EA026152B1 - СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ с-kit - Google Patents

СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ с-kit Download PDF

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Publication number
EA026152B1
EA026152B1 EA201490545A EA201490545A EA026152B1 EA 026152 B1 EA026152 B1 EA 026152B1 EA 201490545 A EA201490545 A EA 201490545A EA 201490545 A EA201490545 A EA 201490545A EA 026152 B1 EA026152 B1 EA 026152B1
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Eurasian Patent Office
Prior art keywords
pyridin
imidazo
methyl
oxadiazol
methylphenyl
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EA201490545A
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English (en)
Russian (ru)
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EA201490545A1 (ru
Inventor
Валентина Мольтени
Ханк Майкл Джеймс Петрасси
Сяолинь Ли
Сяодун Лю
Джон Лорен
Джульет Набакка
Бао Нгуйен
Винс ЕХ
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Новартис Аг
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Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201490545A1 publication Critical patent/EA201490545A1/ru
Publication of EA026152B1 publication Critical patent/EA026152B1/ru

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
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    • A61P11/00Drugs for disorders of the respiratory system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems

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  • General Chemical & Material Sciences (AREA)
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  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201490545A 2011-09-01 2012-08-29 СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ с-kit EA026152B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161530038P 2011-09-01 2011-09-01
PCT/US2012/052802 WO2013033167A1 (en) 2011-09-01 2012-08-29 Compounds and compositions as c-kit kinase inhibitors

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EA201490545A1 EA201490545A1 (ru) 2014-07-30
EA026152B1 true EA026152B1 (ru) 2017-03-31

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US (3) US8569283B2 (OSRAM)
EP (1) EP2751104B1 (OSRAM)
JP (1) JP6134319B2 (OSRAM)
KR (1) KR101962495B1 (OSRAM)
CN (1) CN103797011B (OSRAM)
AP (1) AP2014007493A0 (OSRAM)
AR (1) AR087753A1 (OSRAM)
AU (1) AU2012302042B2 (OSRAM)
BR (1) BR112014004560A2 (OSRAM)
CA (1) CA2845169C (OSRAM)
CL (1) CL2014000492A1 (OSRAM)
CO (1) CO6900141A2 (OSRAM)
CR (1) CR20140107A (OSRAM)
CU (1) CU20140024A7 (OSRAM)
EA (1) EA026152B1 (OSRAM)
ES (1) ES2761332T3 (OSRAM)
GT (1) GT201400034A (OSRAM)
IL (1) IL231227A0 (OSRAM)
MA (1) MA35460B1 (OSRAM)
MX (1) MX339937B (OSRAM)
PE (1) PE20140909A1 (OSRAM)
PH (1) PH12014500372A1 (OSRAM)
PL (1) PL2751104T3 (OSRAM)
PT (1) PT2751104T (OSRAM)
SG (1) SG2014014369A (OSRAM)
TN (1) TN2014000068A1 (OSRAM)
TW (1) TW201313717A (OSRAM)
UY (1) UY34301A (OSRAM)
WO (1) WO2013033167A1 (OSRAM)
ZA (1) ZA201401175B (OSRAM)

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KR20210142154A (ko) 2019-03-21 2021-11-24 옹쎄오 암 치료를 위한 키나제 억제제와 조합된 dbait 분자
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MX2021013814A (es) * 2019-05-13 2022-02-10 Novartis Ag Formas cristalinas de n-(5-(5-((1r,2s)-2-fluorociclopropil)-1,2,4- oxadiazol-3-yl)-2- metilfenil)imidazo[1,2-a]piridin-3-carboxamida.
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JP2023551434A (ja) 2020-11-19 2023-12-08 サード ハーモニック バイオ, インコーポレイテッド 選択的c-kitキナーゼ阻害剤の医薬組成物ならびにその作製および使用のための方法
KR20230157400A (ko) 2021-03-16 2023-11-16 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 항박테리아성 화합물
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KR20230157445A (ko) 2021-03-17 2023-11-16 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 항박테리아성 화합물
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CN120677155A (zh) * 2022-12-07 2025-09-19 第三谐波生物股份有限公司 作为c-Kit激酶抑制剂的化合物和组合物
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Cited By (1)

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US12310963B2 (en) 2019-08-29 2025-05-27 Tarapeutics Science Inc. Pyrazole derivatives and use thereof

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KR20140075692A (ko) 2014-06-19
TW201313717A (zh) 2013-04-01
AP2014007493A0 (en) 2014-03-31
CN103797011B (zh) 2016-03-30
CA2845169A1 (en) 2013-03-07
UY34301A (es) 2013-04-05
MA35460B1 (fr) 2014-09-01
IL231227A0 (en) 2014-04-30
AR087753A1 (es) 2014-04-16
PH12014500372A1 (en) 2014-04-07
ES2761332T3 (es) 2020-05-19
GT201400034A (es) 2015-02-19
MX2014002484A (es) 2014-11-25
EP2751104A1 (en) 2014-07-09
AU2012302042B2 (en) 2016-03-31
CO6900141A2 (es) 2014-03-20
US20140228347A1 (en) 2014-08-14
PT2751104T (pt) 2019-12-16
WO2013033167A1 (en) 2013-03-07
ZA201401175B (en) 2015-01-28
US20130059832A1 (en) 2013-03-07
KR101962495B1 (ko) 2019-03-26
CU20140024A7 (es) 2014-04-24
EA201490545A1 (ru) 2014-07-30
US9023839B2 (en) 2015-05-05
CL2014000492A1 (es) 2014-10-03
TN2014000068A1 (en) 2015-07-01
CA2845169C (en) 2022-04-19
PE20140909A1 (es) 2014-07-20
CR20140107A (es) 2014-05-02
US20140031333A1 (en) 2014-01-30
AU2012302042A1 (en) 2014-04-17
BR112014004560A2 (pt) 2017-04-04
EP2751104B1 (en) 2019-09-25
SG2014014369A (en) 2014-09-26
US8569283B2 (en) 2013-10-29
PL2751104T3 (pl) 2020-04-30
MX339937B (es) 2016-06-17
CN103797011A (zh) 2014-05-14
JP6134319B2 (ja) 2017-05-24
JP2014525448A (ja) 2014-09-29
US8754071B2 (en) 2014-06-17

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