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1. (WO2012101064) N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2012/101064    International Application No.:    PCT/EP2012/050907
Publication Date: 02.08.2012 International Filing Date: 20.01.2012
IPC:
C07D 405/14 (2006.01), A61K 31/506 (2006.01), A61P 9/00 (2006.01), A61P 29/00 (2006.01), A61P 35/00 (2006.01)
Applicants: NOVARTIS AG [CH/CH]; Lichtstrasse 35 CH-4056 Basel (CH) (For All Designated States Except US).
BARSANTI, Paul, A. [GB/US]; (US) (For US Only).
HU, Cheng [CN/US]; (US) (For US Only).
JIN, Xianming [US/US]; (US) (For US Only).
NG, Simon, C. [US/US]; (US) (For US Only).
PFISTER, Keith, B. [US/US]; (US) (For US Only).
SENDZIK, Martin [DE/US]; (US) (For US Only).
SUTTON, James [US/US]; (US) (For US Only)
Inventors: BARSANTI, Paul, A.; (US).
HU, Cheng; (US).
JIN, Xianming; (US).
NG, Simon, C.; (US).
PFISTER, Keith, B.; (US).
SENDZIK, Martin; (US).
SUTTON, James; (US)
Agent: STRANG, Andrea; Novartis Pharma AG Patent Department CH-4002 Basel (CH)
Priority Data:
61/437,113 28.01.2011 US
Title (EN) N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
(FR) COMPOSÉS À BASE DE N-ACYL-PYRIMIDINE-BIARYL CONVENANT COMME INHIBITEURS DE PROTÉINE KINASE
Abstract: front page image
(EN)The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
(FR)La présente invention concerne un composé représenté par la formule générale (1) ainsi que certains de ses sels pharmaceutiquement admis, ses énantiomères, stéréoisomères, rotamères, tautomères, diastéréomères ou racémiques. Dans cette formule générale (1), l'un de X et Y est N, et l'autre est alors un atome de carbone éventuellement substitué, et les Z2 à Z5 sont un ou deux atomes d'azote. Ces composés, qui inhibent l'activité de CDK9, conviennent donc comme produits pharmaceutiques et composants de compositions pharmaceutiques. L'invention concerne également des procédés permettant de traiter une maladie ou un état médié par CDK9 en utilisant le composé de l'invention ou des compositions comprenant de tels composés.
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, QA, RO, RS, RU, RW, 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, RW, 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)