IL297883A - acss2 inhibitors based on imidazole 3-oxide derivatives and methods for their use - Google Patents

acss2 inhibitors based on imidazole 3-oxide derivatives and methods for their use

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Publication number
IL297883A
IL297883A IL297883A IL29788322A IL297883A IL 297883 A IL297883 A IL 297883A IL 297883 A IL297883 A IL 297883A IL 29788322 A IL29788322 A IL 29788322A IL 297883 A IL297883 A IL 297883A
Authority
IL
Israel
Prior art keywords
linear
branched
substituted
unsubstituted
methyl
Prior art date
Application number
IL297883A
Other languages
English (en)
Hebrew (he)
Inventor
Philippe Nakache
Omri Erez
Simone Botti
Andreas Goutopoulos
Harry Finch
Original Assignee
Metabomed Ltd
Philippe Nakache
Omri Erez
Simone Botti
Andreas Goutopoulos
Harry Finch
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 Metabomed Ltd, Philippe Nakache, Omri Erez, Simone Botti, Andreas Goutopoulos, Harry Finch filed Critical Metabomed Ltd
Publication of IL297883A publication Critical patent/IL297883A/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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    • A61K31/41641,3-Diazoles
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    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Publication number Priority date Publication date Assignee Title
US12133852B2 (en) 2017-11-15 2024-11-05 Epivario, Inc. ACSS2 inhibitors and methods of use thereof
US11739078B2 (en) 2019-02-22 2023-08-29 Insilico Medicine Ip Limited Methods of inhibiting kinases
US12441689B2 (en) * 2019-05-14 2025-10-14 Epivario, Inc. ACSS2 inhibitors and methods of use thereof
CA3164134A1 (en) 2019-12-06 2021-06-10 Vertex Pharmaceuticals Incorporated Substituted tetrahydrofurans as modulators of sodium channels
CN112480085B (zh) * 2020-12-17 2022-10-25 上海英诺富成生物科技有限公司 一种化合物或其药学上可接受的盐、异构体、前药、多晶型物或溶剂化物
CA3208490A1 (en) 2021-02-24 2022-09-01 Aleksandrs Zavoronkovs Analogs for the treatment of disease
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
CN114044754A (zh) * 2021-11-23 2022-02-15 贵州大学 一类5-三氟甲基-4-吡唑衍生物的制备方法及其在抑制肿瘤细胞上的应用
CN114716380B (zh) * 2022-04-01 2024-06-21 新乡医学院 一种相转移催化的4-取代吡唑酮类化合物不对称氟化方法
CN116808042A (zh) * 2023-08-08 2023-09-29 江苏省人民医院(南京医科大学第一附属医院) 乙酰辅酶a合成酶2抑制剂在治疗胰腺神经内分泌肿瘤中的应用
CN118344267A (zh) * 2024-04-17 2024-07-16 广东广康生化科技股份有限公司 一种联苯肼酯高效合成新方法

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE140966C (https=)
DE2324893A1 (de) 1973-05-17 1974-12-12 Hoechst Ag 1-hydroxy-imidazole und verfahren zu ihrer herstellung
US3905997A (en) 1974-06-21 1975-09-16 Warner Lambert Co 3-Aryl-5-oxo-2-pyrazoline-4-carboxanilides and process therefor
US4207317A (en) * 1978-03-13 1980-06-10 Ciba-Geigy Corporation 1-Aryl-4-carbamoyl-pyrazolin-5-ones
DD140966A1 (de) * 1978-12-28 1980-04-09 Doerthe Creuzburg Mittel zur regulierung des pflanzenwachstums
JPH11291635A (ja) * 1998-04-06 1999-10-26 Mitsubishi Paper Mills Ltd 感熱記録材料
CN1325385A (zh) * 1998-11-09 2001-12-05 詹姆斯·布莱克基金有限公司 胃泌素和缩胆囊素受体配体
AR034897A1 (es) * 2001-08-07 2004-03-24 Hoffmann La Roche Derivados n-monoacilados de o-fenilendiaminas, sus analogos heterociclicos de seis miembros y su uso como agentes farmaceuticos
EP1429765A2 (en) * 2001-09-14 2004-06-23 Methylgene, Inc. Inhibitors of histone deacetylase
MX2007007226A (es) * 2004-12-17 2007-08-21 Lilly Co Eli Antagonistas receptores novedosos de hormona concentradora de melanina (mch).
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
JP2013526540A (ja) * 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
US9073911B2 (en) * 2011-06-09 2015-07-07 Hoffmann-La Roche Inc. Pyrazole derivatives
EP2794592A1 (en) * 2011-12-23 2014-10-29 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
WO2017120194A1 (en) 2016-01-05 2017-07-13 Incyte Corporation Pyridine and pyridimine compounds as pi3k-gamma inhibitors
US11795162B2 (en) * 2017-08-18 2023-10-24 Saint Louis University Modulators of the estrogen-related receptor
EP3687628A4 (en) * 2017-09-26 2021-09-22 The Trustees of The University of Pennsylvania COMPOSITIONS AND METHODS TO INHIBIT ACSS2
CA2984073A1 (en) 2017-10-27 2019-04-27 Nuchem Therapeutics Inc. Inhibitors of polynucleotide repeat-associated rna foci and uses thereof
KR20200089291A (ko) * 2017-11-15 2020-07-24 메타보메드 리미티드 Acss2 저해제 및 이의 사용 방법
US12441689B2 (en) * 2019-05-14 2025-10-14 Epivario, Inc. ACSS2 inhibitors and methods of use thereof

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