[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

EA201490971A1 - Производные урацила в качестве ингибиторов axl и c-met киназы - Google Patents

Производные урацила в качестве ингибиторов axl и c-met киназы

Info

Publication number
EA201490971A1
EA201490971A1 EA201490971A EA201490971A EA201490971A1 EA 201490971 A1 EA201490971 A1 EA 201490971A1 EA 201490971 A EA201490971 A EA 201490971A EA 201490971 A EA201490971 A EA 201490971A EA 201490971 A1 EA201490971 A1 EA 201490971A1
Authority
EA
Eurasian Patent Office
Prior art keywords
axl
uracil
derivatives
kinase inhibitors
met kinase
Prior art date
Application number
EA201490971A
Other languages
English (en)
Other versions
EA023521B1 (ru
Inventor
Реддеппаредди Данду
Роберт Л. Хадкинз
Курт А. Джозеф
Кэтрин П. Праути
Рабиндранатх Трипатхи
Original Assignee
Сефалон, Инк.
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 Сефалон, Инк. filed Critical Сефалон, Инк.
Publication of EA201490971A1 publication Critical patent/EA201490971A1/ru
Publication of EA023521B1 publication Critical patent/EA023521B1/ru

Links

Classifications

    • 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
    • C07D401/02—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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D405/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Aiming, Guidance, Guns With A Light Source, Armor, Camouflage, And Targets (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы Iили его фармацевтически приемлемым формам соли, в которой R, R, R, R, D, W, R, R, R, Y, R, X, E и G имеют определенные здесь значения, к способам лечения и их применениям.
EA201490971A 2011-11-14 2012-11-14 ПРОИЗВОДНЫЕ УРАЦИЛА В КАЧЕСТВЕ ИНГИБИТОРОВ AXL И c-MET КИНАЗЫ EA023521B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161559312P 2011-11-14 2011-11-14
PCT/US2012/065019 WO2013074633A1 (en) 2011-11-14 2012-11-14 Uracil derivatives as axl and c-met kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201490971A1 true EA201490971A1 (ru) 2014-09-30
EA023521B1 EA023521B1 (ru) 2016-06-30

Family

ID=47297443

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490971A EA023521B1 (ru) 2011-11-14 2012-11-14 ПРОИЗВОДНЫЕ УРАЦИЛА В КАЧЕСТВЕ ИНГИБИТОРОВ AXL И c-MET КИНАЗЫ

Country Status (26)

Country Link
US (5) US9029538B2 (ru)
EP (2) EP3045453A1 (ru)
JP (2) JP6051434B2 (ru)
KR (1) KR20140090678A (ru)
CN (2) CN103958497B (ru)
AR (1) AR088872A1 (ru)
AU (2) AU2012339640B2 (ru)
BR (1) BR112014011548A2 (ru)
CA (1) CA2852697A1 (ru)
DK (1) DK2780338T3 (ru)
EA (1) EA023521B1 (ru)
ES (1) ES2614824T3 (ru)
HK (1) HK1202528A1 (ru)
HU (1) HUE033032T2 (ru)
IL (3) IL232405A (ru)
MX (1) MX342241B (ru)
PH (2) PH12014500883A1 (ru)
PL (1) PL2780338T3 (ru)
PT (1) PT2780338T (ru)
SG (2) SG10201510307WA (ru)
SI (1) SI2780338T1 (ru)
TW (1) TWI562989B (ru)
UA (1) UA114900C2 (ru)
UY (1) UY34451A (ru)
WO (1) WO2013074633A1 (ru)
ZA (1) ZA201402940B (ru)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2780338T (pt) 2011-11-14 2017-02-17 Ignyta Inc Derivados de uracil como inibidores da quinase axl e c-met
CN102643268B (zh) * 2011-12-30 2014-05-21 沈阳药科大学 喹啉类及噌啉类化合物及其应用
US20140121126A1 (en) * 2012-10-25 2014-05-01 Memorial Sloan-Kettering Cancer Center Methods of detecting axl and gas6 in cancer patients
AR096816A1 (es) 2013-07-08 2016-02-03 Bayer Cropscience Ag Derivados de arilsulfuro y arilsulfóxido de seis miembros enlazados con c-n como agentes para combatir parásitos
TWI649308B (zh) 2013-07-24 2019-02-01 小野藥品工業股份有限公司 喹啉衍生物
TW201536291A (zh) * 2013-08-02 2015-10-01 Cephalon Inc 單獨使用ＡＸＬ／ｃＭＥＴ抑制劑或與其它藥劑組合使用以治療多種癌症之方法
CN105980381A (zh) * 2013-11-08 2016-09-28 拜耳医药股份有限公司 取代的尿嘧啶及其用途
US9695131B2 (en) 2013-11-08 2017-07-04 Bayer Pharma Aktiengesellschaft Substituted uracils as chymase inhibitors
US9771333B2 (en) 2013-11-20 2017-09-26 Signalchem Lifesciences Corp. Quinazoline derivatives as TAM family kinase inhibitors
KR102398473B1 (ko) 2013-11-27 2022-05-16 시그널켐 라이프사이언시즈 코포레이션 Tam 패밀리 키나제 억제제로서의 아미노피리딘 유도체
DK3087070T3 (en) * 2013-12-26 2017-12-04 Ignyta Inc PYRAZOLO [1,5-A] PYRIDINE DERIVATIVES AND PROCEDURES FOR THEIR USE
JP6708130B2 (ja) * 2014-12-25 2020-06-10 小野薬品工業株式会社 キノリン誘導体
CN106046007B (zh) * 2015-04-07 2019-02-05 广东众生睿创生物科技有限公司 酪氨酸激酶抑制剂及包含该酪氨酸激酶抑制剂的药物组合物
AU2016249860B2 (en) * 2015-04-14 2019-10-10 Lead Discovery Center Gmbh Quinoline derivatives as TAM RTK inhibitors
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
CN106467541B (zh) * 2015-08-18 2019-04-05 暨南大学 取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
EP3359526A4 (en) 2015-10-05 2019-04-03 The Trustees of Columbia University in the City of New York ACTIVATORS OF AUTOPHAGIC RIVER AND PHOSPHOLIPASE D AND PURIFICATION OF PROTEIN AGGREGATES INCLUDING TAU AND TREATMENT OF PROTEINOPATHIES
EP3421039B1 (en) 2016-02-26 2021-10-06 ONO Pharmaceutical Co., Ltd. Drug for cancer therapy characterized by administering combination between axl inhibitor and immune checkpoint inhibitor
HRP20231614T1 (hr) 2016-03-28 2024-03-15 Incyte Corporation Spojevi pirolotriazina kao tam inhibitori
EP3490561A4 (en) * 2016-08-01 2020-04-08 Ignyta, Inc. COMBINATIONS FOR THE TREATMENT OF CANCER
US9957233B1 (en) 2016-08-05 2018-05-01 Calitor Sciences, Llc Process for preparing substituted quinolin-4-ol compounds
WO2018039275A1 (en) 2016-08-24 2018-03-01 Ignyta, Inc. Combinations for the treatment of cancer
CN106543145B (zh) * 2016-10-28 2019-07-19 山西医科大学 c-Met激酶抑剂3-(4-氟苯基)嘧啶酮-5-甲酸酰胺衍生物、制备方法与应用
CN108250200A (zh) * 2016-12-28 2018-07-06 中国科学院上海药物研究所 一种具有Axl抑制活性的化合物及其制备和应用
MX2019008787A (es) 2017-01-26 2019-09-11 Ono Pharmaceutical Co Sal de etano-sulfonato del derivado de quinolina.
CN108623568B (zh) * 2017-03-21 2022-04-19 南京汇诚制药有限公司 9,10二氢菲类丙型肝炎病毒抑制剂的盐型及其制备
WO2019039525A1 (ja) 2017-08-23 2019-02-28 小野薬品工業株式会社 Ａｘｌ阻害剤を有効成分として含むがん治療剤
GEP20227429B (en) 2017-09-27 2022-10-25 Incyte Corp Salts of pyrrolotriazine derivatives useful as tam inhibitors
US11826363B2 (en) 2017-10-13 2023-11-28 Ono Pharmaceutical Co., Ltd. Therapeutic agent for solid cancers, which comprises Axl inhibitor as active ingredient
CN107573340B (zh) * 2017-10-23 2020-11-24 江西科技师范大学 2-氨甲酰基-4-芳杂吡啶类化合物的制备及应用
JP7377798B2 (ja) * 2017-11-24 2023-11-10 南京明徳新薬研発有限公司 ｃ－ＭＥＴ／ＡＸＬ阻害剤としてのウラシル系化合物
US20210177828A1 (en) * 2018-01-17 2021-06-17 Nanjing Transthera Biosciences Co., Ltd. Tam family kinase /and csf1r kinase inhibitor and use thereof
WO2019213340A1 (en) * 2018-05-03 2019-11-07 Bristol-Myers Squibb Company Uracil derivatives as mer-axl inhibitors
CN110511218A (zh) * 2018-05-21 2019-11-29 中国科学院上海药物研究所 一类并环吡唑啉酮甲酰胺类化合物及其制备方法、药物组合物和用途
EP3810596B1 (en) * 2018-06-01 2022-11-30 Rigel Pharmaceuticals, Inc. Quinoline derivatives useful as tyrosine kinase inhibitors
SG11202013163TA (en) 2018-06-29 2021-01-28 Incyte Corp Formulations of an axl/mer inhibitor
WO2020038460A1 (zh) * 2018-08-24 2020-02-27 南京药捷安康生物科技有限公司 一种新型的喹啉衍生物抑制剂
US20210355107A1 (en) * 2018-08-27 2021-11-18 Beijing Yuezhikangtai Biomedicines Co., Ltd. Multi-substituted pyridone derivatives and medical use thereof
UY38349A (es) 2018-08-30 2020-03-31 Array Biopharma Inc Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y met
TWI840423B (zh) 2018-10-12 2024-05-01 美商拓臻股份有限公司 甲狀腺素受體β促效劑化合物
CN111196814B (zh) * 2018-11-19 2022-12-06 北京赛特明强医药科技有限公司 芳环连二噁烷并喹唑啉或喹啉类化合物、组合物及其应用
CN111320609A (zh) 2018-12-13 2020-06-23 拓臻股份有限公司 一种THRβ受体激动剂化合物及其制备方法和用途
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN111840299A (zh) * 2019-04-30 2020-10-30 武汉盛云生物医药科技有限责任公司 一种喹啉类化合物在制备治疗癌症药物中的应用
WO2020238802A1 (zh) * 2019-05-24 2020-12-03 南京明德新药研发有限公司 一种c-MET/AXL抑制剂的晶型
KR20220011705A (ko) * 2019-05-24 2022-01-28 메드샤인 디스커버리 아이엔씨. c-MET/AXL 억제제로서의 결정형
US20220324869A1 (en) * 2019-09-06 2022-10-13 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Compound having axl and c-met kinase inhibitory activity, preparation thereof and application thereof
CN112625026B (zh) * 2019-09-24 2022-09-09 药捷安康(南京)科技股份有限公司 Tam家族激酶抑制剂的喹啉衍生物
CA3155924A1 (en) * 2019-09-26 2021-04-01 Exelixis, Inc. PYRIDONE COMPOUNDS AND METHODS OF USE IN MODULATING A PROTEIN KINASE
WO2021076691A1 (en) 2019-10-16 2021-04-22 Chemocentryx, Inc. Heteroaryl-biphenyl amides for the treatment of pd-l1 diseases
CA3152714A1 (en) 2019-10-16 2021-04-22 Pingchen Fan Heteroaryl-biphenyl amines for the treatment of pd-l1 diseases
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR20230017165A (ko) 2020-03-06 2023-02-03 인사이트 코포레이션 Axl/mer 및 pd-1/pd-l1 억제제를 포함하는 병행 요법
GB202004960D0 (en) * 2020-04-03 2020-05-20 Kinsenus Ltd Inhibitor compounds
CN113620873B (zh) * 2020-05-07 2023-12-08 沈阳药科大学 含锌结合基以及喹啉骨架的化合物的制备方法和用途
EP4167991A4 (en) * 2020-06-23 2024-07-24 ChemoCentryx, Inc. METHODS OF TREATING CANCER WITH HETEROARYL-BIPHENYLAMIDE DERIVATIVES
US20250017921A1 (en) * 2020-09-08 2025-01-16 Ideaya Biosciences Inc. Pharmaceutical combination and tumor treatment
CN112675170B (zh) * 2021-02-03 2022-02-01 南华大学附属第一医院 V027-0576在制备抗肿瘤药物中的应用
JP2024507794A (ja) * 2021-02-19 2024-02-21 エグゼリクシス， インコーポレイテッド ピリドン化合物および使用方法
WO2022220227A1 (ja) * 2021-04-14 2022-10-20 エーザイ・アール・アンド・ディー・マネジメント株式会社 テトラヒドロピリドピリミジン化合物
CN117412953A (zh) * 2021-05-12 2024-01-16 微境生物医药科技(上海)有限公司 Axl抑制剂
WO2022266236A1 (en) 2021-06-18 2022-12-22 Aligos Therapeutics, Inc. Methods and compositions for targeting pd-l1
US20240317692A1 (en) * 2021-07-13 2024-09-26 Nippon Soda Co., Ltd. Method for producing uracil compound
IT202100022682A1 (it) * 2021-09-01 2023-03-01 Luigi Frati Derivati pirimidinici e loro uso nel trattamento di tumori
CN116693452B (zh) * 2023-05-24 2024-07-02 中山大学 一种喹啉衍生物及其制备方法和应用
WO2024259060A1 (en) * 2023-06-16 2024-12-19 Kinnate Biopharma Inc. Inhibitors of met kinase

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997017329A1 (fr) 1995-11-07 1997-05-15 Kirin Beer Kabushiki Kaisha Derives de quinoline et derives de quinazoline inhibant l'autophosphorylation d'un recepteur de facteur de croissance originaire de plaquettes, et compositions pharmaceutiques les contenant
JP2001500890A (ja) 1996-09-25 2001-01-23 ゼネカ リミテッド Ｖｅｇｆのような成長因子の作用を阻害するキノリン誘導体
CN1183114C (zh) 1999-01-22 2005-01-05 麒麟麦酒株式会社 喹啉衍生物及喹唑啉衍生物
US7732613B2 (en) * 2005-09-14 2010-06-08 Bristol-Myers Squibb Company Met kinase inhibitors
US20080004273A1 (en) 2006-05-30 2008-01-03 Stephane Raeppel Inhibitors of protein tyrosine kinase activity
WO2007146824A2 (en) 2006-06-08 2007-12-21 Array Biopharma Inc. Quinoline compounds and methods of use
CN101679313A (zh) * 2007-04-13 2010-03-24 休普基因公司 用于治疗癌症或过度增殖性疾病的axl激酶抑制剂
SI2947072T1 (sl) 2008-03-17 2017-03-31 Ambit Biosciences Corporation 1-(3-(6,7-dimetoksikinazolin-4-iloksi)fenil)-3-(5-1,1,1-trifluoro-2- metilpropan-2-il)izoksazol-3-il)urea kot modulator raf kinaze pri zdravljenju rakavih bolezni
ES2391373T3 (es) * 2008-04-16 2012-11-23 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Derivados de quinoleína como inhibidores de la cinasa AXL
UY31800A (es) * 2008-05-05 2009-11-10 Smithkline Beckman Corp Metodo de tratamiento de cancer usando un inhibidor de cmet y axl y un inhibidor de erbb
EP2311809A1 (en) 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Quinolinyloxyphenylsulfonamides
EP2423208A1 (en) * 2010-08-28 2012-02-29 Lead Discovery Center GmbH Pharmaceutically active compounds as Axl inhibitors
PL2694075T3 (pl) 2011-04-01 2016-09-30 Inhibitor 3-kinazy fosfoinozytydowej z grupą wiążącą cynk
PT2780338T (pt) * 2011-11-14 2017-02-17 Ignyta Inc Derivados de uracil como inibidores da quinase axl e c-met

Also Published As

Publication number Publication date
BR112014011548A2 (pt) 2017-05-09
EP2780338A1 (en) 2014-09-24
IL232405A (en) 2017-02-28
IL232405A0 (en) 2014-07-01
HUE033032T2 (hu) 2017-11-28
US9120778B2 (en) 2015-09-01
CA2852697A1 (en) 2013-05-23
IL245658A0 (en) 2016-06-30
JP2017071612A (ja) 2017-04-13
US9745283B2 (en) 2017-08-29
PH12014500883A1 (en) 2022-05-11
CN108047201A (zh) 2018-05-18
PH12016501535A1 (en) 2017-05-22
JP6404299B2 (ja) 2018-10-10
SG10201510307WA (en) 2016-01-28
JP6051434B2 (ja) 2016-12-27
CN103958497B (zh) 2017-09-01
US20140275077A1 (en) 2014-09-18
MX342241B (es) 2016-09-21
HK1202528A1 (en) 2015-10-02
MX2014005766A (es) 2014-05-30
US20170320853A1 (en) 2017-11-09
AU2012339640B2 (en) 2017-01-05
IL245658A (en) 2017-06-29
US9522902B2 (en) 2016-12-20
UY34451A (es) 2013-05-31
JP2014533287A (ja) 2014-12-11
IL252517A0 (en) 2017-07-31
EP2780338B1 (en) 2016-11-09
US20150209358A1 (en) 2015-07-30
AR088872A1 (es) 2014-07-16
PT2780338T (pt) 2017-02-17
EP3045453A1 (en) 2016-07-20
US20150210670A1 (en) 2015-07-30
UA114900C2 (uk) 2017-08-28
ES2614824T3 (es) 2017-06-02
EA023521B1 (ru) 2016-06-30
WO2013074633A1 (en) 2013-05-23
ZA201402940B (en) 2017-08-30
AU2017201042A1 (en) 2017-03-09
SI2780338T1 (sl) 2017-04-26
CN103958497A (zh) 2014-07-30
NZ624945A (en) 2015-09-25
US9029538B2 (en) 2015-05-12
US10017496B2 (en) 2018-07-10
TWI562989B (en) 2016-12-21
KR20140090678A (ko) 2014-07-17
NZ712194A (en) 2016-05-27
AU2012339640A1 (en) 2014-06-05
DK2780338T3 (en) 2016-12-19
SG11201402004YA (en) 2014-05-29
TW201332992A (zh) 2013-08-16
PL2780338T3 (pl) 2017-04-28
US20170050949A1 (en) 2017-02-23

Similar Documents

Publication Publication Date Title
EA201490971A1 (ru) Производные урацила в качестве ингибиторов axl и c-met киназы
CY1122266T1 (el) Ενωσεις 3-αμινοκυκλοαλκυλιου ως ror-gamma-t αναστολεις και χρησεις αυτων
EA201590748A1 (ru) Противовирусные соединения против rsv
EA201590224A1 (ru) Имидазотриазинкарбонитрилы, используемые в качестве ингибиторов киназы
EA202090291A2 (ru) Производные бипиразола в качестве ингибиторов jak
EA201690752A1 (ru) Ингибиторы g12c kras
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201100580A1 (ru) Имидазопиридазинкарбонитрилы, используемые в качестве ингибиторов киназы
EA201071339A1 (ru) Фосфорсодержащие производные в качестве ингибиторов киназы
UA111075C2 (uk) Триазолопіридинові сполуки як інгібітори кінази рім
EA201190227A1 (ru) Оксазолзамещенные индазолы в качестве ингибиторов pi3-киназ
EA201492204A1 (ru) Нуклеозиды на основе урацила и спирооксетана
EA201390766A1 (ru) БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ
EA201790418A1 (ru) Пиримидиниловые ингибиторы тирозинкиназы
UA113470C2 (xx) Піримідинові та піридинові сполуки та їх застосування
EA201500298A1 (ru) Алкоксипиразолы в качестве активаторов растворимой гуанилатциклазы
EA201591360A1 (ru) Азабензимидазолы в качестве ингибиторов изозимов фдэ4 для лечения цнс и других расстройств
EA201500182A1 (ru) 4-МЕТИЛ-2,3,5,9,9b-ПЕНТААЗАЦИКЛОПЕНТА[a]НАФТАЛИНЫ
EA201490474A1 (ru) Аминохиназолины в качестве ингибиторов киназ
EA201491376A1 (ru) Производные 1h-пирроло[2,3-b]пиридина и их применение в качестве ингибиторов киназы
EA201370211A1 (ru) Ингибиторы протеинкиназы
EA201490846A1 (ru) Новые производные арилхинолина
EA201490471A1 (ru) Пиридазиноновые соединения и их применение в качестве ингибиторов daao
EA201590552A1 (ru) Аминохинолины в качестве ингибиторов киназы
EA201301130A1 (ru) Имидазопиридазины в качестве ингибиторов акт киназы

Legal Events

Date Code Title Description
PC4A Registration of transfer of a eurasian patent by assignment
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU