AU2020392087B2 - Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use - Google Patents

Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use

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Publication number
AU2020392087B2
AU2020392087B2 AU2020392087A AU2020392087A AU2020392087B2 AU 2020392087 B2 AU2020392087 B2 AU 2020392087B2 AU 2020392087 A AU2020392087 A AU 2020392087A AU 2020392087 A AU2020392087 A AU 2020392087A AU 2020392087 B2 AU2020392087 B2 AU 2020392087B2
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AU
Australia
Prior art keywords
trifluoromethyl
methyl
pyrazol
pyrimidin
imidazo
Prior art date
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Active
Application number
AU2020392087A
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English (en)
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AU2020392087A1 (en
Inventor
Jennifer R. Allen
Michela BELTRANI
Matthew P. Bourbeau
Teodora P. DAMYANOVA
Iain Lingard
Ana E. MINATTI
Paolo VINCETTI
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Amgen Inc
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Amgen Inc
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Publication of AU2020392087A1 publication Critical patent/AU2020392087A1/en
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Publication of AU2020392087B2 publication Critical patent/AU2020392087B2/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2020392087A 2019-11-25 2020-11-24 Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use Active AU2020392087B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962939821P 2019-11-25 2019-11-25
US62/939,821 2019-11-25
PCT/US2020/062020 WO2021108408A1 (en) 2019-11-25 2020-11-24 Heterocyclic compounds as delta-5 desaturase inhibitors and methods of use

Publications (2)

Publication Number Publication Date
AU2020392087A1 AU2020392087A1 (en) 2022-06-09
AU2020392087B2 true AU2020392087B2 (en) 2025-10-23

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AU2020392087A Active AU2020392087B2 (en) 2019-11-25 2020-11-24 Heterocyclic compounds as Delta-5 Desaturase inhibitors and methods of use

Country Status (21)

Country Link
US (3) US11512097B2 (https=)
EP (1) EP4065223A1 (https=)
JP (2) JP7254246B2 (https=)
KR (2) KR20230154292A (https=)
CN (2) CN114728167B (https=)
AR (1) AR120556A1 (https=)
AU (1) AU2020392087B2 (https=)
BR (1) BR112022010054A2 (https=)
CA (1) CA3162281A1 (https=)
CL (2) CL2022001357A1 (https=)
CO (1) CO2022008690A2 (https=)
CR (1) CR20220308A (https=)
IL (1) IL293191B2 (https=)
JO (1) JOP20220125A1 (https=)
MX (1) MX2022006281A (https=)
PE (1) PE20231097A1 (https=)
PH (1) PH12022551282A1 (https=)
SA (1) SA522432710B1 (https=)
TW (2) TWI815061B (https=)
UY (1) UY38971A (https=)
WO (1) WO2021108408A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11220510B2 (en) * 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
CN114728167B (zh) 2019-11-25 2024-03-19 安进公司 作为δ-5脱饱和酶抑制剂的杂环化合物以及使用方法
CN115557903A (zh) * 2022-09-27 2023-01-03 山东潍坊润丰化工股份有限公司 一种特草定的制备方法
CN120435293A (zh) 2022-11-23 2025-08-05 安进公司 选择使用fads-1抑制剂治疗fads1介导的疾病或障碍的患者

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090253704A1 (en) * 2008-04-04 2009-10-08 Dmitry Koltun PYRROLOTRIAZINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
WO2011114148A1 (en) * 2010-03-17 2011-09-22 Astrazeneca Ab 4h- [1, 2, 4] triazolo [5, 1 -b] pyrimidin-7 -one derivatives as ccr2b receptor antagonists

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3130633A1 (de) 1981-08-01 1983-02-17 Basf Ag, 6700 Ludwigshafen 7-amino-azolo(1,5-a)pyrimidine und diese enthaltende fungizide
DE3786365T2 (de) 1986-04-07 1993-10-21 Ihara Chemical Ind Co 5H-1,3,4-Thiadiazolo[3,2-a]pyrimidin-5-on-Derivate und diese enthaltende Gartenbau- und landwirtschaftliche Fungizidmittel.
EP0948496A2 (en) 1996-12-05 1999-10-13 Amgen inc. Substituted pyrimidinone and pyridone compounds and methods of use
US6096753A (en) 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
US6537998B1 (en) * 1999-10-15 2003-03-25 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
MXPA02003614A (es) 1999-10-15 2002-10-23 Neurocrine Biosciences Inc Antagonistas del receptor de la hormona liberadora de ganadotropina y metodos relacionados con los mismos..
TW200401770A (en) 2002-06-18 2004-02-01 Sankyo Co Fused-ring pyrimidin-4(3H)-one derivatives, processes for the preparation and uses thereof
JP2004107228A (ja) 2002-09-17 2004-04-08 Nippon Nohyaku Co Ltd 双環性ピリミジノン誘導体及びこれを有効成分とする除草剤
AR049769A1 (es) 2004-01-22 2006-09-06 Novartis Ag Derivados de pirazolo(1,5-a)pirimidin 7-il-amina para utilizarse en el tratamiento de enfermedades dependientes de la quinasa de proteina
US20050222171A1 (en) 2004-01-22 2005-10-06 Guido Bold Organic compounds
US7906645B2 (en) 2004-12-24 2011-03-15 Astrazeneca Ab Heterocyclic compounds as ccr2b antagonists
JP2008546843A (ja) 2005-06-27 2008-12-25 アムゲン インコーポレイティッド 抗炎症性アリールニトリル化合物
WO2007027012A1 (en) 2005-07-18 2007-03-08 Samsung Electronics Co., Ltd. Video coding method and apparatus for reducing mismatch between encoder and decoder
US20080200480A1 (en) 2005-07-27 2008-08-21 Basf Aktiengesellschaft Fungicidal 6-Phenyltriazolopyrimidinylamines
US20080312078A1 (en) 2005-07-27 2008-12-18 Basf Aktiengesellschaft 6-Phenyl-Pyrazolopyrimidine-7-Ylamine Fungicides
CN101227819A (zh) 2005-07-27 2008-07-23 巴斯福股份公司 杀真菌剂5-甲基-6-苯基三唑并嘧啶基胺
BRPI0616985B1 (pt) 2005-10-06 2021-10-26 Merck Sharp & Dohme Corp. Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto
CA2664375A1 (en) 2006-09-28 2008-04-03 Novartis Ag Pyrazolo [1, 5-a] pyrimidine derivatives and their therapeutic use
CA2665476A1 (en) 2006-10-05 2008-04-10 Cv Therapeutics, Inc. Bicyclic nitrogen-containing heterocyclic compounds for use as stearoyl coa desaturase inhibitors
WO2008057601A2 (en) 2006-11-08 2008-05-15 The Rockefeller University Organic compounds
US20080194557A1 (en) 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
WO2008089310A2 (en) 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of obesity
US8211828B2 (en) 2007-01-19 2012-07-03 Basf Se Fungicidal mixtures of 1-methylpyrazol-4-ylcarboxanilides and azolopyrimidinylamines
EP2131658A2 (en) 2007-01-30 2009-12-16 Basf Se Method for improving plant health
US8461077B2 (en) 2007-03-23 2013-06-11 Basf Se Combinations of active substances
WO2009086303A2 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
US8119647B2 (en) 2008-04-23 2012-02-21 Glenmark Pharmaceuticals S.A. Fused pyrimidineone compounds as TRPV3 modulators
US20100099561A1 (en) 2008-10-15 2010-04-22 E.I. Du Pont De Nemours And Company Heterobicyclic alkylthio-bridged isoxazolines
US20100190747A1 (en) 2009-01-27 2010-07-29 Hideo Suzuki Fused ring compound and use thereof
KR101763656B1 (ko) 2009-06-29 2017-08-01 인사이트 홀딩스 코포레이션 Pi3k 저해물질로서의 피리미디논
WO2012011592A1 (ja) 2010-07-23 2012-01-26 武田薬品工業株式会社 複素環化合物およびその用途
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
WO2013177538A2 (en) 2012-05-24 2013-11-28 Colorado State University Research Foundation Inhibition of delta-6 desaturase for the treatment of cardiometabolic disease
KR20150130491A (ko) 2013-03-13 2015-11-23 제넨테크, 인크. 피라졸로 화합물 및 그것의 용도
EP3041474B1 (en) 2013-09-05 2020-03-18 Genentech, Inc. Antiproliferative compounds
WO2015064714A1 (ja) 2013-10-31 2015-05-07 国立大学法人東京大学 オートタキシン阻害活性を有する1-置換イミダゾピリミジノン誘導体
WO2015135094A1 (en) 2014-03-13 2015-09-17 Genentech, Inc. Therapeutic compounds and uses thereof
CA2946702C (en) 2014-04-23 2022-06-28 Mitsubishi Tanabe Pharma Corporation Bicyclic or tricyclic heterocyclic compound
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
JP6791717B2 (ja) 2015-10-22 2020-11-25 田辺三菱製薬株式会社 医薬組成物
JP2017091808A (ja) 2015-11-10 2017-05-25 株式会社フジクラ 酸化物超電導線材の製造方法及び超電導コイルの製造方法
WO2017112678A1 (en) 2015-12-21 2017-06-29 Rima Mcleod Compounds and methods for treating, detecting, and identifying compounds to treat apicomplexan parasitic diseases
JP6832430B2 (ja) 2016-08-31 2021-02-24 アジオス ファーマシューティカルズ, インコーポレイテッド 細胞代謝過程の阻害剤
WO2018039972A1 (en) * 2016-08-31 2018-03-08 Agios Pharmaceuticals, Inc. Inhibitors of cellular metabolic processes
CN106749271B (zh) 2016-12-07 2019-04-05 青岛科技大学 一类[1,2,4]-三氮唑并[1,5-a]嘧啶酮类杂环化合物、其制备方法及其用途
WO2018213365A1 (en) 2017-05-15 2018-11-22 Dana-Farber Cancer Institute, Inc. Compounds for treating dengue virus infection and other viral infections
WO2018229683A1 (en) 2017-06-15 2018-12-20 Novartis Ag 5,6-fused-bicyclic compounds and compositions for the treatment of parasitic diseases
SG11202002218VA (en) 2017-09-15 2020-04-29 Aduro Biotech Inc Pyrazolopyrimidinone compounds and uses thereof
CN114728167B (zh) 2019-11-25 2024-03-19 安进公司 作为δ-5脱饱和酶抑制剂的杂环化合物以及使用方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090253704A1 (en) * 2008-04-04 2009-10-08 Dmitry Koltun PYRROLOTRIAZINONE DERIVATIVES FOR USE AS STEAROYL CoA DESATURASE INHIBITORS
WO2011114148A1 (en) * 2010-03-17 2011-09-22 Astrazeneca Ab 4h- [1, 2, 4] triazolo [5, 1 -b] pyrimidin-7 -one derivatives as ccr2b receptor antagonists

Also Published As

Publication number Publication date
AU2020392087A1 (en) 2022-06-09
JP2022549739A (ja) 2022-11-28
JP7254246B2 (ja) 2023-04-07
TW202132317A (zh) 2021-09-01
TW202409042A (zh) 2024-03-01
CN114728167B (zh) 2024-03-19
KR20230154292A (ko) 2023-11-07
IL293191A (en) 2022-07-01
US20210221824A1 (en) 2021-07-22
KR102598203B1 (ko) 2023-11-03
JOP20220125A1 (ar) 2023-01-30
JP7698676B2 (ja) 2025-06-25
CL2022001357A1 (es) 2023-03-10
US20230159560A1 (en) 2023-05-25
US20210188874A1 (en) 2021-06-24
IL293191B2 (en) 2025-09-01
CO2022008690A2 (es) 2022-06-30
CN118161500A (zh) 2024-06-11
PH12022551282A1 (en) 2023-11-29
AR120556A1 (es) 2022-02-23
EP4065223A1 (en) 2022-10-05
US12448396B2 (en) 2025-10-21
JP2023078418A (ja) 2023-06-06
SA522432710B1 (ar) 2025-05-29
WO2021108408A1 (en) 2021-06-03
BR112022010054A2 (pt) 2022-08-16
UY38971A (es) 2021-06-30
TWI815061B (zh) 2023-09-11
TWI867822B (zh) 2024-12-21
MX2022006281A (es) 2022-06-08
CN114728167A (zh) 2022-07-08
US11512097B2 (en) 2022-11-29
CR20220308A (es) 2022-08-04
CL2023002486A1 (es) 2024-01-12
CA3162281A1 (en) 2021-06-03
IL293191B1 (en) 2025-05-01
KR20220106159A (ko) 2022-07-28
PE20231097A1 (es) 2023-07-18

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