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1. (WO2015121212) NEW COMPOUNDS HAVING A SELECTIVE PDE4D INHIBITING ACTIVITY
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2015/121212    International Application No.:    PCT/EP2015/052683
Publication Date: 20.08.2015 International Filing Date: 10.02.2015
IPC:
C07D 231/12 (2006.01), C07D 401/06 (2006.01), C07D 403/06 (2006.01), C07D 413/06 (2006.01), C07D 261/04 (2006.01), C07D 261/08 (2006.01), A61K 31/5377 (2006.01), A61K 31/454 (2006.01), A61K 31/42 (2006.01), A61K 31/422 (2006.01), A61K 31/496 (2006.01), A61P 25/28 (2006.01)
Applicants: UNIVERSITÀ DEGLI STUDI DI GENOVA [IT/IT]; Via Balbi, 5 I-16126 Genova (IT).
THE TRUSTEES OF COLUMBIA UNIVERSITY [US/US]; 412 Low Memorial Library 535 West 116th Street New York, New York 10027 (US).
MAASTRICHT UNIVERSITY [NL/NL]; Minderbroedersberg 4-6 NL-6211 LK Maastricht (NL)
Inventors: BRUNO, Olga; (IT).
BRULLO, Chiara; (IT).
ROMUSSI, Alessia; (IT).
FEDELE, Ernesto; (IT).
RICCIARELLI, Roberta; (IT).
ARANCIO, Ottavio; (US).
PRICKAERTS, Jos; (NL)
Agent: FERRECCIO, Rinaldo; (IT)
Priority Data:
14425015.6 14.02.2014 EP
Title (EN) NEW COMPOUNDS HAVING A SELECTIVE PDE4D INHIBITING ACTIVITY
(FR) NOUVEAUX COMPOSÉS PRÉSENTANT UNE ACTIVITÉ D'INHIBITION SÉLECTIVE VIS-À-VIS DE PDE4D
Abstract: front page image
(EN)Compounds of formula (I), wherein Z = cyclopentyl. cyclopropylmethyl, -CH3; R' = -CH3, CHF2, X= formula (II) (III) (IV) (V) Y = - CO; -C=O(CH2), -CH(OH)-CH2, -CH2-C=O, -CH2-CH2-C=O; -CH2-CH(OH)-CH2, -CH2- CH(OCOR1)-CH2 NR2 = -N(CH2-CH2OH)2, formula (VI) (VII) (VIII) (IX) (X) (XI) R1 = optionally substituted C1-C8 alkyl, optionally substituted aryl; optionally substituted aralkyl, preferably C1-C3 alkyl, more preferably CH3; and enantiomers, diastereoisomers and pharmaceutically acceptable salts thereof; these compounds have a PDE4D inhibiting activity and can be used as a medicament for treating dementia, in particular Alzheimer disease, and for improving memory.
(FR)La présente invention concerne des composés de formule (I), dans laquelle Z = cyclopentyle. cyclopropylméthyle, -CH3; R' = -CH3, CHF2, X= formule (II) (III) (IV) (V) Y = -CO; -C=O(CH2), -CH(OH)-CH2, -CH2-C=O, -CH2-CH2-C=O; -CH2-CH(OH)-CH2, -CH2-CH(OCOR1)-CH2 NR2 = -N(CH2-CH2OH)2, formule (VI) (VII) (VIII) (IX) (X) (XI) R1 = groupe alkyle en C1-C8 éventuellement substitué, groupe aryle éventuellement substitué; groupe aralkyle éventuellement substitué, de préférence groupe alkyle en C1-C3, plus préférablement groupe CH3; et leurs énantiomères, diastéréoisomères et sels pharmaceutiquement acceptables; ces composés ont une activité d'inhibition de la PDE4D et peuvent être utilisés comme médicament pour traiter la démence, notamment la maladie d'Alzheimer, et pour améliorer la mémoire.
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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)