WIPO logo
Mobile | Deutsch | Español | Français | 日本語 | 한국어 | Português | Русский | 中文 | العربية |
PATENTSCOPE

Search International and National Patent Collections
World Intellectual Property Organization
Search
 
Browse
 
Translate
 
Options
 
News
 
Login
 
Help
 
Machine translation
1. (WO2014179401) 2-ARYLNAPHTHYRIDIN-4-ONES AS POTENT ANTITUMOR AGENTS TARGETING TUMORIGENIC CELL LINES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2014/179401    International Application No.:    PCT/US2014/036046
Publication Date: 06.11.2014 International Filing Date: 30.04.2014
IPC:
C07D 471/04 (2006.01), C07D 487/04 (2006.01), A61K 31/4745 (2006.01), A61P 35/00 (2006.01)
Applicants: KUO, Sheng-Chu; (TW).
LEE, Kuo-Hsiung [US/US]; (US).
HUANG, Li-Jiau; (TW).
WU, Tian-Shung; (TW).
LIU, Chin-Yu; (TW).
CHENG, Yung-Yi; (TW).
CHANG, Ling-Chu; (TW).
CHOU, Li-Chen; (TW).
HUANG, Chi-Hung; (TW).
TSAI, Meng-Tung; (TW).
LIAO, Chih-Chang; (TW).
HSU, Mei-Hua; (TW).
LIN, Hui-Yi; (TW).
WAY, Tzong-Der; (TW).
TENG, Che-Ming; (TW)
Inventors: KUO, Sheng-Chu; (TW).
LEE, Kuo-Hsiung; (US).
HUANG, Li-Jiau; (TW).
WU, Tian-Shung; (TW).
LIU, Chin-Yu; (TW).
CHENG, Yung-Yi; (TW).
CHANG, Ling-Chu; (TW).
CHOU, Li-Chen; (TW).
HUANG, Chi-Hung; (TW).
TSAI, Meng-Tung; (TW).
LIAO, Chih-Chang; (TW).
HSU, Mei-Hua; (TW).
LIN, Hui-Yi; (TW).
WAY, Tzong-Der; (TW).
TENG, Che-Ming; (TW)
Agent: FICHTER, Richard; (US)
Priority Data:
61/817,390 30.04.2013 US
Title (EN) 2-ARYLNAPHTHYRIDIN-4-ONES AS POTENT ANTITUMOR AGENTS TARGETING TUMORIGENIC CELL LINES
(FR) 2-ARYLNAPHTYRIDIN-4-ONES EN TANT QU'AGENTS ANTITUMORAUX PUISSANTS CIBLANT DES LIGNÉES CELLULAIRES TUMORIGÈNES
Abstract: front page image
(EN)In order to search for new antitumor drug candidates from 2-arylnaphthyridin-4-ones (ANs), we have designed and synthesized a series of 3 '-hydroxy or 6-hydroxy derivatives of ANs. Following the antitumor activity screening, most of these compounds were found to exhibit significant activity. Among them, 2-(3-hydroxyphenyl)-5-methyl-1,8-naphthyridin-4(1H)-one (67) was the most promising. In a preliminary action mechanism study, the treatment of Hep3B hepatoma cells with compound (67) reveals that its mechanism of action is affect on microtubule and metastasis-related proteins. Then, the corresponding phosphate prodrug (86) of compound (67) was tested against Hep3B xenograft nude mice model for antitumor activity.
(FR)Afin de rechercher de nouveaux médicaments candidats antitumoraux à partir de 2-arylnaphtyridin-4-ones (AN), nous avons conçu et synthétisé une série de dérivés 3'-hydroxy ou 6-hydroxy d'AN. A la suite du criblage de l'activité antitumorale, nous avons découvert que la plupart de ces composés présentent une activité significative. Parmi eux, la 2-(3-hydroxyphényl)-5-méthyl-1,8-naphtyridin-4(1H)-one (67) était la plus prometteuse. Dans une étude de mécanisme d'action préliminaire, le traitement de cellules d'hépatome Hep3B avec le composé (67) révèle que son mécanisme d'action affecte les protéines associées aux microtubules et aux métastases. Ensuite, le promédicament phosphate (86) correspondant du composé (67) a été testé sur un modèle de souris nude à xénogreffe Hep3B en vue de détecter son activité antitumorale.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, IR, IS, JP, KE, KG, 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, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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, 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, KM, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)