TW201946627A - 治療癌症的shp2抑制劑組合物和方法 - Google Patents

治療癌症的shp2抑制劑組合物和方法 Download PDF

Info

Publication number
TW201946627A
TW201946627A TW108112247A TW108112247A TW201946627A TW 201946627 A TW201946627 A TW 201946627A TW 108112247 A TW108112247 A TW 108112247A TW 108112247 A TW108112247 A TW 108112247A TW 201946627 A TW201946627 A TW 201946627A
Authority
TW
Taiwan
Prior art keywords
formula
shp2
cancer
allosteric
alkyl
Prior art date
Application number
TW108112247A
Other languages
English (en)
Chinese (zh)
Inventor
大衛 E 王爾德
艾斯畢諾沙 卡洛斯 史塔湖特
羅伯特 J 尼柯爾
Original Assignee
美商銳新醫藥公司
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 美商銳新醫藥公司 filed Critical 美商銳新醫藥公司
Publication of TW201946627A publication Critical patent/TW201946627A/zh

Links

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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further 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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/495—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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic 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
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING 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
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING 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
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/156—Polymorphic or mutational markers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (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)
TW108112247A 2018-04-10 2019-04-09 治療癌症的shp2抑制劑組合物和方法 TW201946627A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862655648P 2018-04-10 2018-04-10
US62/655,648 2018-04-10

Publications (1)

Publication Number Publication Date
TW201946627A true TW201946627A (zh) 2019-12-16

Family

ID=66248820

Family Applications (1)

Application Number Title Priority Date Filing Date
TW108112247A TW201946627A (zh) 2018-04-10 2019-04-09 治療癌症的shp2抑制劑組合物和方法

Country Status (14)

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

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11466017B2 (en) 2011-03-10 2022-10-11 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
WO2017210134A1 (en) 2016-05-31 2017-12-07 Board Of Regents, University Of Texas System Heterocyclic inhibitors of ptpn11
PT3468972T (pt) 2016-06-14 2020-08-21 Novartis Ag Compostos e composições para inibir a atividade da shp2
IL311645B2 (en) 2016-07-12 2025-11-01 Revolution Medicines Inc 2,5- disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines asallosteric shp2 inhibitors
EP3515916B1 (en) 2016-09-22 2023-06-07 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
CA3051054A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
CN110446709B (zh) 2017-01-23 2023-09-12 锐新医药公司 作为变构shp2抑制剂的二环化合物
US11591336B2 (en) 2017-05-26 2023-02-28 D. E. Shaw Research, Llc Substituted pyrazolo[3,4-b]pyrazines as SHP2 phosphatase inhibitors
TWI852912B (zh) 2017-09-07 2024-08-21 美商銳新醫藥公司 Shp2抑制劑組合物以及治療癌症的方法
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
BR112020007058A2 (pt) 2017-10-12 2020-10-06 Revolution Medicines, Inc. compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
US12138263B2 (en) 2018-03-21 2024-11-12 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof
CN117263942A (zh) 2018-03-21 2023-12-22 传达治疗有限公司 Shp2磷酸酶抑制剂及其使用方法
KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
PL3833670T3 (pl) 2018-08-10 2024-08-19 Navire Pharma, Inc. Pochodne 6-(4-amino-3-metylo-2-oksa-8-azaspiro[4.5]dekan-8-ylo)-3-(2,3-dichlorofenylo)-2-metylopirymidyn-4(3h)-onu oraz powiązane związki jako inhibitory ptpn11 (shp2) do leczenia raka
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
CN117143079A (zh) 2018-11-06 2023-12-01 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
CA3142430A1 (en) 2019-06-07 2020-12-10 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
EP4034539A1 (en) 2019-09-24 2022-08-03 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
PH12022551102A1 (en) 2019-11-08 2023-11-20 Revolution Medicines Inc Bicyclic heteroaryl compounds and uses thereof
EP4069301A1 (en) * 2019-12-04 2022-10-12 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
US20230090389A1 (en) 2020-02-28 2023-03-23 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
CA3217084A1 (en) 2021-05-05 2022-11-10 Farbod Shojaei Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
WO2022235822A1 (en) 2021-05-05 2022-11-10 Huabio International, Llc Shp2 inhibitor monotherapy and uses thereof
JP7656087B2 (ja) * 2021-05-13 2025-04-02 中国科学院上海薬物研究所 Shp2活性を阻害する複素環化合物、その製造方法および使用
TW202313041A (zh) 2021-06-09 2023-04-01 瑞士商諾華公司 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合
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
US20240374571A1 (en) 2021-09-01 2024-11-14 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
CN116063307B (zh) * 2021-10-29 2025-08-19 中国药科大学 Shp2与cdk4/6双靶点抑制化合物合成及其制备方法与应用

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
AU2002334773A1 (en) * 2001-10-01 2003-04-14 Mount Sinai School Of Medicine Noonan syndrome gene
US20080274469A1 (en) * 2005-10-21 2008-11-06 The Regents Of The University Of California C-Kit Oncogene Mutations in Melanoma
NZ623069A (en) 2009-08-17 2015-11-27 Sloan Kettering Inst Cancer Heat shock protein binding compounds, compositions, and methods for making and using same
US8673913B2 (en) * 2009-11-13 2014-03-18 Case Western Reserve University SHP-2 phosphatase inhibitor
EP2826586A1 (en) 2013-07-18 2015-01-21 Siemens Aktiengesellschaft A method and a system for machining an object
WO2015107494A1 (en) 2014-01-17 2015-07-23 Novartis Ag 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
ES2699351T3 (es) 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de SHP2
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
ES2824576T3 (es) 2015-06-19 2021-05-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
EP3310779B1 (en) 2015-06-19 2019-05-08 Novartis AG Compounds and compositions for inhibiting the activity of shp2
WO2016203406A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
US11008372B2 (en) 2015-11-07 2021-05-18 Board Of Regents, The University Of Texas System Targeting proteins for degradation
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
KR102218333B1 (ko) 2016-06-07 2021-02-22 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
IL311645B2 (en) 2016-07-12 2025-11-01 Revolution Medicines Inc 2,5- disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines asallosteric shp2 inhibitors

Also Published As

Publication number Publication date
IL277783A (en) 2020-11-30
US20210154190A1 (en) 2021-05-27
EP3773590A1 (en) 2021-02-17
KR20200143417A (ko) 2020-12-23
CA3096535A1 (en) 2019-10-17
CN112203689A (zh) 2021-01-08
IL277783B2 (en) 2024-07-01
IL277783B1 (en) 2024-03-01
AU2019251207A1 (en) 2020-11-19
WO2019199792A1 (en) 2019-10-17
JP2021521155A (ja) 2021-08-26
CO2020012588A2 (es) 2020-10-30
MX2020010719A (es) 2020-11-06
BR112020020743A2 (pt) 2021-02-02
SG11202009793TA (en) 2020-10-29

Similar Documents

Publication Publication Date Title
KR20200143417A (ko) Shp2 억제제 조성물, 암을 치료하는 방법 및 shp2 돌연변이를 갖는 대상체를 확인하는 방법
TWI852912B (zh) Shp2抑制劑組合物以及治療癌症的方法
CN111164083B (zh) 用于抑制bmp信号传导的新型alk2抑制剂和方法
JP7491914B2 (ja) SMARCA2及び/又はSMARCA4のディグレーダーとしてのタンパク質分解誘導キメラ(Protac)
CN113473990A (zh) 用于治疗癌症的shp2抑制剂组合物
WO2020073945A1 (zh) 双环类衍生物抑制剂、其制备方法和应用
CN111349087B (zh) 用于抑制肌成束蛋白的化合物和方法
CN110785418A (zh) 作为irak4调节剂的异二氢吲哚酮衍生物
ES3009382T3 (en) Pyrazolo[1,5-a]pyrimidine-based compounds, compositions comprising them and methods of their use
JP2017503815A (ja) がんまたは炎症性疾患を処置するための置換されたピロロピリジンおよびピロロピラジン
CN104211703B (zh) 一类作为布鲁顿激酶抑制剂的稠杂环化合物
JP2020524692A (ja) Irak4調節因子としてのベンゾフラン
CN105593231B (zh) 构象限制的PI3K和mTOR抑制剂
WO2014187262A1 (zh) 一类布鲁顿激酶抑制剂
CN108368112B (zh) 治疗性化合物、组合物和它们的使用方法
CN108658976B (zh) 一类新型吡唑并[4,3-c]吡啶-4(5)-酮布鲁顿激酶抑制剂
CN112739701A (zh) 具有表皮生长因子受体突变的抑制效果的新型融合嘧啶骨架磺酰胺衍生物
CN120035595A (zh) 噻唑并[5,4-d]嘧啶化合物、包含其的组合物及其用途
CN117460723A (zh) 药物化合物
HK1258765B (en) Therapeutic compounds, compositions and methods of use thereof