substituted by alkyl; alkenyl; alkynyl, provided a triple bond is not adjacent to X; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl in which heterocyclyl may optionally be substituted by alkyl; -alkyl-carbocyclyl in which carbocyclyl may optionally be substituted by alkyl; aryl; heteroaryl; or H; X represents S or NR3; R3 represents H or C1-4 alkyl.Type: ApplicationFiled: November 28, 2007Publication date: September 4, 2008Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Daniel Ramsbeck, Mirko Buchholz, Andre J. Niestroj
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Publication number: 20080153892Abstract: 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 dementiaType: ApplicationFiled: March 12, 2008Publication date: June 26, 2008Applicant: Probiodrug AGInventors: Stephan Schilling, Andre J. Niestroj, Ulrich Heiser, Mirko Buchholz, Hans-Ulrich Demuth