(19)
(11) EP 3 307 251 B8

(12) CORRECTED EUROPEAN PATENT SPECIFICATION
Note: Bibliography reflects the latest situation

(15) Correction information:
Corrected version no 1 (W1 B1)

(48) Corrigendum issued on:
01.12.2021 Bulletin 2021/48

(45) Mention of the grant of the patent:
20.10.2021 Bulletin 2021/42

(21) Application number: 16730210.8

(22) Date of filing: 09.06.2016
(51) International Patent Classification (IPC): 
C07D 239/47(2006.01)
C07K 16/00(2006.01)
C07D 201/00(2006.01)
(52) Cooperative Patent Classification (CPC):
C12Y 207/01048; A61P 35/00; A61K 9/2004; C07D 239/47; A61K 31/513; G01N 2800/52; A61K 9/4841; A61K 2039/505
 
C-Sets:
A61K 31/513, A61K 2300/00;
(86) International application number:
PCT/US2016/036768
(87) International publication number:
WO 2016/201146 (15.12.2016 Gazette 2016/50)

(54)

FLUOROCYCLOPENTENYLCYTOSINE USES AND PROCESSES OF PREPARATION

FLUOROCYCLOPENTENYLCYTOSIN, VERWENDUNG UND VERFAHREN ZUR HERSTELLUNG

UTILISATIONS DE FLUOROCYCLOPENTÉNYLCYTOSINE ET PROCÉDÉS DE PRÉPARATION DE CE COMPOSÉ


(84) Designated Contracting States:
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

(30) Priority: 09.06.2015 US 201562173174 P
27.08.2015 US 201562210708 P
01.02.2016 US 201662289801 P
07.04.2016 US 201662319369 P

(43) Date of publication of application:
18.04.2018 Bulletin 2018/16

(60) Divisional application:
21203072.0

(73) Proprietor: Ocuphire Pharma, Inc.
Rockville, MD 20850 (US)

(72) Inventors:
  • LEE, Young Bok
    Rockville, Maryland 20850 (US)
  • KIM, Deog Joong
    Rockville, Maryland 20850 (US)
  • PETERS, Godefridus J.
    1007 MB Amsterdam (NL)
  • SARKISJAN, Dzjemma
    92360 Meudon (FR)
  • MAZHARI, Reza
    Rockville, Maryland 20850 (US)

(74) Representative: dompatent von Kreisler Selting Werner - Partnerschaft von Patent- und Rechtsanwälten mbB 
Deichmannhaus am Dom Bahnhofsvorplatz 1
50667 Köln
50667 Köln (DE)


(56) References cited: : 
WO-A2-2005/097757
US-A1- 2014 275 537
   
  • Mi Young Yang ET AL: "A novel cytidine analog, RX-3117, shows potent efficacy in xenograft models, even in tumors that are resistant to gemcitabine", Anticancer research, December 2014 (2014-12), page 6951, XP055289638, Greece Retrieved from the Internet: URL:http://ar.iiarjournals.org/content/34/ 12/6951.full.pdf [retrieved on 2016-07-22] cited in the application
  • WON JUN CHOI ET AL: "Fluorocyclopentenyl-cytosine with Broad Spectrum and Potent Antitumor Activity +", JOURNAL OF MEDICINAL CHEMISTRY, vol. 55, no. 9, 10 May 2012 (2012-05-10), pages 4521-4525, XP055120207, ISSN: 0022-2623, DOI: 10.1021/jm3004009 cited in the application
  • ISTVAN UDVAROS ET AL: "A phase 1 exploratory study of RX-3117 to determine oral bioavailability in cancer subjects with solid tumors.", JOURNAL OF CLINICAL ONCOLOGY, vol. 33, no. 15 (suppl), 20 May 2015 (2015-05-20), page e13545, XP055290526,
   
Note: Within nine months from the publication of the mention of the grant of the European patent, any person may give notice to the European Patent Office of opposition to the European patent granted. Notice of opposition shall be filed in a written reasoned statement. It shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention).