(WO/2003/080076) NOVEL THERAPEUTIC USE OF RIBOSIDE OF 5-AMINOIMIDAZOLE-4- CARBOXAMIDE (ACADESINE)

(WO/2003/080076) NOVEL THERAPEUTIC USE OF RIBOSIDE OF 5-AMINOIMIDAZOLE-4- CARBOXAMIDE (ACADESINE)

Latest bibliographic data on file with the International Bureau
Pub. No.:  WO/2003/080076   International Application No.:  PCT/ES2003/000130
Publication Date:02.10.2003 International Filing Date:20.03.2003
IPC: A61K 31/7056 (2006.01)
Applicants:ADVANCED IN VITRO CELL TECHNOLOGIES, S.L. [ES/ES]; Baldiri i Reixach 10-12, 08028 Barcelona (ES) (All Except US).
LÓPEZ BLANCO, José Manuel [ES/ES]; (ES) (US Only).
CAMPÁS MOYA, Clara [ES/ES]; (ES) (US Only).
GIL SANTANO, Juan [ES/ES]; (ES) (US Only).
Inventors:LÓPEZ BLANCO, José Manuel; (ES).
CAMPÁS MOYA, Clara; (ES).
GIL SANTANO, Juan; (ES).
Agent:PORTELA, Sergio; ABG Patentes, S.L., Orense 16, 28020 Madrid (ES).
Priority Data:
P200200760 21.03.2002 ES
Title:

(EN) NOVEL THERAPEUTIC USE OF RIBOSIDE OF 5-AMINOIMIDAZOLE-4- CARBOXAMIDE (ACADESINE)

(ES) NUEVO USO TERAPÉUTICO DEL RIBÓSIDO DE 5-AMINOIMIDAZOL-4-CARBOXAMIDA (ACADESINA)

Abstract:

(EN) The invention relates to a novel therapeutic use of riboside of 5-aminoimidazole-4-carboxamide (acadesine). Acadesine (also known as AICA riboside or AICAR) does not inhibit apoptosis in lymphocytes, as would be expected, but it does induce apoptosis in the B-cells of patients with B-type lymphoproliferative diseases, such as chronic B-cell (B-CLL) lymphatic leukaemia, splenic marginal zone lymphoma (SMZL), mantle cell lymphoma (MCL), follicular lymphoma (FL), lymphoplasmacytic lymphoma (LPL) and Waldenstrom's syndrome (WS). The T-cells are not affected. As a result, acadesine and the bioprecursors thereof (e.g. the mono, di- and tri-5'-phosphates thereof) are converted into therapeutic agents that can be used against lymphoproliferative diseases in humans. The surprising characteristic whereby the T-cells are barely affected means that the adverse secondary effect (immunosuppression) is slight, which represents a therapeutic advantage offered by acadesine over cladribine, fludarabine and other nucleosides known in the art.

(ES) La acadesina (también conocida como AICA ribósido o AICAR) no inhibe la apoptosis en linfocitos, como se podría esperar, pero induce apoptosis en las células B de pacientes con enfermedades linfoproliferativas de tipo B, tales como la leucemia linfática crónica de células B (B-CLL), el linfoma esplénico de zona marginal (SMZL), el linfoma de células del manto (MCL), el linfoma folicular (FL), el linfoma linfoplasmacítico (LPL), y el síndrome de Waldenstrom (WS). Las células T no se ven afectadas. Esto convierte a la acadesina y a sus bioprecursores (p.ej. sus mono-, di- y tri-5'-fosfatos) en agentes terapéuticos útiles contra las enfermedades linfoproliferativas en humanos. La característica sorprendente de que las células T apenas se afectan significa que el efecto secundario adverso (inmunosupresión) es pequeño, lo que representa una ventaja terapéutica de la acadesina sobre la cladribina, la fludarabina y otros nucleósidos conocidos en la técnica.

Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NI, NO, NZ, OM, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Org. (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (EAPO) (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC, NL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (OAPI) (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language:Spanish (ES)
Filing Language:Spanish (ES)

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