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1. (WO2018219921) SUBSTITUTED PYRROLIDINYL AND PIPERIDINYL PYRAZOLOPYRIDAZINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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Pub. No.: WO/2018/219921 International Application No.: PCT/EP2018/064029
Publication Date: 06.12.2018 International Filing Date: 29.05.2018
IPC:
C07D 487/04 (2006.01) ,A61K 31/045 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
045
Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
Applicants:
ESTEVE PHARMACEUTICALS, S.A. [ES/ES]; Passeig de la Zona Franca, 109, 4ª Planta 08038 Barcelona, ES
Inventors:
ALMANSA-ROSALES, Carmen; ES
DÍAZ-FERNÁNDEZ, José-Luís; ES
FERNANDEZ-DONIS, Ariadna; ES
YENES-MINGUEZ, Susana; ES
Priority Data:
17382309.730.05.2017EP
Title (EN) SUBSTITUTED PYRROLIDINYL AND PIPERIDINYL PYRAZOLOPYRIDAZINE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN
(FR) DÉRIVÉS DE PYRROLIDINYLE ET DE PYRAZOLOPYRIDAZINE PIPÉRIDINYLE SUBSTITUÉS PRÉSENTANT UNE ACTIVITÉ MULTIMODALE CONTRE LA DOULEUR
Abstract:
(EN) The present invention relates to substituted pyrrolidinyl and piperidinyl pyrazolo[3,4-d]pyridazine derivatives having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the Noradrenaline transporter (NET), to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
(FR) La présente invention concerne des dérivés de pyrrolidinyle et de pyrazolo[3,4-d]pyridazine pipéridinyl substitués ayant une double activité pharmacologique à la fois envers la sous-unité α2δ, en particulier la sous-unité α2δ-1, du canal calcique sensible à la tension et du transporteur de noradrénaline (NET), l'invention concerne également des procédés de préparation de tels composés, des compositions pharmaceutiques les comprenant, ainsi que leur utilisation thérapeutique, en particulier pour traiter la douleur.
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: English (EN)
Filing Language: English (EN)