TW201605859A - 作為酪蛋白激酶１δ／ε抑制劑之新穎經取代之吡唑并－哌 - Google Patents

作為酪蛋白激酶１δ／ε抑制劑之新穎經取代之吡唑并－哌 Download PDF

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TW201605859A
TW201605859A TW103139448A TW103139448A TW201605859A TW 201605859 A TW201605859 A TW 201605859A TW 103139448 A TW103139448 A TW 103139448A TW 103139448 A TW103139448 A TW 103139448A TW 201605859 A TW201605859 A TW 201605859A
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TW103139448A
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阿潘德 維拉帕斯
奇坦 帕達美克 達尼
佩尹 劉
馬克Ｄ 瓦特曼
布萊德利Ｃ 皮爾斯
艾瑞卡 雅羅喬
畢瑞斯渥 達斯古塔
加拉斯 蘇瑞德瑞 奈爾
沙克希 庫馬瑞 賈納卡瑞曼
錢德雷席克爾 瑞迪 瑞加瑞迪
麥圖 馬立卡吉那 萊歐
奧爾 莫希 塞爾凡 蘇比哈 卡路琵雅
班迪瑞迪 索巴 瑞迪
波里奇拉 那嘉拉許彌
拉傑許 歐卡德斯 寶拉
席帕 荷利哈提 馬赫斯瓦倫帕
庫瑪拉佛 沙瓦庫瑪
迪巴卡 穆立克
拉米許 西斯特拉
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必治妥美雅史谷比公司
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Publication of TW201605859A publication Critical patent/TW201605859A/zh

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D487/10—Spiro-condensed systems
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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
    • C07D491/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW103139448A 2013-11-14 2014-11-13 作為酪蛋白激酶１δ／ε抑制劑之新穎經取代之吡唑并－哌 TW201605859A (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361904116P 2013-11-14 2013-11-14

Publications (1)

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TW201605859A true TW201605859A (zh) 2016-02-16

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TW103139448A TW201605859A (zh) 2013-11-14 2014-11-13 作為酪蛋白激酶１δ／ε抑制劑之新穎經取代之吡唑并－哌

Country Status (9)

Country Link
US (3) US9273058B2 (https=)
EP (2) EP3068784B1 (https=)
JP (2) JP6494624B2 (https=)
CN (2) CN105916856B (https=)
AR (1) AR098414A1 (https=)
ES (2) ES2718218T3 (https=)
TW (1) TW201605859A (https=)
UY (1) UY35834A (https=)
WO (2) WO2015073763A1 (https=)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR098414A1 (es) 2013-11-14 2016-05-26 Bristol Myers Squibb Co PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e
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
MA41338B1 (fr) * 2015-01-16 2019-07-31 Hoffmann La Roche Composés de pyrazine pour le traitement de maladies infectieuses
JP6904970B2 (ja) 2016-03-07 2021-07-21 エナンタ ファーマシューティカルズ インコーポレイテッド Ｂ型肝炎抗ウイルス剤
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
EP3458455B1 (en) * 2016-05-20 2021-06-16 F. Hoffmann-La Roche AG Novel pyrazine compounds with oxygen, sulfur and nitrogen linker for the treatment of infectious diseases
EP3481835A4 (en) 2016-07-05 2020-02-26 Blade Therapeutics, Inc. CALPAIN MODULATORS AND THERAPEUTIC USE THEREOF
EP3484886B1 (en) * 2016-07-14 2020-03-04 Hoffmann-La Roche AG 6,7-dihydro-4h-pyrazolo[1,5-a]pyrazine and 6,7-dihydro-4h-triazolo[1,5-a]pyrazine compounds for the treatment of infectious diseases
BR112019006110A2 (pt) 2016-09-28 2019-09-10 Blade Therapeutics Inc moduladores de calpaína e usos terapêuticos dos mesmos
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
CA3070004A1 (en) 2017-07-27 2019-01-31 Jiangsu Hengrui Medicine Co., Ltd. Piperazine heteroaryl derivative, preparation method therefor and use of same in medicine
US10952978B2 (en) 2017-08-28 2021-03-23 Enanta Pharmaceuticals, Inc. Hepatitis B antiviral agents
US11292791B2 (en) 2017-09-15 2022-04-05 Forma Therapeutics, Inc. Tetrahydro-imidazo quinoline compositions as CBP/P300 inhibitors
PE20201170A1 (es) 2017-11-01 2020-10-28 Bristol Myers Squibb Co Compuestos biciclicos en puente como moduladores del receptor farnesoide x
US11058678B2 (en) 2018-01-22 2021-07-13 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
WO2019191166A1 (en) * 2018-03-29 2019-10-03 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
CN111484442B (zh) * 2018-06-01 2021-11-09 杭州阿诺生物医药科技有限公司 一种具有抗肿瘤活性的csf1r抑制剂中间体的制备方法
IL279734B2 (en) 2018-06-29 2024-11-01 Forma Therapeutics Inc Inhibiting creb binding protein (cbp)
UY38383A (es) 2018-09-21 2020-04-30 Enanta Pharm Inc Heterociclos funcionalizados como agentes antivirales
US11198693B2 (en) 2018-11-21 2021-12-14 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
CA3126334A1 (en) 2019-01-11 2020-07-16 Shionogi & Co., Ltd. Dihydropyrazolopyrazinone derivative having mgat2 inhibitory activity
AU2020210998A1 (en) * 2019-01-25 2021-09-16 Jiangsu Hengrui Medicine Co., Ltd. Crystal form of 1,2,3-triazolo(1,5-a)pyrazines derivative and preparation method for crystal form
CN111484497B (zh) * 2019-01-25 2021-07-02 江苏恒瑞医药股份有限公司 咪唑并[1,5-a]吡嗪类衍生物的可药用盐、晶型及其制备方法
CN111484498B (zh) * 2019-01-25 2021-05-14 江苏恒瑞医药股份有限公司 咪唑并[1,5-a]吡嗪类化合物的晶型及其制备方法
CA3128946A1 (en) 2019-02-07 2020-08-13 Bayer Aktiengesellschaft 3-amino-2-[2-(acylamino)pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one as csnk1 inhibitors
US12351577B2 (en) 2019-03-15 2025-07-08 Forma Therapeutics, Inc. Inhibiting cyclic AMP-responsive element-binding protein (CREB)
WO2020247444A1 (en) 2019-06-03 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
WO2020247561A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc, Hepatitis b antiviral agents
WO2020247575A1 (en) 2019-06-04 2020-12-10 Enanta Pharmaceuticals, Inc. Hepatitis b antiviral agents
US11738019B2 (en) 2019-07-11 2023-08-29 Enanta Pharmaceuticals, Inc. Substituted heterocycles as antiviral agents
US11236108B2 (en) 2019-09-17 2022-02-01 Enanta Pharmaceuticals, Inc. Functionalized heterocycles as antiviral agents
WO2021188414A1 (en) 2020-03-16 2021-09-23 Enanta Pharmaceuticals, Inc. Functionalized heterocyclic compounds as antiviral agents
WO2022023341A1 (en) 2020-07-29 2022-02-03 Bayer Aktiengesellschaft Substituted 1 h-pyrrolo[3,2-b]pyridin compounds and methods of use thereof
CN114057745A (zh) * 2020-07-29 2022-02-18 江苏恒瑞医药股份有限公司 一种三氮唑并[1,5-a]吡嗪制备方法及其应用
JP2023541465A (ja) * 2020-09-17 2023-10-02 ヤンセン ファーマシューティカ エヌ．ベー． カゼインキナーゼ１デルタモジュレーター
US11795168B2 (en) 2020-09-23 2023-10-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (CREB) binding protein (CBP)
US11801243B2 (en) 2020-09-23 2023-10-31 Forma Therapeutics, Inc. Bromodomain inhibitors for androgen receptor-driven cancers
WO2022166778A1 (zh) * 2021-02-04 2022-08-11 江苏恒瑞医药股份有限公司 一种衣壳蛋白抑制剂的药物组合物及其制备方法
EP4469457A4 (en) * 2022-01-27 2026-01-21 Broad Inst Inc CSNK1 SUBSTITUTE HETEROCYCLIC INHIBITORS
AU2023296166A1 (en) * 2022-06-13 2024-11-28 Shionogi & Co., Ltd. Crystal of dihydropyridinone derivative or solvate thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL160915A0 (en) * 2001-09-19 2004-08-31 Aventis Pharma Sa Indolizines inhibiting kinase proteins
DE602004020685D1 (de) * 2003-12-11 2009-05-28 Aventis Pharma Inc Substituierte 1h-pyrroloä3,2-b, 3,2-c und 2,3-cüpyridin-2-carbonsäureamide und verwandte analoga als inhibitoren von caseinkinase-i-epsilon
US20050222171A1 (en) * 2004-01-22 2005-10-06 Guido Bold Organic compounds
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
CN101417999A (zh) 2007-10-25 2009-04-29 上海恒瑞医药有限公司 哌嗪类衍生物,其制备方法及其在医药上的应用
EP2085398A1 (en) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, a process for their preparation and their use as medicine
CN102223798A (zh) 2008-09-24 2011-10-19 巴斯夫欧洲公司 用于防治无脊椎动物害虫的吡唑化合物
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
WO2010059836A1 (en) 2008-11-20 2010-05-27 Decode Genetics Ehf Substituted aza-bridged bicyclics for cardiovascular and cns disease
TW201035102A (en) 2009-03-04 2010-10-01 Gruenethal Gmbh Sulfonylated tetrahydroazolopyrazines and their use as medicinal products
FR2960876B1 (fr) * 2010-06-03 2012-07-27 Sanofi Aventis Derives de 3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide leur preparation et leur application en therapeutique.
CN102372716A (zh) 2010-08-09 2012-03-14 江苏恒瑞医药股份有限公司 酞嗪酮类衍生物、其制备方法及其在医药上的应用
US9226929B2 (en) 2011-03-02 2016-01-05 Bayer Intellectual Property Gmbh Pharmaceutically active disubstituted triazine derivatives
AR098414A1 (es) 2013-11-14 2016-05-26 Bristol Myers Squibb Co PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e

Also Published As

Publication number Publication date
CN105916856A (zh) 2016-08-31
UY35834A (es) 2015-05-29
CN105916855A (zh) 2016-08-31
US9598423B2 (en) 2017-03-21
JP6494622B2 (ja) 2019-04-03
EP3068785B1 (en) 2019-06-26
JP2016537366A (ja) 2016-12-01
CN105916856B (zh) 2018-09-25
JP6494624B2 (ja) 2019-04-03
US20160122358A1 (en) 2016-05-05
EP3068784A1 (en) 2016-09-21
EP3068785A1 (en) 2016-09-21
AR098414A1 (es) 2016-05-26
US20150133428A1 (en) 2015-05-14
US9273058B2 (en) 2016-03-01
WO2015073767A1 (en) 2015-05-21
WO2015073763A1 (en) 2015-05-21
US20160311824A1 (en) 2016-10-27
ES2744636T3 (es) 2020-02-25
CN105916855B (zh) 2019-03-15
JP2016537369A (ja) 2016-12-01
EP3068784B1 (en) 2019-02-20
ES2718218T3 (es) 2019-06-28

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