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1. (WO2010136491) BICYCLIC INDOLE-PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2010/136491    International Application No.:    PCT/EP2010/057244
Publication Date: 02.12.2010 International Filing Date: 26.05.2010
Chapter 2 Demand Filed:    21.12.2010    
IPC:
C07D 487/04 (2006.01), C07D 495/04 (2006.01), C07D 513/04 (2006.01), A61K 31/519 (2006.01), A61K 31/52 (2006.01), A61P 37/00 (2006.01)
Applicants: 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).
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).
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: HEIROTH, Ulrike; Grenzacherstrasse 124 CH-4070 Basel (CH)
Priority Data:
61/181,458 27.05.2009 US
Title (EN) BICYCLIC INDOLE-PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
(FR) COMPOSÉS BICYCLIQUES INDOLE-PYRIMIDINE INHIBITEURS DE PI3K SÉLECTIFS POUR P110 DELTA ET LEURS 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, (iv) X1 is CR7 and X2 is O, or (v) X1 is CR7 and X2 is NR2, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PBK, 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 concerne des composés de formule I (Ia et Ib) dans laquelle (i) X1 est N et X2 est S, (ii) X1 est CR7 et X2 est S, (iii) X1 est N et X2 est NR2, (iv) X1 est CR7 et X2 est O, ou (v) X1 est CR7 et X2 est NR2, y compris leurs stéréoisomères, tautomères, métabolites et sels pharmaceutiquement acceptables, qui sont utiles pour inhiber l'isoforme delta de PBK et pour traiter les troubles médiés par les kinases lipidiques, tels que l'inflammation, les troubles immunologiques et le cancer. L'invention concerne également des procédés d'utilisation de composés de formule I pour le diagnostic, la prévention et le traitement in vitro, in situ et in vivo de tels troubles dans des cellules mammaliennes, ou d'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)