BR112021017495A2 - Derivado de pirazina e sua aplicação na inibição de shp2 - Google Patents

Derivado de pirazina e sua aplicação na inibição de shp2

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Publication number
BR112021017495A2
BR112021017495A2 BR112021017495A BR112021017495A BR112021017495A2 BR 112021017495 A2 BR112021017495 A2 BR 112021017495A2 BR 112021017495 A BR112021017495 A BR 112021017495A BR 112021017495 A BR112021017495 A BR 112021017495A BR 112021017495 A2 BR112021017495 A2 BR 112021017495A2
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Brazil
Prior art keywords
pyrazine derivative
application
shp2
inhibition
shp2 inhibition
Prior art date
Application number
BR112021017495A
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English (en)
Inventor
Haifeng Sun
Jinchang Lu
Kuifeng Wang
Mengnan Ma
Tao Zhang
Original Assignee
Suzhou Genhouse Pharmaceutical Co Ltd
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Publication date
Application filed by Suzhou Genhouse Pharmaceutical Co Ltd filed Critical Suzhou Genhouse Pharmaceutical Co Ltd
Publication of BR112021017495A2 publication Critical patent/BR112021017495A2/pt

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    • C07ORGANIC CHEMISTRY
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    • 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
    • C07D491/02Heterocyclic 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 two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • C07DHETEROCYCLIC COMPOUNDS
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Abstract

derivado de pirazina e sua aplicação na inibição de shp2. a presente invenção está relacionada a um derivado de pirazina, a uma aplicação deste na inibição de shp2 e a um composto de fórmula (i), ou sais farmaceuticamente aceitáveis, ésteres, isômeros, solvatos, pró-fármacos ou marcadores isotópicos deste. a estrutura do composto de fórmula (i) é como apresentada a seguir. o novo derivado de pirazina fornecido pela presente invenção possui excelente atividade de inibição de shp2 e pode ser usado para evitar e/ou tratar doenças ou distúrbios mediados ou dependentes de proteína tirosina quinase fosfatase não receptora.
BR112021017495A 2019-03-04 2020-03-02 Derivado de pirazina e sua aplicação na inibição de shp2 BR112021017495A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201910160960.7A CN111647000B (zh) 2019-03-04 2019-03-04 吡嗪类衍生物及其在抑制shp2中的应用
PCT/CN2020/077391 WO2020177653A1 (zh) 2019-03-04 2020-03-02 吡嗪类衍生物及其在抑制shp2中的应用

Publications (1)

Publication Number Publication Date
BR112021017495A2 true BR112021017495A2 (pt) 2021-12-14

Family

ID=72337672

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021017495A BR112021017495A2 (pt) 2019-03-04 2020-03-02 Derivado de pirazina e sua aplicação na inibição de shp2

Country Status (14)

Country Link
US (2) US20220127276A1 (pt)
EP (1) EP3936502A4 (pt)
JP (1) JP2022523786A (pt)
KR (1) KR20210135561A (pt)
CN (2) CN111647000B (pt)
AU (1) AU2020233038A1 (pt)
BR (1) BR112021017495A2 (pt)
CA (1) CA3132395A1 (pt)
CL (1) CL2021002308A1 (pt)
CO (1) CO2021013140A2 (pt)
IL (1) IL286069A (pt)
MX (1) MX2021010625A (pt)
SG (1) SG11202109603SA (pt)
WO (1) WO2020177653A1 (pt)

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AU2019346118B2 (en) 2018-09-29 2024-05-16 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of SHP2
WO2021257736A1 (en) 2020-06-18 2021-12-23 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
WO2022006780A1 (en) * 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting activity of shp2
IL301062A (en) 2020-09-03 2023-05-01 Revolution Medicines Inc Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
PE20231207A1 (es) 2020-09-15 2023-08-17 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer
AU2022271243A1 (en) * 2021-05-05 2023-11-30 Huyabio International, Llc Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
CN117500811A (zh) 2021-05-05 2024-02-02 锐新医药公司 共价ras抑制剂及其用途
WO2022235864A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors
EP4333850A1 (en) * 2021-05-05 2024-03-13 Huyabio International, LLC Shp2 inhibitor monotherapy and uses thereof
CA3217092A1 (en) * 2021-05-05 2022-11-10 Farbod Shojaei Combination therapies comprising shp2 inhibitors and egfr tyrosine kinase inhibitors
CN115340559A (zh) * 2021-05-12 2022-11-15 药雅科技(上海)有限公司 Shp2磷酸酶杂环类抑制剂的制备及其应用
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AU2022274936A1 (en) * 2021-05-13 2023-12-07 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Heterocyclic compound for inhibiting shp2 activity, preparation method therefor and use thereof
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TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途
WO2023031781A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
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WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
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CN115521305A (zh) * 2022-09-20 2022-12-27 中国药科大学 Shp2&nampt双靶向化合物及其药物组合物和用途
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JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
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Also Published As

Publication number Publication date
KR20210135561A (ko) 2021-11-15
WO2020177653A1 (zh) 2020-09-10
CN111647000A (zh) 2020-09-11
CN111647000B (zh) 2021-10-12
CL2021002308A1 (es) 2022-05-20
CN113474338A (zh) 2021-10-01
MX2021010625A (es) 2021-10-26
CO2021013140A2 (es) 2021-11-30
SG11202109603SA (en) 2021-10-28
US11827644B2 (en) 2023-11-28
AU2020233038A1 (en) 2021-10-21
EP3936502A1 (en) 2022-01-12
IL286069A (en) 2021-10-31
EP3936502A4 (en) 2023-02-15
CA3132395A1 (en) 2020-09-10
US20230227464A1 (en) 2023-07-20
JP2022523786A (ja) 2022-04-26
US20220127276A1 (en) 2022-04-28

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