SG11202112226WA - Acss2 inhibitors and methods of use thereof - Google Patents

Acss2 inhibitors and methods of use thereof

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Publication number
SG11202112226WA
SG11202112226WA SG11202112226WA SG11202112226WA SG11202112226WA SG 11202112226W A SG11202112226W A SG 11202112226WA SG 11202112226W A SG11202112226W A SG 11202112226WA SG 11202112226W A SG11202112226W A SG 11202112226WA SG 11202112226W A SG11202112226W A SG 11202112226WA
Authority
SG
Singapore
Prior art keywords
methods
acss2
inhibitors
acss2 inhibitors
Prior art date
Application number
SG11202112226WA
Inventor
Philippe Nakache
Omri Erez
Simone Botti
Andreas Goutopoulos
Harry Finch
Original Assignee
Metabomed Ltd
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
Priority claimed from US16/411,168 external-priority patent/US10851064B2/en
Application filed by Metabomed Ltd filed Critical Metabomed Ltd
Publication of SG11202112226WA publication Critical patent/SG11202112226WA/en

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    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41521,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
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US11834441B2 (en) 2019-12-06 2023-12-05 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
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Family Cites Families (19)

* Cited by examiner, † Cited by third party
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DE2324893A1 (en) * 1973-05-17 1974-12-12 Hoechst Ag 5-Phenylcarbamoyl-4-methyl-1-hydroxy-imidazoles - with coccidiostatic and trematocidal activity
US4207317A (en) * 1978-03-13 1980-06-10 Ciba-Geigy Corporation 1-Aryl-4-carbamoyl-pyrazolin-5-ones
DD140966A1 (en) * 1978-12-28 1980-04-09 Doerthe Creuzburg MEANS FOR REGULATING PLANT GROWTH
JPH11291635A (en) * 1998-04-06 1999-10-26 Mitsubishi Paper Mills Ltd Thermosensitive recording material
AR034897A1 (en) * 2001-08-07 2004-03-24 Hoffmann La Roche N-MONOACILATED DERIVATIVES OF O-PHENYLENDIAMINS, THEIR HETEROCICLICAL ANALOGS OF SIX MEMBERS AND THEIR USE AS PHARMACEUTICAL AGENTS
MXPA04002397A (en) * 2001-09-14 2004-12-02 Methylgene Inc Inhibitors of histone deacetylase.
SI1828177T1 (en) * 2004-12-17 2009-02-28 Lilly Co Eli Novel mch receptor antagonists
WO2007026215A1 (en) * 2005-08-29 2007-03-08 Glenmark Pharmaceuticals S.A. Pyrazole derivatives as cannabinoid receptor ligands, pharmaceutical compositions containing? them, and processes for their preparation
EP2569287B1 (en) * 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US9073911B2 (en) * 2011-06-09 2015-07-07 Hoffmann-La Roche Inc. Pyrazole derivatives
WO2013096060A1 (en) * 2011-12-23 2013-06-27 Novartis Ag Compounds for inhibiting the interaction of bcl2 with binding partners
WO2013159224A1 (en) * 2012-04-25 2013-10-31 University Of Manitoba 2-carbamo(thio)yl-1,3- dioxopropyl derivatives in cancer therapy
WO2015175845A1 (en) * 2014-05-15 2015-11-19 Peloton Therapeutics, Inc. Benzimidazole derivatives and uses thereof
TW201734003A (en) * 2016-01-05 2017-10-01 英塞特公司 Pyridine and pyridimine compounds as PI3K-gamma inhibitors
WO2019036562A1 (en) * 2017-08-18 2019-02-21 Saint Louis University Err inverse agonists
JP7423068B2 (en) * 2017-09-26 2024-01-29 ザ トラスティーズ オブ ザ ユニバーシティ オブ ペンシルバニア Compositions and methods of inhibiting ACSS2
CA2984073A1 (en) * 2017-10-27 2019-04-27 Nuchem Therapeutics Inc. Inhibitors of polynucleotide repeat-associated rna foci and uses thereof
AU2018370096B2 (en) * 2017-11-15 2023-08-31 Metabomed Ltd ACSS2 inhibitors and methods of use thereof
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