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1. (WO2010024783) BIARYLRHODANINE AND PYRIDYLRHODANINE COMPOUNDS AND THEIR USE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2010/024783    International Application No.:    PCT/SG2009/000301
Publication Date: 04.03.2010 International Filing Date: 27.08.2009
Chapter 2 Demand Filed:    21.06.2010    
IPC:
C07D 417/06 (2006.01), A61P 35/00 (2006.01), C07D 417/14 (2006.01), A61K 31/426 (2006.01), C07D 277/04 (2006.01), A61K 31/427 (2006.01), C07D 277/36 (2006.01)
Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH [SG/SG]; 1 Fusionopolis Way #20-10 Connexis Singapore 138632 (SG) (For All Designated States Except US).
NATIONAL UNIVERSITY OF SINGAPORE [SG/SG]; 21 Lower Kent Ridge Road Singapore 119077 (SG) (For All Designated States Except US).
CHAI, Christina, L., L. [AU/SG]; (SG) (For US Only).
BERNARDO, Paul, H. [US/SG]; (SG) (For US Only).
XU, Jin [SG/SG]; (SG) (For US Only).
YU, Victor, C. [CN/SG]; (SG) (For US Only).
WAN, Kah-Fei [MY/SG]; (SG) (For US Only).
MOK, Henry, Y., K. [CN/SG]; (SG) (For US Only).
SIVARAMAN, Thirunavukkarasu [IN/SG]; (SG) (For US Only).
KJRISHNAMOORTHY, Janarthanan [IN/SG]; (SG) (For US Only)
Inventors: CHAI, Christina, L., L.; (SG).
BERNARDO, Paul, H.; (SG).
XU, Jin; (SG).
YU, Victor, C.; (SG).
WAN, Kah-Fei; (SG).
MOK, Henry, Y., K.; (SG).
SIVARAMAN, Thirunavukkarasu; (SG).
KJRISHNAMOORTHY, Janarthanan; (SG)
Agent: YU SARN AUDREY & PARTNERS; 24 Raffles Place #27-01 Clifford Centre Singapore 048621 (SG)
Priority Data:
61/092,141 27.08.2008 US
Title (EN) BIARYLRHODANINE AND PYRIDYLRHODANINE COMPOUNDS AND THEIR USE
(FR) COMPOSÉS DE BIARYLRHODANINE ET DE PYRIDYLRHODANINE ET LEUR UTILISATION
Abstract: front page image
(EN)The present invention pertains generally to the field of therapeutic compounds, and more specifically to compounds related to rhodanine, which compounds are inter alia inhibitors and/or binders of antiapoptotic/pro-survival Bcl-2 proteins such as Bcl-XL and/or Mcl-1. More specifically, the present invention is concerned with Rhodanine- based Pan-Bcl-2 inhibitors and Mcl-1 -specific inhibitors as anti-cancer compounds. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit and/or bind Bcl-2 proteins such as Bcl-XL and/or Mcl-1, and in the treatment of diseases and conditions that are mediated by Bcl-2 proteins, that are ameliorated by the inhibition of Bcl-2 protein function (such as Bcl-XL and/or Mcl-1 ) including proliferative conditions such as cancer, optionally in combination with another agent.
(FR)La présente invention concerne généralement le domaine de composés thérapeutiques, et plus spécifiquement des composés apparentés à la rhodanine, lesdits composés étant, entre autre, des inhibiteurs et/ou des liants de protéines antiapoptotiques/pro-survie Bcl-2 telles que Bcl-XL et/ou Mcl-1. Plus spécifiquement, la présente invention concerne des inhibiteurs pan-Bcl-2 à base de rhodanine et des inhibiteurs spécifiques de Mcl-1 en tant que composés anticancéreux. La présente invention concerne en outre des compositions pharmaceutiques comprenant de tels composés, et l'utilisation de tels composés et compositions, in vitro et in vivo, pour inhiber et/ou se lier à des protéines Bcl-2 telles que Bcl-XL et/ou Mcl-1, et dans le traitement de maladies et d'affections qui sont véhiculées par des protéines Bcl-2, qui sont améliorées par l'inhibition de la fonction de protéines Bcl-2 (telles que Bcl-XL et/ou Mcl-1) comprenant des affections prolifératives telles que le cancer, facultativement en combinaison avec un autre agent.
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, 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, 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)