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1. (WO2011135520) PIPERAZINOTRIAZINES AS PI3K INHIBITORS FOR USE IN THE TREATMENT ANTIPROLIFERATIVE DISORDERS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2011/135520    International Application No.:    PCT/IB2011/051829
Publication Date: 03.11.2011 International Filing Date: 27.04.2011
IPC:
A61K 31/53 (2006.01), A61P 35/00 (2006.01), C07D 403/04 (2006.01)
Applicants: UNIVERSITY OF BASEL [CH/CH]; Unitectra, Technology Transfer Schützenmattstrasse 16 CH-4003 Basel (CH) (For All Designated States Except US).
CMILJANOVIC, Vladimir [RS/CH]; (CH) (For US Only).
CMILJANOVIC, Natasa [RS/CH]; (CH) (For US Only).
GIESE, Bernd [DE/CH]; (CH) (For US Only).
WYMANN, Matthias [CH/CH]; (CH) (For US Only)
Inventors: CMILJANOVIC, Vladimir; (CH).
CMILJANOVIC, Natasa; (CH).
GIESE, Bernd; (CH).
WYMANN, Matthias; (CH)
Priority Data:
1007227.0 30.04.2010 GB
Title (EN) PIPERAZINOTRIAZINES AS PI3K INHIBITORS FOR USE IN THE TREATMENT ANTIPROLIFERATIVE DISORDERS
(FR) PIPÉRAZINOTRIAZINES COMME INHIBITEURS DE PI3K POUR UNE UTILISATION DANS LE TRAITEMENT DE TROUBLES ANTIPROLIFÉRATIFS
Abstract: front page image
(EN)The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl- sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.
(FR)L'invention concerne des composés de formule (I) dans laquelle R1 est méthyle, n-hexyle, aminoéthyle, méthylaminoéthyle, éthylaminoéthyle, diméthylaminoéthyle, acryloylaminoéthyle, méthacryloylaminoéthyle, méthoxyéthyle, éthoxyéthyle, d-C4-alkyl-sulfonyle, acryloyle ou méthacryloyle; ou R1 est aminoéthyle, acryloyle ou acryloylaminoéthyle portant un liant et une étiquette, et R2 et R3, indépendamment l'un de l'autre, sont hydrogène ou CrC4-alkyle, ou R2 et R3 forment conjointement un pont méthylène ou éthylène; et des tautomères, des solvates et des sels pharmaceutiquement acceptables de ceux-ci. Ces composés sont efficaces dans la prévention ou le traitement d'une maladie ou d'un trouble modulé par des kinases PI3 et/ou mTOR, en particulier dans le traitement d'un trouble hyperprolifératif.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, 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, 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, PE, PG, PH, PL, PT, RO, RS, RU, 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, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, 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, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)