WO2021185348A1 - Dérivé d'acrylamide substitué et composition et utilisation associée - Google Patents

Dérivé d'acrylamide substitué et composition et utilisation associée Download PDF

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Publication number
WO2021185348A1
WO2021185348A1 PCT/CN2021/081756 CN2021081756W WO2021185348A1 WO 2021185348 A1 WO2021185348 A1 WO 2021185348A1 CN 2021081756 W CN2021081756 W CN 2021081756W WO 2021185348 A1 WO2021185348 A1 WO 2021185348A1
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WO
WIPO (PCT)
Prior art keywords
alkyl
halogen
optionally substituted
group
haloalkyl
Prior art date
Application number
PCT/CN2021/081756
Other languages
English (en)
Chinese (zh)
Inventor
王义汉
赵九洋
邢青峰
李焕银
艾义新
Original Assignee
深圳市塔吉瑞生物医药有限公司
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 深圳市塔吉瑞生物医药有限公司 filed Critical 深圳市塔吉瑞生物医药有限公司
Publication of WO2021185348A1 publication Critical patent/WO2021185348A1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • 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

Abstract

L'invention concerne un dérivé d'acrylamide substitué, une composition comprenant ledit composé, et une utilisation associée. Le dérivé d'acrylamide substitué est un composé représenté par la formule (I), ou un tautomère, un stéréoisomère, un promédicament, une forme cristalline, un sel, un hydrate ou un solvate pharmaceutiquement acceptable de celui-ci. Le composé et la composition associée peuvent être utilisés pour préparer un médicament pour le traitement et/ou la prévention de tumeurs médiées par l'EGFR et/ou l'HER2 kinase sauvages et/ou mutants.
PCT/CN2021/081756 2020-03-20 2021-03-19 Dérivé d'acrylamide substitué et composition et utilisation associée WO2021185348A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN202010200352.7 2020-03-20
CN202010200352 2020-03-20

Publications (1)

Publication Number Publication Date
WO2021185348A1 true WO2021185348A1 (fr) 2021-09-23

Family

ID=77770496

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2021/081756 WO2021185348A1 (fr) 2020-03-20 2021-03-19 Dérivé d'acrylamide substitué et composition et utilisation associée

Country Status (2)

Country Link
CN (1) CN113493439B (fr)
WO (1) WO2021185348A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010065898A2 (fr) * 2008-12-05 2010-06-10 Principia Biopharma Inc. Inactivation d'egfr kinase par l'intermédiaire d'inhibiteurs améliorés par électrophilie
CN104854107A (zh) * 2012-11-15 2015-08-19 药品循环公司 作为激酶抑制剂的吡咯并嘧啶化合物
CN106928231A (zh) * 2015-12-31 2017-07-07 合肥中科普瑞昇生物医药科技有限公司 一类新型的egfr野生型和突变型的激酶抑制剂
CN109310671A (zh) * 2016-01-21 2019-02-05 淄博百极常生制药有限公司 布鲁顿酪氨酸激酶抑制剂

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201718572A (zh) * 2015-06-24 2017-06-01 普林斯匹亞生物製藥公司 酪胺酸激酶抑制劑
JP6737952B2 (ja) * 2016-08-17 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Ｓｈｅｎｚｈｅｎ ＴａｒｇｅｔＲｘ，Ｉｎｃ． チロシンキナーゼ活性を阻害するための縮合二環式化合物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010065898A2 (fr) * 2008-12-05 2010-06-10 Principia Biopharma Inc. Inactivation d'egfr kinase par l'intermédiaire d'inhibiteurs améliorés par électrophilie
CN104854107A (zh) * 2012-11-15 2015-08-19 药品循环公司 作为激酶抑制剂的吡咯并嘧啶化合物
CN106928231A (zh) * 2015-12-31 2017-07-07 合肥中科普瑞昇生物医药科技有限公司 一类新型的egfr野生型和突变型的激酶抑制剂
CN109310671A (zh) * 2016-01-21 2019-02-05 淄博百极常生制药有限公司 布鲁顿酪氨酸激酶抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
WANG, AOLI ET AL.: "Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2- ylmethoxy)phenyl)-lH-pyrazolo[3, 4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode", JOURNAL OF MEDICINAL CHEMISTRY, vol. 60, no. 7, 10 March 2017 (2017-03-10), pages 2944 - 2962, XP055405186, DOI: 10.1021/acs.jmedchem.6b01907 *

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CN113493439B (zh) 2022-10-14
CN113493439A (zh) 2021-10-12

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