WO2018001084A1 - Inhibiteur de protéine de choc thermique, son procédé de fabrication et son application - Google Patents

Inhibiteur de protéine de choc thermique, son procédé de fabrication et son application Download PDF

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Publication number
WO2018001084A1
WO2018001084A1 PCT/CN2017/088019 CN2017088019W WO2018001084A1 WO 2018001084 A1 WO2018001084 A1 WO 2018001084A1 CN 2017088019 W CN2017088019 W CN 2017088019W WO 2018001084 A1 WO2018001084 A1 WO 2018001084A1
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WO
WIPO (PCT)
Prior art keywords
group
compound
alkyl
heat shock
shock protein
Prior art date
Application number
PCT/CN2017/088019
Other languages
English (en)
Chinese (zh)
Inventor
张健存
林财
李德耀
邹晴安
张袁超
顾自强
Original Assignee
广州市恒诺康医药科技有限公司
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 广州市恒诺康医药科技有限公司 filed Critical 广州市恒诺康医药科技有限公司
Publication of WO2018001084A1 publication Critical patent/WO2018001084A1/fr

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Classifications

    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/42—Oxazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

La présente invention concerne le domaine de la chimie pharmaceutique. L'invention porte sur un inhibiteur de protéine de choc thermique, sur son procédé de fabrication et sur son application. L'inhibiteur de protéine de choc thermique a une structure caractéristique représentée par la formule I. Le composé peut inhiber une activité de la protéine de choc thermique 90 et peut être utilisé pour préparer un produit pharmaceutique antitumoral.
PCT/CN2017/088019 2016-06-29 2017-06-13 Inhibiteur de protéine de choc thermique, son procédé de fabrication et son application WO2018001084A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201610509310.5A CN107540624B (zh) 2016-06-29 2016-06-29 热休克蛋白抑制剂及其制备方法和应用
CN201610509310.5 2016-06-29

Publications (1)

Publication Number Publication Date
WO2018001084A1 true WO2018001084A1 (fr) 2018-01-04

Family

ID=60785913

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2017/088019 WO2018001084A1 (fr) 2016-06-29 2017-06-13 Inhibiteur de protéine de choc thermique, son procédé de fabrication et son application

Country Status (2)

Country Link
CN (1) CN107540624B (fr)
WO (1) WO2018001084A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116284202A (zh) * 2023-03-28 2023-06-23 华侨大学 白桦脂酸的PROTACs化合物及其制备方法和应用

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113087658B (zh) * 2021-04-06 2022-05-17 北京大学深圳研究生院 具有热休克热蛋白70抑制活性的化合物及其应用

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072051A1 (fr) * 2003-02-11 2004-08-26 Vernalis (Cambridge) Limited Composes d'isoxazole utiles comme inhibiteurs des proteines de choc thermique
WO2007096194A1 (fr) * 2006-02-27 2007-08-30 Novartis Ag Dérivés radiomarqués d'isoxazole pouvant être employés dans le marquage et le diagnostic de la fonctionnalité de hsp90
WO2008097640A2 (fr) * 2007-02-08 2008-08-14 Synta Pharmaceuticals Corp. Composés à base de triazole modulant l'activité de hsp90
WO2010017545A2 (fr) * 2008-08-08 2010-02-11 Synta Pharamceuticals Corp. Composés de triazole qui modulent l'activité hsp90
WO2012084602A1 (fr) * 2010-12-20 2012-06-28 Sigma-Tau Research Switzerland S.A. Composés aryl triazole ayant une activité anti-tumorale
CN106349180A (zh) * 2015-07-14 2017-01-25 上海翰森生物医药科技有限公司 4,5‑二苯基异噁唑衍生物及其制备方法和应用
CN106349233A (zh) * 2015-07-15 2017-01-25 上海翰森生物医药科技有限公司 3,4‑二苯基‑4h‑1,2,4‑三唑衍生物及其制备方法和应用

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072051A1 (fr) * 2003-02-11 2004-08-26 Vernalis (Cambridge) Limited Composes d'isoxazole utiles comme inhibiteurs des proteines de choc thermique
WO2007096194A1 (fr) * 2006-02-27 2007-08-30 Novartis Ag Dérivés radiomarqués d'isoxazole pouvant être employés dans le marquage et le diagnostic de la fonctionnalité de hsp90
WO2008097640A2 (fr) * 2007-02-08 2008-08-14 Synta Pharmaceuticals Corp. Composés à base de triazole modulant l'activité de hsp90
WO2010017545A2 (fr) * 2008-08-08 2010-02-11 Synta Pharamceuticals Corp. Composés de triazole qui modulent l'activité hsp90
WO2012084602A1 (fr) * 2010-12-20 2012-06-28 Sigma-Tau Research Switzerland S.A. Composés aryl triazole ayant une activité anti-tumorale
CN106349180A (zh) * 2015-07-14 2017-01-25 上海翰森生物医药科技有限公司 4,5‑二苯基异噁唑衍生物及其制备方法和应用
CN106349233A (zh) * 2015-07-15 2017-01-25 上海翰森生物医药科技有限公司 3,4‑二苯基‑4h‑1,2,4‑三唑衍生物及其制备方法和应用

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BROUGH PAUL A. ET AL.: "4, 5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer", J. MED. CHEM., vol. 51, no. 2, 20 November 2007 (2007-11-20), pages 196 - 218, XP002506225, ISSN: 0022-2623 *
TADDEI MAURIZIO ET AL.: "Synthesis and Evaluation of New Hsp90 Inhibitors Based on a 1, 4, 5-Trisubstituted 1, 2, 3-Triazole Scaffold", J. MED. CHEM., vol. 57, no. 6, 3 March 2014 (2014-03-03), pages 2258 - 2274, XP055226908, ISSN: 0022-2623 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116284202A (zh) * 2023-03-28 2023-06-23 华侨大学 白桦脂酸的PROTACs化合物及其制备方法和应用

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Publication number Publication date
CN107540624B (zh) 2020-06-16
CN107540624A (zh) 2018-01-05

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