PE20221264A1 - Inhibidores de egfr - Google Patents

Inhibidores de egfr

Info

Publication number
PE20221264A1
PE20221264A1 PE2022001323A PE2022001323A PE20221264A1 PE 20221264 A1 PE20221264 A1 PE 20221264A1 PE 2022001323 A PE2022001323 A PE 2022001323A PE 2022001323 A PE2022001323 A PE 2022001323A PE 20221264 A1 PE20221264 A1 PE 20221264A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
compound
independently
egfr inhibitors
Prior art date
Application number
PE2022001323A
Other languages
English (en)
Inventor
John Emmerson Campbell
Thomas A Dineen
Natasja Brooijmans
Jason D Brubaker
Meredith Suzanne Eno
Joseph L Kim
Aysegul Ozen
Emanuele Perola
Brett D Williams
Douglas Wilson
Kevin J Wilson
Savi Christopher De
Original Assignee
Blueprint Medicines Corp
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 Blueprint Medicines Corp filed Critical Blueprint Medicines Corp
Publication of PE20221264A1 publication Critical patent/PE20221264A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged 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
    • C07D491/04—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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • C07D491/08—Bridged 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
    • 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
    • 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
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Abstract

La presente invencion se refiere a un compuesto de formula (I) o una sal farmaceuticamente aceptable, donde: Z es O o NH; cada A1, A2 y A3 son independientemente N o CR, donde R es H, halogeno o CH3; el anillo A es un heterociclilo de 4 a 12 miembros; cada R1 es independientemente halogeno, CN, OH, entre otros; m es 0 a 6; R2 es H, halogeno, alquilo C1-C4, entre otros; R3 y R4 son H o metilo; R5 es H, alquilo C1-C4, entre otros; R6 es H o alquilo C1-C4 opcionalmente sustituido. Tambien se refiere a una composicion farmaceutica. Dicho compuesto es un inhibidor eficaz de ciertas formas mutantes del receptor del factor de crecimiento epidermico (EGFR), incluidas las mutaciones L858R, T790M y C797S, siendo util en el tratamiento de cancer.
PE2022001323A 2019-12-23 2020-12-22 Inhibidores de egfr PE20221264A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962953030P 2019-12-23 2019-12-23
PCT/US2020/066629 WO2021133809A1 (en) 2019-12-23 2020-12-22 Inhibitors of mutant forms of egfr

Publications (1)

Publication Number Publication Date
PE20221264A1 true PE20221264A1 (es) 2022-08-16

Family

ID=74186977

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022001323A PE20221264A1 (es) 2019-12-23 2020-12-22 Inhibidores de egfr

Country Status (19)

Country Link
US (2) US20230056541A1 (es)
EP (1) EP4081515A1 (es)
JP (1) JP2023508976A (es)
KR (1) KR20230005112A (es)
CN (1) CN115135642A (es)
AR (1) AR121044A1 (es)
AU (1) AU2020412710A1 (es)
BR (1) BR112022012585A2 (es)
CA (1) CA3163007A1 (es)
CL (1) CL2022001731A1 (es)
CO (1) CO2022010317A2 (es)
CR (1) CR20220354A (es)
EC (1) ECSP22057865A (es)
IL (1) IL294251A (es)
MX (1) MX2022007969A (es)
PE (1) PE20221264A1 (es)
TW (1) TW202138364A (es)
UY (1) UY39002A (es)
WO (1) WO2021133809A1 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20221264A1 (es) * 2019-12-23 2022-08-16 Blueprint Medicines Corp Inhibidores de egfr
TW202140473A (zh) 2020-01-15 2021-11-01 美商纜圖藥品公司 Map4k1抑制劑
EP4304727A1 (en) 2021-03-10 2024-01-17 Blueprint Medicines Corporation Egfr inhibitors
CN117881670A (zh) * 2021-06-23 2024-04-12 缆图药品公司 制备egfr抑制剂的方法
EP4359400A1 (en) * 2021-06-23 2024-05-01 Blueprint Medicines Corporation Salt and crystal forms of an epidermal growth factor receptor inhibitor
WO2023283130A1 (en) * 2021-07-04 2023-01-12 Newave Pharmaceutical Inc. Isoquinoline derivatives as mutant egfr modulators and uses thereof
WO2023288264A1 (en) * 2021-07-15 2023-01-19 Blueprint Medicines Corporation Map4k1 inhibitors
IL311028A (en) * 2021-08-27 2024-04-01 Shanghai Hansoh Biomedical Co Ltd Nitrogen - contains a derivative of a heterocyclic inhibitor, and the preparation of a method for it and its use
WO2023071998A1 (zh) * 2021-10-26 2023-05-04 杭州德睿智药科技有限公司 新型嘧啶或三嗪取代吡啶并杂环化合物
CN116159062A (zh) * 2021-11-24 2023-05-26 上海艾力斯医药科技股份有限公司 药物组合物及其用途
CN116478136A (zh) * 2022-01-17 2023-07-25 苏州浦合医药科技有限公司 2-哌啶基或2-吡唑基取代的嘧啶化合物作为egfr抑制剂
TW202400579A (zh) * 2022-03-17 2024-01-01 大陸商上海翰森生物醫藥科技有限公司 含氮雜環類衍生物抑制劑、其製備方法和應用
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WO2023196283A1 (en) 2022-04-05 2023-10-12 Blueprint Medicines Corporation Egfr inhibitors
WO2023241618A1 (zh) * 2022-06-14 2023-12-21 南京明德新药研发有限公司 氨基嘧啶类化合物及其应用
WO2024008048A1 (zh) * 2022-07-04 2024-01-11 杭州德睿智药科技有限公司 新型嘧啶或三嗪取代吡啶并杂环化合物
WO2024059169A1 (en) 2022-09-14 2024-03-21 Blueprint Medicines Corporation Egfr inhibitors
CN115650958A (zh) * 2022-10-14 2023-01-31 中国药科大学 2-氨基嘧啶类化合物及其制备方法、用途和药物组合物
CN115626939B (zh) * 2022-12-01 2023-06-16 北京鑫开元医药科技有限公司 一种egfr降解剂、制备方法、药物组合物及其应用
CN116969923A (zh) * 2023-01-18 2023-10-31 北京鞍石生物科技有限责任公司 杂芳基氨基化合物及其制备方法和应用
CN115974845A (zh) * 2023-01-19 2023-04-18 奥锐特药业股份有限公司 奥希替尼中间体的制备方法

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MX2015006152A (es) 2012-11-20 2016-01-20 Genentech Inc Compuestos de aminopirimidina como inhibidores de mutantes de egfr que contienen t7 9 0m.
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TW202140473A (zh) 2020-01-15 2021-11-01 美商纜圖藥品公司 Map4k1抑制劑

Also Published As

Publication number Publication date
JP2023508976A (ja) 2023-03-06
EP4081515A1 (en) 2022-11-02
BR112022012585A2 (pt) 2022-09-27
AR121044A1 (es) 2022-04-13
AU2020412710A1 (en) 2022-08-11
TW202138364A (zh) 2021-10-16
CA3163007A1 (en) 2021-07-01
ECSP22057865A (es) 2022-11-30
KR20230005112A (ko) 2023-01-09
CO2022010317A2 (es) 2022-10-21
MX2022007969A (es) 2022-12-13
UY39002A (es) 2021-07-30
CR20220354A (es) 2022-12-19
WO2021133809A1 (en) 2021-07-01
CL2022001731A1 (es) 2023-07-14
IL294251A (en) 2022-08-01
US11718602B2 (en) 2023-08-08
US20230056541A1 (en) 2023-02-23
US20230026209A1 (en) 2023-01-26
CN115135642A (zh) 2022-09-30

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