| EP2838888 - THIADIAZOLIDINEDIONES AS GSK-3 INHIBITORS [Right-click to bookmark this link] | Status | No opposition filed within time limit Status updated on 16.02.2018 Database last updated on 11.04.2026 | |
| Former | The patent has been granted Status updated on 10.03.2017 | ||
| Former | Grant of patent is intended Status updated on 06.11.2016 | Most recent event Tooltip | 28.09.2018 | Lapse of the patent in a contracting state New state(s): MC | published on 31.10.2018 [2018/44] | Applicant(s) | For all designated states ASD Therapeutics Partners LLC 5 Rose Court Warren, NJ 07059 / US | [2015/09] | Inventor(s) | 01 /
MEDINA PADILLA, Miguel C/ La Baneza, 42 C, 6° D E-28035 Madrid / ES | 02 /
DOMÍNGUEZ CORREA, Juan Manuel C/ Arturo Soria, 333 - 10 F E-28033 Madrid / ES | 03 /
DE CRISTOBAL BLANCO, Javier C/ Doctor Gómez Ulla, 20 - 4° B E-28028 Madrid / ES | 04 /
FUERTES HUERTA, Ana C/ Alenza, 9 - 5° D E-28003 Madrid / ES | 05 /
SÁNCHEZ-QUESADA, Jorge C/ Vital Aza, 96 - 2° B E-28017 Madrid / ES | 06 /
LÓPEZ OGALLA, Javier C/ Isabel Colbrand 16, Portal H, 2°, 2 E-28050 Madrid / ES | 07 /
HERRERO SANTOS, Susana C/ San José, 9 Esc. Izq. - 2° C E-28921 Alcorcón - Madrid / ES | 08 /
PÉREZ DE LA CRUZ MORENO, María Ángeles Ctra. del Plantío, 100 - 2° B E-28221 Majadahonda - Madrid / ES | 09 /
MARTÍNEZ MONTERO, Olga Av. de los Artesanos, 64 - 2, 7° 3 E-28760 Tres Cantos -Madrid / ES | 10 /
RODRÍGUEZ SALGUERO, Beatriz Av. Oliva, 67 - 3° B E-28222 Majadahonda - Madrid / ES | 11 /
PALOMO NICOLAU, Francisco C/ Félix Yuste, 22 E-28804 Alcalá de Henares / ES | [2015/35] |
| Former [2015/09] | 01 /
MEDINA PADILLA, Miguel Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | ||
| 02 /
DOMÍNGUEZ CORREA, Juan Manuel Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 03 /
DE CRISTOBAL BLANCO, Javier Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 04 /
FUERTES HUERTA, Ana Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 05 /
SÁNCHEZ-QUESADA, Jorge Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 06 /
LÓPEZ OGALLA, Javier Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 07 /
HERRERO SANTOS, Susana Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 08 /
PÉREZ DE LA CRUZ MORENO, María Ángeles Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 09 /
MARTÍNEZ MONTERO, Olga Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos -Madrid / ES | |||
| 10 /
RODRÍGUEZ SALGUERO, Beatriz Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | |||
| 11 /
PALOMO NICOLAU, Francisco Noscira S.A. Avda. de la Industria 52 E-28760 Tres Cantos - Madrid / ES | Representative(s) | ABG Intellectual Property Law, S.L. Avenida de Burgos, 16D Edificio Euromor 28036 Madrid / ES | [N/P] |
| Former [2015/09] | ABG Patentes, S.L. Avenida de Burgos, 16D Edificio Euromor 28036 Madrid / ES | Application number, filing date | 13705492.0 | 22.02.2013 | [2017/15] | WO2013EP53554 | Priority number, date | EP20120382066 | 24.02.2012 Original published format: EP 12382066 | [2015/09] | Filing language | EN | Procedural language | EN | Publication | Type: | A1 Application with search report | No.: | WO2013124413 | Date: | 29.08.2013 | Language: | EN | [2013/35] | Type: | A1 Application with search report | No.: | EP2838888 | Date: | 25.02.2015 | Language: | EN | The application published by WIPO in one of the EPO official languages on 29.08.2013 takes the place of the publication of the European patent application. | [2015/09] | Type: | B1 Patent specification | No.: | EP2838888 | Date: | 12.04.2017 | Language: | EN | [2017/15] | Search report(s) | International search report - published on: | EP | 29.08.2013 | Classification | IPC: | C07D285/08, C07D417/06, A61K31/433, A61P25/28, A61P3/10 | [2015/09] | CPC: |
C07D285/08 (EP,US);
A61P11/00 (EP);
A61P19/10 (EP);
A61P25/00 (EP);
A61P25/02 (EP);
A61P25/28 (EP);
A61P27/06 (EP);
A61P29/00 (EP);
A61P3/00 (EP);
A61P3/10 (EP);
A61P31/12 (EP);
A61P37/02 (EP);
| Designated contracting states | AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LI, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR [2015/09] | Extension states | BA | 22.09.2014 | ME | 22.09.2014 | Title | German: | THIADIAZOLIDINDIONE ALS GSK-3-INHIBITOREN | [2016/17] | English: | THIADIAZOLIDINEDIONES AS GSK-3 INHIBITORS | [2015/09] | French: | THIADIAZOLIDINEDIONES EN TANT QU'INHIBITEURS DE GSK-3 | [2016/17] |
| Former [2015/09] | THIADIAZOLIDINDIONE ALS GSK-3-HEMMER | ||
| Former [2015/09] | THIADIAZOLIDINEDIONES SOUS FORME D'INHIBITEURS DE GSK-3 | Entry into regional phase | 22.09.2014 | National basic fee paid | 22.09.2014 | Designation fee(s) paid | 22.09.2014 | Examination fee paid | Examination procedure | 23.12.2013 | Request for preliminary examination filed International Preliminary Examining Authority: EP | 22.09.2014 | Amendment by applicant (claims and/or description) | 22.09.2014 | Examination requested [2015/09] | 23.09.2015 | Despatch of a communication from the examining division (Time limit: M04) | 09.12.2015 | Reply to a communication from the examining division | 22.01.2016 | Despatch of a communication from the examining division (Time limit: M02) | 09.03.2016 | Reply to a communication from the examining division | 02.05.2016 | Despatch of a communication from the examining division (Time limit: M04) | 02.09.2016 | Reply to a communication from the examining division | 30.09.2016 | Despatch of a communication from the examining division (Time limit: M01) | 19.10.2016 | Reply to a communication from the examining division | 07.11.2016 | Communication of intention to grant the patent | 06.03.2017 | Fee for grant paid | 06.03.2017 | Fee for publishing/printing paid | 06.03.2017 | Receipt of the translation of the claim(s) | Divisional application(s) | The date of the Examining Division's first communication in respect of the earliest application for which a communication has been issued is 23.09.2015 | Opposition(s) | 15.01.2018 | No opposition filed within time limit [2018/12] | Fees paid | Renewal fee | 22.01.2015 | Renewal fee patent year 03 | 18.01.2016 | Renewal fee patent year 04 | 16.01.2017 | Renewal fee patent year 05 |
| Opt-out from the exclusive Tooltip competence of the Unified Patent Court | See the Register of the Unified Patent Court for opt-out data | ||
| Responsibility for the accuracy, completeness or quality of the data displayed under the link provided lies entirely with the Unified Patent Court. | Lapses during opposition Tooltip | MC | 12.04.2017 | RS | 12.04.2017 | SM | 12.04.2017 | IS | 12.08.2017 | [2018/44] |
| Former [2018/13] | RS | 12.04.2017 | |
| SM | 12.04.2017 | ||
| IS | 12.08.2017 | ||
| Former [2017/51] | RS | 12.04.2017 | |
| IS | 12.08.2017 | Cited in | International search | [XI] NASIM S ET AL: "N-Chlorosuccinimide is a convenient oxidant for the synthesis of 2,4-disubstituted 1,2,4-thiadiazolidine-3,5-diones", TETRAHEDRON LETTERS, ELSEVIER, AMSTERDAM, NL, vol. 50, no. 3, 21 January 2009 (2009-01-21), pages 257 - 259, XP025875880, ISSN: 0040-4039, [retrieved on 20081105], DOI: 10.1016/J.TETLET.2008.10.136 DOI: http://dx.doi.org/10.1016/j.tetlet.2008.10.136 | [XI] MARTINEZ A ET AL: "First Non-ATP Competitive Glycogen Synthase Kinase 3.beta. (GSK-3.beta.) Inhibitors: Thiadiazolidinones (TDZD) as Potential Drugs for the Treatment of Alzheimer's Disease", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 45, no. 6, 1 January 2002 (2002-01-01), pages 1292 - 1299, XP002292084, ISSN: 0022-2623, DOI: 10.1021/JM011020U DOI: http://dx.doi.org/10.1021/jm011020u | [XI] EMMA M. TURNER ET AL: "Small Molecule Inhibitors of Regulators of G Protein Signaling (RGS) Proteins", ACS MEDICINAL CHEMISTRY LETTERS, vol. 3, no. 2, 9 February 2012 (2012-02-09), pages 146 - 150, XP055026893, ISSN: 1948-5875, DOI: 10.1021/ml200263y DOI: http://dx.doi.org/10.1021/ml200263y | by applicant | CHEMISTRY & BIOLOGY, vol. 7, no. 10, 2000, pages 793 - 803 | COGHLAN ET AL., CURR. OPINION GENETICS DEV., vol. 10, no. 5, 2000, pages 508 - 514 | AVILA, J.: "Role of tau protein in both physiological and pathological conditions.", PHYSIOL. REV., vol. 84, 2004, pages 361 - 84 | CIRC RES., vol. 104, no. 11, 2009, pages 1240 - 52 | JUHASZOVA M.; MIURA T.; MIKI T. ET AL.: "Role of glycogen synthase kinase-3beta in cardioprotection", GSK-3BETA, A THERAPEUTIC TARGET FOR CARDIOMYOCYTE PROTECTION, vol. 73, no. 7, 2009, pages 1184 - 92 | ELDAR-FINKELMAN, H.: "Glycogen synthase kinase 3: an emerging therapeutic target", TRENDS. MOL. MED., vol. 8, 2002, pages 126 - 32, XP002243394, DOI: doi:10.1016/S1471-4914(01)02266-3 DOI: http://dx.doi.org/10.1016/S1471-4914(01)02266-3 | ASENJO, A.: "Residues in human respiratory syncytial virus P protein that are essential for its activity on RNA viral synthesis", VIRUS RES., vol. 132, 2008, pages 160 - 73, XP022482225 | HERNNDEZ F: "The role of GSK3 in Alzheimer disease", BRAIN RES BULL., vol. 80, no. 4-5, 2009, pages 248 - 50, XP026662850, DOI: doi:10.1016/j.brainresbull.2009.05.017 DOI: http://dx.doi.org/10.1016/j.brainresbull.2009.05.017 | FORLENZA O. V: "Increased platelet GSK3B activity in patients with mild cognitive impairment and Alzheimer's disease", J PSYCHIATR RES., vol. 45, no. 2, 2011, pages 220 - 4, XP027579428 | MASAHIRO N.; HIDEAKI H.: "Glycogen synthase kinase-3beta is associated with Parkinson's disease", NEUROSCIENCE LETTERS, vol. 449, no. 2, 2009, pages 103 - 107, XP025742553, DOI: doi:10.1016/j.neulet.2008.10.104 DOI: http://dx.doi.org/10.1016/j.neulet.2008.10.104 | SCHAFFER, B.: "Association of GSK3B with Alzheimer disease and frontotemporal dementia.", ARCH. NEUROL., vol. 65, 2008, pages 1368 - 74 | HANGER D.P.; NOBLE W.: "Functional implications of glycogen synthase kinase-3-mediated tau phosphorylation", INT J ALZHEIMERS DIS., vol. 2011, 2011, pages 352805 | BUEE, L.: "Tau protein isoforms, phosphorylation and role in neurodegenerative disorders", BRAIN RESEARCH REVIEWS, vol. 33, 2000, pages 95 - 130 | DEWHURST S.: "Glycogen synthase kinase 3 beta (GSK-3 beta) as a therapeutic target in neuroAIDS", J NEUROIMMUNE PHARMACOL., vol. 2, no. 1, 2007, pages 93 - 96, XP019486384 DOI: http://dx.doi.org/10.1007/s11481-006-9051-1 | CARMICHAEL: "Glycogen synthase kinase-3beta inhibitors prevent cellular polyglutamine toxicity caused by the Huntington's disease mutation", J BIOL CHEM., vol. 277, no. 37, 2002, pages 33791 - 8, XP008113076, DOI: doi:10.1074/jbc.M204891200 DOI: http://dx.doi.org/10.1074/jbc.M204891200 | TANJI K.: "Glycogen synthase kinase-3beta phosphorylates synphilin-I in vitro", NEUROPATHOLOGY, vol. 23, no. 3, 2003, pages 199 - 202 | ROEW MK.: "GSK-3 is a viable potential target for therapeutic intervention in bipolar disorder", NEUROSCI BIOBEHAV REV., vol. 31, no. 6, 2007, pages 920 - 931 | LI X: "Glycogen Synthase Kinase-3?, mood stabilizers, and neuroprotection", BIPOLAR DISORD., vol. 4, no. 2, 2002, pages 137 - 144 | WADA A.: "Lithium and neuropsychiatric therapeutics: neuroplasticity via glycogen synthase kinase-3beta, beta-catenin, and neurotrophin cascades", J PHARMACOL SCI., vol. 110, no. 1, 2009, pages 14 - 28 | "The role of glycogen synthase kinase-3beta in schizophrenia", DRUG NEWS PERSPECT., vol. 20, no. 7, 2007, pages 437 - 45 | KOROS E.; DORNER-CIOSSEK C.; LOVESTONE S.: "Schizophrenia as a GSK-3 dysregulation disorder", TRENDS NEUROSCI., vol. 30, no. 4, 2007, pages 142 - 9, XP022003424, DOI: doi:10.1016/j.tins.2007.02.002 DOI: http://dx.doi.org/10.1016/j.tins.2007.02.002 | CHEN G.: "The mood-stabilizing agent valproate inhibits the activity of glycogen synthase kinase-3", J NEUROCHEM., vol. 72, no. 3, 1999, pages 1327 - 30 | JOPE R.S.; ROH M.S.: "Glycogen synthase kinase-3 (GSK3) in psychiatric diseases and therapeutic interventions", CURR DRUG TARGETS., vol. 7, no. 11, 2006, pages 1421 - 34 | BEAULIEU J.M.: "Role of GSK3 beta in behavioral abnormalities induced by serotonin deficiency", PROC NATL ACAD SCI U S A., vol. 105, no. 4, 2008, pages 1333 - 8 | BEAULIEU J.M.: "Lithium antagonizes dopamine-dependent behaviors mediated by an AKT/glycogen synthase kinase 3 signaling cascade", PROC NATL ACAD SCI U S A., vol. 101, no. 14, 2004, pages 5099 - 104 | LIU F.: "Overexpression of DyrklA contributes to neurofibrillary degeneration in Down syndrome", FASEB J., vol. 22, no. 9, 2008, pages 3224 - 33 | YUSKAITIS C.J.: "Lithium ameliorates altered glycogen synthase kinase-3 and behavior in a mouse model of fragile X syndrome", BIOCHEM PHARMACOL., vol. 79, no. 4, 2010, pages 632 - 46, XP002642831, DOI: doi:10.1016/J.BCP.2009.09.023 DOI: http://dx.doi.org/10.1016/J.BCP.2009.09.023 | DUGO L.: "Glycogen synthase kinase 3beta as a target for the therapy of shock and inflammation", SHOCK., vol. 27, no. 2, 2007, pages 113 - 23 | SASAKI C.: "Different expression of glycogen synthase kinase-3beta between young and old rat brains after transient middle cerebral artery occlusion.", NEUROL RES., vol. 23, no. 6, 2001, pages 588 - 92 | BEUREL E.: "Innate and adaptive immune responses regulated by glycogen synthase kinase-3 (GSK3", TRENDS IMMUNOL., vol. 31, no. 1, 2010, pages 24 - 31, XP026826336 | DE SARNO P.: "Lithium prevents and ameliorates experimental autoimmune encephalomyelitis", J IMMUNOL., vol. 181, no. 1, 2008, pages 338 - 45, XP002742397, DOI: doi:10.4049/jimmunol.181.1.338 DOI: http://dx.doi.org/10.4049/âjimmunol.181.1.338 | WATASE K.: "Lithium therapy improves neurological function and hippocampal dendritic arborization in a spinocerebellar ataxia type I mouse model", PLOS MED, vol. 4, no. 5, 2007, pages 836 - 847 | HAN F.: "Accumulation of beta- amyloid in the brain microvessels accompanies increased hyperphosphorylated tau proteins following microsphere embolism in aged rats", NEUROSCIENCE., vol. 153, no. 2, 2008, pages 414 - 27, XP022639006, DOI: doi:10.1016/j.neuroscience.2008.02.044 DOI: http://dx.doi.org/10.1016/j.neuroscience.2008.02.044 | YANG W.: "Upregulation of GSK3? expression in frontal and temporal cortex in ALS with cognitive impairment (ALSci", BRAIN RES., vol. 1196, 2008, pages 131 - 139, XP022482962, DOI: doi:10.1016/j.brainres.2007.12.031 DOI: http://dx.doi.org/10.1016/j.brainres.2007.12.031 | PREZ M.: "Prion peptide induces neuronal cell death through a pathway involving glycogen synthase kinase 3", BIOCHEM J., vol. 372, 15 December 2002 (2002-12-15), pages 129 - 36, XP009103717, DOI: doi:10.1042/BJ20021596 DOI: http://dx.doi.org/10.1042/BJ20021596 | WANG G.R.: "Changes of tau profiles in brains of the hamsters infected with scrapie strains 263 K or 139 A possibly associated with the alteration of phosphate kinases", BMC INFECT DIS., vol. 1, no. 10, 2010, pages 86 | YUAN Y: "Overexpressed alpha-synuclein regulated the nuclear factor-kappaB signal pathway", CELL MOL NEUROBIOL., vol. 28, no. 1, 2008, pages 21 - 33, XP019570977 | JIN J.: "GSK3beta-cyclin D3-CUGBPI-eIF2 pathway in aging and in myotonic dystrophy", CELL CYCLE., vol. 8, no. 15, 2009, pages 2356 - 9 | DILL, J.: "Inactivation of glycogen synthase kinase 3 promotes axonal growth and recovery in the CNS", J NEUROSCI., vol. 28, 2008, pages 8914 - 28 | COHEN P.: "The role ofprotein phosphorylation in human health and disease.", EUR J BIOCHEM., vol. 268, no. 19, 2001, pages 5001 - 10 | CUZZOCREA, S.: "Glycogen synthase kinase-3b inhibition attenuates the degree of arthritis caused by type II collagen in the mouse", CLIN. IMMUNOL., vol. 120, 2006, pages 57 - 67, XP024911179, DOI: doi:10.1016/j.clim.2006.03.005 DOI: http://dx.doi.org/10.1016/j.clim.2006.03.005 | HU, X: "IFN-g suppresses IL-10 production and synergizes with TLR2 by regulating GSK3 and CREB/AP-1 proteins", IMMUNITY, vol. 24, 2006, pages 563 - 574, XP002672717, DOI: doi:10.1016/j.immuni.2006.02.014 DOI: http://dx.doi.org/10.1016/j.immuni.2006.02.014 | DUGO, L.: "GSK-3b inhibitors attenuate the organ injury/dysfunction caused by endotoxemia in the rat", CRIT. CARE MED., vol. 33, 2005, pages 1903 - 1912 | BENTLEY J.K.: "Airway smooth muscle hyperplasia and hypertrophy correlate with glycogen synthase kinase-3(beta) phosphorylation in a mouse model of asthma", AM J PHYSIOL LUNG CELL MOL PHYSIOL., vol. 296, no. 2, 2009, pages L176 - 84 | EVENSON, A.R.: "GSK-3b inhibitors reduce protein degradation in muscles from septic rats and in dexamethasone treated myotubes. Int", J BIOCHEM. CELL. BIOL., vol. 37, 2005, pages 2226 - 2238 | WHITTLE, B.J.: "Reduction of experimental colitis in the rat by inhibitors of glycogen synthase kinase-3b", BR. J. PHARMACOL., vol. 147, 2006, pages 575 - 582 | DUGO, L.: "Glycogen synthase kinase-3b inhibitors protect against the organ injury and dysfunction caused by hemorrhage and resuscitation", SHOCK, vol. 25, 2006, pages 485 - 491 | GONG R.: "Glycogen synthase kinase 3beta: a novel marker and modulator of inflammatory injury in chronic renal allograft disease", AM J TRANSPLANT., vol. 8, no. 9, 2008, pages 1852 - 63 | LENZ, S.P.: "Lithium chloride enhances survival of NZB/W lupus mice: influence of melatonin and timing of treatment", INT. J. IMMUNOPHARMACOL., vol. 17, 1995, pages 581 - 592 | HARDT, SE.; SADOSHIMA, J.: "Glycogen synthase kinase-3beta: a novel regulator of cardiac hypertrophy and development", CIRC. RES., vol. 90, 2002, pages 1055 - 63, XP002340821, DOI: doi:10.1161/01.RES.0000018952.70505.F1 DOI: http://dx.doi.org/10.1161/01.RES.0000018952.70505.F1 | BOWES A.J: "Valproate attenuates accelerated atherosclerosis in hyperglycemic apoE-deficient mice: evidence in support of a role for endoplasmic reticulum stress and glycogen synthase kinase-3 in lesion development and hepatic steatosis", AM J PATHOL., vol. 174, no. 1, 2009, pages 330 - 42 | BADORFF C.: "Fas receptor signaling inhibits glycogen synthase kinase 3? and induces cardiac hypertrophy following pressure overload", J CLIN. INVEST., vol. 109, no. 3, 2002, pages 373 - 381 | MA X: "Epub. Delayed Re-endothelialization with Rapamycin-coated Stents is Rescued by the Addition of a Glycogen Synthase Kinase 3 Beta Inhibitor", CARDIOVASC RES., 2010 | GALLICCHIO, V. S.: "Lithium and the Cell", 1991, ACADEMIC, pages: 185 - 198 | WAGMAN A.S.: "Discovery and development of GSK3 inhibitors for the treatment of type 2 diabetes", CURR PHARM DES., vol. 10, no. 10, 2004, pages 1105 - 37, XP009058198, DOI: doi:10.2174/1381612043452668 DOI: http://dx.doi.org/10.2174/1381612043452668 | LYUBIMOVA A.: "Neural Wiskott-Aldrich syndrome protein modulates Wnt signaling and is required for hair follicle cycling in mice", J CLIN INVEST., vol. 120, no. 2, 2010, pages 446 - 56, XP002633044, DOI: doi:10.1172/JCI36478 DOI: http://dx.doi.org/10.1172/JCI36478 | WU C.H.: "Glycogen synthase kinase-3 regulates the phosphorylation of severe acute respiratory syndrome coronavirus nucleocapsid protein and viral replication", JBIOL CHEM., vol. 284, no. 8, 2009, pages 5229 - 39 | XU C.M.: "Glycogen synthase kinase 3beta in the nucleus accumbens core mediates cocaine-induced behavioral sensitization", J NEUROCHEM., vol. 111, no. 6, 2009, pages 1357 - 68 | WANG F.S.: "Inhibition of glycogen synthase kinase- 3beta attenuates glucocorticoid-induced bone loss", LIFE SCI., vol. 85, no. 19-20, 2009, pages 685 - 92, XP026720544, DOI: doi:10.1016/j.lfs.2009.09.009 DOI: http://dx.doi.org/10.1016/j.lfs.2009.09.009 | WANG W.H.: "Increased expression of the WNT antagonist sFRP-1 in glaucoma elevates intraocular pressure", J CLIN INVEST., vol. 118, no. 3, 2008, pages 1056 - 64, XP008153320, DOI: doi:10.1172/JCI33871 DOI: http://dx.doi.org/10.1172/JCI33871 | COHEN, P.; GOEDERT, M: "GSK3 inhibitors: development end therapeutic potential", NATURE REVIEWS, vol. 3, 2004, pages 479 - 487 | HERNNDEZ, F.: "GSK3 Inhibitors and Disease", MINI-REVIEWS IN MEDICINAL CHEMISTRY, vol. 9, no. 9, 2009, pages 1024 - 1029 | MEDINA, M.; CASTRO, A.: "Glycogen synthase kinase-3 (GSK-3) inhibitors reach the clinic", CURR. OPIN. DRUG DISCOV. DEVELOP., vol. 11, no. 4, 2008, pages 533 - 543 | "Glycogen Synthase Kinase 3 (GSK-3) and its inhibitors", 2006, JOHN WILEY & SONS, INC. | LECLERC, S.: "Indirubins inhibit glycogen synthase kinase-3 beta and CDK5lp25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors?", J BIOL. CHEM., vol. 276, 2001, pages 251 - 60 | SMITH, D.: "3-Anilino- 4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3", BIOORG. MED. CHEM. LETT., vol. 11, 2001, pages 635 - 9, XP004230079, DOI: doi:10.1016/S0960-894X(00)00721-6 DOI: http://dx.doi.org/10.1016/S0960-894X(00)00721-6 | WITHERINGTON, J.: "5-arylpyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3", BIOORG. MED. CHEM. LETT., vol. 13, 2003, pages 1581 - 4, XP002298542, DOI: doi:10.1016/S0960-894X(03)00135-5 DOI: http://dx.doi.org/10.1016/S0960-894X(03)00135-5 | LEOST, M.: "Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25", EUR. J. BIOCHEM., vol. 267, 2000, pages 5983 - 94, XP002384290, DOI: doi:10.1046/j.1432-1327.2000.01673.x DOI: http://dx.doi.org/10.1046/j.1432-1327.2000.01673.x | BHAT, R.: "Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418", J BIOL. CHEM., vol. 278, 2003, pages 45937 - 45, XP002999443, DOI: doi:10.1074/jbc.M306268200 DOI: http://dx.doi.org/10.1074/jbc.M306268200 | MARTINEZ, A.: "First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease", J MED. CHEM., vol. 45, 2002, pages 1292 - 9, XP002292084, DOI: doi:10.1021/jm011020u DOI: http://dx.doi.org/10.1021/jm011020u | J. 5 MED. CHEM., vol. 45, 2002, pages 1292 - 1299 | MARTINEZ, A. ET AL., BIOORG. MED. CHEM., vol. 5, 1997, pages 1275 - 1283 | KROGSGAARD-LARSEN; TAYLOR; FRANCIS ET AL.: "Textbook of Drug design and Discovery", April 2002 | "Stedman's Medical Spellchecker, ", 2006, LIPPINCOTT WILLIAMS & WILKINS |