WO2013177349A3 - Quinazolinediones as tankyrase inhibitors - Google Patents

Quinazolinediones as tankyrase inhibitors Download PDF

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Publication number
WO2013177349A3
WO2013177349A3 PCT/US2013/042332 US2013042332W WO2013177349A3 WO 2013177349 A3 WO2013177349 A3 WO 2013177349A3 US 2013042332 W US2013042332 W US 2013042332W WO 2013177349 A3 WO2013177349 A3 WO 2013177349A3
Authority
WO
WIPO (PCT)
Prior art keywords
quinazolinediones
hydrogen
relates
tankyrase inhibitors
tankyrase
Prior art date
Application number
PCT/US2013/042332
Other languages
French (fr)
Other versions
WO2013177349A2 (en
Inventor
Richard M. Keenan
Aaron Bayne Miller
Donghui Qin
Original Assignee
Glaxosmithkline Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of WO2013177349A2 publication Critical patent/WO2013177349A2/en
Publication of WO2013177349A3 publication Critical patent/WO2013177349A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96—Two oxygen atoms

Abstract

This invention relates to compounds of Formula (I) and (l)(a) wherein R1, R2 and R3 are each independently hydrogen, halo, C1-C4alkyl, or C1-C4alkoxy; R4 is hydrogen or methyl; provided that at least one of R1, R2 and R3 is not hydrogen; or a pharmaceutically acceptable salt thereof. As well as the use of quinazolinediones for the modulation, notably the inhibition of the activity of tankyrases (TNKS1 and TNKS2). Suitably, the present invention relates to the use of quinazolinediones in the treatment of cancer, fibrosis and other hyperproliferative diseases through this mechanism.
PCT/US2013/042332 2012-05-25 2013-05-23 Quinazolinediones as tankyrase inhibitors WO2013177349A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261651687P 2012-05-25 2012-05-25
US61/651,687 2012-05-25
US201361773300P 2013-03-06 2013-03-06
US61/773,300 2013-03-06

Publications (2)

Publication Number Publication Date
WO2013177349A2 WO2013177349A2 (en) 2013-11-28
WO2013177349A3 true WO2013177349A3 (en) 2014-01-16

Family

ID=49624519

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2013/042332 WO2013177349A2 (en) 2012-05-25 2013-05-23 Quinazolinediones as tankyrase inhibitors

Country Status (1)

Country Link
WO (1) WO2013177349A2 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX346147B (en) 2012-03-07 2017-03-09 Inst Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use.
CA2922469A1 (en) 2013-09-11 2015-03-19 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
UY36060A (en) 2014-04-02 2015-10-30 Bayer Pharma AG AZOL COMPOUNDS REPLACED WITH AMIDA
WO2017055316A1 (en) 2015-10-01 2017-04-06 Bayer Pharma Aktiengesellschaft Amido-substituted azole compounds
WO2017055313A1 (en) 2015-10-01 2017-04-06 Bayer Pharma Aktiengesellschaft Amido-substituted azole compounds
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
WO2018078009A1 (en) 2016-10-29 2018-05-03 Bayer Pharma Aktiengesellschaft Amido-substituted cyclohexane derivatives
WO2018078005A1 (en) 2016-10-29 2018-05-03 Bayer Pharma Aktiengesellschaft Amido-substituted azaspiro derivatives as tankyrase inhibitors
WO2018087126A1 (en) 2016-11-09 2018-05-17 Bayer Pharma Aktiengesellschaft Amido-substituted cyclohexane derivatives as inhibitors of tankyrase
CN112898221B (en) * 2019-12-03 2023-12-08 浙江京新药业股份有限公司 Preparation method of benzoxazine diketone compound C and intermediate thereof
CN112624911A (en) * 2021-01-15 2021-04-09 阿里生物新材料（常州）有限公司 2-chloro-3-fluoro-4- (trifluoromethyl) benzaldehyde and synthetic method thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011042145A1 (en) * 2009-10-07 2011-04-14 Siena Biotech S.P.A. Wnt pathway antagonists
US20110136813A1 (en) * 2008-05-27 2011-06-09 Lawrence Lum Wnt protein signalling inhibitors
US20120058987A1 (en) * 2009-03-27 2012-03-08 Sanofi Therapeutic uses of quinazolinedione derivatives
US20120122863A1 (en) * 2007-08-16 2012-05-17 Boehringer Ingelheim International Gmbh Quinazolinedione Chymase Inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120122863A1 (en) * 2007-08-16 2012-05-17 Boehringer Ingelheim International Gmbh Quinazolinedione Chymase Inhibitors
US20110136813A1 (en) * 2008-05-27 2011-06-09 Lawrence Lum Wnt protein signalling inhibitors
US20120058987A1 (en) * 2009-03-27 2012-03-08 Sanofi Therapeutic uses of quinazolinedione derivatives
WO2011042145A1 (en) * 2009-10-07 2011-04-14 Siena Biotech S.P.A. Wnt pathway antagonists

Also Published As

Publication number Publication date
WO2013177349A2 (en) 2013-11-28

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