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1. (WO2010138589) BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2010/138589    International Application No.:    PCT/US2010/036199
Publication Date: 02.12.2010 International Filing Date: 26.05.2010
IPC:
C07D 487/04 (2006.01), C07D 491/04 (2006.01), C07D 513/04 (2006.01), A61K 31/519 (2006.01), A61P 35/00 (2006.01), A61P 9/00 (2006.01), A61P 29/00 (2006.01), A61P 25/00 (2006.01)
Applicants: GENENTECH, INC. [US/US]; 1 DNA Way South San Francisco, California 94080 (US) (For All Designated States Except US).
F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basel (CH) (For All Designated States Except US).
CASTANEDO, Georgette [US/US]; (US) (For US Only).
CHAN, Bryan [CA/US]; (US) (For US Only).
GOLDSTEIN, David Michael [US/US]; (US) (For US Only).
KONDRU, Rama K. [IN/US]; (US) (For US Only).
LUCAS, Matthew C. [GB/US]; (US) (For US Only).
PALMER, Wylie Solang [US/US]; (US) (For US Only).
PRICE, Stephen [GB/GB]; (GB) (For US Only).
SAFINA, Brian [US/US]; (US) (For US Only).
SAVY, Pascal Pierre Alexandre [FR/GB]; (GB) (For US Only).
SEWARD, Eileen Mary [IE/GB]; (GB) (For US Only).
SUTHERLIN, Daniel P. [US/US]; (US) (For US Only).
SWEENEY, Zachary Kevin [US/US]; (US) (For US Only)
Inventors: CASTANEDO, Georgette; (US).
CHAN, Bryan; (US).
GOLDSTEIN, David Michael; (US).
KONDRU, Rama K.; (US).
LUCAS, Matthew C.; (US).
PALMER, Wylie Solang; (US).
PRICE, Stephen; (GB).
SAFINA, Brian; (US).
SAVY, Pascal Pierre Alexandre; (GB).
SEWARD, Eileen Mary; (GB).
SUTHERLIN, Daniel P.; (US).
SWEENEY, Zachary Kevin; (US)
Agent: ANDRUS, Alex; Genentech, Inc. 1 DNA Way, MS-49 South San Francisco, California 94080 (US)
Priority Data:
61/181,452 27.05.2009 US
61/287,607 17.12.2009 US
Title (EN) BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
(FR) COMPOSÉS PYRIMIDINES BICYCLIQUES INHIBITEURS DE PI3K SÉLECTIFS POUR P110 DELTA, ET PROCÉDÉS D'UTILISATION
Abstract: front page image
(EN)Formula (I) ((Ia) and (Ib)) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
(FR)L'invention porte sur des composés de Formule (I) ((Ia) et(Ib)), où (i) X1 représente N et X2 représente S, (ii) X1 représente CR7 et X2 représente S, (iii) X1 représente N et X2 représente NR2, ou (iv) X1 représente CR7 et X2 représente O, comprenant des stéréo-isomères, des tautomères, des métabolites et des sels pharmaceutiquement acceptables de ceux-ci, lesquels composés sont utiles pour inhiber l'isoforme delta de PI3K, et pour traiter des troubles à médiation par des lipides kinases, tels qu'une inflammation, une maladie immunologique et un cancer. L'invention porte sur des procédés d'utilisation des composés de Formule (I) pour un diagnostic in vitro, in situ et in vivo, une prévention ou un traitement de tels troubles dans des cellules de mammifère, ou des états pathologiques associés.
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, 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)