JP7608166B2 - Mgat2阻害活性を有するジヒドロピラゾロピラジノン誘導体 - Google Patents

Mgat2阻害活性を有するジヒドロピラゾロピラジノン誘導体 Download PDF

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JP7608166B2
JP7608166B2 JP2020565216A JP2020565216A JP7608166B2 JP 7608166 B2 JP7608166 B2 JP 7608166B2 JP 2020565216 A JP2020565216 A JP 2020565216A JP 2020565216 A JP2020565216 A JP 2020565216A JP 7608166 B2 JP7608166 B2 JP 7608166B2
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JPWO2020145369A1 (ja
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佑介 舘野
学 加藤
俊博 和田
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Shionogi and Co Ltd
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    • 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
    • C07D487/10Spiro-condensed systems
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/499Spiro-condensed pyrazines or piperazines
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
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  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020565216A 2019-01-11 2020-01-10 Mgat2阻害活性を有するジヒドロピラゾロピラジノン誘導体 Active JP7608166B2 (ja)

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JP2019003073 2019-01-11
JP2019003073 2019-01-11
PCT/JP2020/000553 WO2020145369A1 (ja) 2019-01-11 2020-01-10 Mgat2阻害活性を有するジヒドロピラゾロピラジノン誘導体

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US (1) US12227509B2 (https=)
EP (1) EP3909583A4 (https=)
JP (1) JP7608166B2 (https=)
KR (1) KR20210114001A (https=)
CN (2) CN119409703A (https=)
AU (1) AU2020207716A1 (https=)
BR (1) BR112021012428A2 (https=)
CA (1) CA3126334A1 (https=)
MX (1) MX2021008050A (https=)
TW (1) TWI840489B (https=)
WO (1) WO2020145369A1 (https=)

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JP2022016394A (ja) * 2020-07-10 2022-01-21 塩野義製薬株式会社 Mgat2阻害活性を有するジヒドロピラゾロピラジノン誘導体を含有する医薬組成物
WO2023038039A1 (ja) 2021-09-08 2023-03-16 塩野義製薬株式会社 抗肥満作用の関与する疾患の予防及び治療用医薬
WO2026008045A1 (zh) * 2024-07-04 2026-01-08 苏州信诺维医药科技股份有限公司 一种含有炔基的螺环化合物及其用途

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007117180A1 (fr) 2006-04-12 2007-10-18 'chemical Diversity Research Institute' Ltd. Bibliothèques combinatoire et focalisée d'azahétérocycles, composition pharmaceutique et procédés de leur fabrication
JP2017508779A (ja) 2014-03-27 2017-03-30 ヤンセン ファーマシューティカ エヌ.ベー. ROS1阻害剤としての置換4,5,6,7−テトラヒドロ−ピラゾロ[1,5−α]ピラジン誘導体および5,6,7,8−テトラヒドロ−4H−ピラゾロ[1,5−α][1,4]ジアゼピン誘導体
WO2017069224A1 (ja) 2015-10-22 2017-04-27 塩野義製薬株式会社 Mgat2阻害活性を有するスピロ環誘導体
JP2017151579A (ja) 2016-02-23 2017-08-31 ブラザー工業株式会社 プログラム
JP2018052818A (ja) 2015-01-28 2018-04-05 武田薬品工業株式会社 スルホンアミド化合物

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1747949A (zh) 2002-12-20 2006-03-15 法马西亚公司 无环吡唑化合物
US8232282B2 (en) 2006-09-28 2012-07-31 Dainippon Sumitomo Pharma Co., Ltd. Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the same
AU2007342368A1 (en) 2007-01-04 2008-07-17 Merck & Co., Inc. Bicyclic spiropiperidine beta-secretase inhibitors for the treatment of Alzheimer's disease
US8389533B2 (en) 2008-04-07 2013-03-05 Amgen Inc. Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors
US20110275647A1 (en) 2009-02-23 2011-11-10 Msd K.K. Pyrimidin-4-(3h)-one derivatives
KR20100097077A (ko) 2009-02-25 2010-09-02 주식회사 중외제약 Hsp90에 대한 억제 효능을 갖는 피리디논 유도체
SG181857A1 (en) 2009-12-23 2012-07-30 Takeda Pharmaceutical Fused heteroaromatic pyrrolidinones as syk inhibitors
JP2014051434A (ja) 2010-12-28 2014-03-20 Dainippon Sumitomo Pharma Co Ltd 二環性ピリミジン誘導体
JP5853033B2 (ja) 2011-03-01 2016-02-09 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap β−セクレターゼ(BACE)の阻害剤として有用な6,7−ジヒドロ−ピラゾロ[1,5−a]ピラジン−4−イルアミン誘導体
WO2012124744A1 (ja) 2011-03-14 2012-09-20 大正製薬株式会社 含窒素縮合複素環化合物
JP6042060B2 (ja) 2011-09-26 2016-12-14 サノフイ ピラゾロキノリノン誘導体、その調製および治療上の使用
PT2573073E (pt) 2011-09-26 2015-02-05 Sanofi Sa Derivados de pirazoloquinolinona, sua preparação e sua utilização terapêutica
CN103012397B (zh) 2011-09-26 2017-03-01 赛诺菲 吡唑并喹啉酮衍生物、其制备方法及其治疗用途
US8791091B2 (en) 2011-12-02 2014-07-29 Bristol-Myers Squibb Company Aryl dihydropyridinone and piperidinone MGAT2 inhibitors
US9073856B2 (en) 2012-01-23 2015-07-07 Eli Lilly And Company Phenyl methanesulfonamide derivatives useful as MGAT-2 inhibitors
AR089771A1 (es) 2012-01-31 2014-09-17 Lilly Co Eli Derivados de bencil sulfonamida utiles como inhibidores de mogat-2
JP5852269B2 (ja) 2012-01-31 2016-02-03 イーライ リリー アンド カンパニー Mogat−2阻害剤として有用な新規モルホリニル誘導体
US9394297B2 (en) 2012-02-28 2016-07-19 Amgen Inc. Amides as pim inhibitors
EP2855483B1 (en) 2012-05-24 2017-10-25 Novartis AG Pyrrolopyrrolidinone compounds
JP2014005245A (ja) 2012-06-26 2014-01-16 Dainippon Sumitomo Pharma Co Ltd 二環性ピリミジン誘導体を含有する医薬組成物
JP2014009165A (ja) 2012-06-27 2014-01-20 Dainippon Sumitomo Pharma Co Ltd 二環性ピリミジン化合物
EP2903985A1 (en) 2012-10-03 2015-08-12 Advinus Therapeutics Limited Spirocyclic compounds, compositions and medicinal applications thereof
MX2015005739A (es) 2012-11-06 2015-09-16 Lilly Co Eli Compuestos novedosos de bencil sulfonamida utiles como inhibidores de mogat-2.
WO2014133134A1 (ja) 2013-02-28 2014-09-04 味の素株式会社 新規テトラヒドロピリドピリミジノン誘導体
CA2907532A1 (en) 2013-03-25 2014-10-02 Sanofi Pyrazolonaphthyridinone derivatives as metap2 inhibitors (methionine aminopeptidase type-2)
CN104109160B (zh) 2013-04-17 2017-12-15 上海翰森生物医药科技有限公司 吡咯并n杂环类化合物及其制备方法和医药用途
SG11201509070YA (en) 2013-05-29 2015-12-30 Bristol Myers Squibb Co Dihydropyridinone mgat2 inhibitors
AR098414A1 (es) 2013-11-14 2016-05-26 Bristol Myers Squibb Co PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e
WO2015112465A1 (en) 2014-01-24 2015-07-30 Merck Sharp & Dohme Corp. Isoquinoline derivatives as mgat2 inhibitors
EP3097095A1 (en) 2014-01-24 2016-11-30 AbbVie Inc. Furo-3-carboxamide derivatives and methods of use
JP6513075B2 (ja) 2014-02-27 2019-05-15 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縮合ピラゾール誘導体
JP2017078024A (ja) 2014-02-28 2017-04-27 味の素株式会社 新規テトラヒドロピリドピリミジノン誘導体
SMT201900256T1 (it) 2014-03-07 2019-07-11 Bristol Myers Squibb Co Inibitori dell'mgat2 diidropiridinonici sostituiti con tetrazolone
SG11201607392SA (en) 2014-03-07 2016-10-28 Bristol Myers Squibb Co Dihydropyridinone mgat2 inhibitors for use in the treatment of metabolic disorders
WO2015191681A2 (en) 2014-06-11 2015-12-17 Bristol-Myers Squibb Company Substituted pyridinones as mgat2 inhibitors
JP2017171579A (ja) * 2014-08-11 2017-09-28 味の素株式会社 新規テトラヒドロピリドピリミジノン誘導体
CN107205993B (zh) 2014-12-06 2021-03-09 细胞内治疗公司 有机化合物
WO2016106009A1 (en) 2014-12-22 2016-06-30 Eli Lilly And Company Erk inhibitors
JP2016164154A (ja) 2015-02-26 2016-09-08 塩野義製薬株式会社 オートタキシン阻害活性を有する7位無置換縮合ピラゾール誘導体
US10335401B2 (en) * 2015-12-21 2019-07-02 Shionogi & Co., Ltd. Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity
JP2020158390A (ja) * 2017-06-20 2020-10-01 塩野義製薬株式会社 Mgat2阻害活性を有する非芳香族複素環誘導体およびそれらを含有する医薬組成物
TWI782056B (zh) * 2017-07-14 2022-11-01 日商鹽野義製藥股份有限公司 具有mgat2抑制活性的縮合環衍生物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007117180A1 (fr) 2006-04-12 2007-10-18 'chemical Diversity Research Institute' Ltd. Bibliothèques combinatoire et focalisée d'azahétérocycles, composition pharmaceutique et procédés de leur fabrication
JP2017508779A (ja) 2014-03-27 2017-03-30 ヤンセン ファーマシューティカ エヌ.ベー. ROS1阻害剤としての置換4,5,6,7−テトラヒドロ−ピラゾロ[1,5−α]ピラジン誘導体および5,6,7,8−テトラヒドロ−4H−ピラゾロ[1,5−α][1,4]ジアゼピン誘導体
JP2018052818A (ja) 2015-01-28 2018-04-05 武田薬品工業株式会社 スルホンアミド化合物
WO2017069224A1 (ja) 2015-10-22 2017-04-27 塩野義製薬株式会社 Mgat2阻害活性を有するスピロ環誘導体
JP2017151579A (ja) 2016-02-23 2017-08-31 ブラザー工業株式会社 プログラム

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Medicinal Chemistry Letters,2008年,Vol. 18,pp. 721-725,DOI: 10.1016/j.bmcl.2007.11.049

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US20220135577A1 (en) 2022-05-05
TWI840489B (zh) 2024-05-01
EP3909583A1 (en) 2021-11-17
BR112021012428A2 (pt) 2021-09-08
KR20210114001A (ko) 2021-09-17
CA3126334A1 (en) 2020-07-16
TW202043235A (zh) 2020-12-01
WO2020145369A1 (ja) 2020-07-16
MX2021008050A (es) 2021-08-05
CN119409703A (zh) 2025-02-11
EP3909583A4 (en) 2022-08-17
AU2020207716A1 (en) 2021-07-15
JPWO2020145369A1 (ja) 2021-11-25
US12227509B2 (en) 2025-02-18
CN113557021A (zh) 2021-10-26

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