PE20220931A1 - Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina - Google Patents

Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina

Info

Publication number
PE20220931A1
PE20220931A1 PE2022000239A PE2022000239A PE20220931A1 PE 20220931 A1 PE20220931 A1 PE 20220931A1 PE 2022000239 A PE2022000239 A PE 2022000239A PE 2022000239 A PE2022000239 A PE 2022000239A PE 20220931 A1 PE20220931 A1 PE 20220931A1
Authority
PE
Peru
Prior art keywords
halogen
hydrogen
alkyl
pyrazine
pyrazolo
Prior art date
Application number
PE2022000239A
Other languages
English (en)
Inventor
Steven Howard
John Walter Liebeschuetz
Tadashi Shimamura
Original Assignee
Otsuka Pharma Co Ltd
Taiho Pharmaceutical Co Ltd
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 Otsuka Pharma Co Ltd, Taiho Pharmaceutical Co Ltd filed Critical Otsuka Pharma Co Ltd
Publication of PE20220931A1 publication Critical patent/PE20220931A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Abstract

La presente invencion se refiere a un compuesto derivado de pirazina de formula (I) o un tautomero o una sal farmaceuticamente aceptable del mismo, donde: R1 es hidrogeno o hidroxilo; R2 y R3 se seleccionan independientemente de hidrogeno, halogeno, alquilo C1-C4, haloalquilo C1-C4, hidroxialquilo C1-C4, CN; X es O o CR4R5; R4 y R5 se seleccionan independientemente de hidrogeno, halogeno, entre otros; R6 y R7 son hidrogeno, alcoxi C1-4 o halogeno, o R6 y R7 se unen para formar un anillo A opcionalmente sustituido por grupos R10; el anillo A es un anillo heterociclico de cinco miembros que contiene nitrogeno, O y S, entre otros; R8 es haloalquilo C1-4, CH3 y halogeno; R9 es hidrogeno, alquilo C1-4, haloalquilo C1-4 y halogeno; R10 es halogeno, ciano, hidroxilo, oxo, alquilo C1-4, entre otros. Tambien se refiere a una composicion farmaceutica y a un proceso de preparacion. Dicho compuesto es un inhibidor de la proteina tirosina fosfatasa 2 (SHP2), siendo util en el tratamiento del cancer.
PE2022000239A 2019-08-20 2020-08-20 Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina PE20220931A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1911928.8A GB201911928D0 (en) 2019-08-20 2019-08-20 Pharmaceutical compounds
PCT/IB2020/057815 WO2021033153A1 (en) 2019-08-20 2020-08-20 Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors

Publications (1)

Publication Number Publication Date
PE20220931A1 true PE20220931A1 (es) 2022-05-31

Family

ID=68099585

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000239A PE20220931A1 (es) 2019-08-20 2020-08-20 Inhibidores de shp2 fosfatasa de tipo pirazolo[3,4-b]pirazina

Country Status (18)

Country Link
US (1) US20230049719A1 (es)
EP (1) EP4017855A1 (es)
JP (1) JP2022546213A (es)
KR (1) KR20220049518A (es)
CN (1) CN114206885A (es)
AU (1) AU2020333251A1 (es)
BR (1) BR112022003184A2 (es)
CA (1) CA3148312A1 (es)
CL (1) CL2022000271A1 (es)
CO (1) CO2022001357A2 (es)
CR (1) CR20220062A (es)
EC (1) ECSP22011086A (es)
GB (1) GB201911928D0 (es)
IL (1) IL289462A (es)
MX (1) MX2022001908A (es)
PE (1) PE20220931A1 (es)
TW (1) TW202124383A (es)
WO (1) WO2021033153A1 (es)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111902415A (zh) 2018-03-02 2020-11-06 大冢制药株式会社 药学化合物
MX2022016355A (es) 2020-06-18 2023-04-03 Revolution Medicines Inc Metodos para retardar, prevenir, y tratar la resistencia adquirida a inhibidores de ras.
EP4183395A1 (en) 2020-07-15 2023-05-24 Taiho Pharmaceutical Co., Ltd. Pyrimidine compound-containing combination to be used in tumor treatment
AU2021344830A1 (en) 2020-09-03 2023-04-06 Revolution Medicines, Inc. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
WO2022060836A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
KR20240004960A (ko) 2021-05-05 2024-01-11 레볼루션 메디슨즈, 인크. Ras 억제제
EP4334324A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
PE20240089A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cancer
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
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
CN116323616A (zh) * 2021-07-07 2023-06-23 浙江同源康医药股份有限公司 用作shp2抑制剂的化合物及其应用
CA3224341A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
WO2023051648A1 (zh) * 2021-09-28 2023-04-06 甘李药业股份有限公司 可用作shp2抑制剂的化合物及其制备方法和用途
WO2023051717A1 (zh) * 2021-09-29 2023-04-06 微境生物医药科技(上海)有限公司 作为shp2抑制剂的稠环化合物
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4801531A (en) 1985-04-17 1989-01-31 Biotechnology Research Partners, Ltd. Apo AI/CIII genomic polymorphisms predictive of atherosclerosis
US5272057A (en) 1988-10-14 1993-12-21 Georgetown University Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase
US5192659A (en) 1989-08-25 1993-03-09 Genetype Ag Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
WO1998004689A1 (en) 1995-07-31 1998-02-05 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
WO2016203405A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
CN109475531B (zh) * 2016-05-31 2021-08-17 得克萨斯州立大学董事会 Ptpn11的杂环抑制剂
CN112250670B (zh) * 2016-06-07 2021-06-08 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
US11529347B2 (en) * 2016-09-22 2022-12-20 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
MX2020011528A (es) 2018-05-02 2021-02-09 Navire Pharma Inc Inhibidores heterociclicos sustituidos de ptpn11.

Also Published As

Publication number Publication date
CO2022001357A2 (es) 2022-03-18
MX2022001908A (es) 2022-04-18
AU2020333251A1 (en) 2022-02-17
CR20220062A (es) 2022-04-20
KR20220049518A (ko) 2022-04-21
EP4017855A1 (en) 2022-06-29
US20230049719A1 (en) 2023-02-16
ECSP22011086A (es) 2022-03-31
JP2022546213A (ja) 2022-11-04
CL2022000271A1 (es) 2022-10-28
CA3148312A1 (en) 2021-02-25
IL289462A (en) 2022-02-01
GB201911928D0 (en) 2019-10-02
BR112022003184A2 (pt) 2022-05-17
WO2021033153A1 (en) 2021-02-25
TW202124383A (zh) 2021-07-01
CN114206885A (zh) 2022-03-18

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