HUE048704T2 - Rákellenes benzopirazinok az FGFR-kinázok gátlásával - Google Patents

Rákellenes benzopirazinok az FGFR-kinázok gátlásával

Info

Publication number
HUE048704T2
HUE048704T2 HUE12794746A HUE12794746A HUE048704T2 HU E048704 T2 HUE048704 T2 HU E048704T2 HU E12794746 A HUE12794746 A HU E12794746A HU E12794746 A HUE12794746 A HU E12794746A HU E048704 T2 HUE048704 T2 HU E048704T2
Authority
HU
Hungary
Prior art keywords
benzopyrazines
anticancer
inhibition
fgfr kinases
fgfr
Prior art date
Application number
HUE12794746A
Other languages
English (en)
Hungarian (hu)
Inventor
Steven John Woodhead
Christopher William Murray
Valerio Berdini
Gordon Saxty
Gilbert Besong
Lieven Meerpoel
Olivier Alexis Georges Querolle
Virginie Sophie Poncelet
Original Assignee
Astex Therapeutics 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 Astex Therapeutics Ltd filed Critical Astex Therapeutics Ltd
Publication of HUE048704T2 publication Critical patent/HUE048704T2/hu

Links

Classifications

    • 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
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/495—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
    • A61K31/535—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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 carbon atoms of the hetero ring
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/02—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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
    • C07D413/02—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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
HUE12794746A 2011-10-28 2012-10-26 Rákellenes benzopirazinok az FGFR-kinázok gátlásával HUE048704T2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161552873P 2011-10-28 2011-10-28
GBGB1118654.1A GB201118654D0 (en) 2011-10-28 2011-10-28 New compounds

Publications (1)

Publication Number Publication Date
HUE048704T2 true HUE048704T2 (hu) 2020-08-28

Family

ID=45373582

Family Applications (1)

Application Number Title Priority Date Filing Date
HUE12794746A HUE048704T2 (hu) 2011-10-28 2012-10-26 Rákellenes benzopirazinok az FGFR-kinázok gátlásával

Country Status (18)

Country Link
US (2) US9303029B2 (cg-RX-API-DMAC10.html)
EP (1) EP2776408B1 (cg-RX-API-DMAC10.html)
JP (1) JP6054406B2 (cg-RX-API-DMAC10.html)
KR (1) KR102086871B1 (cg-RX-API-DMAC10.html)
CN (1) CN104024233B (cg-RX-API-DMAC10.html)
AU (1) AU2012328171B2 (cg-RX-API-DMAC10.html)
BR (1) BR112014010183B8 (cg-RX-API-DMAC10.html)
CA (1) CA2853401C (cg-RX-API-DMAC10.html)
DK (1) DK2776408T3 (cg-RX-API-DMAC10.html)
ES (1) ES2765031T3 (cg-RX-API-DMAC10.html)
GB (1) GB201118654D0 (cg-RX-API-DMAC10.html)
HR (1) HRP20192102T1 (cg-RX-API-DMAC10.html)
HU (1) HUE048704T2 (cg-RX-API-DMAC10.html)
IN (1) IN2014MN00986A (cg-RX-API-DMAC10.html)
MX (1) MX356205B (cg-RX-API-DMAC10.html)
RU (1) RU2639863C2 (cg-RX-API-DMAC10.html)
SI (1) SI2776408T1 (cg-RX-API-DMAC10.html)
WO (1) WO2013061081A1 (cg-RX-API-DMAC10.html)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
CA2943687C (en) 2014-03-26 2024-02-13 Astex Therapeutics Ltd Combinations of an fgfr inhibitor and an igf1r inhibitor
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
KR102344105B1 (ko) 2014-08-18 2021-12-29 에자이 알앤드디 매니지먼트 가부시키가이샤 모노시클릭 피리딘 유도체의 염 및 이의 결정
CN104370825B (zh) * 2014-09-29 2017-04-19 人福医药集团股份公司 作为激酶抑制剂的取代杂环化合物及其制备方法和用途
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
JP6503450B2 (ja) 2015-03-25 2019-04-17 国立研究開発法人国立がん研究センター 胆管癌治療剤
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
US11542247B2 (en) 2015-09-23 2023-01-03 Janssen Pharmaceutica Nv Bi-heteroaryl substitute 1,4-benzodiazepines and uses thereof for the treatment of cancer
ES2811845T3 (es) 2015-09-23 2021-03-15 Janssen Pharmaceutica Nv Heterociclos tricíclicos para el tratamiento del cáncer
SG10201913213WA (en) 2015-12-17 2020-03-30 Eisai R&D Man Co Ltd Therapeutic agent for breast cancer
BR112018068681A2 (pt) 2016-03-16 2019-01-15 Bayer Cropscience Ag derivados de n-(cianobenzil)-6-(ciclopropil-carbonilamino)-4-(fenil)-piridina-2-carboxamida e compostos relacionados como pesticidas e agentes de proteção de plantas
JP7206188B2 (ja) * 2016-10-10 2023-01-17 ディベロップメント センター フォー バイオテクノロジー Ｉｉｉ型受容体チロシンキナーゼ阻害剤としてのキノキサリン化合物
EP3284739A1 (de) 2017-07-19 2018-02-21 Bayer CropScience Aktiengesellschaft Substituierte (het)arylverbindungen als schädlingsbekämpfungsmittel
JP7168149B2 (ja) * 2018-02-08 2022-11-09 ▲ザン▼州片仔▲ファン▼薬業股▲フン▼有限公司 Ｆｇｆｒ阻害剤としてのピラジン－２（１ｈ）－オン系化合物
CN111712245A (zh) 2018-03-28 2020-09-25 卫材R&D管理有限公司 用于肝细胞癌的治疗剂
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
EP3898615A1 (en) * 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN114174270B (zh) 2019-08-08 2023-06-06 漳州片仔癀药业股份有限公司 吡嗪-2(1h)-酮类化合物的a晶型和b晶型及其制备方法
CN110981819B (zh) * 2019-12-24 2022-07-01 广西师范大学 一种喹喔啉类信号通路抑制剂及其制备方法和应用
US20250313544A1 (en) * 2022-05-10 2025-10-09 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of glutathione s-transferase zeta 1 (gstz1) and methods of use
WO2025019622A2 (en) * 2023-07-18 2025-01-23 Elixiron Immunotherapeutics Inc. Method of enhanced absorption of quinoxaline type iii receptor tyrosine kinase inhibitors
WO2025067450A1 (zh) * 2023-09-28 2025-04-03 福贝生物医药科技(北京)有限公司 一种固体分散体、药物组合物、其制备方法及其用途

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2940972A (en) 1957-06-27 1960-06-14 Thomae Gmbh Dr K Tri-and tetra-substituted pteridine derivatives
US4666828A (en) 1984-08-15 1987-05-19 The General Hospital Corporation Test for Huntington's disease
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
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
GB9125001D0 (en) 1991-11-25 1992-01-22 Ici Plc Heterocyclic compounds
EP0763537A3 (en) 1993-05-14 1997-10-22 Genentech Inc Non-peptides farnesyl transfer inhibitors
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US5882864A (en) 1995-07-31 1999-03-16 Urocor Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate disease
US6218529B1 (en) 1995-07-31 2001-04-17 Urocor, Inc. Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer
TW472045B (en) 1996-09-25 2002-01-11 Astra Ab Protein kinase C inhibitor compounds, method for their preparation, pharmaceutical composition thereof and intermediate used for their preparation
BR9809501A (pt) 1997-05-28 2000-06-20 Rhone Poulenc Rorer Pharma Composto, composição farmacêutica, e, processos para inibir a atividade da tirosina quinase pdgf, para inibir a atividade da tirosina quinase lck, para inibir a proliferação celular, diferenciação ou liberação de mediador em um paciente, para tratar uma patologia ligada a um distúrbio hiperproliferativo, para tratar a restenose, e, para tratar inflamação em um paciente
UA71555C2 (en) 1997-10-06 2004-12-15 Zentaris Gmbh Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives
JP2002534512A (ja) 1999-01-15 2002-10-15 ノボ ノルディスク アクティーゼルスカブ 非ペプチドｇｌｐ−１アゴニスト
CA2393896A1 (en) 1999-09-15 2001-03-22 Warner-Lambert Company Pteridinones as kinase inhibitors
DE10013318A1 (de) 2000-03-17 2001-09-20 Merck Patent Gmbh Formulierung enthaltend Chinoxalinderivate
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
EP1458383B1 (en) 2001-12-18 2007-11-21 Merck & Co., Inc. Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5
US7402585B2 (en) 2001-12-24 2008-07-22 Astrazeneca Ab Substituted quinazoline derivatives as inhibitors of aurora kinases
JP2003213463A (ja) 2002-01-17 2003-07-30 Sumitomo Chem Co Ltd 金属腐食防止剤および洗浄液
CA2480800C (en) 2002-04-08 2008-09-23 Mark T. Bilodeau Inhibitors of akt activity
US20040097725A1 (en) 2002-07-10 2004-05-20 Norman Herron Charge transport compositions and electronic devices made with such compositions
US7825132B2 (en) 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
US7208493B2 (en) 2002-10-03 2007-04-24 Targegen, Inc. Vasculostatic agents and methods of use thereof
AR043059A1 (es) * 2002-11-12 2005-07-13 Bayer Pharmaceuticals Corp Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
ATE433967T1 (de) 2003-01-17 2009-07-15 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
US7244739B2 (en) 2003-05-14 2007-07-17 Torreypines Therapeutics, Inc. Compounds and uses thereof in modulating amyloid beta
NZ544112A (en) 2003-05-23 2010-01-29 Zentaris Gmbh Novel pyridopyrazines and use thereof as kinase modulators
DE10323345A1 (de) 2003-05-23 2004-12-16 Zentaris Gmbh Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren
WO2005007099A2 (en) 2003-07-10 2005-01-27 Imclone Systems Incorporated Pkb inhibitors as anti-tumor agents
AU2004259000A1 (en) * 2003-07-21 2005-02-03 Bethesda Pharmaceuticals, Inc. Design and synthesis of optimized ligands for PPAR
EP1651631A1 (en) 2003-08-01 2006-05-03 Genelabs Technologies, Inc. Bicyclic imidazol derivatives against flaviviridae
PL1673092T3 (pl) 2003-10-17 2008-01-31 4 Aza Ip Nv Pochodne pterydyny podstawione heterocyklem i ich zastosowanie w leczeniu
AU2004288709B2 (en) 2003-11-07 2011-01-06 Novartis Vaccines And Diagnostics, Inc. Methods for synthesizing quinolinone compounds
AU2004295058B9 (en) 2003-11-20 2011-06-30 Janssen Pharmaceutica N.V. 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors
WO2005054231A1 (en) 2003-11-24 2005-06-16 F.Hoffmann-La Roche Ag Pyrazolyl and imidazolyl pyrimidines
EP2228369A1 (en) 2003-12-23 2010-09-15 Astex Therapeutics Ltd. Pyrazole derivatives as protein kinase modulators
US7205316B2 (en) 2004-05-12 2007-04-17 Abbott Laboratories Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
US7098222B2 (en) 2004-05-12 2006-08-29 Abbott Laboratories Bicyclic-substituted amines having cyclic-substituted monocyclic substituents
NZ553087A (en) 2004-08-31 2010-12-24 Astrazeneca Ab Quinazolinone derivatives and their use as B-raf inhibitors
EP1805174A1 (en) 2004-10-14 2007-07-11 F.Hoffmann-La Roche Ag 1,5-naphthyridine azolidinones having cdk1 antiproliferative activity
WO2006040568A1 (en) * 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
CN102861019B (zh) 2004-12-24 2016-05-25 诺华股份有限公司 治疗或预防神经性疼痛的药物
JP2008530030A (ja) 2005-02-14 2008-08-07 バイオノミックス リミテッド 新規なチューブリン重合阻害剤
EP1853261B1 (de) 2005-03-03 2017-01-11 Universität des Saarlandes Selektive hemmstoffe humaner corticoidsynthasen
EP1881986A2 (en) 2005-05-12 2008-01-30 Merck & Co., Inc. Tyrosine kinase inhibitors
EP1881981A1 (en) 2005-05-18 2008-01-30 Wyeth 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of tpl2 kinase and methods of making and using the same
GB0513692D0 (en) 2005-07-04 2005-08-10 Karobio Ab Novel pharmaceutical compositions
CN101296909B (zh) * 2005-08-26 2011-10-12 默克雪兰诺有限公司 吡嗪衍生物及其作为pi3k抑制剂的应用
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
CA2628039A1 (en) 2005-11-11 2007-05-18 Aeterna Zentaris Gmbh Novel pyridopyrazines and their use as modulators of kinases
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
MY159523A (en) 2005-12-21 2017-01-13 Janssen Pharmaceutica Nv Triazolopyridazines as tyrosine kinase modulators
WO2007125405A2 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
GB0609621D0 (en) 2006-05-16 2006-06-21 Astrazeneca Ab Novel co-crystal
WO2007135027A1 (de) 2006-05-24 2007-11-29 Boehringer Ingelheim International Gmbh Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind
WO2008003702A2 (en) 2006-07-03 2008-01-10 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Fused bicyclic compounds interacting with the histamine h4 receptor
JP2008127446A (ja) 2006-11-20 2008-06-05 Canon Inc １，５−ナフチリジン化合物及び有機発光素子
CA2672828A1 (en) 2006-12-13 2008-06-26 Schering Corporation Methods of treatment
BRPI0720695A2 (pt) 2006-12-21 2014-02-18 Plexxikon Inc Compostos e métodos para modulação de cinase, e indicações para estes
CN101679408B (zh) 2006-12-22 2016-04-27 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
EA200900819A1 (ru) 2006-12-22 2010-02-26 Новартис Аг Хиназолины для ингибирования pdk1
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
EP2150255A4 (en) * 2007-05-10 2011-10-05 Glaxosmithkline Llc CHINOXALINE DERIVATIVES AS P13 KINASE INHIBITORS
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
JP2010529031A (ja) 2007-05-29 2010-08-26 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害剤としてのナフチリジン誘導体
AR066879A1 (es) 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
CN101784520B (zh) 2007-06-20 2014-07-02 田边三菱制药株式会社 磺酰基丙二酰胺衍生物和其药物用途
JP5548123B2 (ja) 2007-06-21 2014-07-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ６−｛ジフルオロ［６−（１−メチル−１Ｈ−ピラゾル−４−イル）［１，２，４］トリアゾロ［４，３−ｂ］ピリダジン−３−イル］メチル｝キノリンの多形および水和物の形態、塩、ならびに製造方法
WO2009019518A1 (en) 2007-08-09 2009-02-12 Astrazeneca Ab Pyrimidine compounds having a fgfr inhibitory effect
EP2173354A4 (en) 2007-08-09 2011-10-05 Glaxosmithkline Llc CHINOXALIN DERIVATIVES AS PI3 KINASE INHIBITORS
US20090054304A1 (en) 2007-08-23 2009-02-26 Kalypsys, Inc. Heterocyclic modulators of tgr5 for treatment of disease
KR101580482B1 (ko) 2007-11-16 2015-12-28 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서의 ４－피라졸릴－ｎ－아릴피리미딘－２－아민 및 ４－피라졸릴－ｎ－헤테로아릴피리미딘－２－아민
CA2722992A1 (en) 2008-05-05 2009-11-12 Schering Corporation Sequential administration of chemotherapeutic agents for treatment of cancer
GEP20125502B (en) 2008-05-23 2012-04-25 Novartis Ag Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors
JP2012509342A (ja) 2008-11-20 2012-04-19 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換ピロロ［２，３−ｂ］−ピリジンおよび−ピラジン
AU2010206161B2 (en) 2009-01-21 2014-08-07 Basilea Pharmaceutica Ag Novel bicyclic antibiotics
US20110288090A1 (en) 2009-02-02 2011-11-24 Armstrong Donna J Inhibitors of AKT Activity
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
MX353776B (es) 2009-06-12 2018-01-29 Abivax Compuestos utiles para tratar cancer.
EP2473504B1 (en) * 2009-09-03 2015-02-25 Bioenergenix Heterocyclic compounds for the inhibition of pask
CN102596932A (zh) * 2009-09-04 2012-07-18 拜耳医药股份有限公司 作为酪氨酸苏氨酸激酶抑制剂的取代氨基喹喔啉
US20110123545A1 (en) 2009-11-24 2011-05-26 Bristol-Myers Squibb Company Combination of vegfr2 and igf1r inhibitors for the treatment of proliferative diseases
EP2332939A1 (en) 2009-11-26 2011-06-15 Æterna Zentaris GmbH Novel Naphthyridine derivatives and the use thereof as kinase inhibitors
CN110269856A (zh) 2010-03-30 2019-09-24 维颂公司 多取代芳族化合物作为凝血酶的抑制剂
GB201007286D0 (en) * 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
WO2011146591A1 (en) 2010-05-19 2011-11-24 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
CN103153062B (zh) 2010-05-24 2015-07-15 因特利凯有限责任公司 杂环化合物及其用途
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
CN102532141A (zh) 2010-12-08 2012-07-04 中国科学院上海药物研究所 [1，2，4]三唑并[4，3-b][1，2，4]三嗪类化合物、其制备方法和用途
US8987257B2 (en) 2011-01-31 2015-03-24 Novartis Ag Heterocyclic derivatives
EP2678018A4 (en) 2011-02-23 2015-09-30 Intellikine Llc COMBINATION OF CHINESE HEMMER AND USES THEREOF
WO2012118492A1 (en) 2011-03-01 2012-09-07 Array Biopharma Inc. Heterocyclic sulfonamides as raf inhibitors
WO2013032951A1 (en) 2011-08-26 2013-03-07 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2755657B1 (en) * 2011-09-14 2017-11-29 Neupharma, Inc. Certain chemical entities, compositions, and methods
EP2757885B1 (en) 2011-09-21 2017-03-15 Neupharma, Inc. Certain chemical entites, compositions, and methods
WO2013052699A2 (en) 2011-10-04 2013-04-11 Gilead Calistoga Llc Novel quinoxaline inhibitors of pi3k
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
JO3210B1 (ar) 2011-10-28 2018-03-08 Merck Sharp & Dohme مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
PT2771342T (pt) 2011-10-28 2016-08-17 Novartis Ag Derivados de purina e o seu uso no tratamento de doença
HK1205528A1 (en) 2012-03-08 2015-12-18 Astellas Pharma Inc. Novel fgfr3 fusion product
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
US20150203589A1 (en) 2012-07-24 2015-07-23 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
CA2943687C (en) 2014-03-26 2024-02-13 Astex Therapeutics Ltd Combinations of an fgfr inhibitor and an igf1r inhibitor
RU2715236C2 (ru) 2014-03-26 2020-02-26 Астекс Терапьютикс Лтд Комбинации
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer

Also Published As

Publication number Publication date
EP2776408B1 (en) 2019-11-06
MX356205B (es) 2018-05-18
US20150031669A1 (en) 2015-01-29
BR112014010183B8 (pt) 2022-09-13
ES2765031T3 (es) 2020-06-05
GB201118654D0 (en) 2011-12-07
RU2014121389A (ru) 2015-12-10
BR112014010183A2 (pt) 2017-05-02
CA2853401C (en) 2022-02-15
US10052320B2 (en) 2018-08-21
DK2776408T3 (da) 2019-12-02
HRP20192102T1 (hr) 2020-02-21
MX2014004861A (es) 2014-08-21
US9303029B2 (en) 2016-04-05
CN104024233A (zh) 2014-09-03
KR20140084063A (ko) 2014-07-04
SI2776408T1 (sl) 2020-02-28
AU2012328171B2 (en) 2017-08-17
BR112014010183B1 (pt) 2022-03-29
AU2012328171A1 (en) 2014-03-27
RU2639863C2 (ru) 2017-12-25
KR102086871B1 (ko) 2020-03-09
IN2014MN00986A (cg-RX-API-DMAC10.html) 2015-04-24
EP2776408A1 (en) 2014-09-17
US20160220564A1 (en) 2016-08-04
JP2014534212A (ja) 2014-12-18
WO2013061081A1 (en) 2013-05-02
JP6054406B2 (ja) 2016-12-27
CA2853401A1 (en) 2013-05-02
CN104024233B (zh) 2017-05-24

Similar Documents

Publication Publication Date Title
AP4060A (en) Anticancer pyridopyrazines via the inhibition of fgfr kinases
HUE048704T2 (hu) Rákellenes benzopirazinok az FGFR-kinázok gátlásával
IL289834A (en) Conversion of tricyclic compounds as fgfr inhibitors
SI2855480T1 (sl) Pteridini kot fgfr inhibitorji
LT2820009T (lt) Serino (treonino) kinazės inhibitoriai
HUE037458T2 (hu) Kinolinok, mint FGFR kináz modulátorok
EP2863956A4 (en) INHIBITORS OF THE MICRO-RNA MIR-15 FAMILY
EP2847186A4 (en) SUBSTITUTED AMINOCHINAZOLINES USE AS CHINESE HEMMER
EP2900243A4 (en) BICYCLIC OXA LACTAM KINASE HEMMER
PL2817286T3 (pl) Inhibitory kinazy do leczenia raka
IL232842A0 (en) Cancer treatment through inhibition of myd88/map erk kinase interaction
GB201215883D0 (en) Enzyme inhibition
GB201215856D0 (en) Enzyme inhibition
GB201212184D0 (en) Landscaping of the Toska Lakes for geoengineering