DK2473504T3 - Heterocykliske forbindelser til inhibering af pask - Google Patents

Heterocykliske forbindelser til inhibering af pask Download PDF

Info

Publication number
DK2473504T3
DK2473504T3 DK10814524.4T DK10814524T DK2473504T3 DK 2473504 T3 DK2473504 T3 DK 2473504T3 DK 10814524 T DK10814524 T DK 10814524T DK 2473504 T3 DK2473504 T3 DK 2473504T3
Authority
DK
Denmark
Prior art keywords
methyl
equiv
mmol
phenylquinoxaline
carboxylate
Prior art date
Application number
DK10814524.4T
Other languages
English (en)
Inventor
John M Mccall
John Mckearn
Donnal L Romero
Michael Clare
Original Assignee
Bioenergenix
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 Bioenergenix filed Critical Bioenergenix
Application granted granted Critical
Publication of DK2473504T3 publication Critical patent/DK2473504T3/da

Links

Classifications

    • 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
    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • C07D241/50—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to ring nitrogen atoms
    • C07D241/54—Nitrogen 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
    • C07D401/04—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
    • C07D401/12—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
    • C07D403/12—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
    • C07D405/02—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
    • C07D405/02—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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D413/02—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
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (9)

1. Forbindelse med strukturformel IV:
(IV) eller et salt eller ester deraf, hvor: Rz er valgt fra OH, NR8, Rg, NRsORg; Ri er valgt fra aryl og heteroaryl, der hver især eventuelt kan være substitueret med én eller flere substituenter valgt fra hydrogen, halo, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, heterarylalkyl, CN, alkoxy, alkylamino, dialkylamino, NHSO2R12, NHSO2NHR12, NHCOR12, NHCONHR12, CONHR12, CONRi2aRi2b, hydroxy, SO2R12, SO2NHR12, CF3, og OCF3; R3 er valgt fra hydrogen, hydroxyl, C1-C5 alkyl, og C1-C5 alkoxy, der hver især eventuelt kan være substitueret; R5 og R6 er uafhængigt valgt fra hydrogen, C1-C6 alkyl, C1-C7 cycloalkyl, C1-C7 heterocycloalkyl, Ci-C5 alkenyl, Ci-C5 alkynyl, aryl, heteroaryl, aralkyl, og heteroaralkyl, eller sammen kan, R5 og R6 danne en heterocycloalkyl eller heteroaryl, der hver især eventuelt kan være substitueret; R8 og Rg hver især er uafhængigt valgt fra hydrogen, C1-C6 alkyl, aryl, heteroaryl, aralkyl og heteroaralkyl, der hver især eventuelt kan være substitueret; og R12, Ri2a og Ri2b er uafhængigt valgt fra hydrogen, C1-C6 alkyl, aryl, heteroaryl, aralkyl, CF3 og heteroaralkyl, der hver især eventuelt kan være substitueret.
2. Forbindelsen ifølge krav 1, hvor Ri er phenyl og har én eller flere substituenter valgt fra hydrogen, halo, alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, aryl, aralkyl, heterocyclyl, heteroaryl, heterarylalkyl, CN, alkoxy, alkylamino, dialkylamino, NHSO2R12, NHSO2NHR12, NHCOR12, NHCONHR12, CONHR12, CONRi2aRi2b, hydroxy og OCF3; og R12, Ri2a og Ri2b er uafhængigt valgt fra hydrogen, C1-C6 alkyl, aryl, heteroaryl, aralkyl og heteroaralkyl, der hver især eventuelt kan være substitueret.
3. Forbindelsen ifølge krav 1, hvor R5 og Re uafhængigt er C1-C6 alkyl.
4. Forbindelsen ifølge krav 1, hvor R3 er hydrogen.
5. Forbindelsen ifølge krav 4, hvor R5 og R6 uafhængigt er C1-C6 alkyl.
6. Forbindelse ifølge krav 1 til anvendelse i fremstillingen af et medikament til forebyggelsen eller behandling af en sygdom eller bedring af tilstandved inhiberingen af PASK.
7. Forbindelse ifølge krav 1 til anvendelse i en fremgangsmåde til behandling af en sygdom omfattende administrationen af en terapeutisk effektiv mængde af denne forbindelse til en patient med behov derfor.
8. Forbindelsen til anvendelse ifølge krav 7, hvor sygdommen er valgt fra cancer og en metabolisk sygdom.
9. Forbindelsen ifølge krav 1, hvor forbindelsen er 2-(4-fluorphenyl)-3-(isopropyl(methyl)amino)quinoxalin-6-carboxylsyre.
DK10814524.4T 2009-09-03 2010-09-02 Heterocykliske forbindelser til inhibering af pask DK2473504T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23974409P 2009-09-03 2009-09-03
PCT/US2010/047736 WO2011028947A2 (en) 2009-09-03 2010-09-02 Heterocyclic compounds for the inhibition of pask

Publications (1)

Publication Number Publication Date
DK2473504T3 true DK2473504T3 (da) 2015-03-16

Family

ID=43649970

Family Applications (1)

Application Number Title Priority Date Filing Date
DK10814524.4T DK2473504T3 (da) 2009-09-03 2010-09-02 Heterocykliske forbindelser til inhibering af pask

Country Status (18)

Country Link
US (5) US8916560B2 (da)
EP (1) EP2473504B1 (da)
JP (1) JP5696856B2 (da)
KR (1) KR101650981B1 (da)
CN (1) CN102656163B (da)
AU (1) AU2010289397B2 (da)
BR (1) BR112012004533B1 (da)
CA (1) CA2772714C (da)
DK (1) DK2473504T3 (da)
EA (1) EA021275B9 (da)
ES (1) ES2534226T3 (da)
HK (1) HK1174636A1 (da)
HU (1) HUE024874T2 (da)
IL (1) IL218292A (da)
MX (1) MX2012002274A (da)
NZ (1) NZ598294A (da)
WO (1) WO2011028947A2 (da)
ZA (1) ZA201201133B (da)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140128392A1 (en) 2009-03-19 2014-05-08 Bioenergenix Heterocyclic compounds for the inhibition of pask
ES2534226T3 (es) 2009-09-03 2015-04-20 Bioenergenix Compuestos heterocíclicos para la inhibición de PASK
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
SG185515A1 (en) 2010-05-13 2012-12-28 Amgen Inc Nitrogen heterocyclic compounds useful as pde10 inhibitors
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
WO2012087872A1 (en) 2010-12-23 2012-06-28 Merck Sharp & Dohme Corp. Quinolines and aza-quinolines as crth2 receptor modulators
WO2012087861A1 (en) 2010-12-23 2012-06-28 Merck Sharp & Dohme Corp. Quinoxalines and aza-quinoxalines as crth2 receptor modulators
US9073902B2 (en) 2011-01-05 2015-07-07 Bioenergenix, Llc Substituted quinoxaline carboxylic acid compounds for the inhibition of PASK
JP6139415B2 (ja) * 2011-03-02 2017-05-31 バイオエナジェニックス Ｐａｓｋの阻害のための複素環化合物
US8916561B2 (en) 2011-03-02 2014-12-23 Bioenergenix, Llc Substituted quinoxaline compounds for the inhibition of PASK
WO2012149157A2 (en) * 2011-04-26 2012-11-01 Bioenergenix Heterocyclic compounds for the inhibition of pask
GB201118675D0 (en) 2011-10-28 2011-12-14 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
GB201118654D0 (en) * 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
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
ES2704744T3 (es) 2012-06-13 2019-03-19 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
WO2014066743A1 (en) 2012-10-25 2014-05-01 Bioenergenix Heterocyclic compounds for the inhibition of pask
WO2014066795A1 (en) 2012-10-25 2014-05-01 Bioenergenix Heterocyclic compounds for the inhibition of pask
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
CN104995182A (zh) 2013-02-07 2015-10-21 默克专利股份公司 被取代的喹喔啉衍生物及其作为mGluR4的正变构调节剂的用途
CN109776525B (zh) 2013-04-19 2022-01-21 因赛特控股公司 作为fgfr抑制剂的双环杂环
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
WO2015059088A1 (de) 2013-10-23 2015-04-30 Bayer Cropscience Ag Substituierte chinoxalin-derivate als schädlingsbekämpfungsmittel
BR112016022062B1 (pt) 2014-03-26 2023-04-11 Astex Therapeutics Limited Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico
HUE053654T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR- és CMET-inhibitorok kombinációi a rák kezelésére
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
WO2015161142A1 (en) 2014-04-18 2015-10-22 Millennium Pharmaceuticals, Inc. Quinoxaline compounds and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016118565A1 (en) 2015-01-20 2016-07-28 Millennium Pharmaceuticals, Inc. Quinazoline and quinoline compounds and uses thereof
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
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
MX2018003294A (es) 2015-09-17 2019-04-25 J Miller Marvin Compuestos heterociclicos que contienen bencilamina y composiciones utiles contra infeccion por micobacterias.
CA2996857C (en) 2015-09-23 2024-05-21 Janssen Pharmaceutica Nv Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer
HRP20220012T1 (hr) 2015-09-23 2022-04-01 Janssen Pharmaceutica Nv Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka
US11633415B2 (en) * 2017-03-31 2023-04-25 The Broad Institute, Inc. Compounds and methods useful for treating or preventing cancers
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
MX2020011639A (es) 2018-05-04 2021-02-15 Incyte Corp Sales de un inhibidor de receptores de factor de crecimiento de fibroblastos (fgfr).
BR112020022392A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation formas sólidas de um inibidor de fgfr e processos para preparação das mesmas
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
IL291901A (en) 2019-10-14 2022-06-01 Incyte Corp Bicyclyl heterocycles as fgr suppressors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN110938061A (zh) * 2019-11-27 2020-03-31 渤海大学 2-(2-苯并呋喃基)-2-喹喔啉甲酸衍生物的合成
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
KR20220131900A (ko) 2019-12-04 2022-09-29 인사이트 코포레이션 Fgfr 억제제의 유도체
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1177642B (de) * 1961-06-29 1964-09-10 Basf Ag Verfahren zur Herstellung von 2,3-Diamino-chinoxalinen
CH419399A (de) * 1962-07-18 1966-08-31 Ciba Geigy Verfahren zur Herstellung neuer Küpenfarbstoffe
HUT64023A (en) 1991-03-22 1993-11-29 Sandoz Ag Process for producing aminoguanidine derivatives and pharmaceutical compositions comprising such compounds
US6331555B1 (en) 1995-06-01 2001-12-18 University Of California Treatment of platelet derived growth factor related disorders such as cancers
US6245760B1 (en) 1997-05-28 2001-06-12 Aventis Pharmaceuticals Products, Inc Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
WO1999042461A1 (en) 1998-02-23 1999-08-26 Warner-Lambert Company Substituted quinoxaline derivatives as interleukin-8 receptor antagonists
CO5150173A1 (es) 1998-12-10 2002-04-29 Novartis Ag Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv
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
DE10013318A1 (de) 2000-03-17 2001-09-20 Merck Patent Gmbh Formulierung enthaltend Chinoxalinderivate
US6777446B2 (en) * 2000-09-05 2004-08-17 Tularik, Inc. FXR modulators
FR2816940A1 (fr) 2000-11-23 2002-05-24 Lipha Derives de 4-(biphenylcarbonylamino)-piperidine, compositions les contenant et leur utilisation
US6319679B1 (en) 2001-01-26 2001-11-20 Board Of Regents, The University Of Texas System PAS kinase
WO2004004774A2 (en) * 2002-07-03 2004-01-15 Esperion Therapeutics, Inc. Compositions comprising panthetine for the treatment of dyslipidemia
JP4607419B2 (ja) * 2002-11-14 2011-01-05 日本エンバイロケミカルズ株式会社 キノキサリン系化合物またはその塩、および、工業用殺菌組成物
AU2003287878A1 (en) * 2002-12-11 2004-06-30 7Tm Pharma A/S Quinoline compounds for use in mch receptor related disorders
US20040204450A1 (en) 2003-03-28 2004-10-14 Pfizer Inc Quinoline and quinoxaline compounds
US7189724B2 (en) 2003-04-15 2007-03-13 Valeant Research And Development Quinoxaline derivatives having antiviral activity
JP2004346016A (ja) * 2003-05-22 2004-12-09 Otsuka Chemical Co Ltd トリフルオロメチルキノキサリン化合物、その製造方法、及び有害生物防除剤
WO2005007099A2 (en) * 2003-07-10 2005-01-27 Imclone Systems Incorporated Pkb inhibitors as anti-tumor agents
US7223759B2 (en) * 2003-09-15 2007-05-29 Anadys Pharmaceuticals, Inc. Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
CA2542329A1 (en) 2003-10-16 2005-04-28 Chiron Corporation 2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines as inhibitors of raf kinase for treatment of cancer
EP1791831A4 (en) 2003-11-19 2009-07-08 Signal Pharm Llc METHOD FOR THE TREATMENT OF DISEASES AND DISORDERS BY TARGETING MULTIPLE KINASES
CA2548172A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
PL1745041T3 (pl) * 2004-04-30 2012-11-30 Genentech Inc Inhibitory chinoksalinowe szlaku sygnałowego hedgehog
JP2008527002A (ja) 2005-01-13 2008-07-24 サートリス ファーマシューティカルズ， インコーポレイテッド 神経変性障害および血液凝固障害を予防および処置するための新規組成物
CA2595486A1 (en) 2005-01-20 2006-07-27 Sirtris Pharmaceuticals, Inc. Use of sirtuin-activating compounds for treating flushing and drug induced weight gain
CA2597456A1 (en) 2005-02-14 2006-08-31 Merck & Co., Inc. Inhibitors of akt activity
WO2006138418A2 (en) 2005-06-14 2006-12-28 President And Fellows Of Harvard College Improvement of cognitive performance with sirtuin activators
KR20080049767A (ko) 2005-08-26 2008-06-04 라보라뚜와르 세로노 에스. 에이. 피라진 유도체 및 ｐｉ３ｋ 억제제로서의 용도
AU2007247385B2 (en) * 2006-05-10 2011-07-14 Novartis Ag Bicyclic derivatives as CETP inhibitors
EP2029734A4 (en) 2006-06-08 2009-11-25 Univ Utah Res Found REGULATION OF ENERGY HOMÉOSTASE BY PAS KINASE
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
JP2012517448A (ja) 2009-02-11 2012-08-02 リアクション バイオロジー コープ． 選択的キナーゼ阻害剤
AU2010219598A1 (en) 2009-03-05 2011-09-22 Astellas Pharma Inc. Quinoxaline compounds
KR101982461B1 (ko) 2009-06-12 2019-05-24 아비박스 조기 노화, 구체적으로 조로증을 치료하는데 유용한 화합물
ES2534226T3 (es) * 2009-09-03 2015-04-20 Bioenergenix Compuestos heterocíclicos para la inhibición de PASK
WO2011114148A1 (en) 2010-03-17 2011-09-22 Astrazeneca Ab 4h- [1, 2, 4] triazolo [5, 1 -b] pyrimidin-7 -one derivatives as ccr2b receptor antagonists
WO2012087861A1 (en) 2010-12-23 2012-06-28 Merck Sharp & Dohme Corp. Quinoxalines and aza-quinoxalines as crth2 receptor modulators
US9073902B2 (en) * 2011-01-05 2015-07-07 Bioenergenix, Llc Substituted quinoxaline carboxylic acid compounds for the inhibition of PASK
JP6139415B2 (ja) * 2011-03-02 2017-05-31 バイオエナジェニックス Ｐａｓｋの阻害のための複素環化合物
US8916561B2 (en) * 2011-03-02 2014-12-23 Bioenergenix, Llc Substituted quinoxaline compounds for the inhibition of PASK
WO2014143167A1 (en) 2013-03-15 2014-09-18 Koenig Mark E Method for processing material for a gasifier

Also Published As

Publication number Publication date
EA021275B9 (ru) 2015-08-31
EA201290078A1 (ru) 2012-11-30
CA2772714C (en) 2017-09-26
CA2772714A1 (en) 2011-03-10
EA021275B1 (ru) 2015-05-29
BR112012004533B1 (pt) 2021-11-09
CN102656163B (zh) 2016-01-13
WO2011028947A2 (en) 2011-03-10
JP5696856B2 (ja) 2015-04-08
US20160229815A1 (en) 2016-08-11
BR112012004533A2 (pt) 2020-06-30
US9193693B2 (en) 2015-11-24
IL218292A0 (en) 2012-04-30
JP2013503896A (ja) 2013-02-04
WO2011028947A3 (en) 2011-08-04
ES2534226T3 (es) 2015-04-20
US10781185B2 (en) 2020-09-22
EP2473504A4 (en) 2013-05-22
KR20120095356A (ko) 2012-08-28
IL218292A (en) 2014-07-31
AU2010289397B2 (en) 2016-05-26
US9868708B2 (en) 2018-01-16
HUE024874T2 (en) 2016-02-29
US20180230108A1 (en) 2018-08-16
NZ598294A (en) 2013-07-26
AU2010289397A1 (en) 2012-03-08
HK1174636A1 (zh) 2013-06-14
US8916560B2 (en) 2014-12-23
US11459307B2 (en) 2022-10-04
US20150031679A1 (en) 2015-01-29
US20120165318A1 (en) 2012-06-28
EP2473504B1 (en) 2015-02-25
KR101650981B1 (ko) 2016-08-24
US20210198216A1 (en) 2021-07-01
MX2012002274A (es) 2012-09-07
ZA201201133B (en) 2013-09-25
CN102656163A (zh) 2012-09-05
EP2473504A2 (en) 2012-07-11

Similar Documents

Publication Publication Date Title
US11459307B2 (en) Heterocyclic compounds for the inhibition of PASK
US8912188B2 (en) Substituted quinoxaline carboxylic acids for the inhibition of PASK
JP5980812B2 (ja) Ｐａｓｋの阻害のための複素環化合物
AU2012204353A1 (en) Heterocyclic compounds for the inhibition of PASK
US8916561B2 (en) Substituted quinoxaline compounds for the inhibition of PASK
US9370522B2 (en) Heterocyclic compounds for the inhibition of PASK