IL277783B2 - Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations - Google Patents

Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations

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Publication number
IL277783B2
IL277783B2 IL277783A IL27778320A IL277783B2 IL 277783 B2 IL277783 B2 IL 277783B2 IL 277783 A IL277783 A IL 277783A IL 27778320 A IL27778320 A IL 27778320A IL 277783 B2 IL277783 B2 IL 277783B2
Authority
IL
Israel
Prior art keywords
allosteric
inhibitor
heterocyclyl
cancer
nrr
Prior art date
Application number
IL277783A
Other languages
English (en)
Hebrew (he)
Other versions
IL277783B1 (en
IL277783A (en
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Revolution Medicines Inc
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Filing date
Publication date
Application filed by Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of IL277783A publication Critical patent/IL277783A/en
Publication of IL277783B1 publication Critical patent/IL277783B1/en
Publication of IL277783B2 publication Critical patent/IL277783B2/en

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    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/4965Non-condensed pyrazines
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12QMEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00Oligonucleotides characterized by their use
    • C12Q2600/156Polymorphic or mutational markers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Wood Science & Technology (AREA)
  • Pathology (AREA)
  • Analytical Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Microbiology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Physics & Mathematics (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Peptides Or Proteins (AREA)
IL277783A 2018-04-10 2019-04-09 Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations IL277783B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862655648P 2018-04-10 2018-04-10
PCT/US2019/026543 WO2019199792A1 (en) 2018-04-10 2019-04-09 Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations

Publications (3)

Publication Number Publication Date
IL277783A IL277783A (en) 2020-11-30
IL277783B1 IL277783B1 (en) 2024-03-01
IL277783B2 true IL277783B2 (en) 2024-07-01

Family

ID=66248820

Family Applications (1)

Application Number Title Priority Date Filing Date
IL277783A IL277783B2 (en) 2018-04-10 2019-04-09 Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations

Country Status (14)

Country Link
US (1) US20210154190A1 (https=)
EP (1) EP3773590A1 (https=)
JP (1) JP2021521155A (https=)
KR (1) KR20200143417A (https=)
CN (1) CN112203689A (https=)
AU (1) AU2019251207A1 (https=)
BR (1) BR112020020743A2 (https=)
CA (1) CA3096535A1 (https=)
CO (1) CO2020012588A2 (https=)
IL (1) IL277783B2 (https=)
MX (1) MX2020010719A (https=)
SG (1) SG11202009793TA (https=)
TW (1) TW201946627A (https=)
WO (1) WO2019199792A1 (https=)

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AU2017274199B2 (en) 2016-05-31 2021-09-23 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
MX383856B (es) 2016-06-14 2025-03-14 Novartis Ag Compuestos y composiciones para inhibir la actividad de shp2.
KR102598895B1 (ko) 2016-07-12 2023-11-07 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
US11529347B2 (en) 2016-09-22 2022-12-20 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
MX2019008695A (es) 2017-01-23 2019-09-11 Revolution Medicines Inc Compuestos biciclicos como inhibidores alostericos de shp2.
MX2019008696A (es) 2017-01-23 2019-09-13 Revolution Medicines Inc Compuestos de piridina como inhibidores de shp2 alostericos.
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
CA3074690A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. Shp2 inhibitor compositions and methods for treating cancer
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
SG11202009245TA (en) 2018-03-21 2020-10-29 Relay Therapeutics Inc Shp2 phosphatase inhibitors and methods of use thereof
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
LT3833670T (lt) 2018-08-10 2024-06-25 Navire Pharma, Inc. 6-(4-amino-3-metil-2-oksa-8-azaspiro[4.5]dekan-8-il)-3-(2,3-dichlorfenil)-2-metilpirimidin-4(3h)-ono dariniai ir susiję junginiai kaip ptpn11 (shp2) inhibitoriai, skirti vėžiui gydyti
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
CN111138412B (zh) 2018-11-06 2023-09-15 上海奕拓医药科技有限责任公司 一种螺芳环化合物及其应用
CN111647000B (zh) 2019-03-04 2021-10-12 勤浩医药(苏州)有限公司 吡嗪类衍生物及其在抑制shp2中的应用
EP3980128A1 (en) 2019-06-07 2022-04-13 Revolution Medicines, Inc. Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor
AU2020354475A1 (en) 2019-09-24 2022-05-05 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of making and using the same
CN112724145A (zh) * 2019-10-14 2021-04-30 杭州雷索药业有限公司 用于抑制shp2活性的吡嗪衍生物
TW202128688A (zh) 2019-11-08 2021-08-01 美商銳新醫藥公司 雙環雜芳基化合物及其用途
WO2021110796A1 (en) * 2019-12-04 2021-06-10 Bayer Aktiengesellschaft Inhibitors of shp2
CN111265529B (zh) * 2020-02-22 2021-07-23 南京大学 蛋白酪氨酸磷酸酶shp2抑制剂在制备治疗银屑病药物中的应用
WO2021171261A1 (en) 2020-02-28 2021-09-02 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
IL308234A (en) 2021-05-05 2024-01-01 Huyabio Int Llc Monotherapy with an SHP2 inhibitor and its uses
CA3217084A1 (en) 2021-05-05 2022-11-10 Farbod Shojaei Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
CN114716448B (zh) * 2021-05-13 2024-01-30 中国科学院上海药物研究所 抑制shp2活性的杂环化合物、其制备方法及用途
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
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Also Published As

Publication number Publication date
CO2020012588A2 (es) 2020-10-30
BR112020020743A2 (pt) 2021-02-02
TW201946627A (zh) 2019-12-16
AU2019251207A1 (en) 2020-11-19
WO2019199792A1 (en) 2019-10-17
CA3096535A1 (en) 2019-10-17
US20210154190A1 (en) 2021-05-27
KR20200143417A (ko) 2020-12-23
IL277783B1 (en) 2024-03-01
JP2021521155A (ja) 2021-08-26
EP3773590A1 (en) 2021-02-17
IL277783A (en) 2020-11-30
CN112203689A (zh) 2021-01-08
MX2020010719A (es) 2020-11-06
SG11202009793TA (en) 2020-10-29

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