Title:
TGFβ INHIBITOR AND PRODRUGS
Document Type and Number:
WIPO Patent Application WO/2020/104648
Kind Code:
A3
Abstract:
A compound of formula (I) with improved TGFβ signaling pathway inhibitory activity, improved therapeutic efficacy and improved toxicity profile, as well as two prodrugs thereof are disclosed. Compositions comprising said TGFβ signaling pathway inhibitor and prodrugs thereof are also disclosed. Additionally, present invention discloses said compound of formula (I) and prodrugs thereof for use in a method of treating diseases responsive to TGFβ signaling pathway inhibition.
Inventors:
TAURIELLO DANIELE (ES)
BYROM DANIEL (ES)
MATARÍN MORALES JOAN ANTONI (ES)
BATLLE GÓMEZ EDUARD (ES)
RIERA ESCALÉ ANTONI (ES)
BYROM DANIEL (ES)
MATARÍN MORALES JOAN ANTONI (ES)
BATLLE GÓMEZ EDUARD (ES)
RIERA ESCALÉ ANTONI (ES)
Application Number:
PCT/EP2019/082215
Publication Date:
July 02, 2020
Filing Date:
November 22, 2019
Export Citation:
Assignee:
FUNDACIO INST DE RECERCA BIOMEDICA IRB BARCELONA (ES)
INST CATALANA RECERCA ESTUDIS AVANCATS (ES)
UNIV BARCELONA (ES)
INST CATALANA RECERCA ESTUDIS AVANCATS (ES)
UNIV BARCELONA (ES)
International Classes:
A61K31/138; A61K31/4709; A61P35/00; C07C217/18; C07D471/00; C07D487/04
Domestic Patent References:
| WO2002094833A1 | 2002-11-28 | |||
| WO2014072517A1 | 2014-05-15 |
Other References:
HONG-YU LI ET AL: "Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-[beta] Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-[beta] Receptor Type I Inhibitor as Antitumor Agent", JOURNAL OF MEDICINAL CHEMISTRY, vol. 51, no. 7, 1 April 2008 (2008-04-01), US, pages 2302 - 2306, XP055577445, ISSN: 0022-2623, DOI: 10.1021/jm701199p
KYOUNG JIN P. YOON ET AL: "Activation of a camptothecin prodrug by specific carboxylesterases as predicted by quantitative structure-activity relationship and molecular docking studies", MOLECULAR CANCER THERAPEUTICS, 1 November 2003 (2003-11-01), United States, pages 1171 - 1181, XP055578086, Retrieved from the Internet
JOCHEN REITER ET AL: "Enzymatic cleavage of lignin β-O-4 aryl ether bonds via net internal hydrogen transfer", GREEN CHEMISTRY, vol. 15, no. 5, 1 January 2013 (2013-01-01), GB, pages 1373, XP055404944, ISSN: 1463-9262, DOI: 10.1039/c3gc40295a
KYOUNG JIN P. YOON ET AL: "Activation of a camptothecin prodrug by specific carboxylesterases as predicted by quantitative structure-activity relationship and molecular docking studies", MOLECULAR CANCER THERAPEUTICS, 1 November 2003 (2003-11-01), United States, pages 1171 - 1181, XP055578086, Retrieved from the Internet
JOCHEN REITER ET AL: "Enzymatic cleavage of lignin β-O-4 aryl ether bonds via net internal hydrogen transfer", GREEN CHEMISTRY, vol. 15, no. 5, 1 January 2013 (2013-01-01), GB, pages 1373, XP055404944, ISSN: 1463-9262, DOI: 10.1039/c3gc40295a
Attorney, Agent or Firm:
MANUEL ILLESCAS Y ASOCIADOS, S.L.U. (ES)
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