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1. (WO2018100048) 2-PHENYL-2H-PYRAZOLO[3,4-D]PYRIDAZINE DERIVATIVES HAVING ACTIVITY AGAINST PAIN
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Pub. No.: WO/2018/100048 International Application No.: PCT/EP2017/080948
Publication Date: 07.06.2018 International Filing Date: 30.11.2017
IPC:
C07D 487/04 (2006.01) ,A61K 31/5025 (2006.01) ,A61P 29/00 (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
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
50
Pyridazines; Hydrogenated pyridazines
5025
ortho- or peri-condensed with heterocyclic ring systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29
Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
Applicants:
ESTEVE PHARMACEUTICALS, S.A. [ES/ES]; Passeig de la Zona Franca, 109, 4ª Planta 08038 Barcelona, ES
Inventors:
CUEVAS-CORDOBES, Felix; ES
ALMANSA-ROSALES, Carmen; ES
Agent:
CARPINTERO LOPEZ, Francisco; ES
Priority Data:
16382576.330.11.2016EP
Title (EN) 2-PHENYL-2H-PYRAZOLO[3,4-D]PYRIDAZINE DERIVATIVES HAVING ACTIVITY AGAINST PAIN
(FR) DÉRIVÉS DE 2-PHÉNYL -2 H-PYRAZOLO [3,4-D] PYRIDAZINE AYANT UNE ACTIVITÉ CONTRE LA DOULEUR
Abstract:
(EN) The present invention relates to 2-phenyl-2H-pyrazolo[3,4-d]pyridazine derivatives of formula (In) having pharmacological activity towards the α2δ subunit, in particular the a28-1 subunit, of the voltage-gated calcium channel, in particular having dual pharmacological activity towards both the a28 subunit, in particular the a28-1 subunit, of the voltage-gated calcium channel and the p-opioid receptor. The present invention also relates 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 2-phényl-2H-pyrazolo[3,4-d]pyridazine de formule (In) ayant une activité pharmacologique envers la sous-unité α2δ, en particulier la sous-unité a28-1, du canal calcique dépendant de la tension, en particulier ayant une double activité pharmacologique envers à la fois, la sous-unité a28, en particulier la sous-unité a28-1, du canal calcique dépendant de la tension et le récepteur p-opioïde. La présente invention concerne également des procédés de préparation de ces composés, des compositions pharmaceutiques les comprenant, ainsi que leur utilisation thérapeutique, en particulier pour le traitement de la douleur.
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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)