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1. (WO2019023815) NEW COMPOUNDS DERIVED FROM PYRIDINE METHYL SULFINYL BENZOXAZOLES AND PYRIDINE METHYL SULFINYL BENZOTHIAZOLES, TAGGED RADIOACTIVELY OR FLUORESCENTLY, AND COMPOSITIONS THEREOF AS SPECIFIC BIOMARKERS FOR THE DIAGNOSIS OF NEURODEGENERATIVE DISEASES AND PATHOLOGIES INVOLVING TAU PROTEIN
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Pub. No.: WO/2019/023815 International Application No.: PCT/CL2018/050059
Publication Date: 07.02.2019 International Filing Date: 30.07.2018
IPC:
C07D 413/12 (2006.01) ,C07D 417/12 (2006.01) ,A61K 31/4439 (2006.01) ,A61K 49/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4427
containing further heterocyclic ring systems
4439
containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49
Preparations for testing in vivo
Applicants:
SERVICIOS CIENTÍFICOS NEUROINNOVATION LIMITADA [CL/CL]; Av. Vitacura 3568, oficina 513, Vitacura Santiago, CL
Inventors:
MACCIONI BARAHONA, Ricardo; CL
ROJO CASTILLO, Leonel; CL
QUIÑONES SEPÚLVEDA, Luis; CL
Agent:
COVARRUBIAS & COMPAÑIA SPA; Enrique Foster Sur 39, Piso 9, Las Condes. Santiago, CL
Priority Data:
1982-201703.08.2017CL
Title (EN) NEW COMPOUNDS DERIVED FROM PYRIDINE METHYL SULFINYL BENZOXAZOLES AND PYRIDINE METHYL SULFINYL BENZOTHIAZOLES, TAGGED RADIOACTIVELY OR FLUORESCENTLY, AND COMPOSITIONS THEREOF AS SPECIFIC BIOMARKERS FOR THE DIAGNOSIS OF NEURODEGENERATIVE DISEASES AND PATHOLOGIES INVOLVING TAU PROTEIN
(FR) NOUVEAUX COMPOSÉS DÉRIVÉS DE PYRIDINMÉTHYLSULFINYLBENZOXAZOLES ET DE PYRIDINMÉTHYLSULFINYLBENZOTHIAZOLES MARQUÉS RADIOACTIVEMENT OU PAR FLUORESCENCE ET LEURS COMPOSITIONS, UTILISÉS COMME BIOMARQUEURS SPÉCIFIQUES POUR LE DIAGNOSTIC DE MALADIES DÉGÉNÉRATIVES ET DE PATHOLOGIES ASSOCIÉES À LA PROTÉINE TAU
(ES) NUEVOS COMPUESTOS DERIVADOS DE PIRIDINMETILSULFINILBENZOXAZOLES Y PIRIDINMETILSULFINIBENZOTIAZOLES, MARCADOS RADIACTIVAMENTE O CON FLUORESCENCIA Y SUS COMPOSICIONES, COMO BIOMARCADORES ESPECIFICOS PARA EL DIAGNOSTICO DE ENFERMEDADES NEURODEGENERATIVAS Y PATOLOGÍAS INVOLUCRADAS CON LA PROTEÍNA TAU
Abstract:
(EN) The present invention relates to pyridine methyl sulfinyl benzoxazole compounds and pyridine methyl sulfinyl benzothiazole compounds, tagged radioactively or fluorescently, and compositions thereof, as specific biomarkers for the diagnosis of neurodegenerative diseases and pathologies involving tau protein, such as Alzheimer’s and other dementias. According to the present invention, the techniques in which the described molecules can be used include: computerised axial tomography (CAT); nuclear magnetic resonance (NMR), both structural NMR (sNMR) and functional NMR (fNMR); single-photon emission computed tomography (SPECT); and positron-emission tomography (PET). Thus, the invention provides a pharmacologically safe tool with high affinity and selectivity for protein structures of tau protein, which allows an application, method or use of said agents to be established for the identification and diagnosis of neurodegenerative diseases, tau pathologies, preferably Alzheimer’s disease.
(FR) La présente invention concerne des composés pyridinméthalsulfinylbenzoxazoles et pyridinméthylsulfinylbenzothiazoles marqués radioactivement ou par fluorescence et leurs compositions, utilisés comme biomarqueurs spécifiques pour le diagnostic de maladies neurodégénératives et de pathologies associées à la protéine tau, telles que la maladie d’Alzheimer et d'autres démences. Selon la présente invention, les techniques permettant d’utiliser les molécules décrites peuvent être : la tomodensitométrie (TDM), la résonance magnétique nucléaire (RMN), tant structurale (RMNs) que fonctionnelle (RMNf), la tomographie d’émission monophotonique (TEMP) et la tomographie par émission de positons (TEP). Ainsi, l'invention offre une solution pharmacologiquement sûre caractérisée par une affinité et une sélectivité élevées pour les structures protéiques de la protéine tau, ce qui permet d'établir une application, une méthode ou l'utilisation desdits agents pour l'identification et le diagnostic de maladies neurodégénératives et de pathologies associées à tau, de préférence la maladie d'Alzheimer.
(ES) La presente invención corresponde a compuestos piridinmetilsulfinilbenzoxazoles y piridinmetilsulfinilbenzotiazoles, marcados 5 radiactivamente o con fluorescencia y sus composiciones, como biornarcadores especificos para el diagnóstico de enfermedades neurodegenerativas y patológicas involucradas con Ia proteína tau tales como AIzheimer y otras demencias. Conforme a Ia presente invención las técnicas donde se pueden emplear las moléculas descritas pueden ser: Tomografia Axial Computarizada 0 (CAT), resonancia magnetica nuclear (NMR), tanto estructural (sNMR) como funcional NMR (fNMR), tomografia computarizada de emisión de fotón único (SPECT) y Ia tomografia de emisión de positrones (PET). De esta forma Ia invención proporciona una herrarnienta farmacolóqicamente segura, con una elevada afinidad y selectividad por estructuras proteicas de proteína tau, lo cual 5 permite establecer una aplicación, método o uso de dichos agentes pare la identificación y diagnóstico de enfermedades neurodegenerativas, tau patologias, de preferencia enfermedad de Alzheirner.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Spanish (ES)
Filing Language: Spanish (ES)