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1. (WO2009139886) TARGETING AN HIV-1 NEF-HOST CELL KINASE COMPLEX
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/139886    International Application No.:    PCT/US2009/002996
Publication Date: 19.11.2009 International Filing Date: 14.05.2009
IPC:
C07D 241/44 (2006.01), C07D 241/40 (2006.01), A61K 31/498 (2006.01), A61P 31/18 (2006.01)
Applicants: UNIVERSITY OF PITTSBURGH-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION [US/US]; 200 Gardner Steel Conference Center Thackeray & O'hara Streets Pittsburgh, PA 15260 (US) (For All Designated States Except US).
EMERT-SEDLAK, Lori [US/US]; (US) (For US Only).
KODAMA, Toshiaki [JP/JP]; (US) (For US Only).
DAY, Billy, W. [US/US]; (US) (For US Only).
DAI, Weixiang [CN/CN]; (US) (For US Only).
TRIBLE, Ronald, P. [US/US]; (US) (For US Only).
SMITHGALL, Thomas, E. [US/US]; (US) (For US Only)
Inventors: EMERT-SEDLAK, Lori; (US).
KODAMA, Toshiaki; (US).
DAY, Billy, W.; (US).
DAI, Weixiang; (US).
TRIBLE, Ronald, P.; (US).
SMITHGALL, Thomas, E.; (US)
Agent: BENT, Stephen, A.; (US)
Priority Data:
61/053,135 14.05.2008 US
Title (EN) TARGETING AN HIV-1 NEF-HOST CELL KINASE COMPLEX
(FR) CIBLAGE D'UN COMPLEXE NEF DE VIH 1/KINASE DE CELLULE HÔTE
Abstract: front page image
(EN)Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3- diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.
(FR)L'invention concerne des médicaments candidats permettant l'inhibition de la réplication du VIH 1 qui puissent cibler les kinases de la famille Src (SFK), telles que Hck, qui interagissent avec la protéine Nef du virus. Des composés caractérisés par cette activité inhibitrice ont été identifiés via un essai permettant de déterminer l'activité de kinase d'une SFK dans un complexe Nef/SFK. Sont illustratives des inhibiteurs identifiés en utilisant l'essai de kinase diverses 2,3-diaminoquinoxalines et furo[2,3-]pyrimidines. Les inhibiteurs selon l'invention se sont avérés stopper la réplication virale du VIH 1 in vitro.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, 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, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)