JOP20220125A1 - مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها - Google Patents

مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها

Info

Publication number
JOP20220125A1
JOP20220125A1 JOP/2022/0125A JOP20220125A JOP20220125A1 JO P20220125 A1 JOP20220125 A1 JO P20220125A1 JO P20220125 A JOP20220125 A JO P20220125A JO P20220125 A1 JOP20220125 A1 JO P20220125A1
Authority
JO
Jordan
Prior art keywords
compounds
delta
methods
heterocyclic compounds
desaturase inhibitors
Prior art date
Application number
JOP/2022/0125A
Other languages
English (en)
Inventor
Jennifer R Allen
Michela Beltrani
Matthew P Bourbeau
Teodora P Damyanova
Paolo Vincetti
Iain Lingard
Ana E Minatti
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of JOP20220125A1 publication Critical patent/JOP20220125A1/ar

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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)

Abstract

: يتعلق الاختراع الحالي بمركبات مفيدة لتثبيط دلتا-5 ديساتوراز ("D5D"). يكون للمركبات صيغة عامة I: I حيث يتم تعريف المتغيرات بالصيغة I في هذه الوثيقة. يقدم هذا الكشف أيضاً تركيبات صيدلانية تشتمل على المركبات، استخدامات المركبات، وتركيبات لمعالجة، على سبيل المثال، اضطراب أيضي أو قلبي وعائي. علاوة على ذلك، يوفر الكشف مركبات وسيطة مفيدة في تخليق المركبات بالصيغة I.
JOP/2022/0125A 2019-11-25 2020-11-24 مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها JOP20220125A1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962939821P 2019-11-25 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 (1)

Publication Number Publication Date
JOP20220125A1 true JOP20220125A1 (ar) 2023-01-30

Family

ID=73855555

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2022/0125A JOP20220125A1 (ar) 2019-11-25 2020-11-24 مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها

Country Status (19)

Country Link
US (3) US11512097B2 (ar)
EP (1) EP4065223A1 (ar)
JP (2) JP7254246B2 (ar)
KR (2) KR20230154292A (ar)
CN (2) CN118161500A (ar)
AR (1) AR120556A1 (ar)
AU (1) AU2020392087A1 (ar)
BR (1) BR112022010054A2 (ar)
CA (1) CA3162281A1 (ar)
CL (2) CL2022001357A1 (ar)
CO (1) CO2022008690A2 (ar)
CR (1) CR20220308A (ar)
IL (1) IL293191A (ar)
JO (1) JOP20220125A1 (ar)
MX (1) MX2022006281A (ar)
PE (1) PE20231097A1 (ar)
TW (2) TW202409042A (ar)
UY (1) UY38971A (ar)
WO (1) WO2021108408A1 (ar)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL293191A (en) 2019-11-25 2022-07-01 Amgen Inc Heterocyclic compounds as delta-5 desaturase inhibitors and methods of use
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
WO2024112763A1 (en) 2022-11-23 2024-05-30 Amgen Inc. Selection of patients for the treatment of fads1-mediated diseases or disorders using fads-1 inhibitors

Family Cites Families (47)

* 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
ES2058069T3 (es) 1986-04-07 1994-11-01 Kumiai Chemical Industry Co Derivados de 5h-1,3,4-tiadiazolo-(3,2-a)-pirimidin-5-ona y nuevo compuesto fungicida agricola-horticola que contiene dicho derivado.
BR9713863A (pt) 1996-12-05 2000-03-14 Amgen Inc Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, processos de profilaxia ou tratamento, para abaixar as concentrações no plasma, para diminuir a produção de prostaglandinas, e, para diminuir a atividade de enzima ciclooxigenase
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
JP2003512379A (ja) 1999-10-15 2003-04-02 ニューロクライン バイオサイエンシーズ， インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法
WO2003106435A1 (en) 2002-06-18 2003-12-24 Sankyo Company, Limited 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
US20050222171A1 (en) 2004-01-22 2005-10-06 Guido Bold Organic compounds
PE20051089A1 (es) 2004-01-22 2006-01-25 Novartis Ag Derivados de pirazolo [1,5-a] pirimidin-7-il-amina como inhibidores de quinasa de proteina
ATE474829T1 (de) 2005-06-27 2010-08-15 Amgen Inc Entzündungshemmende arylnitrilverbindungen
WO2007027012A1 (en) 2005-07-18 2007-03-08 Samsung Electronics Co., Ltd. Video coding method and apparatus for reducing mismatch between encoder and decoder
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
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
JP5152922B2 (ja) 2005-10-06 2013-02-27 メルク・シャープ・アンド・ドーム・コーポレーション プロテインキナーゼを阻害するためのピラゾロ［１，５−ａ］ピリミジン誘導体の使用およびプロテインキナーゼを阻害する方法
MX2009002995A (es) 2006-09-28 2009-04-01 Novartis Ag Derivados de pirazolo-[1,5-a]-pirimidina y su uso terapeutico.
US8173661B2 (en) 2006-11-08 2012-05-08 The Rockefeller University Alpha-IIB-beta-3 inhibitors and uses thereof
WO2008089310A2 (en) 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of obesity
US20080194557A1 (en) 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
UA96178C2 (ru) 2007-01-19 2011-10-10 Басф Се Фунгицидная смесь, средство на ее основе, способ получения средства, способ борьбы с фитопатогенными грибами и посевной материал
WO2008092836A2 (en) 2007-01-30 2008-08-07 Basf Se Method for improving plant health
BRPI0809045A2 (pt) 2007-03-23 2014-09-02 Basf Se Combinações de substância ativa, uso de combinações de substância ativa, métodos para combater fungos fitopatogênicos indesejáveis, para preparar agentes pesticidas, e para tratar sementes, e, produto de revestimento de semente
US8642660B2 (en) 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan of eukaryotic organisms
EP2274308A1 (en) * 2008-04-04 2011-01-19 Gilead Sciences, Inc. Pyrrolotriazinone derivatives for use as stearoyl coa desaturase inhibitors
US8119647B2 (en) 2008-04-23 2012-02-21 Glenmark Pharmaceuticals S.A. Fused pyrimidineone compounds as TRPV3 modulators
US20100190747A1 (en) 2009-01-27 2010-07-29 Hideo Suzuki Fused ring compound and use thereof
RS53494B9 (sr) 2009-06-29 2020-11-30 Incyte Holdings Corp Pirimidinoni kao inhibitori pi3k
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
JPWO2012011592A1 (ja) 2010-07-23 2013-09-09 武田薬品工業株式会社 複素環化合物およびその用途
WO2012125629A1 (en) 2011-03-14 2012-09-20 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
WO2014139326A1 (en) 2013-03-13 2014-09-18 Genentech, Inc. Pyrazolo compounds and uses thereof
KR20160049003A (ko) 2013-09-05 2016-05-04 제넨테크, 인크. 항증식성 화합물
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
BR112016024455B1 (pt) 2014-04-23 2023-02-07 Mitsubishi Tanabe Pharma Corporation Composto heterocíclico bicíclico ou tricíclico
WO2016183063A1 (en) 2015-05-11 2016-11-17 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
US11414385B2 (en) 2015-12-21 2022-08-16 The University Of Chicago Compounds and methods for treating, detecting, and identifying compounds to treat apicomplexan parasitic diseases
WO2018039972A1 (en) * 2016-08-31 2018-03-08 Agios Pharmaceuticals, Inc. Inhibitors of cellular metabolic processes
EP3507290A1 (en) 2016-08-31 2019-07-10 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
US20200360381A1 (en) 2017-05-15 2020-11-19 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
PE20210340A1 (es) 2017-09-15 2021-02-22 Aduro Biotech Inc Compuestos que contienen pirazolopirimidinona y sus usos
IL293191A (en) 2019-11-25 2022-07-01 Amgen Inc Heterocyclic compounds as delta-5 desaturase inhibitors and methods of use

Also Published As

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

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