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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BR
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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    • 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
    • AHUMAN NECESSITIES
    • 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
    • AHUMAN NECESSITIES
    • 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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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Engineering & Computer Science (AREA)
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  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
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  • Communicable Diseases (AREA)
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  • Urology & Nephrology (AREA)
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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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CA3112322A1 (en) 2018-09-29 2020-04-02 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2
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WO2022006780A1 (en) * 2020-07-08 2022-01-13 Novartis Ag Manufacture of compounds and compositions for inhibiting activity of shp2
WO2022060583A1 (en) 2020-09-03 2022-03-24 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
US11690915B2 (en) 2020-09-15 2023-07-04 Revolution Medicines, Inc. Ras inhibitors
AR125782A1 (es) 2021-05-05 2023-08-16 Revolution Medicines Inc Inhibidores de ras
AU2022271243A1 (en) * 2021-05-05 2023-11-30 Huyabio International, Llc Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
EP4333850A1 (en) * 2021-05-05 2024-03-13 Huyabio International, LLC Shp2 inhibitor monotherapy and uses thereof
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
WO2022235815A1 (en) * 2021-05-05 2022-11-10 Huabio International, Llc Combination therapies comprising shp2 inhibitors and egfr tyrosine kinase inhibitors
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ras阻害剤及びその使用
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WO2023122938A1 (en) * 2021-12-28 2023-07-06 Js Innomed Holdings Ltd. Heterocyclic compounds as shp2 inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
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Also Published As

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

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