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91. 发明专利

SG11201506609VA NOVEL INHIBITORS 未知
公开(公告)号：SG11201506609VA
公开(公告)日：2015-09-29
申请号：SG11201506609V
申请日：2014-03-14
申请人： PROBIODRUG AG
发明人： HEISER ULRICH , BUCHHOLZ MIRKO , SOMMER ROBERT , DEMUTH HANS-ULRICH , MEYER ANTJE
IPC分类号： C07D413/04 , A61K31/437 , A61P25/00
摘要： The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R1, R2, R3, R4 and R5 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.

92. 发明专利

PL2328930T3 Przeciwciała skierowane przeciwko piroglutaminianowi białka chemotaktycznego monocytów typu 1 (MCP-1 N1pE) 未知
公开(公告)号：PL2328930T3
公开(公告)日：2015-05-29
申请号：PL09782017
申请日：2009-08-20
申请人： PROBIODRUG AG
发明人： CYNIS HOLGER , DEMUTH HANS-ULRICH , GANS KATHRIN , KAMPFER SONJA , RAHFELD JENS-ULRICH , SCHILLING STEPHAN
IPC分类号： C07K16/24 , A61K39/395

93. 发明专利

CY1110171T1 ΙΑΤΡΙΚΗ ΧΡΗΣΗ ΑΝΑΣΤΟΛΕΩΝ ΓΛΟΥΤΑΜΙΝΙΚΩΝ ΚΑΙ ΓΛΟΥΤΑΜΙΚΩΝ ΚΥΚΛΑΣΩΝ ΓΙΑ ΘΕΡΑΠΕΙΑ ΤΗΣ ΑΣΘΕΝΕΙΑΣ ΤΟΥ ALZHEIMER ΚΑΙ ΤΟΥ ΣΥΝΔΡΟΜΟΥ DOWN 未知
公开(公告)号：CY1110171T1
公开(公告)日：2015-01-14
申请号：CY101100612
申请日：2010-07-05
申请人： PROBIODRUG AG
发明人： DEMUTH HANS-ULRICH , HOFFMANN TORSTEN , NIESTROJ ANDRÉ J , SCHILLING STEPHAN , HEISER ULRICH
IPC分类号： A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4745 , A61P25/00 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： Ηπαρούσαεφεύρεσηπαρέχεινέαφυσιολογικάυποστρώματαγλουταμινικήςκυκλάσηςθηλαστικών (QC, EC 2.3.2.5), νέουςτελεστέςτης QC, μεθόδουςδιαλογήςτέτοιωντελεστών, καιτηχρήσητέτοιωντελεστώνκαιφαρμακευτικώνσυνθέσεωνπουπεριέχουντέτοιουςτελεστέςγιατηθεραπείακαταστάσεωνπουμπορούνναθεραπευτούνμερύθμισητηςδράσηςτης QC. Προτιμούμενεςσυνθέσειςπεριέχουνεπιπλέοναναστολείςτης DP IV ήενζύμωνπουομοιάζουνμε DP IV γιατηθεραπείαή τηβελτίωσηκαταστάσεωνπουμπορούνναδεχθούνθεραπείαμερύθμισητηςδράσηςτης QC καιτης DP IV.

94. 发明专利

DK2206496T3 Screening af inhibitorer af pyroglutaminsyredannelse i amyloid beta-peptid 未知
公开(公告)号：DK2206496T3
公开(公告)日：2014-12-15
申请号：DK10159763
申请日：2004-05-05
申请人： PROBIODRUG AG
发明人： DEMUTH HANS-ULRICH , HEISER ULRICH , HOFFMANN TORSTEN , NIESTROJ ANDRÉ J , SCHILLING STEPHAN
IPC分类号： C12Q1/00 , A61K31/00 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4745 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561

95. 发明专利

ES2481823T3 Inhibidores heterocíclicos de glutaminil ciclasa (QC, EC 2.3.2.5) 未知
公开(公告)号：ES2481823T3
公开(公告)日：2014-07-31
申请号：ES11707182
申请日：2011-03-10
申请人： PROBIODRUG AG
发明人： HEISER ULRICH , GAERTNER ULF-TORSTEN , DEMUTH HANS-ULRICH
IPC分类号： C07D403/04 , A61K31/4184 , A61K31/454 , A61K31/4709 , A61K31/5377 , A61P1/04 , A61P25/18 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , C07D401/04 , C07D403/10 , C07D403/14 , C07D405/10
摘要： Un compuesto de fórmula (I):**Fórmula** o una sal farmacéuticamente aceptable, solvato o polimorfo del mismo, incluidos todos los tautómeros y estereoisómeros del mismo, en la que: R1 representa -alquilo C1-6, -arilo, -alquil C1-6-arilo, -cicloalquilo, -alquil C1-6-cicloalquilo, -heteroarilo, -alquil C1-6- heteroarilo, -heterociclilo, -alquil C1-6-heterociclilo, -cicloalquilo sustituido con fenilo, -cicloalquilo sustituido con fenoxi, -fenilo sustituido con cicloalquilo, -fenilo sustituido con fenoxi, -fenilo sustituido con fenilo, heterociclilo sustituido con fenilo, heteroarilo sustituido con fenilo, fenilo sustituido con heterociclilo, fenilo sustituido con heteroarilo, fenilo sustituido con -O-cicloalquilo o fenilo sustituido con -cicloalquil-heterociclilo; y donde cualquiera de los grupos arilo, cicloalquilo, heterociclilo, heteroarilo, fenilo o fenoxi anteriormente citados puede estar opcionalmente sustituido con uno o más grupos seleccionados de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, -tioalquilo C1-6, -SO-alquilo C1-4, -SO2-alquilo C1-4, alcoxi C1-6-, -Ocicloalquilo C3-8, cicloalquilo C3-8, -SO2-cicloalquilo C3-8, -SO-cicloalquilo C3-6, alqueniloxi C3-6-, alquiniloxi C3-6-, -C(O)-alquilo C1-6, -C(O)O-alquilo C1-6, alcoxi C1-6-alquilo C1-6-, nitro, halógeno, ciano, hidroxilo, -C(O)OH, - NH2, -NH-alquilo C1-4, -N(alquil C1-4)(alquilo C1-4), -C(O)N(alquil C1-4)(alquilo C1-4), -C(O)NH2, -C(O)NH(alquilo C1-4) y -C(O)NH(cicloalquilo C3-10); R2 representa -alquilo C1-6, haloalquilo C1-6, -arilo, -alquil C1-6-arilo, -cicloalquilo, -alquil C1-6-cicloalquilo, -heteroarilo, - alquil C1-6-heteroarilo, -heterociclilo o -alquil C1-6-heterociclilo; y donde cualquiera de los grupos arilo, heteroarilo o heterociclilo anteriormente citados puede estar opcionalmente sustituido con uno o más grupos seleccionados de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, -tioalquilo C1-6, -SO-alquilo C1-4, -SO2-alquilo C1-4, alcoxi C1-6-, -O-cicloalquilo C3-8, cicloalquilo C3-8, -SO2-cicloalquilo C3-8, -SO-cicloalquilo C3-6, alqueniloxi C3-6-, alquiniloxi C3-6-, -C(O)alquilo C1-6, -C(O)Oalquilo C1-6, alcoxi C1-6-alquilo C1-6-, nitro, halógeno, ciano, hidroxilo, -C(O)OH, -NH2, -NH-alquilo C1-4, - N(alquilo C1-4)(alquilo C1-4), -C(O)N(alquilo C1-4)(alquilo C1-4), -C(O)NH2, -C(O)NH(alquilo C1-4) y - C(O)NH(cicloalquilo C3-10); R3 representa alquilo C1-6 o haloalquilo C1-6; n representa 0; y Ra representa alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, -tioalquilo C1-6, -SO-alquilo C1-4, -SO2-alquilo C1-4, alcoxi C1-6-, -O-cicloalquilo C3-8, cicloalquilo C3-8, -SO2-cicloalquilo C3-8, -SO-cicloalquilo C3-6, alqueniloxi C3-6-, alquiniloxi C3-6-, -C(O)alquilo C1-6, -C(O)O-alquilo C1-6, alcoxi C1-6-alquilo C1-6-, nitro, halógeno, ciano, hidroxilo, - C(O)OH, -NH2, -NH-alquilo C1-4, -N(alquilo C1-4)(alquilo C1-4), -C(O)N(alquilo C1-4)(alquilo C1-4), -C(O)NH2, - C(O)NH(alquilo C1-4) y -C(O)NH(cicloalquilo C3-10).

96. 发明专利

CA2524009C USE OF EFFECTORS OF GLUTAMINYL AND GLUTAMATE CYCLASES 未知
公开(公告)号：CA2524009C
公开(公告)日：2014-04-29
申请号：CA2524009
申请日：2004-05-05
申请人： PROBIODRUG AG
发明人： DEMUTH HANS-ULRICH , HOFFMANN TORSTEN , NIESTROJ ANDRE J , SCHILLING STEPHAN , HEISER ULRICH
IPC分类号： C12Q1/48 , A61K31/00 , A61K31/395 , A61K31/4164 , A61K31/417 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4192 , A61K31/4745 , C07D231/12 , C07D233/54 , C07D403/06 , C07D405/06 , C07D409/06 , C07D471/04 , C07F9/572 , C07F9/59 , C07F9/6506 , C07F9/6561
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC, methods for screeing 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.

97. 发明专利

SG194770A1 RADIOLABELLED GLUTAMINYL CYCLASE INHIBITORS 未知
公开(公告)号：SG194770A1
公开(公告)日：2013-12-30
申请号：SG2013081567
申请日：2012-05-24
申请人： PROBIODRUG AG
发明人： HEISER ULRICH , RAMSBECK DANIEL , DEMUTH HANS-ULRICH
摘要： The invention relates to the use of radiolabelled glutaminyl cyclase (QC) inhibitors as imaging agents, in particular but not exclusively as medical imaging agents for the detection of neurological disorders. The invention also relates to pharmaceutical compositions comprising said radiolabelled inhibitors and to methods and kits for detecting neurological disorders.

98. 发明专利

MX2013010571A ENSAYO DE DIAGNOSTICO DE ANTICUERPO. 未知
公开(公告)号：MX2013010571A
公开(公告)日：2013-12-02
申请号：MX2013010571
申请日：2012-03-16
申请人： PROBIODRUG AG
发明人： KLEINSCHMIDT MARTIN , SCHILLING STEPHAN , RAHFELD JENS-ULRICH , DEMUTH HANS-ULRICH , EBERMANN KRISTIN
IPC分类号： C07K16/18 , G01N33/68
摘要： La presente invención pertenece a ensayos de diagnóstico novedosos para el diagnóstico de amiloidosis, en particular enfermedad de Alzheimer, y aspectos relacionados. En particular, se proporcionan anticuerpos monoclonales y un ensayo de anticuerpo.

99. 发明专利

BRPI0718507A2 未知
公开(公告)号：BRPI0718507A2
公开(公告)日：2013-11-12
申请号：BRPI0718507
申请日：2007-09-21
申请人： PROBIODRUG AG
发明人： SCHILLING STEPHAN , CYNIS HOLGER , RAHFELD JENS-ULRICH , DEMUTH HANS-ULRICH
IPC分类号： C12N15/54 , A61K31/4164 , C07D233/54 , C07D235/06 , C07D403/12 , C07D405/12 , C07D417/12 , C12N9/10
摘要： The present invention relates to novel glutaminyl-peptide cyclotransferase-like proteins (QPCTLs), which are isoenzymes of glutaminyl cyclase (QC, EC 2.3.2.5), and to isolated nucleic acids coding for these isoenzymes, all of which are useful for the discovery of new therapeutic agents, for measuring cyclase activity, and for determining the inhibitory activity of compounds against these glutaminyl cyclase isoenzymes.

100. 发明专利

CA2542419C USE OF GLUTAMYL CYCLASE INHIBITORS IN THE TREATMENT OF FAMILIAL BRITISH DEMENTIA AND FAMILIAL DANISH DEMENTIA 未知
公开(公告)号：CA2542419C
公开(公告)日：2013-06-04
申请号：CA2542419
申请日：2004-10-15
申请人： PROBIODRUG AG
发明人： SCHILLING STEPHAN , HOFFMANN TORSTEN , NIESTROJ ANDRE JOHANNES , DEMUTH HANS-ULRICH , HEISER ULRICH
IPC分类号： A61K31/00 , A61K31/13 , A61K31/4178 , A61K31/4184 , A61P25/28 , A61P35/00
摘要： The present invention provides novel physiological substrates of mammalian glutaminyl cyclase (QC, EC 2.3.2.5), new effectors of QC and the use of such effectors and pharmaceutical compositions comprising such effectors for the treatment of diseases that can be treated by modulation of QC-activity, e.g. diseases selected from the group consisting of duodenal cancer with or w/o Helicobacter pylori infections, colorectal cancer, Zolliger-Ellison syndrome, Familial British Dementia and Familial Danish Dementia. (see formula 1)

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