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CY1118644T1 - Ενωση καρβοξαμιδιου πυραζινης - Google Patents

Ενωση καρβοξαμιδιου πυραζινης

Info

Publication number
CY1118644T1
CY1118644T1 CY20171100230T CY171100230T CY1118644T1 CY 1118644 T1 CY1118644 T1 CY 1118644T1 CY 20171100230 T CY20171100230 T CY 20171100230T CY 171100230 T CY171100230 T CY 171100230T CY 1118644 T1 CY1118644 T1 CY 1118644T1
Authority
CY
Cyprus
Prior art keywords
egfr
mutation
positive
another embodiment
lung cancer
Prior art date
Application number
CY20171100230T
Other languages
English (en)
Inventor
Takahiro Matsuya
Yutaka Kondoh
Itsuro Shimada
Shigetoshi Kikuchi
Maiko Iida
Kenichi Onda
Hiroki Fukudome
Yukihiro Takemoto
Nobuaki Shindou
Hideki Sakagami
Hisao Hamaguchi
Original Assignee
Astellas Pharma Inc.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48799179&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CY1118644(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astellas Pharma Inc. filed Critical Astellas Pharma Inc.
Publication of CY1118644T1 publication Critical patent/CY1118644T1/el

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms
    • C07D241/28—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

[Πρόβλημα] Μια ένωση η οποία είναι χρήσιμη ως ένας αναστολέας στη δραστηριότητα της κινάσης μετάλλαξης Τ790Μ του EGFR παρέχεται. [Μέσα για Επίλυση] Οι παρόντες εφευρέτες έχουν ερευνήσει μια ένωση έχοντας μια ανασταλτική δράση σε μια κινάση μετάλλαξης Τ790Μ του EGFR, και έχουν βρει ότι μια ένωση πυραζινκαρβοξαμιδίου έχει μια ανασταλτική δράση σε μια κινάση μετάλλαξης Τ790Μ του EGFR, συμπληρώνοντας ως εκ τούτου την παρούσα εφεύρεση. Η ένωση πυραζινκαρβοξαμιδίου της παρούσας εφεύρεσης έχει μια ανασταλτική δράση σε μια κινάση μετάλλαξης Τ790Μ του EGFR, και μπορεί να χρησιμοποιηθεί ως ένας παράγων για πρόληψη και/ή αγωγή του θετικού σε μετάλλαξη Τ790Μ του EGFR καρκίνου, σε μια άλλη ενσωμάτωση, του θετικού σε μετάλλαξη Τ790Μ του EGFR καρκίνου του πνευμόνων, σε μια ακόμη άλλη ενσωμάτωση, του θετικού σε μετάλλαξη Τ790Μ του EGFR μη-μικροκυτταρικού καρκίνου των πνευμόνων, σε ακόμη περαιτέρω μια άλλη ενσωμάτωση, του θετικού σε πρωτεΐνη μετάλλαξης Τ790Μ του EGFR καρκίνου, σε ακόμη περαιτέρω μια άλλη ενσωμάτωση, του θετικού σε πρωτεΐνη μετάλλαξης Τ790Μ του EGFR καρκίνου των πνευμόνων, σε ακόμη περαιτέρω μια άλλη ενσωμάτωση, του ανθεκτικού σε αναστολέα κινάσης τυροσίνης του EGFR καρκίνου, σε μια ακόμη περαιτέρω άλλη ενσωμάτωση, του ανθεκτικού σε αναστολέα κινάσης τυροσίνης του EGFR καρκίνου των πνευμόνων, και σε ακόμη περαιτέρω μια άλλη ενσωμάτωση, του ανθεκτικού σε αναστολέα κινάσης τυροσίνης του EGFR μη-μικροκυτταρικού καρκίνου των πνευμόνων, ή των παρόμοιων.
CY20171100230T 2012-01-17 2017-02-20 Ενωση καρβοξαμιδιου πυραζινης CY1118644T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2012007525 2012-01-17
PCT/JP2013/050579 WO2013108754A1 (ja) 2012-01-17 2013-01-15 ピラジンカルボキサミド化合物

Publications (1)

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CY1118644T1 true CY1118644T1 (el) 2017-07-12

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ID=48799179

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US (1) US9085540B2 (el)
EP (1) EP2805940B1 (el)
JP (1) JP5532366B2 (el)
KR (1) KR101985050B1 (el)
CN (1) CN104080774B (el)
AR (1) AR089727A1 (el)
AU (1) AU2013210438B2 (el)
BR (1) BR112014017466A8 (el)
CA (1) CA2860765C (el)
CY (1) CY1118644T1 (el)
DK (1) DK2805940T3 (el)
EA (1) EA026353B1 (el)
ES (1) ES2613399T3 (el)
HK (1) HK1203491A1 (el)
HR (1) HRP20170226T1 (el)
HU (1) HUE033177T2 (el)
IL (1) IL233437A (el)
LT (1) LT2805940T (el)
ME (1) ME02648B (el)
MX (1) MX355434B (el)
PH (1) PH12014501456A1 (el)
PL (1) PL2805940T3 (el)
PT (1) PT2805940T (el)
RS (1) RS55704B1 (el)
SI (1) SI2805940T1 (el)
SM (2) SMT201700094T1 (el)
TW (1) TWI532727B (el)
UA (1) UA111010C2 (el)
WO (1) WO2013108754A1 (el)
ZA (1) ZA201405045B (el)

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TWI798334B (zh) * 2018-01-31 2023-04-11 大陸商迪哲（江蘇）醫藥股份有限公司 Ｅｒｂｂ／ｂｔｋ抑制劑
JP7201800B2 (ja) * 2018-09-30 2023-01-10 メッドシャイン ディスカバリー インコーポレイテッド Ｆｌｔ３およびａｘｌの阻害剤としての３，９－ジアザスピロ［５，５］ウンデカン系化合物
CN112062728A (zh) * 2019-05-25 2020-12-11 上海鑫凯化学科技有限公司 一种3,5-二氯-6-乙基吡嗪甲酰胺的合成方法
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JP2024509625A (ja) 2021-03-15 2024-03-04 ノバルティス アーゲー ベンゾイソオキサゾール誘導体及びその使用
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